Identification of a Tryptanthrin Metabolite in Rat Liver Microsomes by Liquid Chromatography/Electrospray Ionization-Tandem Mass Spectrometry(Biopharmacy)

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概要

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• Tryptanthrin originally isolated from Isatis tinctoria L. has been characterized to have anti-inflammatory activities through the dual inhibition of cyclooxygenase-2 and 5-lipoxygenase mediated prostaglandin and leukotriene syntheses. To characterize phase I metabolite(s), tryptanthrin was incubated with rat liver microsomes in the presence of NADPH-generating system. One metabolite was identified by liquid chromatography, electrospray ionization-tandem mass spectrometry. M1 could be identified as a metabolite mono-hydroxylated on the aromatic ring of indole moiety from the MS^2 spectra of protonated tryptanthrin and M1. The structure of metabolite was confirmed as 8-hydroxytryptanthrin with a chemically synthesized authentic standard. The formation of M1 was NADPH-dependent and was inhibited by SKF-525A, a general CYP-inhibitor, indicating the cytochrome P450 (CYP)-mediated reaction. In addition, it was proposed that M1 might be formed by CYP 1A in rat liver microsomes from the experiments with enriched rat liver microsomes.

• 2007-10-01

著者

• Lee Sang

  韓国

• Kim Dong

  College Of Pharmacy Kyung Hee University

• Jahng Yurngdong

  College Of Pharmacy Yeungnam University

• Jeong Tae

  College of Pharmacy, Yeungnam University

• Lee Sang

  College Of Agriculture And Life Sciences Kyungpook National University

• Jeong Tae

  College Of Pharmacy Yeungnam University

• KIM Ghee

  College of Pharmacy, Yeungnam University

• KIM Dong

  Bioanalysis and Biotransformation

• Kim Ghee

  College Of Pharmacy Yeungnam University

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