当前位置： SCI文献检索 > FITOTERAPIA期刊下所有文献 > In vivo metabolism of 8,2'-diprenylquercetin 3-methyl ether and the distribution of its metabolites in rats by HPLC-ESI-IT-TOF-MSn.

In vivo metabolism of 8,2'-diprenylquercetin 3-methyl ether and the distribution of its metabolites in rats by HPLC-ESI-IT-TOF-MSn.

Abstract：

:8,2'-Diprenylquercetin 3-methyl ether, a natural product with prominent anti-breast cancer activity, is the main active constituent of Sinopodophylli Fructus. A high-performance liquid chromatography with a diode array detector coupled with electrospray ionization ion trap time-of-flight multistage mass spectrometry (HPLC-DAD-ESI-IT-TOF-MSn) method was established and applied to profile and identify the metabolites of 8,2'-diprenylquercetin 3-methyl ether as well as study their distribution in rat organs for the first time. A total of 100 new metabolites were tentatively identified in rats. The metabolic reactions of 8,2'-diprenylquercetin 3-methyl ether in rats in vivo were hydroxylation, methylation, glucuronidation, dehydrogenation, sulfation, polymerization and cysteine conjugation as well as the specific reactions of leucine/isoleucine, proline, and vitamin C conjugation. The detected metabolites included 77 in faeces, 50 in urine, 11 in plasma, 50 in the small intestine, 32 in the stomach, 23 in the liver, 9 in the lungs, 9 in the spleen, 8 in the heart, and 6 in the kidneys. The results indicated that the small intestine, stomach, and liver were the major organs for the distribution of 8,2'-diprenylquercetin 3-methyl ether metabolites. Furthermore, 27 metabolites showed various bioactivities predicted by the analysis of "PharmMapper", among which 9 metabolites showed anti-cancer activity. These results are very useful for understanding the metabolism and pharmacological actions as well as the effective forms and toxic actions of 8,2'-diprenylquercetin 3-methyl ether in vivo; moreover, they will lay the foundation for further studies on the metabolism of prenylflavonoid compounds.

journal_name

Fitoterapia

journal_title

Fitoterapia

authors

Ma LM,Xu F,Wang JZ,Shang MY,Liu GX,Cai SQ

doi

10.1016/j.fitote.2019.104191

subject

Has Abstract

pub_date

2019-09-01 00:00:00

pages

104191

eissn

0367-326X

issn

1873-6971

pii

S0367-326X(19)30773-7

journal_volume

137

pub_type

杂志文章

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