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  • 标题:Aromatization of 19-Oxygenated Androst-4-ene-3, 6, 17-triones with Human Placental Microsomes
  • 本地全文:下载
  • 作者:Mitsuteru NUMAZAWA ; Takanori SUGIYAMA ; Masao NAGAOKA
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:1998
  • 卷号:21
  • 期号:3
  • 页码:289-292
  • DOI:10.1248/bpb.21.289
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:To gain insight into the aromatization sequence of androst-4-ene-3, 6, 17-trione (1), a suicide substrate of aromatase, the aromatization of its 19-hydroxy and 19-oxo analogs 2 and 3 with human placental microsomes, was studied using GC-MS. Steroids 2 and 3 were separately incubated with the microsomes in the presence of NADPH in air. The GC-MS analysis of the trimethylsilyl derivative of the aromatization product indicated that both the 19-oxygenated steroids 2 and 3 were aromatized to yield 6-oxoestrogens, 6-oxoestrone (4) and 6-oxoestradiol (5), in each experiment. The aromatization rates of substrates 2 and 3 were 605±48 and 1794±75 pmol/mg protein/10 min, respectively. These relatively higher rates, compared to that of the parent steroid 1 (73.2±6.6 pmol/mg protein/10 min), indicates that the suicide substrate 1 is aromatized through the 19-oxygenated intermediates 2 and 3.
  • 关键词:aromatization;androst-4-ene-3, 6, 17-trione;19-oxygenated analog;suicide substrate;GC-MS analysis
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