药食两用中药中脂肪酶以及α-葡萄糖苷酶抑制剂的筛选

Screening of pancreatic lipase and α-glucosidase inhibitors from Chinese dietary herbs

目的:通过对部分药食两用中药材提取物进行筛选,寻找新的脂肪酶以及α-葡萄糖苷酶的天然抑制剂。方法:采用酶活性测定法,用奥利司他(orlistat),阿卡波糖(acarbose)作为阳性对照对所选39个科别下的63种药食两用中药提取物进行筛选,分别测定其对脂肪酶和α-葡萄糖苷酶活性的抑制效力。结果:荷叶,姜黄,荜茇,桑枝以及桑白皮的药材提取物均显示出了较强的脂肪酶以及α-葡萄糖苷酶的共同抑制作用,它们对脂肪酶的半数抑制浓度分别为(28.00±5.51),(5.24±0.51),(14.76±2.58),(4.78±0.58),(3.41±0.67)mg.L-1;对α-葡萄糖苷酶的半数抑制浓度分别为(1.98±0.13),(0.18±0.007),(0.71±0.08),(0.077±0.005),(0.089±0.006)g.L-1。结论:此次筛选为进一步发现新的脂肪酶以及α-葡萄糖苷酶的抑制剂,开发新型降脂降糖天然药物和保健品奠定了一定基础。

The present study was conducted to develop new inhibitors of pancreatic lipase and α-glucosidase from Chinese dietary herbs.Sixty-three dietary herbs from 39 taxonomic families were selected and extracted with aqueous ethanol or water.The extracts were then tested with in vitro enzyme assays for their ability to inhibit pancreatic lipase and α-glucosidase activities.Orlistat and acarbose were used as two positive controls.The extracts of Nelumbo nucifera,Curcuma longa,Piper longum and Morus alba showed strong pancreatic lipase inhibitory effects with IC50 at（28.00±5.51）,（5.24±0.51）,（14.76±2.58）,（4.78±0.58）,（3.41±0.67） mg·L^-1,respectively.These extracts also showed potent α-glucosidase inhibitory activities with IC50 at（1.98±0.13）,（0.18±0.007）,（0.71±0.08）,（0.077±0.005）,（0.089±0.006） g·L^-1,respectively.The results provide useful information for developing new drugs or natural health products for hyperlipidemia and hypoglycemia from Chinese dietary herbs.