Abstract:
: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.
journal_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Lee SK,Kim GH,Kim DH,Kim DH,Jahng Y,Jeong TCdoi
10.1248/bpb.30.1991subject
Has Abstractpub_date
2007-10-01 00:00:00pages
1991-5issue
10eissn
0918-6158issn
1347-5215pii
JST.JSTAGE/bpb/30.1991journal_volume
30pub_type
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