School of Pharmaceutical Sciences, Universiti Sains Malaysia, Pulau Pinang 11800, Malaysia.
BMC Complement Altern Med. 2012 Oct 8;12:176. doi: 10.1186/1472-6882-12-176.
In the present study, we tested a 50% ethanolic extract of Orthosiphon stamineus plants and its isolated bioactive compound with respect to their α-glucosidase and α-amylase inhibitory activities.
Bioactive flavonoid sinensetin was isolated from 50% ethanolic extract of Orthosiphon stamineus. The structure of this pure compound was determined on the NMR data and the α-glucosidase and α-amylase inhibitory activities of isolated sinensetin and 50% ethanolic extract of Orthosiphon stamineus were evaluated.
In vitro studies of a 50% ethanolic extract of O. stamineus and the isolated sinensetin compound showed inhibitory activity on α-glucosidase (IC50: 4.63 and 0.66 mg/ml, respectively) and α-amylase (IC50: 36.70 mg/ml and 1.13 mg/ml, respectively). Inhibition of these enzymes provides a strong biochemical basis for the management of type 2 diabetes via the control of glucose absorption.
Alpha-glucosidase and α-amylase inhibition could the mechanisms through which the 50% ethanolic extract of O. stamineus and sinensetin exert their antidiabetic activity, indicating that it could have potential use in the management of non-insulin-dependent diabetes.
本研究旨在测试毛喉鞘蕊花植物的 50%乙醇提取物及其分离的生物活性化合物对α-葡萄糖苷酶和α-淀粉酶的抑制活性。
从毛喉鞘蕊花的 50%乙醇提取物中分离出生物活性类黄酮圣草次苷。根据 NMR 数据确定该纯化合物的结构，并评估分离得到的圣草次苷和毛喉鞘蕊花 50%乙醇提取物的α-葡萄糖苷酶和α-淀粉酶抑制活性。
体外研究表明，毛喉鞘蕊花 50%乙醇提取物和分离得到的圣草次苷化合物对α-葡萄糖苷酶（IC50：分别为 4.63 和 0.66mg/ml）和α-淀粉酶（IC50：分别为 36.70mg/ml 和 1.13mg/ml）均具有抑制活性。这些酶的抑制作用为通过控制葡萄糖吸收来管理 2 型糖尿病提供了强有力的生化基础。
α-葡萄糖苷酶和α-淀粉酶抑制作用可能是毛喉鞘蕊花 50%乙醇提取物和圣草次苷发挥抗糖尿病活性的机制，表明其在非胰岛素依赖型糖尿病的治疗中可能具有潜在的应用价值。
