Wang Xin, Liu Quan, Zhu Hongbo, Wang Hongqing, Kang Jie, Shen Zhufang, Chen Ruoyun
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Acta Pharm Sin B. 2017 May;7(3):342-346. doi: 10.1016/j.apsb.2016.12.007. Epub 2017 Jan 24.
-Glucosidase and lipase inhibitors play important roles in the treatment of hyperglycaemia and dyslipidemia. To identify novel naturally occurring inhibitors, a bioactivity-guided phytochemical research was performed on the pu-erh tea. One new flavanol, named (-)-epicatechin-3---coumarate (), and known analogs (-) were isolated from the aqueous extract of the pu-erh tea. Their structures were determined by spectroscopic and chemical methods. Furthermore, the water extract of pu-erh tea and its fractions exhibited inhibitory activities against -glucosidases and lipases ; compound showed moderate inhibitory effect against sucrase with an IC value of 32.5 μmol/L and significant inhibitory effect against maltase with an IC value of 1.3 μmol/L. Compounds , , and displayed moderate activity against a lipase with IC values of 16.0, 13.6, 19.8, and 13.3 μmol/L, respectively.
α-葡萄糖苷酶和脂肪酶抑制剂在高血糖和血脂异常的治疗中发挥着重要作用。为了鉴定新型天然存在的抑制剂，对普洱茶进行了生物活性导向的植物化学研究。从普洱茶的水提取物中分离出一种新的黄烷醇，命名为(-)-表儿茶素-3-O-香豆酸酯()，以及已知类似物(-)。通过光谱和化学方法确定了它们的结构。此外，普洱茶的水提取物及其馏分对α-葡萄糖苷酶和脂肪酶表现出抑制活性；化合物对蔗糖酶表现出中等抑制作用，IC50值为32.5 μmol/L，对麦芽糖酶表现出显著抑制作用，IC50值为1.3 μmol/L。化合物、、和对脂肪酶表现出中等活性，IC50值分别为16.0、13.6、19.8和13.3 μmol/L。
