Use of bioconversion for the preparation of [4-14C]-labeled 7 alpha- and 7 beta-hydroxylated derivatives of dehydroepiandrosterone and epiandrosterone

Steroids. 2002 Dec;67(13-14):1121-7. doi: 10.1016/s0039-128x(02)00072-7.

Abstract

The 7 alpha- and 7 beta-hydroxylated derivatives of [4-14C]-dehydroepiandrosterone were prepared with use of the yeast-expressed human cytochrome p4507B1. Epiandrosterone (EPIA), 5 alpha-androstane-3beta,17 beta-diol, and 5 alpha-androstane-3,17-dione were obtained after incubation of [4-14C]-5 alpha-dihydrotestosterone with Escherichia coli-expressed (3beta,17 beta)-hydroxysteroid dehydrogenase from Pseudomonas testosteroni. The 7 alpha- and 7 beta-hydroxylated derivatives of [4-14C]-EPIA produced were prepared after incubation with mycelium of Rhizopus nigricans. Each labeled steroid was purified by chromatography and identified by crystallization to constant specific activity after isotopic dilution with each authentic steroid carrier. Production yields and radio-purity measurements allowed the use of such procedures for the preparation of the described radio-steroids for studies of metabolism and mode of action.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Androstane-3,17-diol / metabolism
  • Androsterone / analogs & derivatives*
  • Androsterone / biosynthesis*
  • Androsterone / chemistry
  • Androsterone / isolation & purification
  • Cholesterol 7-alpha-Hydroxylase / metabolism
  • Chromatography, High Pressure Liquid
  • Dehydroepiandrosterone / analogs & derivatives
  • Dehydroepiandrosterone / metabolism
  • Escherichia coli
  • Humans
  • Hydroxylation
  • Hydroxysteroid Dehydrogenases / metabolism
  • Molecular Structure
  • Pseudomonas / enzymology
  • Rhizopus

Substances

  • Androstane-3,17-diol
  • Dehydroepiandrosterone
  • Androsterone
  • Hydroxysteroid Dehydrogenases
  • Cholesterol 7-alpha-Hydroxylase