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Open AccessCommunication
Mar. Drugs 2015, 13(2), 727-740; doi:10.3390/md13020727

In Vivo Metabolism Study of Xiamenmycin A in Mouse Plasma by UPLC-QTOF-MS and LC-MS/MS

1,2
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4
,
3,5
and
1,*
1
Key Laboratory of Systems Biomedicine, Shanghai Center for Systems Biomedicine, Shanghai Jiao Tong University, Shanghai 200240, China
2
Instrumental Analysis Center, Shanghai Jiao Tong University, Shanghai 200240, China
3
State Key Laboratory of Microbial Metabolism and School of Life Science & Biotechnology, Shanghai Jiao Tong University, Shanghai 200240, China
4
Waters Corporation, Building 13, No. 1000 Jinhai Road, Pudong New District, Shanghai 201206, China
5
Institute of Oceanology, Shanghai Jiao Tong University, Shanghai 200240, China
*
Author to whom correspondence should be addressed.
Academic Editor: Keith Glaser
Received: 5 December 2014 / Accepted: 13 January 2015 / Published: 28 January 2015
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Abstract

Xiamenmycin A is an antifibrotic leading compound with a benzopyran skeleton that is isolated from mangrove-derived Streptomyces xiamenensis. As a promising small molecule for fibrotic diseases, less information is known about its metabolic characteristics in vivo. In this study, the time-course of xiamenmycin A in mouse plasma was investigated by relative quantification. After two types of administration of xiamenmycin A at a single dose of 10 mg/kg, the plasma concentrations were measured quantitatively by LC-MS/MS. The dynamic changes in the xiamenmycin A concentration showed rapid absorption and quick elimination in plasma post-administration. Four metabolites (M1–M4) were identified in blood by UPLC-QTOF-MS, and xiamenmycin B (M3) is the principal metabolite in vivo, as verified by comparison of the authentic standard sample. The structures of other metabolites were identified based on the characteristics of their MS and MS/MS data. The newly identified metabolites are useful for understanding the metabolism of xiamenmycin A in vivo, aiming at the development of an anti-fibrotic drug candidate for the therapeutic treatment of excessive fibrotic diseases. View Full-Text
Keywords: Streptomyces xiamenensis; xiamenmycin; benzopyran; antifibrosis Streptomyces xiamenensis; xiamenmycin; benzopyran; antifibrosis
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Lei, F.; Gao, D.; Zhang, X.; Xu, J.; Xu, M.-J. In Vivo Metabolism Study of Xiamenmycin A in Mouse Plasma by UPLC-QTOF-MS and LC-MS/MS. Mar. Drugs 2015, 13, 727-740.

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