紫杉叶素抑制大鼠和人类的11β-羟基类固醇脱氢酶2。
Taxifolin inhibits rat and human 11β-hydroxysteroid dehydrogenase 2.
作者信息
Wu Chengyun, Cao Shuyan, Hong Tingting, Dong Yaoyao, Li Chao, Wang Qiufan, Sun Jianliang, Ge Ren-Shan
机构信息
Department of Respiratory Medicine, The Second Affiliated Hospital and Yuying Children's Hospital of Wenzhou Medical University, Wenzhou, Zhejiang 325027, China.
Center of Scientific Research, The Second Affiliated Hospital and Yuying Children's Hospital of Wenzhou Medical University, Wenzhou, Zhejiang 325027, China.
出版信息
Fitoterapia. 2017 Sep;121:112-117. doi: 10.1016/j.fitote.2017.07.004. Epub 2017 Jul 12.
Taxifolin is a flavonoid in food plants. Kidney 11β-hydroxysteroid dehydrogenase 2 (11β-HSD2) is an NAD-dependent oxidase that inactivates glucocorticoid cortisol (human) or corticosterone (rodents) into biologically inert 11 keto glucocorticoids. The present study investigated the effects of taxifolin on rat and human kidney microsomal 11β-HSD2. Taxifolin noncompetitively inhibited rat and human 11β-HSD2 against steroid substrates, with IC values of 33.08 and 13.14μM, respectively. Administration of 5 and 10mg/kg taxifolin for 30min ex vivo inhibited 11β-HSD2 significantly and also in vivo decreased cortisol metabolism, as shown in the significant increase of area under curve (AUC). This result shows that taxifolin is a potent 11β-HSD2 inhibitor, possibly causing side effects.
紫杉叶素是食用植物中的一种类黄酮。肾脏11β - 羟基类固醇脱氢酶2（11β - HSD2）是一种依赖NAD的氧化酶，可将糖皮质激素皮质醇（人类）或皮质酮（啮齿动物）转化为生物惰性的11 - 酮糖皮质激素。本研究调查了紫杉叶素对大鼠和人类肾脏微粒体11β - HSD2的影响。紫杉叶素对类固醇底物非竞争性抑制大鼠和人类的11β - HSD2，其IC值分别为33.08和13.14μM。离体给予5和10mg/kg紫杉叶素30分钟可显著抑制11β - HSD2，并且在体内也降低了皮质醇代谢，曲线下面积（AUC）显著增加即表明了这一点。该结果表明紫杉叶素是一种有效的11β - HSD2抑制剂，可能会引起副作用。
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