Extracts of G. sylvestre exhibited significant inhibitory activity against α-glucosidase. - GreenMedInfo Summary
Rapid Screening forα-Glucosidase Inhibitors fromby Affinity Ultrafiltration-HPLC-MS.
Front Pharmacol. 2017 ;8:228. Epub 2017 Apr 27. PMID: 28496409
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, thestudy revealed that the extract ofexhibited significant inhibitory activity againstα-glucosidase with ICat 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. 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 incould also be goodα-glucosidase inhibitors due to their synergistic effects. Taken together, the proposed method combing α-glucosidase and UF-HPLC-MS presents high efficiency for rapidly screening and identifying potential inhibitors of α-glucosidase from complex natural products, and could be further explored asa valuable high-throughput screening (HTS) platform in the early anti-diabetic drug discovery stage.