Novel Type 1 5a-Reductase Inhibitors With Antiproliferative Potential On LNCaP Cells

June 2023 in “ Oriental Journal of Chemistry/Oriental journal of chemistry ”

Marisa Cabeza, Luis A. Menes, Evelyn Fuentes, Iván Bahena, Yvonne Heuze

type 1 5a-reductase inhibitors dehydroepiandrosterone derivatives testosterone dihydrotestosterone finasteride DHEA derivatives DHT

Studysummary This study demonstrated that derivatives of dehydroepiandrosterone (2a-b, 3a-f, and 4a-f) significantly reduced viable LNCaP prostate cancer cells, suggesting potential therapeutic use for metastatic prostate cancer, while finasteride did not alter cell viability. Our plain-language summary of this paper — not a Tressless recommendation.

The study found that dehydroepiandrosterone derivatives 2a-b, 3a-f, and 4a-f significantly reduced the proliferation of LNCaP cells, a type of prostate cancer cell, compared to testosterone treatment. Unlike finasteride, these derivatives decreased cell viability and inhibited the conversion of testosterone to dihydrotestosterone at high concentrations. This suggests that these derivatives have potential as therapeutic agents for treating metastatic prostate cancer.

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research Activity of Steroid 4 and Derivatives 4a–4f as Inhibitors of the Enzyme 5α-Reductase Type 1

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This study identified that derivatives 4, 4b, and 4c strongly inhibited the enzyme type 1 5α-reductase and decreased reproductive organ weights in hamsters, suggesting potential as prodrugs for prostate tumor growth inhibition.

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This study found that several dehydroepiandrosterone ester derivatives effectively reduced prostate and seminal vesicle weight in gonadectomized hamsters treated with testosterone, demonstrating potential antiandrogen effects comparable to Finasteride.

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This study found that the binding of finasteride to the enzyme 5a-reductase occurs at a slower rate than previously assumed, complicating the estimation of its real inhibitory constant.