某些黄酮类和三萜皂苷类化合物对豚鼠肾的11β-羟化类固醇脱氢酶的抑制作用(英文)

Inhibition of 11β-hydroxysteroid dehydrogenase obtained from guinea pig kidney by some bioflavonoids and triterpenoids

目的:研究某些生物黄酮和三萜皂苷对豚鼠肾皮质11β羟化类固醇脱氢酶(11β-OHSD)的抑制作用.方法:肾皮质微粒体制备中加入氢化可的松,NADP,triton DF-18和被研究的化合物分别经37℃,1 h孵育,在HPLC梯度洗脱条件下,测定氢化可的松成为可的松的转化率来表示11β-OHSD的活性.结果:甘草酸、柚皮素、非瑟素、大黄素对11β-OHSD抑制的IG_(50)分别为254,336,470,527 μmol·L^(-1).齐墩果酸抑制此酶的IC_(50)值为黄芪甲苷的两倍.柚皮素对此酶的抑制是竞争性的.结论:柚皮素、非瑟素、大黄素等类似甘草酸,它们对肾皮质的11β-OHSD有不同程度的抑制作用.

AIM: To study the inhibitory effect of some bioflavonoids and triterpenoids on 11β-hydroxy-steroid dehydrogenase (11β-OHSD) from guinea pig kidney. METHOD: The 11β-OHSD of kidney cortex microsomes in addition of cortisol was incubated in the presence of NADP, Triton DF-18, and the test compounds at 37℃ for 1 h. The enzyme activity was assayed by measuring the rate of conversion of cortisol to cortisone eluted withHPLC gradient analysis. RESULTS: The IC50 (95 % confidence limits)values of glycyrrhizic acid, naringenin, fisetin, emodin were 254 (202 - 320), 336 (270-418), 470 (392-564), and 527 (425 -653)μmol·L-1, respectively. The inhibitory effect of oleanolic acid was 2-fold stronger than that of astramembranin I. The mode of action of naringenin was competitive inhibition. CONCLUSION: The test compounds inhibited the 11β-OHSD in kidney cortex with different potencies as glycyrrhizic acid did.