Testosterone 5α-Reductase Inhibitors, Menaquinone 7 Produced by a Bacillus and Phenazine Methosulfate

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Menaquinone 7 (MW : 649,C_<46>H_<64>O_2), a natural electron acceptor for steroid ring A dehydrogenations, produced by Bacillus sp. SNU-299,was isolated as a rat prostate testosterone 5α-reductase inhibitor with an IC_<50> value of 4.0×10^<-5> M from the cultured broth. Phylloquinone was as active as the purified microbial metabolite with an IC_<50> value of 6.6×10^<-4> M. On the basis of this evidence, the inhibitory activities of electron carriers, menadione, phenazine methosulfate, and 2,6-dichlorophenolindophenol, for rat prostate testosterone 5α-reductase were tested, and the IC_<50> values were 3.1×10^<-6> M, 4.9×10^<-8> M, 8.9×10^<-5> M, respectively. A product of the 5α-reductase enzyme reaction and an electron and proton carrier, NADP^+, inhibited the 5α-reduction by rat prostate testerone 5α-reductase with an IC_<50> value of 9.2×10^<-5> M. However, the inhibition effect of a proton carrier, carbonylcyanide-m-chlorophenylhydrazone, for rat prostate testosterone 5α-reductase was substantially inactive.
公益社団法人日本薬学会の論文
1999-12-15