1,274 results on '"Inhibitory activity"'
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2. Exploring the Pharmacological Potential of Isoquinoline Derivatives: A Comprehensive Review.
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Mahadeviah, Chitrashree, Nagaraj, Purushotham Karadigere, Pasha, Thoppalada Yunus, and Marathi, Priyanka
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HETEROCYCLIC compounds , *DNA replication , *ORGANIC compounds , *LEWIS acids , *ANTINEOPLASTIC agents , *ISOQUINOLINE alkaloids , *ISOQUINOLINE - Abstract
The core structure is an aromatic heterocyclic organic compound i.e. Isoquinoline. Both the structures of Isoquinoline and quinoline contain a fused ring structure of benzene and pyridine. Isoquinoline, the pyridine counterpart, has a pKb of 8.6 and a pKa of 5.14, making it a weak basic. When it comes into contact with Lewis acids, such BF3, it protonates and becomes a salt. This process produces adducts. The liquid form of Isoquinoline is colorless, hygroscopic, and it has an unpleasant smell. Isoquinoline derivatives are a very significant group of natural and synthetic compounds which show various Pharmacological activities like anti-cancer, anti-oxidant, anti-microbial, anti-inflammatory, anti-microbial, analgesic, anti-fungal, anti-viral, antispasmodic and an enzyme inhibitor. Morphine and codeine are the most extensively characterized Isoquinoline alkaloids. They are made from either tyrosine or phenylalanine. Some of the Isoquinoline nucleus-containing drugs available in the market were Nelfinavir, Apomorphine, Quinapril, Praziquantel, Solifenacin, Papaverine, Metocurine, Tubocurarine. Isoquinoline alkaloids with anticancer properties may be therapeutically to target specific binding to nucleic acids, modulating polynucleic acid stability. These binds change the way that duplex B-form DNA interacts with proteins involved in DNA replication, repair, or transcription. [ABSTRACT FROM AUTHOR]
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- 2024
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3. 抗菌肽F1高产菌株筛选鉴定及其对多重耐药菌 生物膜形成的抑制作用.
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王群, 吴嘉诺, 叶铸明, 刘静乐, 王娟, 杨志杰, and 曹庸
- Abstract
Copyright of Modern Food Science & Technology is the property of Editorial Office of Modern Food Science & Technology and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)
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- 2024
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4. Different Combinations of Nitrogen and Carbon Sources Influence the Growth and Postbiotic Metabolite Characteristics of Lactiplantibacillus plantarum Strains Isolated from Malaysian Foods.
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Zheng, Qinri, Chia, Suet Lin, Saad, Norazalina, Song, Adelene Ai-Lian, Loh, Teck Chwen, and Foo, Hooi Ling
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BIOACTIVE compounds ,HYDROXYL group ,CELL populations ,DEXTROSE ,METABOLITES ,LACTIC acid - Abstract
Postbiotic metabolites produced by Lactiplantibacillus plantarum strains isolated from Malaysian food have been extensively reported for their positive effects on health. Understanding the effects of different combinations of carbon and nitrogen sources on the growth and corresponding characteristics of postbiotic metabolites produced by different strains of L. plantarum is important for various applications. Hence, the effects of different combinations of carbon (glucose, lactose, sucrose and dextrose) and nitrogen (X-SEED Kat, X-SEED Peptone, X-SEED Nucleo Advanced, Nucel875 MG, FM888 and FM902) sources on the growth of six strains of L. plantarum (RG11, RG14, RI11, RS5, TL1 and UL4) and the functional characteristics (bacteriocin inhibitory activity, antioxidant activity and lactic acid concentration) of their respective postbiotic metabolites were investigated in this study. UL4 produced the highest viable cell population with sucrose and Nucel875 nitrogen source. The UL4 strain also produced the strongest bacteriocin inhibitory activity with dextrose and FM888 nitrogen source. In comparison, the RI11 strain produced the highest lactic acid concentration with dextrose and Nucel875 nitrogen source and the highest reducing power of RS5 and TL1 postbiotic metabolites was achieved with MRS medium. In the combination of sucrose and X-Seed KAT nitrogen source, RG14 produce the highest hydroxyl radical scavenging activity. The effects of different combinations of carbon and nitrogen sources on the viable cell population of L. plantarum strains and the respective functional characteristics of postbiotic metabolites were strain dependent. The current study also revealed that fermentation media were an important factor that greatly impacted the functionalities of postbiotic metabolites due to the presence of various bioactive compounds that contributed to high antioxidant and antimicrobial properties. The results of this study will facilitate the subsequent medium design and optimisation for the development and production of specific postbiotic metabolites produced by the respective L. plantarum strain for their applications in various industries. [ABSTRACT FROM AUTHOR]
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- 2024
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5. Trichoderma atroviride isolated from diseased apple stem have possible biocontrol effect and tolerance toward azoxystrobin and difenoconazole
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Haichun Cun, Pengbo He, Shahzad Munir, Pengfei He, Yixin Wu, Hui Zhang, Baohua Kong, and Yueqiu He
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Apple root rot ,Trichoderma atroviride ,Identification ,Inhibitory activity ,Tolerance ,Colonization ,Agriculture - Abstract
Abstract Background Apple root rot (ARR) is a typical soil-borne disease that seriously threatens the development of the apple industry. In this study, a biocontrol fungus named AT-1 was screened from the basal tissue of apple stem recovered from root rot infection, and it was identified as Trichoderma atroviride based on morphological characteristics and amplification of the ITS, LSU, and TEF 1 genes. Limited knowledge is present in using Trichoderma against ARR disease. Results In subsequent experiments, a potential biocontrol strain (AT-1) had significant antagonistic activity and easily parasitized a variety of ARR pathogens such as Rosellinia necatrix, Phytopythium vexans, and Athelia rolfsii. The lowest antifungal rate recorded was still more than 40%. In addition, different chemical fungicides were tested against pathogens and biocontrol strains. The control effect was 94.79% in May and 83.41% in August, when T. atroviride AT-1 was applied along with fungicides. Applying chemical fungicides brought more sensitivity against R. necatrix. Trichoderma strains had a good tolerance for azoxystrobin SC and difenoconazole WG fungicides. The antimicrobial strains effectively colonized in apple stem base for more than 1 month, produced many conidia, occupied a favorable niche, and finally, controlled the disease with more than 80% in the field. Conclusion Overall results suggested that T. atroviride AT-1 had a good potential in the prevention and control of ARR and had a good resistance against the applied fungicides, which can provide strain resources and a theoretical basis for ARR control.
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- 2024
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6. Characterization and angiotensin-converting enzyme inhibitory activity of peptides of seabuckthorn (Hippophae rhamnoides L.) seed meal
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Yuanju Zheng, Di Wang, Yunxi Zhou, Michael Yuen, Tina Yuen, Hywel Yuen, and Qiang Peng
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seabuckthorn ,angiotensin-converting enzyme (ace) ,inhibitory activity ,molecular docking ,Food processing and manufacture ,TP368-456 ,Biotechnology ,TP248.13-248.65 - Abstract
Given the side effects associated with synthetic antihypertensive drugs, there is a growing need among researchers to investigate angiotensin-converting enzyme (ACE) inhibitory peptides derived from food protein as safer therapeutic alternatives. This study used seabuckthorn (Hippophae rhamnoides L.) seed meal as the raw material, and the protein was extracted by alkaline extraction and acid precipitation. After enzymatic digestion, peptides with molecular weight less than 3 kDa were selected for study. The screened peptide had an IC50 value of 4.358 mg/mL on ACE with a non-competitive inhibition mechanism and good inhibition stability. By employing infrared (IR) analysis, exclusively β-fold and β-helix structures were identified in the hydrolysate, while no other structural motifs were detected. X-ray diffraction revealed that it had an irregular amorphous structure. The peptide contains 17 amino acids that are both highly acidic and hydrophobic, with glutamic acid ranking first in terms of the number of individual amino acids. Compared with the database (NCBI, Uniport), ten peptides with ACE inhibitory activity were detected, and molecular docking showed the mechanism of each peptide inhibiting ACE, FRVAWTEKNDGQRAPLANN, LIISVAYARVAKKLWLCNMIGDVT-TEQY, VIRSRASDGCLEVKEFEDIPP, AGGGG-GGGGGGSRRL, LQPREGPAGGTT-ALREELSLGPEAALDTPPAGP, DDEARINQLFL, FAVSTLTSYDWSDRDDATQGR-KL, RQLSLEGSGLGVEDLKDN, GGGGGGGGGGGGGGGIGGGGGGGGGGGAR, and KEALGEGCFGNRIDRIGD. According to the results, AGGGGGG-GGGGSRRL is more stable in binding to ACE and may have better inhibitory activity. It has been shown that seabuckthorn protein can be an alternative source of ACE inhibitory peptides.
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- 2024
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7. Rosa × damascena Herrm. From Azaran region, Kashan: rich in saturated and unsaturated fatty acids with inhibitory effect against Proteus mirabilis
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Mansureh Ghavam
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Essential oil ,Rosa ,Fatty acids ,Inhibitory activity ,Kashan ,Other systems of medicine ,RZ201-999 - Abstract
Abstract Background One of the most widely used medicinal plants in Iranian traditional medicine, Rosa × damascena Herrm. (mohammadi flower) that the people of Kashan use as a sedative and to treat nervous diseases and constipation. In this research, the yield, chemical composition and antimicrobial activity of the essential oil of this plant were evaluated for the first time from Azaran region, Kashan. Methods The essential oil was extracted by means of hydrodistillation (Clevenger), and its chemical compounds were identified and determined by GC/MS. The antimicrobial activity of the essential oil was determined by the diffusion method in agar, the minimum growth inhibitory concentration (MIC) and the minimum concentration capable of killing bacterial/fungal microorganisms (MBC/MFC). Results The results showed that the yield of essential oil was 0.1586 ± 0.0331% (w/w). Based on the results of the chemical composition analysis of R. x damascena essential oil, 19 different compounds (98.96%) were identified. The dominant and main components of the essential oil were oleic acid (48.08%), palmitic acid (15.44%), stearic acid (10.17%), citronellol (7.37%) and nonadecane (3.70%). Based on the results of diffusion in agar, the highest zone of inhibition against Candida albicans (ATCC 10231) was ~ 9.5 mm. The strongest inhibitory activity of R. x damascena essential oil against Gram-negative Proteus mirabilis (ATCC 43071) was with the diameter of the inhibition zone (~ 9 mm), which was equal to the strength of rifampin (~ 9 mm). Conclusion Therefore, this essential oil is a promising natural option rich in fatty acids, which can be a potential for the production of natural antimicrobials against infectious diseases, especially urinary tract infections.
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- 2024
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8. The Influence of Different Polyphenols on the Digestibility of Various Kinds of Starch and the Value of the Estimated Glycemic Index.
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Kwaśny, Dominika, Borczak, Barbara, Kapusta-Duch, Joanna, and Kron, Ivan
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CORNSTARCH ,GLYCEMIC index ,MOLECULAR structure ,EPIGALLOCATECHIN gallate ,STARCH - Abstract
Featured Application: This research has contributed to a greater understanding of the influence of polyphenols on starch digestibility and its glycemic index. This may ultimately facilitate the development of traditional starchy products, such as bread, with a reduced glycemic index without compromising their organoleptic characteristics (e.g., color, taste, aroma, and texture). Considering the prevalence of diet-related diseases, new ways of preventing them are being sought. One of them is the addition of polyphenols to high-starch products to inhibit their digestibility and reduce their glycemic index. Therefore, this study aimed to investigate the differences between polyphenols popular in food ((+)catechin, epigallocatechin gallate, quercetin, kaempferol, naringenin, hesperidin, trans-ferulic acid, and p-coumaric acid), in terms of their impact on wheat, rice, potato, and maize starch digestibility. Polyphenols were added to starch separately, before and after its pasting, in one of the following doses: 5, 10, and 20 mg. Starch was digested in the presence of single polyphenols to measure RDS (rapidly digestible starch), SDS (slowly digestible starch), RS (resistant starch), and TS (total starch) content. On that basis, the SDI (starch digestion index) was calculated, and the GI (glycemic index) was estimated. The results show that polyphenols inhibit starch digestion at different levels depending on the type of tested starch and the time of polyphenol addition. However, in terms of RDS, TS, and eGI (estimated glycemic index), the greatest impact was observed for epigallocatechin gallate in a dose of 20 mg most frequently, independently of the kind of tested starch and the time of polyphenol addition. [ABSTRACT FROM AUTHOR]
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- 2024
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9. Retention of Phytochemical Compounds and Antioxidative Activity in Traditional Baked Dish "proja" Made from Pigmented Maize.
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Šimurina, Olivera, Filipčev, Bojana, Kiprovski, Biljana, Nježić, Zvonko, Janić Hajnal, Elizabet, and Đalović, Ivica
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FLAVONOIDS ,PHENOLS ,RADICALS (Chemistry) ,CORN ,DOUGH ,FLOUR - Abstract
Two genotypes of pigmented maize (black (BM) and red (RM)) were used as flour ingredients in several formulations of the traditional baked maize dish "proja". This study investigated the stability of phytochemical compounds and antioxidant activity in proja as affected by baking and different acidity degrees of dough formulations. Compared to RM proja, all BM proja formulations were significantly higher in antioxidant compounds and exhibited the highest inhibitory activity (73–85%) against DPPH. There was a strong significant correlation between DPPH inhibition and total phenolics (r
2 = 0.95), flavonoids (r2 = 0.96), and anthocyanins (r2 = 0.97) in baked proja. After baking, 67–85% of total phenolics were retained. The fate of flavonoids and anthocyanins after baking was variable: from 70% degradation to liberation. Dough acidity significantly and positively affected the content of phenolics, flavonoids, and anthocyanins in BM proja (r2 = 0.70, 0.82, and 0.47, respectively). Baking increased antioxidant activity against DPPH,• OH, and O2 •− radicals in proja, except for ≈10% decline of DPPH inhibition in BM proja. In RM proja, retention of inhibitory capacity against O2 •− was highly correlated to flavonoid retention (r2 = 0.71). Using pigmented maize flour in proja baking resulted in proja with appreciable content of total phenolics, flavonoids, anthocyanins, and high antioxidant activity, confirming the significant improvement of the nutrient profile of this traditional food. [ABSTRACT FROM AUTHOR]- Published
- 2024
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10. Evaluation of the Antifungal and Biochemical Activities of Fungicides and Biological Agents against Ginseng Sclerotinia Root Rot Caused by Sclerotinia nivalis.
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Feng, Shi, Wang, Chunlin, Xu, Zhaoyang, Dou, Baozhu, Wang, Xue, Yang, Lina, Lu, Baohui, and Gao, Jie
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GINSENG ,BACILLUS amyloliquefaciens ,CELL permeability ,MEMBRANE permeability (Biology) ,FUNGICIDES ,ROOT rots ,BIOLOGICAL pest control agents - Abstract
The objective of this study was to identify effective agents for the prevention and control of ginseng Sclerotinia root rot disease caused by Sclerotinia nivalis. The inhibitory effects of 16 chemical fungicides and 10 biocontrol agents (strains) on mycelial growth and sclerotium formation in S. nivalis were determined using a plate confrontation essay. The results showed that the best chemical agents for inhibiting the mycelial growth and sclerotium formation of S. nivalis were fluconazole and fludioxonil, while Bacillus amyloliquefaciens FS6 and B. subtilis (Kono) were the best biocontrol agents (strains). The results of field trials in 2022 and 2023 showed that the control effects of fluconazole and fludioxonil on ginseng Sclerotinia root rot disease were 90.60–98.16%, and those of the biocontrol agents B. amyloliquefaciens FS6 and B. subtilis (Kono) were 94.80–97.24%, respectively. Chemical agents produced abnormal and twisted mycelia, while the biocontrol agents increased mycelial branching, dilated the mycelium tip, and revealed an abnormal balloon. All of the fungicides decreased the ergosterol content, changed the cell membrane permeability, and increased the protein and nucleic acid permeability. These results suggest that these are potential agents for controlling ginseng Sclerotinia root rot disease, and their biochemical mechanisms of chemical and biocontrol of this disease were demonstrated. [ABSTRACT FROM AUTHOR]
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- 2024
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11. New stilbene metabolites isolated from the tuber of Bletilla striata and their biological assessment.
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Qiao, Jin-Wei, Zhang, Nan, Cai, Ming, Zhang, Wei, and Wang, Ju-Tao
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TUBERS ,STILBENE derivatives ,METABOLITES ,ANTI-inflammatory agents ,PHENANTHRENE ,STILBENE ,NITRIC oxide - Abstract
A phytochemical investigation of the tuber of Bletilla striata afforded eight stilbene derivatives, including a new bibenzyl (1) and two new phenanthrene (2 and 3). The structures of these compounds were elucidated using a combination of spectroscopic analyses. Further, the anti-inflammatory activity of all the compounds was evaluated to assess their capability to inhibit nitric oxide (NO) production by RAW 264.7 macrophages. The bioactive screening revealed that compounds 4 and 7 exhibited moderate inhibitory effects against NO production with the IC
50 values 38.7 and 16.7 μM, respectively. [ABSTRACT FROM AUTHOR]- Published
- 2024
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12. Rosa × damascena Herrm. From Azaran region, Kashan: rich in saturated and unsaturated fatty acids with inhibitory effect against Proteus mirabilis.
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Ghavam, Mansureh
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THERAPEUTIC use of flowers ,BACTERIAL disease prevention ,THERAPEUTIC use of essential oils ,MYCOSES ,BACILLUS (Bacteria) ,UNSATURATED fatty acids ,PHYTOCHEMICALS ,STAPHYLOCOCCUS aureus ,SALMONELLA ,PROTEUS diseases ,ANTI-infective agents ,PLANT extracts ,CANDIDA albicans ,PERSIAN medicine ,ESCHERICHIA coli ,MEDICINAL plants ,ONE-way analysis of variance ,ORGANIC compounds ,STAPHYLOCOCCUS ,DATA analysis software ,COMPARATIVE studies ,GRAM-negative bacteria ,SATURATED fatty acids ,RIFAMPIN ,PSEUDOMONAS - Abstract
Background: One of the most widely used medicinal plants in Iranian traditional medicine, Rosa × damascena Herrm. (mohammadi flower) that the people of Kashan use as a sedative and to treat nervous diseases and constipation. In this research, the yield, chemical composition and antimicrobial activity of the essential oil of this plant were evaluated for the first time from Azaran region, Kashan. Methods: The essential oil was extracted by means of hydrodistillation (Clevenger), and its chemical compounds were identified and determined by GC/MS. The antimicrobial activity of the essential oil was determined by the diffusion method in agar, the minimum growth inhibitory concentration (MIC) and the minimum concentration capable of killing bacterial/fungal microorganisms (MBC/MFC). Results: The results showed that the yield of essential oil was 0.1586 ± 0.0331% (w/w). Based on the results of the chemical composition analysis of R. x damascena essential oil, 19 different compounds (98.96%) were identified. The dominant and main components of the essential oil were oleic acid (48.08%), palmitic acid (15.44%), stearic acid (10.17%), citronellol (7.37%) and nonadecane (3.70%). Based on the results of diffusion in agar, the highest zone of inhibition against Candida albicans (ATCC 10231) was ~ 9.5 mm. The strongest inhibitory activity of R. x damascena essential oil against Gram-negative Proteus mirabilis (ATCC 43071) was with the diameter of the inhibition zone (~ 9 mm), which was equal to the strength of rifampin (~ 9 mm). Conclusion: Therefore, this essential oil is a promising natural option rich in fatty acids, which can be a potential for the production of natural antimicrobials against infectious diseases, especially urinary tract infections. [ABSTRACT FROM AUTHOR]
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- 2024
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- View/download PDF
13. Inhibitory mechanism on tyrosinase activity of flavonoids from flower buds of Sophora japonica L
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Yunfeng Ma, Chaoyang Zhang, Jinlin Li, Jiayan Xiong, and Bao-Lin Xiao
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Tyrosinase ,Flavonoids ,Sophora japonica L ,HPLC fingerprints ,Inhibitory activity ,Molecular docking ,Science (General) ,Q1-390 ,Social sciences (General) ,H1-99 - Abstract
The flower buds of Sophora japonica L. (FBSJ) have long been applied as Traditional Chinese Medicine (TCM) and functional food in East Asia. In this study, extracts of FBSJ from 11 different locations were analyzed using the HPLC method to establish their HPLC fingerprints. By determining the IC50 on tyrosinase activity, it was discovered that the extract from Kunming, Yunnan Province exhibited the strongest inhibitory activity. Further analysis, including partial least squares regression coefficient analysis and grey correlation analysis, regarded kaempferol, isorhamnetin, and quercetin as the compounds with significant tyrosinase inhibitory activities. To understand the inhibition mechanism of tyrosinase activity, various analytical techniques such as enzymatic kinetic analysis, fluorescence quenching, circular dichroism (CD), molecular docking, and molecular dynamics simulation were employed. The results revealed that quercetin, isorhamnetin, and kaempferol exhibited higher inhibitory activity and binding energy compared with kojic acid, indicating their potential value as natural tyrosinase inhibitors. This research provides a solid theoretical foundation for studying the application and mechanism of flavonoids against tyrosinase in FBSJ.
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- 2024
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14. Design, Synthesis, and Characterization of Some Oxadiazole Derivatives and Their S-Glucosides Bearing Thiazole Scaffold
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Dekate, Shital M., Hatzade, Kishor M., Ghatole, Ajay M., Ghosh, Arindam, Series Editor, Chua, Daniel, Series Editor, de Souza, Flavio Leandro, Series Editor, Aktas, Oral Cenk, Series Editor, Han, Yafang, Series Editor, Gong, Jianghong, Series Editor, Jawaid, Mohammad, Series Editor, Rattan, Sunita, editor, Gupta, Bhuvanesh, editor, Jeyaseelan, Christine, editor, and Gupta, Anita, editor
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- 2024
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15. HPTLC quantification of quercetin from leaf extracts of C. occidentalis L. and its inhibitory activity against protease enzyme of P. falciparum
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Muhammad, Ibrahim Isyaku and Pandey, Devendra Kumar
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- 2024
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16. The influence of Lactobacillus plantarum fermentation in selenium-enriched Brassica napus L.: changes in the nutritional constituents, bioactivities and bioaccessibility
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Wen Wang, Zhixiong He, Ruiying Zhang, Min Li, Zhenxia Xu, and Xia Xiang
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Se-enriched Brassica napus L. ,Fermentation ,Antioxidant activity ,Inhibitory activity ,Bioaccessibility ,Genetics ,QH426-470 - Abstract
Selenium (Se)-enriched Brassica napus L. is a valuable organic Se supplement. In this study, the fermentation broth enriched with organic Se (FFS) was prepared using Lactobacillus plantarum to ferment the substrate of Se-enriched Brassica napus L. Significant increases were observed after fermentation in total sugars, reducing sugars, soluble proteins, total phenolic content (TPC), and total flavonoid content (TFC). The organic Se was retained at a concentration of 54.75 mg/g in the freeze-dried sample. Principal component analysis and cluster analysis showed good separation between the FFS and unfermented (FS) groups. Fragrant 2-ethyloxetane had the highest content among all volatiles, while sinapine had the highest content among all phenolic compounds. The fermentation process showed remarkable improvement in the abundance and concentration of volatile compounds and phenolic contents, making FFS exhibit strong antioxidant activity and inhibitory capacity against α-glucosidase activity. The bioaccessibility of phenolic compounds was significantly greater in FFS compared to FS. ADMET analysis revealed that the majority of phenolic compounds contained in FFS did not exhibit mutagenicity toxicity, hepatotoxicity, skin sensitization, or blood-brain barrier penetration, indicating a favorable level of biosafety. Overall, our study provides a new insight into the further utilization of Se-enriched Brassica napus L. in foods.
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- 2024
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17. The Inhibition and Interaction Effect of Whole Grain Highland Barley Extract on α-glucosidase Inhibitory Activity
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REN Xin, LIU Xuan, WANG Bu-zhen, ZHANG Min, and WANG Lin-xuan
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whole grain highland barley ,hypoglycemic active ingredients ,α-glucosidase ,inhibitory activity ,synergistic compatibility ,Food processing and manufacture ,TP368-456 ,Nutrition. Foods and food supply ,TX341-641 - Abstract
Highland barley is a unique cereal in the Qinghai-Tibet Plateau of China, and has good effects on improving blood glucose metabolism. However, its specific hypoglycemic ingredients and compatibility are not yet clear. In this manuscript, the polyphenols, polysaccharides, and peptides in whole grain highland barley (WHB) were extracted. And the α-glucosidase inhibitory activity of 3 key active ingredients components and their interaction were investigated. The optimal reaction system for measuring α-glucosidase inhibitory activity using the microplate method was first determined through single factor experiments and Box-Benhnken response surface optimization experiments, i.e., 0.5 U/mL of enzyme concentration, 80 mmol/L of buffer concentration, and 5 mmol/L of substrate concentration. The results showed that all 3 WHB extracts exhibited good α-glucosidase inhibitory activity, with WHB polyphenols having the strongest inhibitory activity. Its inhibition rate reached 83.63% ± 2.92%, corresponding to an IC50 of 0.18 mg/mL. In addition, any 2 hypoglycemic ingredients combinations of the 3 WHB extracts had a certain synergistic effect. Our results will provide guidance for dietary choices in blood glucose control populations and new evidence for the development of functional foods.
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- 2024
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18. Investigation of the inhibitory activity of extracts, fractions and secondary metabolites of Silene spp. (Caryophylaceae) and Serratula cupuliformis (Asteraceae) on the «entry» of herpes simplex type 2 into sensitive cells of the Vero line
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E. I. Каzachinskaia, L. N. Zibareva, E. S. Filonenko, A. V. Ivanova, Yu. V. Коnonova, А. A. Chepurnov, and A. M. Shestopalov
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hsv‐2 ,herbal preparations ,inhibitory activity ,Ecology ,QH540-549.5 - Abstract
In vitro analysis of the inhibitory activity of extracts, fractions and secondary metabolites of plants of the genus Silene (Caryophylaceae) and Serratula cupuliformis (Asteraceae) to the «entry» of herpes simplex type 2 (HSV‐2) into sensitive cells of the Vero line.Ethanol extracts and butanol fractions of Silene spp. and Serratula cupuliformis were prepared. The flavonoid shaftoside and the ecdysteroid 20‐hydroxyecdysone from Lychnis chalcedonica were isolated. For analysis of biologically active substances (BAS) the HPLC method was used. The samples were dissolved in distilled water or DMSO. The laboratory strain MS HSV‐2 was grown on Vero cell culture. In vitro analysis of the inhibitory activity of the herbal preparations on «entry» of HSV‐2 was performed in Vero cell culture by direct inactivation (neutralisation) of virions with 103 PFU /ml.Effective concentrations (EC50) have been identified in the range of 50 % from 2.12±0.47 to 180.99±49.24 μg/ml when preparations were dissolved in water and from 1.99±0.44 to 57.42±14.74 μg/ml when they were dissolved in DMSO. Such results for some samples is comparable to the EC50 of comparison preparations (dry ethanol extracts of spice of cloves, chaga and licorice root). The results obtained suggest the presence of BAS in the herbal preparations studied that act destructively on HSV‐2 virions and affect one of the main stages of its «life» cycle – the «entry» of the virus into sensitive cells.
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- 2024
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19. Protein Tyrosine Phosphatase 1B Inhibitors of Pueraria lobata Based on the Spectrum–Effect Relationship by Q-Marker Selection.
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Zhang, Yong, Liu, Haipeng, Lv, Tianci, Xiao, Mengqian, and Gao, Guihua
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PHOSPHOPROTEIN phosphatases , *PHOSPHATASE inhibitors , *GREY relational analysis , *INSULIN receptors , *PUERARIA , *HIGH performance liquid chromatography , *PROTEIN-tyrosine phosphatase - Abstract
Pueraria lobata (P. lobata), a traditional anti-diabetic medicine mainly composed of flavonoids and isoflavones, has a long history in diabetes treatment in China. However, the anti-diabetic active component is still unclear. Recently, protein tyrosine phosphatase 1B (PTP1B) has been a hot therapeutic target by negatively regulating insulin signaling pathways. In this study, the spectrum–effect relationship analysis method was first used to identify the active components of P. lobata that inhibit PTP1B. The fingerprints of 12 batches of samples were established using high-performance liquid chromatography (HPLC), and sixty common peaks were identified. Meanwhile, twelve components were identified by a comparison with the standards. The inhibition of PTP1B activity was studied in vitro by using the p-nitrophenol method, and the partial least squares discriminant analysis, grey relational analysis, bivariate correlation analysis, and cluster analysis were used to analyze the bioactive compounds in P. lobata. Peaks 6, 9 (glycitin), 11 (genistin), 12 (4′-methoxypuerarin), 25, 34, 35, 36, 53, and 59 were considered as potentially active substances that inhibit PTP1B. The in vitro PTP1B inhibitory activity was confirmed by glycitin, genistin, and 4′-methoxypuerarin. The IC50s of the three compounds were 10.56 ± 0.42 μg/mL, 16.46 ± 0.29 μg/mL, and 9.336 ± 0.56 μg/mL, respectively, indicating the obvious PTP1B inhibitory activity. In brief, we established an effective method to identify PTP1B enzyme inhibitors in P. lobata, which is helpful in clarifying the material basis of P. lobata on diabetes. Additionally, it is evident that the spectrum–effect relationship method serves as an efficient approach for identifying active compounds, and this study can also serve as a reference for screening bioactive constituents in traditional Chinese medicine. [ABSTRACT FROM AUTHOR]
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- 2024
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20. 己唑醇及其复配剂对河南省禾谷镰孢菌的抑制活性及 对小麦赤霉病的室内防效.
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李梦雨, 高续恒, 钱乐, 姜佳, and 刘圣明
- Abstract
Fusarium graminearum is the dominant pathogen causing wheat Fusarium head blight (FHB) in Henan Province. To elucidate the inhibitory activity of hexaconazole against F. graminearum in Henan Province, this study determined the toxicity of hexaconazole on F. graminearum at different developmental stages and the inhibitory activity of hexaconazole against 205 F. graminearum strains collected from six regions in Henan Province was determined using the mycelial growth rate method. Finally, the coleoptiles of wheat inoculation were used to determine the indoor control efficacy of hexaconazole against FHB. The results indicated significant variations in inhibitory activity of hexaconazole against F. graminearum at different developmental stages, with EC50/(μg/mL) values ranking as follows: spore germination (22.5750) > sporulation quantity (2.1686) > sprout tube elongation (0.8922) > smycelium growth (0.3862). The EC50 value of hexaconazole against 205 strains of F. graminearum ranged from 0.0345 to 0.9439 μg/mL, with an average EC50 value of (0.3578 ± 0.1928) μg/mL. The frequency distribution of sensitivity exhibited a continuous single-peak curve, suggesting the absence of subpopulations with reduced sensitivity to hexaconazole. The results of the combination toxicity between hexaconazole and carbendazim, fluoxazonil, phenamacril, prochloraz, and pydiflumetofen revealed various additive or synergistic effects. The synergy ratio (SR) ranged from 0.5042 to 3.7293, with the maximum value observed at a ratio of m (hexaconazole) : m (pydiflumetofen) = 1 : 5 (SR = 3.7293), yielding an actual EC50 value of 0.0133 μg/mL. The results of indoor control efficacy showed that the combined fungicides exhibited significantly higher control efficacy compared to single fungicides, namely carbendazim, hexaconazole, and pydiflumetofen. The control efficacy of m (hexaconazole) : m (pydiflumetofen) = 1 : 5 on coleoptiles of wheat was 93.93% at a concentration of 9 μg/mL. In practical applications, hexaconazole should be combined or rotated with fluoxazonil or pydiflumetofen to prevent or delay the development of field resistance. This study provides crucial theoretical and data support for the rational use of hexaconazole and comprehensive control of FHB. [ABSTRACT FROM AUTHOR]
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- 2024
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21. Unraveling the microbial status of wild bee's honey from North India.
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Thakur, Bharti, Devi, Sunita, Thakur, Meena, Parihar, Akwal, Sagar, Vinay, and Devi, Diksha
- Subjects
- *
HONEYBEES , *BACILLUS pumilus , *BACILLUS subtilis , *KLEBSIELLA pneumoniae , *PSEUDOMONAS aeruginosa - Abstract
To the best of our knowledge, this paper presents the first report on the microbial status of wild bees (A. dorsata and A. florea) honey collected from different northern states of India. In total, 17 bacterial morphotypes (9 from A. dorsata and 8 from A. florea) were recovered. The bacterial load (log CFU/g) was observed to be maximum (4.01) in A. dorsata honey from Sirmour-Puruwala whereas, lowest load (3.49) was recorded in Punjab-Rupnagar honey. Likewise, A. florea honey from Sirmour-Kala Amb and Punjab-Doraha were recorded with maximum and minimum bacterial loads of 4.17 and 3.40, respectively. Observance of lower bacterial load than hazardous limit ensured its safety for human consumption. Three most dominant bacteria viz., AD1, HF7 and AF4 were identified as Micrococcus endophyticus (MT938911), Bacillus subtilis subsp. stercoris (MT764923) and Bacillus pumilus (MT764923), respectively through 16S rRNA ribotyping. Moreover, the inhibitory activity of honey was good to excellent against Salmonella typhi NCTC 786 and fair to good against Bacillus subtilis ATCC 6633, Pseudomonas aeruginosa ATCC 10662 and Klebsiella pneumoniae ATCC 13883. The Escherichia coli ATCC 1041 was the most sensitive bacterium among all. These results justify wild bees honey as a natural remedy for curing and preventing numerous human ailments. [ABSTRACT FROM AUTHOR]
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- 2024
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22. Virtual Screening of a-glucosidase and a-amylase Inhibitors from Soybean Peptides and Its Activity Validation in Vitro.
- Author
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Xue Sen, Wu Jingfan, Cao Shufang, Bai Miao, Zhu Danshi, Liu He, and Yang Lina
- Subjects
SOY proteins ,PEPTIDES ,HYDROGEN bonding interactions ,CHYMOTRYPSIN ,AMYLASES ,DIGESTIVE enzymes ,TRYPSIN - Abstract
The objective: To delay the digestion of carbohydrates by inhibiting the activity of carbohydrate digestive enzymes, thereby preventing and controlling the effects of diabetes has become a research hotspot across multiple fields. j8 Conglycinin is the most abundant functional protein in soy protein, but it is unknown whether the peptides produced after gastrointestinal digestion possess the activity to inhibit carbohydrate digestive enzymes. Method: Conglycinin was subjected to simulated gastrointestinal digestion, and glucosidase inhibitory peptides and amylase inhibitory peptides were selected through virtual screening and ADMET prediction, and the inhibitory effects of the peptides on " --glucosi-dase and " --amylase were tested. Results: ! --Conglycinin was virtually digested into 95 small molecular peptides by pepsin, trypsin, and chymotrypsin; eight "--glucosidase inhibitory peptides and "--amylase inhibitory peptides were selected; it was found that hydrogen bonds and electrostatic interactions play an important role in the binding of peptides with glucosidase and amylase; in vitro verification found that the tetrapeptide EASY has a strong inhibitory effect on glucosidase, with an IC0 value of 208.6 g/mL, and no obvious inhibitory effect on amylase was observed. Conclusion: The glucosidase inhibitory peptide EASY possesses the activity to inhibit carbohydrate digestive enzymes and may become a potential inhibitor for controlling diabetes. [ABSTRACT FROM AUTHOR]
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- 2024
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23. The sesquiterpenes with the COVID-19 Mpro inhibitory activity from the Carpesium abrotanoides L.
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Fan, Yu-Wen, Ao, Zhuo-Yi, Zhang, Wei-Jie, Chen, Jia-Yan, Lian, Xin, Chen Pan, Yong-, Chen, Li-Ping, Wu, Jie-Wei, and Yuan, Jie
- Subjects
SESQUITERPENES ,COVID-19 ,NUCLEAR magnetic resonance spectroscopy ,PLANT extracts ,COUMARINS - Abstract
The extract of the whole plant of Carpesium abrotanoides L. yielded four new sesquiterpenes including a novel skeleton (claroguaiane A, 1), two guaianolides (claroguaianes B–C, 2–3), and one eudesmanolide (claroeudesmane A, 4), together with three known sesquiterpenoids (5–7). The structures of the new compounds were elucidated by spectroscopic analysis especially 1D and 2D NMR spectroscopy and HRESIMS data. Additionally, all the isolated compounds were preliminarily evaluated for the inhibitive activity of COVID-19 M
pro . As a result, compound 5 showed moderate activity with an IC50 value of 36.81 μM and compound 6 exhibited a potent inhibitory effect with an IC50 value of 16.58 µM, while other compounds were devoid of noticeable activity (IC50 > 50 μM). [ABSTRACT FROM AUTHOR]- Published
- 2024
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24. 基于α-葡萄糖苷酶抑制活性评价青稞 全粉提取物抑制效果及其相互作用.
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任 欣, 刘 璇, 王补珍, 张 敏, and 王林萱
- Abstract
Copyright of Science & Technology of Cereals, Oils & Foods is the property of Science & Technology of Cereals, Oils & Foods Editorial Office and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)
- Published
- 2024
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25. INHIBITORY ACTIVITY OF LACTIC ACID BACTERIA ISOLATED FROM TILAPIA GUT AGAINST STREPTOCOCCUS AGALACTIAE.
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KELANY, NOURA, KOTB, SABER, ABDEL-MOHSEIN, HOSNIA, and ISMAIL, ABD EL-MOEZ
- Subjects
- *
LACTIC acid bacteria , *STREPTOCOCCUS agalactiae , *STREPTOCOCCUS thermophilus , *TILAPIA , *STREPTOCOCCAL diseases , *DRUG resistance in bacteria , *NILE tilapia - Abstract
Tilapia culture offers cheap high-quality protein for the human population demand. However, with intensification, the cultured tilapia become threatened by Streptococcus infection, and antibiotic resistance emergence in aquaculture. Therefore, probiotics were investigated to be used as an alternative for antibiotics to treat Streptococcus infections. In the current study, probiotic lactic acid bacteria count ranged from 5.67 to 5.78 log10 CFU/g of tilapia gut microflora. The conventional biochemical tests were carried out for the lactic acid bacteria isolates identification. Only seven native isolates which exhibited inhibitory properties against Streptococcus agalactiae with an inhibition zone 26-50 mm in diameter were selected for characterization. All probiotic isolates were negative for hemolysis and produced both amylase and lipase enzymes. The selected strains tolerated the fish's gastrointestinal acidic and bile conditions. The promising features of the isolated strains indicate that probiotic bacteria of aquatic origin can be considered a safe alternative for pathogen control. [ABSTRACT FROM AUTHOR]
- Published
- 2024
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26. Evaluation of Inhibitory Activities of Different Chinese Herbal Medicine Plant Extracts Against Banana Fusarium Wilt Disease
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Yongfeng HUANG, Dandan XIANG, Zhenxing JIANG, Chunyu LI, and Weirong HU
- Subjects
chinese herbal medicine plant ,extract ,fraction separation ,banana fusarium wilt ,inhibitory activity ,Agriculture - Abstract
【Objective】The research aims to investigate the inhibitory effects of different Chinese herbal medicine extracts on banana Fusarium wilt, and to screen effective plant resources for the control of banana Fusarium wilt.【Method】Tests were carried out on 29 Chinese herbal medicines, including Rheum palmatum and Andrographis paniculata, and the effective active ingredients were extracted by ethanol extraction. The inhibitory effects of different extracts on Foc TR4 were detected by the growth rate method, and the ethanol extracts of Rheum palmatum were extracted by using four solvents with different polarities, namely, petroleum ether, chloroform, ethyl acetate and n-butanol. The inhibitory effects of the extracts on the spores germination of banana Fusarium wilt were determined by the pendant drop method, and the effects of the extracts on the mycelial morphology of banana Fusarium wilt were observed.【Result】The inhibitory effects of 29 herbal medicine extracts on Foc TR4 showed great differences, and four extracts, including Rheum palmatum, Andrographis paniculata, Sophora flavescens, and Chrysanthemum indicum had better inhibitory effects on Foc TR4, among which the best inhibitory effect was achieved by Rheum palmatum extract, with the inhibitory rate of 6 mg/mL Rheum palmatum extract being 48.57%, and the EC50 of the mycelial growth being 6.68 mg/mL, while the EC50 of the spore germination was 4.60 mg/mL. Through observation by light microscope, the Rheum palmatum extract had a certain destructive effect on Foc TR4 mycelium, which produced a large number of branches and adhesions and caused uneven mycelial growth; among the four extraction fractions of the ethanolic crude extracts of Rheum palmatum, namely, petroleum ether, chloroform, ethyl acetate and n-butanol, the extract fraction of ethyl acetate showed the best inhibitory effects on the growth and spore germination of Foc TR4 mycelium, and the inhibition rate of mycelial growth could reach 85.68% when the concentration was 10 mg/mL. The EC50 value of ethyl acetate extract fraction of Rheum palmatum extract on Foc TR4 was 0.16 mg/mL.【Conclusion】The Rheum palmatum extract was screened out from 29 Chinses herbal medicine extracts with better inhibitory effect, and its main effective inhibitory component against banana Fusariu wilt Foc TR4 was in the ethyl acetate extract fraction was further clarified, which could provide a reference for the research and development of new pesticides from plant resources for the prevention and control of banana Fusarium wilt.
- Published
- 2024
- Full Text
- View/download PDF
27. The Heating Under Micro Variable Pressure (HUMVP) Process to Decrease the Level of Saponin in Quinoa: Evidence of the Antioxidation and the Inhibitory Activity of α-Amylase and α-Glucosidase
- Author
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Ligen Wu and Anna Wang
- Subjects
quinoa ,saponin ,heating under micro variable pressure ,inhibitory activity ,Chemical technology ,TP1-1185 - Abstract
To reduce the level of saponin while preserving essential nutrients and antioxidative properties in quinoa (Chenopodium quinoa), this study delves into the optimization of the HUMVP process and thoroughly examines its effects on antioxidation as well as its inhibitory influence on α-amylase and α-glucosidase. The optimal HUMVP conditions involved wetting quinoa grains with 6% water (pH = 6.0) and subjecting them to a 4 min treatment under 0.35 MPa pressure. The values of •OH, DPPH, and ABTS•+ scavenging rate of the extracts from the quinoa sample (named Q2HUMVP) treated under the optimum HUMVP process were 70.02, 87.13, and 50.95%, respectively. Furthermore, the treatment preserved 95.20% of polyphenols and 73.06% of flavonoids, while the saponin content was reduced to 23.13% of that in raw quinoa. Notably, Q2HUMVP extracts demonstrated superior inhibitory activity against α-amylase and α-glucosidase compared to dehulled quinoa samples. The inhibition exhibited by the quinoa sample extracts on α-amylase and α-glucosidase was found to be reversible.
- Published
- 2024
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28. Trichoderma atroviride isolated from diseased apple stem have possible biocontrol effect and tolerance toward azoxystrobin and difenoconazole
- Author
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Cun, Haichun, He, Pengbo, Munir, Shahzad, He, Pengfei, Wu, Yixin, Zhang, Hui, Kong, Baohua, and He, Yueqiu
- Published
- 2024
- Full Text
- View/download PDF
29. 不同中草药植物提取物对香蕉枯萎病菌抑菌活性评价.
- Author
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黄永丰, 项丹丹, 江振兴, 李春雨, and 胡位荣
- Abstract
【Objective】The research aims to investigate the inhibitory effects of different Chinese herbal medicine extracts on banana Fusarium wilt, and to screen effective plant resources for the control of banana Fusarium wilt. 【Method】Tests were carried out on 29 Chinese herbal medicines, including Rheum palmatum and Andrographis paniculata, and the effective active ingredients were extracted by ethanol extraction. The inhibitory effects of different extracts on Foc TR4 were detected by the growth rate method, and the ethanol extracts of Rheum palmatum were extracted by using four solvents with different polarities, namely, petroleum ether, chloroform, ethyl acetate and n-butanol. The inhibitory effects of the extracts on the spores germination of banana Fusarium wilt were determined by the pendant drop method, and the effects of the extracts on the mycelial morphology of banana Fusarium wilt were observed.【Result】The inhibitory effects of 29 herbal medicine extracts on Foc TR4 showed great differences, and four extracts, including Rheum palmatum, Andrographis paniculata, Sophora fl avescens, and Chrysanthemum indicum had better inhibitory effects on Foc TR4, among which the best inhibitory effect was achieved by Rheum palmatum extract, with the inhibitory rate of 6 mg/mL Rheum palmatum extract being 48.57%, and the EC50 of the mycelial growth being 6.68 mg/mL, while the EC50 of the spore germination was 4.60 mg/mL. Through observation by light microscope, the Rheum palmatum extract had a certain destructive effect on Foc TR4 mycelium, which produced a large number of branches and adhesions and caused uneven mycelial growth; among the four extraction fractions of the ethanolic crude extracts of Rheum palmatum, namely, petroleum ether, chloroform, ethyl acetate and n-butanol, the extract fraction of ethyl acetate showed the best inhibitory effects on the growth and spore germination of Foc TR4 mycelium, and the inhibition rate of mycelial growth could reach 85.68% when the concentration was 10 mg/mL. The EC50 value of ethyl acetate extract fraction of Rheum palmatum extract on Foc TR4 was 0.16 mg/mL.【Conclusion】The Rheum palmatum extract was screened out from 29 Chinses herbal medicine extracts with better inhibitory effect, and its main effective inhibitory component against banana Fusariu wilt Foc TR4 was in the ethyl acetate extract fraction was further clarified, which could provide a reference for the research and development of new pesticides from plant resources for the prevention and control of banana Fusarium wilt. [ABSTRACT FROM AUTHOR]
- Published
- 2024
- Full Text
- View/download PDF
30. Effect of in vitro simulated digestion on the biological activities of purified phenolic compounds from Moringa oleifera leaves.
- Author
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Hamed, Yahya S., Akhtar, Hafiz Muhammad Saleem, Rayan, Ahmed M., and Zeng, Xiaoxiong
- Subjects
- *
MORINGA oleifera , *PHENOLS , *DIGESTION , *GUT microbiome , *GLUCOSE metabolism , *PLANT polyphenols - Abstract
Summary: The biological activities of Moringa oleifera leaf polyphenols were tested after in vitro gastrointestinal (GI) digestion and colonic fermentation (CF). Following in vitro GI digestion and CF, total phenolic compounds (TPC) were reduced by 30% and 38.82%, respectively. Moringa polyphenol extract (MPPE) substantially reduced pancreatic lipase and α‐glucosidase inhibition by 5.63% and 14.20% after GI digestion and 27.41% and 34.01% after CF. In contrast, inhibitory activity against α‐amylase was eliminated with GI digestion and CF. Slight decreases in both antioxidant activity assays (DPPH and ABTS) after GI digestion and CF were observed. Cytotoxic activity against HeLa and HepG2 cancer cells was decreased after GI digestion and CF while anti‐proliferation activity against HepG2 cells was improved after CF. MPPE significantly affected the abundance of gut microbiota groups, accordingly, could improve glucose metabolism, decline the energy harvest and subsequently reduce the risk of obesity. [ABSTRACT FROM AUTHOR]
- Published
- 2024
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31. INHIBITION OF ALPHA-GLUCOSIDASE BY POLYSACCHARIDES FROM WATER LETTUCE (Pistia stratiotes) LEAF EXTRACTS WITH DIFFERENT EXTRACTION METHODS.
- Author
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Sudirman, Sabri, Ghaisani, Aatikah Dewi, Widiastuti, Indah, Herpandi, Sirat, Yohana Novelina, and Janna, Miftahul
- Subjects
- *
LETTUCE , *POLYSACCHARIDES , *MONOSACCHARIDES , *ALPHA-glucosidases , *BLOOD sugar , *HOT water , *METABOLIC disorders , *DIABETES - Abstract
Diabetes mellitus (DM) is a metabolic disorder that has a significant impact on the quality of life and health. This condition is indicated by high blood glucose or hyperglycemia. Alpha-glucosidase is an important enzyme during carbohydrate digestion to obtain monosaccharides such as glucose. This study aimed to investigate the alpha-glucoside inhibitory activity of polysaccharides from water lettuce (Pistia stratiotes) leaf with different extraction methods. The leaf was extracted by hot water extraction (HWE) and ultrasoundassisted extraction (UAE). The total sugar, crude fiber, and alpha-glucosidase inhibitory activity were analysis by in vitro, then an independent-sample t-test was used to analyze the statistically different. The UAE method showed a high yield of crude extract than the HWE method. However, the total sugar of HWE is higher than UAE, whereas no different of crude fiber level. The extract from the HWE method more effectively inhibits the alpha-glucosidase activity when compared to UAE. Therefore, hot water extraction is the suitable method to extract polysaccharides from a water lettuce (Pistia stratiotes) leaf. This condition also indicated polysaccharides extract potential to develop as an antidiabetes agent. [ABSTRACT FROM AUTHOR]
- Published
- 2024
- Full Text
- View/download PDF
32. The Volatile Constituents from Lepidium sativum and Tridax procumbens Shoots Exhibit Antimicrobial Effect and Inhibitory Activities Against α-Amylase Enzyme and 2,2-Diphenyl-1-Picrylhydrazyl (DPPH) Radical.
- Author
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Gafar, Maryam K., Okoye, Ikechukwu F., Olatunji, Lawal K., Ahmad, Jamilu, Umar, Aminat O., Ibrahim, Oluwatoyin S., Salim, Fatimah, and Ahmad, Rohaya
- Subjects
LEPIDIUM ,VOLATILE organic compounds ,PLANT shoots ,BETA-amylase ,RADICALS (Chemistry) - Abstract
The bioprospecting of wild functional food plants used in the urban communities in developing countries as sources of food and medicine has been on the rise steadily. Lepidium sativum and Tridax procumbens are wild edible plants in Nigeria with tremendous ethnomedicinal uses. In this research, volatile extracts were obtained from the shoots of the two plants via steam distillation and subjected to Gas Chromatography Mass Spectrometry analysis, antimicrobial analysis and inhibitory activities against α-amylase enzyme and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical, respectively. A white color volatile extract was obtained from L. sativum shoot while a translucent volatile extract with sweet scent was obtained from T. procumbensshoot. Both extracts consist of vary constituents of phytochemicals. The extract from L. sativum only showed moderately susceptibility against Streptococcus pneumonea with zone of inhibition of 11.5 mm among the selected microbes while extract from T. procumbens showed a broader susceptibility towards more microbes with higher zone of inhibition values and a better inhibitory activity against Staphylococcus aureus with minimum inhibition concentration MIC of 31.23 mg/g. Both extracts have better alpha-amylase inhibitory activity with EC
50 values of 134.48 µg/mL (L. sativum) and 106.74 µg/mL (T. procumbens), respectively when compared to the EC50 value of 165.93 µg/mL of the standard drug acarbose. However, the standard drug (ascorbic acid) exhibited better inhibitory activity against DPPH radical with EC50 value of 41.69 µg/mL when compared to their EC50 values of 47.71 and 48.63 µg/mL, respectively. The results show that the volatile extracts contain phytochemicals with antimicrobial, anti-diabetic and antioxidant potentials [ABSTRACT FROM AUTHOR]- Published
- 2024
- Full Text
- View/download PDF
33. Novel phenolic metabolites isolated from plant endophytic fungus Fusarium guttiforme.
- Author
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Yue, Jing-Yi, Wang, Rui, Xu, Tao, Wang, Ju-Tao, Yu, Yang, and Cai, Bai-Xiang
- Subjects
PLANT-fungus relationships ,ENDOPHYTIC fungi ,PHYTOPATHOGENIC fungi ,OPTICAL rotatory dispersion ,FUSARIUM ,METABOLITES ,CARNOSIC acid ,NITRIC oxide - Abstract
Two new phenolic compounds Fusagunolics A (1) and B (2) were isolated from the plant endophytic fungus Fusarium guttiforme, in addition to the previously known metabolites (3-6). The structures of these compounds was elucidated using a combination of spectroscopic analyses, including UV, HRESIMS, 1 D, and 2 D NMR, as well as electronic circular dichroism (ECD) and the optical rotatory dispersion (ORD). Further, the anti-inflammatory activity of all the compounds was evaluated to assess their capability to inhibit nitric oxide (NO) production by RAW 264.7 macrophages. The bioactive screening revealed that compounds 2 and 6 exhibited moderate inhibitory effects against NO production with the IC
50 values 28.6 and 37.6 μM, respectively. [ABSTRACT FROM AUTHOR]- Published
- 2024
- Full Text
- View/download PDF
34. Synthesis of curcumin derivatives for suppression of castration-resistant prostate cancer.
- Author
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Gong, Shunze, Yuan, Chixiang, Hu, Hang, and Xu, Defeng
- Subjects
- *
CASTRATION-resistant prostate cancer , *ANDROGEN receptors , *CURCUMIN , *NUCLEAR magnetic resonance , *HIGH performance liquid chromatography , *ALDOL condensation - Abstract
In this work, 20 curcumin derivatives containing halogen atoms or nitrogen atoms were synthesized for suppression of castration-resistant prostate cancer. These curcumin derivatives were prepared by aldol condensation between the substituted benzaldehydes and acetylacetone or ethyl 3-acetyl-4-oxopentanoate. All synthesized compounds were characterized by 1H nuclear magnetic resonance, 13C nuclear magnetic resonance, high resolution mass, ultraviolet–visible spectroscopy, fluorescence spectroscopy, and high-performance liquid chromatography. The in vitro cytotoxicity of the prepared compounds against 22Rv1 cells was evaluated by the standard MTT assay. The compounds with good inhibitory activity against 22Rv1 cells were further tested for androgen receptor suppression effect. The results show that all compounds were successfully prepared and the purities are all over 90%. Among all synthesized compounds, compound p and s exhibit better inhibitory activity against 22Rv1 cells as compared to dimethylcurcumin, compound q and r display similar inhibitory activity against 22Rv1 cells as compared to dimethylcurcumin. Compounds p-s also demonstrate enhanced androgen receptor suppression effect against 22Rv1 cells as compared to dimethylcurcumin. This work indicates that compounds p-s show promising inhibitory activity against castration-resistant prostate cancer cells by suppression of androgen receptor. [ABSTRACT FROM AUTHOR]
- Published
- 2024
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35. The behavior of the Bacillus probiotic species under conditions of co-cultivation
- Author
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O. V. Knysh, A. V. Martynov, S. I. Pokhyl, and N. I. Skliar
- Subjects
bacillus ,b. clausii ,b. coagulans ,b. subtilis ,cocultivation ,inhibitory activity ,swimming ,swarming ,Medicine - Abstract
Combining probiotic bacteria is a promising strategy to increase the effectiveness and avoid side effects of probiotic therapy. Bacteria that find themselves in a common environment are able to both change their properties and show new ones under the influence of each other. The change of colonization and antagonistic properties, which provide bacteria with competitive advantages in the development of new spaces, deserves special attention. The aim of this research was to study the features of the mutual influence of probiotic bacilli: B. clausii, B. coagulans and B. subtilis on growth, swimming and swarming motility when co-cultivated on agar media of different solidity. Materials and methods. The study used commercial strains of bacilli from three probiotic preparations: Enterogermina, Lactovit forte and Subalin. The ability of the studied species of bacilli to influence each other’s growth was investigated by the agar block method (using 1.5 % nutrient agar) and the spot-on-lawn assay (using 0.7 % nutrient agar). The study of the mutual influence on swimming and swarming activity was carried out when bacilli were cultivated on 0.25 % and 0.70 % tryptone agar, respectively. The diameters of swimming halos and migration swarms formed by monoand mixed cultures were measured, and the areas covered by them were compared. The phenotypes of the meeting of swarms formed by cultures spotted on the swarm plates at different locations were also investigated. Results. The studied probiotic species of the bacilli did not show a strong ability to inhibit each other’s growth. The B. clausii culture had no inhibitory effect, and the B. coagulans culture demonstrated a moderate inhibitory influence on the growth of the other two species of bacilli when using both diffusion methods. The B. subtilis culture showed moderate or weak inhibitory activity against the B. clausii culture and weak or no inhibitory activity against the B. coagulans culture using the agar block method or spot-on-lawn assay, respectively. The B. coagulans + B. subtilis, B. clausii + B. coagulans and B. clausii + B. subtilis mixed cultures showed moderate, weak and no inhibitory activity against third cultures, respectively. The studied species of bacilli showed different swimming ability and swarming potential as well as the ability to influence each other’s motility. Swimming halos formed by the B. clausii + B. subtilis and B. clausii + B. сoagulans + B. subtilis mixed cultures covered significantly larger plate areas than the swimming halos formed by each culture separately during the same cultivation time. The highest swarming potential was observed in B. coagulans culture and B. cla usii + B. coagulans + B. subtilis mixed culture. The studied bacilli did not show the ability to merge swarms, but, on the contrary, their swarms at the point of contact formed visible “boundary” or “intermediate” lines, demonstrating the ability to identify nonself. Conclusions. The obtained results indicate the ability of the probiotic species of bacilli: B. clausii, B. coagulans and B. subtilis to mutually influence growth, swimming and swarm motility. The highest indicators of swimming and swarming of the triple mixed culture indicate an increase in the colonization potential of the studied bacilli when they are combined. The hypothesis of mutual induction of inhibitory compounds production by bacilli, which may increase the overall antagonistic potential of the triple mixed culture, is subject to further confirmation.
- Published
- 2023
- Full Text
- View/download PDF
36. A method for obtaining aqueous and dry ethanol extracts of grass (a mixture of flowers with leaves) and a stalk of St. John's wort (Hypericum perforatum L.) with inhibitory activity on the replication of the SARS‐CoV‐2 coronavirus in vitro
- Author
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Е. I. Каzachinskaia, Yu. V. Коnonova, A. V. Ivanova, L. N. Zibareva, А. А. Chepurnov, V. V. Romanyuk, A. A. Biibolatov, М. А. Gulyaeva, and А. М. Shestopalov
- Subjects
sars‐cov‐2 ,st john's wort (hypericum perforatum l.) ,inhibitory activity ,Ecology ,QH540-549.5 - Abstract
Aim. In vitro evaluation of the inhibitory activity of aqueous extracts and dry ethanol extracts of St John's wort (Hypericum perforatum L.) on the replication of SARS-CoV-2 according to three experimental schemes – direct inactivation (neutralisation) of the virus as well as "prevention" and "treatment" of cells.Materials and Methods. The laboratory strain SARS-CoV-2/human/RUS/Nsk-FRCFTM-1/2020 was passed on Vero cell culture. Water extracts and dry ethanol extracts of parts of H. perforatum L. collected during the flowering period in the Novosibirsk region were prepared. Dry extracts were dissolved in DMSO. Comparison samples are dry ethanol extracts of chaga, cloves and black tea.Results. It is shown that the aqueous extract of grass (a mixture of flowers with leaves) of H. perforatum L. with direct inactivation of the virus it is active in dilution of 1/4096. For the dry ethanol extract of the herb H. perforatum L., 50 % effective concentrations (EC50) were found equal to 2.44±0.87; 8.79±1.91 and 14.65±1.91 μg/ml respectively with direct inactivation as well as according to the "preventive" scheme and with the "treatment" of cells. Taking into account cytotoxicity, as well as in comparison with control samples, the values of selective indices (SI50) of the studied herbal preparations during direct inactivation were higher than with other experimental schemes and were distributed as follows (in descending order): 204.92; 153.68; 115.27; 32.01 and 21.33 for dry ethanol extracts of black tea from India, cloves, herbs, a mixture of flowers with leaves, of H. perforatum, chaga and the stems of H. perforatum respectively. The HPLC method has shown that the ethanol extract of the herb H. perforatum L. contains a greater amount of flavonoids than the extract of stems. Nevertheless, antiviral activity was also detected for the extract of stems of this plant with EC50 equal to 14.65±1.91; 78.13±20.05 and 117.19±15.31 μg/ml (according to three experimental schemes), respectively.Conclusion. For the preparation of antiviral drugs the whole plant of H. perforatum L., including stems, can be used as raw materials.
- Published
- 2023
- Full Text
- View/download PDF
37. Different Combinations of Nitrogen and Carbon Sources Influence the Growth and Postbiotic Metabolite Characteristics of Lactiplantibacillus plantarum Strains Isolated from Malaysian Foods
- Author
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Qinri Zheng, Suet Lin Chia, Norazalina Saad, Adelene Ai-Lian Song, Teck Chwen Loh, and Hooi Ling Foo
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Lactiplantibacillus plantarum ,postbiotic ,antioxidant activity ,lactic acid ,inhibitory activity ,Chemical technology ,TP1-1185 - Abstract
Postbiotic metabolites produced by Lactiplantibacillus plantarum strains isolated from Malaysian food have been extensively reported for their positive effects on health. Understanding the effects of different combinations of carbon and nitrogen sources on the growth and corresponding characteristics of postbiotic metabolites produced by different strains of L. plantarum is important for various applications. Hence, the effects of different combinations of carbon (glucose, lactose, sucrose and dextrose) and nitrogen (X-SEED Kat, X-SEED Peptone, X-SEED Nucleo Advanced, Nucel875 MG, FM888 and FM902) sources on the growth of six strains of L. plantarum (RG11, RG14, RI11, RS5, TL1 and UL4) and the functional characteristics (bacteriocin inhibitory activity, antioxidant activity and lactic acid concentration) of their respective postbiotic metabolites were investigated in this study. UL4 produced the highest viable cell population with sucrose and Nucel875 nitrogen source. The UL4 strain also produced the strongest bacteriocin inhibitory activity with dextrose and FM888 nitrogen source. In comparison, the RI11 strain produced the highest lactic acid concentration with dextrose and Nucel875 nitrogen source and the highest reducing power of RS5 and TL1 postbiotic metabolites was achieved with MRS medium. In the combination of sucrose and X-Seed KAT nitrogen source, RG14 produce the highest hydroxyl radical scavenging activity. The effects of different combinations of carbon and nitrogen sources on the viable cell population of L. plantarum strains and the respective functional characteristics of postbiotic metabolites were strain dependent. The current study also revealed that fermentation media were an important factor that greatly impacted the functionalities of postbiotic metabolites due to the presence of various bioactive compounds that contributed to high antioxidant and antimicrobial properties. The results of this study will facilitate the subsequent medium design and optimisation for the development and production of specific postbiotic metabolites produced by the respective L. plantarum strain for their applications in various industries.
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- 2024
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38. The Influence of Different Polyphenols on the Digestibility of Various Kinds of Starch and the Value of the Estimated Glycemic Index
- Author
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Dominika Kwaśny, Barbara Borczak, Joanna Kapusta-Duch, and Ivan Kron
- Subjects
starch digestibility ,polyphenol ,glycemic index ,inhibitory activity ,molecular structure ,epigallocatechin gallate ,Technology ,Engineering (General). Civil engineering (General) ,TA1-2040 ,Biology (General) ,QH301-705.5 ,Physics ,QC1-999 ,Chemistry ,QD1-999 - Abstract
Considering the prevalence of diet-related diseases, new ways of preventing them are being sought. One of them is the addition of polyphenols to high-starch products to inhibit their digestibility and reduce their glycemic index. Therefore, this study aimed to investigate the differences between polyphenols popular in food ((+)catechin, epigallocatechin gallate, quercetin, kaempferol, naringenin, hesperidin, trans-ferulic acid, and p-coumaric acid), in terms of their impact on wheat, rice, potato, and maize starch digestibility. Polyphenols were added to starch separately, before and after its pasting, in one of the following doses: 5, 10, and 20 mg. Starch was digested in the presence of single polyphenols to measure RDS (rapidly digestible starch), SDS (slowly digestible starch), RS (resistant starch), and TS (total starch) content. On that basis, the SDI (starch digestion index) was calculated, and the GI (glycemic index) was estimated. The results show that polyphenols inhibit starch digestion at different levels depending on the type of tested starch and the time of polyphenol addition. However, in terms of RDS, TS, and eGI (estimated glycemic index), the greatest impact was observed for epigallocatechin gallate in a dose of 20 mg most frequently, independently of the kind of tested starch and the time of polyphenol addition.
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- 2024
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39. Retention of Phytochemical Compounds and Antioxidative Activity in Traditional Baked Dish 'proja' Made from Pigmented Maize
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Olivera Šimurina, Bojana Filipčev, Biljana Kiprovski, Zvonko Nježić, Elizabet Janić Hajnal, and Ivica Đalović
- Subjects
phenolics ,anthocyanins ,flavonoids ,inhibitory activity ,thermal processing ,phenolic compounds stability ,Chemical technology ,TP1-1185 - Abstract
Two genotypes of pigmented maize (black (BM) and red (RM)) were used as flour ingredients in several formulations of the traditional baked maize dish “proja”. This study investigated the stability of phytochemical compounds and antioxidant activity in proja as affected by baking and different acidity degrees of dough formulations. Compared to RM proja, all BM proja formulations were significantly higher in antioxidant compounds and exhibited the highest inhibitory activity (73–85%) against DPPH. There was a strong significant correlation between DPPH inhibition and total phenolics (r2 = 0.95), flavonoids (r2 = 0.96), and anthocyanins (r2 = 0.97) in baked proja. After baking, 67–85% of total phenolics were retained. The fate of flavonoids and anthocyanins after baking was variable: from 70% degradation to liberation. Dough acidity significantly and positively affected the content of phenolics, flavonoids, and anthocyanins in BM proja (r2 = 0.70, 0.82, and 0.47, respectively). Baking increased antioxidant activity against DPPH, •OH, and O2•− radicals in proja, except for ≈10% decline of DPPH inhibition in BM proja. In RM proja, retention of inhibitory capacity against O2•− was highly correlated to flavonoid retention (r2 = 0.71). Using pigmented maize flour in proja baking resulted in proja with appreciable content of total phenolics, flavonoids, anthocyanins, and high antioxidant activity, confirming the significant improvement of the nutrient profile of this traditional food.
- Published
- 2024
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40. Evaluation of the Antifungal and Biochemical Activities of Fungicides and Biological Agents against Ginseng Sclerotinia Root Rot Caused by Sclerotinia nivalis
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Shi Feng, Chunlin Wang, Zhaoyang Xu, Baozhu Dou, Xue Wang, Lina Yang, Baohui Lu, and Jie Gao
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Sclerotinia nivalis ,fungicides ,inhibitory activity ,control effects ,biochemical mechanisms ,Panax ginseng ,Biology (General) ,QH301-705.5 - Abstract
The objective of this study was to identify effective agents for the prevention and control of ginseng Sclerotinia root rot disease caused by Sclerotinia nivalis. The inhibitory effects of 16 chemical fungicides and 10 biocontrol agents (strains) on mycelial growth and sclerotium formation in S. nivalis were determined using a plate confrontation essay. The results showed that the best chemical agents for inhibiting the mycelial growth and sclerotium formation of S. nivalis were fluconazole and fludioxonil, while Bacillus amyloliquefaciens FS6 and B. subtilis (Kono) were the best biocontrol agents (strains). The results of field trials in 2022 and 2023 showed that the control effects of fluconazole and fludioxonil on ginseng Sclerotinia root rot disease were 90.60–98.16%, and those of the biocontrol agents B. amyloliquefaciens FS6 and B. subtilis (Kono) were 94.80–97.24%, respectively. Chemical agents produced abnormal and twisted mycelia, while the biocontrol agents increased mycelial branching, dilated the mycelium tip, and revealed an abnormal balloon. All of the fungicides decreased the ergosterol content, changed the cell membrane permeability, and increased the protein and nucleic acid permeability. These results suggest that these are potential agents for controlling ginseng Sclerotinia root rot disease, and their biochemical mechanisms of chemical and biocontrol of this disease were demonstrated.
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- 2024
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41. Preparation of Artemisia argyi Polysaccharide Gelatin Microspheres and Their in Vitro Release Properties
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Yunpeng WANG, Xiaomiao ZHANG, Weihong XIE, and Yi ZHANG
- Subjects
artemisia argyi polysaccharide ,gelatin microspheres ,process optimisation ,structural characterization ,release in vitro ,α-glucosidase ,α-amylase ,inhibitory activity ,Food processing and manufacture ,TP368-456 - Abstract
Artemisia argyi polysaccharide gelatin microspheres were prepared by emulsification-chemical crosslinking method using gelatin as the boating material. The effects of the concentration of Artemisia argyi polysaccharide, gelatin mass fraction, oil-water ratio, and emulsifier concentration on the encapsulation rate and drug loading capacity of the microspheres were investigated. The optimal preparation prescription was determined by single-factor and response surface analysis. The morphology of Artemisia argyi polysaccharide gelatin microspheres was observed by scanning electron microscope (SEM). The slow-release effect and the inhibition of α-glucosidase and α-amylase activities were investigated by the determination of release degree. The results showed that the optimal prescription was as follows: The concentration of Artemisia argyi polysaccharide 15 mg/mL, oil-water ratio 3.8:1, emulsifier concentration 1.2% and the gelatin mass fraction 10.20%, and the encapsulation rate and drug loading capacity was 63.80% and 9.38% respectively. Under the SEM, the microspheres appeared round and the average particle size was 59.593 μm. The results of release degree showed that the cumulative release rate of Artemisia argyi polysaccharide was about 60% and 80% at 12 h in pH 2.5 (simulated gastric acid) and 7.4 (simulated intestinal fluid) media, respectively. The inhibition of α-glucosidase and α-amylase by microspheres releasing polysaccharides in pH7.4 release medium was 31.31% and 17.15%, respectively. It was demonstrated that the microspheres prepared from Artemisia argyi polysaccharide and gelatin had an enteric slow-release effect and specific in vitro hypoglycemic activity, which provided a theoretical basis for the development of the products of Artemisia argyi polysaccharide for regulating blood glucose.
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- 2023
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42. Pure Thymol, and its Nanoliposome and Nanoparticle Forms, Inhibit Trichomonas vaginalis Infection in Culture
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Solalehsadat Jalili, Farzaneh Mirzaei, Vahid Ramezani, Hamed Ghoshouni, and Mohsen Zabihi
- Subjects
inhibitory activity ,nanopreparations ,nanoliposomes ,thymol ,trichomonas vaginalis infection ,Toxicology. Poisons ,RA1190-1270 - Abstract
Background: There is a rising trend in the use of herbal stem cell remedies among the populace due to the belief that such remedies have all-encompassing health benefits, and without side effects. However, there is little or no scientific data reported on their safety profile. This study addressed the toxicological effects of STC-30, one of the popular polyherbal stem cell remedies used in several countries of the world including Nigeria, Ghana, Australia, among others. Methods: The inhibitory activity of thymol and the nano-preparations were evaluated qualitatively versus Metronidazole against T. vaginalis in TYI-S33 culture medium. The live T. vaginalis parasites were counted on a hemocytometer, the inhibition rate was assessed and the data analyzed statistically. Results: Thymol and its two nanopreparations at varying concentrations inhibited T. vaginalis in culture after 24, 48, or 72 hours of incubation. The inhibition of T. vaginalis was also achieved in culture with Metronidazole at 65 µg/ml. Conclusion: The percent inhibition of T. vaginalis by thymol and its nanopreparations depended on the duration of incubation and the concentration. Thymol and its nanoliposome preparation showed a lower inhibitory effect (IC50) on T. vaginalis than that of the thymol nanoparticles after 24 or 48 hours of treatment. However, the efficacy of the three thymol forms did not significantly differ after 72 hours of treatment.
- Published
- 2023
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43. Isolation and identification of active ingredients and biological activity of Dioscorea nipponica Makino
- Author
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Guangqing Xia, Guanshu Zhao, Shichun Pei, Yanping Zheng, Hao Zang, and Li Li
- Subjects
Dioscorea nipponica Makino ,Active ingredients ,Separation and identification ,Antioxidant activity ,Inhibitory activity ,Other systems of medicine ,RZ201-999 - Abstract
Abstract This study reported the isolation and identification of bioactive compounds from Dioscorea nipponica Makino, a plant used in traditional medicine for various ailments. Nine compounds were isolated, including a new compound named as diosniposide E, which was elucidated by analyzing its 1H-NMR, 13C-NMR, DEPT, COSY, HMBC and MS data and comparing them with data available in literature. The other eight compounds were identified as known compounds. Theoretical calculations of energy and the generation of a molecular electrostatic potential surface map were employed to assess the antioxidant capacity of nine compounds, the calculation results exhibited that compounds 5 and 6 had strong antioxidant capacities. To further evaluate the antioxidant activities of the investigated compounds, the DPPH and ABTS assays were conducted. The results from the DPPH scavenging activity test revealed that compounds 4–6 exhibited enhanced scavenging activities compared to L-ascorbic acid, while displaying similar efficacy to trolox. Moreover, the ABTS scavenging activities of compounds 4–6 were found to surpass those of L-ascorbic acid and trolox. In terms of α-glucosidase inhibition, compounds 3 and 4 displayed remarkable inhibitory activities that surpassed the effects of acarbose. Additionally, compound 2 exhibited potent anticholinesterase activities, outperforming donepezil. This research provides insights into the potential bioactive compounds present in Dioscorea nipponica Makino and may contribute to its use in traditional medicine.
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- 2023
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44. Gene expression levels and inhibitory effect of 7-[(7-methoxy-4,5-dihydro-1H-benzo[g]indazol-3-yl)carbonyl]-2-phenyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]Pyrimidin-9(1H)-one (MCL) against AP2-I and BDP1 in malaria experimental models
- Author
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David O Oladejo, Dorathy O Anzaku, Collins O Mamudu, Temitope Elugbadebo, Titilope M Dokunmu, Ezekiel F Adebiyi, and Emeka EJ Iweala
- Subjects
Plasmodium falciparum ,Plasmodium berghei ,Antimalarial drug resistance ,Gene expression ,MCL ,Inhibitory activity ,Science - Abstract
Resistance to antimalarial drugs leads a global recurrence of malaria, posing a significant challenge to malaria control. This study aimed to assess gene expression and resistance profiles in clinical isolates, and validate the inhibitory effect of MCL compound against PbAP2-I and PbBDP1 genes in vivo. Malaria prevalence rate throughout the clinical study period stood at 12.24%. Blood samples were obtained from 182 malaria outpatients and 30 P. berghei-infected mice treated with varying MCL concentrations. DNA and RNA were extracted. PfAP2-I, PfBDP1, PfMDR1, and PfK13 genes were amplified using Real-time qPCR and sequenced for mutation profiling. Relative gene expression of AP2-I and BDP1 genes in P. falciparum and P. berghei-treated mice was carried out by Reverse-transcription PCR. The data were analyzed using ANOVA at P
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- 2024
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45. Study on the Inhibitory Activity of Benzo[d]imidazo[2,1-b]thiazole Compounds Containing Chromone in Lung Cancer Cells.
- Author
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Lujing, He, Ting, He, Longhui, Li, Xue, Jiang, Xiaoyan, Liu, Yuxin, Zhang, Shengjun, Li, Feng, Li, Qingsong, Zhou, Qidong, Tu, Jielian, Wu, and Shanshan, Luo
- Subjects
- *
LUNG cancer , *CANCER cells , *CONDENSATION reactions , *ANTINEOPLASTIC agents , *DEATH rate , *THIAZOLES , *RING formation (Chemistry) - Abstract
In recent years, lung cancer has become one of the most common malignant tumors in the world, which seriously threatens the life and health of mankind. Lung cancer is also the most common cancer in China. According to the latest report released by the National Cancer Center, the incidence and fatality rate of lung cancer in China rank first among malignant tumors, which has brought great disease burden to the Chinese. In this paper, using ethyl acetoacetate as the starting material, eight benzo[d]imidazolium[2,1-b]thiazole target compounds containing chromone were synthesized in five steps through alpha halogenation, cyclization, hydrolysis, condensation and cyclization reaction. MTT assay was used to evaluate the in vitro inhibitory activity of the target compounds on A549 and H2228 cancer cells. The IC50 values of the target compounds to A549 and H2228 cell lines ranged from 17.63 to 369.09 μmol/L. Some target compounds have moderate anti-tumor activity in vitro, which could be used to prepare related anti-tumor drugs for lung cancer. [ABSTRACT FROM AUTHOR]
- Published
- 2023
- Full Text
- View/download PDF
46. The Inhibitory Effect of Conocarpus Lancifolius Leaf Extract on Protease Produced by Clinical Pseudomonas Aeruginosa Isolate.
- Author
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K. A., Asawer. and Shawkat, M. S.
- Subjects
- *
PSEUDOMONAS aeruginosa , *PROTEOLYTIC enzymes , *RHAMNOLIPIDS , *PLANT extracts , *SKIM milk - Abstract
The study was aimed at inhibiting the protease produced by Pseudomonas aeruginosa using an 80% alcoholic extract of Conocarpus lancifolius leaves. A total of 146 isolates of P. aeruginosa that were isolated and identified by microscopic and biochemical tests were 51 isolates submitted to primary and secondary screening techniques in order to choose the qualified P. aeruginosa isolate for protease synthesis. Among these isolates, forty-seven isolates showed hydrolysis zones on skim milk media (primary screening); six isolates were chosen for secondary screening. The result revealed that P. aeruginosa P51 had the highest ability to produce the enzyme, with a specific activity of 15.9 U/mg protein. In addition, the study included extracting the leaves of C. lancifolius using 80% ethanolic alcohol and conducting the GC-MC assay and the HPLC assay of the plant extract. The results revealed a significantly decreased specific activity of protease from 15.9 to 1.2 U/mg after treatment with 0.8 µg/ml of alcoholic extract of C. lancifolius leaves. [ABSTRACT FROM AUTHOR]
- Published
- 2023
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47. Quantitative tools in microbial and chemical risk assessment.
- Author
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Zabulionė, Aelita and Valdramidis, Vasilis P
- Subjects
- *
FOOD labeling , *RISK assessment , *LACTIC acid bacteria , *FOOD pathogens , *SOFTWARE development tools , *FOOD additives - Abstract
The popularity of biological origin food protection substances is driven by demands from consumers for natural and clean label product, increasing various food‐related safety and health concerns and sustainability issues. Lactic acid bacteria (LAB) are most promising because they are a large group of beneficial microorganisms commonly used in food protection due to their ability to inhibit the growth of pathogenic bacteria and enhance food safety. Extensive scientific research has been conducted to understand the mechanisms by which LAB exert their protective effects in various food systems. Even though LAB activity against various food pathogens and spoilers is distinguished, use of cell‐free supernatant (CFS) is still under investigation. This report is dedicated to present how qualitative measures can elaborate in new bacteria‐origin food additive investigation. As part of the EU‐FORA programme, the fellow was involved in the risk assessment tasks and projects which include gaining basic knowledge in predicative microbiology fundamentals, including different types of modelling strategies; delivering essential understanding about experimental design, knowledge in three specific software tools (MATLAB, GInaFiT and DMFit) and gained overall understanding what are the main differences while modelling growth or inactivation models. Secondary activities were included as a way to expand competences beyond qualitative measures to overall all activities done regarding risk assessment and build a strong network of food safety experts and professionals to continue engaging in risk assessment beyond fellowship programme. [ABSTRACT FROM AUTHOR]
- Published
- 2023
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48. Inhibitory Activity of 4-Benzylidene Oxazolones Derivatives of Cinnamic Acid on Human Acetylcholinesterase and Cognitive Improvements in a Mouse Model.
- Author
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Ramírez-Ruiz, Alma Marisol, Ávila-Cossío, Martha Elena, Estolano-Cobián, Arturo, Cornejo-Bravo, José Manuel, Martinez, Ana Laura, Córdova-Guerrero, Iván, Cota-Ramírez, Bibiana Roselly, Carranza-Ambriz, Krysta Paola, Rivero, Ignacio A., and Serrano-Medina, Aracely
- Subjects
- *
CINNAMIC acid derivatives , *ACETYLCHOLINESTERASE , *RECOGNITION (Psychology) , *LABORATORY mice , *ANIMAL disease models - Abstract
We synthesized seven (Z)-benzylidene-2-(E)-styryloxazol-5(4H)-ones derivatives of cinnamic acid and evaluated the ability of these compounds to inhibit human acetylcholinesterase (hAChE). The most potent compound was evaluated for cognitive improvement in short-term memory. The seven compounds reversibly inhibited the hAChE between 51 and 75% at 300 μM, showed an affinity (Ki) from 2 to 198 μM, and an IC50 from 9 to 246 μM. Molecular docking studies revealed that all binding moieties are involved in the non-covalent interactions with hAChE for all compounds. In addition, in silico pharmacokinetic analysis was carried out to predict the compounds' blood–brain barrier (BBB) permeability. The most potent inhibitor of hAChE significantly improved cognitive impairment in a modified Y-maze test (5 μmol/kg) and an Object Recognition Test (10 μmol/kg). Our results can help the rational design of hAChE inhibitors to work as potential candidates for treating cognitive disorders. [ABSTRACT FROM AUTHOR]
- Published
- 2023
- Full Text
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49. Impact of pyraclostrobin on the growth of Fusarium pseudograminearum and its control efficacy against wheat crown rot in Henan Province, China.
- Author
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Hou, Ying, Chen, Yawei, Wang, Lili, Zheng, Yiheng, Liu, Shengming, and Xu, Jianqiang
- Subjects
FUSARIUM ,FIELD research ,CARBENDAZIM ,CONIDIA ,WHEAT ,FUNGICIDES - Abstract
Fusarium crown rot of wheat (FCR) is mainly caused by Fusarium pseudograminearum and is a major disease in the Huang-huai wheat growing region in China, leading to a potential yield loss. In order to evaluate the effect of pyraclostrobin on the growth of F. pseudograminearum and its control efficacy, the inhibitory activity of pyraclostrobin against the growth of F. pseudograminearum was studied, and field trials of pyraclostrobin against FCR was carried out. The results showed that pyraclostrobin had strong inhibitory effect on four growth stages of F. pseudograminearum. The EC
50 value of pyraclostrobin to mycelial growth was 0.1168–10.3378 μg/mL with an average of (3.5348 ± 3.0044) μg/mL, and with the shortening of branch spacing, the branching number increased as well as the bending of the hyphal apex at the edge of the mycelia. The EC50 value of pyraclostrobin on conidial germination was 0.0052–0.2498 μg/mL with an average of (0.0782 ± 0.0504) μg/mL, and there was an increased chance that conidia will germinate from intermediate cells. The EC50 value of pyraclostrobin on germ tube elongation was 0.0244–0.0605 μg/mL, which could make the middle cells of the conidia to swell and become deformed, but the teratogenic effect on the germ tube was not obvious. Pyraclostrobin can delay conidia sporulation time and make the conidia cells enlarged and deformed. The EC50 value of sporulation was 0.0170–0.0225 μg/mL. The results of field trials in Xin'an County and Yichuan County of Luoyang City showed that compared with carbendazim, pyraclostrobin had higher control effect on FCR at the jointing stage and the filling stage, with the control effect being more than 50%. It also reduced the rate of white spikes of wheat at the milky stage, but the control effect of pyraclostrobin at the filling stage decreased. At the same time, pyraclostrobin soaking increased the plant height, stem girth and 1,000 grain weight of wheat. Pyraclostrobin could be used as an alternative fungicide in the integrated management of FCR. [ABSTRACT FROM AUTHOR]- Published
- 2023
- Full Text
- View/download PDF
50. 粗毛纤孔菌子实体提取物体外对癌细胞的抑制作用 及化学成分分析.
- Author
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昝立峰, 郭海燕, 杨香瑜, and 乔莉娟
- Subjects
FRUITING bodies (Fungi) ,HELA cells ,TANDEM mass spectrometry ,CELL lines ,POLYPHENOLS ,ETHANOL ,ETHYL acetate - Abstract
Copyright of Acta Edulis Fungi is the property of Acta Edulis Fungi and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)
- Published
- 2023
- Full Text
- View/download PDF
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