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.
Methyl salicylate-2-O-β-d-lactoside (MSL) is a natural salicylate derivative from the traditional Chinese medicine of Gaultheria 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.
Institute of Materia Medica, Peking Union Medical College &Chinese Academy of Medical Sciences, Beijing 100050, China; Pharmacy Department, China-Japan Friendship Hospital, Beijing 100029, China.
Dan
D
Zhang
Institute of Materia Medica, Peking Union Medical College &Chinese Academy of Medical Sciences, Beijing 100050, China.
Chao
C
Huang
Binzhou Medical University, Yantai 256603, China.
Wenyu
W
Xin
Institute of Materia Medica, Peking Union Medical College &Chinese Academy of Medical Sciences, Beijing 100050, China.
Xiaowei
X
Ma
Department of Pharmacology, Institute of Clinical Medical Sciences, China-Japan Friendship Hospital, Beijing 100029, China.
Weiku
W
Zhang
Institute of Materia Medica, Peking Union Medical College &Chinese Academy of Medical Sciences, Beijing 100050, China. Electronic address: ttzhang@imm.ac.cn.
Tiantai
T
Zhang
Institute of Materia Medica, Peking Union Medical College &Chinese Academy of Medical Sciences, Beijing 100050, China. Electronic address: dugh@imm.ac.cn.
Guanhua
G
Du
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics* / Q000652:urine; D001711:Biotransformation; D002138:Calibration; D002851:Chromatography, High Pressure Liquid; D005243:Feces / Q000737:chemistry; D007785:Lactose / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000652:urine; D057230:Limit of Detection; D013058:Mass Spectrometry; D011786:Quality Control; D051381:Rats; D015203:Reproducibility of Results; D012459:Salicylates / Q000493:pharmacokinetics* / Q000652:urine; D014018:Tissue Distribution
D000894:Anti-Inflammatory Agents, Non-Steroidal; D012459:Salicylates; C000597005:methyl salicylate 2-O-lactoside; D007785:Lactose
Metabolites; Methylsalicylate-2-O-beta-d-lactoside; Pharmacokinetic; Tandem mass spectrometry