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-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 as a valuable high-throughput screening (HTS) platform in the early anti-diabetic drug discovery stage.
Highlights
Characterized by high blood glucose levels, diabetes mellitus (DM) has become one of the most serious chronic endocrine metabolic dysfunction
Our present work offers a powerful tool for discovering bioactive components from complex natural products
Α-Glucosidase powder were obtained from Sigma-Aldrich (Missouri, USA). p-nitrophenyl α-D-glucopyranoside and acarbose were bought from Uteam-BIOTECH (Shanghai, China) and Yuanye Bio-Technology Co., Ltd (Shanghai, China), respectively
Summary
Characterized by high blood glucose levels, diabetes mellitus (DM) has become one of the most serious chronic endocrine metabolic dysfunction. Repeated postprandial hyperglycemia may facilitate the development of the above serious adverse effects, and, in extreme cases, the risk of mortality. In clinical trials, those complications could be delayed or prevented by the intensive postprandial hyperglycemia control (Li et al, 2015; Liu et al, 2016; Zhang et al, 2016). Those complications could be delayed or prevented by the intensive postprandial hyperglycemia control (Li et al, 2015; Liu et al, 2016; Zhang et al, 2016) To this end, postprandial blood glucose, especially in non-insulin-dependent T2DM patients, has attracted growing attentions as a potential therapeutic target
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