Dihydrotestosterone (DHT, 5α-dihydrotestosterone, 5α-DHT, androstanolone or stanolone) is an endogenous androgen sex steroid and hormone. The enzyme 5α-reductase catalyzes the formation of DHT from testosterone in certain tissues including the prostate gland, seminal vesicles, epididymides, skin, hair follicles, liver, and brain. This enzyme mediates reduction of the C4-5 double bond of testosterone. Relative to testosterone, DHT is considerably more potent as an agonist of the androgen receptor (AR). In addition to normal biological functions, DHT also plays an important causative role in a number of androgen-dependent conditions including hair conditions like hirsutism (excessive facial/body hair growth) and pattern hair loss (androgenic alopecia or pattern baldness) and prostate diseases such as benign prostatic hyperplasia (BPH) and prostate cancer.
An androgen antagonist (anti-androgen) can broadly be defined as any compound that has the biological effect of blocking or suppressing the action of DHT (Dihydrotestosterone) within the human body.
This may occur at any point in the hypothalamic-pituitary-gonadal-end-organ axis and could be through a direct effect on gonadotropin production at the level of the pituitary or by competing for binding sites at the receptor level on the normally androgen sensitive tissues in the body.
Androgens themselves have a diverse range of effects in both males and females and their dysregulation can give rise to a variety of clinical disorders, including polycystic ovarian syndrome, the most common endocrine disorder in females, which affects up to 7% of the population; hirsutism; acne vulgaris; prostatic hyperplasia; and male pattern baldness.
There are already several medical treatments that act as androgen antagonists and have recognized uses; however, in recent years, there has been an increasing demand for complementary and alternative therapies, and this has included an interest in the development and use of more plant-derived anti-androgen therapies.
This is especially relevant as some medications currently in use have been found to have sub-optimal efficacy in clinical practice, and many patients are keen to try ‘natural’ or ‘alternative’ approaches as opposed to synthetically derived compounds.