Novel Antiandrogenic 5α-Reductase Inhibitors with Antioxidant Activity

Background. Steroids are biomolecules with a basic structure made up of cyclopentanoperhydrophenanthrene. Two steroids derived from cholesterol are testosterone, as natural androgen, and progesterone, as natural antiandrogen. Reactive oxygen species (ROS) may act as a metabolic signal-mediating response to changes in glucose, and hormones. Antiandrogens can be prescribed to treat an array of diseases and disorders as Gender dysphoria. In men, antiandrogens are most frequently used to treat prostate cancer and hyperplasia. Methods.The present study has the aim of pharmacological evaluation of several new steroid derivatives that were prepared from the commercially available 16-dehydropregnenolone acetate. The biological activity of the new steroidal derivatives was determined. The neuroprotection effect of the steroids was demostrated using the biomarkers of oxidative stress on male rat brain and liver with hypoglycemia induced. Enzyme kinetics was demostrated by the inhibition of 5α-reductase enzyme on myelin of brain. Conclusion. This study suggest that steroid 12 derivatives with an electrophilic center can interact more efficiently with the 5α-reductase enzyme and then induce neuroprotection in hypoglycemia animal model. Further research with clinically meaningful endpoints is needed to optimize the use of antiandrogens in these hormonal therapies.