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Antioxidant,antimicrobial,and α-glucosidase inhibitory activities of saponin extracts from walnut(Juglans regia L.) leaves 被引量:1
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作者 Youssef Elouafy Adil El Yadini +9 位作者 Salma Mortada Mohamed Hnini Hicham Harhar Asaad Khalid Ashraf NAbdalla Abdelhakim Bouyahya Khang Wen Goh Long Chiau Ming My El Abbes Faouzi Mohamed Tabyaoui 《Asian Pacific Journal of Tropical Biomedicine》 SCIE CAS 2023年第2期60-69,共10页
Objective:To investigate the relationship between triterpenoid saponin content and antioxidant,antimicrobial,and α-glucosidase inhibitory activities of 70%ethanolic,butanolic,aqueous,supernate and precipitate extract... Objective:To investigate the relationship between triterpenoid saponin content and antioxidant,antimicrobial,and α-glucosidase inhibitory activities of 70%ethanolic,butanolic,aqueous,supernate and precipitate extracts of Juglans regia leaves.Methods:Triterpenoid saponins of different Juglans regia leaf extracts were measured by the vanillin method.Antioxidant activity was evaluated against DPPH and ABTS free radicals.We also assessed α-glucosidase inhibitory and antimicrobial activities of the leaf extracts.Pearson’s correlation coefficient was evaluated to determine the correlation between the saponin content and biological activities.Results:The butanolic extract was most effective against DPPH with an IC50of 6.63μg/mL,while the aqueous extract showed the highest scavenging activity against ABTS free radical with an IC50of 42.27μg/mL.Pearson’s correlation analysis indicated a strong negative correlation (r=-0.956) between DPPH radical scavenging activity (IC50) and the saponin content in the samples examined.In addition,the aqueous extract showed the best α-glucosidase inhibitory activity compared with other extracts.All the extracts had fair antibacterial activity against Bacillus subtilis,Escherichia coli,and Klebsiella pneumoniae except for the aqueous extract.Conclusions:Juglans regia extracts show potent antioxidant,antimicrobial,and α-glucosidase inhibitory activities.There is a correlation between saponin levels in Juglans regia leaf extracts and the studied activities.However,additional research is required to establish these relationships by identifying the specific saponin molecules responsible for these activities and elucidating their mechanisms of action. 展开更多
关键词 Juglans regia leaves Triterpenoid saponin Antioxidant activity DPPH ABTS Antidiabetic activity α-glucosidase Antimicrobial activity
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α-Glucosidase inhibitors isolated from medicinal plants 被引量:3
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作者 Zhenhua Yin Wei Zhang +2 位作者 Fajin Feng Yong Zhang Wenyi Kang 《Food Science and Human Wellness》 SCIE 2014年第3期136-174,共39页
Objective:α-Glucosidase inhibitors can be used as a new class of antidiabetic drug.By competitively inhibiting glycosidase activity,these inhibitors help to prevent the fast breakdown of sugars and thereby control th... Objective:α-Glucosidase inhibitors can be used as a new class of antidiabetic drug.By competitively inhibiting glycosidase activity,these inhibitors help to prevent the fast breakdown of sugars and thereby control the blood sugar level.This study provides a wealth of information aboutα-glucosidase inhibitors isolated from medicinal plants;this knowledge will be useful in finding more potent antidiabetic candidates from the natural resources for the clinical development of antidiabetic therapeutics.Results:411 compounds exhibitingα-glucosidase inhibitory activity were summarized and isolated them from medicinal plants.The compound classes isolated include:terpenes(61)from 14 genus,alkaloids(37)from 11 genus,quinines(49)from 4 genus,flavonoids(103)from 24 genus,phenols(37)from 9 genus,phenylpropanoids(73)from 20 genus,sterides(8)from 5 genus,and other types of compounds(43).Conclusion:Compounds withα-glucosidase inhibitory activity are abundant in nature and can be obtained from several sources.They have highα-glucosidase inhibitory potential,and can be clinically developed for treating diabetes mellitus. 展开更多
关键词 α-glucosidase inhibitor inhibitory activity Medicinal plants
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Evaluation of bioactive flavonoids in Citri Reticulatae Pericarpium from different regions and its association with antioxidant andα-glucosidase inhibitory activities 被引量:1
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作者 Na Liu Jia-Chen Sun +4 位作者 Wen-Na Yang Di Liang Lan-Ping Guo Xia Li Wen-Yuan Gao 《Traditional Medicine Research》 2022年第1期1-9,共9页
Background:To explore the differences of 14 batches of Citri Reticulatae Pericarpium from different regions.Methods:The main aim of this study was to develop a high-performance liquid chromatography method-photodiode ... Background:To explore the differences of 14 batches of Citri Reticulatae Pericarpium from different regions.Methods:The main aim of this study was to develop a high-performance liquid chromatography method-photodiode array detection for determining the contents of five flavonoids and the chromatographic fingerprints of Citri Reticulatae Pericarpium from different regions.Theα-glucosidase inhibitory activities and antioxidant properties of Citri Reticulatae Pericarpium,based on free-radical scavenging assays against 1,1-diphenyl-2-picrylhydrazyl,2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid),and hydroxyl radicals,were estimated and compared.Results:Among the tested compounds,the content of hesperidin(13.386-68.235 mg/g)was the highest and that of hesperitin(0.045-0.277 mg/g)was the lowest.In comparing different sources of Citri Reticulatae Pericarpium,the contents of narirutin in Citri Reticulatae Pericarpium from Guangdong(0.824-0.851 mg/g)and Sichuan(1.069-1.204 mg/g)provinces of China were lower than in other provinces.In contrast,nobiletin(8.429-12.237 mg/g)and tangeretin(3.947-4.613 mg/g)were most abundant in Guangdong sources of Citri Reticulatae Pericarpium,followed by samples from Sichuan Province(nobiletin:6.761-7.658 mg/g;tangeretin:3.422-3.933 mg/g).Correlation analysis showed that nobiletin and tangeretin were the main contributors to the antioxidant capacity,and narirutin was the main active component inhibiting theα-glucosidase activity of Citri Reticulatae Pericarpium.Conclusion:This work revealed that the intrinsic quality of Citri Reticulatae Pericarpium was affected by different growing regions,which provides a scientific basis for controlling the quality of Citri Reticulatae Pericarpium and rationally developing and utilizing Citri Reticulatae Pericarpium. 展开更多
关键词 Citri Reticulatae Pericarpium FLAVONOIDS HPLC-PDA antioxidant activity α-glucosidase inhibitory activity
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α-Glucosidase inhibitor produced by an endophytic fungus, Xylariaceae sp. QGS 01 from Quercus gilva Blume 被引量:1
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作者 Anastasia Wheni Indrianingsih Sanro Tachibana 《Food Science and Human Wellness》 SCIE 2017年第2期88-95,共8页
Xylariaceae sp.QGS 01,an endophytic fungus isolated from the stem of Quercus gilva Blume showed high-glucosidase inhibitory activity.α-Glucosidase inhibitor have the role as one of carbohydrate-hydrolyzing enzymes to... Xylariaceae sp.QGS 01,an endophytic fungus isolated from the stem of Quercus gilva Blume showed high-glucosidase inhibitory activity.α-Glucosidase inhibitor have the role as one of carbohydrate-hydrolyzing enzymes to postpone absorption of glucose in the digestive organs.The α-glucosidase inhibitor constituents were isolated from the ethyl acetate extract of the mycellium of endophytic fungi Xylariaceae sp.QGS 01 using a bioassay-guided fractionation technique.Further separation and purification of the active fraction led to the isolation of constituents with strong inhibitory activities against-glucosidase:8-hydroxy-6,7-dimethoxy-3-methylisocoumarine(1)with inhibitory concentration(IC50)values against-glucosidase from Saccharomyces cerevisiae of 41.75μg/mL,while quercetin as the standard had an IC50 value of 4.80g/mL.The results of the present study showed that the endophytic fungus Xylariaceae sp.QGS 01 is potentially a rich source of antidiabetic medicine. 展开更多
关键词 Endophytic fungi Quercus qilva Blume α-glucosidase inhibitory activity Xylariaceae sp. Isocoumarine derivative
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Cucurbitane-Type Triterpene Glycosides from Momordica charantia and Their α-Glucosidase Inhibitory Activities
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作者 Ya Gao Jian-Chao Chen +3 位作者 Xing-Rong Peng Zhong-Rong Li Hai-Guo Su Ming-Hua Qiu 《Natural Products and Bioprospecting》 CAS 2020年第3期153-161,共9页
Ten cucurbitane-type triterpene glycosides,including five new compounds named charantosides H(1),J(2),K(3),momor-characoside A(4),goyaglycoside-l(5),and five known compounds(6-10),were isolated from the EtOAc extract ... Ten cucurbitane-type triterpene glycosides,including five new compounds named charantosides H(1),J(2),K(3),momor-characoside A(4),goyaglycoside-l(5),and five known compounds(6-10),were isolated from the EtOAc extract of Momor-dica charantia fruits.The chemical structures of these compounds were identified by 1D and 2D NMR and HRESIMS spectroscopic analyses.Configurations of new compounds were determined by ROESY correlations and comparison of their 13C NMR data with literature reported values.All compounds were evaluated for their inhibition againstα-glucosidase,in which compounds 2,5,7,8,9 showed moderate inhibitory activities with IC50 values ranging from 28.40 to 63.26μM comparing with the positive control(acarbose,IC5087.65±6.51μM). 展开更多
关键词 Momordica charantia Cucurbitane-type triterpene glycosides α-glucosidase inhibitory activity
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Antioxidant and α-glucosidase inhibitor activities of natural compounds isolated from Quercus gilva Blume leaves 被引量:4
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作者 Anastasia Wheni Indrianingsih Sanro Tachibana +1 位作者 Rizna Triana Dewi Kazutaka Itoh 《Asian Pacific Journal of Tropical Biomedicine》 SCIE CAS 2015年第9期722-728,共7页
Objective: To isolate and investigate antioxidant and α-glucosidase inhibitor compounds in the leaves of Quercus gilva Blume(Q. gilva).Methods: Dry leaves of Q. gilva were extracted with methanol and the methanolic e... Objective: To isolate and investigate antioxidant and α-glucosidase inhibitor compounds in the leaves of Quercus gilva Blume(Q. gilva).Methods: Dry leaves of Q. gilva were extracted with methanol and the methanolic extract was further separated by silica gel column chromatography using several solvents with increasing polarity. The antioxidant activities of the isolated compounds were evaluated using various in vitro assays: 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity, hydrogen peroxide radical scavenging activity, β-carotene bleaching assay, and reducing power assay. The α-glucosidase inhibitory assay was conducted against α-glucosidase from Saccharomyces cerevisiae.Results: Three compounds were isolated and their structures were identii ed as catechin(1), epicatechin(2), and tiliroside(3) using an instrumental analysis. Compound 2 had higher antioxidant activity with inhibitory concentrations(IC50) of(22.55 ± 2.23) μmol/L than that of quercetin, which was used as the standard, with an IC50 of(28.08 ± 2.39) μmol/L, followed by compound 1 with IC50 of(40.86 ± 3.45) μmol/L. On the other hand, compound 3 had the lowest antioxidant activity with an IC50 of(160.24 ± 8.15) μmol/L. However, compound 3 had the highest α-glucosidase inhibitory activity with an IC50 of(28.36 ± 0.11) μmol/L, followed by compounds 1 and 2 with(168.60 ± 5.15) and(920.60 ± 10.10) μmol/L, respectively.Conclusions: The results obtained for the antioxidant activities and α-glucosidase inhibitory activities in a methanolic extract from the leaves of Q. gilva coni rmed the potential of this plant as a source of natural antioxidants and antidiabetic medicine. 展开更多
关键词 QUERCUS gilva Blume ANTIOXIDATIVE activity α-glucosidase inhibitor Lineweaver-Burk PLOT
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α-Glucosidase Inhibitory Activities of Lutein and Zeaxanthin Purified from Green Alga Chlorella ellipsoidea 被引量:4
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作者 QI Jia KIM Sang Moo 《Journal of Ocean University of China》 SCIE CAS CSCD 2018年第4期983-989,共7页
α-Glucosidase inhibitors are used therapeutically to treat type-2 diabetes mellitus. Through a bioassay-guided fractionation technique, three carotenoids,(all-E)-lutein,(all-E)-zeaxanthin and(9-Z)-zeaxanthin, were pu... α-Glucosidase inhibitors are used therapeutically to treat type-2 diabetes mellitus. Through a bioassay-guided fractionation technique, three carotenoids,(all-E)-lutein,(all-E)-zeaxanthin and(9-Z)-zeaxanthin, were purified from the green alga Chlorella ellipsoidea, in which(all-E)-lutein and(9-Z)-zeaxanthin had potent α-glucosidase inhibitory activity. IC_(50) values of(all-E)-lutein and(9-Z)-zeaxanthin were 70 and 53.5 μmol L^(-1) against Saccharomyces cerevisiae α-glucosidase, respectively, with non-competitive inhibition. In addition, IC_(50) values of(9-Z)-zeaxanthin against Bacillus stearothermophilus and rat-intestinal α-glucosidase were 805.1 and 671.2 μmol L^(-1), respectively. The K_i values of(all-E)-lutein and(9-Z)-zeaxanthin against S. cerevisiae α-glucosidase were 78.1 and 16.5 μmol L^(-1), respectively. Therefore, C. ellipsoidea carotenoids might be utilized as a novel candidate to prevent type-2 diabetes mellitus related disorders in food and medical industry. 展开更多
关键词 type-2 diabetes MELLITUS α-glucosidase inhibitor carotenoids CHLORELLA ellipsoidea
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Identification of α-glucosidase inhibitors from Clinacanthus nutans leaf extract using liquid chromatography-mass spectrometry-based metabolomics and protein-ligand interaction with molecular docking 被引量:1
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作者 Suganya Murugesu Zalikha Ibrahim +6 位作者 Qamar Uddin Ahmed Bisha Fathamah Uzir Nik Idris Nik Yusoff Vikneswari Perumal Faridah Abas Khozirah Shaari Alfi Khatib 《Journal of Pharmaceutical Analysis》 SCIE CAS CSCD 2019年第2期91-99,共9页
The present study used in vitro and in silico techniques, as well as the metabolomics approach to characterise α-glucosidase inhibitors from different fractions of Clinacanthus nutans. C. nutans is a medicinal plant ... The present study used in vitro and in silico techniques, as well as the metabolomics approach to characterise α-glucosidase inhibitors from different fractions of Clinacanthus nutans. C. nutans is a medicinal plant belonging to the Acanthaceae family, and is traditionally used to treat diabetes in Malaysia. nHexane, n-hexane: ethyl acetate(1:1, v/v), ethyl acetate, ethyl acetate: methanol(1:1, v/v), and methanol fractions were obtained via partitioning of the 80% methanolic crude extract. The in vitro α-glucosidase inhibitory activity was analyzed using all the fractions collected, followed by profiling of the metabolites using liquid chromatography combined with mass spectrometry. The partial least square(PLS) statistical model was developed using the SIMCA P^+14.0 software and the following four inhibitors were obtained:(1) 4,6,8-Megastigmatrien-3-one;(2) N-Isobutyl-2-nonen-6,8-diynamide;(3) 1′,2′-bis(acetyloxy)-3′,4′-didehydro-2′-hydro-β, ψ-carotene; and(4) 22-acetate-3-hydroxy-21-(6-methyl-2,4-octadienoate)-olean-12-en-28-oic acid. The in silico study performed via molecular docking with the crystal structure of yeast isomaltase(PDB code: 3 A4 A) involved a hydrogen bond and some hydrophobic interactions between the inhibitors and protein. The residues that interacted include ASN259, HID295, LYS156, ARG335,and GLY209 with a hydrogen bond, while TRP15, TYR158, VAL232, HIE280, ALA292, PRO312, LEU313,VAL313, PHE314, ARG315, TYR316, VAL319, and TRP343 with other forms of bonding. 展开更多
关键词 Clinacanthus nutans LC-MS-QTOF Metabolomics α-glucosidase inhibitorS DIABETES MOLECULAR DOCKING
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Screening ofα-glucosidase inhibitors in large-leaf yellow tea by offline bioassay coupled with liquid chromatography tandem mass spectrometry 被引量:3
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作者 You Wu Zisheng Han +8 位作者 Mingchun Wen Chi-Tang Ho Zongde Jiang Yijun Wang Na Xu Zhongwen Xie Jinsong Zhang Liang Zhang Xiaochun Wan 《Food Science and Human Wellness》 SCIE 2022年第3期627-634,共8页
Larger-leaf yellow tea(LYT)is a characteristic type of Chinese tea produced in Huoshan County,Anhui Province,which is made by mature leaves with stems.According to recent report,LYT showed competitive effects in anti-... Larger-leaf yellow tea(LYT)is a characteristic type of Chinese tea produced in Huoshan County,Anhui Province,which is made by mature leaves with stems.According to recent report,LYT showed competitive effects in anti-hyperglycemia in comparison to other teas such as green or black tea.However,the bioactive compounds of LYT are still undiscovered so far.For this purpose,5 fractions of LYT were prepared by sequential extraction.The in vitro bioassay results indicated that the ethyl acetate fraction of LYT had the strongest inhibitory effects onα-glucosidase andα-amylase.Fluorescence-quenching analysis and proteinbinding test revealed that the compounds of ethyl acetate fraction could inhibitα-glucosidase andα-amylase activities through binding to enzymes or other mechanisms.All chromatographic peaks of high-performance liquid chromatography(HPLC)of ethyl acetate fraction were separated and collected.The purified compounds were identified by liquid chromatography-mass spectrometry(LC-MS),and subsequently screened by calculating their inhibition ratio onα-glucosidase at the real concentration in LYT infusion.The results showed that(-)-epigallocatechin gallate,(-)-gallocatechin gallate,caffeine,N-ethyl-2-pyrrolidone-substituted flavan-3-ols were effective inhibitors forα-glucosidase. 展开更多
关键词 Larger-leaf yellow tea ANTI-HYPERGLYCEMIA α-glucosidase Mass spectrometry Separation
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New flavanone-monoterpene hybrids as α-glucosidase inhibitors from the root bark of Morus alba
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作者 Lin-Lin Tian Hua Zhang 《TMR Modern Herbal Medicine》 CAS 2022年第4期37-41,共5页
Objective The Morus alba root bark is a well-known Chinese herbal medicine called Sang-Bai-Pi and has often been used to relieve the hyperglycemic symptom of diabetes patients.The current work aims to further explore ... Objective The Morus alba root bark is a well-known Chinese herbal medicine called Sang-Bai-Pi and has often been used to relieve the hyperglycemic symptom of diabetes patients.The current work aims to further explore its bioactive constituents with α-glucosidase inhibitory activity for the potential treatment of diabetes.Methods A combination of different separating techniques including routine column chromatograph and HPLC especially on chiral columns were applied for the isolation of target molecules,while comprehensive spectroscopic experiments comprising MS,NMR,ECD,etc.were carried out to complete the structural assignment.The anti-hyperglycemic property of the isolates was evaluated by an in vitro α-glucosidase inhibitory bioassay.Results Two pairs of new flavanone-monoterpene hybrid enantiomers were isolated and identified,and an interesting phenomenon of mutual transformation between these cometabolites were detected,which resulted in their regio-isomerization and enantiomerization.The bioassay results revealed remarkable α-glucosidase inhibitory activity for these fascinating molecules.Conclusions The Morus alba root bark is a rich source of bioactive flavonoid derivatives and deserves further investigations to develop new potential chemotherapies for diabetes control and treatment. 展开更多
关键词 Morus alba Flavanone Regio-isomerization ENANTIOMERIZATION α-glucosidase inhibition
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Blood glucose-lowering activity of protocatechuic acid is mediated by inhibiting a-glucosidase
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作者 Huafang Ding Shouhe Huang +6 位作者 Chui Yiu Chook Erika Kwek Chi Yan Kaying Ma Jianhui Liu Hanyue Zhu Zhenyu Chen 《Food Science and Human Wellness》 SCIE CSCD 2024年第3期1212-1219,共8页
α-Glucosidase inhibitors are effective in controlling postprandial hyperglycemia,which play crucial roles in the management of type 2 diabetes.Protocatechuic acid(PCA)is one of phenolic acids existing not only in var... α-Glucosidase inhibitors are effective in controlling postprandial hyperglycemia,which play crucial roles in the management of type 2 diabetes.Protocatechuic acid(PCA)is one of phenolic acids existing not only in various plant foods but also as a major microbial metabolite of dietary anthocyanins in the large colon.The present study investigated the inhibitory mechanism of PCA on a-glucosidase in vitro and examined its effect on postprandial blood glucose levels in vivo.Results from in vitro experiments demonstrated that PCA was a mix-type inhibitor of a-glucosidase.Driven by hydrogen bonds and van der Waals interactions,PCA reversibly bound withα-glucosidase to form a stable a-glucosidase-PCA complex in a spontaneous manner.The computational simulation found that PCA could insert into the active cavity of a-glucosidase and establish hydrogen bonds with catalytic amino acid residues.PCA binding aroused the steric hindrance for substrates to enter active sites and caused the structural changes of interacted catalytic amino acid residues.PCA also exhibited postprandial hypoglycemic capacity in diabetic mice.This study may provide the theoretical basis for the application of PCA as an active ingredient of functional foods in dietary management of diabetes. 展开更多
关键词 Protocatechuic acid α-glucosidase Postprandial hyperglycemia Inhibition mechanism
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Bioassay-guided isolation of α-Glucosidase inhibitory constituents from Hypericum sampsonii
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作者 TAO Linlan XU Shuangyu +6 位作者 ZHANG Zizhen LI Yanan YANG Jue GU Wei YI Ping HAO Xiaojiang YUAN Chunmao 《Chinese Journal of Natural Medicines》 SCIE CAS CSCD 2023年第6期443-453,共11页
This study employed the α-glucosidase inhibitory activity model as an anti-diabetic assay and implemented a bioactivity-guided isolation strategy to identify novel natural compounds with potential therapeutic propert... This study employed the α-glucosidase inhibitory activity model as an anti-diabetic assay and implemented a bioactivity-guided isolation strategy to identify novel natural compounds with potential therapeutic properties.Hypericum sampsonii was investigated,leading to the isolation of two highly modified seco-polycyclic polyprenylated acylphloroglucinols(PPAPs)(1 and 2),eight phenolic derivatives(3-10),and four terpene derivatives(11-14).The structures of compounds 1 and 2,featuring an unprecedented octahydro-2H-chromen-2-one ring system,were fully characterized using extensive spectroscopic data and quantum chemistry calculations.Six compounds(1,5-7,9,and 14)exhibited potential inhibitory effects against α-glucosidase,with IC_(50) values ranging from 0.050±0.0016 to 366.70±11.08μg·mL^(-1).Notably,compound 5(0.050±0.0016μg·mL^(-1))was identified as the most potential α-glucosidase inhibitor,with an inhibitory effect about 6900 times stronger than the positive control,acarbose(IC_(50)=346.63±15.65μg·mL^(-1)).A docking study was conducted to predict molecular interactions between two compounds(1 and 5)and α-glucosidase,and the hypothetical biosynthetic pathways of the two unprecedented seco-PPAPs were proposed. 展开更多
关键词 Hypericum sampsonii Chemical constituents Structure elucidation α-glucosidase Molecular docking
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A New Alkaloid from Bombycis Feculae and Its α-Glucosidase Inhibitory Activity 被引量:2
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作者 ZHU Yuan-yuan1,WANG Zhi-hong2,QI Hui1,BAI Gang1 1.Tianjin Key Laboratory of Molecular Drug Research,College of Pharmacy,Nankai University,Tianjin 300071,China 2.College of Chemistry,Nankai University,Tianjin 300071,China 《Chinese Herbal Medicines》 CAS 2011年第1期64-65,74,共3页
Objective To study the chemical constituents of Bombycis Feculae.Methods Chemical constituents were isolated by HPLC-ELSD.The structures of the isolated compounds were determined by spectral means.Results Two compound... Objective To study the chemical constituents of Bombycis Feculae.Methods Chemical constituents were isolated by HPLC-ELSD.The structures of the isolated compounds were determined by spectral means.Results Two compounds were isolated and identified as 1-deoxynojirimycin(1)and(2R,3R,5R)-2-(hydroxymethyl) piperidine-3,5-diol,named as 1,3-dideoxygalatonojirimycin(2).Conclusion Compound 2 is a new alkaloid.The extract of Bombycis Feculae,compound 1 and compound 2 show inhibitory activities againstα-glucosidase. 展开更多
关键词 ALKALOID Bombycis Feculae 1-DEOXYNOJIRIMYCIN 1 3-dideoxygalatonojirimycin α-glucosidase inhibitor
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Novel carbohydrate-triazole derivatives as potentialα-glucosidase inhibitors 被引量:2
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作者 ZHANG Zi-Pei XUE Wan-Ying +3 位作者 HU Jian-Xing XIONG De-Cai WU Yan-Fen YE Xin-Shan 《Chinese Journal of Natural Medicines》 SCIE CAS CSCD 2020年第10期729-737,共9页
A series of novel pyrano[2,3-d]trizaole compounds were synthesized and theirα-glucosidase inhibitory activities were evaluated by in vitro enzyme assay.The experimental data demonstrated that compound 10 f showed up ... A series of novel pyrano[2,3-d]trizaole compounds were synthesized and theirα-glucosidase inhibitory activities were evaluated by in vitro enzyme assay.The experimental data demonstrated that compound 10 f showed up to 10-fold higher inhibition(IC5074.0±1.3μmol·L-1)than acarbose.The molecular docking revealed that compound 10 f could bind toα-glucosidase via the hydrophobic,π-πstacking,and hydrogen bonding interactions.The results may benefit further structural modifications to find new and potentα-glucosidase inhibitors. 展开更多
关键词 Pyrano[2 3-d]trizaole α-glucosidase inhibitor Enzyme assay Molecular docking
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Bioactive constituents from the leaves of Quercus phillyraeoides A.Gray for-glucosidase inhibitor activity with concurrent antioxidant activity 被引量:2
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作者 Anastasia Wheni Indrianingsih Sanro Tachibana 《Food Science and Human Wellness》 SCIE 2016年第2期85-94,共10页
Severalα-glucosidase inhibitory constituents were isolated from the methanolic extract of the leaves of Quercus phillyraeoides A.Gray(Q.phillyraeoides)using a bioassay-guided fractionation technique.Further separatio... Severalα-glucosidase inhibitory constituents were isolated from the methanolic extract of the leaves of Quercus phillyraeoides A.Gray(Q.phillyraeoides)using a bioassay-guided fractionation technique.Further separation and purification of the methanol-soluble fraction led to the isolation of constituents with moderate and strong inhibitory activities againstα-glucosidase:α-sitosterol-d-glucoside(1)and condensed tannin fractions(2,3,4,5,and 6).Compound 1 and fractions 2-6 had inhibitory concentration(IC50)values againstm-glucosidase from Saccharomyces cerevisiae of 118.8,2.79,2.78,3.10,2.60,and 3.14μg/mL,respectively,while quercetin as the standard had an IC50 value of 4.80mg/mL.Furthermore,the significant antioxidant activities were evaluated using several assays,such as the DPPH radical scavenging,hydrogen peroxide radical scavenging,reducing power,andβ-carotene-linoleate bleaching assays,and the results suggested that the isolated constituents showed their possible application for treating the hyperglycemia-induced oxidative stress.The results of the present study showed the potential of Q.phillyraeoides as a rich source of natural antidiabetic medicine. 展开更多
关键词 Quercus phillyraeoides A.Gray α-glucosidase inhibitor Antioxidative activity Lineweaver–Burk plot
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Tsaokols A and B,unusual flavanol-monoterpenoid hybrids asα-glucosidase inhibitors from Amomum tsao-ko
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作者 Xiao-Feng He Ji-Jun Chen +5 位作者 Tian-Ze Li Jing Hu Xu-Ke Zhang Yuan-Qiang Guo Xue-Mei Zhang Chang-An Geng 《Chinese Chemical Letters》 SCIE CAS CSCD 2021年第3期1202-1205,共4页
Tsaokols A(1)and B(2),two complicated flavanol-monoterpenoid hybrids,were isolated from the dried fruits of Amomum tsao-ko under the guidance of LCMS and bioassay.Their structures were determined by extensive spectros... Tsaokols A(1)and B(2),two complicated flavanol-monoterpenoid hybrids,were isolated from the dried fruits of Amomum tsao-ko under the guidance of LCMS and bioassay.Their structures were determined by extensive spectroscopic analyses and electronic circular dichroism(ECD)calculations.Compounds 1 and2 shared a flavanol backbone fused with 5/7 and 5/6 bicyclic monoterpenoid scaffolds,which were biogenetically condensed by Michael addition and acetalization.Compounds 1 and 2 exhibited significantα-glucosidase inhibitory activity with IC_(50)values of 18.8 and 38.6μmol/L(acarbose,IC_(50)=213μmol/L).Docking study supported the strong interactions of 1 and 2 bonding with enzyme by mainly hydrophobic and hydrogen-bond effects.Compounds 1 and 2 could be fast distinguished by the diagnostic ions at m/z 289 and 313 in negative MS^(2)experiments. 展开更多
关键词 Amomum tsao-ko ZINGIBERACEAE Flavanol-monoterpenoid hybrids α-glucosidase inhibitors
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Discovery of pyrogallol thermal reaction products from a model process of roasting coffee beans as potentα-glucosidase inhibitors
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作者 Hui Wang Xiaoli Kang +5 位作者 Shiwei Sun Yichen Yin Kun Jiang Guodong Tang Xinning Tang Wei Wang 《Food Bioscience》 SCIE 2022年第2期719-725,共7页
The roasting process of pyrogallol,a polyphenol compound distributed in coffee beverages,significantly enhanced itsα-glucosidase inhibitory activity.In this study,a bioassay-guided isolation of the thermal reaction p... The roasting process of pyrogallol,a polyphenol compound distributed in coffee beverages,significantly enhanced itsα-glucosidase inhibitory activity.In this study,a bioassay-guided isolation of the thermal reaction products of pyrogallol led to the identification of two potentα-glucosidase inhibitors,4-4′dimer of pyrogallol(4,4′-DP)and 4-5′dimer of pyrogallol(4,5′-DP).Theirα-glucosidase inhibitory activity was higher than that of pyrogallol,as evidenced by comparing the IC_(50)values(206.2±1.2μM for 4,4′-DP,187.6±2.6μM for 4,5′-DP,2660±60.1μM for pyrogallol).And the roasting products were more potentα-glucosidase inhibitors compared to acarbose(IC_(50)=695±12.7μM).Enzyme kinetics demonstrated that 4,4′-DP and 4,5′-DP inhibitedα-glucosidase in an uncompetitive and a non-competitive manner,respectively.Docking simulations revealed that the main interaction forces between these two compounds andα-glucosidase were hydrogen bonding and hydrophobic effect.These results suggested that a simple roasting process might increase theα-glucosidase inhibitory activity of pyrogallol-containing foods such as coffee beverages. 展开更多
关键词 PYROGALLOL ROASTING α-glucosidase inhibitors Inhibition type Molecular docking
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Structural Elucidation and Total Synthesis of Trichodermotin A,A Natural α-Glucosidase Inhibitor from Trichoderma asperellum
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作者 Muyuan Yu Fengqing Wang +7 位作者 Si Yao Yi Zang Chong Dai Yu Liang Mi Zhang Lianghu Gu Hucheng Zhu Yonghui Zhang 《Chinese Journal of Chemistry》 SCIE CAS CSCD 2022年第18期2219-2225,共7页
A pair of alkaloid enantiomers possessing a novel 1-oxaspiro[4.4]non-3-ene-2,7-dione skeleton,trichodermotin A(1),was obtained from the fungus Trichoderma asperellum.Spectroscopic data,X-ray diffraction,and ECD calcul... A pair of alkaloid enantiomers possessing a novel 1-oxaspiro[4.4]non-3-ene-2,7-dione skeleton,trichodermotin A(1),was obtained from the fungus Trichoderma asperellum.Spectroscopic data,X-ray diffraction,and ECD calculations were used to establish its structure and absolute configuration.(−)-1 showed significantα-glucosidase inhibitory activity(IC_(50)=10.1μmol/L vs.60.1μmol/L of positive control).A plausible biosynthetic pathway originating from L-β-phenylalanine was proposed,and a facile total synthesis was further accomplished.The key reaction of our synthetic strategy was a domino aza-Michael/lactonization in one pot,leading to the pivotal 4-amino-oxaspiro[4.4]octane scaffold. 展开更多
关键词 Trichoderma asperellum ALKALOID α-glucosidase inhibitory activity Molecular docking Total synthesis
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Screening of probiotics with efficient α-glucosidase inhibitory ability and study on the structure and function of its extracellular polysaccharide
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作者 Jia-Bin Wang Le-Yi Yu +3 位作者 Xu Zeng Jun-Wei Zheng Bin Wang Li Pan 《Food Bioscience》 SCIE 2022年第1期131-145,共15页
Inhibition ofα-glucosidase activity is an important strategy in lowering the concentration of blood sugar.In this paper,using domestic and foreign characteristic food-derived substances as the sources of lactobacillu... Inhibition ofα-glucosidase activity is an important strategy in lowering the concentration of blood sugar.In this paper,using domestic and foreign characteristic food-derived substances as the sources of lactobacillus,the performance of them were evaluated by measuring the strains’α-glucosidase inhibitory ability.Finally,the cell-free extracellular supernatants(CFS)of Lactobacillus rhamnosus LB1lac10 was determined to have the highest α-glucosidase inhibition ability.Based on the Nanopore third-generation sequencing technology platform,the genome of LB1lac10 was sequenced and functional gene annotation was performed.After that,the biological activity and structural composition of the exopolysaccharide produced by L.rhamnosus LB1lac10 were studied.The purified exopolysaccharide EPS1-1 also showed efficientα-glucosidase inhibitory ability.The structure and conformation characteristics of EPS1-1 were further analyzed.The EPS1-1 from L.rhamnosus LB1lac10 had a molecular weight of 88,650 Da,and it was mainly composed of mannose,glucuronic acid,glucose,xylose,galactose,and arabinose.From the FT-IR and NMR analyses,EPS1-1 had functional groups of a typical polysaccharide structure and contained two types of glycosidic bonds with α-configuration pyranose.The main glycosidic bond corresponded to→4)-α-D-Glcp-(1→,which might be an important reason why EPS1-1 could inhibit α-glycosidase.Thermodynamic studies showed that EPS1-1 had high heat resistance to meet the needs of food processing.The results suggested that L.rhamnosus LB1lac10 could be used as a potential probiotic to lower blood sugar,and the EPS1-1 has the potential to serve as a naturalα-glycosidase inhibitor to regulate the concentration of blood glucose. 展开更多
关键词 Lactobacillus rhamnosus α-glucosidase inhibitory activity Third-generation sequencing Extracellular polysaccharide Probiotic activity
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Inhibitory activities of microalgal fucoxanthin againstα-amylase,α-glucosidase, and glucose oxidase in 3T3-L1cells linked to type 2 diabetes 被引量:7
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作者 KAWEE-AI Arthitaya KIM Aaron Taehwan KIM Sang Moo 《Journal of Oceanology and Limnology》 SCIE CAS CSCD 2019年第3期928-937,共10页
Postprandial hyperglycemia is an early indication of type 2 diabetes and the target of many anti-diabetic and anti-obesity studies.α-Glucosidase and α-amylase are the crucial factors in regulating starch digestion a... Postprandial hyperglycemia is an early indication of type 2 diabetes and the target of many anti-diabetic and anti-obesity studies.α-Glucosidase and α-amylase are the crucial factors in regulating starch digestion and glucose absorption,making them key targets for many studies to treat postprandial hyperglycemia.We studied the inhibitory activities of microalgal fucoxanthin against rat-intestinalα-glucosidase and pancreaticα-amylase along with the antidiabetic eff ect to induce diff erentiation in 3T3-L1 pre-adipocytes using Oil Red-O staining.Fucoxanthin displayed strong hindrance activities towardα-amylase in a concentration-dependent manner,with an IC50 value of 0.68mmol/L,whereas weak inhibitory activity against α-glucosidase,with an IC 50 value of 4.75 mmol/L.Fucoxanthin also considerably elevated glucose oxidase activity in 3T3-L1 cells by 31.3%at 5μmol/L.During adipocyte differentiation,fucoxanthin showed lipid accumulation in 3T3-L1 cells with no cytotoxicity up to 20μmol/L.However,fucoxanthin had no inhibitory activity on glucose-6-phosphate dehydrogenase.These results suggest that fucoxanthin might be useful for the prevention of obesity or diabetes by inhibiting carbohydrate-hydrolyzing enzymes and lipid accumulation and be utilized as an ingredient for a functional food or dietary supplement. 展开更多
关键词 α-glucosidase AMYLASE diabetes FUCOXANTHIN glucose OXIDASE MICROALGAE
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