Abstract

The inhibition of α-glucosidase and DPP enzymes capable of effectively reducing blood glucose level in the management of type 2 diabetes. The purpose of the present study is to evaluate the inhibitory potential of α-glucosidase and DPP (IV) activity including with the 2-NBDG uptake assay and insulin secretion activities through in vitro studies. The selected of active compounds obtained from the screening of compounds by LC-MS were docked with the targeted enzyme that involved in the mechanism of T2DM. From the results, root extracts displayed a better promising outcome in α-glucosidase (IC₅₀ 2.72 ± 0.32) as compared with the fruit extracts (IC₅₀ 3.87 ± 0.32). Besides, root extracts also displayed a better activity in the inhibition of DPP (IV), enhance insulin secretion and glucose uptake activity. Molecular docking results revealing that phlorizin binds strongly with α-glucosidase, DPP (IV) and Insulin receptor (IR) enzymes with achieving the lowest binding energy value. The present work suggests several of the compounds have the potential that contribute towards inhibiting α-glucosidase and DPP (IV) and thus effective in lowering post-prandial hyperglycaemia.

摘要

在治疗2型糖尿病时，能够有效降低血糖水平的α-葡萄糖苷酶和DPP酶的抑制作用。本研究的目的是通过体外研究评估α-葡萄糖苷酶和DPP（IV）活性的抑制潜力，包括2- NBDG摄取测定法和胰岛素分泌活性。通过LC-MS筛选化合物而获得的活性化合物的选择与涉及T2DM机理的目标酶对接。从结果来看，与水果提取物（IC ₅₀）相比，根提取物在α-葡萄糖苷酶（IC ₅₀ 2.72±0.32）中显示出更好的前景3.87±0.32）。此外，根提取物还具有更好的抑制DPP（IV）的活性，增强胰岛素分泌和葡萄糖摄取活性。分子对接结果表明，phlorizin与α-葡萄糖苷酶，DPP（IV）和胰岛素受体（IR）酶牢固结合，并实现了最低的结合能值。目前的工作表明，几种化合物具有抑制α-葡萄糖苷酶和DPP（IV）的潜力，因此可有效降低餐后高血糖症。