College of Veterinary Medicine, Hunan Agricultural University, Changsha, 410128, Hunan, China; Hunan Engineering Technology Research Center of Veterinary Drugs, Hunan Agricultural University, Changsha, 410128, Hunan, China.
College of Veterinary Medicine, Hunan Agricultural University, Changsha, 410128, Hunan, China.
J Ethnopharmacol. 2020 Apr 24;252:112617. doi: 10.1016/j.jep.2020.112617. Epub 2020 Jan 24.
Herbal medicine contains hundreds of natural products, and studying their absorption, metabolism, distribution, and elimination presents great challenges. Gelsemium elegans (G. elegans) is a flowering plants in the Loganiaceae family. The plant is known to be toxic and has been used for many years as a traditional Chinese herbal medicine for the treatment of rheumatoid arthritis, neuropathic pain, spasticity, skin ulcers and cancer. It was also used as veterinary drugs for deworming, promoting animal growth, and pesticides. At present, studies on the metabolism of G. elegans have primarily focused on only a few single available reference ingredients, such as koumine, gelsemine and gelsedine.
The goal of this work is to elucidate the overall metabolism of whole G. elegans powder in goats using high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (HPLC/QqTOF-MS).
Analyses of plasma, urine and fecal samples identified or tentatively characterized a total of 44 absorbed natural products and 27 related produced metabolites. Gelsedine-type, sarpagine-type and gelsemine-type alkaloids were the compounds with the highest metabolite formation. In the present study, most natural products identified in G. elegans were metabolized through glucuronidation and oxidation. Hydrogenation, dehydrogenation and demethylation also occurred.
To our knowledge, this is the first report of the metabolite profiling of the G. elegans crude extract in goats, which is of great significance for a safer and more rational application of this herbal medicine.
草药中包含数百种天然产物,研究其吸收、代谢、分布和消除具有很大的挑战性。钩吻(G. elegans)是马钱科植物。该植物已知具有毒性,并已被多年来用作治疗类风湿性关节炎、神经痛、痉挛、皮肤溃疡和癌症的传统中药。它也被用作兽医药物,用于驱虫、促进动物生长和杀虫剂。目前,对钩吻代谢的研究主要集中在少数几种单一的可用参考成分上,如钩吻素甲、钩吻素乙和钩吻素丙。
本工作的目的是使用高效液相色谱-四极杆飞行时间质谱联用(HPLC/QqTOF-MS)阐明整个钩吻粉末在山羊体内的整体代谢情况。
对血浆、尿液和粪便样本的分析共鉴定或初步表征了 44 种吸收的天然产物和 27 种相关的代谢产物。钩吻碱型、马钱子碱型和钩吻素型生物碱是形成代谢物最多的化合物。在本研究中,在钩吻中鉴定出的大多数天然产物通过葡萄糖醛酸化和氧化代谢。还发生了加氢、脱氢和去甲基化。
据我们所知,这是首次在山羊中报告钩吻粗提取物的代谢产物谱,这对于更安全和更合理地应用这种草药具有重要意义。