川芎哚大鼠体内代谢转化研究  

STUDIES ON METABOLIC TRANSFORMATION OF PERLOLYRINE IN RATS

作　　者：唐刚华[1] 姜国辉[2] 王世真[2] 郑连芳[2] 

机构地区：[1]第一军医大学南方医院南方PET中心,广东广州510515 [2]中国医学科学院,中国协和医科大学北京协和医院核医学科,北京100730

出　　处：《药学学报》2000年第6期457-460,共4页Acta Pharmaceutica Sinica

基　　金：国家教委高等学校博士学科点专项科研基金! ( 93 94);国家自然科学基金!( 3 95 70 2 2 4)

摘　　要：目的　研究川芎有效成分川芎哚在大鼠体内的代谢转化。方法　分别ig川芎哚和 [2 - 15N]川芎哚后 ,尿样经酶水解、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、提取 (提取物为酸性水溶部分 )并硅烷化 ,用GC MS测定。结果　在碱性和中性提取物中 ,检出原型川芎哚及其一种代谢物 ;在酸性水溶性提取物中 ,检出川芎哚的另两种代谢物。AIM To study the metabolism of perlolyrine, an active ingredient from the traditional Chinese herb, Chuanxiong, Ligusticum wallichii Franch in rats. METHODS After oral administration of perlolyrine and [2- 15 N] perlolyrine, the rat urine samples were hydrolyzed with glucuronidase, alkalinized with NaHCO 3—Na 2CO 3 and extracted with ethyl ether—isopropyl alcohol. The organic phases (neutral and basic fraction) were concentrated for TMS derivatization. The aqueous phase was acidified with sulfuric acid, taken to dryness and extracted with methanol (water soluble acidic fractions) and concentrated for TMS derivatization. The TMS derivatives were determined by GC MS. RESULTS Perlolyrine and one metabolite were found from the neutral and basic fraction, and two different metabolites were found from the water soluble acid fraction. CONCLUSION It was proposed that the major metabolic pathways of perlolyrine were the hydroxylation of perlolyrine and the oxidation of its hydroxylmethyl group.

关 键 词：川芎哚 代谢转化 气相色谱-质谱联用 中药 

分 类 号：R285[医药卫生—中药学]