Effects of Steroid 5.ALPHA.-Reductase Inhibitor ONO-9302 and Anti-Androgen Allylestrenol on the Prostatic Growth, and Plasma and Prostatic Hormone Levels in Rats.

Abstract

ABSTRACT-ONO-9302

Novel actions of progesterone: what we know today and what will be the scenario in the future?

“…Another mechanism attributed to progesterone is inhibition of pituitary LH release and action as an anti‐androgen in addition to 5 α ‐reductase‐blocking action [59] . In a study in rats, comparing the progesterone derivative allylestrenol with epristeride (5 α ‐reductase inhibitor), the former reduced the dihydrotestosterone and testosterone content of the prostate and plasma testosterone, LH and FSH levels suggesting the therapeutic potential of progesterone derivatives in the treatment of BPH [75] …”

“…[59] In a study in rats,comparing the progesterone derivative allylestrenol with epristeride (5a-reductase inhibitor), the former reduced the dihydrotestosterone and testosterone content of the prostate and plasma testosterone, LH and FSH levels suggesting the therapeutic potential of progesterone derivatives in the treatment of BPH. [75] Several progesterone derivatives were analysed further, in various studies, in regard to their 5a-reductase activity and role in prostate hypertrophy and cancer; [76][77][78] some compounds inhibited growth of cell lines of both prostate cancer and lymphocytes, without any toxic effects in vivo. [76] In studies comparing some progesterone derivatives of 17a-acetoxyprogesterone [77,79] with testosterone in gonadectomized male hamsters, significant decrease in prostrate weight was observed in the progesterone-derivative group, [77,79] as compared with testosterone-treated hamsters, and enzymatic activity was reduced [80] by 50%.…”

Role of aldo-keto reductases in development of prostate and breast cancer

“…An additional member, AKR1E1, identified in mice, has similar genomic organization to aldose reductase (AKR1B) (6,7). The enzymes in this family carry out a wide range of biological and pathological functions, including carbonyl detoxification, osmolytic regulation, hormonal metabolism, diabetic complications, and tumor development (8)(9)(10)(11)(12)(13)(14)(15)(16).…”

Testosterone 5?-reductase inhibitor bisnaphthoquinone derivative fromImpatiens balsamina

“…5a-Reductase inhibitors, selective inhibitors of DHT biosynthesis, are new classes of substances with very specific effects on type I and type II 5a-reductase. They may be of use for treatment of androgen-related skin disorders (Chen et al, 1996) such as acne (De Raeve et al, 1995;Ellsworth et al, 1996) and male pattern alopecia as well as benign prostate hypertrophy (Yasuda et al, 1997). Finasteride (Rasmusson et al, 1986) and epristeride (Holt et al, 1990) have been developed as steroidal 5a-reductase inhibitors.…”