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An in vitro metabolic system of gut flora and the metabolism of ginsenoside Rg3 and cholic acid.

European journal of drug metabolism and pharmacokinetics (2013-06-12)
Chunyan Zhao, Runbin Sun, Bei Cao, Shenghua Gu, Jieyu Zhao, Linsheng Liu, Xinwen Wang, Weibin Zha, Xiaoyi Yu, Wenjing Xiao, Yong Mao, Chun Ge, Jiaqi Ju, Lixiang Aa, Fei Fei, Yi Ding, Jiye Aa, Guangji Wang
ABSTRAKT

For orally administered drugs, the metabolism of a drug by the gut flora plays an important role in the bioavailability, activation and disposition of the drug in vivo. However, no in vitro system is currently available to evaluate the metabolism of a drug by the gut flora before the drug is absorbed into the body. This paper presents an in vitro metabolic system in an anaerobic environment that could be used to evaluate the metabolism of an endogenous compound, cholic acid, and a xenobiotic compound, ginsenoside Rg3. We showed that the proliferation of the anaerobic bacteria of the gut content of hamsters produced a similar composition of gut flora in a culture medium for yeast to that in vivo. Incubation of ginsenoside Rg3 and cholic acid in the anaerobic in vitro system efficiently produced the metabolites Rh2 and deoxycholic acid, respectively, similar to those seen in the gut content in vivo. In comparison with in vivo analysis, this anaerobic in vitro metabolic system is convenient, reproducible, economic and animal saving, and can easily be applied to assess the transformation and disposition of a drug before it enters into the circulatory system.

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Sigma-Aldrich
Cholic acid, from bovine and/or ovine, ≥98%
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3-Ethyl-2,4-pentanedione, mixture of tautomers, 98%
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Sodium hydroxide solution, 49-51% in water, eluent for IC
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Methanol, suitable for NMR (reference standard)
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Sodium hydroxide concentrate, 0.1 M NaOH in water (0.1N), Eluent concentrate for IC
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Diethyl ether
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Sodium hydroxide, BioUltra, suitable for luminescence, ≥98.0% (T), pellets
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Sodium hydroxide solution, 1.0 N, BioReagent, suitable for cell culture
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Heptane, analytical standard
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Diethyl ether, analytical standard
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Methanol, analytical standard
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Cholic acid, European Pharmacopoeia (EP) Reference Standard
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Heptane, Pharmaceutical Secondary Standard; Certified Reference Material
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