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目的研究异钩藤碱(Isorhy)在猫体内的代谢并同步观察其可能的药理活性。方法麻醉猫静脉注射异钩藤碱5 mg/kg后,观察家猫血压的变化,收集0～3 h的血浆样品,用氢氧化钠—乙醚(1∶5)提取异钩藤碱及其代谢物,高效液相色谱法(HPLC)分离收集色谱峰流分,以液相色谱/质谱(LC/MS)测定异钩藤碱代谢物1(metabolite 1)分子离子峰的质荷比(m/z);代谢物1以60 ℃减压蒸馏24 h,同法测定代谢物1裂解物(metabolite 2)的分子离子峰m/z,根据m/z推测二者的化学结构。结果异钩藤碱代谢物1的相对分子质量为386,其热裂解化合物(metabolite2)相对分子质量为300,代谢产物在降压方面的药理作用贡献不大。结论①异钩藤碱代谢物的相对分子质量为386,为异钩藤碱的加氢还原产物;②代谢物不稳定,加热易裂解,其相对分子质量为300;③代谢物没有表现出心血管药理活性。
Objective To study the metabolism of Isorhy in cats and observe its possible pharmacological activities simultaneously. METHODS: After anesthetized cats were intravenously injected with isorhyncholine 5 mg/kg, the changes of blood pressure in cats were observed, plasma samples were collected for 0-3 h, and isoarginine and its metabolites were extracted with sodium hydroxide-diethyl ether (1:5). The peak fraction of the chromatographic peaks was collected by high performance liquid chromatography (HPLC) and the mass/charge ratio (m/z) of the molecular ion peak of metabolite 1 (metabolite 1) was determined by liquid chromatography/mass spectrometry (LC/MS). Metabolite 1 was decompressed and distilled at 60 °C for 24 h. The molecular ion peak m/z of the metabolite 1 lysate (metabolite 2) was determined in the same manner. The chemical structure of the two was estimated from m/z. Results The relative molecular mass of metarhizine metabolite 1 was 386, and the molecular weight of metabolite 2 was 300. The metabolites did not contribute much to the pharmacological effects of hypotension. Conclusion 1 The metabolite of isorhynchoine has a relative molecular weight of 386, which is the product of hydrogenation reduction of isorhinine; 2 the metabolite is unstable, and it is easily cleavable by heating; its molecular weight is 300; 3 metabolites do not show heart Vascular pharmacological activity.