川芎哚在大鼠体内的代谢转化  

Studies on Urinary Metabolites of Perlolyrine in Rats

作　　者：姜国辉[1] 唐刚华[1] 王世真[1] 汪聪慧 郑连芳 

机构地区：[1]中国医学科学院

出　　处：《中国医学科学院学报》2000年第2期154-158,共5页Acta Academiae Medicinae Sinicae

基　　金：高等学校博士学科点专项科研基金!(9394);国家自然科学基金!(39570224)资助

摘　　要：目的　研究中药川芎中有效生物碱川芎哚在大鼠体内的代谢转化。方法　给大鼠灌胃分别给予川芎哚和氘标记川芎哚后 ,收集尿样。将尿样本经酶水解、碱化、有机溶剂提取 ;有机相 (碱性和中性部分 )经浓缩并硅烷化 ,水相经酸化、吹干、提取 (提取物为酸性水溶性部分 )并硅烷化。采用气相层析 -质谱联用仪测定提取的样品。结果　在碱性和中性提取物中 ,共检出原型川芎哚及其一种代谢物 ;在酸性水溶性提取物中 ,共检出川芎哚的另外两种代谢物。Objective To study the metabolism of perlolyrine in rats, which is an active ingredient from the traditional Chinese herb, Ligusticum Wallichii Franch. Methods After administration of perlolyrine and deuterated perlolyrine, the rat urines were hydrolyzed with glucuronidase, basified with NaHCO 3—Na 2CO 3, extracted with ethyl ether — isopropyl alcohol. The organic phases (neutral and basic fractions) were concentrated for trimethylsilyl (TMS) derivatives. The aqueous phase were acidified with sulfuric acid, taken to dryness and extracted with methanol (water soluble acidic fractions) and concentrated for TMS derivatives. The TMS derivatives were determined by gas chromatograph mass spectrometry (GCMS). Results Perlolyrine and one metabolite were found from the neutral and basic fractions, and two different metabolites were found from the water soluble acidic fractions. Conclusions It was proposed that the major metabolic pathways of perlolyrine were that the hydroxylation of perlolyrine and the oxidation of its hydroxylmethyl group.

关 键 词：川芎哚 氘标记川芎哚 体内代谢 GC-MS 

分 类 号：R285.5[医药卫生—中药学]