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Pharmaceutics 2018, 10(4), 178; https://doi.org/10.3390/pharmaceutics10040178

Metabolic Stability and Metabolite Characterization of Capilliposide B and Capilliposide C by LC–QTRAP–MS/MS

1
School of Pharmacy, Weifang Medical University, 7166 Baotong West Street, Weifang 261053, Shandong, China
2
School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, 13 Hangkong Road, Wuhan 430030, Hubei, China
3
Department of Biomedical Engineering, Zhejiang University, Hangzhou 310027, Zhejiang, China
*
Author to whom correspondence should be addressed.
Received: 13 August 2018 / Revised: 27 September 2018 / Accepted: 4 October 2018 / Published: 8 October 2018
(This article belongs to the Special Issue Preclinical Pharmacokinetics and Bioanalysis)
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Abstract

Capilliposide B (LC-B) and Capilliposide C (LC-C), two new triterpenoid saponins extracted from Lysimachia capillipes Hemsl, exhibit potential anticancer activity both in vitro and in vivo. However, their metabolic process remains unclear. In this study, the metabolic stability of LC-B, LC-C, and Capilliposide A (LC-A, a bioactive metabolite of LC-B and LC-C) was investigated in human, rat, and mouse liver microsomes, respectively. Thereafter, their metabolites were identified and characterized after oral administration in mice. As a result, species difference was found in the metabolic stability of LC-B and LC-C. All three compounds of interest were stable in human and rat liver microsomes, but LC-B and LC-C significantly degraded in mouse liver microsomes. The metabolic instability of LC-B and LC-C was mainly caused by esterolysis. Moreover, 19 metabolites were identified and characterized in mouse biological matrices. LC-B and LC-C mainly underwent deglycosylation and esterolysis, accompanied by dehydration, dehydrogenation, and hydroxylation as minor metabolic reactions. Finally, the metabolic pathway of LC-B and LC-C in mice was proposed. Our results updated the preclinical metabolism and disposition process of LC-B and LC-C, which provided additional information for better understanding efficacy and safety. View Full-Text
Keywords: Capilliposide B; Capilliposide C; metabolic stability; metabolism; LC-MS/MS Capilliposide B; Capilliposide C; metabolic stability; metabolism; LC-MS/MS
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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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Cheng, Z.; Zhou, X.; Du, Z.; Li, W.; Hu, B.; Tian, J.; Zhang, L.; Huang, J.; Jiang, H. Metabolic Stability and Metabolite Characterization of Capilliposide B and Capilliposide C by LC–QTRAP–MS/MS. Pharmaceutics 2018, 10, 178.

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