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左旋紫草素体内代谢研究

李慧义, 罗淑荣, 周同惠   

  1. 中国医学科学院中国协和医科大学药物研究所, 北京 100050
  • 收稿日期:1999-03-18 修回日期:1999-04-18 出版日期:1999-09-15 发布日期:1999-09-15

Metabolism of Shikonin in Rats

Li Huiyi, Luo Shurong, Zhou Tonghui   

  1. Instltute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050
  • Received:1999-03-18 Revised:1999-04-18 Online:1999-09-15 Published:1999-09-15

摘要: 本文对紫草素在大鼠体内的生物转化进行了研究。对经苯巴比妥预处理(i.p. 60 mg·kg-1·day, 3)Wistar种健康雄性大鼠腹腔注射紫草素(20 mg·kg-1), 收集到的胆汁和血样分别经β-葡萄糖醛酸酶水解后, 用乙酸乙酯提取。建立RP-HPLC/DAD方法对紫草素及其代谢物在大鼠胆汁和尿样中的分布进行了初步考察。根据色谱峰的保留时间和紫外光谱分析, 大鼠的胆汁和尿样中分别有10个代谢物。

关键词: 左旋紫草素, 生物转化, 酶水解, 代谢产物

Abstract: The metabolism of shikonin in rats was studied. Shikonin was administered (i.p.) to healthy, male Wistar rats pretreated with phenobarbital (PB, i.p., 60 mg·kg-1, once a day, 3 d) by asingle dose of 20 mg·kg-1, urine and bile were collected. The bile and urine samples wererespectively hydrolyzed with β-glucuronidase, extracted with ethyl acetate and the extractive concentrated in vacuum. The residues were dissolved in methanol and analyzed by a RP-HPLC/DADsystem for identification of shikonin metabolites. It has been proved that shikonin is metabolizedvery fast in the body and the metabolites are excreted mainly throngh the bile. The chromatograms and spectra showed that there were ten shikonin metabolites with similar UV spectra in the bile andurine respectively. The difference between in vivo and in vitro metabolic profiles of shikonin wasalso discussed.

Key words: Shikonin, In vivo metabolism, RP-HPLC, DAD

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