Fujii T, Miyazaki H, Nambu K, Kagemoto A, Hashimoto M
Radioisotopes. 1984 Aug;33(8):519-25.
Dehydrocorydaline, an alkaloid from Corydalis bulbosa possessing anti-ulceric activity, was labeled by methyl-14C at position 13, and its disposition and metabolism were studied in mice and rats after oral (50 mg/kg) or intravenous (6.8 mg/kg) administration. Blood levels were as low as 0.5 (mice) and 0.06 (rats) microgram eq./ml at maximum, conceivably due to its poor absorption from digestive tracts. Radiometric and autoradiographic studies after oral administration of 14C-dehydrocorydaline revealed that appreciable radioactivity was distributed in rather restricted organs, namely, digestive tracts, liver and kidney. Comparison of distribution with that after intravenous administration suggested that the compound is subject to the significant first pass effect by the liver. The distribution pattern of radioactivity in the liver was heterogeneous regardless to administration routes. Radiometry and autoradiography also revealed that the disposition did not differ significantly from each other in normal rats and those with experimentally induced gastric ulcer. Excretion of radioactivity occurred largely in feces. Excretion via urine and bile was quite minor. Metabolite analysis suggested that dehydrocorydaline was metabolized by O-demethylation and subsequent conjugation with glucuronic acid. However, metabolites were minor relative to the unchanged compound.
脱氢紫堇碱是一种来自紫堇的具有抗溃疡活性的生物碱，在其13位用甲基-14C进行标记，然后在小鼠和大鼠口服（50mg/kg）或静脉注射（6.8mg/kg）后研究其分布和代谢情况。血药浓度最高时分别低至0.5（小鼠）和0.06（大鼠）微克当量/毫升，这可能是由于其从消化道吸收较差。口服14C-脱氢紫堇碱后的放射性测量和放射自显影研究表明，相当数量的放射性分布在相当有限的器官中，即消化道、肝脏和肾脏。将其分布与静脉注射后的分布进行比较表明，该化合物受到肝脏显著的首过效应。无论给药途径如何，肝脏中放射性的分布模式都是不均匀的。放射性测量和放射自显影还表明，正常大鼠和实验性胃溃疡大鼠的分布情况没有显著差异。放射性主要通过粪便排出。经尿液和胆汁的排泄量相当少。代谢物分析表明，脱氢紫堇碱通过O-去甲基化以及随后与葡萄糖醛酸结合进行代谢。然而，相对于未变化的化合物，代谢物含量较少。
