Search

Background: Romdoul (Sphaerocoryne affinis) is a flowering plant of the Annonaceae family and has been used customarily in folk medicine. The bioactivities of this plant, especially the anti-cancer effect, however, remain surprisingly few. Objective: this study aimed to elucidate the anti-leukemic effect of romdoul fruit extracts and their underlining mechanisms. Methods: The extracts were prepared from fresh fruits and the phytochemical contents were evaluated by biochemical assays and HPLC method. The promising extract was identified via the inhibition of HL60 as well as normal NIH-3T3 cell densities utilizing MTT assay. The underline mechanism of the extract's effect was studied by accessing the treated HL60 cell population overtime (via MTT assay). The morphology of abnormal cells was examined by bright-field microscopic imaging. Hallmarks of apoptosis including nucleus characteristics and caspase 3 activation were analyzed by fluorescence imaging. The underline mechanisms of apoptosis and proliferation inhibition were accessed via RT-qPCR examination of involved genes. Results: Our findings showed that the ethyl acetate extract of romdoul fruit (SA-EA) was found to be an exceptional anti-leukemic candidate (IC50 was as low as 4.11 μg/mL). More interestingly, the treated HL60 cells expressed nuclear fragmentation and caspase 3 activation, indicating the effect could follow an apoptotic mechanism. Importantly, the transcription assessment of apoptotic and proliferative genes suggested that SA-EA might suppress the growth of HL60 cells and induce p21-dependent apoptotic pathway. Conclusion: This study demonstrated one of the first scientific evidence for the anti-cancer activity of Sphaerocoryne affinis fruit-derived extract. Thus, our findings exhibited a novel and promising anti-leukemic candidate for future studies. [ABSTRACT FROM AUTHOR]

For a long time, fungi have been considered the richest source of bioactive metabolites with numerous applications. Hence, this study was performed to identify various bioactive compounds contained in the ethyl acetate extract of the fungus Aspergillus niger that isolates from infected garlic by using Gas Chromatography-Mass Spectrometry and their effect on seed germination of Zucchini. The current results showed a variety of bioactive compounds such as n-hexadecanoic acid, Hexadecanoic acid, Methyl stearate, Benzoic acid, Hexamethyl-1,3,5-trithiane, and cis-aconitic anhydride with an area percentage of 15.37, 13.93, 6.87, 5.67, 4.75 and 3.59% respectively. The results were performed using the fungus extract that protected the zucchini seed from pathogenic fungi (Botrytis cinerea, Fusarium oxysporum, and Rhizoctonia solani) when soaking for less than 72 h and promoted increased seed germination by high percentage ratio of seeding (66.67%, 80.00%, and 80.00%) respectively, radical length (66.67, 80.00 and 7.67), plumule length (4.67, 7.67 and 6.00) and Number of secondary roots (7.00,8.00 and 7.00) respectively compared with control treatment.

Inflammation and collagen-degrading enzymes’ overexpression promote collagen decomposition, which affects the structural integrity of the extracellular matrix. The polysaccharide and peptide extracts of the green alga Caulerpa microphysa (C. microphysa) have been proven to have anti-inflammatory, wound healing, and antioxidant effects in vivo and in vitro. However, the biological properties of the non-water-soluble components of C. microphysa are still unknown. In the present study, we demonstrated the higher effective anti-inflammatory functions of C. microphysa ethyl acetate (EA) extract than water extract up to 16–30% in LPS-induced HaCaT cells, including reducing the production of interleukin (IL)-1β, IL-6, IL-8, and tumor necrosis factor-α (TNF-α). Furthermore, the excellent collagen homeostasis effects from C. microphysa were proven by suppressing the matrix metalloproteinase-1 (MMP-1) secretion, enhancing type 1 procollagen and collagen expressions dose-dependently in WS1 cells. Moreover, using UHPLC-QTOF-MS analysis, four terpenoids, siphonaxanthin, caulerpenyne, caulerpal A, and caulerpal B, were identified and may be involved in the superior collagen homeostasis and anti-inflammatory effects of the C. microphysa EA extract.

(1) Background: Due to the wide application in medicinal and pharmaceutical chemistry of flavonoid molecules, which are one of the most famous types of secondary plant metabolites, our work has come within the framework of bio-consulting to help in the identification of the molecule(s) responsible for the antibacterial effect which will be the active principle of a natural antibiotic developed from Algerian fir using bioinformatics tools. (2) Methods: The docking method was used to test the antiviral activity on SARS-CoV-2 virus and the antibacterial activity on Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli of 12 polyphenolic molecules present in the ethyl acetate and n-butanol extracts of Numidian fir leaves, and identify the molecules responsible for these specific biological activities. (3) Results: The findings revealed that it is possible that two molecules, hyperoside and quercitrin, have a high capacity to inhibit SARS-CoV-2, and it is important to mention that they are the most quantitatively abundant molecules in the extract. The molecule luteolin-7-glucoside is probably responsible for the antibacterial activity in the extract against Gram-negative bacteria such as Escherichia coli, and the molecule hesperidin is responsible for the antibacterial activity in the extract against Gram-positive bacteria such as Staphylococcus aureus. [ABSTRACT FROM AUTHOR]

Background: Plantago major, historically renowned for its medicinal attributes across diverse cultures, has recently been under the research spotlight for its antihypertrophic scar effects. Aim: To investigate the efficacy of Plantago major extracts in the treatment of hypertrophic scars, particularly comparing the effects of methanol and ethyl acetate extracts. Methodology: Samples of the plant, procured from Baghdad's Al-Salihiya Neighbourhood in November 2021, underwent authentication at the Iraqi local Herbarium in the Al-Razi centre for alternative medicine. Using the Soxhlet apparatus, the dried plant material was extracted with methanol and subsequently partitioned with ethyl acetate. Both the ethyl acetate and methanol extracts were later formulated into ointments. Results: The ointments were tested on hypertrophic scars induced in rats. Three groups of 12 rats each were used—ethyl acetate, methanol, and a control group using only Vaseline. Both extracts demonstrated efficacy in reducing scars, with the methanol extract showing more pronounced results. Conclusion: The methanol extract displayed superior outcomes, potentially attributable to its richer phytochemical content compared to the ethyl acetate extract.

Introduction: Pulmonary fibrosis is a terminal lung disease characterized by fibroblast proliferation, extracellular matrix accumulation, inflammatory damage, and tissue structure destruction. The pathogenesis of this disease, particularly idiopathic pulmonary fibrosis (IPF), remains unknown. Macrophages play major roles in organ fibrosis diseases, including pulmonary fibrosis. The phenotype and polarization of macrophages are closely associated with pulmonary fibrosis. A new direction in research on anti-pulmonary fibrosis is focused on developing drugs that maintain the stability of the pulmonary microenvironment. Methods: We obtained gene sequencing data and clinical information for patients with IPF from the GEO datasets GSE110147, GSE15197, GSE24988, GSE31934, GSE32537, GSE35145, GSE53845, GSE49072, GSE70864, and GSE90010. We performed GO, KEGG enrichment analysis and GSEA analysis, and conducted weighted gene co-expression network analysis. In addition, we performed proteomic analysis of mouse lung tissue. To verify the results of bioinformatics analysis and proteomic analysis, mice were induced by intratracheal instillation of bleomycin (BLM), and gavaged for 14 days after modeling. Respiratory function of mice in different groups was measured. Lung tissues were retained for histopathological examination, Western Blot and real-time quantitative PCR, etc. In addition, lipopolysaccharide, interferon-g and interleukin-4 were used to induce RAW264.7 cells for 12h in vitro to establish macrophage inflammation and polarization model. At the same time, HG2 intervention was given. The phenotype transformation and cytokine secretion of macrophages were investigated by Western Blot, RT-qPCR and flow cytometry, etc. Results: Through bioinformatics analysis and experiments involving bleomycininduced pulmonary fibrosis in mice, we confirmed the importance of macrophage polarization in IPF. The analysis revealed that macrophage polarization in IPF involves a change in the phenotypic spectrum. Furthermore, experiments demonstrated high expression of M2-type macrophage-associated biomarkers and inducible nitric oxide synthase, thus indicating an imbalance in M1/M2 polarization of pulmonary macrophages in mice with pulmonary fibrosis. Discussion: Our investigation revealed that the ethyl acetate extract (HG2) obtained from the roots of Prismatomeris connata Y. Z. Ruan exhibits therapeutic efficacy against bleomycin-induced pulmonary fibrosis. HG2 modulates macrophage polarization, alterations in the TGF-β/Smad pathway, and downstream protein expression in the context of pulmonary fibrosis. On the basis of our findings, we believe that HG2 has potential as a novel traditional Chinese medicine component for treating pulmonary fibrosis. [ABSTRACT FROM AUTHOR]

Dandang Gendis (Clinachantus nutans L.) is a plant commonly used in traditional medicine. Based on the empirical experience of people, dandang gendis leaves are believed to possess antidiabetic and antibacterial properties. This study aimed to determine the LD50 value to assess the toxicity level of the extract and the resulting toxic effects of dandang gendis leaves. The Thompson-Weil calculation method was employed in this study, utilising 25 mice divided into 5 groups of 5 mice each. Group one served as a control (Na-CMC 1%), while the other four groups were treated with graded concentrations of 2.5% w/v, 5% w/v, 10% w/v, and 20% w/v of the extract. The extract was orally administered only once at the beginning of the study period. After administration, the mice were observed at specific intervals: 0, 0.5, 1, 2, 3, 4, 12, and 24 hours. Subsequent observations were made after 24 hours, and the mice were monitored for delayed toxic effects over 14 days. From acute toxicity testing of the ethyl acetate extract of dandang gendis leaves, the LD50 value was 6.15 g/kg BW, showing the extract is not toxic at this oral dose in mice. Further research may be necessary to fully understand the potential health benefits and risks associated with dandang gendis, particularly as an antidiabetic agent. [ABSTRACT FROM AUTHOR]

Background: Cynomorium songaricum Rupr. has long been used as an anti-inflammatory, antidepressant, and anti-aging agent in traditional Chinese medicine in Asia. Its ethyl acetate extract (ECS) has been identified as the main antioxidant component with neuroprotective and estrogen-like effects. However, the potential of ECS in treating depression has not been explored yet. Methods: We identified the primary metabolites in ECS in this study using liquid chromatography-electrospray tandem mass spectrometry (LC-MS/MS). Network analysis was used to find the potential targets and pathways associated with the anti-neuroinflammatory depression action of the ECS. In addition, we established a corticosterone (CORT)-induced depression mouse model to assess ECS's antidepressant effects by monitoring various behavioral changes (e.g., sucrose preference, forced swimming, tail suspension, and open field tests) and biochemical indices of the hippocampus, and validating the network analysis results. Significant pathways underwent verification through western blotting based on network analysis prediction. Results: Our study demonstrates that ECS possesses significant antidepressant activity. The LC-MS/MS analysis of ECS identified 30 main metabolites, including phloridzin, phlorizin, ursolic acid, and naringenin, as well as other flavonoids, terpenoids, and phenolic acids. These metabolites were found to be associated with 64 candidate target proteins related to neuroinflammatory depression from the database, and ten hub proteins were identified through filtration: CXCL8, ICAM1, NOS2, SELP, TNF, IL6, APP, ACHE, MAOA and ADA. Functional enrichment analyses of the candidate targets revealed their primary roles in regulating cytokine production, inflammatory response, cytokine activity, and tumor necrosis factor receptor binding. In vivo, ECS improved hippocampal neuroinflammation in the mouse model. Specifically, ECS reduced the expression of inflammatory factors in the hippocampus, inhibited M1 microglial cell polarization, and alleviated depression through the regulation of the NF-κB-NLRP3 inflammation pathway. Conclusion: Based on experimental and network analysis, this study revealed for the first time that ECS exerted antidepression effect via anti-neuroinflammation. Our research provides valuable information on the use of ECS as an alternative therapeutic approach for depression. [ABSTRACT FROM AUTHOR]

The role of oxidants and proinflammatory cytokines in the pathogenesis of pneumonia caused by Staphylococcus aureus (S. aureus) has been demonstrated. The present study aims to investigate the protective effect of ethyl acetate extract (EtOAc) obtained from Usnea longissima (UL) against acute oxidative and inflammatory lung damage due to S. aureus infection in rats. Albino Wistar-type male rats were divided into three groups: Healthy (HG), S. aureus inoculated (SaG), and S. aureus inoculated + ULEtOAc administered (SUL). SaG (n = 6) and SUL (n = 6) group rats' left nostrils (excluding HG) were inoculated with 0.1 ml bacterial mixture. After 24 hours, ULEtOAc (50 mg/kg) was administered orally to the SUL group, and the same volume of normal saline was administered orally to the HG (n = 6) and SaG groups. This procedure was performed once a day for seven days. Levels of oxidant and antioxidant parameters such as malondialdehyde (MDA) and total glutathione (tGSH), as well as pro-inflammatory cytokine levels such as nuclear factor-kappa B (NF-kB), tumor necrosis factor- alpha (TNF-α), interleukin-one beta (IL-1p), were measured in removed lung tissues. Tissues were also examined histopathologically. Biochemical results showed that ULEtOAc significantly suppressed the increase of MDA, NF-kB, TNF-α, and IL-1p levels and the decrease of tGSH caused by S. aureus in lung tissue. S. aureus inoculation caused severe mononuclear cell infiltration in interstitial areas, severe lymphoid hyperplasia in bronchial-associated lymphoid tissue and severe alveolar edema, histopathologically. Treatment with ULEtOAc had an attenuating effect on these histopathological findings. Experimental results from this study suggest that ULEtOAc may be beneficial in treating S. aureus-induced oxidative and inflammatory lung damage. [ABSTRACT FROM AUTHOR]

This study aimed to explore the antibacterial and larvicidal potential of actinobacterial strains isolated from soil samples of Pakistan. Out of fourteen purified actinobacteria, antibiotic susceptibility profile confirmed five isolates showing resistance against tested antibiotics (ampicillin; lincomycin; rifampicin and erythromycin). Ribotyping confirmed that these isolates belong to Streptomyces species and were identified as S. monticola, S. septentrionalis, S. polaris, S. desertarenae and S. lutosisoli. Primary screening of the five isolates using cross streak method showed excellent zone of inhibition (ZI 10-27 mm) against tested pathogens (Escherichia coli, Klebsiella pneumoniae, Bacillus licheniformis, Pseudomonas aeruginosa and Bacillus subtilis). Secondary screening using ethyl acetate extracts also showed significant ZI in the range of 06 - 14.0 mm (P ≤ 0.05) against these pathogens thus confirming their bioactive potential. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of screened Actinomycetes was in the range of 1.3 - 3.5 mgmL-1 and 1.9 - 4.0 mgmL-1 of bacterial biomass, respectively. Three isolates, S. monticola, S. septentrionalis and S. polaris showed 100 % mortality at 1000 ppm against Anopheles 3rd instar larvae. These findings indicated that actinobacterial isolates possess antibacterial and larvicidal potential. Further extraction and purification of bioactive components from these bacterial may be a good source of novel antibiotics and natural-insecticides. [ABSTRACT FROM AUTHOR]

A study was focused on biocidal and repellent efficiencies of leaf extracts of Chromolaena odorata (L) (Asteraceae), Gliricidia sepium (Jacq.) (Fabaceae), Coleus aromaticus Benth, Hyptis suaveolens (L.)Poit. (Lamiaceae) and Artemisia vulgaris L. (Asteraceae), against Odoiporus longicollis, banana pseudostem weevil. Ethanol leaf extracts of the above plants were primarily analysed for the mortality and repellency activity, the results showed that among the extracts G. sepium was most effective. Further G. sepium in various solvents like petroleum ether, chloroform, ethyl acetate, ethanol and water were analysed for the biocidal and repellency assays, and found that, the ethyl acetate solvent of G. sepium elicited maximum effectiveness. The ethyl acetate extract of G. sepium is found as a promising biopesticide. [ABSTRACT FROM AUTHOR]

(1) Background: Due to the wide application in medicinal and pharmaceutical chemistry of flavonoid molecules, which are one of the most famous types of secondary plant metabolites, our work has come within the framework of bio-consulting to help in the identification of the molecule(s) responsible for the antibacterial effect which will be the active principle of a natural antibiotic developed from Algerian fir using bioinformatics tools. (2) Methods: The docking method was used to test the antiviral activity on SARS-CoV-2 virus and the antibacterial activity on Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli of 12 polyphenolic molecules present in the ethyl acetate and n-butanol extracts of Numidian fir leaves, and identify the molecules responsible for these specific biological activities. (3) Results: The findings revealed that it is possible that two molecules, hyperoside and quercitrin, have a high capacity to inhibit SARS-CoV-2, and it is important to mention that they are the most quantitatively abundant molecules in the extract. The molecule luteolin-7-glucoside is probably responsible for the antibacterial activity in the extract against Gram-negative bacteria such as Escherichia coli, and the molecule hesperidin is responsible for the antibacterial activity in the extract against Gram-positive bacteria such as Staphylococcus aureus.

Date palm (Phoenix dactylifera L.) fruits contain high concentrations of phenolic compounds, particularly flavonoids and other micronutrients, which impact human health due to their potent antioxidant, anti-inflammatory, and anticancer characteristics. In the present study, the effect of ethyl acetate, hydroethanol, hydromethanol, and aqueous extract from three date palm varieties (i.e., Ajwa, Siwi, and Sukkari) on phytochemical profiles and antioxidant and anticancer activities was investigated. Fruit extracts were screened for their antioxidant activity using the DPPH· method. Phenolic constituents were quantified and identified using HPLC-DAD. Extracts (ethyl acetate, hydroethanol, and hydromethanol) were assessed for cytotoxicity on nine human cancer cell lines, i.e., MG-63, HCT116, MCF7, MDA-MB-231, HEPG2, HUH7, A549, H460, and HFB4, using the sulphorhodamine-B (SRB) assay. Results showed that the ethyl acetate extract of the Sukkari fruits has the greatest antioxidant potential with an IC50 value of 132.4 ± 0.3 μg·mL−1, while the aqueous extract of Ajwa date fruits exhibited the lowest antioxidant effect with an IC50 value of 867.1 ± 0.3 μg·mL−1. The extracts exhibited potent to moderate anticancer activities against the investigated cancer cell line in a source-dependent manner. Methanol extract of Siwi fruits exhibited the most potent anticancer activity (IC50 = 99 ± 1.6 µg·mL−1), followed by the same extract of Sukkari fruits with an IC50 value of 119 ± 3.5 µg·mL−1 against the cell line of human breast cancer (MDA-MB-231). Additionally, principal component analysis (PCA) was investigated to determine the relationship among the investigated traits and treatments. Our findings reveal that date palm fruit-derived extracts are excellent sources of biologically active constituents and substantiate their potential use in new anticancer strategies from natural resources. [ABSTRACT FROM AUTHOR]

Diarrhea is a symptom experienced by nearly everyone, generally considered an increase in the volume, fluidity, and/or frequency of stools. Chronic diarrhea may affect ~5% of people in industrialized countries, and acute or chronic infectious diarrhea remains an important cause of morbidity in developing countries. The Crassulaceae family of plants includes the Bryophyllum pinnatum (Lam.) Oken plant, which is well renowned for its therapeutic properties. The main aim of the research is to assess the antidiarrheal property using Mgso4 induced diarrheal model and isolate an active compound. Both EAE and EE exhibited consistent effects. The Percentage of Inhibition of T1 (EE 200 mg/kg), T2 (EE 400 mg/kg), T3 (EAE 200 mg/kg) and T4 (EAE 400mg/kg) groups was found 41.51%, 61.32%, 32.56% and 52.78% respectively with standard Loperamide drug (at 3 mg/kg dose, p.o.). T2 (EE 400mg/kg) showed better outcomes because of isolated flavonoid substance, 4, 5, 7-trihydroxy flavones as a yellow pigment from ethanol-DCM, with the aid of analysis using UV, IR, NMR and mass spectroscopy, the substance, was characterized and identified as 4, 5, 7-trihydroxy flavones, with the chemical formula C15H10O5 from EE extract of Bryophyllum pinnatum (Lam.) Oken plant leaves. Finally, it can be concluded that flavonoids are responsible for the antidiarrheal activity and this may be used to determine the precise function of herbal medicine in contemporary society. [ABSTRACT FROM AUTHOR]

Corydalis saxicola which belongs to the family of Papaveraceae, is always used to treat various diseases such as hepatitis B, cirrhosis, furuncle, acute icteric hepatitis, and advanced cancer as traditional Zhuang medicine in Guangxi province. To study the anti-inflammatory activity of the chemical constituents of C. saxicola, silica gel, MCI, Sephadex LH-20 column chromatography and preparative high performance liquid chromatography were used to separate the chemical constituents from the ethyl acetate fraction of 95% ethanol extract of C. saxicola. Their structures were identified by nuclear magnetic resonance (NMR) and high resolution mass spectrum (HR-MS). In addition, the anti-inflammatory activity was evaluated by the mouse macrophage RAW264.7 induced by lipopolysaccharide (LPS). The results showed that 13 chemical compounds were isolated and identified as coptisine (1), berberine hydrochloride (2), crinumaquine (3), worenine (4), dehydrocavidine (5), (-)-tetrahydropalmatine (6), jatrorrhizine (7), corydaldine (8), N-trans-feruloyl tyramine (9), dibutylterephthalate (10), kaempferol (11), isololiolide (12), loliolide (13) respectively. Compounds 3, 4,8-13 were isolated from this plant for the first time. Compounds 4, 9 and 11 showed good inhibitory effects on LPS induced NO production by macrophage RAW264.7 with IC50 values of (18.8 ± 0.2), (29.1 ± 0.3), (18.0 ± 0.1) μmol·L-1 respectively, which was better than the positive control indomethacin, exhibited good potential in the research and development of anti-inflammatory drugs. These results can clarify the anti-inflammatory material basis of C. saxicola, and provide a scientific theoretical basis for its further utilization.

Context: Among the Tujia people, the root or rhizome of Trillium tschonoskii Maxim.in Bull.Acad (TTM) is considered a miraculous herb for headaches. Previous studies have shown ethyl acetate extract (TTM1) can protect SH-SY5Y cells against glutamate injury. Objective: This study clarified TTM1's mechanism against glutamate-induced cell damage, focusing on the regulation of apoptosis. The compounds were separated, identified, and performed molecular docking with pro-apoptotic proteins. Materials and Methods: SH-SY5Y cells were treated with glutamate (2 mM) for 12 hour, and the effect of TTM1 (2.5, 5, 10, and 20 μg/mL) was evaluated with MTT and LDH release assays, taking EGb761(40 μg/mL) as a control. Cell apoptosis was detected with Hoechst 33258 and Annexin V-FITC and measurements of intracellular calcium and caspase-3. The major components were separated and identified by LCMS-IT-TOF and NMR, then the proapoptotic activity of TTM1 was confirmed by molecular docking method. Results: TTM1 protected SH-SY5Y cells by resisting apoptosis, TTM1 (10 and 20 μg/mL) decreased apoptotic bodies and nuclear fragments, increased the proportion of normal cells to 68.38 ± 5.63% and 92.80 ±.88%, decreased VA cells to 4.30 ±.76% and 3.58 ±.45% and caspase-3 to.365 ±.034 and.344 ±.047 ng/mL.TTM1 (10 μg/mL) decreased intracellular free calcium to 2.77 ±.40. Polyphyllin VI and pennogenin 3-O-β-chacotrioside were identified in TTM1 at 15.04% and 2.84%, and had potential anti-apoptosis activities. Discussion and Conclusions: Folk records of TTM for headache may be related to its anti-apoptosis of nerve cells. Identification and content determination of index components based on effective extract provides research paradigms for rare and endangered ethnic plants. [ABSTRACT FROM AUTHOR]

Ovarian cancer is a common gynecological malignant tumor. The traditional treatment method is mainly surgery and chemotherapy, but the problems of recurrence and drug resistance need to be solved urgently. The application of traditional Chinese medicine in the tumor treatment is increasingly extensive, the ethyl acetate parts in many kinds of traditional Chinese medicine have anti-tumor effect. As a kind of medicinal insect, the blaps rynchopetera fairmaire has the antibacterial and antioxidant effects, and there are many folk prescriptions for anti-tumor treatment. The ethyl acetate extract of blaps rynchopetera fairmaire, as the most abundant part containing phenols, can significantly inhibit the growth of ovarian cancer cells by scavenging DPPH free radicals and regulating STAT3/VEGF signaling pathway. At the same time, by down-regulating the expression of β-catenin, CyclinD1 protein, blocking Wnt signaling pathway, affecting the cell cycle, so as to inhibit the proliferation of cancer cells and anti-tumor properties. Based on the existing research results, the effects of ethyl acetate extract of blaps rynchopetera fairmaire on ovarian cancer are reviewed, and hope to develop the new medicinal insect resources and provide the new ideas for the treatment of ovarian cancer. [ABSTRACT FROM AUTHOR]

• Cymodocea serrulata was used as sample of interest for biological applications. • Extraction was performed using hexane, ethyl acetate, chloroform, diethyl ether, methanol, acetone solvents. • Ethyl acetate extract of C. serrulata (CSEA) showed significant larvicidal activity than other extracts. • Mosquito larvae, zebrafish embryo and brine shrimp larvae toxic results received considerable attention from CSEA extract. Of late, the advent of bioactive drug candidates from marine resources, particularly marine plants, has received more attention. Owing to the increased resistance in mosquitoes, the prevalence of deadly diseases is becoming tougher to treat. The purpose of this study was to determine the toxicity for Artemia salina and insecticide potential of the ethyl acetate (EA) extract of the seagrass Cymodocea serrulata (CS) against Anopheles, Aedes and Culex mosquitoes. The seagrass extract showed the highest mortality rate against Anopheles stephensi with LC50 and LC90 values of 10.663 and 117.01, respectively, followed by Aedes aegypti 12.190 and 170.523, and Culex quinquefasciatus 14.322 and 326.431 μg/mL. Larvae treated with C. serrulata ethyl acetate extract (CSEA) showed histological changes such as epithelial, muscular and adipose tissue. Biosafety assessments with CSEA extract on Danio rerio embryos and Artemia salina nauplii were found to be safe. The functional groups such as carboxylic acids, alkanes, alkynes, amides, phenolic and aromatic compounds from CSEA extract were identified by FTIR spectra. HPLC showed a strong peak at 2.518, and later eight compounds were identified by GCMS analysis. Among them, octadecadienoic acid is the main compound with 41.65%. In this experiment, we concluded that the seagrass C. serrulata has high mosquito larval control properties and negligible toxicity to non-target organisms. Therefore, this potential seagrass due to its extensive properties, can be expanded for the development of environmentally friendly pesticides against dengue, malaria, and filariasis vectors. [ABSTRACT FROM AUTHOR]

The emergence of drugs from marine sources, particularly marine plants, has increased in recent years. Hence, the purpose of this study was to assess, evaluate the phytochemical profile, antibacterial, and antioxidant activity of Cymodocea serrulata extract. Furthermore, qualitatively analyzed the predominant components present in the extract which showed considerable antibacterial and antioxidant activities. The qualitative phytochemical analysis results revealed that the ethyl acetate extract contained more number of pharmaceutically valuable phytochemicals than other solvent extracts. The ethyl acetate extract showed excellent antibacterial activity against S. aureus (20 mm) followed by P. aeruginosa (18.11 mm), E. coli (17.20 mm) , B. subtilis (17.11 mm) , C. diphtheriae (17.10 mm) and C. pneumoniae (17.0 mm) at the concentration of 75 mg ml−1. The antioxidant activity results revealed that the crude ethyl acetate extract of C. serrulata demonstrated significant free radicals scavenging activity ranging from 25.562 ± 1.62 %, 63.615 ± 1.02 %, 75.524 ± 0.48 %, and 88.048 ± 1.28 % for DPPH, FRAP, H 2 O 2 , and nitric oxide radicals scavenging assays at the concentration of 100 mg ml−1 respectively. Furthermore, the GC-MS analysis results revealed that the ethyl acetate extract contained 14 major components, the majority of which had previously been identified as pharmaceutically valuable components. These findings concluded that the components present in the ethyl acetate extract of C. serrulate have pharmaceutical value and may be useful to the humanity. [Display omitted] • C. serrulata ethyl acetate extract possess fine antibacterial activity. • The crude ethyl acetate extract contained more numbers of phytochemicals. • S. aureus is extremely sensitive to ethyl acetate extract at 75 mg ml−1 concentration. • The ethyl acetate extract showed significant free radicals scavenging activities. • GC-MS analysis revealed that the ethyl acetate extract contains 14 major components. [ABSTRACT FROM AUTHOR]

Corydalis saxicola which belongs to the family of Papaveraceae, is always used to treat various diseases such as hepatitis B, cirrhosis, furuncle, acute icteric hepatitis, and advanced cancer as traditional Zhuang medicine in Guangxi province. To study the anti-inflammatory activity of the chemical constituents of C. saxicola, silica gel, MCI, Sephadex LH-20 column chromatography and preparative high performance liquid chromatography were used to separate the chemical constituents from the ethyl acetate fraction of 95% ethanol extract of C. saxicola. Their structures were identified by nuclear magnetic resonance (NMR) and high resolution mass spectrum (HR-MS) . In addition, the anti-inflammatory activity was evaluated by the mouse macrophage RAW264.7 induced by lipopolysaccharide (LPS) . The results showed that 13 chemical compounds were isolated and identified as coptisine (1), berberine hydrochloride (2), crinumaquine (3), worenine (4), dehydrocavidine (5), (-) -tetrahydropalmatine (6), jatrorrhizine (7), corydaldine (8), N-trans-feruloyl tyramine (9), dibutylterephthalate (10), kaempferol (11), isololiolide (12), loliolide (13) respectively. Compounds 3, 4, 8-13 were isolated from this plant for the first time. Compounds 4, 9 and 11 showed good inhibitory effects on LPS induced NO production by macrophage RAW264.7 with IC50 values of (18.8 ± 0.2), (29.1 ± 0.3), (18.0 ± 0.1) μmol·L-1 respectively, which was better than the positive control indomethacin, exhibited good potential in the research and development of anti-inflammatory drugs. These results can clarify the anti-inflammatory material basis of C. saxicola, and provide a scientific theoretical basis for its further utilization. [ABSTRACT FROM AUTHOR]

The medicinal plant Aaronsohnia pubescens is currently used in the algerian phytotherapy to treat several disorders. In order to investigate the potential influence of A. pubescens, six extracts were screened for their antioxidant and anti-amylase capacities. Antioxidant ability was evaluated by different assays as well as scavenging effect of free radicals (DPPH, ABTS, GOR and hydroxyl radical), metal chelating, reducing power, CUPRAC and total antioxidant capacity. Total phenolic and flavonoid contents in these extracts were also measured. Phenolic compounds in different extracts were identified using the HPLC-DAD analysis. The total phenolic contents of these extracts ranged from 70 to 335.9 mg GAE/g. Generally, the highest amounts of total phenolic and flavonoid contents were observed in ethyl acetate and n-butanol extracts, which may explain their strong antioxidant activity. All extracts demonstrated a significant inhibitory activity on a-amylase. Based on these findings, A. pubescens could serve as a source of natural compounds for oxidative damage and diabetes mellitus management. [ABSTRACT FROM AUTHOR]

Vernonia amygdalina was reported to be used as a therapy for Diabetes Mellitus (DM). One of the mechanisms of therapy DM was to inhibit the action of the α-amylase enzyme. This study aimed to prove the presence of compounds that could inhibit the action of α-amylase. Vernonia amygdalina leaves were macerated with methanol and partitioned into n-hexane, dichloromethane (DCM), and ethyl acetate (EtOAc). Furthermore, they were tested for α-amylase inhibitory activity and analyzed using liquid chromatography-high resolutions mass spectrometry (LC-HRMS). Molecular docking and molecular dynamics simulation (MD simulation) examined unique compounds in the extract with good activity and chromatogram results. The EtOAc extracts showed potential as α-amylase inhibitors indicated by their IC50 values, namely 3.0 μg/mL. There are five unique compounds in the EtOAc extract predicted as 3-[(2Z)-3,7-dimethylocta-2,6-dien-1-yl]-2,4-dihydroxy-6-(2-phenylethyl)benzoic acid (compound 1), 2-hexylpentanedioic acid (compound 2), (2E,4E)-5-[1-hydroxy-2,6-dimethyl-4-oxo-6-({3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl] oxy}methyl)cyclohex-2-en-1-yl]-3-methylpenta-2,4-dienoic acid (compound 3), 3,5,5-trimethyl-4-(3-{[3,4,5-trihydroxy-6-(hydroxymethyl)oxan-1-yl)oxy}butyl)cyclohex-2-en-1-one (compound 4), and 2-{[(6E)-2,10-dihydroxy-2,6,10-trimethyldodeca-6,11-dien-3-yl]oxy}-6-(hydroxymethyl)oxane-3, 4,5-triol (compound 5). The molecular docking analysis showed that compound 3 had better interaction energy (Ei) (-8.59 kcal/mol) and inhibition constant (Ki) values (0.503 μM) than acarbose. These data were supported by MD simulations based on the parameters of RMSD value, the radius of gyration, and protein-ligand interaction energy.

Osteosarcoma weakens the bone by destroying tissue. It originates from immature bone cells, which typically give rise to new bone tissue. Medicinal herbs are a potential source for an extensive range of phytochemicals with anticipated anticancer activity. The present study was to form an impression of the medicinal herb Vachellia nilotica leaves extract and its fractions as a cancer therapeutic agent against Osteosarcoma cell lines (MG 63). This study used the MTT assay, DPPH, Cell cycle analysis, and Alizarin red S dye to investigate the effects of crude ethyl acetate extract and its fractions on viability, antioxidant capacity, and mineralization, respectively. To determine the pharmacokinetic properties of the discovered substances and assess their potential toxicity, computer-assisted analysis was performed. The investigation reveals that fraction 1E considerably lowers the percentage viability of human osteosarcoma MG 63. The effect was shown in the dose and time-dependent manner. Furthermore, fraction 1E exhibited the highest radical scavenging activity and showed the least mineralizing activity after the treatment. Positive pharmacokinetic properties of the phytochemicals were observed, making them an excellent starting point for the development of drugs. Thus, the present study highlighted the potency of the V.nilotica ethyl acetate extract and its bioactive fractions against Osteosarcoma and their role in the cell cycle. The study also concludes the In-silico targeted proteins about the disease, which is the first time reported as per our knowledge and the literature available. [Display omitted] [ABSTRACT FROM AUTHOR]

Abstract Background Sedum emarginatum Migo(S. emarginatum) has anti-tumor and anti-oxidant effects. This study aimed to screen the extractions of S. emarginatum against liver cancer in vitro and explore its anti-liver cancer mechanism. Methods The CCK-8(Cell Counting Kit-8) method was used to detect the inhibitory effect of different extracts of S. emarginatum on the proliferation of liver cancer HepG2 cells. The morphological changes of the cells after administration were observed with microscopy, cell apoptosis was detected by flow cytometry, and the expression of Bax, Bcl-2 and Caspase-3 mRNA in the cells were detected by RT-PCR (Reverse Transcription-Polymerase Chain Reaction) to explore the mechanism of action. Results CCK-8 method test results showed that among the different extracts of S. emarginatum, the ethyl acetate extract(1000 μg/ml, 2000 μg/ml, 2500 μg/ml, 3000 μg/ml) and n-butanol extract(1000 μg/ml, 2000 μg/ml, 2500 μg/ml, 3000 μg/ml) have the strongest inhibitory effect on the proliferation of HepG2 cells. In these 4 concentrations, the inhibitory effect increased as the concentration increased. The IC50 of the ethyl acetate extract on HepG2 cells was less than that of the n-butanol extract, so the ethyl acetate extract has a better proliferation inhibitory effect on HepG2 cells than the n-butanol extract, followed by the 70% ethanol extract(3000 μg/ml) and the water extract(3000 μg/ml), petroleum ether extract was the weakest. The results of microscopy showed that ethyl acetate extract caused hepatocarcinoma HepG2 cell morphology changed, cell density decreased, and suspension cells increased. Moreover, the results of flow cytometry showed that the ethyl acetate extract of S. emarginatum could induce HepG2 cell apoptosis at the concentrations of 2500μg/ml and 3000μg/ml. RT-PCR results showed that the expression of Bax mRNA was up-regulate by the middle(2500 μg/ml) and high(3000 μg/ml) dose groups of ethyl acetate extract. The expression of Caspase-3 mRNA was up-regulated by the low(2000 μg/ml), medium(2500 μg/ml) and high(3000 μg/ml) dose groups of ethyl acetate extract. The expression of Bcl-2 mRNA was down-regulated by the high(3000 μg/ml) dose group of ethyl acetate extract. Conclusion The ethyl acetate extract of S. emarginatum has the best effect on human liver cancer HepG2 cells. Its anti-hepatocellular mechanism may be related to affect the expression of apoptosis genes (Bax, Bcl-2 and Caspase-3mRNA) and promote the apoptosis of liver cancer cells. It provided a reference for the research and development of drugs for the treatment of liver cancer.

To study the allelopathic effect of the extracts of Landoltia punctata, the changes of cell density of Microcystis aeruginosa were measured. The anti-algae allelopathic effect of different organic solvent extracts of L. punctata was evaluated, and the physiological, biochemical indexes were determined to discuss the mechanism of algal inhibition. The results showed that the petroleum ether, dichloromethane and ethyl acetate extracts showed various inhibitory effects on M. aeruginosa. Among them, ethyl acetate extract was the most strongly allelopathic part with the semi-effect concentration(EC50) of 59.6 mg L−1, the central polarity part of inhibitory activity. The contents of chlorophyll a(Chl a) and phycobiliproteins(PBPs) of M. aeruginosa were decreased under the concentration of 200 mg L−1 ethyl acetate extract, which indicated that the photosynthesis of M. aeruginosa was inhibited. The consent of microcystins was lower compared to control under 200 mg L−1. The contents of superoxide dismutase(SOD), malondialdehyde(MDA) and hydrogen peroxide(H2O2) of cell pellets were firstly increased and then decreased, which suggested that the algal cells were seriously damaged by oxidation. The results indicated that the extracts of L. punctata had inhibitory effect on M. aeruginosa, and the ethyl acetate extract was the central part of the inhibitory substances, which affected photosynthesis and caused peroxidation damage to inhibit cell proliferation. These findings will be helpful for exploration and application of allelopathic effects of L. punctata in harmful algae control.

Finding a potential bioactive compound against a specific mosquito vector is an urgent requirement. Thus, this research was designed to separate the significant compounds present in the crude ethyl acetate extract of Cymodocea serrulata through Thin Layer Chromatography (TLC), Column Chromatography (CC), and High Performance Liquid Chromatography (HPLC). Furthermore, the larvicidal and pupicidal activity of different concentrations (100, 300, 500, 700, and 900 g mL−1) of separated fraction against 4th instar larvae of Culex quinquefasciatus in 24 h of treatment. Interestingly, 7 fractions were obtained from crude ethyl acetate extract by TLC. One fraction (7a) from out of 7 was further separated into fractions 7a and 7b through CC and preparative TLC. Furthermore, the HPLC analysis result revealed that the fraction-7a contained 2 major peaks and 25 minor peaks. The fraction 7a was selected based on the R f value and examined their larvicidal and pupicidal activity on 4th instar larvae and pupa of C. quinquefasciatus. Interestingly, the increased concentration (900 µg mL−1) of fraction-7a of ethyl acetate extracts of C. serrulata showed excellent larvicidal and pupicidal activities as 98.66 ± 1.88 % and 98 ± 5.65 %, respectively. These findings imply that the fraction 7a of C. serrulata ethyl acetate extract could be used as a mosquito vector control agent. [Display omitted] • Crude ethyl acetate extract of Cymodocea serrulata contain 7 major fractions • The fraction-7a contain 2 major and 25 minor peaks under HPLC analysis • Fraction-7a of ethyl acetate extract possess larvicidal activity as 98.66 % • C. serrulata ethyl acetate extract fraction-7a possess 98 % o pupicidal activity • Fraction-7a has fine larvicidal and pupicidal activity on C. quinquefasciatus [ABSTRACT FROM AUTHOR]

Saccharum officinarum is the main cash crop in sugar processing industry, and its leaves are characteristic Yao medicine in Guangxi with a long history. Our recent study showed that its ethyl acetate extract was partly responsible for its in vitro anti-tumor activity. In order to clarify the chemical constituents of this part, the modern separation and purification techniques, such as silica gel column chromatography, Sephadex LH-20 column chromatography, and semi-preparative high-performance liquid chromatography were used to identify the structures of the isolates by their physicochemical properties and modern spectral analysis. The results were as follows: Twenty compounds were all isolated and identified as 3, 4-dihydroxybenzaldehyde(1), methyl 3, 4-dihydroxy-benzoate(2), 3, 4-dihydroxy-benzoic acid(3), 3-hydroxy-4-methoxybenzoic acid(4), p-hydroxy-benzoic acid(5), p-hydroxybenzyl aldehyde(6), p-hydroxy-cinnamic acid(7), syringic acid(8), 3, 5-dihydroxy-hydroquinone(9),1-hydroxy-benzoyl-4-O-α-L-rhamnopyranoside(10), p-hydroxy-benzoyl-β-D-glucopyranoside(11), quercetin(12), tricin(13), tamarixetin(14),isorhamnetin(15), 5, 3', 4'-trihydroxy-7-methoxy-flavanone(16), 7-O-Methyleriodictyol(17), [(E)-4-(1S,3R,4R)-1-hydroxy-4,5,5-trimethyl-7-oxabicyclo [4.1.0]heptan-1-yl]but-1-en-3-o-ne(18), blumenol A(19)and thymidine(20), respectively. Compounds 1-4, 6, 9-11, 13-16, 18 and 20 were isolated and identified from this plant for the first time. The results provide some basis for its further development. [ABSTRACT FROM AUTHOR]

Bryophyllum pinnatum Lam. (Oken) (Crassulaceae) are commonly known as miracle plant. Traditionally, this plant is used to heal wounds and to treat diarrhoea. For this reason, the main aim of the present study is to evaluate the antidiarrheal activity using castor oil-induced diarrhea model. Loperamide drug (3 mg dose, p.o.) was used as standard drug. The EAE and EE at 200 mg dose and 400 mg dose, p.o. respectively produced dose-dependent protection of mice with significant P value (P<0.001). Both extracts of plant produced dose-dependent and significant P-value (P <0.001) towards antimotility effect compared with negative control (castor oil) group in model. EE (400 mg dose p.o.) possess better antidiarrheal potential in mice groups due to presence of flavone. 5-methyl-4,5,7-trihydroxy flavone was isolated from the ethanol extract. Finally, it can be concluded that, Bryophyllum pinnatum Lam. (Oken) leaves can be used ethnomedicinally to treat, counterbalance, bulwark, and control diarrhea. [ABSTRACT FROM AUTHOR]

The aim of this study was to determine the in vivo hypoglycaemic activity of ethyl acetate extract of Notonia grandiflora (EANG) in albino wistar rats. EANG was orally administrated to STZ (40 mg/kg, i.p, b.w) induced diabetic rats at the doses of 100 and 200 mg/kg b.w for 21 days. The effect of EANG on blood glucose, body weight, plasma insulin, urea, uric acid, creatinine, Hb, HbA1C, liver glycogen content, bilirubin level, liver enzymes (Serum glutamate pyruvate transaminases, serum glutamate oxaloacetate transaminases, alkaline phosphatase) were measured in the diabetic rats. Treatment of EANG significantly lowered the levels of blood glucose and glycosylated haemoglobin. It also restored body weight, liver glycogen content, and serum insulin level in diabetic rats in a dose-dependent manner. A significant reduction in the activity of liver function enzymes associated with diabetes and serum levels of renal parameters after treatment with EANG was observed, signifying the protective effects of EANG in diabetes-associated complications. Hence, it could be used as a safer complementary drug in the management of diabetes and associated complications. [ABSTRACT FROM AUTHOR]

Abstract Background Gastric cancer is one of the most leading causes of cancer death worldwide. Therefore, treatment studies have been being conducted, one of which is screening of novel agents from medicinal herbs. Elephantopus mollis Kunth (EM) belonging to Asteraceae family is a perennial herb with several therapeutic properties including anticancer activity. However, the effect of this species on gastric cancer has not been reported yet. In this study, cytotoxicity of different EM crude extracts was investigated on AGS gastric cancer cell line. Besides, the effects of extract on nuclear morphology, caspase-3 activation, and gene expression were also explored. Results The results showed that ethyl acetate extract exhibited a remarkably inhibitory ability (IC50 = 27.5 μg/ml) on the growth of AGS cells, while causing less toxicity to normal human fibroblasts. The extract also induced apoptotic deaths in AGS cells as evidenced by cell shrinkage, formation of apoptotic bodies, nuclear fragmentation, caspase-3 activation, and the upregulation of BAK and APAF-1 pro-apoptotic genes related to mitochondrial signaling pathway. Specifically, BAK and APAF-1 mRNA expression levels showed 2.57 and 2.71-fold increases respectively. Conclusions The current study not only proved the anti-gastric cancer activity of EM ethyl acetate extract but also proposed its molecular mechanism. The extract could be a potential candidate for further investigation.

Context: Vernonia amygdalina has been reported as a potential antidiabetic agent. One of the mechanisms in diabetes mellitus treatment is the inhibition of the α-amylase enzyme’s action. Objective: This study is aimed to identify the presence of secondary metabolites in Vernonia amygdalina leaf extract, which has the potential as α-amylase inhibitors through phytochemical screening combined with metabolomic analysis. Materials and methods: Methanol extract from Vernonia amygdalina leaf was partitioned into n-hexane, dichloromethane (DCM), and ethyl acetate. From this process, methanol, hexane, DCM, and ethyl acetate extracts were obtained. These extracts were then being tested for phytochemical screening, α-amylase inhibition, and FTIR. Then FTIR data were used for metabolomic analysis (PCA and PLS). Results: The results of the α-amylase inhibition test showed that the ethyl acetate extract had the smallest IC50 average value, which was 3.00 μg/mL. Based on the phytochemical screening test results, the extract showed positive for the presence of compounds such as flavonoids, phenols, tannins, alkaloids, and saponins. From the PCA analysis (Bi-plot), the wavenumbers that were influential in the ethyl acetate extract were 1436 to 1681 and 3341 to 3348 cm−1. In theory, functional groups such as CH, CC, CO, NH, and OH appeared on the absorption. From the PLS analysis, these wavenumbers affected the activity. Conclusion: The most potential extract as an α-amylase inhibitor was the ethyl acetate extract. Based on phytochemical screening tests and metabolomic analysis, it was proven that this extract contained compounds as hypoglycemic agents.

Date palm (Phoenix dactylifera L.) fruits contain high concentrations of phenolic compounds, particularly flavonoids and other micronutrients, which impact human health due to their potent antioxidant, anti-inflammatory, and anticancer characteristics. In the present study, the effect of ethyl acetate, hydroethanol, hydromethanol, and aqueous extract from three date palm varieties (i.e., Ajwa, Siwi, and Sukkari) on phytochemical profiles and antioxidant and anticancer activities was investigated. Fruit extracts were screened for their antioxidant activity using the DPPH· method. Phenolic constituents were quantified and identified using HPLC-DAD. Extracts (ethyl acetate, hydroethanol, and hydromethanol) were assessed for cytotoxicity on nine human cancer cell lines, i.e., MG-63, HCT116, MCF7, MDA-MB-231, HEPG2, HUH7, A549, H460, and HFB4, using the sulphorhodamine-B (SRB) assay. Results showed that the ethyl acetate extract of the Sukkari fruits has the greatest antioxidant potential with an IC50 value of 132.4 ± 0.3 μg·mL−1, while the aqueous extract of Ajwa date fruits exhibited the lowest antioxidant effect with an IC50 value of 867.1 ± 0.3 μg·mL−1. The extracts exhibited potent to moderate anticancer activities against the investigated cancer cell line in a source-dependent manner. Methanol extract of Siwi fruits exhibited the most potent anticancer activity (IC50 = 99 ± 1.6 µg·mL−1), followed by the same extract of Sukkari fruits with an IC50 value of 119 ± 3.5 µg·mL−1 against the cell line of human breast cancer (MDA-MB-231). Additionally, principal component analysis (PCA) was investigated to determine the relationship among the investigated traits and treatments. Our findings reveal that date palm fruit-derived extracts are excellent sources of biologically active constituents and substantiate their potential use in new anticancer strategies from natural resources.

Abstract: Curry Plant (Murraya koenigii (Linn.) Spreng) is one of the plants that thrive in Indonesia. Curry contains secondary metabolites of alkaloids and flavonoids that have the potential as antioxidants. Antioxidants can reduce the activity of free radicals that can cause degenerative diseases such as cancer, coronary heart disease, and premature ageing of body cells by donating the protons to free radical compounds. This study aimed to determine the antioxidant activity and identify the active compound class of ethyl acetate fraction from curry leaves. Separation of secondary metabolites of ethyl acetate extracts was carried out by column chromatography method, which obtained 5 different fractions. The antioxidant activity of fractions A, B, C, D, and E was tested using the DPPH (2,2-diphenyl-1-picrylhydrazyl) method with variations concentrations of 25, 50, 100, 200, and 400 ppm, and ascorbic acid was used as a comparison which measured at a wavelength of 517 nm. The results showed that fractions A and E have weak antioxidant activities, while fractions B, C, and D showed moderate antioxidant activities. The highest antioxidant activity was found in fraction B with an IC50 value of 341.38 ppm, where the fraction showed the presence of secondary metabolites of alkaloids and terpenoids. Abstrak: Tanaman kari ((Murraya koenigii (Linn.) Spreng) merupakan salah satu tanaman yang tersebar di Indonesia. Kari mengandung senyawa metabolit sekunder alkaloid dan flavonoid yang memiliki potensi sebagai antioksidan. Antioksidan dapat mengurangi aktivitas radikal bebas yang dapat menyebabkan penyakit degeneratif seperti kanker, penyakit jantung coroner dan penuaan sel dengan cara menyumbangkan proton pada senyawa radikal bebas. Tujuan dari penelitian ini adalah untuk menentukan aktivitas antioksidan dan mengidentifikasi kelas senyawa aktif fraksi etil asetat dari daun kari. Pemisahan metabolit sekunder dari ekstrak etil asetat dilakukan menggunakan metode kromatografi kolom dengan menghasilkan 5 fraksi yang berbeda. Aktivitas antioksidan dari fraksi A, B, C ,D ,dan E dilakukan menggunakan metode DPPH (1,1-diphenil-2-pikrilhydrazil) dengan variasi konsentrasi 25, 50, 100, 200, dan 400 ppm dan asam askorbat digunakan sebagai perbandingan yang diukur pada panjang gelombang 517 nm. Hasil menunjukkan bahwa fraksi A dan E memiliki aktivitas antioksidan yang lemah, sedangkan fraksi B, C, dan D menunjukkan aktivitas antioksidan sedang. Aktivitas antioksidan yang paling tinggi ditemukan pada fraksi B dengan IC50 341,38 ppm. Fraksi tersebut menunjukkan adanya kandungan senyawa metabolit sekunder alkaloid dan terpenoid.

The aqueous extract was prepared from the Aloe ferox, and Commipora abyssinica combined to develop a botanical mosquito larvicide. The aqueous extract and the solvent fractions obtained using liquid–liquid extraction were tested against Culex pipiens larvae for larvicidal potential. The maximum larvicidal activity was recorded for the ethyl acetate (EtOAc) extract with LC50 values of 28.24 µg/mL followed by hexane (104.42 µg/mL), water (140.24 µg/mL), and chloroform (211.41 µg/mL) extract against the Cx. pipiens third instar 24 h post-treatment. In midguts of EtOAc extract-treated larvae, Longitudinal sections showed edema between the degenerated epithelial cells and degraded microvilli. The extract caused a dose‐dependent decrease in the percentage of cell viability of HUVEC cells suing MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) assay. The IC50 value of the EtOAc extract was 143.6 µg/mL and displayed chromosomal condensation. The total phenolic and flavonoid contents calculated were 15.9 GAE/g (gallic acid equivalent per gram) and 3.69 QurE/g (Qurcetin equivalent per gram), respectively. GC–MS analysis showed that the major chemical components of the EtOAc extract were methyl ester of hexadecanoic acid (28%), 3-benzylbutanoate (9.4%), methyl ester of octadecanoic acid (8.6%), and alpha-muurolene (5.3%). The current investigations revealed the possible use of this botanical combination as a larvicide against Cx. pipiens larvae.

The inhibitory effect against 5-α reductase of the ethyl acetate (EA) extract from Physalis angulata was evaluated in vitro using mouse prostate homogenates, and the suppression of benign prostatic hyperplasia (BPH) was assessed in a mouse model of testosterone-induced BPH. The EA extract exhibited a potentially inhibitory effect on 5-α reductase with an IC 50 of 197 μg/ml. In BPH mice, the EA extract at a dose of 12 mg/kg was comparable to finasteride 5 mg/kg in suppressing BPH in terms of reducing absolute enlarged prostate weight (p < 0.05 vs. BPH group) and mitigating the hypertrophy of glandular elements and prostate connective tissue. Identification of chemical ingredients in the EA extract by UPLC-QTOF-MS revealed 37 substances belonging chiefly to flavonoids and physalins. Further quantification of the EA extract by HPLC-PDA methods revealed that chlorogenic acid, and rutin were the main components. Molecular docking studies of chlorogenic acid and rutin on 5-α reductase showed their high affinity to the enzyme with binding energies of −9.3 and − 9.2 kcal/mol, respectively compared with finasteride (− 10.3 kcal/mol). Additionally, chlorogenic acid inhibited 5-α reductase with an IC 50 of 12.07 µM while rutin did not. The presence of chlorogenic acid in the EA extract may explain the inhibitory effects of the EA extract on 5-α reductase, and thus the suppression of BPH. [Display omitted] [ABSTRACT FROM AUTHOR]

Geum urbanum L. is a medicinal plant used from ancient time against gastro-intestinal disorders, bleeding and inflammation of mucous membranes, gums (gingivitis), etc. In our previous works, we demonstrated the antibacterial and antioxidant properties of ethyl acetate (EtOAc) extracts in vitro. The aim of this study was to evaluate the possibility of the EtOAc fraction from aerial parts to provoke acute and subacute toxicity by its internal daily administration (per os) in healthy H- albino male and female mice. We used three concentrations of treatment according to their biological activity potential of application − 20, 70 and 210 mg/kg. All animals were observed and recorded periodically for clinical signs, mortality and changes in their behavior (incl. hypo-activity, aggression, etc.). The body weight was measured at every 5 days up to the end of the experiment (a total 28 days). We studied the biochemical parameters (superoxide anion radical, hydrogen peroxide, superoxide dismutase, lipid peroxidation and damaged proteins in blood plasma and brain) and complete hematological parameters, and the histopathological findings in mouse spleens and Payer’s patches. The investigated extract did not show any signs of significant acute and subacute toxicity at the highest applied test-concentration, and therefore, we encouraged its possible application as food additive for various infectious diseases.

This study aims to investigate the mechanism(s) included in the bronchodilation effect exerted by Nigella sativa. Ethyl acetate extract (NS.EA) was prepared using a maceration method. Adult albino rats were recruited for thoracotomy and removal of the trachea. After cutting into pieces, the tissue was set in organ bath. The influence of cumulative concentrations of ethyl acetate extract was examined on contractile responses of isolated trachea to acetylcholine using different blockers such as Nifedipine (Ca2+channel blocker), Tetraethylammonium (Ca2+-activated K+ channel blocker), 4-aminopyridine (voltage-dependent K+ channel blocker), Glibenclamide (ATP-sensitive K+ channel blocker), BaCl2 (inward rectifier K+ channel blocker), methylene blue (soluble gaunylate cyclase inhibitor) and indomethacin (non-selective cyclooxygenase inhibitor). Significant inhibition of bronchodilation was observed when tracheal rings were pretreated with indomethacin and BaCl2 with (P50s were (5.635, 6.9, 7.86 and 4.987 mg/ml) respectively. Conversely, 4-AP, GLIB and TEA showed no significant changes in the bronchodilation induced by the extract. Therefore, The Emax value for indomethacin significantly reduced from 101.34 to 73.28%, BaCl2 from 53.62 to 30.31%, methylene blue from 55.78 to 38.94% and nifedipine from 101.34 to 80.88%. On the other hand, the Emax for 4-AP and GLIB were non-significantly reduced from 53.62 to 40.14 and 40.13% respectively; and TEA more or less unchanged to 54.34%. In general, ethyl acetate extract of N. sativa induces bronchodilation through four mechanisms (activation of Kir channel, non-selective cyclooxygenase and to lesser extent the soluble guanylate cyclase, and blockade of Ca2+ channel).

Objective: To investigate the osteoblastogenic activity of the ethyl acetate (EtOAc) extract of Smilax glabra Roxb roots and its major active compound astilbin. Methods: Astilbin was isolated from EtOAc extract using silica gel chromatography combined with fraction crystallization. Chemical structure of astilbin was determined by analysis of the spectroscopic data in comparison with the literature. MTT method was used to detect the toxicity. Alkaline phosphatase (ALP) activity was determined by the spectrophotometric method at 405 nm using p-nitrophenyl phosphate as a substrate. Calcium deposition was stained with alizarin red-S, distained with cetylpyridium chloride, and quantified at 562 nm. In silico model for astilbin-ALP interaction was analyzed using AutoDock 4.2.6. The changes in expression of osteoblast differentiation related genes were determined using quantitative real-time PCR. Results: Both the EtOAc extract and astilbin had no toxicity toward osteoblast MC3T3-E1 cells at 5.0, 10, 25, and 50 μg/mL. At 25 μg/ mL, they enhanced ALP activity and mineralization of osteoblasts up to 30% and 55% for the EtOAc extract and 22% and 41% for astilbin, respectively. Molecular docking analysis of astilbin-ALP interaction revealed Arg167, Asp320, His324, and His437 were key residues participating in hydrophobic interaction; meanwhile, His434 and Thr436 residues were involved in hydrogen bond formation in the active site of human tissue-nonspecific ALP. Moreover, the expression level of genes opn, col1, osx, and runx2 were up-regulated in astilbin treated samples with the fold changes as 2.2; 3.7; 4.1; 2.3, respectively at 10 μg/mL (P

Background: Sedum emarginatum Migo(S. emarginatum) has anti-tumor and anti-oxidant effects. This study aimed to screen the extractions of S. emarginatum against liver cancer in vitro and explore its anti-liver cancer mechanism. Methods: The CCK-8(Cell Counting Kit-8) method was used to detect the inhibitory effect of different extracts of S. emarginatum on the proliferation of liver cancer HepG2 cells. The morphological changes of the cells after administration were observed with microscopy, cell apoptosis was detected by flow cytometry, and the expression of Bax, Bcl-2 and Caspase-3 mRNA in the cells were detected by RT-PCR (Reverse Transcription-Polymerase Chain Reaction) to explore the mechanism of action. Results: CCK-8 method test results showed that among the different extracts of S. emarginatum, the ethyl acetate extract(1000 μg/ml, 2000 μg/ml, 2500 μg/ml, 3000 μg/ml) and n-butanol extract(1000 μg/ml, 2000 μg/ml, 2500 μg/ml, 3000 μg/ml) have the strongest inhibitory effect on the proliferation of HepG2 cells. In these 4 concentrations, the inhibitory effect increased as the concentration increased. The IC50 of the ethyl acetate extract on HepG2 cells was less than that of the n-butanol extract, so the ethyl acetate extract has a better proliferation inhibitory effect on HepG2 cells than the n-butanol extract, followed by the 70% ethanol extract(3000 μg/ml) and the water extract(3000 μg/ml), petroleum ether extract was the weakest. The results of microscopy showed that ethyl acetate extract caused hepatocarcinoma HepG2 cell morphology changed, cell density decreased, and suspension cells increased. Moreover, the results of flow cytometry showed that the ethyl acetate extract of S. emarginatum could induce HepG2 cell apoptosis at the concentrations of 2500μg/ml and 3000μg/ml. RT-PCR results showed that the expression of Bax mRNA was up-regulate by the middle(2500 μg/ml) and high(3000 μg/ml) dose groups of ethyl acetate extract. The expression of Caspase-3 mRNA was up-regulated by the low(2000 μg/ml), medium(2500 μg/ml) and high(3000 μg/ml) dose groups of ethyl acetate extract. The expression of Bcl-2 mRNA was down-regulated by the high(3000 μg/ml) dose group of ethyl acetate extract. Conclusion: The ethyl acetate extract of S. emarginatum has the best effect on human liver cancer HepG2 cells. Its anti-hepatocellular mechanism may be related to affect the expression of apoptosis genes (Bax, Bcl-2 and Caspase-3mRNA) and promote the apoptosis of liver cancer cells. It provided a reference for the research and development of drugs for the treatment of liver cancer. [ABSTRACT FROM AUTHOR]

Abstract Background Adenanthera pavonina L. is an important medicinal plant and its barks are used in traditional medicine for treating different diseases. Therefore, a phytochemical investigation was carried out to isolate and identify secondary metabolites from its barks. Results Seven compounds namely ethyl 3,3-dimethyl-13-hydroxytridecanoate (1), stigmasta-5,22-dien-3β-ol (2), tert.butyl tridecanoate (3), 6-α-hydroxy stigmast-20(21)-en-3-one (4) of dichloromethane extract and 18-(2′, 3′-dihydroxyphenyl)nonadec-17-en-2-ol (5), 1-(N-propyl amino)-2-henecosanone (6), and stigmast–5(6), 20(21)-diene-3-one (7) were isolated from the barks of Adenanthera pavonina Linn. Of these compounds, 1, 4, 5, 6, and 7 appear new. The structures of these compounds were elucidated by spectroscopic techniques, mainly by NMR. Conclusions Five new and two known compounds have been isolated and characterized from the bark of A. pavonina. The isolated compounds could be a potential template for the synthesis and development of new lead compounds with interesting pharmacological properties. Graphical abstract

Aim: The aim of the study included the effect of aqueous extract (AE) and ethyl acetate extract (EAE) on blood sugar in diabetic rats and their effects on liver enzymes and lipid panel in control and diabetic rats. Furthermore, the antioxidant activity of the EAE was studied in vitro and compared with AE. Materials and Methods: Sugar and antioxidant content of AE and EAE were determined. In vitro antioxidant activity of AE and EAE was estimated by 2, 2-diphenyl-1-picrylhydrazyl and ABTS*+ radical scavenging assay, ferric-reducing antioxidant power assay, and total antioxidant assay. To study the effect of the extracts on blood glucose level (BGL), lipid profile, and liver function in non-diabetic and diabetic rats, five groups of six rats each were treated with distilled water, AE, EAE, glibenclamide (GLB), and sucrose for 8 days. Plasma glucose level (PGL), total cholesterol (TC), triglycerides (TG), transaminases (alanine transaminase [ALT] and aspartate transaminase [AST]), and alkaline phosphatase (ALP) were determined. The effect of the interventions on BGL after acute administration also was investigated. Diabetes was induced by streptozotocin injection. Results: EAE contains significantly lower content of fructose and glucose than AE (p

This study explores the anti-inflammatory potential of an endophytic fungus, Trametes versicolor CL-1, isolated from the fruit tissues of Rosa roxburghii. Morphological and molecular analyses confirmed the identity of CL-1. An ethyl acetate extract (CL-E) from its fermentation broth was subjected to UPLC-HRMS and GNPS molecular networking. The analysis revealed a diverse array of secondary metabolites, including 11 terpenes, 7 flavonoids, 10 cinnamic acid derivatives, 6 oligopeptides, and 9 fatty acids, as verified by LC-MS/MS. Notably, CL-E exhibited significant in vitro anti-inflammatory activity in RAW264.7 cells. Furthermore,  molecular docking studies predicted favorable binding interactions of key compounds 1 within CL-E with the NLRP3 inflammasome (PDB ID: 6NPY). These findings suggest T. versicolor CL-1 as a promising source of natural anti-inflammatory agents and unveil R. roxburghii as a potential reservoir for discovering novel bioactive metabolites., (© 2024 Wiley‐VCH GmbH.)

Background: Gastric cancer is one of the most leading causes of cancer death worldwide. Therefore, treatment studies have been being conducted, one of which is screening of novel agents from medicinal herbs. Elephantopus mollis Kunth (EM) belonging to Asteraceae family is a perennial herb with several therapeutic properties including anticancer activity. However, the effect of this species on gastric cancer has not been reported yet. In this study, cytotoxicity of different EM crude extracts was investigated on AGS gastric cancer cell line. Besides, the effects of extract on nuclear morphology, caspase-3 activation, and gene expression were also explored. Results: The results showed that ethyl acetate extract exhibited a remarkably inhibitory ability (IC50 = 27.5 μg/ml) on the growth of AGS cells, while causing less toxicity to normal human fibroblasts. The extract also induced apoptotic deaths in AGS cells as evidenced by cell shrinkage, formation of apoptotic bodies, nuclear fragmentation, caspase-3 activation, and the upregulation of BAK and APAF-1 pro-apoptotic genes related to mitochondrial signaling pathway. Specifically, BAK and APAF-1 mRNA expression levels showed 2.57 and 2.71-fold increases respectively. Conclusions: The current study not only proved the anti-gastric cancer activity of EM ethyl acetate extract but also proposed its molecular mechanism. The extract could be a potential candidate for further investigation. [ABSTRACT FROM AUTHOR]

In this study, we aimed at evaluating in vitro and in vivo anti-inflammatory activity of various extracts of the rhizomes of Globba pendula Roxb. Three extracts (n-hexane, ethyl acetate, and water) were screened for their inhibitory effect on NO production by lipopolysaccharide-stimulated RAW 264.7 macrophages. The ethyl acetate extract of G. pendula rhizomes (EGP) showed a potential effect with an IC50 value of 32.45 µg/mL. For in vivo study, the ethyl acetate extract was further investigated for its anti-inflammatory effect using collagen antibody-induced arthritic mice (CAIA). The level of arthritis in experimental mice significantly reduced (P < .05) after treatment with EGP at a dose of 500 mg/kg body weight (b.w.). This study also revealed that EGP is orally non-toxic. Ethyl p-methoxy cinamate was identified as the main constituent of EGP, which may result in its anti-inflammatory effect. [ABSTRACT FROM AUTHOR]

In this study, to provide a basis for the controlling of citrus canker disease, endophytic fungi from different citrus disease-resistant cultivars were isolated and identified by using a tissue culture method, and the method based on morphology combined with molecular biology, respectively. Representative endophytic fungi were selected based on the antagonism results in pre-experimental, to determine the antibacterial activity with their ethyl acetate extracts from the fermented culture against pathogen Xanthomonas citri subsp. citri, using a toxic medium coating method. The results were as follows:(1)A total of 72 endophytic fungi were obtained from different citrus cultivars and classified into 14 genera. Fungal isolates belong to phylum Ascomycota and Basidiomycota. The frequent genera were Colletotrichum, Guignardia, Alternaria and Fusarium.(2)The diversity indices of endophytic fungi from different citrus as follow: Citrus unshiu Marc.(Guilin)> C. reticulata Blanco cv. Shatangju(Guilin)> C. reticulata Blanco cv. Shatangju(Wuzhou).(3)The diversities indices of endophytic fungi were different, which were isolated from different tissues of citrus associated with different geographical location. The similarity of endophytic fungi in the citrus samples collected from Wuzhou and those from Guilin was low.(4)The antibacterial activity of ethyl acetate extracts from the fermented culture of 30 endophytic fungi were determined against pathogen Xanthomonas citri subsp. citri in vitro assay. Most of their extracts exhibited significant inhibition. Among them, the MIC values of dominant genera, specific genera and shared genus were 0.312 5-10 mg·mL-1, 0.156-5 mg·mL-1 and 0.312 5-2.5 mg·mL-1, respectively. The results indicate that the endophytic fungi in citrus disease-resistant cultivars are rich in diversity, and most of their extracts exhibit inhibition against X. citri subsp. citri. The antibacterial activity of specific genera is generally better than the dominant genera, and all of the strains in the shared genus Fusarium displayed significant inhibition against X. citri subsp. citri. [ABSTRACT FROM AUTHOR]

Moringa olifera Lam. which called "Miracle tree" was an enormous usage of medical, nutritional and economic benefits so its leaves and roots extracts were vitro examined for phytochemicals contents, antioxidant, and cytotoxicity against MCF-7 cell line. Leaves and roots both extracts were estimate using 2,2-di phenyl-1-picryl hydrazyl (DPPH) radical scavenging assay and high performance liquid chromatography (HPLC) to determine phenolic and flavonoids compounds. The leaves aqueous and ethyl acetate extracts contained a significantly (p

The present study investigated the anti-microbial and anti-mycotoxigenic activities of the ethyl acetate extract (EA) and a bioactive compound obtained from an endophytic fungus Alternaria alternata isolated from Catharanthus roseus leaves. A. alternata was identified using PCR-based 5.8S rDNA sequencing. The EA and bioactive compound, p-Coumaric acid (PC), showed concentration-dependent broad-spectrum anti-microbial activity against the tested bacteria, yeast, and fungi with MICs ranging from 7.8 to 250 µg/mL. The in vitro production of aflatoxin B1 (AFB1) from Aspergillus flavus and fumonisin B1 (FB1) from Fusarium verticillioides was completely inhibited by EA and PC at 400 µg/mL. The synthesis of the membrane-bound ergosterol from A. flavus and F. verticillioides was strongly inhibited by PC at 200 µg/mL. The EA and PC were found to show significant anti-microbial and anti-mycotoxigenic activities, hence, they could be explored as protective agents for preventing microbial deterioration and mycotoxins accumulation in food and feedstuffs during pre- and post-harvest and storage.