选择性抑制11β-HSD1的天然产物研究进展

Research progress on natural products with selective inhibition against 11β-HSD1

11β-羟类固醇脱氢酶(11β-hydroxysteroid dehydrogenase,11β-HSD)是糖皮质激素的代谢酶。研究表明,抑制局部11β-HSD亚型11β-HSD1的高表达,降低糖皮质激素的局部效应,成为治疗糖尿病和代谢综合征的一种新策略,所以选择性11β-HSD1抑制剂的研究,将成为2型糖尿病新药开发的一个方向。天然产物是新药开发的宝库和源泉,综述近10年来关于选择性抑制11β-HSD1的天然产物的研究进展,以期为11β-HSD1抑制剂的研究开发提供参考。

11β-Hydroxysteroid dehydrogenase（11β-HSD） is a metabolic enzyme of glucocorticoid. Growing evidence suggests that inhibiting over-expression of 11β-HSD1 and reducing partial effects of glucocorticoid could be the strategy to treat type 2 diabetes, as well as metabolic syndrome. Researching and developmenting selective 11β-HSD1 inhibitors may become a new direction. As natural products（NPs） have represented a cornerstone of pharmaceutical research, literatures on the development of natural products with selective inhibition against 11β-HSD1 published during the last 10 years were selected, and the inhibitors were classified according to the way how to find them. This paper will provide reference for the further research on the selective 11β-HSD1 inhibitors.