Abstract
Ardipusilloside I, extracted from Ardisia pusilla A.DC, effectively inhibits the progression of several cancers in animal models and
is a potential anti-cancer drug candidate. However, the metabolism and pharmacokinetic
characteristics of ardipusilloside I remain unknown. In this study, we developed a
highly sensitive liquid chromatography-tandem MS method to determine the ardipusilloside
I concentration in rat plasma using ginsenoside Re (whose structure is similar to
ardipusilloside I) as the internal standard. After oral administration of ardipusilloside
I, its four possible metabolites (M1, M2, M3, and M4, whose structures were determined
by MS) were detected in the content from rat small intestine. In rat plasma, however,
only M3 and M4 were detected after oral administration of ardipusilloside I. None
of the metabolites were detected in plasma samples after intravenous administration
of ardipusilloside I to rats. These results indicated that the metabolites, but not
the drug itself, were absorbed into plasma after oral administration of ardipusilloside
I to rats and that M3 and M4 may be responsible for the antitumor activity of orally
administered ardipusilloside I in rat models of cancer.
Key words
ardipusilloside I–LC-MS/MS - pharmacokinetic -
Ardisia pusilla
- Myrsinaceae
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Dr. Si-Yuan Zhou
Department of Pharmaceutics
School of Pharmacy
Fourth Military Medical University
17 Changle West Road
Xi'an, 710032
China
Phone: +86 29 84 77 67 83
Fax: +86 29 84 77 92 12
Email: zhousy@fmmu.edu.cn
Dr. Yi Gu
Department of Pharmacy
School of Stomatology
Fourth Military Medical University
17 Changle West Road
Xi'an, 710032
China
Phone: +86 29 84 77 67 83
Fax: +86 29 84 77 92 12
Email: guyi@fmmu.edu.cn
