Preclinical pharmacokinetic evaluation and metabolites identification of methyl salicylate-2-O-β-d-lactoside in rats using LC-MS/MS and Q-TOF-MS methods.
Preclinical pharmacokinetic evaluation and metabolites identification of methyl salicylate-2-O-β-d-lactoside in rats using LC-MS/MS and Q-TOF-MS methods.
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DOI：
10.1016/j.jpba.2015.02.022
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发表时间：
2015-05
影响因子：
3.4
通讯作者：
Dan Zhang;Chaoqing Huang;Wenyu Xin;Xiaowei Ma;Weiku Zhang;Tiantai Zhang;G. Du
中科院分区：
文献类型：
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作者：
Dan Zhang;Chaoqing Huang;Wenyu Xin;Xiaowei Ma;Weiku Zhang;Tiantai Zhang;G. Du
水杨酸甲酯-2-O-β-d-乳糖苷（Methyl salicylate-2-O-β-d-lactoside，MSL）是从中药云南白珠（Gaultheria yunnanensis（Franch.）G. yunnanensis）。作为一种非甾体抗炎药，MSL具有显著的抗关节炎作用，但几乎没有胃肠道毒性。本文介绍了大鼠口服和静脉注射MSL及其代谢产物的药代动力学、分布、排泄和鉴定。通过UPLC-MS/MS对生物样品进行定量，并通过Q-TOF-MS鉴定尿液和粪便中的代谢物。这些结果将支持未来的研究，从而导致该药物的临床开发。
Methyl salicylate-2-O-β-d-lactoside (MSL) is a natural salicylate derivative from the traditional Chinese medicine ofGaultheria yunnanensis(Franch.) Rehder (G. yunnanensis). As a non-steroidal anti-inflammatory drug (NSAID), MSL exerts a significant anti-arthritis effect but hardly has any gastrointestinal toxicity. In this paper, the pharmacokinetics, distribution, excretion and identification of MSL and its metabolites are described following rat oral and intravenous administration. The biological samples were quantified by UPLC–MS/MS and the metabolites in urine and feces were identified by using Q-TOF-MS. These results will support future investigations leading to clinical development of this drug.