14 alpha-hydroxyandrost-4-ene-3,6,17-trione as a mechanical-based irreversible inhibitor of estrogen biosynthesis

Various derivatives of androst-4-ene-3,17-dione derived from microbial transformation were evaluated as inhibitors of human placental aromatase. 14 alpha-Hydroxyandrost-4-ene-3,6,17-trione was the most potent inhibitor showing a time-dependent, pseudo-first-order inactivation of aromatase in the pre...

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Bibliographic Details
Published inChemical & pharmaceutical bulletin Vol. 38; no. 10; pp. 2834 - 2837
Main Authors Yoshihama, M, Tamura, K, Nakakoshi, M, Nakamura, J, Fujise, N, Kawanishi, G
Format Journal Article
LanguageEnglish
Published Japan 01.10.1990
Subjects
Androstenols - pharmacology
Animals
Aromatase - metabolism
Depression, Chemical
Estrogen Antagonists - pharmacology
Estrogens - biosynthesis
Female
Humans
In Vitro Techniques
Male
Microsomes - drug effects
Microsomes - enzymology
Microsomes - metabolism
Organ Size - drug effects
Placenta - drug effects
Placenta - enzymology
Placenta - metabolism
Pregnancy
Rats
Rats, Inbred Strains
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Summary:Various derivatives of androst-4-ene-3,17-dione derived from microbial transformation were evaluated as inhibitors of human placental aromatase. 14 alpha-Hydroxyandrost-4-ene-3,6,17-trione was the most potent inhibitor showing a time-dependent, pseudo-first-order inactivation of aromatase in the presence of reduced nicotinamide adenine dinucleotide phosphate with apparent Ki of 1.3 microM and Kinact of 0.23 min-1. This compound also inhibited aromatase in rat ovary and suppressed serum estradiol levels in in vivo experiments.
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ISSN:0009-2363
DOI:10.1248/cpb.38.2834