Metabolites and the pharmacokinetics of kobophenol A from Caragana sinica in rats.

Abstract:

:This research aims to study the metabolism and pharmacokinetics of phytoestrogen kobophenol A (1), the main active compound of Caragana sinica (Buc'hoz) Rehd. (Fabaceae), in rats. Metabolites of 1 in rats' feces were isolated and purified by multi-chromatograph techniques; three new metabolites of 1, named koboquinone A (M1), koboquinone B (M2) and koboquinone C (M3), were isolated, purified from rats' feces after they being orally administered with 1. Structure identification of the metabolites was fulfilled by spectroscopic analysis. M1 and M2 are structurally different to those natural occurring stilbene tetramers, which also have para-quinone structure. M1 also showed the activity of stimulating the proliferation of cultured osteoblasts. The pharmacokinetics of 1 in rats could be described by a two-compartmental model (P<0.05). The half-life was 0.68 h for i.v. administration and 5.78 h for oral administration. The oral bioavailability of 1 was calculated to be 2.0%; rats tissue distribution experiments show that 1 was prominently concentrated in livers. Both of the low oral bioavailability and the rapid reduction of 1 in blood indicated a suitable formulation is needed while it is developed as a new drug.

journal_name

J Ethnopharmacol

authors

Liang GL,Bi JB,Huang HQ,Zhang S,Hu CQ

doi

10.1016/j.jep.2005.05.016

keywords:

subject

Has Abstract

pub_date

2005-10-03 00:00:00

pages

324-9

issue

1-3

eissn

0378-8741

issn

1872-7573

pii

S0378-8741(05)00330-2

journal_volume

101

pub_type

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