某些生物类黄酮和三萜类化合物对豚鼠肾脏来源的11β-羟基类固醇脱氢酶的抑制作用。
Inhibition of 11 beta-hydroxysteroid dehydrogenase obtained from guinea pig kidney by some bioflavonoids and triterpenoids.
作者信息
Zhang Y D, Wang M S
机构信息
Department of Pharmacology, Cornell University Medical College, New York, NY 10021, USA.
出版信息
Zhongguo Yao Li Xue Bao. 1997 May;18(3):240-4.
AIM
To study the inhibitory effect of some bioflavonoids and triterpenoids on 11 beta-hydroxysteroid dehydrogenase (11 beta-OHSD) from guinea pig kidney.
METHOD
The 11 beta-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 degrees C for 1 h. The enzyme activity was assayed by measuring the rate of conversion of cortisol to cortisone eluted with HPLC 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) mumol.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 11 beta-OHSD in kidney cortex with different potencies as glycyrrhizic acid did.
目的
研究某些生物黄酮类化合物和三萜类化合物对豚鼠肾脏11β-羟基类固醇脱氢酶（11β-OHSD）的抑制作用。
方法
在存在烟酰胺腺嘌呤二核苷酸磷酸（NADP）、聚乙二醇辛基苯基醚（Triton DF-18）和受试化合物的情况下，将添加皮质醇的肾皮质微粒体的11β-OHSD在37℃孵育1小时。通过测量用高效液相色谱梯度分析洗脱的皮质醇向可的松的转化速率来测定酶活性。
结果
甘草酸、柚皮素、非瑟酮、大黄素的半数抑制浓度（IC50）（95%置信限）值分别为254（202 - 320）、336（270 - 418）、470（392 - 564）和527（425 - 653）μmol·L-1。齐墩果酸的抑制作用比星膜菌素I强2倍。柚皮素的作用模式为竞争性抑制。
结论
受试化合物与甘草酸一样，以不同的效力抑制肾皮质中的11β-OHSD。
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