47 results on '"Esra Karadağ A"'
Search Results
2. Comparison of Chemical Profiles of Aronia melanocarpa Fruit Extracts
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Eda Sönmez Gürer, Ayşe Esra Karadağ, and Ayhan Altıntaş
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aronia melanocarpa ,hplc ,extract ,phenolic compound ,anthocyanin ,Agriculture ,Agriculture (General) ,S1-972 - Abstract
The chokeberry plant, which is native to North America and the south of Canada, is a deciduous, shrub-shaped, berry-like plant belonging to the Rosaceae family, which survives for many years. It is seen as a plant that adapts easily to almost every climatic condition and soil and has many beneficial properties for health. Within the scope of this study, methanol, 70% ethanol, ethanol, ethyl acetate, hexane and water extracts were prepared from the fruits collected from the Aronia melanocarpa (Michx.) Elliott plant, which is cultivated in the Kırklareli region. The chemical contents of the obtained extracts were clarified by high performance liquid chromatography. It was determined that phenolic compounds such as ferulic acid, caffeic acid, quercetin, quercetin-3-galactoside, p-coumaric acid were found in the extracts, and ethyl acetate extract was found to have the richest phenolic substance profile. Malvin anthocyanin compound was detected only in methanol extract.
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- 2023
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3. In Vitro Antiviral Evaluations of Coldmix®: An Essential Oil Blend against SARS-CoV-2
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Kemal Hüsnü Can Başer, Ayşe Esra Karadağ, Sevde Nur Biltekin, Murat Ertürk, and Fatih Demirci
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Eucalyptus ,Abies ,essential oils ,ACE2 ,coronavirus ,antiviral ,Biology (General) ,QH301-705.5 - Abstract
Coldmix® is a commercially available Eucalyptus aetheroleum and, Abies aetheroleum blend for medicinal applications. In this present study, the in vitro antiviral potential of Coldmix®, and its major constituents 1,8-cineole and α-pinene were evaluated by using the in vitro ACE2 enzyme inhibition assay as well as the direct contact test against SARS-CoV-2. The observed ACE2 enzyme inhibitory activity of Coldmix®, 1,8-cineole, and α-pinene were 72%, 88%, and 80%, respectively; whereas in the direct contact test in the vapor phase, the destruction of the virus was 79.9% within 5 min and 93.2% in the 30th min, respectively. In a similar Coldmix® vapor phase setup using the in vitro cytotoxicity cell assay, E6 VERO healthy cells were experimentally not affected by toxicity. According to the promising initial antiviral results of Coldmix® and the individually tested constituents, detailed further in vivo evaluation using different virus classes is suggested.
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- 2023
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4. Comparative In Vitro and In Silico Enzyme Inhibitory Screening of Rosa x damascena and Pelargonium graveolens Essential Oils and Geraniol
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Ayşe Esra Karadağ, Sevde Nur Biltekin, Betül Demirci, Fatih Demirci, and Usman Ghani
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angiotensin converting enzyme II ,cholinesterase ,cyclooxygenase ,lipoxygenase ,cytotoxicity ,Botany ,QK1-989 - Abstract
The present work aims to evaluate Rosa x damascena Herrm. and Pelargonium graveolens L’Hér. essential oils, and the major constituent geraniol for their in vitro and in silico inhibitory activities against 5-lipoxygenase (5-LOX), cyclooxygenase (COX), acetyl cholinesterase (AChE), butyryl cholinesterase (BuChE), and angiotensin converting enzyme (ACE2) enzymes. Geraniol most potently inhibited the ACE2 relative to other enzymes. R. damascena essential oil moderately inhibited the cancer cell lines with no toxic effects on healthy HEK 293 cells. P. graveolens essential oil inhibited a number of cancer cell lines including A549, MCF7, PC3, and HEK 293 that are reported here for the first time. The molecular docking of geraniol with the target enzymes revealed that it binds to the active sites similar to that of known drugs. Geraniol carries the potential for further drug development due to its drug-like binding mode for the target enzymes. Our work confirms that these essential oils possess similar biological activities due to their similar phytochemistry in terms of the major constituents of the plants. The promising biological activities reported in this work further warrant the inclusion of in vivo studies to establish safe use of the target essential oils and their constituents.
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- 2023
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5. In Vitro Anti-Inflammatory and Anticancer Evaluation of Mentha spicata L. and Matricaria chamomilla L. Essential Oils
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Sevde Nur Biltekin, Ayşe Esra Karadağ, Fatih Demirci, and Betül Demirci
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General Chemical Engineering ,General Chemistry - Published
- 2023
6. YABANMERSİNİ (VACCİNİUM MYRTİLLUS L.) MEYVE ÖZÜ'NÜN MİDE KANSERİ, AGS HÜCRE HATTI ÜZERİNDE ANTİOKSİDAN AKTİVİTESİ VE ANTİ-KANSER ETKİLERİ
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Nihal KARAKAŞ, Mehmet Evren OKUR, Tuğba SAĞIR, Damla ULUDAĞ, Derya Çiçek POLAT, and Ayşe Esra KARADAĞ
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Pharmacology ,Pharmaceutical Science - Abstract
Objective: Vaccinium myrtillus L. fruits are consumed as food. This research was aimed to evaluate V. myrtillus methanol extract antioxidant and cytotoxic activities and determine its anti-cancer potential to further study against gastric cancer. Material and Method: V. myrtillus fruit (Bilberry) methanol extract was examined for its antioxidant activities by ABTS•+ and DPPH• assays. The phytochemical analysis of the extract was studied by HPLC method. The cytotoxic effect of V. myrtillus fruit methanol extract on gastric cancer cell line AGS was measured by Cell Titer-Glo assay. Additionally, as healthy control, fibroblast like human mesenchymal stem cell line was used for testing anti-cancer efficacy. Result and Discussion: V. myrtillus fruit methanol extract showed 0.1413 and 0.0439 mg/mL IC50 values as antioxidant activity by ABTS•+ and DPPH• assays, respectively. Malvidin-3-O-Glucoside was detected as an anthocyanin compound by HPLC method. Cytotoxicity analysis showed that among different concentrations (0.5-10 mg/ml), the most significantly, 2 mg/ml of Bilberry extract treatment decreased the viability of AGS gastric cancer cells while sparing healthy MSC cells. This data suggests the further analysis of Bilberry extract on several cancer cell lines as well as the determination of a potential active substance in the extract.
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- 2022
7. CYTOTOXIC EFFECTS OF ARCTIUM MINUS METHANOL EXTRACT ON VARIOUS CANCER CELL LINES
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Ayşe Arzu ŞAKUL, Yasemin YOZGAT BYRNE, Ayşe Esra KARADAĞ, Ebrar ALTINALAN, Şeyma ÇİMEN, and Mehmet Evren OKUR
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Arctium minus ssp. minus ,cancer ,cell death ,cell viability ,cytotoxicity ,Pharmacology ,Farmakoloji ve Eczacılık ,Pharmaceutical Science ,hücre canlılığı ,hücre ölümü ,kanser ,sitotoksisite ,Pharmacology and Pharmacy - Abstract
Objective: This study aimed to evaluate the cytotoxic effects of Arctium minus (Hill) Bernh. ssp. minus methanol extract derived from aerial parts on cancer cell lines.Material and Method: For cytotoxicity assays, two different human breast cancer cell lines (MCF-7 and MDA-MB-231) and healthy human fibroblast cell line (MRC-5)as a control were used. Cell viability determination was performed using the CellTiter-Blue method. One-Way ANOVA and Tukey post test were used for statistical analysis.Result and Discussion: Cell viability has been detected between ratios of 27.8-38.7% for MCF-7 cancer cell line, and a significant cytotoxic activity was observed via the analysis (1 mg/mL extract treatment p< 0.022). However, 47.8-59.7% cell viability was observed for MDA-MB-231 cancer cell line, and MRC-5 healthy fibroblast cell line did not demonstrate any cell viability (92.4-105.4% cell viability). Depending on these data, MCF-7 cancer cell line and MRC-5 fibroblast healthy cell line were treated with Arcitum minus extract, then cell viability was detected by flow cytometry technique. The ratio of the cell death was higher in MCF-7 cancer cell line (98%) compared with the MRC-5 fibroblast healthy cell line (25%) after the Arctium minus extract treatment. In conclusion, Arctium minus ssp. minus extract has significantly decreased the cell viability in MCF-7 cancer cell line when compared with the MCR-5 fibroblast normal cell line., Amaç: Bu çalışmada Arctium minus (Hill) Bernh. ssp. minus’un toprak üstü kısımlarından elde edilen metanol ekstresinin kanser hücre hatları üzerindeki sitotoksik etkilerinin değerlendirilmesi amaçlanmıştır.Gereç ve Yöntem: Arctium minus (Hill) Bernh. ssp. minus’un metanol ekstresinin, iki farklı insan meme kanseri hücre hattına (MCF-7 ve MDA-MB-231) ve kontrol olarak normal insan fibroblast hücre hattına (MRC-5) uygulanması ile in vitro sitotoksik etkileri araştırılmıştır. Hücre canlılık tayini CellTiter-Blue metodu kullanılarak gerçekleştirilmiştir. İstatistiksel analiz için One-Way ANOVA ve Tukey post-hoc testi kullanılmıştır.Sonuç ve Tartışma: Analizlerde, MCF-7 kanser hücrelerinde hücre canlılığı %27,8 -38,7 oranında belirlenmiş olup önemli derecede sitotoksik aktivite tespit edilmiştir (1 mg/mL ekstre uygulaması için p
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- 2022
8. Herbal Preparations Used Against Fatty Liver Disease: Systematic Review
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Ayşe Esra KARADAĞ and Fatih DEMİRCİ
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- 2022
9. Development, characterization of naringenin-loaded promising microemulsion formulations, and demonstration of anti-aging efficacy by in vitro enzyme activity and gene expression
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Dilara Şahin, Emre Şefik Çağlar, Tuğçe Boran, Ayşe Esra Karadağ, Gül Özhan, and Neslihan Üstündağ Okur
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Naringenin ,Cell Culture ,Gene Expressions ,Pharmaceutical Science ,Anti-Elastase ,Antiaging ,Microemulsion - Abstract
This study aims to produce microemulsion formulations containing naringenin for anti-aging reasons. For this purpose, formulations of topical microemulsions including different cosurfactants and surfactants were developed, and a triangle phase diagram was utilized to determine the optimal microemulsion system. On the developed microemulsion formulations, characterization studies were performed. Ex vivo permeation-penetrating and in vitro release experiments were conducted. Anti-elastase, anti-collagenase, anti-tyrosinase, and antioxidant properties of the formulations were also evaluated. Experiments were conducted on cytotoxicity, cellular ROS, gene expression levels of oxidative stress-related genes, and cell culture. Droplet size, polydispersity index, zeta potential, pH, viscosity, turbidity of naringenin loaded formulations were found between 0.9147 ± 0.0316 and 1.938 ± 0.085 nm, 0.373 ± 0.025 and 0.410 ± 0.019, −0.0517 ± 0.0138 and −0.0990 ± 0.0110 mV, 5.110 ± 0.006 and 5.530 ± 0.006, 163.33 ± 5.77 and 450.00 ± 0.00 cP, 5.723 ± 0.068 and 9.323 ± 0.264 NTU, respectively. At the end of 24 h, the in vitro release research shows that more than 50% of naringenin has been released. Elastase and collagenase enzyme inhibitions of naringenin loaded formulations were found between 31.98 ± 0.15 and 41.74 ± 0.09%, 39.99 ± 0.19 and 47.78 ± 0.04%, respectively. Furthermore, NRF-2 and HO-1 gene expression levels did not show a significant change in the cells exposed to only naringenin loaded formulations. To conclude, developed microemulsions seem to be promising formulations that can be used for anti-aging purposes. University of Health Sciences Lahore
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- 2023
10. Bioautography for evaluation of several Lavandula L. and origanum species antimicrobial and antioxidant activity
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Şule Nur KaravuŞ, Ayşegül ÇaŞkurlu, Ayşe Esra KaradaĞ, and Fatih Demİrcİ
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Lavandula ,Bioautography ,Origanum ,General Medicine ,Antioxidant ,Essential Oil - Abstract
In the search of bioactive natural compounds, bioautography of plant extracts were associated in an antioxidant screening. Due to containing variety of phenolic compounds Lavandula and Origanum species are important medicinal plants. The antioxidant and free radical scavenging activities of Lavandula angustifolia, L. stoechas, L. heterophylla, Origanum majorana, O. onites, O. vulgare, O. minituflorum, and their main phenolic compounds linalool and carvacrol was carried out by TLC-bioautography method based on the DPPH· andABTS·+ assays to compare essential oils and known main active constituents. The antimicrobial activity of the materials was tested using the in vitro broth microdilution assay towards two different microorganisms. Methicillin-resistant Staphylococcus aureus and Streptococcus mutans were used for the study. As a result of our studies, it is determined that O. vulgare showed the highest activity against S. mutans and O. onites and O. vulgare showed the highest activity against MRSA. compared to the tested antibiotic.
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- 2023
11. Chemical characterization and multidirectional biological effects of different solvent extracts of arum elongatum: in vitro and in silico approaches
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Mohamad Fawzi Mahomoodally, Gokhan Zengin, Seebaluck‐Sandoram Roumita, Giovanni Caprioli, Ahmed M. Mustafa, Diletta Piatti, Evren Yıldıztugay, Gunes Ak, Ayşe Esra Karadağ, Asaad Khalid, Ashraf N. Abdalla, Abdullahi Ibrahim Uba, and Fatih Demirci
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Arum ,Molecular Medicine ,Bioactive Agent ,Natural Enzyme Inhibitors ,Bioengineering ,Phenolic Composition ,General Chemistry ,General Medicine ,Molecular Biology ,Biochemistry - Abstract
Arum elongatum (Araceae) is widely used traditionally for the treatment of abdominal pain, arterial hypertension, diabetes mellitus, rheumatism and hemorrhoids. This study investigated the antioxidant properties, individual phenolic compounds, total phenolic and total flavonoid contents (HPLC/MS analysis), reducing power and metal chelating effects of four extracts obtained from A. elongatum (ethyl acetate (EA), methanol (MeOH), methanol/water (MeOH/water) and infusion). The inhibitory activity of the extracts were also determined against acetylcholinesterase, butyrylcholinesterase, tyrosinase, amylase and glucosidase enzymes. The MeOH/water extracts contained the highest amount of phenolic contents (28.85 mg GAE/g) while the highest total flavonoid content was obtained with MeOH extract (36.77 mg RE/g). MeOH/water demonstrated highest antioxidant activity against DPPH center dot radical at 38.90 mg Trolox equivalent per gram. The infusion extract was the most active against ABTS(+center dot) (133.08 mg TE/g). MeOH/water extract showed the highest reducing abilities with the CUPRAC value of 102.22 mg TE/g and the FRAP value of 68.50 mg TE/g. A strong metal chelating effect was observed with MeOH/water extract (35.72 mg EDTAE/g). The PBD values of the extracts ranged from 1.01 to 2.17 mmol TE/g. EA extract displayed the highest inhibitory activity against AChE (2.32 mg GALAE/g), BChE (3.80 mg GALAE/g), alpha-amylase (0.56 mmol ACAE/g) and alpha-glucosidase (9.16 mmol ACAE/g) enzymes. Infusion extract was the most active against tyrosinase enzyme with a value of 83.33 mg KAE/g. A total of 28 compounds were identified from the different extracts. The compounds present in the highest concentration were chlorogenic acids, 4-hydroxybenzoic acid, caffeic acid, p-coumaric acid, ferulic acid, isoquercitrin, delphindin 3,5-diglucoside, kaempferol-3-glucoside and hyperoside. The biological activities of A. elongatum extracts could be due to the presence of compounds such as gallic acid, chlorogenic acids, ellagic acid, epicatechin, catechin, kaempferol, 4-hydroxybenzoic acid, caffeic acid, p-coumaric acid, ferulic acid, quercetin, isoquercitrin, and hyperoside. Extracts of A. elongatum showed promising biological activities which warrants further investigations in an endeavor to develop biopharmaceuticals.
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- 2023
12. In Vivo Wound Healing and In Vitro Anti-Inflammatory Activity Evaluation of Phlomis russeliana Extract Gel Formulations
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Mehmet Evren Okur, Ayşe Esra Karadağ, Neslihan Üstündağ Okur, Yağmur Özhan, Hande Sipahi, Şule Ayla, Benay Daylan, Betül Demirci, and Fatih Demirci
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P. russeliana ,bioactivity-guided fractionation ,wound healing ,anti-inflammatory ,phytochemical analyses ,mice ,Organic chemistry ,QD241-441 - Abstract
The air-dried aerial parts of Phlomis russeliana (Sims) Lag. Ex Benth. was extracted by methanol and fractionated by n-hexane, dichloromethane, and ethyl acetate, respectively. The wound healing properties of P. russeliana extract gel was evaluated using the in vivo excisional wound model using Balb-c mice. Initially, the P. russeliana methanol extract showed LOX inhibitory activity at IC50 = 23.2 µg/mL, whereas the DPPH• assay showed IC50 = 0.89 mg/mL, and the ABTS• assay showed IC50 = 0.99 mg/mL, respectively. In addition, a remarkable anti-inflammatory activity was observed in the cell culture assay. Thereafter, activity-guided fractionation was performed by LOX enzyme inhibition assays, and the structures of the two most active fractions were revealed by both GC–FID and GC/MS analyses, simultaneously. Phytol and 1-heptadecanoic acid were characterized as the active constituents. Moreover, the P. russeliana extract gel formulation was applied for in vivo tests, where the new gel formulation supported the in vitro anti-inflammatory activity findings. As a conclusion, this experimental results support the wound healing evidence based on the ethnobotanical application of Phlomis species with further potential.
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- 2020
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13. <scp> Rosmarinus officinalis </scp> L. essential oil encapsulated in new microemulsion formulations for enhanced antimicrobial activity
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Ayşe Esra Karadağ, Fatih Demirci, Betül Demirci, and Neslihan Üstündağ Okur
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Antifungal ,biology ,Chemistry ,medicine.drug_class ,General Chemical Engineering ,Rosmarinus Officinalis L ,Antimicrobial ,biology.organism_classification ,Microemulsion ,Rosmarinus ,Essential Oil ,Surfaces, Coatings and Films ,law.invention ,Pulmonary surfactant ,law ,Surfactant ,Officinalis ,medicine ,Food science ,Physical and Theoretical Chemistry ,Essential oil - Abstract
In this present study, Rosmarinus officinalis essential oil and its new microemulsions (MEs) were evaluated both for the in vitro antibacterial and antifungal activity. The essential oil composition was verified initially both by GC-FID and GC/MS, where camphor (19.5%), 1,8-cineol (12%), and verbenone (11.1%) were characterized as the main constituents. A titration method was used and utilized to formulate the MEs. The preparation was formulated using isopropyl myristate as an oil phase, where sorbitan monolaurate and macrogol-glycerol ricinoleate were used as surfactants. In the same system, ethanol was utilized as co-surfactant and distilled water as aqueous phase. A total of 0.1% (w/w) of R. officinalis essential oil was dissolved within the formulation, and evaluated for characteristic parameters such as viscosity, pH, electrical conductivity, refractive index, polydispersity index (PDI), droplet size, and zeta potential, respectively. The pH value was 6.2, where the average microemulsion droplet size was 4.58 +/- 0.137 nm; the PDI value was found as 0.219 +/- 0.016. The viscosity of the microemulsion was determined as 6.93 +/- 0.015 cP. The conductivity of MEs was found as 10 mu S/cm; finally, the zeta potential was determined as 0.391 +/- 0.012 mV. The antimicrobial potential of the preparations was compared using the in vitro broth microdilution, and poisoned PDA assay. A significant increase in the anti-Candidal activity of the micro-emulsified essential oil (15.6 mu g/ml) was observed, however, the antibacterial susceptibility was rather low at the tested concentrations. In addition, the novel microemulsion preparation significantly inhibited mycelial growth of the plant pathogens used in the study, suggesting its selective antifungal potential.
- Published
- 2021
14. Binary Synergistic Combinations of Lavender and Fennel Essential Oils with Amoxicillin
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Ayşe Esra Karadağ, Ayşegül Çaşkurlu, Betül Demirci, and Fatih Demirci
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Pharmacology ,Complementary and alternative medicine ,Organic Chemistry ,Drug Discovery ,Pharmaceutical Science ,Molecular Medicine ,Analytical Chemistry - Abstract
Microbial resistance is an important problem in modern healthcare systems. In addition to drug resistance, the side effects of current antibiotic applications are also known issues. In this present study, binary combinations of amoxicillin with European Pharmacopoeia quality lavender (Lavandula angustifolia) and fennel (Foeniculum vulgare) essential oils were evaluated against human pathogenic microbial strains. The checkerboard method was used to quantify the efficacy of the essential oils in combination with amoxicillin. As an initial result, remarkable in vitro antimicrobial activity was observed at relatively low amoxicillin concentrations using different oil combinations against Staphylococcus aureus ATCC 6538, Enterococcus faecalis ATCC 29212, Bacillus cereus ATCC 14579, Escherichia coli NRRL B-3008, Salmonella typhi (clinical isolate), respectively. Fractional inhibitory concentrations were calculated and interpreted in terms of addition, synergy, antagonism, or indifferent. A synergistic interaction with the combination F. vulgare essential oil and amoxicillin (fractional inhibitory concentration index = 8.05 × 10−4) was observed against the pathogens E. faecalis and Escherichia coli. Both essential oils together and in combination with amoxicillin showed a synergistic effect with possible future applications.
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- 2022
15. Hemostatic Activity of Cistus creticus Extract in Wistar Albino Rats
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Fatma Tosun, Etil Guzelmeric, Fatih Demirci, Erdem Yesilada, Neslihan Üstündağ Okur, Ayşegül Çaşkurlu, Mehmet Evren Okur, and Ayşe Esra Karadağ
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Hemostatic Agent ,biology ,Traditional medicine ,010405 organic chemistry ,Tail Bleeding ,Hyperoside ,Cistaceae ,biology.organism_classification ,01 natural sciences ,Blood Stopper ,Coagulating Activity ,0104 chemical sciences ,HPTLC ,010404 medicinal & biomolecular chemistry ,Cistus creticus ,chemistry.chemical_compound ,chemistry ,In vivo ,Flavonoid Glycoside ,Topical Application ,General Pharmacology, Toxicology and Pharmaceutics - Abstract
Aerial part preparations of Cistus creticus L., Cistaceae, are traditionally used in Anatolia as a hemostatic agent. The air-dried aerial parts were extracted with methanol. Gels were prepared, followed by the hemostatic activity evaluation using Wistar albino rats in vivo tail tip amputation model. The chemical characterization of the total extract was performed by high-performance thin-layer chromatography. The methanol extract was loaded to a hydrogel base to complete a concentration of 2.5 and 7.5%. As a result, the 2.5% extract gel was found more effective on both bleeding time and amount. Hyperoside and tiliroside, which may be the components responsible for the hemostatic properties of the analyzed plant material, were dereplicated as major constituents.
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- 2020
16. In Vitro and In Silico Evaluation of ACE2 and LOX Inhibitory Activity of Origanum Essential Oils and Carvacrol
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Fatih Demirci, Kerem Teralı, Ayşe Esra Karadağ, Sevde Nur Biltekin, Ezgi Ak Sakallı, Betül Demirci, Müberra Koşar, and K. Hüsnü Can Başer
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Pharmacology ,Complementary and alternative medicine ,Organic Chemistry ,Drug Discovery ,Pharmaceutical Science ,Molecular Medicine ,Analytical Chemistry - Abstract
Origanum spp. are used both for culinary purposes and for their biological activities. In this study, commercial Origanum majorana, Origanum minutiflorum, Origanum vulgare, and Origanum onites essential oils and their prominent constituent carvacrol were evaluated for their in vitro and in silico angiotensin-converting enzyme 2 and lipoxygenase enzyme inhibitory potentials. The essential oils were analysed by gas chromatography-flame ionisation detection and gas chromatography-mass spectrometry, where carvacrol was identified as the major component (62 – 81%), confirming the quality. In vitro enzyme inhibition assays were conducted both with the essential oils (20 µg/mL) and with carvacrol (5 µg/mL). The comparative values of angiotensin-converting enzyme 2 percent inhibition for O. majorana, O. minutiflorum, O. vulgare, and O. onites essential oils were determined as 85.5, 79.1, 74.3, and 42.8%, respectively. As a result of the enzyme assays, carvacrol showed 90.7% in vitro angiotensin-converting enzyme 2 inhibitory activity. The in vitro lipoxygenase inhibition of the essential oils (in the same order) was 89.4, 78.9, 81.1, and 73.5%, respectively, where carvacrol showed 74.8% inhibition. In addition, protein–ligand docking and interaction profiling was used to gain structural and mechanistic insights into the angiotensin-converting enzyme 2 and lipoxygenase inhibitory potentials of major Origanum essential oil constituents. The in silico findings agreed with the significant enzyme inhibition activity observed in vitro. Further in vivo studies are suggested to confirm the safety and efficacy of the oils.
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- 2022
17. Chemical Characterization and Multidirectional Biological Effects of Different Solvent Extracts of Arum elongatum: in Vitro and in Silico Approaches.
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Fawzi Mahomoodally, Mohamad, Zengin, Gokhan, Roumita, Seebaluck‐Sandoram, Caprioli, Giovanni, Mustafa, Ahmed M., Piatti, Diletta, Yıldıztugay, Evren, Ak, Gunes, Esra Karadağ, Ayşe, Khalid, Asaad, Abdalla, Ashraf N., Ibrahim Uba, Abdullahi, and Demirci, Fatih
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- 2023
- Full Text
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18. In Vitro Anti-Helicobacter Pylori and Antimycobacterial Activity Evaluation Of Selected Plants From Turkey
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Ayşe Esra Karadağ, Fatma Tosun, and Ayşegül Çaşkurlu
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Lathyrus ,Fen ,biology ,Traditional medicine ,medicine.drug_class ,Ulmus ,Science ,Mikobakter ,General Medicine ,Glaucium ,Helicobacter pylori ,biology.organism_classification ,Antimycobacterial ,Echium,Glacium,Helicobacter pylori ,Helicobacter Pylori ,In vitro ,Mycobacterium ,Helikobakter Pilori ,Echium ,medicine - Abstract
In this study, the extracts of Ulmus minor Mill. subsp. minor (Ulmaceae), Lathyrus pratensis L. (Leguminosae), Glaucium leiocarpum Bois. (Papaveraceae), and Echium vulgare L. (Boraginacea) were investigated for their in vitro anti-Helicobacter pylori and antimycobacterial activity. The air-dried plant material was powdered and extracted with 70% ethanol by maceration. The extract was filtered and evaporated to dryness under the vacuum and then dissolved in a waterethanol (90:10) mixture and extracted with dichloromethane and ethyl acetate, respectively. Antibacterial activity was investigated by microdilution method against Helicobacter pylori ATCC 43504, Mycolicibacterium smegmatis ATCC 14468 and Mycobacterium avium ATCC 25291. The ethyl acetate extract of U. minor showed activity with MIC of 250 µg / mL against H. pylori. The other extracts showed no or weak inhibitory activity at >2000 µg/mL concentrations against the tested microorganisms. In conclusion, ethyl acetate extract of U. minor may be used for the treatment of H. pylori infections. Bu çalışmada, Ulmus minor Mill. subsp. minor (Ulmaceae), Lathyrus pratensis L. (Leguminosae), Glaucium leiocarpum Bois. (Papaveraceae) ve Echium vulgare L. (Boraginacea) ekstrelerinin antihelikobakter pilori ve antimikobakter aktiviteleri in vitro olarak incelenmiştir. Kurutulmuş bitki materyalleri toz edildikten sonra %70’lik etanolle masere edilmiştir. Ekstreler süzülerek vakum altında yoğunlaştırıldıktan sonra su-etanol (90:10) karışımında çözülerek sırasıyla diklorometan ve etilasetat ile alt ekstreleri hazırlanmıştır. Antibakteriyel aktivitesi in vitro broth mikrodilüsyon yöntemi ile Helicobacter pylori ATCC 43504, Mycolicibacterium smegmatis ATCC 14468 ve Mycobacterium avium ATCC 25291’a karşı araştırılmıştır. U. minor’un etilasetat ekstresinin MİK değeri H. pilori’ye karşı 250 µg/mL olarak kaydedilmiştir. Test edilen konsantrasyonlarda (2000 µg/mL) diğer ekstreler belirgin bir MİK değeri göstermemiştir. Sonuç olarak U. minor yapraklarının etilasetat ekstresinin H. pilori enfeksiyonlarında tedavi edici olarak kullanılabileceği düşünülmektedir.
- Published
- 2020
19. Opuntia ficus indica Fruits Ameliorate Cisplatin-Induced Nephrotoxicity in Mice
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Derya Çiçek Polat, İsmail Seçkin, Sibel Demirci, Mehmet Evren Okur, Ayşe Esra Karadağ, and Şule Ayla
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0301 basic medicine ,Pharmacology ,Creatinine ,Antioxidant ,ABTS ,Chemistry ,DPPH ,medicine.medical_treatment ,Pharmaceutical Science ,General Medicine ,Nephrotoxicity ,03 medical and health sciences ,chemistry.chemical_compound ,030104 developmental biology ,0302 clinical medicine ,030220 oncology & carcinogenesis ,medicine ,Myricetin ,Quercetin ,Blood urea nitrogen - Abstract
This study aims to determine the potential renal protective effects of Opuntia ficus-indica (L.) Miller (OFI) fruits against cisplatin-induced nephrotoxicity in mice. The antioxidant activity of OFI methanol extract was calculated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis-3-ethylbenzthiazoline-6-sulfonic acid (ABTS) free radical scavenging assays. Furthermore, the LC-mass spectroscopy (MS) analysis of the OFI fruit extract was carried out. Mice were treated with OFI extract (250 mg/kg) for 10 d and injected with a single dose of cisplatin (20 mg/kg) on the 7th day. The blood samples were collected to measure blood urea nitrogen (BUN) and serum creatinine level on the 10th day. Their kidneys were removed for histopathological examination. The renal morphological alterations were assessed through the mesangial matrix index and transmission electron microscopy (TEM). The OFI fruit extract showed significant in vitro antioxidant activity. In further, it was revealed that the cisplatin-induced nephrotoxicity in mice was ameliorated; this outcome was supported by both histological examination results and the depicted reduced levels of BUN and serum creatinine. The potent antioxidant compounds which were detected in the extract of OFI fruits such as myricetin, quercetin, luteolin might be responsible for the observed renoprotective effect. The results clarified that the OFI fruit extract could ameliorate cisplatin-induced renal toxicity in mice via including antioxidant and renoprotective compounds.
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- 2020
20. A novel approach in the treatment of osteoarthritis: In vitro and in vivo evaluation of Allium sativum microemulsion
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Mehmet Evren Okur, Bircan Kolbaşı, Mustafa Şahin, Ayşe Esra Karadağ, Rengin Reis, Emre Şefik Çağlar, Arife Ahsen Kaplan, Hande Sipahi, İlknur Keskin, Bahtiyar Demiralp, and Neslihan Üstündağ Okur
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General Chemical Engineering ,Allium Sativum ,Cell Culture ,Osteoarthritis ,Surfactant ,Physical and Theoretical Chemistry ,Microemulsion ,Surfaces, Coatings and Films ,Rats - Abstract
Osteoarthritis (OA) is the most prevalent kind of joint disease, affecting millions of individuals worldwide. Allium sativum L. was used as a therapeutic agent in the microemulsion system against osteoarthritis due to allicin's high antioxidant and anti-inflammatory effects. HPLC was used to evaluate the chemical components of the Allium sativum methanol extract. Water-in-oil (w/o) type of microemulsions loaded with Allium sativum extract was produced. To create the microemulsions, a titration approach was employed. The microemulsions were prepared using isopropyl myristate (IPM) as oil, Polysorbate 60, Sorbitan monolaurate 80 as surfactants, and Polyethylene glycol 400, ethanol as cosurfactants. The pH, droplet size, viscosity, polydispersity index values were measured to characterize of microemulsions. In addition, L929 healthy mouse fibroblasts and CHON-001 healthy human cartilage fibroblast cells were tested for cytocompatibility in vitro. The therapeutic potential of Allium sativum microemulsion was investigated in rats that had osteoarthritis surgically simulated. HPLC analysis revealed a significant concentration of allicin in the extract. The titration approach was used to create an A. sativum microemulsion (AS) with a narrow droplet size and PDI range. In L929 and CHON-001 cells, cytocompatibility experiments revealed that the maximum dosages of AS microemulsion 5% (v/v) exerted 93.41 +/- 3.11% and 75.59 +/- 2.69% cell viabilities, respectively. Different concentrations of AS (1.25%, 2.5%, and 5% v/v) demonstrated cytoprotective efficacy against H2O2-induced oxidative damage. When compared to the control group, in vivo investigations revealed fewer irregularities on the articular surface and typically arranged chondrocytes in the positive control and treated groups. Health Sciences University Scientific Research Projects Coordination Unit
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- 2022
21. PHLOMIS PUNGENS’İN FİTOKİMYA VE İN VİTRO FARMAKOLOJİK ETKİLERİNİN DEĞERLENDİRİLMESİ
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Fatih Demirci, Rengin Reis, Ayşe Esra Karadağ, Rana Arslan, Betül Demirci, Mehmet Evren Okur, and Hande Sipahi
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Inflammation ,Pharmacology ,Lamiaceae ,Hücre Kültürü ,biology ,Traditional medicine ,Farmakoloji ve Eczacılık ,Macrophage ,Cell Culture ,Cell culture,fibroblast,inflammation,Lamiaceae,macrophage ,Pharmaceutical Science ,biology.organism_classification ,In vitro ,Enflamasyon,fibroblast,hücre kültürü,Lamiaceae,makrofaj ,Phlomis ,Phytochemical ,Enflamasyon ,Fibroblast ,Pharmacology and Pharmacy ,Makrofaj - Abstract
Amaç: Bu çalışmada, Phlomis pungens Willd. topraküstü kısımlarından elde edilen ekstrelerin in vitro yara iyileşmesi, antiinflamatuar, antimikrobiyal ve antioksidan aktivitesinin araştırılması amaçlanmıştır. Gereç ve Yöntem: Biyoaktif hekzan ekstresinin uçucu bileşenlerini belirlemek için fitokimyasal analiz GC-MS kullanılarak yapılmıştır. P. pungens ekstresinin yara iyileştirme aktivitesi, in vitro antimikrobiyal, antioksidan, antiinflamatuar etkinlikleri değerlendirilmiş ve ek olarak ekstrenin in vitro sitotoksisitesi de değerlendirilmiştir. Sonuç ve Tartışma: P. pungens metanol ekstresi, 78,2 µg/mL'de (IC50) 5-LOX inhibe edici aktivite gösterirken, DPPH yöntemi ile antioksidan aktivitesi IC50=2.41mg/mL ve ABTS IC50=3.32 mg/mL olarak bulunmuştur. Ekstre, doza bağlı olarak anti-inflamatuar aktivite gösterirken, L-NAME ve P. pungens metanol ekstresi, LPS ile uyarılan PGE2 üretimini önemli ölçüde azaltmıştır. Strach metodu sonuçlarına göre doza bağlı etki ile hücre göç hızında bir artış gözlemlenmiştir. Bulgularımız, starch testine göre P. pungens metanol ekstresinin yara iyileşmesinde rol oynayabileceğini ve antioksidan ve antiinflamatuar aktivitesinin de katkıda bulunduğu düşündürmüştür. İn vivo koşullar altında in vitro aktiviteyi doğrulamak için başka değerlendirmeler devam etmektedir., Objective: This study aimed to investigate the in vitro wound healing, anti-inflammatory, antimicrobial and antioxidant activity of Phlomis pungens Willd. extract derived from the aerial parts. Material and Method: The phytochemical analysis was performed using GC-MS in order to identify the volatile components of the bioactive Hex extract. The wound healing activity of P. pungens extract was evaluated based on in vitro antimicrobial, antioxidant, anti-inflammatory, and, scratch activity was studied. In addition, the in vitro cytotoxicity of the extract was also evaluated. Result and Discussion: P. pungens methanol extract depicted a 5-LOX inhibitory activity at 78.2µg/mL (IC50), while the antioxidant activity by DPPH radical provided an IC50=2.41mg/mL, and the ABTS radical showed IC50=3.32mg/mL, respectively. The extract showed dose-dependently anti-inflammatory activity while L-NAME and P. pungens methanol extract significantly decreased LPS stimulated PGE2 production. According to the scratch assay results, all treatments led to an increase in cell migration rate with a dose-dependent effect. Our findings suggested that P. pungens methanol extract may have a role in wound healing according to the scratch test, and it is thought that its antioxidant and anti-inflammatory activity also contributed. Further evaluations are ongoing to confirm the in vitro activity under in vivo conditions.
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- 2021
22. Phytochemical Compounds Loaded to Nanocarriers as Potential Therapeutic Substances for Alzheimer's Disease-Could They be Effective?
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Panoraia I. Siafaka, Neslihan Üstündağ Okur, Derya Çiçek Polat, Ayşe Esra Karadağ, Rabia Edibe Parlar Köprülü, Ioannis D. Karantas, Gökçe Mutlu, Emre Şefik Çağlar, and Mehmet Evren Okur
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Pharmacology ,Alzheimer Disease ,Drug Discovery ,Phytochemicals ,Anti-Inflammatory Agents ,Brain ,Humans ,Antioxidants ,Aged - Abstract
Abstract: Alzheimer’s disease accounts for a high percentage of dementia cases in elderly individuals. This type of brain disease is caused by damage to the brain cells affecting the ability of the patients to communicate, as well as their thinking, behavior, and feelings. Although numerous research laboratories focus on advancements in treating Alzheimer’s disease, the currently approved pharmacological approaches seem to only alleviate the symptoms. Consequently, there is an urgent need for alternative pharmacological options that can prevent the progressive impairment of neurons. Natural substances were used in ancient times to treat various disorders given their biological activities such as antioxidant, anti-inflammatory, and antiapoptotic properties. Besides, their cost-effectiveness and accessibility to anyone who needs them are their most significant characteristics. Therefore, the possible use of phytochemical compounds for the possible management or even prevention of Alzheimer’s disease is currently under investigation. This review article summarizes the present status of Alzheimer’s disease diagnosis and underlying mechanisms, the potential phytochemicals and their carriers, along with future perspectives. In the future, natural substances can play a role as an adjunct therapy for neurodegenerative forms of dementia, such as Alzheimer’s disease.
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- 2021
23. In vitro ACE2 and 5-LOX inhibition of rosmarinus officinalis l. essential oil and its major component 1,8-cineole
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Ayşe Esra Karadağ, Sevde Nur Biltekin, Fatih Demirci, and Betül Demirci
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Pharmacology ,biology ,Chemistry ,Component (thermodynamics) ,Organic Chemistry ,1,8-Cineole ,ACE2 ,Plant Science ,biology.organism_classification ,Rosmarinus Officinalis L ,Rosmarinus ,In vitro ,law.invention ,Essential Oil ,law ,Drug Discovery ,Officinalis ,Food science ,5-LOX ,Essential oil - Abstract
In this present study, Rosmarinus officinalis L. essential oil, and its major component 1,8-cineole was evaluated in vitro for angiotensin converting enzyme 2 (ACE2), as well as for 5-lipoxygenase (5-LOX) enzyme inhibitory activity. The essential oil composition was confirmed both by GC-FID and GC/MS, where 1,8-cineole (62.7%), alpha-pinene (12.6 %), and camphor (8.3 %) were identified as the main constituents. Activity studies were performed at concentrations of 20 mu g/mL for essential oil, and 5 mu g/mL for the major compound 1,8-cineole, which were compared experimentally with standards. The essential oil was evaluated using a fluorometric multiplate based enzyme inhibition kit, where the ACE2 inhibition of Rosmarinus aetheroleum was 20%, while the 5-LOX inhibition was observed as 81.1%, respectively. In addition, the major constituent 1,8-cineole also showed remarkable ACE2 inhibition with 89.2%, and 5-LOX inhibition with 37.2%, respectively. As a result, the cineole chemotype rosemary essential oil, and its major constituent 1,8-cineol may have antiviral potential applications against coronaviruses due to ACE2 enzyme inhibition with anti-inflammatory effects. Further in vivo studies are needed to confirm the efficacy of essential oils and their constituents. Anadolu University
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- 2021
24. Chemical characterization of Glaucosciadium cordifolium (Boiss.) B. L. Burtt & P. H. Davis essential oils and their antimicrobial, and antioxidant activities
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Ayşe Esra Karadağ, Betül Demirci, Ömer Çeçen, Fatma Tosun, Anadolu Üniversitesi, and Çeçen, Ömer
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antioxidant ,Antioxidant ,DPPH ,gas chromatography ,medicine.medical_treatment ,Bacillus cereus ,Pharmaceutical Science ,Sabinene ,Pharmacy ,medicine.disease_cause ,law.invention ,mass specrometry ,Apiaceae,Glaucosciadium cordifolium,antimicrobial,antioxidant,gas chromatography,mass spectrometry ,chemistry.chemical_compound ,Listeria monocytogenes ,law ,medicine ,Food science ,Essential oil ,biology ,Farmakoloji ve Eczacılık ,Glaucosciadium cordifolium ,Acinetobacter ,biology.organism_classification ,Antimicrobial ,chemistry ,antimicrobial ,Pharmacology and Pharmacy ,Apiaceae - Abstract
CECEN, Omer/0000-0002-1315-9876, WOS: 000484810700006, Chemical composition of volatile oils obtained from the roots, fruits and aerial parts of Glaucosciadium cordifolium (Boiss.) B. L. Burtt& P. H. Davis (Apiaceae) were analyzed using gas chromatography-flame ionization detector/mass spectrometry, simultaneously. Furthermore, antimicrobial and antioxidant activities of G. cordifolium volatile oils were investigated for possible utilization. Total of 62 volatile compounds were identified in G. cordifolium essential oils, where the main component was characterized as alpha-pinene in all parts, commonly. the other main components were beta-pinene (15.7%), (Z)-beta-ocimene (14%) and sabinene (7%) in the volatile oil of the aerial part; sabinene (10.1%), beta-pinene (10.1%) and alpha-phellandrene (5.3%) in the essential oil of the fruits; hexadecane (12.2%), tetradecane (11.9%), octadecane (7.4%) in the essential oil obtained from the root, respectively. the in vitro microdilution method was used for the antimicrobial activity testing against Salmonella typhi ATCC 6539, Acinetobacter baumanii ATCC 19606, Bacillus cereus ATCC 14579, Staphylococcus aereus ATCC 6538, Listeria monocytogenes ATCC 19115, Helicobacter pylori ATCC 43504 and Mycobacterium avium ATCC 25291. the best antimicrobial activity of the volatile oils was against L. monocytogenes among the tested microorganisms. in addition, DPPH center dot-ABTS(center dot) scavenging activity was tested, none of the essential oils showed any significant antioxidant activity.
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- 2019
25. Türkiye’deki Bazı Tıbbi ve Aromatik Bitkilerin Antioksidan Potansiyalleri ve Fenolik Kompozisyonları
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Ayşe Esra Karadağ
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Tibbi ve aromatik bitkiler, insanlik tarihinin ilk zamanlarindan beri sadece gida ve kozmetik amacli olarak degil ayni zamanda hastalik risklerine karsi geleneksel tedavi amaci ile de kullanilmistir. Tuketilmeleri ile beraber dejeneratif hastaliklarla ilgili riskleri azaltma potansiyellerinin, sahip olduklari antioksidan ozellik gosteren biyoaktif bilesikler, ozellikle fenolik maddelerle ilgili oldugu son yillarda yapilan calismalarla ortaya konulmustur. Gunumuzde saglikli beslenme ve fonksiyonel gidalara olan ilginin artmasi ile beraber, bu bitkilerin uretimi ve kullanimlariyla ilgili talebin onumuzdeki yillarda artacagi ongorulmektedir. Calismamizda, ulkemizde siklikla tuketilen bazi tibbi ve aromatik bitkilerin ( adacayi, anason, cemen, ihlamur, melisa, defne yapragi, nane, reyhan, rezene ve sinameki) toplam fenolik madde miktarlari, antioksidan potansiyelleri, ve fenolik kompozisyonlari belirlenmistir. Toplam fenolik madde icerigi acisindan en zengin bitkiler adcayi, ihlamur, defne ve melisa (16.89-21.12 mg GAE/g bitki), en dusuk bitkiler ise anason, cemen ve rezene yapragi (3.47-3.77 mg GAE/g bitki) olarak belirlenmistir. Dort farkli yontemle, 2,2’-azinobis(3-etilbenzotiazolin-6-sulfonik asit) (ABTS), 1,1-difenil-2-pikrilhidrazil (DPPH), ferrik iyonu indirgeyici antioksidan potansiyeli (FRAP) ve bakir (II) iyonu indirgeyici antioksidan kapasitesi tayini, belirlenen toplam antioksidan kapasitesi sonuclarina gore ihlamur, adacayi, defne yapragi ve melisa en yuksek antioksidan potanisyele sahip bitkiler olmuslardir. Toplam fenolik madde icerigi ile antioksidan potansiyeli arasinda onemli derecede yuksek korelasyon oldugu (R 2 =0.0.87-0.89) gozlenmistir. EC50 degeri, DPPH ve ABTS analizleri acisindan degerlendirildiginde, en yuksek ihlamur (5.93±0.53 ve 1.05±0.03 mg bitki/mL) ve en dusuk anason (82.13±12.08 ve 12.08±0.79 mg bitki/mL) bitkilerine ait olmustur. Calismamizda belirlenen fenolik madde icerigi acisindan ise, protokatesuik asit, kafeik asit, klorojenik asit ve ferulik asitin bu bitkilerde en sik belirlenen fenolik asitler oldugu ve flavaonoidlerden ise kuersetin ve kamferolun belirlendigi gorulmustur.
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- 2019
26. Tilia tomentosa moench çiçeklerinin uçucu bileşenlerinin ve çeşitli in vitro biyolojik aktivitelerinin incelenmesi
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Mehmet Evren Okur, Ayşe Esra Karadağ, Betül Demirci, Nihal Karakaş, Şükran Kültür, and Nurşah Öztunç
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Tilia tomentosa ,biology ,Traditional medicine ,Health Care Sciences and Services ,Chemistry ,Cell culture,Tilia tomentosa,antimicrobial,cell regenerator ,Hücre kültürü,Tilia tomentosa,Antimikrobiyal,Hücre yenileyici,GC/MS ,General Medicine ,Sağlık Bilimleri ve Hizmetleri ,biology.organism_classification - Abstract
Aim: The aim of this study was to investigate the volatile components, total phenolic content, and in vitro antioxidant, antimicrobial and cell viability activities of Tilia tomentosa Moench. (Malvaceae) flower n-hexane extract. Methods: The dried plant material was powdered and extracted with n-hexane by maceration. The volatile components of the extract were investigated by Gas Chromatography / Mass Spectroscopy (GC/MS) and the total phenolic content was determined using the Folin-Ciocalteu method. The antioxidant capacity was tested in vitro DPPH and ABTS radical scavenging methods. Antimicrobial activity was investigated by microdilution method against microorganisms of Pseudomonas aeruginosa ATCC 10145, Escherichia coli NRLL B-3008, Staphylococcus aereus ATCC 6538, Helicobacter pylori ATCC 43504 and Mycobacterium smegmatis ATCC 25291. The effect on cell viability in vitro was determined by measuring the metabolic activity of the cells. Results: The ABTS and DPPH radical scavenging activity of T. tomentosa n-hexane extract was found as 1.94 and 1.03, respectively. In addition, the increased activity of the extract on in vitro cell viability was determined. It was observed that the extract was effective only against Staphylococcus aureus at a dose of 125 µg/mL. The major volatile component of the extract was camphor (17.7%). Conclusion: T. tomentosa n-hexane extract has a positive effect on cell viability, and it has a moderate level of antioxidant activity. For these reasons, the extract may be used as a cell regenerator., Amaç: Tilia tomentosa Moench. (Malvaceae) bitkisininçiçeklerinden elde edilen n-hekzanekstresinin uçucu bileşenleri, toplam fenolik madde miktarı, in vitro antioksidan, antimikrobiyal ve hücre canlılığıaktivitelerinin araştırılması amaçlanmıştır. Yöntem: Kurutulan bitki materyali toz edildikten sonra, n-hekzan kullanılarak maserasyon yöntemiile ekstre hazırlanmıştır. Uçucu bileşenleri Gaz Kromatografisi/KütleSpektroskopisi (GC/MS) ile araştırılmış, toplam fenolik madde miktarıFolin-Ciocalteu yöntemi kullanılarak belirlenmiştir. Antioksidan kapasitesiDPPH ve ABTS radikal süpürücü yöntemleri ile in vitro olarak test edilmiştir. Antimikrobiyal aktivitesi Pseudomonas aeruginosa ATCC 10145, Escherichia coli NRLL B-3008, Staphylococcusaereus ATCC 6538, Helicobacter pylori ATCC 43504 ve Mycobacteriumsmegmatis ATCC 25291 mikroorganizmalarına karşı mikrodilüsyon yöntemikullanılarak araştırılmıştır. In vitro hücre canlılığı üzerine etkisihücrelerin metabolik olarak aktif olma durumlarının ölçümü ile belirlenmiştir. Bulgular: T. tomentosa n-hekzan ekstresinin ABTS ve DPPHradikal süpürücü etkisi sırasıyla 1.94 ve 1.03 olarak bunmuştur. Ek olarak,ekstrenin in vitro hücre canlılığıüzerinde azalan dozlarda artan aktivitesi tespit edilerek en yüksek aktivite 1mg/mL dozunda gözlemlenmiştir. Ekstrenin denenen suşlardan yalnızca Staphylococcus aureus mikroorganizmasınakarşı 125 µg/mL dozda etkili olduğugörülmüştür. Ayrıca major uçucu bileşeni %17.7 oranında kafur olarak tespitedilmiştir. Sonuç: T. tomentosa n-hekzan ekstresinin, hücre canlılığı üzerinde olumlu etkiye sahipolduğu ve orta düzeyde antioksidan etkinliğe sahip olduğundan dolayı hücreyenileyici olarak kullanılabileceği düşünülmektedir.
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- 2019
27. In vitro and in silico Evaluation of ACE2 and LOX Inhibitory Activity of Eucalyptus Essential Oils, 1,8-Cineole, and Citronellal
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Ezgi Ak Sakallı, Kerem Teralı, Ayşe Esra Karadağ, Sevde Nur Biltekin, Müberra Koşar, Betül Demirci, K. Hüsnü Can Başer, and Fatih Demirci
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Pharmacology ,Eucalyptus ,Complementary and alternative medicine ,Drug Discovery ,1,8-Cineole ,Citronellal ,ACE2 ,LOX ,Plant Science ,General Medicine ,Essential Oil - Abstract
Eucalyptus essential oils are well-known and used especially in upper respiratory tract pathologies or diseases as herbal drug preparations. In the present study, the in vitro angiotensin-converting enzyme 2 (ACE2) and lipoxygenase (LOX) enzyme inhibitory potentials of commercial Eucalyptus globulus Labill. and Eucalyptus citriodora Hook. essential oils were evaluated for their potential anti-coronavirus disease 2019 (COVID-19), and anti-inflammatory effects. In addition, the major components, 1,8-cineole and citronellal, were evaluated for their ability to bind at the active site of either human ACE2 or human 5-LOX using an in silico setting. Before activity evaluation, Eucalyptus globulus and E citriodora essential oils were analysed by GC/FID and GC/MS, where 1,8-cineole (30%), and citronellal (80%) were identified as the major components, respectively. The in vitro ACE2 inhibition was calculated as 94.9% for E globulus, and that of E citriodora essential oil as 83.4%. In vitro LOX inhibition experiments for essential oils in the same order showed inhibitions of 71.3 and 91.4%, respectively, at 20 µg/mL test concentrations in microplate-based fluorometric assays. In addition, protein–ligand docking, and interaction profiling was used to gain structural and mechanistic insights into the in silico ACE2 and LOX inhibitory potentials of the major Eucalyptus essential oil constituents, 1,8-cineole as well as citronellal. The resulting data supported the in vitro findings; however, further in vivo studies are needed to confirm the activity. Anadolu University
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- 2022
28. Anti-inflammatory, analgesic and in vivo-in vitro wound healing potential of the Phlomis rigida Labill. extract
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Şule Ayla, Hande Sipahi, Mehmet Evren Okur, Ayşe Esra Karadağ, Fatih Demirci, Şükran Kültür, Yağmur Özhan, Benay Daylan, and Betül Demirci
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Antioxidant ,DPPH ,medicine.drug_class ,medicine.medical_treatment ,Anti-Inflammatory Agents ,Antioxidants ,Anti-inflammatory ,Anti-Inflammatory ,Inhibitory Concentration 50 ,Mice ,Phlomis ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,In vivo ,Drug Discovery ,medicine ,Animals ,030304 developmental biology ,Inflammation ,Pharmacology ,Analgesics ,Mice, Inbred BALB C ,0303 health sciences ,Wound Healing ,ABTS ,biology ,Traditional medicine ,Plant Extracts ,Free Radical Scavengers ,biology.organism_classification ,Phytochemical Analyses ,RAW 264.7 Cells ,chemistry ,030220 oncology & carcinogenesis ,P. Rigida ,Antimicrobial ,Wound healing ,Cell culture assays - Abstract
Ethnopharmacological relevance The preparations of Phlomis aerial parts are used traditionally in Anatolia for wound healing and in inflammatory disorders. Methods For the identification of the active fraction, the air dried aerial parts of Phlomis rigida Labill. were extracted by methanol and fractionated successively by n-hexane, dichloromethane and ethyl acetate, respectively. The phenolic constituents were characterized by the Folin-Ciocaltheu method; the antioxidant activity was performed by ABTS and DPPH radical scavenging assays. In vitro anti-inflammatory activity was evaluated by LOX enzyme inhibition, spectrophotometrically as well as cell cultures. The wound healing properties of P. rigida extract gels were studied via in vitro cell culture methods and in vivo by excisional wound model using Balb-c mice. The P. rigida extract was analyzed and characterized by GC-FID, GC-MS, and LC-MS. Results The P. rigida methanol extract showed moderate LOX inhibitory at IC50 = 19.5 ± 2.8 μg/mL whereas the antioxidant activity was by DPPH• IC50 = 0.89 mg/mL, and by ABTS• IC50 = 0.99 mg/mL, respectively. In addition, a remarkable P. rigida extracts anti-inflammatory activity was observed in the cell culture assay, which was then confirmed by the in vitro wound healing activity applied at 0.125–0.5 mg/mL concentrations, resulting in a dose-dependent increase in wound closure at the final stage. The P. rigida gel formulation was prepared to evaluate the extract in vivo, whereas the experimental results of the new gel formulation supported the findings of the in vitro wound healing activity. Conclusion The findings of this in vitro and in vivo study suggest that the wound healing and anti-inflammatory properties provide a scientific evidence of the ethnopharmacological application of Phlomis species.
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- 2021
29. Composición química, actividades antibacterianas y antioxidantes de Cnidium silaifolia ssp. orientale (Boiss.) de aceites esenciales de tutin
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Fatma Tosun, Betül Demirci, Fatih Demirci, Ayşe Esra Karadağ, Ömer Çeçen, and Çeçen, Ömer
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0301 basic medicine ,Antioxidant ,DPPH ,medicine.medical_treatment ,Bacillus cereus ,Cnidium Silaifolium Ssp. Orientale ,medicine.disease_cause ,03 medical and health sciences ,chemistry.chemical_compound ,0404 agricultural biotechnology ,Apiacea ,medicine ,Antioxidante ,TX341-641 ,Food science ,Cnidium silaifolium ssp. orientale ,030109 nutrition & dietetics ,biology ,Nutrition. Foods and food supply ,Organic Chemistry ,fungi ,food and beverages ,04 agricultural and veterinary sciences ,Tutin ,Antimicrobial ,biology.organism_classification ,Ascorbic acid ,040401 food science ,Antimicrobiano ,chemistry ,Staphylococcus aureus ,Trolox ,Food Science ,Apiaceae - Abstract
The chemical compositions of the essential oils (EOs) obtained by hydrodistillation from different parts of Cnidium silaifolium ssp. orientale (Boiss.) Tutin were analyzed both by GC-FID and GC/MS, simultaneously. One hundred nine compounds representing 90.1% of the total volatiles in the EOs were identified with the main characteristic compounds α-pinene (50.3%) in the root, germacrene D (20.3%) in the fruit, and β-caryophyllene (18.7%) in the aerial parts of C. silaifolium ssp. orientale. The antimicrobial activity against human pathogenic Gram-negative and Gram-positive bacteria was evaluated by the in vitro microdilution method. Antibacterial succeptibility was observed from the root and aerial part EOs against Staphylococcus aureus (0.039 and 0.156 mg/mL, respectively); while the fruit EO was most effective against Bacillus cereus at 0.07 mg/mL. The antioxidant capacities of the EOs were also evaluated by in vitro DPPH• and ABTS•+ scavenging assays, where no significant activity was observed compared to ascorbic acid and Trolox. Se analizó por GC-FID y GC-MS la composición química de los aceites esenciales (AE) obtenidos por hidrodestilación de diferentes partes de Cnidium silaifolium ssp. orientale (Boiss.) tutin. Ciento nueve compuestos, que representan el 90.1% del total de volátiles de los AE, se identificaron. Los compuestos característicos principales fueron α-pineno (50.3%) en la raíz, germacreno D (20.3%) en la fruta y β-cariofileno (18.7%) en las partes aéreas de C. silaifolium ssp. orientale. La actividad antimicrobiana contra bacterias Gram negativas y Gram positivas patógenas humanas se evaluó mediante el método de microdilución in vitro. La susceptibilidad antibacteriana contra Staphylococcus aureusse observó desde la raíz a la parte aérea AEs (0.039 y 0.156 mg/mL, respectivamente), mientras que la fruta EO fue más efectiva contra Bacillus cereus a 0.07 mg/mL. La capacidad antioxidante de los AE también se evaluó mediante ensayos de eliminación in vitro de DPPH• y ABTS•+, donde no se observó actividad significativa en comparación con el ácido ascórbico y Trolox.
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- 2021
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30. Laurocerasus officinalis Roem. meyve ekstrelerinin mide kanseri hücrelerinde kaspaz aracılı apoptoz yoluyla sitotoksik etkilerinin incelenmesi
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Nihal Karakaş, Derya Çiçek Polat, Mehmet Evren Okur, Ayşe Esra Karadağ, and Nurşah Öztunç
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Programmed cell death ,Rosaceae ,Clinical Biochemistry ,Mide Kanseri ,Apoptosis ,Antioksidan Aktivite ,Biochemistry ,03 medical and health sciences ,0302 clinical medicine ,Molecular Biology ,Caspase ,Gastric cancer cell ,030304 developmental biology ,Laurocerasus Officinalis ,0303 health sciences ,biology ,Chemistry ,Biochemistry (medical) ,Antioxidant Activity ,biology.organism_classification ,Apoptoz ,Gastric Cancer ,030220 oncology & carcinogenesis ,Officinalis ,biology.protein ,Cancer research - Abstract
Objectives: Laurocerasus officinalis Roem. fruits are traditionally used for several health problems. Although there are some studies about its antiproliferative effects on different cancer cells, no study was reported about its potential therapeutic efficacy against gastric cancers which is the most malignant disease in the digestive system with high morbidity and mortality. Methods: This study was aimed to evaluate L. officinalis fruit extract phytochemical contents as well as to compare anticancer effects on gastric cancer cells. The antioxidant activities were determined by ABTS and DPPH assays. Anticancer effects were measured by cell viability assays, then apoptotic proteins were analyzed by western blotting and flow cytometry. Results: Laurocerasus officinalis fruit methanol extract showed moderate antioxidant activity by ABTS(center dot) and DPPH center dot assays. Significant cytotoxic activities and caspase mediated apoptosis were detected in the extract treated MKN-45 and AGS gastric cancer cells respectively while sparing healthy cells. Conclusion: Our results showed that the L. officinalis Roem. extract has significant anticancer efficacy on gastric cancer cell lines; therefore, it can be further studied to determine its potential therapeutic components. Giriş: Laurocerasus officinalis Roem. meyveleri halk arasında çeşitli sağlık problemlerine karşı kullanılmaktadır. Farklı kanser hücreleri üzerindeki antiproliferatif etkileri ile ilgili bazı çalışmalar olmakla birlikte, sindirim sistemindeki ciddi bir rahatsızlık olan, yüksek morbidite ve mortaliteye sahip mide kanserlerine karşı herhangi bir çalışma bildirilmemiştir. Yöntem: Bu çalışma L. officinalis meyve ekstrelerinin fitokimyasal analizi ile beraber karşılaştırmalı olarak mide kanseri hücrelerine karşı sitotoksik etkilerinin incelenmesini amaçlamıştır. Antioksidan aktivite ABTS ve DPPH yöntemleriyle araştırılmıştır. Antikanser etkinliği ise hücre canlılığı yöntemi ile araştırılmış ve sonrasında apoptotik proteinleri western blot ve flow sitometre yöntemleri ile ölçülmüştür. Sonuçlar: L. officinalis meyve metanol ekstresi, ABTS ve DPPH testlerine göre orta düzeyde antioksidan aktivite göstermiştir. Sağlıklı hücrelerde sitotoksik etki gözlemlenmezken, ekstre uygulanmış MKN-45 ve AGS mide kanseri hücrelerinde önemli sitotoksik aktiviteler ve kaspaz aracılı apoptoz saptanmıştır. Tartışma: Sonuçlar, L. officinalis Roem ekstresinin mide kanseri hücre hatları üzerinde önemli antikanser etkinliğine sahip olduğunu göstermiştir; bu nedenle, potansiyel terapötik bileşenlerini belirlemek için ileri çalışmalar gerçekleştirilebilecektir.
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- 2021
31. Volatile components and antimicrobial activity of the N-Hexane extracts of neomuretia pisidica (Kit tan) Kljuykov, Degtjareva & Zakharova
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Betül Demirci, Fatma Tosun, Ayşe Esra Karadağ, Ömer Çeçen, Ayvaz Ünal, and Çeçen, Ömer
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Limonene ,Volatile Compounds ,Apiaceae ,Chromatography ,biology ,Methyl linoleate ,Plant Science ,biology.organism_classification ,Antimicrobial ,Biochemistry, Genetics and Molecular Biology (miscellaneous) ,Antimicrobial Activity ,Hexane ,chemistry.chemical_compound ,Camphor ,Neomuretia pisidica,Apiaceae,Volatile compounds,antimicrobial ,chemistry ,Health Care Sciences and Services ,Neomuretia Pisidica ,Sağlık Bilimleri ve Hizmetleri ,Pharmacology, Toxicology and Pharmaceutics (miscellaneous) ,Verbenone ,Hexanol - Abstract
The fruits, aerial parts and roots of Neomuretia pisidica (Kit Tan) Kljuykov, Degtjareva & Zakharova were extracted with n-hexane. Total of 18 compounds were characterised by GC analyses of the n-hexane extracts. Main volatile components of the n-hexane extract of aerial parts were characterized as 1,8-cineole (23.4 %), camphor (21.4 %), 2-ethyl hexanol (14.6 %), α-pinene (7.2 %), and verbenone (6.4 %). Methyl linoleate (19.3 %), 1,8-cineole (16.5 %), camphor (13.2 %), α-pinene (6.1 %) and 2-ethyl hexanol (4.9 %) were found in the n-hexane extract of roots. Whereas, 1,8-cineole (23.3 %), camphor (20.3 %), 2-ethyl hexanol (14.2 %), α-pinene (9.9 %), and limonene (4.1%) were the major components of the n-hexane extract of fruits. Antimicrobial activity were identified using a microdilution assay against selected human pathogenic strains. The most potent inhibitor activities with 156 µg/mL concentrations were detected against S. aureus and E. faecalis.
- Published
- 2021
32. Rinaldo Marmara, Osmanlı Başkentinde Bir Levanten Semti: Galata-Pera
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Esra Karadağ
- Subjects
Social ,Yayın değerlendirme,Rinaldo Marmara,Osmanlı Başkentinde Bir Levanten Semti: Galata-Pera ,General Medicine ,Sosyal - Abstract
Levanten bir aileden gelme bir araştırmacı olarak kaleme aldığı bu çalışmasında Rinaldo Marmara, net bir tanımı olmayan Levanten kavramını ve İstanbul’da, Galata-Pera bölgesinde yaşamış olan Levantenleri inceliyor. Marmara’nın ileri düzeydeki İtalyanca ve Fransızcası ile Osmanlı tarihçiliğinin temel sorunlarından biri olan yabancı arşivlerin yeterince kullanıl(a)maması problemini aşarak mevzubahis konu hakkında literatürdeki boşluğu doldurma gayesi kitabın en önemli özelliği olarak göze çarpıyor. Levanten kelimesi, üzerinde hâlâ tartışmaların devam ettiği, tam olarak neyi içine aldığı yahut neyi dışarıda bıraktığı netleşmemiş, farklı şekillerde yorumlanan bir kavram olarak karşımıza çıkmaktadır. Yapılan tanımların vardığı ortak sonuç Levantenlerin köken olarak Avrupalı oldukları ve Osmanlı topraklarında yaşadıklarıdır.1 Fakat hangi dönemde yaşadıkları, tam olarak hangi milletlere mensup olduklarına dair bir görüş birliği yoktur.
- Published
- 2020
33. Evaluation of in vitro anti-cancer effects of Styphnolobium japonicum root extract in human colon (HT-9), brain (U-87), and prostate (PC-3) cancer cell lines
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Nurşah Öztunç, Mehmet Evren Okur, Ayşe Esra Karadağ, Fatih Demirci, Nihal Karakaş, and İbrahim Serkut Tosyali
- Subjects
Western Blotting ,Styphnolobium Japonicum (Sophora Japonica) ,Cytotoxicity ,Pharmaceutical Science ,Pharmacy ,chemistry.chemical_compound ,Matrine ,Health Care Sciences and Services ,Viability assay ,Gallic acid ,Sağlık Bilimleri ve Hizmetleri ,Cytotoxicity,Styphnolobium japonicum (Sophora japonica),antioxidant,cancer cell lines,western blotting,flow cytometry analysis ,Flow Cytometry Analysis ,biology ,Farmakoloji ve Eczacılık ,Styphnolobium japonicum ,biology.organism_classification ,Molecular biology ,Oxymatrine ,chemistry ,Cell culture ,Apoptosis ,Cancer Cell Lines ,Cancer cell ,Antioxidant ,Pharmacology and Pharmacy - Abstract
Background and Aims: Styphnolobium japonicum (L.) Schott. (Sophora japonica) is a medicinal plant applied for various diseases, in the traditional medicine field. The evaluation of methanol extract of S. japonicum root derived from the Pharma Grade plant drug, was performed in terms of various in vitro biological activities.Methods: The LC-MS analysis was used for the chemical characterization of the methanol extract. The anti-cancer activity was evaluated in colon (HT-9), brain (U-87), and prostate (PC-3) cancer cells by Cell Titer Glo viability assay (Promega) and western blot analysis of PARP (Poly ADP-ribose polymerase) cleavage.Results: The relative amounts of matrine and oxymatrine in the extract were found as 0.49 +/- 0.006 mg/mL and 0.27 +/- 0.016 mg/mL, respectively. The S. japonicum extract showed 53.17 +/- 0.97 mg of gallic acid (GA)/g corresponding to the total phenolic amounts, resulting in relatively moderate antioxidant activity (1.94 +/- 0.23 and 2.79 +/- 0.15 mg/mL) on the in vitro2,2'-azino-bis(3ethylbenzothiazoline-6-sulfonic acid (ABTS center dot) and 2,2-diphenyl-1-picrylhydrazyl (DPPH center dot) assays. Treatment with 10 mg/mL S. japonica root extract for 24h resulted in a significant decrease in cell viability. The cell viability of U-87, HT-29, and PC-3 cancer cell lines was determined as 35 +/- 2.21%, 14 +/- 2.11%, and 46 +/- 5.67%, respectively. The extract showed 5.104, 5.012 and 0.555 mg/mL IC50 values for HT-29, U-87, and PC-3 cell lines, respectively. Particularly, the IC50 value of PC-3 cancer cell line was significantly lower than the healthy human fibroblast cells. In further, the apoptosis in S. japonicum root extract treated PC-3 cells was detected through flow cytometry analysis of Annexin V positive cells and western blot analysis of PARP cleavage.Conclusion: It can be concluded that the methanol extract in determined doses induces the apoptosis of the PC-3 cancer cells, without any significant cytotoxic effect on healthy human fibroblast cells. In addition, the LCMS analysis showed the presence of matrine and oxymatrine, which are known for their anticancer activity. To the best of our knowledge, these are the first preliminary results indicating the possible use of S. japonicum root extract. Thus, the methanol extract can be further studied for its therapeutic potential of primarily prostate and other cancer types.
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- 2020
34. Antimicrobial activities of mouthwashes obtained from various combinations of Elettaria cardamomum Maton., Lavandula angustifolia Mill. and Salvia triloba L. essential oils
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İlker Demirbolat, Panoraia I. Siafaka, Murat Kartal, Ayşe Esra Karadağ, Neslihan Üstündağ Okur, Ayşe Pınar Yağcılar, and Esra Ipekci
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Lavandula angustifolia ,Salmonella ,food.ingredient ,biology ,Traditional medicine ,Lavender ,SAGE ,Elettaria cardamomum ,Bacillus cereus ,Plant Science ,Salvia ,Antimicrobial ,medicine.disease_cause ,biology.organism_classification ,Biochemistry, Genetics and Molecular Biology (miscellaneous) ,food ,Health Care Sciences and Services ,medicine ,Formulation,Lavandula angustifolia,Elettaria cardamomum,Salvia triloba,mouthwash,antimicrobial ,Sağlık Bilimleri ve Hizmetleri ,Pharmacology, Toxicology and Pharmaceutics (miscellaneous) - Abstract
Essential oils generally show significant antimicrobial activity.Herein,the aim was to obtained the volatileoils ofElettaria cardamomum Maton., Lavandula angustifolia Mill. and Salvia triloba L. and to investigate the antimicrobial activity of mouthwashes formulated with different combinations of E. cardamomum, L. angustifolia and S. triloba essential oils (v/v; 0.1/0.25/0.1; 0.2/0.25/0.1; 0.3/0.1/0.1 in 10 mL).The antimicrobial evaluation was performed using the disc diffusion method against the human pathogenic Staphylococcus aureus ATCC 6538, Escherichia coli NRLL B-3008,Bacillus cereus 14579, Salmonella typhiiclinical isolated. In the present study, among the tested bacteria, S. typhii was the more sensitive to the moutwash formulations, while B. Cereusand E. coli were the most resistant.
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- 2020
35. Polypodium vulgare ile yara iyileşme alanina alternatif bir yaklaşim
- Author
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Mehmet Evren Okur, Ayşe Esra Karadağ, Ekrem Musa Özdemir, Şule Ayla, Nuray Kepil, Mehmet Yalçın Günal, Ayşe Arzu Şakul, Benay Daylan, Sebnem Batur, ALKÜ, and 0-belirlenecek
- Subjects
antioxidant ,Polypodium vulgare ,Wound healing ,Pharmacology ,polypodium vulgare ,In vivo ,Medicine ,Original Study ,Yara İyileşmesi ,biology ,Epidermis (botany) ,business.industry ,Granulation tissue ,General Medicine ,biology.organism_classification ,antioksidan ,Staining ,medicine.anatomical_structure ,biology.protein ,Immunohistochemistry ,yara iyileşmesi ,Antioxidant ,business ,Platelet-derived growth factor receptor - Abstract
Objective: In this study, we examined the effects of Polypodium vulgare L. (Polypodiaceae) as a candidate to be used for wound healing scarred area. We investigated the antibacterial, and antioxidant activity of P. Vulgare on both in vivo, and in vitro wound healing using an excisional wound model in mice.Method: We used 32 Balb-c mice equally divided into four groups: Group 1 control, Group 2 vehicle, Group 3 Polypodium vulgare, and Group 4 Centella asiatica extract (CAE). All treatments were applied topically once in a day. The scar area, percentage wound closure and epithelization time were measured. PDGF, VEGF, and collagen immunohistochemical staining were used for evaluation.Results: CAE and P. vulgare extract groups were observed to be more effective than the control and vehicle groups in terms of new vascular, epidermal and granulation tissue organization. PDGF, VEGF, and collagen immunohistochemical staining was stronger in the P.vulgare extract and CAE groups compared to the control and vehicle groups. In the P. vulgare and CAE groups, PDGF staining intensity was stronger than the control and vehicle groups, but VEGF and collagen staining in P. vulgare group was not different from the control group.Conclusion: P. vulgare had an effect on the injured area by regenerating the epidermis and increasing vascularization. P. vulgare extract with known antioxidant, and antimicrobial activities may be helpful as a supportive treatment in wound healing. Amaç: Bu çalışmada Polypodium vulgare L. (Polypodiaceae), yara iyileşme adayı olma potansi yeli açısından değerlendirildi. Farelerde eksizyonel bir yara modeli kullanılarak hem in vivo hem de in vitro yara iyileşmesinde P.vulgare’nin antimikrobiyal ve antioksidan aktivitesini araştırdık. Yöntem: Eşit olarak dört gruba ayrılmış toplam 32 Balb-c faresi kullandık; Grup 1 kontrol, grup 2 taşıyıcı grup 3 Polipodyum vulgare, grup 4 Centella asiatica özütü (CAE). Tüm tedaviler topikal olarak günde bir kez uygulandı. Yara izi alanı, yara kapanma yüzdesi ve epitelizasyon süresi ölçül dü. İmmünhistokimyasal değerlendirmede PDGF, VEGF ve kollajen boyaları kullanıldı. Bulgular: C A E v e P. v u l g a r e e k s t r a k t g r u p l a r ı n ı n y e n i v a s k ü l e r o r g a n i z a s y o n , e p i d e r m i s v e granülasyon doku organizasyonu açısından kontrol ve taşıyıcı gruplarından daha etkili olduğu gözlenmiştir. PDGF, VEGF ve kollajen immünohistokimyasal boyama, P.vulgare ekstraktı ve CAE gruplarında kontrol ve taşıyıcı gruplarına göre daha kuvvetliydi. P. vulgare ve CAE grubunda PDGF boyama yoğunluğu, kontrol ve taşıyıcı gruplarından daha kuvvetliydi, ancak P. vulgare grubundaki VEGF ve kollajen boyama, kontrol grubundan farklı değildi. Sonuç: P. vulgare yara iyileşmesini ve granülasyon dokusunu, epidermal rejenerasyonu ve anjiyogenezi arttırdı. Antioksidan ve antimikrobiyal aktiviteleri ile bilinen P. vulgare ekstraktı, yara iyileşmesini desteklemek için yararlı olabilir.
- Published
- 2020
36. Alloksan ile diyabet oluşturulmuş farelerde naringin jelin yara iyileştirici etkiler
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Hande Sipahi, Ayşe Esra Karadağ, Cemre Şahin Şenyüz, Ekrem Musa Özdemir, Sebnem Batur, Ayşe Arzu Şakul, Şule Ayla, Mehmet Evren Okur, Ahmet Aydin, Şaziye Sezin Yücelik, and Benay Daylan
- Subjects
Pharmacology ,Wound Healing ,Hücre Kültürü ,business.industry ,Cell Culture ,Pharmaceutical Science ,Granulation tissue ,medicine.disease_cause ,Antimicrobial ,chemistry.chemical_compound ,medicine.anatomical_structure ,chemistry ,In vivo ,Alloxan ,HET-CAM ,medicine ,Diabetes Mellitus ,Irritation ,Wound healing ,business ,Cytotoxicity ,Naringin ,Yara İyileşmesi - Abstract
Objective: The aim of this study was to investigate the effects of naringin, a known flavonoid, on in vitro cytotoxicity, irritation and in vivo potential efficacy when topically applied to the diabetic wound. Material and Method: In vitro direct contact assay and hen's egg chorio-allantoin membrane tests were used to evaluate irritation, and cytotoxicity potential of Naringin. In vitro antimicrobial activity was also tested. Topical treatments were administered once a day on the wound. Wound lesions were photographed and statistically analyzed. After the 10th day, histopathological parameters of tissues were assessed. Result and Discussion: The results showed that naringin gel has no cytotoxicity and irritation potential. Also, it displayed a weak antimicrobial effect. Aside from these, in vivo studies revealed that naringin gel showed statistically higher wound contraction and re-epithelialization, the thickness of granulation tissue, angiogenesis scores. The results indicated that naringin gel effectively enhanced diabetic wound healing, and so this formulation could be considered a promising therapeutic alternative for treating diabetic wounds. Amaç: Bu çalışmanın amacı, bir flavonoid olan Naringin’in in vitro sitotoksisite, irritasyon ile diyabetik yara üzerindeki in vivo potansiyel etkilerini araştırmaktı. Gereç ve Yöntem: Naringin'in irritasyon ve sitotoksisite potansiyelini değerlendirmek için in vitro doğrudan temas deneyi ve tavuk yumurtası korio-allantoin membran testleri kullanıldı. Aynı zamanda in vitro antimikrobiyal etkinlikte test edildi. Topikal tedaviler günde bir kez yaraya uygulandı. Yara lezyonları fotoğraflandı ve istatistiksel olarak analiz edildi. 10. günden sonra dokuların histopatolojik parametrelerideğerlendirildi.Sonuç ve Tartışma: Sonuçlar, naringin jelin sitotoksisite ve tahriş potansiyeli olmadığını göstermiştir. Ayrıca, zayıf bir antimikrobiyal etki gösterdi. Bunların yanı sıra, in vivo çalışmalar naringin jelin istatistikselolarak daha yüksek yara kapanması ve re-epitelyalizasyon, granülasyon dokusunun kalınlığı ve anjiyogenezskorları gösterdiğini ortaya koymuştur. Sonuçlar, naringin jelin diyabetik yara iyileşmesini etkili bir şekilde arttırdığını gösterdi ve bu nedenle bu formülasyon, diyabetik yaraların tedavisi için umut verici bir terapötik alternatif olarak düşünülebilir.
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- 2020
37. Antimicrobial, anticholinesterase evaluation and chemical characterization of essential oil Phlomis kurdica Rech. fil. Growing in Turkey
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Betül Demirci, Şükran Kültür, K. Hüsnü Can Başer, Ayşe Esra Karadağ, Fatih Demirci, and Anadolu Üniversitesi
- Subjects
GC ,P. Kurdica ,biology ,Traditional medicine ,010405 organic chemistry ,Chemistry ,GC/MS ,MS ,General Chemistry ,kurdica ,Cholinesterase ,Antimicrobial ,biology.organism_classification ,01 natural sciences ,0104 chemical sciences ,law.invention ,010404 medicinal & biomolecular chemistry ,Phlomis ,law ,Chemical constituents ,Lamiaceae ,GC-FID ,Essential oil - Abstract
Demirci, Fatih/0000-0003-1497-3017, WOS: 000524573700001, The Phlomis kurdica Rech.fil. (Lamiaceae) essential oil was investigated for its chemical constituents and in vitro biological activities. Volatile components were characterized, antimicrobial and anticholinesterase activities were performed. the oil was analyzed both by gas chromatography-mass spectrometry and gas chromatography-flame ionization detector, simultaneously. the in vitro antimicrobial microdilution method was used against Bacillus cereus ATCC 14579, Pseudomonas aeruginosa ATCC 10145, Escherichia coli NRLL B-3008, Staphylococcus aureus ATCC 6538, Helicobacter pylori ATCC 43504, Staphylococcus epidermidis ATCC 14990, and Candida albicans ATCC 90028, respectively. Additionally, the cholinesterase enzyme inhibition activities were tested in vitro using the Ellman method. A total of forty-four different volatile constituents were identified, where the main components were characterized as germacrene D (55.4%), (Z)-beta-farnesene (11.2%), and hexadecanoic acid (8.4%), respectively. the P. kurdica oil showed moderate inhibition of cholinesterases, where inhibitory antimicrobial activity was against B. cereus among the tested microorganisms.
- Published
- 2020
38. In Vitro ACE2 and 5-LOX Enzyme Inhibition by Menthol and Three Different Mint Essential Oils
- Author
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Fatih Demirci, Sevde Nur Biltekin, Betül Demirci, and Ayşe Esra Karadağ
- Subjects
Pharmacology ,ACE2 ,LOX ,Plant Science ,General Medicine ,In vitro ,Essential Oil ,Menthol ,chemistry.chemical_compound ,Enzyme inhibition ,Complementary and alternative medicine ,chemistry ,Biochemistry ,Drug Discovery ,Mentha - Abstract
Mentha arvensis L., M. citrata L., and M. spicata L. (family Lamiaceae) essential oils, and their characteristic constituent, menthol, were evaluated in vitro for angiotensin converting enzyme 2 (ACE2) and 5-lipoxygenase (5-LOX) enzyme inhibitory activity. The chemical compositions of M. arvensis, M. citrata, and M. spicata essential oils were analysed both by GC-FID, and GC/MS; 82.0%, 38.1%, and 0.4% menthol were identified, respectively. M. spicata essential oil contained 88.2% carvone as its major component. The enzyme inhibitory activities of the essential oils were evaluated using a fluorometric multiplate based enzyme inhibition kit; the ACE2 inhibitions produced by M. arvensis, M. citrata, and M. spicata essential oils were 33%, 22%, and 73%, while the 5-LOX inhibitions were 84%, 79%, and 70%, respectively. In addition, menthol also showed remarkable ACE2 inhibition of 99.8%, whereas the 5-LOX inhibition was 79.9%. As a result, menthol and the three different mint essential oils may have antiviral potential applications against coronaviruses due to their ACE2 enzyme inhibition and anti-inflammatory features. However, further in vivo studies are needed to confirm the safety and efficacy.
- Published
- 2021
39. Matrin ve oksimatrinin mikrobiyal transformasyonu ve metabolitlerinin in vitro biyolojik aktivitelerinin incelenmesi
- Author
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Ayşe Esra Karadağ and Fatih Demirci
- Subjects
chemistry.chemical_classification ,biology ,Metabolite ,General Medicine ,biology.organism_classification ,Antimicrobial ,medicine.disease_cause ,Enterococcus faecalis ,Microbiology ,chemistry.chemical_compound ,Enzyme ,Oxymatrine ,chemistry ,Biotransformation ,Matrine ,Staphylococcus aureus ,Health Care Sciences and Services ,medicine ,Biyotransformasyon,kolinesteraz,lipooksijenaz,matrin,oksimatrin ,Biotransformation,cholinesterase,lipoxygenase,matrine,oxymatrine ,Sağlık Bilimleri ve Hizmetleri - Abstract
Aim: It is aimed to examine the comparative biological activities of metabolites of matrine and oxymatrine compounds which were obtained by microbial transformation. Methods: After the cultivation of 30 different microorganisms in liquid medium, the transformation of substrates to new media was observed by adding them separately. The metabolites were initially identified by thin layer chromatography. Antimicrobial activity was investigated by microdilution method against microorganisms of Pseudomonas aeruginosa ATCC 10145, Escherichia coli NRLL B-3008, Staphylococcus aureus ATCC 6538, Helicobacter pylori ATCC 43504, Streptococcus epidermidis ATCC 14990, andCandida albicans ATCC 90028. The acetylcholinesterase enzyme inhibition was investigated by Ellman's method. 5-lipoxygenase enzyme inhibition experiments were determined by Baylac’s colorimetric method. Results: The biotransformation of the matrine with Mucor ramannianus and Enterococcus faecalis resulted in two metabolites (M1 and M2). Matrine was obtained as a metabolite by the biotransformation of oxymatrine with 5 different microorganisms. Conclusion: Matrine, oxymatrine, M1 and M2 metabolites were not effective for antimicrobial activity. Matrine (10.47%), oxymatrine (21.11%), M1 (24.23%) and M2 (26.42%) metabolites showed moderate activity compared to standard NDGA (96.35%) for 5-lipoxygenase enzyme inhibition. When acetylcholinesterase/ butyrylcholinesterase enzyme inhibitions are evaluated in terms of matrine (34,16%/ 20,49%), oxymatrine (23.68%/ 22.76%), M1 (27.72%/ 22.05%) and M2 (30.63%/23.98%) however, a slight increase in activity was observed in metabolites., Amaç: Matrin ve oksimatrin bileşiklerinin mikrobiyal transformasyon yolu ile metabolitlerin karşılaştırmalı olarak biyolojik aktivitelerinin incelenmesi hedeflenmiştir. Yöntem:30 farklı mikroorganizmanın sıvı besiyerinde üretilmesinden sonra, substratların ayrı ayrı ortama eklenerek yeni maddelere dönüşümü gözlemlenmiştir. Üretilen yeni maddeler besiyerinden uygun koşullarda ekstre edilerek, İnce Tabaka Kromatografisi ile maddelerin varlığı tespit edilmiştir. Antimikrobiyal aktivitePseudomonas aeruginosa ATCC 10145, Escherichia coli NRLL B-3008,Streptococcus epidermidis ATCC 14990, Staphylococcus aureus ATCC 6538, Helicobacter pylori ATCC 43504 ve Candida albicans ATCC 90028mikroorganizmalarına karşı mikrodilüsyon yöntemi kullanılarak incelenmiştir. Asetilkolinesteraz enzim inhibisyonu Ellman metodu ile araştırılmıştır. 5-lipooksijenaz enzim inhibisyonu deneyleri ise kolorimetrik yöntemlebelirlenmiştir. Bulgular: Matrin substratından Mucor ramannianus ve Enterococcus faecalis ile mikrobiyal biyotransformasyon sonucu iki metabolit (M1 ve M2) oluşmuştur. Oksimatrin substratının beş farklı mikroorganizma ile biyotransformasyonu sonucu matrin metabolit olarak elde edilmiştir. Sonuç: Matrin, oksimatrin, M1 ve M2 metabolitlerinin antimikrobiyal açıdan etkili olmadığı tespit edilmiştir. Matrin (%10.47), oksimatrin (%21.11), M1 (%24.23) ve M2 (%26.42)’nin 5-LOX enzim inhibisyonu açısından standart NDGA (%96.35) ile kıyaslandığında orta düzeyde aktivite gösterdiği görülmüştür. Asetilkolinesteraz/ bütirilkolinesteraz enzim inhibisyonu matrin (%34.16/ %20.49), oksimatrin (%23.68/ %22.76), M1 (%27.72/ %22.05) ve M2 (%30.63/ %23.98) açısından değerlendirildiğinde ise metabolitlerde az da olsa aktivitede artış gözlemlenmiştir.
- Published
- 2019
40. In vitro antibacterial, antioxidant, anti-inflammatory and analgesic evaluation of Rosmarinus officinalis L. flower extract fractions
- Author
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Fatih Demirci, Deborah Orak, Hande Sipahi, Betül Demirci, Kemal Hüznü Can Başer, Ayşegül Çaşkurlu, Mehmet Evren Okur, Ayşe Esra Karadağ, Karadağ, A.E., Demirci, B., Çaşkurlu, A., Demirci, F., Okur, M.E., Orak, D., Başer, K.H.C., Yeditepe Üniversitesi, Anadolu Üniversitesi, Eczacılık Fakültesi, Farmakognozi Anabilim Dalı, Demirci, Betül, Demirci, Fatih, and Başer, K. Hüsnü Can
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0106 biological sciences ,ABTS ,biology ,Traditional medicine ,DPPH ,Rosmarinic acid ,Plant Science ,biology.organism_classification ,01 natural sciences ,Rosmarinus ,Rosmarinus Officinalis ,0104 chemical sciences ,Borneol ,Antibacterial ,Anti-Inflammatory ,010404 medicinal & biomolecular chemistry ,Camphor ,chemistry.chemical_compound ,chemistry ,Officinalis ,Rosmarinus officinalis ,Anti-inflammatory ,Antioxidant ,Quercetin ,010606 plant biology & botany - Abstract
Rosmarinus officinalis L. (rosemary) is a common culinary spice and herbal drug, which is used for centuries all over the world. In this present study, apolar to polar fractions of R. officinalis flowers were evaluated for their in vitro antioxidant, antibacterial, cytotoxic, anti-inflammatory and analgesic activities, respectively. Phytochemical compositions of R. officinalis extract fractions were analyzed by GC–MS and LC–MS. The antioxidant capacity of the fractions was evaluated by using the DPPH• and ABTS• methods. The antibacterial potential was determined using the in vitro broth microdilution assay against a panel of human pathogens. The analgesic and anti-inflammatory activities were investigated measuring nitric oxide (NO) and prostaglandin E2 (PGE2) production in LPS-stimulated cells, respectively. In addition, in vitro cytotoxicity of the extract fractions was evaluated on RAW 264.7 murine macrophage cells by using the MTT assay. The constituents of the polar fractions were identified as rosmarinic acid, luteolin, quercetin and apigenin by LC techniques, whereas the n-hexane fraction was analyzed by GC–MS to determine the main volatile components camphor (19.6%), 1,8-cineole (11.7%), verbenone (11.5%), borneol (10.6%), ?-pinene (5.8%), and linalool (5.7%). According to the bioactivity results, the polar fraction showed the highest antioxidant activity, whereas n-hexane fraction was found to be most effective against Staphylococcus aureus (78 µg/mL). The n-hexane fraction (100 µg/mL) reduced the LPS-induced NO and PGE2 production capability. In conclusion, R. officinalis flower n-hexane and ethyl acetate fractions exhibited remarkable in vitro antibacterial, antioxidant, anti-inflammatory and analgesic activities possibly due to their polyphenol content, to the best of our knowledge for the first time. © 2019 South African Association of Botanists
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- 2019
41. In vitro cytotoxicity evaluation of Marrubium vulgare L. methanol extract
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Fatih Demirci, Rabia Yılmaz, Aye Esra Karadağ, Nihal Karakaş, Mehmet Evren Okur, Anadolu Üniversitesi, Sağlık Bilimleri Enstitüsü, Demirci, Fatih, and Tıp Fakültesi
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Traditional medicine ,biology ,Cytotoxicity-1 ,In vitro cytotoxicity ,U87-3 ,Marrubium vulgare ,T98G-5 ,biology.organism_classification ,Ln229-4 ,chemistry.chemical_compound ,chemistry ,Marrubium Vulgare-6 ,Methanol ,Glioblastoma Multiforme Cell Lines-2 - Abstract
WOS: 000476616000014, Marrubiuni vulgare L. (Lamiaceae) is a herbal drug used for centuries for many diseases. In this present study the plant material was acquired from commercial sources in pharma grade (PhEur 8.0) quality. The methanol extract of the aerial parts was evaluated for its in vitro cytotoxic activity by measuring the percentage of viable cells (U87 LN229 and T98G glioblastoma multiforme cell lines) using a luminescence system, and the antioxidant activities by ABTS and DPPH radical scavenging spectrophotometrically. As a result, the methanol extract of M. vulgare showed 48.97 +/- 0.82 mg of GA/g corresponding to the total phenolic amounts, and moderate antioxidant activity (1.33 and 2.08) by ABTS. and DPPH. assays. To the best of knowledge, after evaluation of the cytotoxicity on M. vulgare treated U87 (IC50:270.3 mu M), LN229 (IC50:343.9 mu M) and T98G (336.6 mu M) glioblastoma multiforme (GBM) cell lines, significant cytotoxic activities with 69.9% (p=0.0081) and 71% cell viability (p=0.0028) was observed in M. vulgare treated U87 and LN229 GBM cell lines, respectively. Overall, further in vitro and in vivo bioactivity studies based on phytochemistry on various M. vulgare preparations are worthwhile in order to discover bioactive secondary metabolites.
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- 2019
42. Antioxidant activity and cytotoxic effects of Prunus spinosa L. fruit extract on various cancer cell lines
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Irem Ozturk, Derya Çiçek Polat, Nihal Karakaş, Mehmet Evren Okur, Ayşe Esra Karadağ, and Şule Ayla
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Antioxidant ,ABTS ,Traditional medicine ,biology ,DPPH ,medicine.medical_treatment ,Cancer ,General Medicine ,medicine.disease ,biology.organism_classification ,chemistry.chemical_compound ,chemistry ,Prunus spinosa ,medicine ,Cytotoxic T cell ,Viability assay ,Cytotoxicity - Abstract
Objective Blackthorn (Prunus spinosa L. (Rosaceae) is a shrup whose fruits are consumed as food in Turkey. This study was aimed to evaluate antioxidant activity of methanol extract of P. spinosa and its cytotoxic effects on cancer cell lines. Method Methanol extract of P. spinosa fruit was evaluated for its in vitro cytotoxic activity on multiform (GBM) brain cancer (LN229, U87 and T98G) and pancreas cancer (PANC-1 and AsPC-1) cell lines. Cell viability assays were performed by calculating the percentage of viable cells using a luminescence system, and spectrophotometrically. measuring its antioxidant ABTS and DPPH radical scavenging activities. Differences were considered as statistically significant at p*
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- 2019
43. Investigation of antioxidant and cytotoxic activities of Opuntia ficus-indica (L.) Mill. fruit extract
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Damla Uludag, Derya Çiçek Polat, Mehmet Evren Okur, Ayşe Esra Karadağ, Nihal Karakaş, and Anadolu Üniversitesi
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Opuntia ficus-indica ,ABTS ,Antioxidant ,antioxidant ,Traditional medicine ,Farmakoloji ve Eczacılık ,Chemistry ,DPPH ,medicine.medical_treatment ,Extract ,Pharmaceutical Science ,food and beverages ,Bain Cancer Cell Line ,Pharmacy ,chemistry.chemical_compound ,Cell culture ,Extract,Opuntia ficus-indica,Brain cancer cell line,Colon cancer cell line,Antioxidant ,Cancer cell ,brain cancer cell line ,medicine ,Cytotoxic T cell ,Viability assay ,Pharmacology and Pharmacy ,Quercetin ,colon cancer cell line - Abstract
okur, mehmet evren/0000-0001-7706-6452, WOS: 000511129700007, Opuntia ficus-indica fruits are claimed to possess several health-beneficial properties. This study was carried out to determine the phytochemicals as well as to compare antioxidant activity and cell viability of the methanol extract of OFI-fruits. Antioxidant activity was evaluated by various in vitro tests such as DPPH and ABTS. LC-MS and HPLC analyses were then performed. the activity of the OFI-fruit extract on viability of U87-MG (glioblastoma multiform), HT-29 (colon cancer) and human primary fibroblast cells was investigated by determining viable cells on a luciferase based system (Cell TiterGlo; Promega; USA). the results showed that OFI-fruits were a source of antioxidant compounds. Moreover, the extract was found to have rich phenolic-flavonoid contents. Quercetin was found in the extract according to LC-MS and HPLC studies. A remarkable increased cell death in the HT-29 and U87 cell lines was detected in a concentration-dependent manner (1-10mg/mL). Among these cell lines, HT-29 responded to OFI-fruit treatment more sensitively to even the lowest dose (1mg/mL). the results of this study showed that the OFI-fruit has significant antioxidant capacity and leads to strong cytotoxic activity on various cancer cells. Therefore, it can be suggested that OFI-fruits may have chemo-preventive potential and can be studied further to clarify cytotoxic abilities.
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- 2019
44. In Vivo Wound Healing and In Vitro Anti-Inflammatory Activity Evaluation of Phlomis russeliana Extract Gel Formulations
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Fatih Demirci, Yağmur Özhan, Hande Sipahi, Şule Ayla, Mehmet Evren Okur, Ayşe Esra Karadağ, Betül Demirci, Benay Daylan, Neslihan Üstündağ Okur, and Anadolu Üniversitesi
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P. Russeliana ,DPPH ,medicine.drug_class ,Ethyl acetate ,Pharmaceutical Science ,030226 pharmacology & pharmacy ,Anti-inflammatory ,Bioactivity-Guided Fractionation ,Analytical Chemistry ,lcsh:QD241-441 ,Anti-Inflammatory ,Mice ,03 medical and health sciences ,Phytol ,chemistry.chemical_compound ,0302 clinical medicine ,lcsh:Organic chemistry ,In vivo ,Drug Discovery ,medicine ,Physical and Theoretical Chemistry ,030304 developmental biology ,Wound Healing ,0303 health sciences ,ABTS ,Chromatography ,integumentary system ,biology ,Organic Chemistry ,biology.organism_classification ,Phytochemical Analyses ,Phlomis ,chemistry ,Chemistry (miscellaneous) ,P. russeliana ,Molecular Medicine ,Wound healing - Abstract
The air-dried aerial parts of Phlomis russeliana (Sims) Lag. Ex Benth. was extracted by methanol and fractionated by n-hexane, dichloromethane, and ethyl acetate, respectively. The wound healing properties of P. russeliana extract gel was evaluated using the in vivo excisional wound model using Balb-c mice. Initially, the P. russeliana methanol extract showed LOX inhibitory activity at IC50 = 23.2 µ, g/mL, whereas the DPPH&bull, assay showed IC50 = 0.89 mg/mL, and the ABTS&bull, assay showed IC50 = 0.99 mg/mL, respectively. In addition, a remarkable anti-inflammatory activity was observed in the cell culture assay. Thereafter, activity-guided fractionation was performed by LOX enzyme inhibition assays, and the structures of the two most active fractions were revealed by both GC&ndash, FID and GC/MS analyses, simultaneously. Phytol and 1-heptadecanoic acid were characterized as the active constituents. Moreover, the P. russeliana extract gel formulation was applied for in vivo tests, where the new gel formulation supported the in vitro anti-inflammatory activity findings. As a conclusion, this experimental results support the wound healing evidence based on the ethnobotanical application of Phlomis species with further potential.
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- 2020
45. Design and synthesis of novel cylopentapyrazoles bearing 1,2,3-thiadiazole moiety as potent antifungal agents
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Hatice Başpınar Küçük, Mustafa Guzel, Ozgecan Savlug Ipek, Ayşe Esra Karadağ, Betül Giray, and Hanife Pekel
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Antifungal Agents ,Cyclopentadiene ,1,2,3-Thiadiazole ,Stereochemistry ,Fungicide ,Protein Data Bank (RCSB PDB) ,Antifungal drug ,Microbial Sensitivity Tests ,01 natural sciences ,Biochemistry ,Plant Pathogen ,Docking ,Structure-Activity Relationship ,chemistry.chemical_compound ,Fusarium ,Antifungal Activity ,Thiadiazoles ,Drug Discovery ,Moiety ,Homology modeling ,Molecular Biology ,Botrytis cinerea ,Dose-Response Relationship, Drug ,Molecular Structure ,Gykopentapyrazole ,biology ,010405 organic chemistry ,Organic Chemistry ,Molecular Modelling Studies ,biology.organism_classification ,Cycloaddition ,0104 chemical sciences ,Molecular Docking Simulation ,010404 medicinal & biomolecular chemistry ,chemistry ,Docking (molecular) ,Drug Design ,Novel Antifungal Drug Development - Abstract
In drug-resistant phytopathogenic fungi, there has been extensive research on microbiological and antifungal drug development. In this study, a novel series of cylopentapyrazole bearing a 1,2,3-thiadiazole ring 2a-e were designed and synthesized according to the principle of combination of bioactive structures. Thus, we have employed a [3 + 2] cycloaddition with 4-methyl-[1,2,3] thiadiazole-5-carboxylic acid hydrazones 1a-e and cyclopentadiene ring. Novel synthesized compounds were identified with IR, 1H and 13C NMR, mass spectrometry and elemental analysis then, antifungal activities were assayed. Based on our study, a combination of the compounds 1a and 2b possess remarkable antifungal activity against Botrytis cinerea AHU 9424 with 100% inhibition. EC50 values were calculated by studying different doses in combinations with high inhibition rates. The combination of 1a + 2b has an EC50 value at 6.37 and 13.85 µg/ml concentrations against B. cinerea and F. culmorum, respectively. The combination of compound 1a + 2b, having a cylopentapyrazole ring on the 1,2,3-thiadiazole backbone, shows promising fungicidal activity and deserves further development. Additionally, the homology model of the CYP51 enzyme that belongs to Fusarium moniliforme was generated using CYP51B (PDB ID: 6CR2), and molecular docking was performed using this homology model for each compound. The results of this study clearly indicate that these novel compounds can be identified as promising lead compounds and potential fungicidal agents in future.
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- 2020
46. In vitro antifungal activity of cistus creticus l. against plant pathogenic fungi
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Ayşegül Çaşkurlu, Fatma Tosun, Yavuz Bülent Köse, and Ayşe Esra Karadağ
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Antifungal ,biology ,medicine.drug_class ,fungi ,food and beverages ,Cistus Creticus L ,Plant Pathogenic Fungi ,General Medicine ,Cistaceae ,biology.organism_classification ,In vitro ,Cistus creticus ,Botany ,medicine - Abstract
Cistus creticus L. is a well-known member of the Cistaceae family. In this present study, methanol extract of aerial parts of C. creticus was evaluated for its antifungal activity against plant pathogenic fungi such as Fusarium moniliforme NRRL 2374, Fusarium culmorum NRRL 3288, Alternaria alternata ATCC 6663, and Botry-tis cinerea AHU 9424, respectively. The in vitro antifungal activity of C. creticus extract was determined by calculating mycelial growth inhibition. It was demonstrated that methanol extract of C. creticus has shown antifungal activity on F. mon-iliforme (36,7%) and B. cinerea (30,2%). Moreover, we are planning to evaluate the active fractions which are responsible for the antifungal activity in further studies.
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- 2020
47. In vitro antimicrobial and antioxidant activity evaluation of melampyrum arvense l. var. elatius boiss. and sedum spurium m. bieb. extracts
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Ayşe Esra Karadağ, Fatma Tosun, and Eczacılık Fakültesi
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Sedum Spurium ,Antioxidant ,biology ,medicine.medical_treatment ,Mycobacteria ,Melampyrum Arvense ,General Medicine ,Antimicrobial ,biology.organism_classification ,In vitro ,Antibacterial ,Sedum spurium ,Botany ,medicine ,Melampyrum arvense - Abstract
Sedum spurium M. Bieb. (Crassulaceae) is a common ornamental plant, whereas, Melampyrum arvense L. var. elatius Boiss. (Orobanchaceae) is a semi-parasitic plant and grows naturally in the fields. In this study, the dichloromethane and ethyl acetate extracts of M. arvense and S. spurium were evaluated for their in vitro antioxidant and antimicrobial activities. The antioxidant activity was evaluated by DPPH•-ABTS• methods. The antimicrobial activity of S. spurium and M. arvense extracts was determined using the in vitro broth microdilution assay against following human pathogenic strains; Staphylococcus aureus ATCC 6538, Enterococcus faecalis ATCC 29212, Escherichia coli NRLL B-3008, Helicobacter pylori ATCC 43504, Mycobacterium smegmatis ATCC 25291, Mycobacterium avium ssp. avium and Pseudomonas aeruginosa ATCC 10145. The extracts showed weak antimicrobial activity against Gram-negative/positive bacteria, having the MIC values of 500-1000 μg/mL. Antibacterial activity was not observed against Mycobacteria at 2000 µg/mL. In addition, antioxidant activity of M. arvense ethyl acetate extract was higher than those of the other extracts.
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- 2019
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