[In vivo study of Chuankezhi metabolism in rat].

药学学报 Pub Date : 2017-03-01

Qian-ru Feng, Jie-jing Yu, Jing-jing Zhan, Yi-juan Xu, Yeuk-lung Chow, Shun-jun Xu, Liu Yang

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引用次数: 0

Abstract

To study the metabolic products of main compounds of Chuankezhi injection in rat, 12 Sprague Dawley rats were classed into 2 groups, a blank control group and an intermuscular administration group, respectively. Rat feces and urine samples were collected from 0−24 h and 24−48 h after administration. All the samples were ultrasonically treated with methanol and then analyzed using LC-LTQ Orbitrap MSn. By comparison with the total ion chromatogram of samples from the blank control group, the metabolites in the samples of drug-treated group were screened. These metabolites were further analyzed by multistage product ion scanning and comparison of retention time with reference substances. As a result, a total of 12 flavonoid metabolites were tentatively identified from the rat feces and no metabolite was discovered in the rat urine. Epimedin C and icariin were detected in the rat blood samples after 30 min of administration, but their metabolites and other original flavones were not detected. Furthermore, no original flavones and their metabolites were detected in rat blood samples after 2 and 4 h of administration. The potential metabolism paths were further characterized and the principal in vivo transformation of flavones from Chuankezhi injection were deglycosylation, dehydration, methylation, oxidation and isomerization in rats.

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川可治在大鼠体内代谢研究。

为研究川可治注射液主要化合物在大鼠体内的代谢产物，将12只SpragueDawley大鼠分别分为空白对照组和肌间给药组。分别于给药后0 ~ 24 h和24 ~ 48 h采集大鼠粪便和尿液。用甲醇对样品进行超声处理，并用LC-LTQ Orbitrap微球进行分析。通过与空白对照组样品的总离子色谱图比较，筛选药物处理组样品中的代谢物。这些代谢物进一步通过多级生产扫描和与对照物的保留时间比较进行分析。结果，从大鼠粪便中初步鉴定出12种黄酮代谢物，而在大鼠尿液中未发现代谢物。给药30 min后，在大鼠血液中检测到淫羊藿苷C和淫羊藿苷，但未检测到它们的代谢物和其他原始黄酮。此外，在给药2和4 h后，大鼠血液样品中未检测到原始黄酮及其代谢物。进一步对川可之注射液的潜在代谢途径进行了表征，发现川可之注射液中黄酮类化合物在大鼠体内的主要转化为去糖基化、脱水、甲基化、氧化和异构化。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

药学学报 Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)

CiteScore

1.20

自引率

0.00%

发文量

期刊介绍： Acta Pharmaceutica Sinica B (APSB) is a bimonthly English peer-reviewed online journal in ScienceDirect, which publishes significant original research articles, communications and high quality reviews of recent advances. APSB encourages submissions from all areas of pharmaceutical sciences, including pharmacology, pharmaceutics, medicinal chemistry, natural products, pharmacognosy, pharmaceutical analysis and pharmacokinetics. APSB is a part of the series Acta Pharmaceutica Sinica, which was founded in 1953. The journal is co-published by Elsevier B.V., in association with the Institute of MateriaMedica, Chinese Academy of Medical Sciences and Chinese Pharmaceutical Association.