川芎哚大鼠体内代谢转化研究

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。结论　川芎哚体内代谢途径可能是川芎哚羟基化和川芎哚羟甲基的氧化。

STUDIES ON METABOLIC TRANSFORMATION OF PERLOLYRINE IN RATS

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 ［2-¹⁵N］ perlolyrine, the rat urine samples were hydrolyzed with glucuronidase, alkalinized with NaHCO₃-Na₂CO₃ 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.