Screening of α-Glucosidase Inhibitors in Extracts of Polygonum bistorta Based on Spectrum-Effect Relationship
Journal Title: Journal of Experimental and Clinical Application of Chinese Medicine - Year 2024, Vol 5, Issue 4
Abstract
Bistortae Rhizoma is a traditional Chinese medicine, which is the dried rhizome of Polygonum bistorta (PB). It has anti-inflammatory, antibacterial, antioxidant, anti-diabetic effects and so on. Among them, there exists a limited number of studies investigating the anti-diabetic effect of PB, and the specific ingredients responsible for this effect remain unclear. To rapidly screen α-glucosidase inhibitors in extracts of PB, this study explored the relation between effective components and enzyme inhibitory activity based on component-effect analysis, revealing its key active component. After the suppressing effect of extracts of PB from different batches on α-glucosidase was tested, high performance liquid chromatography (HPLC) was employed to plot fingerprint of PB and evaluate the similarity of fingerprint. Combined with HPLC-Q-Orbitrap high-resolution mass spectrometry (HRMS)/MS qualitative analysis, the grey relational analysis and partial least squares regression analysis were performed to screen active components, and molecular docking was used for activity validation. The results indicated that the 11 batches of PB extracts can effectively inhibit α-glucosidase, with half-maximal inhibitory concentration (IC50) of 1.71-35.62 µg/mL, which had stronger inhibitory activity compared to the positive control acarbose (IC50 of 148.00 µg/mL). Among them, the PB07 batch of PB extract derived from Shandong province exerted the best inhibitory effect, with an IC50 of 1.71 µg/mL. The grey relational analysis and partial least squares regression analysis revealed that in the 11 batches of samples, 7 characteristic peaks had a relatively large correlation value with the inhibitory activity of PB on α-glucosidase, and the regression coefficient was positively correlated with inhibitory activity, indicating the importance of variables and high contribution. Through secondary mass spectrometry and database comparison, the 7 components were identified as 6-O-galloylglucose, L-tryptophan, (+)-gallocatechin-(4α→8)-(+)-catechin, deacetyl asperuloside, chlorogenic acid, catechin-5-O-glucoside, and digalloylglucose. It is noteworthy that the 7 components were all identified as α-glucosidase inhibitors in PB extract for the first time. Further molecular docking results showed that the binding energies of the 7 active components to α-glucosidase were all less than -6.0 kcal/mol, hinting significant inhibitory activity of α-glucosidase. Among them, the binding energy of catechin-5-O-glucoside was the lowest (-8.7 kcal/mol), which impacted enzyme active center mainly through hydrogen bonding. The results of this study provide research ideas for the development of hypoglycemic drugs using PB in the future.
Authors and Affiliations
Qi Huang, Weiqi Yang, Xiaofei Li, Liqiao Xie, Dan Tang, Zhengming Qian
Keywords
Related Articles
- EP ID EP754224
- DOI -
- Views 33
- Downloads 0
Screening of α-Glucosidase Inhibitors in Extracts of Polygonum bistorta Based on Spectrum-Effect Relationship
Bistortae Rhizoma is a traditional Chinese medicine, which is the dried rhizome of Polygonum bistorta (PB). It has anti-inflammatory, antibacterial, antioxidant, anti-diabetic effects and so on. Among them, there exists...
The Therapy Based on Traditional Chinese Medicine for Otolithiasis
Background: Otolithiasis (also named benign paroxysmal positional vertigo, BPPV) is one of the most common illness for hospital visits. Residual dizziness and recurrence after reduction are problems for the treating BPPV...
Andrographolide: A Review on Experimental Clinical Trials and Applications
Throughout human history, plants have been used for medicinal purposes. Plants can synthesise a vast range of chemical compounds that possess biological activities and can be employed as medicines. Andrographis paniculat...
Application of Tongbian Scraping Combined with Suhuang Zhike Capsule in Chronic Obstructive Pulmonary Disease
Objective: This study investigates the application of Tongbian scraping combined with Suhuang Zhike capsule in chronic obstructive pulmonary disease (COPD). Methods: 43 patients with COPD treated with Tongbian scraping c...
Automated, Microscopic Measurement of Fibrinaloid Microclots and Their Degradation by Nattokinase, the Main Natto Protease
Nattokinase, from the Japanese fermented food natto, is a protease with fibrinolytic activity that can thus degrade conventional blood clots. In some cases, however, including in Long COVID, fibrinogen can polymerise int...