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Preclinical Pharmacokinetics of Scoparone, Geniposide and Rhein in an Herbal Medicine Using a Validated LC-MS/MS Method

Overview
Journal Molecules
Publisher MDPI
Specialty Biology
Date 2018 Oct 27
PMID 30360359
Citations 10
Authors
Affiliations
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Abstract

The herbal formula Yin-Chen-Hao-Tang has been reported to have anti-fibrosis properties. The aim of this study was to reveal the pharmacokinetic characteristics of bioactive compounds in this herbal formula. A new high-performance liquid chromatography-tandem mass spectrometry method was developed and validated for simultaneous determination of scoparone, geniposide and rhein in rat plasma. A pharmaceutical herbal powder was administered to rats at doses of 1 g/kg and 3 g/kg orally. The method showed excellent linearity (r² > 0.999) and validation was successfully conducted for the pharmacokinetic study. The results show that the C values and areas under the curve of scoparone, geniposide and rhein were higher and not proportional to the dose in rat plasma, while the T and half-life values were consistent in the group that received 1 g/kg. The clearance of the higher dose (3 g/kg) did not decrease proportionally to that of the low dose. The results showed the nonlinear pharmacokinetic properties of scoparone, geniposide and rhein in Yin-Chen-Hao-Tang that suggested possible accumulation of bioactive compounds through oral administration. This pharmacokinetic study reveals that an increased dose of this herbal formula would largely increase the maximum concentration and bioavailability of scoparone, geniposide and rhein.

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References
1.
Meyer R, Hagemeyer C, Knoth R, KURZ G, Volk B . Oxidative hydrolysis of scoparone by cytochrome p450 CYP2C29 reveals a novel metabolite. Biochem Biophys Res Commun. 2001; 285(1):32-9. DOI: 10.1006/bbrc.2001.5111. View

2.
Wang X, Sun W, Sun H, Lv H, Wu Z, Wang P . Analysis of the constituents in the rat plasma after oral administration of Yin Chen Hao Tang by UPLC/Q-TOF-MS/MS. J Pharm Biomed Anal. 2008; 46(3):477-90. DOI: 10.1016/j.jpba.2007.11.014. View

3.
Tsang S, Bian Z . Anti-fibrotic and anti-tumorigenic effects of rhein, a natural anthraquinone derivative, in mammalian stellate and carcinoma cells. Phytother Res. 2014; 29(3):407-14. DOI: 10.1002/ptr.5266. View

4.
Cai Y, Sun M, Xing J, Corke H . Antioxidant phenolic constituents in roots of Rheum officinale and Rubia cordifolia: structure-radical scavenging activity relationships. J Agric Food Chem. 2004; 52(26):7884-90. DOI: 10.1021/jf0489116. View

5.
Cai H, Song Y, Xia W, Jin M . Aqueous extract of Yin-Chen-Hao decoction, a traditional Chinese prescription, exerts protective effects on concanavalin A-induced hepatitis in mice through inhibition of NF-kappaB. J Pharm Pharmacol. 2006; 58(5):677-84. DOI: 10.1211/jpp.58.5.0013. View