Rapid Screening for α-Glucosidase Inhibitors from Gymnema sylvestre by Affinity Ultrafiltration-HPLC-MS

Frontiers in Pharmacology
Guilin Chen, Ming-Quan Guo

Abstract

Gymnema sylvestre R. Br. (Asclepiadaceae) has been known to posses potential anti-diabetic activity, and the gymnemic acids were reported as the main bioactive components in this plant species. However, the specific components responsible for the hypoglycemic effect still remain unknown. In the present study, the in vitro study revealed that the extract of G. sylvestre exhibited significant inhibitory activity against α-glucosidase with IC50 at 68.70 ± 1.22 μg/mL compared to acarbose (positive control) at 59.03 ± 2.30 μg/mL, which further indicated the potential anti-diabetic activity. To this end, a method based on affinity ultrafiltration coupled with liquid chromatography mass spectrometry (UF-HPLC-MS) was established to rapidly screen and identify the α-glucosidase inhibitors from G. sylvestre. In this way, 9 compounds with higher enrichment factors (EFs) were identified according to their MS/MS spectra. Finally, the structure-activity relationships revealed that glycosylation could decrease the potential antisweet activity of sapogenins, and other components except gymnemic acids in G. sylvestre could also be good α-glucosidase inhibitors due to their synergistic effects. Taken together, the proposed method combing α-gluco...Continue Reading

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Citations

Nov 13, 2018·Phytotherapy Research : PTR·Fiaz AlamMohammad Hassham Hassan Bin Asad
Nov 19, 2019·Frontiers in Pharmacology·Farzana KhanMohammad A Rashid
Feb 9, 2021·Journal of Diabetes and Metabolic Disorders·Vishakha Parab Gaonkar, Kirankumar Hullatti
Mar 14, 2019·Journal of Agricultural and Food Chemistry·Yumeng LiZesheng Zhang
Aug 1, 2020·Endocrine, Metabolic & Immune Disorders Drug Targets·Shahzad KhanMohammad A Kamal

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Methods Mentioned

BETA
column chromatography
glycosylation

Software Mentioned

SigmaPlot

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