In Vitro Inhibition Assay: This work was performed at the MDS Pharma Services, Pharmacology Laboratories, Taiwan. The assay was an in vitro evaluation of the ability of an extract or a pure compound to inhibit the steroid 5alpha -reductase enzyme from metabolizing testosterone into dihydrotestosterone. This is an enzyme-immunoassay (EIA) for quantitative determination of testosterone in human serum or plasma. The significance of this type of inhibition is that it can lead to eradication of benign prostatic hyperplasia (BPH). Two distinct isozymes are found in mice, rats, monkeys and humans: type 1 and II. Each of these isozymes is differentially expressed in tissues and developmental stages. In human, type 1 steroid 5alpha -reductase is predominant in the sebaceous glands of most regions of skin, including scalp and liver and is responsible for approximately one third of circulating DHT. Inhibitors of steroid 5alpha -reductase may be of benefit in the treatment of androgenetic alopecia.
Inhibition of human 5alpha-2 reductase expressed in HEK293 cells assessed as suppression of conversion of [3]androstenedione at 10 uM incubated for 30 mins by radioactivity-based HPLC analysis
Inhibition of human 5alpha-2 reductase expressed in HEK293 cells assessed as suppression of conversion of [3]androstenedione at 2 uM incubated for 30 mins by radioactivity-based HPLC analysis
Inhibition of human 5alpha-2 reductase expressed in HEK293 cells assessed as suppression of conversion of [3]androstenedione incubated for 30 mins by radioactivity-based HPLC analysis
Inhibitory concentration against human recombinant steroid 5-alpha-reductase type 2 in stably transfected chinese hamster ovary 1827 cells using [3H]testosterone
Inhibition of human 5alpha reductase 2 expressed in HEK293 cells assessed as inhibition of conversion of [14C]4-androstene-3,17-dione to [14C]5R-androstane-3,17-dione at 0.3 uM after 3 hrs