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

doi:10.1248/CPB.38.2834

Paper

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

Published Oct 25, 1990 · M. Yoshihama, K. Tamura, M. Nakakoshi

Chemical & pharmaceutical bulletin

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17

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0

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Abstract

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.

In Vitro Study

Study Snapshot

14 alpha-hydroxyandrost-4-ene-3,6,17-trione is a potent and irreversible inhibitor of estrogen biosynthesis, suppressing serum estradiol levels in vivo.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

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

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References

Citations

Microbial biotransformation of bioactive and clinically useful steroids and some salient features of steroids and biotransformation

Microbial biotransformation of steroids yields novel metabolites with diverse activities, potentially benefiting chemoprevention and treatment of diseases like cancer, osteoporosis, HIV, and AIDS.

Biological transformations of steroidal compounds: A review

Microbial transformations of steroidal compounds can create diverse, biologically potent compounds with diverse structures, offering a model for mammalian metabolism.

Fundamentals of Steroid Chemistry and Biochemistry

Steroids are unique chemical compounds found throughout the animal and plant kingdom, with potential medicinal effects for various diseases and chemoprevention strategies.

Substituted androstanes as aromatase inhibitors

Substituted androstanes show potential as aromatase inhibitors for treating hormone-dependent mammary and ovarian tumors and benign prostatic tumors.

Aromatase Inhibitors and Breast Cancer

Aromatase inhibitors can effectively treat breast cancer, but resistance can develop when they are stopped, and their antitumor effect can be restored when they are resumed.