College of Forestry, Northwest A&F University, Yangling, China.
Qinling National Forest Ecosystem Research Station, Huoditang, China.
Vet Med Sci. 2021 Sep;7(5):2086-2092. doi: 10.1002/vms3.499. Epub 2021 May 6.
Gelsemium is a small genus of flowering plants from the family Loganiaceae comprising five species, three of which, Gelsemium sempervirens (L.) J. St.-Hil., G. elegans Benth and G. rankinii Small, are particularly popular. Compared with other alkaloids from G. elegans, gelsemine, gelsevirine and koumine exhibit equally potent anxiolytic effects and low toxicity. Although the pharmacological activities and metabolism of koumine and gelsemine have been reported in previous studies, the species differences of gelsevirine metabolism have not been well studied. In this study, the metabolism of gelsevirine was investigated by using liver microsomes of humans, pigs, goats and rats by means of HPLC-QqTOF/MS. The results indicated that the metabolism of gelsevirine in liver microsomes had qualitative and quantitative species differences. Based on the results, the possible metabolic pathways of gelsevirine in liver microsomes were proposed. Investigation of the metabolism of gelsevirine will provide a basis for further studies of the in vivo metabolism of this drug.
钩吻是马钱科钩吻属的常绿木质藤本植物，包含 5 个物种，其中 3 个物种，即钩吻（Gelsemium sempervirens）、钩吻素子（Gelsemium elegans）和钩吻碱（G. rankinii），尤其受欢迎。与钩吻中的其他生物碱相比，钩吻碱、钩吻宁和钩吻甲素具有同等的抗焦虑作用和较低的毒性。虽然以前的研究已经报道了钩吻甲素和钩吻碱的药理学活性和代谢，但钩吻宁代谢的种属差异尚未得到很好的研究。本研究采用人、猪、山羊和大鼠肝微粒体，通过 HPLC-QqTOF/MS 研究了钩吻宁的代谢情况。结果表明，肝微粒体中钩吻宁的代谢存在定性和定量的种属差异。基于这些结果，提出了肝微粒体中钩吻宁可能的代谢途径。对钩吻宁代谢的研究将为进一步研究该药物的体内代谢提供依据。
