Kang Wenyi, Zhang Li, Song Yanli
Institute of Natural Products, Pharmaceutical College, Henan University, Kaifeng 475004, China.
Zhongguo Zhong Yao Za Zhi. 2009 May;34(9):1104-7.
To search alpha-glucosidase inhibitors from Rubia cordifolia.
The alpha-glucosidase inhibitors were isolated by the column chromatographic techniques and the bioassay-guided method in vitro. A combination of MS and NMR spectroscopy was used to identify the chemical structures. The inhibitory kinetics of the inhibitors were also investigated.
The chloroform extract showed high inhibitory activity, and three active compounds were isolated and identified as 1,3-dihydroxy-2-methylanthraquinone (1), 1-hydroxy-2-methylanthraquinone (2) and 1,2-dihydroxyanthraquinone (3). The IC5o values of compound 1-3 were all lower than that of acarbose. Compound 1 and 2 shown competitive type manner on alpha-glucosidase, whereas compound 3 shown noncompetitive type model.
Compounds 1-3 as strong inhibitors of alpha-glucosidase were reported for the first time.
从茜草中寻找α-葡萄糖苷酶抑制剂。
采用柱色谱技术和体外生物活性导向法分离α-葡萄糖苷酶抑制剂。结合质谱和核磁共振光谱鉴定化学结构。还研究了抑制剂的抑制动力学。
氯仿提取物显示出高抑制活性，分离并鉴定出三种活性化合物，分别为1,3-二羟基-2-甲基蒽醌（1）、1-羟基-2-甲基蒽醌（2）和1,2-二羟基蒽醌（3）。化合物1-3的IC50值均低于阿卡波糖。化合物1和2对α-葡萄糖苷酶表现出竞争性抑制类型，而化合物3表现出非竞争性抑制模式。
首次报道化合物1-3为α-葡萄糖苷酶的强效抑制剂。
