Serenoa repens (Serenoa repens W. Bartram Small, fructus), dry extract titrated to 45% in fatty acids; Pygeum africanum (Pygeum africanum Hook. f., cortex), dry extract titrated to 10% in phytosterols; Stinging Nettle (Urtica dioica L., radix) root, dry extract titrated to 0.8% in beta-sitosterol; Green Tea (Camellia sinensis L. Kuntze, folium), dry extract titrated to 98% in total polyphenols and to 40% in epigallocatechin gallate; Soya Isoflavones, titrated to 40%; Lycopene; Astaxanthin; L-Cysteine; Beta-Sitosterol; Grape (Vitis vinifera L., semen) seeds, dry extract titrated to 95% in proanthocyanidins; Sorbitol; Cellulose; Talc; Cutin; Magnesium Stearate.
Serenoa repens, dry extract titrated to 45% in fatty acids in a suitable dose (640 mg daily) replacing 320 mg of fat-soluble extract titrated to 90% in fatty acids
Serenoa repens (Saw Palmetto, Sabal serrulata, Dwarf palm) is a small broad-leaved plant with dark red berries native to the United States (specifically Florida) as well as Southern Europe and North Africa.
The berry extract contains one main active ingredient, beta-sitosterol, as well as other sterols, free fatty acids, carotenoids, essential oils and polysaccharides.
Natives used the berries to treat urologic dysfunction, prostate inflammation, erectile dysfunction and testicular atrophy.
As early as the late 20th century, the extract was included in the official American pharmacopoeia. However, it was only recently that its efficacy in treating benign prostate hyperplasia was acknowledged by a series of controlled clinical trials conducted on approximately 3,000 patients.
Its mechanism of action is not known: it may depend on the combination of an antagonistic effect on sex hormones, anti-inflammatory action and alteration of cholesterol metabolism.
In the United States, the National Institute of Health has also shown its interest in the small palm. However, the literature published so far is inadequate, especially with regard to the duration of trials and the variability of research protocols.
The lipophilic extract (90-95% of fatty acids and sterols) of the berries of Serenoa repens has long been used as an adjuvant in the treatment of benign prostatic hyperplasia stage I and II and the symptoms associated with it.
Taken orally, it has been shown to have clear anti-androgenic effects, inhibiting the enzyme 5-alpha-reductase.
In short, the efficacy of Serenoa repens is given by the synergy of different mechanisms of action:
- Inhibition of 5-alpha-reductase, an enzyme involved in converting testosterone to dihydrotestosterone (DHT)
- Selective local antagonism of the link between dihydrotestosterone and androgen receptors.
Hence it can be considered a sound alternative to synthetic drugs in the treatment of benign prostatic hypertrophy (BPH) and in the treatment of androgenetic alopecia (AGA).
Pygeum africanum, dry extract titrated to 10% in phytosterols
Pygeum africanum (Prunus africana) (African plum tree) is an evergreen species whose beneficial properties on the urinary tract were already known to native African populations. The active ingredients obtained from the bark include fatty acids, sterols such as beta-sitosterin, triterpenes and two alcohols, namely tetracosanol and docosanol.
The American Journal of Medicine recently published all the results concerning 18 trials on the efficacy of Pygeum africanum: the data showed that the extract balances the urinary flow and irritative symptoms in patients with prostatic hypertrophy.
Its peripheral antiandrogen action is similar to that of Serenoa repens, as its ingredients include the 5-alpha-reductase inhibitor, beta-sitosterol. As pentacyclic triterpenes act on 5-alpha-lipo-oxygenase, they are likely to be responsible for reducing the production of leukotrienes, which function as local mediators of inflammation in atopic dermatitis and psoriasis.
Mechanisms of action of Pygeum africanum:
– inhibition of 5-alpha-reductase activity;
– peripheral receptor antagonist action;
– anti-leukotriene action;
– weak oestrogen-like action.
Stinging nettle root, dry extract titrated to 0.8% in beta-sitosterol
Stinging nettle has long been widely used in herbal medicine as well, for its diuretic and anti-inflammatory properties; in addition, it is considered useful against benign prostatic hypertrophy.
Its diuretic and anti-inflammatory actions are mainly attributed to stinging nettle leaves, and especially to the caffeic acid derivates that are contained in stinging nettle. Several clinical trials confirmed these properties of the plant. In particular, such studies showed that stinging nettle extracts exert their anti-inflammatory action through different mechanisms, such as inhibition of leukotriene synthesis by the enzyme 5-lipoxygenase and inhibition of inflammatory prostaglandin production through cyclooxygenase.
Stinging nettle is known to be useful against benign prostatic hypertrophy (BPH), although the exact mechanism of action is not clear yet.
In vitro studies showed that the stinging nettle root extract has a high affinity for SHBG (Sex Hormone Binding Globulin) and can bind it to its receptors in prostatic tissue.
Stinging nettle has also been shown to inhibit aromatase (an enzyme responsible for converting androgens to oestrogens) in the prostate.
Green Tea, dry extract titrated to 98% in polyphenols and 40% in EGCG
For a few years green tea has been studied for its effects on the health and longevity of populations who regularly consume it in large quantities. Epigallocatechin gallate (EGCG) is the catechin to which several studies have attributed an outstanding role in the beneficial effects of green tea.
The primary action of EGCG is to strengthen endogenous antioxidant defences (catalase, superoxide dismutase and glutathione peroxidase), thereby reducing cellular damage. This has beneficial effects on all tissues.
Catechins can act as antioxidants by chelating metals, thereby reducing the formation of free radicals, scavenging the hydroxyl and superoxide radicals, inhibiting lipid peroxidation and transferring a hydrogen atom to peroxide radicals, allowing the autocatalytic process as typical of oxidative reactions to be interrupted. Antioxidant activity is responsible for anticancer and antiatherosclerotic effects.
The antimutagenic effect is a consequence of such action: in vitro data revealed, on the one hand, inhibition of oncogenesis as induced by certain chemical compounds found in tobacco (nitrosamines, potent lung cancer inducers) and, on the other, reduced lipid peroxidation as induced by exposure to x ray. Further studies conducted on humans support the possibility that green tea consumption may prevent some forms of cancer, especially in the gastrointestinal tract (stomach, small intestine, pancreas, colon). In vitro data showed that the green tea extract has an inhibiting effect on the growth of tumour cells in the mammary gland. Dysregulated interactions between cellular receptors and tumour promoters, growth and hormonal factors, seems to be a possible mechanism. In animal models, the green tea extract inhibited the formation of skin lesions and tumours induced by UVB exposure.
Numerous epidemiological studies examined the association between tea consumption and the development of cardiovascular diseases. A recent meta-analysis provided some interesting data, suggesting that green tea polyphenols protect LDL from peroxidation. It was also shown to improve endothelium-dependent vasodilation. A study conducted on 550 middle-aged men followed for 15 years showed that daily intake of at least 30 mg of polyphenols reduced the risk of coronary heart disease mortality by 70%. In another study, 520 men and women (age: ³30 years) who underwent coronary arteriography were asked to fill in a questionnaire on eating habits, clinical risk factors and lifestyles. The results showed that green tea consumption, especially in men, is inversely associated with the development of coronary atherosclerosis.
The green tea extract interestingly serves as a functional food in weight control. In some clinical trials, the polyphenols found in this plant were shown to help stimulate fat metabolism and oxidation. Green tea acts on the fat reserves of the body, boosting both the production of adrenalin and the combustion of reserve fats; these properties are further enhanced by diuretic action. In a double-blind trial, 60 obese women (age: 30-45 years) were divided into two groups: one was assigned to receive a diet (1,800 kcal) and green tea capsules (250 mg 3 times daily); the other was assigned to receive a diet and placebo. After 2 weeks, the group receiving green tea had lost twice as much weight as the placebo group. After 4 weeks, the group receiving green tea had lost 2.90 kg vs. 0.97 kg in the placebo group.
Furthermore, EGCG helps inhibit the enzyme 5-alpha-reductase (mainly type I), which is most responsible for sebum overproduction, and thus for underlying skin and hair diseases, as it converts testosterone to more harmful DHT (dihydrotestosterone). Indeed this type of isoenzyme is plentifully available in sebaceous glands, and has been found to be one of the main causes of acne. Green tea acts on this process by increasing SHBG (sex-hormone binding globulin), which prevents testosterone from converting to DHT.
Soya isoflavones
Soya beans are a legume which has been known for several millenniums for its beneficial effects on health in general and hair in particular. Its seeds have a high protein content (40%) and significant amounts of essential amino acids as well as vitamins, glucides, unsaturated fatty acids and mineral salts. They also contain isoflavones, which act as phyto-oestrogens: genistein, daidzein, glycitein, biochanin and formononetin. Isoflavones function as weak oestrogens, helping reduce testosterone and oestrogen levels and increasing the amount of SHBG. Daidzein, a soya bean phyto-oestrogen, is converted to its main metabolite, equol, by intestinal flora. Studies conducted at Colorado State University’s Department of Biomedical Sciences showed that equol blocks the activity of DHT, occupying its receptor site.
- Rich in proteins and essential amino acids
- Rich in vitamins, mineral salts, glucides, unsaturated fatty acids, isoflavones
- Antioxidant, effective in reducing cholesterol
- Daidzein occupies the DHT follicle receptor through its metabolite, equol
Useful in fighting the negative effects of androgenetic alopecia and benign prostatic hypertrophy.
Lycopene
Lycopene is the predominant carotenoid in tomatoes and the human body, followed by beta-carotene, lutein and zeaxanthin. The human body cannot synthesize lycopene; hence it must be obtained through the diet. Over 80% of the lycopene found in the human body comes from the consumption of tomatoes and tomato products.
Lycopene was shown to activate the antioxidant response of the human body, through SOD (superoxide dismutase).
Hence the group receiving lycopene experienced increased production of SOD, a potent antioxidant enzyme. In addition, they showed a decrease of DNA damage in blood cells.
Lycopene is used in many formulations of prostate food supplements, since it seems to act as a 5-alpha-reductase inhibitor.
Astaxanthin
Astaxanthin has significant beneficial effects in diseases involving the central nervous system as well as in neurodegenerative diseases, diseases involving the eyes, joints, heart, diabetes, inflammatory states and immune dysfunctions. Some recent studies showed significant astaxanthin activity in inhibiting the enzyme 5-alpha-reductase, thus proving this molecule effective in reducing the symptoms of prostatic hyperplasia and in fighting prostate cancer. According to these studies, the same compound seems to increase the efficacy of the Serenoa repens extract in its anti-DHT activity and is likely to be useful against androgenetic alopecia as well.
Beta-sitosterol
Beta-sitosterol is a steroid which can be extracted from Saw Palmetto (Serenoa repens), Pygeum africanum (of which it is the main active ingredient) and Hypoxis rooperi (a plant with anti-DHT properties). It has the characteristics of both a replaced 17-progestogen and a weak oestrogen (and anti-oestrogen). It is able to bind to both 5-alpha reductase (type I and type II) and cytosolic androgen receptors which bind to dihydrotestosterone (which is responsible for androgenetic alopecia) and other androgens. It also binds to cell membrane oestrogen receptors, activating them, though acting as an anti-oestrogen, preventing the receptors to bind to real oestrogens. At the hair follicle level, such activation can promote the activation of the cell membrane adenylyl cyclase, which, in turn, stimulates the mitosis of the hair matrix, thereby helping to maintain the anagen phase and optimize the catagen phase.
Grape seeds, dry extract titrated to 95% in proanthocyanidins
Oligomeric proanthocyanidins (OPCs) belong to the vast reign of bioflavonoids, natural substances that in recent studies have shown remarkable antioxidant and healing properties.
OPCs are a unique example of biologically active antioxidants tested pharmacologically and clinically, for the prevention and treatment of cardiovascular diseases.
Even more remarkable are the antioxidant properties that some studies have shown to be similar to those of two enzymes involved in fighting oxidative damage, such as superoxide dismutase (SOD) and catalase.
In addition, the strong scavenging power of OPCs against free radicals was found to be the basis for vasoprotective activity: they improve the elasticity and functionality of the capillary bed, thereby promoting tissue vascularization.
In the rat, proanthocyanidins have been shown in vitro to promote epithelial proliferation and in vivo to trigger the development of the hair follicle, thereby prolonging the anagen phase. The grape seed extract contains pro-anthocyans, procyanidin B2, flavonoids, vitamins and trace elements.
L-cysteine
This sulphur-containing amino acid plays a key role in the endogenous synthesis of skin appendages, including hair, nails and epidermis.
As it is essential in keratinization processes, it is plentifully available on the outermost layer of the hair cuticle. Scientific animal tests showed that cysteine deficiency results in markedly reduced hair production. Hence cysteine is used to stimulate the growth of hair and nails, while enhancing their strength.
Recommended intake: 2 tablets of Vitaminity DHT-Blocker daily, with plenty of water. The tablets can be taken at any time of the day, with or between meals.
