Lee, Sang Kyu Kim, Ghee Hwan Kim, Dong Hyeon Kim, Dong Hyun Jahng, Yurngdong Jeong, Tae Cheon 2024-01-21T00:31:22Z 2024-01-21T00:31:22Z 2021-09-02 2007-10 0918-6158 https://pubs.kist.re.kr/handle/201004/134073 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 MS2 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. English PHARMACEUTICAL SOC JAPAN ISATIS-TINCTORIA PURE TRYPTANTHRIN PRINCIPLE ANALOGS AGENTS Identification of a tryptanthrin metabolite in rat liver microsomes by liquid chromatography/electrospray ionization-tandem mass spectrometry Article 10.1248/bpb.30.1991 1 BIOLOGICAL & PHARMACEUTICAL BULLETIN, v.30, no.10, pp.1991 - 1995 BIOLOGICAL & PHARMACEUTICAL BULLETIN 30 10 1991 1995 scie scopus 000250796400037 2-s2.0-35348929342 Pharmacology & Pharmacy Pharmacology & Pharmacy Article ISATIS-TINCTORIA PURE TRYPTANTHRIN PRINCIPLE ANALOGS AGENTS tryptanthrin rat liver microsome LC-ESI/MS metabolite cytochrome P450 (CYP)