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Molecules 2015, 20(11), 20569-20581; doi:10.3390/molecules201119719

Ardipusilloside-I Metabolites from Human Intestinal Bacteria and Their Antitumor Activity

1
State Key Laboratory of Military Stomatology, Department of Pharmacy, School of Stomatology, The Fourth Military Medical University, Xi’an 710032, China
2
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
*
Author to whom correspondence should be addressed.
Academic Editor: Nigel Brunton
Received: 29 September 2015 / Revised: 7 November 2015 / Accepted: 9 November 2015 / Published: 19 November 2015
(This article belongs to the Special Issue New Technologies for the Recovery of Natural Products)
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Abstract

Ardipusilloside-I (ADS-I) is a triterpenoid saponin extracted from Ardisia pusilla DC, and has been demonstrated to have potent antitumor activity. However, ADS-I metabolism in humans has not been investigated. In this study, we studied the biotransformation of ADS-I in human intestinal bacteria, and examined the in vitro antitumor activity of the major metabolites. Ultra-high performance liquid chromatography–tandem mass spectrometry (UHPLC–MS/MS) was used to detect ADS-I biotransformation products, and their chemical structures were identified by high performance liquid chromatography–nuclear magnetic resonance (HPLC–NMR). The antitumor activity of the major metabolites was determined by the MTT assay. Here, we show that main reaction seen in the metabolism of ADS-I in human intestinal bacteria was deglycosylation, which produced a total of four metabolites. The structures of the two major metabolites M1 and M2 were confirmed by using NMR. MTT assay showed that ADS-I metabolites M1 and M2 have the same levels of inhibitory activities as ADS-I in cultured SMMC-7721 cells and MCF-7 cells. In conclusion, this study demonstrates deglycosylation as a primary pathway of ADS-I metabolism in human intestinal bacteria, and suggests that the pharmacological activity of ADS-I may be mediated, at least in part, by its metabolites. View Full-Text
Keywords: ardipusilloside-I; human intestinal bacteria; metabolism; UHPLC–MS; HPLC–NMR; antitumor activity ardipusilloside-I; human intestinal bacteria; metabolism; UHPLC–MS; HPLC–NMR; antitumor activity
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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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MDPI and ACS Style

Cao, W.-Y.; Wang, Y.-N.; Wang, P.-Y.; Lei, W.; Feng, B.; Wang, X.-J. Ardipusilloside-I Metabolites from Human Intestinal Bacteria and Their Antitumor Activity. Molecules 2015, 20, 20569-20581.

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