Summary of Effects of Plant Derived Anti-Androgens
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4.7. Reishi (Ganoderma lucidum)
Red reishi, commonly known as LingZhi in Chinese, is a mushroom thought to have many health benefits. In a research study exploring the anti-androgenic effects of 20 species of mushrooms, reishi mushrooms had the strongest action in inhibiting testosterone (3). That study found that reishi mushrooms significantly reduced levels of 5-alpha reductase, preventing conversion of testosterone into the more potent DHT. High levels of DHT are a risk factor for conditions such as benign prostatatic hypertrophy (BPH), acne, and baldness.
4.8. Licorice (Glycyrrhiza glabra)
Licorice is a flavorful substance that has been used in food and medicinal remedies for thousands of years. It is also known as “sweet root,” licorice root contains a compound that is about 50 times sweeter than sugar. It has been used in both Eastern and Western medicine to treat a variety of illnesses ranging from the common cold to liver disease. Licorice affects the endocrine system because it contains isoflavones (phytoestrogens), which are chemicals found in plants that may mimic the effects of estrogen and relieve menopausal symptoms and menstrual disorders. Licorice may also reduce testosterone levels, which can contribute to hirsutism in women.
A small clinical trial published in 2004 by Armanini and colleagues found that licorice root significantly decreases testosterone levels in healthy female volunteers. Women taking daily licorice root experienced a drop in total testosterone levels after 1 month and testosterone levels returned to normal after discontinuation. It is unclear as to whether licorice root affects free testosterone levels (4). The endocrine effect is thought to be due to phytoestrogens and other chemicals found in licorice root, including the steroid glycyrrhizin and glycyrrhetic acid, which also have a weak anti-androgen effect (5, 6).
4.9. White Peony (Paeonia lactiflora)
Chinese peony is a widely grown ornamental plant with several hundred selected cultivars. Many of the cultivars have double flowers with the stamens modified into additional petals. White peony has been important in traditional Chinese medicine and has been shown to affect human androgen levels in vitro. In a 1991 study in the American Journal of Chinese Medicine Takeuchi et al described the effects of paeoniflorin, a compound found in white peony that inhibited the production of testosterone and promoted the activity of aromatase, which converts testosterone into estrogen (7). To date, there have been no studies that translate or explore the clinical effects.
4.10. Green Tea (Camellia sinensis)
In addition to supporting the cardiovascular system and somewhat reducing the risk of cancer and type 2 diabetes (8), green tea may also have an important anti-androgen effect because it contains epigallocatechins, which inhibit the 5-alpha-reductase conversion of normal testosterone into DHT. As previously noted, this anti-androgen mechanism may help to reduce the risk of BPH, acne, and baldness. As yet, no randomized controlled trials of green tea for these androgen dependent conditions have been conducted.
4.11. Spearmint (Mentha spicata [Labiatae])
Spearmint, usually taken in the form of tea, has been thought for many years to have testosterone reducing properties. It is commonly used in Middle Eastern regions as an herbal remedy for hirsutism in females. Its anti-androgenic properties reduce the level of free testosterone in the blood, while leaving total testosterone and DHEAS unaffected, as demonstrated in a study from Turkey by Akdogan and colleagues, in which 21 females with hirsutism (12 with polycystic ovary syndrome and 9 with idiopathic hirsutism) drank a cup of herbal tea steeped with M. spicata twice daily for 5 days during the follicular phases of their menstrual cycles. After treatment with the spearmint tea, the patients had significant decreases in free testosterone with increases in luteinizing hormone, follicle-stimulating hormone, and estradiol (9). There were no significant decreases in total testosterone or DHEAS levels. This study was followed by a randomized clinical trial by Grant (10), which showed that drinking spearmint tea twice daily for 30 days (vs. chamomile tea, which was used as a control) significantly reduced plasma levels of gonadotropins and androgens in patients with hirsutism associated with polycystic ovarian syndrome. There was a significant change in patients’ self-reported dermatology-related quality of life indices, but no objective change on the Ferriman-Gallwey scale. It is possible that sustained daily use of spearmint tea could result in further abatement of hirsutism.
4.12. Black Cohosh (Actaea racemosa)
Black cohosh (Actaea racemosa) is a plant of the buttercup family. Extracts from these plants are thought to possess analgesic, sedative, and anti-inflammatory properties. Black cohosh preparations (tinctures or tablets of dried materials) are used to treat symptoms associated with menopause, such as hot flashes, although the efficacy has been questioned (11). The inhibitory effects of black cohosh extracts (Cimicifuga syn. Actaea racemosa L.) on the proliferation of human breast cancer cells has been reported recently (12), and Hostsanka. et al (13) have examined the plant’s effects on prostate cancer, another androgen hormone-dependent, epidemiologically important tumor. In that study, the inhibitory effect of an isopropanolic extract of black cohosh (iCR) on cell growth in androgen-sensitive LNCaP and androgen-insensitive PC-3 and DU 145 prostate cancer cells was investigated.
The authors found that regardless of hormone sensitivity, the growth of prostate cancer cells was significantly and dose-dependently down regulated by iCR. At a concentration between 37.1 and 62.7 μg/ml, iCR caused 50% cell growth inhibition in all cell lines after 72h. Increases in the levels of the apoptosis-related M30 antigen of approximately 1.8-, 5.9-, and 5.3-fold over untreated controls were observed in black cohosh-treated PC-3, DU 145, and LNCaP cells, respectively, with the induction of apoptosis being dose- and time-dependent.
Black cohosh extract was therefore shown to kill both androgen-responsive and non-responsive human prostate cancer cells by induction of apoptosis and activation of caspases. This finding suggested that the cells’ hormone responsive status was not a major determinant of the response to the iCR, and indicated that the extract may represent a novel therapeutic approach for the treatment of prostate cancer.
4.13. Chaste Tree (Vitex agnus-castus)
Chaste tree (or chasteberry) is a native of the Mediterranean region and is traditionally used to correct hormone imbalances. In ancient times, it was believed to be an anaphrodisiac, hence the name chaste tree. Clinical studies have demonstrated effectiveness of medications produced from extract of the plant in the management of premenstrual syndrome (PMS) and cyclical mastalgia (14). The mechanism of action is presumed to be via dopaminergic effects resulting in changes of prolactin secretion from the anterior pituitary. At low doses, it blocks the activation of D2 receptors in the brain by competitive binding, causing a slight increase in prolactin release. In higher concentrations, the binding activity is sufficient to reduce the release of prolactin (15).
Reduction in prolactin levels affects FSH and estrogen levels in females and testosterone levels in men. There is as yet no information regarding its efficacy in endocrine disease states such as PCOS, however, one small-scale study has demonstrated this prolactin reducing effect in a group of healthy males, and the implication is that it could be of use in mild hyperprolactinemia (16, 17). One could also theorize that it could be refined for use as a male contraceptive, because testosterone reduction should reduce libido and sperm production. This topic is further explored in a review by Grant & Anawalt (18).
4.14. Saw Palmetto (Serenoa repens)
Saw palmetto is a small palm tree native to eastern regions of the United States. Its extract is believed to be a highly effective anti-androgen as it contains phytoesterols. This has been the subject of a great deal of research with regards to the treatment of BPH (19, 20), androgenic alopecia (21), and PCOS (22). However, controlled trials and other convincing research on its efficacy are still lacking. In the context of BPH, there have been 2 reasonably sized clinical trials that found that saw palmetto extract use showed no difference in comparison to placebo (23, 24). In meta-analyses, it has been shown to be safe and effective in mild to moderate BPH when compared to finasteride, tamsulosin, and placebo (25, 26). However, a more recent meta-analysis showed that it is only superior specifically with regards to the symptom of nocturia (27). Therefore, evidence for its routine use is far from convincing and additional research is necessary to determine its true effectiveness.
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