Pharmazie. 2016 Jul 7;71(7):420-424. doi: 10.1691/ph.2016.6569.
To find new, plant based drugs for the treatment of obesity and/or diabetes mellitus type 2 through the inhibition of essential digestive enzymes, in vitro tests were carried out on selected plants or fungi with weight-reducing, blood glucose-reducing or related potential, used in Traditional Chinese Medicine (TCM). Aqueous and methanolic extracts of 32 Chinese herbal medicines were assayed for their in vitro inhibitory activity against pancreatic lipase (PL) and α-amylase (PA). PL activity was measured by using an enzymatic in vitro assay based on the hydrolysis kinetics of an oleate ester of 4-methylumbelliferone. For the determination of α-amylase activity an enzyme assay based on the hydrolytic cleavage of a modified starch derivative was used. Our findings have shown that the methanolic extract of Lycopus lucidus Turcz. var. hirtus Regel (Lamiaceae) was a very effective PL inhibitor (IC50: 88.3±4.1 μg/mL). A high anti-amylase activity showed the methanolic extract of Trichosanthes kirilowii Maxim. (Curcurbitaceae, IC50: 248.8±67.3 μg/mL). This work provides a priority list of interesting plants for further study with respect to the treatment of obesity and associated metabolic diseases.
为了通过抑制关键消化酶来寻找用于治疗肥胖症和/或2型糖尿病的新型植物源药物，对具有减肥、降血糖或相关潜力的选定植物或真菌进行了体外试验，这些植物或真菌在传统中药（TCM）中使用。测定了32种中草药的水提取物和甲醇提取物对胰脂肪酶（PL）和α-淀粉酶（PA）的体外抑制活性。通过基于4-甲基伞形酮油酸酯水解动力学的酶体外测定法测量PL活性。对于α-淀粉酶活性的测定，使用了基于修饰淀粉衍生物水解裂解的酶测定法。我们的研究结果表明，光萼水苏（Lycopus lucidus Turcz. var. hirtus Regel，唇形科）的甲醇提取物是一种非常有效的PL抑制剂（IC50：88.3±4.1μg/mL）。栝楼（Trichosanthes kirilowii Maxim.，葫芦科）的甲醇提取物显示出高抗淀粉酶活性（IC50：248.8±67.3μg/mL）。这项工作提供了一份关于治疗肥胖症和相关代谢疾病的进一步研究的有趣植物优先清单。
