In Vitro and In Vivo Effects of 17β-N-(4-Phenylcarbamoyl) Androst-4-en-3-one Derivatives as 5α-Reductase Inhibitors on Androgen-Dependent Glands

    September 2020 in “ Current Enzyme Inhibition ”
    Marisa Cabeza, Lucero Bautista, Eugene Bratoeff, Juan Rodríguez Soriano, Yvonne Heuze
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    TLDR Three compounds were found to inhibit a prostate disease-related enzyme and reduce prostate size more effectively than the current treatment, suggesting they could be used for treating benign prostatic hyperplasia.
    The study investigated the activity of four derivatives of 17β-phenyl carbamoyl-androst-4-en-3-one as inhibitors of the 5α-reductase enzyme, which is involved in prostate diseases. The in vitro effects of these compounds were tested on the human prostate enzyme, 5α-reductase, and their in vivo effects were studied in a hamster model of prostate hypertrophy. The results showed that three of the compounds (1, 3, and 4) significantly inhibited the in vitro activity of the 5α-reductase enzyme more effectively than finasteride, a known 5α-reductase inhibitor. These compounds also reduced the size of hamster flank organs and the weight of the prostate more effectively than finasteride, without causing toxic effects. The study concluded that these compounds could have potential therapeutic use for the treatment of benign prostatic hyperplasia.
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