Key Lab of Drug Metabolism and Pharmacokinetics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu, P. R. China.
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, P. R. China.
J Sep Sci. 2021 May;44(10):2097-2112. doi: 10.1002/jssc.202000898. Epub 2021 Apr 9.
The metabolic profiles of Tanreqing injection, which is a traditional Chinese medicine recommended for complementary administration to treat a novel coronavirus, have remained unclear, which inhibit the understanding of the effective chemical compounds of Tanreqing injection. In this study, a sensitive high-performance liquid chromatography quadrupole time-of-flight mass spectrometry method was used to identify the compounds and metabolites in various biosamples, including plasma, bile, liver, lung, kidney, urine, and feces, following the intravenous administration of Tanreqing injection in rats. A total of 89 compounds were characterized in the biosamples of Tanreqing injection-treated rats including 25 precursor constituents and 64 metabolites. Nine flavonoid compounds, twelve phenolic acids, and four iridoid glycosides were identified in the rats. Their metabolites were mainly produced by glucuronidation, deglucuronidation, glycosylation, deglycosylation, methylation, demethylation, N-heterocyclisation, sulphation, dehydroxylation, decarboxylation, dehydration, hydroxylation, and corresponding recombination reactions. This study was the first to comprehensively investigate the metabolic profile of Tanreqing injection and provides a scientific basis to further elucidate the pharmacodynamic material basis and therapeutic mechanism of Tanreqing injection.
注射用痰热清是一种推荐用于辅助治疗新型冠状病毒的中药,其代谢谱仍不清楚,这阻碍了对注射用痰热清有效化学化合物的理解。在这项研究中,采用了一种灵敏的高效液相色谱-四极杆飞行时间质谱法,用于鉴定静脉注射用痰热清在大鼠体内各种生物样本(包括血浆、胆汁、肝、肺、肾、尿和粪便)中的化合物和代谢物。在注射用痰热清处理的大鼠的生物样本中,共鉴定出 89 种化合物,包括 25 种前体成分和 64 种代谢物。在大鼠中鉴定出了 9 种类黄酮化合物、12 种酚酸和 4 种环烯醚萜苷。它们的代谢物主要通过葡萄糖醛酸化、去葡萄糖醛酸化、糖基化、去糖基化、甲基化、去甲基化、N-杂环化、硫酸化、去羟化、脱羧化、脱水、羟化和相应的重组反应生成。本研究首次全面研究了注射用痰热清的代谢谱,为进一步阐明注射用痰热清的药效物质基础和治疗机制提供了科学依据。