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J Enzyme Inhib Med Chem ; 24(6): 1211-9, 2009 Dec.
Article in English | MEDLINE | ID: mdl-19912054

ABSTRACT

Anaerobic incubation of prednisone 1 with human intestinal bacteria (HIB) afforded nine metabolites: 5beta-androst-1-ene-3,11,17-trione 3, 3alpha-hydroxy-5alpha-androstane-11,17-dione 4, 3beta,17alpha,20-trihydroxy-5alpha-pregnan-11-one 5, 3alpha,17alpha-dihydroxy-5alpha-pregnane-11,20-dione 6, 3alpha,17alpha-dihydroxy-5beta-pregnane-11,20-dione 7, 3beta,17beta-dihydroxy-5alpha-androstan-11-one 8beta, 3beta,17alpha-dihydroxy-5alpha-androstan-11-one 8alpha, 3alpha,17beta-dihydroxy-5alpha-androstan-11-one 9beta, and 3alpha,17alpha-dihydroxy-5alpha-androstan-11-one 9alpha. The structures of these metabolites (3-9) were elucidated using several spectroscopic techniques. Computer-aided prediction of potential biological activities of the isolated prednisone metabolites (3-9) revealed potential inhibition of prostaglandin E2 9-ketoreductase (PGE2 9-KR). Docking studies applied to PGE2 9-KR allowed recommendation of the metabolites 4, 8beta, and 8alpha for further pharmacological study as PGE2 9-KR inhibitors.


Subject(s)
Anti-Inflammatory Agents/metabolism , Bacteria/metabolism , Intestines/microbiology , Prednisone/metabolism , Anaerobiosis , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/pharmacokinetics , Bacteria/growth & development , Biotransformation , Computer Simulation , Humans , Hydroxyprostaglandin Dehydrogenases/antagonists & inhibitors , Hydroxyprostaglandin Dehydrogenases/metabolism , Prednisone/chemistry , Prednisone/pharmacokinetics , Spectrum Analysis
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