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Journal of Functional Foods · 2024 · IF 3.8

Inhibition and effect of almond hull extract on activities of α-amylase and α-glucosidase, and postprandial glucose in normal SD rats

Yuyang Yao,Juer Liu,Qiming Miao,Xinyue Zhu,Lu Sun,Wei Hua,Na Zhang,Guangwei Huang,Roger Ruan,Yanling Cheng,Shengquan Mi

Controlling postprandial hyperglycemia is considered as a viable prophylactic treatment for type 2 diabetes mellitus. A major strategy in decreasing postprandial glucose involves inhibition of the carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase. The aim of this study was to evaluate the hypoglycemic potential of almond hull extract in vitro and in vivo. The in vitro results showed that, among the 0 %, 30 %, 50 % and 80 % ethanol extracts of almond hull, the 50 % ethanol extracts demonstrated the most significant inhibition of digestive enzymes. With in vivo tests, the blood glucose concentration in the control rats increased sharply near the peak glucose level in 15 min, while the peak glucose level of rats loading the almond hull extract occurred in 30 min. Therefore, almond hull extract can reduce postprandial blood glucose levels and delay the time to peak by about 15 min, providing a sustained and gradual release of energy.

研究领域: 药理学 · 代谢病研究
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LWT-FOOD SCIENCE AND TECHNOLOGY · 2023 · IF 6

Natural α-glucosidase and α-amylase inhibitors from raspberry (Rubus corchorifolius L.) leaf-tea: Screening, identification and molecular docking analysis

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.

研究领域: 食品科学 · 植物化学 · 分子生物学
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LWT-FOOD SCIENCE AND TECHNOLOGY · 2019 · IF 3.714

Antioxidant activity and α-amylase and α-glucosidase inhibitory activity of a fermented tannic acid product: Trigalloylglucose

Ru-yi Li,Shaoman Wang,David Julian McClements,Yin Wan,Cheng-mei Liu,Gui-ming Fu

Small molecules with beneficial biological activities can be generated by controlled fermentation of natural food products. In this study, the fermentation products of tannic acid by Aspergillus carbonarius FCYN212 were isolated and identified. Two major chemical structures were obtained: gallic acid (GA) and 3,4,6-tri- O -galloyl- d -glucose (TGG). GA and TGG exhibited stronger free radical scavenging ability and ferric-reducing power than butylated hydroxyanisole (BHA). Additionally, TGG demonstrated significant dose-dependent enzyme inhibitory activities against α-amylase and α-glucosidase with IC 50 values of 334.6 ± 8.9 and 46.5 ± 1.6 μM, respectively. Notably, TGG was a mixed type inhibitor of α-amylase and α-glucosidase according to a Dixon plot. This study revealed the antioxidant and enzyme inhibitory potential of TGG isolated from a fermented extract of tannic acid. TGG may therefore serve as an antioxidant and antidiabetic ingredient in functional or medical foods.

研究领域: 食品科学 · 生物化学
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2021 · IF 5.279

Inhibition Mechanism of α-Amylase/α-Glucosidase by Silibinin, Its Synergism with Acarbose, and the Effect of Milk Proteins

Jichen Yang,Huan Li,Xiaoli Wang,Chuanying Zhang,Guo Feng,Xin Peng

As a natural flavonolignan, silibinin is reported to possess multiple biological activities, while the inhibitory potential of silibinin on carbohydrate-hydrolyzing enzymes is still unclear. Therefore, in this study, the inhibitory effect and underlying mechanism of silibinin against α-amylase/α-glucosidase were investigated. The results indicated that silibinin showed a strong inhibitory efficiency against α-amylase/α-glucosidase in noncompetitive manners and exhibited synergistic inhibition against α-glucosidase with acarbose. However, interestingly, the inhibitory effect of silibinin was significantly hindered in various milk protein-rich environments, but this phenomenon disappeared after simulated gastrointestinal digestion of milk proteins in vitro. Furthermore, silibinin could combine with the inactive site of α-amylase/α-glucosidase and change the microenvironment and secondary structure of the enzymes, thereby influencing the catalytic efficiency of enzymes. This research suggested that silibinin could be used as a novel carbohydrate-hydrolyzing enzyme inhibitor, and milk beverages rich in silibinin had the potential for further application in antidiabetic dietary or medicine.

研究领域: 食品科学 · 生物化学 · 药理学
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MOLECULES · 2023 ·Vol. 28 ·期 7 ·3202 · IF 4.6

Study on the Hydration of α-Pinene Catalyzed by α-Hydroxycarboxylic Acid–Boric Acid Composite Catalysts

Zhonglei Meng,Rongxiu Qin,Rusi Wen,Guiqing Li,Zhongyun Liang,Junkang Xie,Zhangqi Yang,Yonghong Zhou

In this study, seven types of α-hydroxycarboxylic acids were selected to form composite catalysts with boric acid, and their catalytic properties were studied using the catalytic hydration of α-pinene. The results showed that the composite catalyst of boric acid and tartaric acid had the highest catalytic activity. With an α-pinene, water, acetic acid, tartaric acid, and boric acid mass ratio of 10:10:25:0.5:0.4, the reaction temperature was 60 °C, the reaction time was 24 h, the conversion of α-pinene was 96.1%, and the selectivity of terpineol was 58.7%. The composite catalyst composed of boric acid and mandelic acid directly catalyzed the hydration of α-pinene in the absence of a solvent. Under the optimal conditions, the conversion of α-pinene reached 96.1%, and the selectivity of terpineol was 55.5%. When the composite catalyst catalyzed α-pinene to synthesize terpineol in one step, the terpineol was optically active, and terpineol synthesized using the two-step method with the dehydration ofp-menthane-1,8-diol monohydrate was racemic. These composite catalysts may offer good application prospects in the synthesis of terpineol.Keywords:α-hydroxycarboxylic acid–boric acid complexes;green catalyst;hydration of α-pinene;solvent-free;terpineol;p-menthane-1,8-diol monohydrate

研究领域: 催化 · 有机化学 · 绿色化学
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PLoS One · 2024 ·Vol. 19 ·期 4 ·e0299218 · IF 2.9

Synthesis of terpinyl acetate from α-pinene catalyzed by α-hydroxycarboxylic acid–boric acid composite catalyst

Zhonglei Meng,Rongxiu Qin,Rusi Wen,Junkang Xie,Guiqing Li,Yonghong Zhou

To enhance the yield of the one-step synthesis of terpinyl acetate from α-pinene and acetic acid, this study evaluated α-hydroxycarboxylic acid (HCA)–boric acid composite catalysts based on orthogonal experimental design. The most important factor affecting the terpinyl acetate content in the product was the HCA content. The catalytic performance of the composite catalyst was related to the pKa1 of HCA. The tartaric acid–boric acid composite catalyst showed the highest catalytic activity. The α-pinene conversion reached 91.8%, and the terpinyl acetate selectivity reached 45.6%. When boric acid was replaced with B2O3, the HCA composite catalyst activity was enhanced, which reduced the use of HCA. When the lactic acid and B2O3 content accounted for 10% and 4% of the α-pinene mass content, respectively, the α-pinene conversion reached 93.2%, and the terpinyl acetate selectivity reached up to 47.1%. In addition, the presence of water was unfavorable to HCA–boric acid composite catalyst. However, a water content less than 1% of the α-pinene mass content improved the catalytic activity of HCA–B2O3. When the tartaric acid–B2O3 was used as catalyst, and the water content was 1% of the α-pinene mass content, the α-pinene conversion was 89.6%, and the terpinyl acetate selectivity was 47.5%.

研究领域: 化学工程 · 催化 · 有机化学
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LWT-FOOD SCIENCE AND TECHNOLOGY · 2020 · IF 4.006

Antioxidant, α-amylase and α-glucosidase inhibitory activities of bound polyphenols extracted from mung bean skin dietary fiber

Yuting Zheng,Shuai Liu,Jianhua Xie,Yi Chen,Ruihong Dong,Xingjie Zhang,Shiqi Liu,Jiayan Xie,Xiaobo Hu,Qiang Yu

In this study, bound polyphenols were extracted from mung bean skin dietary fiber by acid hydrolysis or alkaline hydrolysis. It was found that alkaline hydrolysis was more thorough than acid hydrolysis, the highest yield of bound polyphenols was 37.638 (mg FAE/g). In addition, the compositions of bound polyphenols were identified and quantified by UPLC-ESI-QTOF-MS/MS and UPLC-ESI-QqQ-MS/MS. In the study of antioxidant properties, we found that with the increase of polyphenol concentration, the scavenging rate of DPPH free radical, the absorption ability of oxygen free radical and the inhibition of ABAP were increased. Moreover, the inhibition rate of bound polyphenols on α-amylase and α-glucosidase increased in a dose dependent manner. The results could provide perspective for using the bound polyphenols in mung bean skin as the functional components of health food.

CAS / MDL: 9032-08-0
研究领域: 食品科学 · 药理学 · 营养学
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JOURNAL OF APPLIED TOXICOLOGY · 2020 ·Vol. 40 ·期 11 ·1526-1533 · IF 2.997

Cantharidin-induced acute hepatotoxicity: the role of TNF-α, IKK-α, Bcl-2, Bax and caspase3

Yalei Yu,Youyou Zhang,Jie Zhang,Chuhuai Guan,Liang Liu,Liang Ren

Cantharidin is of high medicinal value but has strong toxicity. Nowadays, multiple research has focused on the mechanism of its antitumor activity while research on toxicological profiles associated with cantharidin poisoning is still limited. Its hepatotoxicity has attracted attention recently for the crucial role of the liver in detoxification. Here, we aim to find a potential mechanism for cantharidin-induced acute hepatotoxicity with a view to assisting subsequent research or clinical use or detoxification. Twenty-one male Sprague-Dawley rats were randomly divided into control, low-dose (1.34 mg/kg) and high-dose (2.67 mg/kg) cantharidin exposure groups. We used hematoxylin-eosin to observe pathological changes and used immunofluorescent staining, western blotting and real-time quantitative polymerase chain reaction to detect the expression of the markers. The main pathological changes in livers of cantharidin-treated rats were necrosis, inflammatory infiltration and hemorrhage. We found coexpression of tumor necrosis factor alpha (TNF-α), IkappaB kinase-alpha (IKK-α) and caspase3 by immunofluorescent staining in livers of cantharidin-treated rats. Compared with the control, the levels of TNF-α, IKK-α and caspase3 increased significantly in the experimental groups ( P < .05). The ratio of B-cell lymphoma-2 (Bcl-2)/Bax increased in the low-dose group but decreased in the high-dose group ( P < .05). Cantharidin exposure raised IKK-α mRNA and caspase3 mRNA levels ( P < .05). In conclusion, the participation of TNF-α, IKK-α, Bcl-2, Bax and caspase3 uncovered a novel mechanism underlying cantharidin-induced acute hepatotoxicity, and the mechanism needs to be studied further.

CAS / MDL: 56-25-7
研究领域: 药理学 · 毒理学 · 分子生物学
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JOURNAL OF MOLECULAR LIQUIDS · 2019 · IF 4.561

Inhibitory mechanism of epicatechin gallate on α-amylase and α-glucosidase and its combinational effect with acarbose or epigallocatechin gallate

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.

研究领域: 生物化学 · 药理学 · 营养学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2017 · IF 3.671

α-chymotrypsin activated and stabilized by self-assembled polypseudorotaxane fabricated with bis-thiolated poly(ethylene glycol) and α-cyclodextrin: Spectroscopic and mechanistic analysis

Jun Zhao,Ji-Duan Lin,Jia-Chen Chen,Guo Chen,Xia-Lan Li,Xiao-Qin Wang,Ming-Xia Chen

The self-assembled polypseudorotaxane (PPRX) fabricated with bis-thiolated poly(ethylene glycol) (PEG) and α-cyclodextrin (α-CyD) acted as an activator for α-chymotrypsin (CT) and retained the activity of CT for a long time up to 7   days. The stabilization mechanism was studied, and the interaction between CT and PPRX was analyzed by using circular dichroism, fluorescence spectra and X-ray powder diffraction (XRD). The bis-thiolated PEG and its assembled PPRX with α-CyD exhibited the interaction with the C -terminal region of the CT’s B-chain probably through PEGylation of the surface disulfide bridge of CT. It caused the aromatic chromophores more exposed to the hydrophilic microenvironment, leading to conformational variation of CT that was revealed by spectroscopic analysis. It rendered the peptide chains in a more flexible and active state. As a comparison, the non-thiolated components could not decorate the surface of CT and performed almost no effect on its stability, which demonstrated that the decoration of the surface disulfide bridge was a key factor in retaining the activity of CT. Due to the activation and stabilization effect, bis-thiolated PEG/α-CyD PPRX was an excellent soft-immobilized carrier for CT, and provided an intriguing method for enzyme’s stabilization.

CAS / MDL: 840-97-1
研究领域: 生物化学 · 酶学 · 材料科学
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Journal of the Australian Ceramic Society · 2018 ·Vol. 55 ·期 1 ·71-76 · IF 0.587

Rapid preparation of α, β-Bi2O3 and α/β-Bi2O3 heterojunction with enhanced photocatalytic properties

Du Xiaoni,Liu Yang,Wang Xiaohong,Feng Jingqing,Ren Chaofei

α-Bi 2 O 3 and β-Bi 2 O 3 nanoparticles were selectively synthesized via one-step solution combustion synthesis (SCS) using bismuth nitrate (Bi(NO 3 ) 3 ·5H 2 O) as the oxidant and tartaric acid (C 4 H 6 O 6 ) as the fuel, and α/β-Bi 2 O 3 heterojunction was rapidly prepared by treating SCS β-Bi 2 O 3 powders with NaOH solution. The physical and chemical properties of as-prepared samples were characterized by XRD, SEM, TEM, PL, and UV-vis techniques. The formation of α/β-Bi 2 O 3 heterojunction can be proven by TEM, UV-vis diffuse reflectance spectra, and PL spectra results. The band gap energies of α-Bi 2 O 3 , β-Bi 2 O 3 , and α/β-Bi 2 O 3 measured by UV-vis diffuse reflectance spectra were estimated to be about 2.9, 2.48, and 2.7 eV, respectively. The PL spectra of α/β-Bi 2 O 3 heterojunction showed higher efficiency of charge separation and transfer across the α–β phase junction than those of α-Bi 2 O 3 and β-Bi 2 O 3 , leading to the enhancement of photocatalytic activity. The synthesized α/β-Bi 2 O 3 heterojunction can degrade 86% of rhodamin B (RhB) after 180 min under visible-light irradiation, better than those of pure α-Bi 2 O 3 (24%, 180 min) and pure β-Bi 2 O 3 (60%, 180 min). Consequently, α/β-Bi 2 O 3 heterojunction is a promising photocatalyst, which can be easily prepared by SCS and post-treatment of NaOH solution.

研究领域: 材料科学 · 环境科学
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LWT-FOOD SCIENCE AND TECHNOLOGY · 2022 · IF 6.056

Phenolics from Sterculia nobilis Smith pericarp by-products delay carbohydrate digestion by uncompetitively inhibiting α-glucosidase and α-amylase

Yujiao Yang,Pingling Zhang,Zhe Huang,Zhengang Zhao

Sterculia nobilis Smith pericarp is a by-product of tropical and subtropical fruit Sterculia nobilis Smith, the functional activity and phytochemical composition of which have not been widely reported. In this work, LC-ESI-MS/MS-MRM technique was used for the qualitative and quantitative analysis of 16 phenolic compounds in the ethyl acetate fraction of Sterculia nobilis Smith pericarp extract (EAF). Luteolin-7-O-glucoside, epicatechin gallate and apigetrin were the principal phenolics in the EAF. The hypoglycemic activity of EAF was examined by α-glucosidase and α-amylase inhibition models. EAF inhibited both α-glucosidase and α-amylase activities reversibly and uncompetitively with half-inhibitory concentration (IC 50 ) values of 69.390 ± 1.410 μg/mL and 2.151 ± 0.044 mg/mL, respectively. Enzyme inhibition mechanism of EAF was studied by spectroscopic methods. The results showed that EAF altered the secondary structure and microenvironment of tyrosine and tryptophan residues of the enzymes. This research demonstrates that Sterculia nobilis Smith pericarp is a potential raw material for production of functional foods at low cost.

CAS / MDL: 9005-84-9
研究领域: 药理学 · 食品科学 · 生物化学 · 植物科学
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