BIOORGANIC CHEMISTRY
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2021
·
IF 5.275
Ke Zhao,Shiwei Sun,Hui Wang,Lin Wang,Guoqing Qin,Jiahe Fan,Mengru Guo,Wei Wang
α -Glucosidase plays an important role in catalyzing the hydrolytic cleavage of disaccharides into monosaccharides. In this study, a phytochemical investigation of the potential α -glucosidase inhibitory fraction from the aerial parts of Euonymus fortunei led to the isolation and identification of two new tetracyclic triterpenoids , fortunenones A and B ( 1 – 2 ), together with 11 known triterpenoids ( 3 – 13 ). Fortunenones A and B are rare C 32 triterpenoids possessing a 24,24-dimethyl group. The partial isolated compounds were evaluated their effects on α -glucosidase, of which echinochlorin D ( 5 ), lupenone ( 7 ), wilforlide B ( 12 ), and wilforlide A ( 13 ) exhibited remarkable inhibitory effects with the half inhibitory concentration ranged from 207.2 × 10 −6 M to 388.3 × 10 −6 M compared with the positive control, acarbose. An enzyme kinetics analysis by Lineweaver-Burk plots revealed that the inhibition types of the four active compounds were all mixed inhibition. Molecular docking further revealed that hydrophobic interactions and hydrogen bonds play an important role in the inhibition of α -glucosidase activity. Our results demonstrate the potential of E. fortunei extract and its constituents to inhibit α -glucosidase.
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RSC Advances
·
2020
·Vol. 10
·期 11
·6491-6496
·
IF 3.119
Rui-Feng Mei,Ya-Xian Shi,Wei-He Duan,Hao Ding,Xiao-Ran Zhang,Le Cai,Zhong-Tao Ding
α-Terpineol (1), the main volatile constituent in some traditional Chinese medicines, has been reported to be metabolized to 4R-oleuropeic acid by the larvae of common cutworms. The present study verified that α-terpineol could be converted to 4R-oleuropeic acid (2) and (1S,2R,4R)-p-menthane-1,2,8-triol (3) by Alternaria alternata fermentation. Using shortened fermentation times, 7-hydroxy-α-terpineol (2a) was identified as an oxidative intermediate, which was consistent with the hypothesis put forward by previous studies. Cytochrome P450 enzymes were also confirmed to catalyze this biotransformation. This is the first study on the biotransformation of α-terpineol by microbial fermentation.
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Natural Product Communications
·
2019
·
IF 0.554
Chengyun He,Xiaoling Liu,Junliang Sun
Baicalein is one of the main bioactive compounds in Scutellaria baicalensis. In this study, its inhibitory mechanism against α-glucosidase from Saccharomyces cerevisiae was clarified based on experimental and molecular simulation methods. According to HPLC analysis, the α-glucosidase inhibitory activity of S. baicalensis (IC50, 6.75 ± 0.08 μg mL−1) was superior to that of acarbose (IC50, 2.52 ± 0.12 mg mL−1). The fluorescence results suggested that baicalein could form a complex with α-glucosidase at the molar ratio of 1 under the drive of hydrogen bonding and van der Waals force. Molecular docking showed that baicalein could form hydrogen bonds with Trp391, Arg428, Gly566,and Glu771 of α-glucosidase, and interacted with Phe385, Phe389, Arg387, Glu429, Phe444, Trp789, and Trp710 by hydrophobic force, which coincided with the experimental results. It can be concluded that baicalein is a potential α-glucosidase inhibitor for controlling the postprandial blood glucose level of diabetics.
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LWT-FOOD SCIENCE AND TECHNOLOGY
·
2022
·
IF 6.056
Fei Peng,Hui Huang,Jia-Xin Lin,Tao Yang,Mingyong Xie,Tao Xiong,Zhen Peng
The effects of Lactiplantibacillus plantarum NCU001043 fermentation on the physicochemical and biological properties of yacon tubers were investigated. The fermentation parameters were first optimized by single-factor tests, then an orthogonal experimental design, which resulted in production of a fermented yacon syrup with excellent sensory attributes and increased antimicrobial activity against Helicobacter pylori . The physicochemical characteristics of the yacon syrup were determined after fermentation under the optimum conditions. Although the total phenolic content of the fermented yacon syrup decreased after fermentation, its antioxidant capacity and glycosidase inhibition activity increased. Spearman correlation analysis indicated that one of the phenolic compounds, 4-hexyloxyphenol, might be the main α-amylase and α-glucosidase inhibitor. Molecular docking indicated that 4-hexyloxyphenol has a strong binding affinity for the active-sites of both enzymes. These findings will facilitate the development of yacon-based functional foods by microbial fermentation and application of Lactiplantibacillus plantarum NCU001043 in food fermentation.
研究领域:
食品科学
·
微生物学
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LWT-FOOD SCIENCE AND TECHNOLOGY
·
2023
·
IF 6
Fangliang Li,Tongjie Luo,Jiale Hou,Tao Fei,Jiachao Zhang,Lu Wang
Raspberry leaf as a tea substitute has been consumed in China for long time. In this work, the inhibitory activities of raspberry leaf-tea (RLT) extract on α -glucosidase ( α -GLU)/ α -amylase ( α -AMY) were measured, and the effects of the RLT extract on the glucose consumption of 3T-3L1 cells were also investigated. Results confirmed that RLT 70% ethanol extract (REE) exhibited strong inhibitory activities on α -GLU/ α -AMY in vitro . In addition, REE remarkably improved the glucose consumption of 3T-3L1 cells. Subsequently, eight major inhibitors including epigallocatechin gallate (EGCG), delphinidin-3- O -glucoside, cyanidin-3-rutinoside, isoorientin, procyanidin C3, dihydromyricetin, rutin, and isovitexin were screened and identified through affinity ultrafiltration combined with HPLC-MS/MS. Confirmation tests verified that these major compounds were responsible the inhibitory activities of the REE on α -GLU/ α -AMY. Molecular docking studies revealed that these inhibitors can well interact with α -GLU/ α -AMY via van der Waals force or hydrogen bonding, thus inhibiting their activities. In a short, raspberry leaf can be exploited as a promising anti-hypoglycemic material. This study provides a theoretical basis for discovering active components from medicinal plants using affinity ultra-filtration with multi-targets.
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Materials Today Communications
·
2023
·
IF 3.8
Jianhui Su,Yan Liu,Xiujing Peng,Guoxin Sun,Xuchuan Jiang
Due to the high activation energy barrier and the sporadic nature of nucleation, the temperature required for the transition from cubic dense γ-Al 2 O 3 to tripartite α-Al 2 O 3 is as high as 1100–1200 °C. In this work, a two-step strategy was employed to reduce the phase transformation temperature, and prepare α-Al 2 O 3 particles with good dispersion. As the first step, 10 nm sheet γ-Al 2 O 3 was obtained by ammonium aluminum carbonate (AACH) decomposition, which was more favorable to the crystal transformation in the next ball-milling processing. In the second step, γ-Al 2 O 3 powder with partial α-Al 2 O 3 produced in situ by ball-milling γ-Al 2 O 3 was calcined, and α-Al 2 O 3 nanoparticles were obtained at just 850 °C. The content of the α-Al 2 O 3 is determined by the Rietveld Refine method. The relationship between ball-milling time and α-Al 2 O 3 content was clarified, and the effect of α-Al 2 O 3 content on the transformation temperature and morphology of γ-Al 2 O 3 was discussed. The results showed that the α-Al 2 O 3 content rises with the increase of ball milling time, and spherical α-Al 2 O 3 nanoparticles can be obtained when the α-Al 2 O 3 content is 5 %. The addition of α-Al 2 O 3 seeds reduces the phase transition temperature but agglomeration exists. Our proposed two-step low-temperature calcination strategy is an important method for the preparation of alumina nanoparticles
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BIOORGANIC CHEMISTRY
·
2021
·
IF 5.275
Chun-Mei Hu,Wen-Jing Wang,Yuan-Na Ye,Yu Kang,Jing Lin,Pan-Pan Wu,Dong-Li Li,Li-Ping Bai,Xue-Tao Xu,Bao-Qiong Li,Kun Zhang
In this study, twenty novel cinnamic acid magnolol derivatives were synthesized, and screened for their anti-hyperglycemic potential. All synthesized compounds exhibited good to moderate α-glucosidase and α-amylase inhibitory activities with IC 50 values: 5.11 ± 1.46–90.26 ± 1.85 µM and 4.27 ± 1.51–49.28 ± 2.54 µM as compared to the standard acarbose (IC 50 : 255.44 ± 1.89 μM and 80.33 ± 2.95 μM, respectively). Compound 6j showed the strongest inhibitory activity against α-glucosidase (IC 50 = 5.11 ± 1.46 µM) and α-amylase (IC 50 = 4.27 ± 1.51 µM). Kinetic study indicated that compound 6j was reversible and a mixed type inhibitor against α-glucosidase and α-amylase. In silico studies revealed the binding interaction between 6j and two enzymes, respectively. Finally, cells cytotoxicity assay revealed that compound 6j showed low toxicity against 3 T3-L1 cells and HepG2 cells.
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JOURNAL OF MOLECULAR LIQUIDS
·
2019
·
IF 4.561
Xiaqing Wu,Mingming Hu,Xing Hu,Huafang Ding,Deming Gong,Guowen Zhang
Suppression of α- amylase and α- glucosidase is favorable for improvement of postprandial hyperglycemia. Here, the inhibitory mechanisms of epicatechin gallate (ECG) on α- amylase and α- glucosidase are explored by enzyme kinetics , spectroscopy and molecular modeling approaches. ECG was found to have strong inhibitory efficiency against α- amylase and α- glucosidase in mixed−type manners with IC 50 values of 45.30 ± 0.22 and 4.03 ± 0.01 μg/mL, respectively. ECG bound to α- amylase and α- glucosidase forming ECG– α- amylase and ECG– α- glucosidase complexes, causing the conformational changes of the enzymes. Molecular simulation exhibited that ECG located into the active pocket of the enzymes likely contributed by some major amino acid residues Gln63 and Asp197 of α- amylase, and Lys156, Ser157, Arg315 and Asp352 of α- glucosidase, which may prevent the entrance of substrate leading to a decline in enzyme activity . Meanwhile, at the constant IC 50 ratios of ECG to acarbose or epigallocatechin gallate, an obvious antagonism was observed in α- amylase inhibition , while additive and synergistic effects for α- glucosidase. These findings suggest that ECG may be a potential inhibitor of α- amylase and α- glucosidase, which could be used as a nutrient supplement for the prevention of diabetes mellitus.
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JOURNAL OF SEPARATION SCIENCE
·
2024
·Vol. 47
·期 14
·2400342
·
IF 2.8
Yue Li,Hongmei Liu,Sikai Wang,Wei Fang,Xinxin Jiang,Guoqi Zhang,Yan Zhao
In this study, a ligand fishing method for the screening of α-glucosidase inhibitors from Ginkgo biloba leaf was established for the first time using α-glucosidase immobilized on the magnetic metal-organic framework. The immobilized α-glucosidase exhibited enhanced resistance to temperature and pH, as well as good thermal stability and reusability. Two ligands, namely quercitrin and quercetin, were screened from Ginkgo biloba leaf and identified by ultra-high performance liquid chromatography-tandem mass spectrometry. The half-maximal inhibitory concentration values for quercitrin and quercetin were determined to be 105.69 ± 0.39 and 83.49 ± 0.79 µM, respectively. Molecular docking further confirmed the strong inhibitory effect of these two ligands. The proposed approach in this study demonstrates exceptional efficiency in the screening of α-glucosidase inhibitors from complex natural medicinal plants, thus exhibiting significant potential for the discovery of antidiabetic compounds.
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MOLECULES
·
2024
·Vol. 29
·期 9
·1971
·
IF 4.2
Hong-Li Huang,Shan Li,Yong-Zheng Lv,Ya-Qian Shi,Tian-Tian Pang,Ru-Fen Zhang,Wenjing Huang,Jianhui Yin,Fei Gao
A novel and efficient method for functionalizing organosulfones has been established, utilizing a visible-light-driven intermolecular radical cascade cyclization ofα-allyl-β-ketosulfones. This process employsfac-Ir(ppy)3as the photoredox catalyst andα-carbonyl alkyl bromide as the oxidizing agent. Via this approach, the substrates experience intermolecular addition ofα-carbonyl alkyl radicals to the alkene bonds, initiating a sequence of C-C bond formations that culminate in the production of organosulfone derivatives. Notably, this technique features gentle reaction conditions and an exceptional compatibility with a wide array of functional groups, making it a versatile and valuable addition to the field of organic synthesis.
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NEUROPHARMACOLOGY
·
2026
·
IF 4.7
Baixue An,Zepei Tang,Ke Hu,Pengcheng Wei,Dongting Zhangsun,Xiaopeng Zhu,Jinpeng Yu,Sulan Luo
67 single-point mutants were generated and then were assessed for properties. • The 152nd, 157th, and 195th residues of α subnuit affect selectivity for [D1G,ΔQ14]LvIC. • Combined mutations show greater impacts on the activity of [D1G,ΔQ14]LvIC. • E152K mutation in rα6/α3 most affects inhibition via ionic interaction with peptide. • The 157th and 195th residues may alter spatial conformation, affecting peptide binding potency. nAChRs containing α6 subunit (α6* nAChRs) are identified as being involved in Parkinson's disease, dyskinesia, drug addiction, and other disorders. Among these, α6β4 nAChR is recognized as a highly promising target for the development of non-opioid analgesics. However, the research advancement on α6β4 nAChR has been hindered primarily by the overlapping tissue distribution with highly homologous α3β4 nAChR, as well as the scarcity of subtype-specific ligands. Recently, the α-conotoxin analogue [D1G, ΔQ14]LvIC was identified to exhibit remarkable selectivity for rα6/α3β4 nAChR with an IC 50 of 19 nM, while showing negligible inhibitory activity against other subtypes, including closely related rα3β4 (IC 50 > 10 μM), demonstrating exceptional subtype selectivity and potency compared to previously reported ligands for this receptor. In this study, we employed a combined approach of PCR-mediated site-directed mutagenesis and two-electrode voltage clamp electrophysiology to identify the determinants governing the [D1G, ΔQ14]LvIC selectivity. 67 single-point mutants of rα6/α3β4 nAChR were generated, systematically replacing each differing residue in rα6/α3 to rα3 subunit. The activity of [D1G, ΔQ14]LvIC was subsequently assessed on the native receptor and its mutants. As the results showed, E152, I157, and T195 in rα6/α3 subunit were identified as essential for [D1G, ΔQ14]LvIC selectivity. Inverse and multiple-point mutants were subsequently constructed and assessed for further validation. Molecular modeling further shed light on the molecular basis for the unique interaction between [D1G, ΔQ14]LvIC and rα6/α3β4 nAChR. These findings advance our understanding of α6β4 nAChR-ligand interactions and pave the way for the rational design of targeted therapeutics. Download: Download high-res image (371KB) Download: Download full-size image
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Foods
·
2026
·Vol. 15
·期 11
·1972
·
IF 6
Shuang Yang,Yongxing Li,Weiyu Han,Wenhao Cao,Zhihui Hu,Zhangliang Zhu,Mei Li,Jianhui Feng,Jinfang Zhang
The global rise in metabolic disorders demands novel interventions targeting starch digestion. This study investigated two dietary phenolic acids (caffeic acid (CA) and p-hydroxycinnamic acid (p-HA)) as inhibitors of α-amylase and α-glucosidase through integrated experimental and computational approaches. Molecular docking showed distinct binding modes, and CA formed stable hydrogen bonds with catalytic residues of α-glucosidase, while p-HA interacted mainly with α-amylase via hydrophobic contacts. Enzyme kinetics revealed concentration-dependent mixed-type inhibition, with CA being more potent against α-glucosidase and p-HA against α-amylase. Spectroscopic analysis indicated both acids induced structural changes in the enzymes, with CA causing greater α-helix reduction (Δ7.03% vs. Δ2.10%) by altering the tryptophan microenvironment. Moreover, both compounds significantly suppress glucose absorption in the proximal small intestine in an ex vivo everted gut sac model, with p-HA exhibiting exceptional efficacy in the duodenum. These findings clarify structure–activity relationships and support the potential use of CA and p-HA as local intestinal agents for modulating carbohydrate absorption.
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