Herbal Male Enhancement Ingredients

LJ100^® is a potent natural product developed by researchers at the University of Malaysia and the Massachusetts Institute of Technology. This patented, highly concentrated (100:1) and standardized (20–22% glycoproteins, 40% glycosaponins, 30% polysaccharides) extract of the herb known as Long Jack, Tongkat Ali, or Pasak Bumi (Eurycoma longifolia Jack) has demonstrated marked effects on sexual function. In the jungles of Southeast Asia, the root of Long Jack has traditionally been used to enhance relaxed vitality, virility, and male libido. Scientific studies demonstrate that the herb can significantly increase signs of sexual arousal,¹ sexual motivation,^2,3 sexual response,⁴ sexual attention,⁵ and libido^6,7 in animals. Researchers suggest that their results support the traditional use of Long Jack as an aphrodisiac and sexual enhancer for men.^8,9 Another animal study confirms that this herb can also have a relaxing, anti-anxiety effect.¹⁰

Further research has examined the effects of LJ100^® on SHBG (sex hormone binding globulin), DHEA (dehydroepiandrosterone – a precursor of testosterone) and testosterone in male volunteers aged 32–51 years. It was found that DHEA levels increased by an average of 47%, while SHBG decreased by 66% after three weeks of treatment. At the same time, testosterone production remained within the normal range. Taken together, these findings explained the overall increase in the availability of free testosterone detected in the blood (up to 73% after three weeks of use).This study also reported that use of LJ100^® brought about major improvements in both physical and psychological aspects of sexual desire and activity, while at the same time increasing blood flow to the penis in more than half of the volunteers. ¹¹

LJ100^® is a highly concentrated extract. Excessive use may result in irritability, impatience, insomnia, and other signs of over-stimulation. While some users can tolerate up to 100 mg/day or more, others may feel this to be excessive. In our formula, LJ100^® acts as a lower-dose synergistic catalyst to enhance the activity of the other male potency herbs.

1. PMID: 15803965
2. PMID: 14964739
3. PMID: 9868556
4. PMID: 13678248
5. PMID: 12685506
6. PMID: 12670032
7. PMID: 9353636
8. PMID: 11507738
9. PMID: 11564133
10. PMID: 10361892
11. Julisasi Tri Hadiah, Kebun Raya Bogor Staff. Eurycoma longifolia Jack. (Pasak Bumi), Explorasi 2.4: 6. Tambi, M.I.M.et al. 2002. Water-soluble extract of Eurycoma longifolia Jack as a potential natural energizer for healthy aging in men. National Population and Family Development Board, Malaysia. Human Reproduction Specialist Center Study.

Cayenne (Capsicum frutescens and related spp.), also known as Chili Pepper, has long been used as a spicy, strongly warming circulatory, digestive, and nervous system stimulant and ‘catalyst’ in formulas to enhance the bioavailability of other ingredients. ¹ Originating from Tropical America, this potent herb was part of the original Mayan recipe for transforming raw chocolate into the spicy, bittersweet fermented drink which they revered as the ‘food of the gods.’² Capsicum species are part of the Materia Medica in traditional systems worldwide, including Ayurveda and TCM.

Cayenne contains a group of pungent principles, the capsaicinoids. The most famous of these is capsaicin, a potent compound that gives hot sauce its fiery flavor. The capsaicinoids are largely responsible for this herb’s peripheral vasodilating properties, which encourage the flow of blood from deep within the body to structures on the surface, including the penis. A recent Japanese study found that even sweet red peppers had a stimulating action on the nervous system in humans.³ Cayenne is also rich in the oil-soluble antioxidants known as carotenoids, including the carotenes, lutein, zeaxanthin, beta-cryptoxanthin, capsanthin, and capsorubin. These antioxidants help protect the blood vessels from free radical damage and lipid peroxidation, thereby enhancing blood flow.⁴ A carotenoid-rich diet is associated with improved parameters of cardiovascular health.⁵

A new clinical study has confirmed in humans the observation that capsaicinoids can act as metabolic stimulants,⁶ an effect which has been noted in several animal studies. A previous study examining digestive energy metabolism in men found that dietary Cayenne had a beta-adrenergic effect, increasing energy expenditure and carbohydrate oxidation after a meal.⁷ Another investigation has reported that four weeks of regular consumption may have cardiovascular benefits specifically for men.⁸ In addition, animal studies have demonstrated that consumption of Cayenne can have anti-inflammatory and antioxidant effects.^9,10

Safety: As a spice, Cayenne has GRAS status (generally recognized as safe). Its pungent constituent, capsaicin, is approved as an OTC product for external use in creams for relieving arthritis and joint pains. The amount of Cayenne used in our formula is within the limits commonly found in certain foods. Although it actually benefits the digestion in many people, those with inflammatory conditions of the digestive tract may need to avoid hot, spicy ingredients including Cayenne. Adverse effects and/or drug interactions are rarely reported for dietary and therapeutic amounts of this herb.¹¹ A recent study found no adverse effects when men ingested a large single dose of concentrated capsaicinoids.¹²

References

1. Green, James. 2007. The Male Herbal. Berkeley, CA: Crossing Press. Pp. 236-7.
2. Grivetti, Louis Evan and Howard-Yana Shapiro, eds. 2009. Chocolate: History, Culture, and Heritage. Hoboken, NJ: Wiley. Pp. 3-5.
3. PMID: 17341828
4. PMID: 16923216
5. PMID: 12828795
6. PMID: 19056576
7. PMID: 8926537
8. PMID: 16929238
9. PMID: 18380920
10. PMID: 12748978
11. Stargrove, Treasure, & McKee. 2008. Herb, Nutrient, and Drug Interactions. St Louis, MO: Mosby Elsevier.
12. PMID: 19037804

Damiana (Turnera aphrodisiaca), also known as Bourrique, is an aromatic bush originating from the Caribbean and Central American regions. The spicy leaves of this much-respected herb have been used by native peoples for generations as a warming, simulating aphrodisiac and sexual energy tonic with mood-elevating effects. Traditionally, Damiana is believed to relax and tonify the nervous system, encourage the circulation, and enhance sexual stamina and performance.¹ Although it has a long history of use and is very popular (especially among Latino men), there has actually been little scientific study of this potent herb until very recently.

The constituents of Damiana include several flavonoids (e.g., luteolin, apigenin, and syringetin) which have been thoroughly studied for their beneficial antioxidant and venotonic effects.²

Other constituents of Damiana having effects on the hormonal system include pinocembrin and acacetin. A new study has discovered that these polyphenolic compounds have significant inhibitory effects on the enzyme known as aromatase, which changes certain steroidal sex hormones from one form to another. Aromatase is responsible for converting androstenedione into estrone, and testosterone into estradiol. When aromatase is inhibited, testosterone can remain present and active in the body for longer periods of time. Damiana’s anti-aromatase activity could help to explain its aphrodisiac effects.³

An animal study has clearly demonstrated that extracts of Damiana have vasodilating effects on erectile (corpus cavernosum) tissue. The researchers noted “highly significant and dose dependent results” which they interpreted to seemingly validate the traditional use of the plant.⁴ A previous animal study found that Damiana extracts stimulated sexual activity and performance and also suggested that their results seemed to support the folk reputation of the herb as an aphrodisiac.⁵ Yet another animal study found that an extract of Damiana had relaxing, anxiety-reducing effects.⁶

The spicy essential oil of Damiana features the compounds caryophyllene oxide, caryophyllene, delta-cadinene, elemene, and 1, 8-cineol. ⁷ Aromatic oils, in general, have been found the enhance the absorption and/or bioavailability of other compounds with which they occur. This oil helps to give Damiana its penetrating, warming characteristics.

Damiana also contains numerous other constituents which have yet to be thoroughly studied, including Z-echinacin, several polyphenols and their glycosides, tannins, terpenoids, polysaccharides, phytosterols, and saponins.⁸ Phytosterols and saponins are found in almost all of the plants traditionally considered to be male tonics, adaptogens, and vitality-enhancers.

Our formula uses a 4:1 concentrated extract of fresh Damiana leaves.

Safety: Damiana has a long history of use and an established safety record. Up until 1947, Damiana leaves and extracts were listed in the U.S. National Formulary and were also official in the British Pharmacopoeia. It is widely used in European phytotherapy. There are no cases of adverse reactions, drug interactions, or contraindications published in the literature.⁹ Use as directed.

References

1. Green, James. 2007. The Male Herbal. Berkeley, CA: Crossing Press. Pp. 246-7.
2. PMID: 17284070
3. PMID: 18948180
4. PMID: 14692728
5. PMID: 10227074
6. PMID: 16635964
7. PMID: 15567246
8. PMID: 16822212
9. Mills & Bone. The Essential Guide to Herbal Safety. St. Louis, MO: Elsevier Churchill Livingstone. Pp. 358-9.

Hawthorne (Crataegus monogyna, C. laevigata) has been used extensively throughout history as well as in contemporary European and American phytotherapy as a nourishing tonic for the circulatory system. The leaf and flower of the Hawthorne tree (Crataegi folium cum flore) are official in the European Pharmacopoeia and are routinely used in integrative practice. In traditional Chinese medicine (TCM), Hawthorne is considered to ‘calm the disturbed heart Shen.’ Shen is often translated to mean ‘spirit.’ In the West, this herb is traditionally thought of as a trophorestorative tonic for the heart and circulatory system.¹

Hawthorne contains an array of bioactive polyphenols including OPCs (oligomeric proanthocyanidins or pycnogenols), phenylpropanoids (e.g., caffeic and chlorogenic acids), and flavonoids (e.g., vitexin and its glycosides, hyperoside, luteolin, and rutin). These polyphenols all have antioxidant, anti-inflammatory, and venotonic properties. Also present are triterpene aglycones including ursolic acid and oleanolic acid.² Ursolic and oleanolic acids have also demonstrated anti-inflammatory, antioxidant, and vasorelaxant properties. ^3,4,5

Hawthorne has a rich content of OPCs, which have been shown to act synergistically with L-arginine to enhance endothelial production of nitric oxide, a potent vasodilator.⁶ The German Commission E monograph on Hawthorne (Crataegi folium cum flore) notes that it can decrease peripheral vascular resistance; in other words, this herb can make it easier for smaller blood vessels such as those in the corpus cavernosa of the penis to fill with blood.⁷

Numerous animal and clinical studies show that Crataegus has positive effects on the cardiovascular system, increasing the efficiency of the circulation without having an overly-stimulating effect and improving the integrity and elasticity of the blood vessels.^8,9 This results in enhanced delivery of oxygen to the tissues, enhanced blood flow, and improved stamina.^10,11

In our formula, the concentrated extract of Hawthorne acts as an antioxidant tonic for the circulatory system. Together with Rhodiola, Goji berry, and ActiVin^®, Hawthorne supplies OPCs that work with L-arginine to enhance the production of endothelial nitric oxide (NO) for a vasodilating effect.^12,13 Interestingly, certain aphrodisiac formulas from TCM also contain OPC-rich herbal ingredients. One such formula, which includes Hawthorne, has been found to increase blood flow to the penis and to enhance sexual behavior in animals.¹⁴

Safety: Hawthorne has an excellent safety record. The ESCOP monograph on Hawthorne lists no restrictions on duration of use, no known contraindications, no reported adverse interactions with drugs, a very low incidence of adverse effects, and no evidence of toxicity even in very large doses.¹⁵ Regular use of large amounts of Hawthorne may potentiate certain cardiac medications; consult with your health care practitioner to see if modification of drug dosage may be required.¹⁶

References

1. Mills & Bone. 2000. Hawthorn. In Principles and Practice of Phytotherapy. New York: Churchill Livingstone. Pp. 437-47.
2. Sticher, O. & B. Meier. Hawthorn (Crataegus): Biological Activity and New Strategies for Quality Control. Chapter 17 inn: Phytomedicines of Europe: Chemistry and Biological Activity. L. D. Lawson and R. Bauer, eds. 1998. ACS Symposium Series #691. Pp. 244-5.
3. PMID: 8847885
4. PMID: 15994040
5. PMID: 16630635
6. PMID: 16635964
7. PMID: 17703218
8. Crataegi folium cum flore (Hawthorn leaf and flower). Commission E Monographs. 1994. Austin, TX: American Botanical Council.
9. PMID: 11887407
10. PMID: 16397846
11. PMID: 15844828
12. PMID: 18254076
13. PMID: 18037769
14. PMID: 17927567
15. PMID: 16819173
16. Crataegi Folium cum Flore. ESCOP Monographs. 2nd Ed. 2003. New York: Thieme. P.99.
17. Mills & Bone. 2005. The Essential Guide to Herbal Safety. St. Louis, MO: Elsevier Churchill Livingstone. Pp. 465-7.

Passion Flower (Passiflora incarnata), also known as Passion Vine or May Pop, is related to the vine that bears the delicious tropical fruit, the Passion fruit (P. edulis). It is native to the warmer temperate and semi-tropical regions of North America. The Cherokee Indians knew Passion Flower by the name of Ocoee. This herb was introduced to Western medicine in the 1800s and became known as a relaxing nervine tonic, used to calm anxiety and restlessness and to restore healthy sleep. Although larger doses of the herb are traditionally understood to have mild sedative properties, smaller doses are considered to have more of a relaxing, restorative tonic effect on the nervous system. Herbs with this type of activity are referred to as ‘trophorestoratives.’ Passion Flower is widely used in Europe and is listed in the British Herbal Pharmacopoeia, the European Pharmacopoeia, the ESCOP monographs, and the German Commission E monographs. Recent animal studies (see below) have found that Passion Flower also has aphrodisiac effects. ¹

Passion Flower contains a complex mixture of flavonoid constituents including vitexin, isovitexin, isoorientin, chrysin, apigenin, luteolin, and their glycosides. A recently discovered phenolic compound in Passion Flower called BZF has demonstrated significant relaxing properties in both animals and humans and has been patented for use in a phytopharmaceutical preparation.^2,3

According to researchers, BZF has also exhibited “aphrodisiac, libido-enhancing, and virility-enhancing properties” in animals.⁴ Extracts of whole Passion Flower have also exhibited aphrodisiac activity.^5,6 Some of the flavonoid constituents, including chrysin and apigenin, have demonstrated activity as aromatase inhibitors, which are compounds that delay the conversion of testosterone to its metabolites.

Older literature had reported that Passion Flower contained harman-type alkaloids, although none of the more recent analyses have been able to detect appreciable concentrations of these constituents in nearly all samples investigated.⁷ Some literature alleging that this herb is contraindicated for co-administration with certain anti-anxiety or antidepressant medications is based the presumed presence of these alkaloids.

Several animal studies have confirmed that extracts of Passion Flower have anxiety- relieving and relaxing effects on the nervous system. ^8,9,10 A human clinical found that Passion Flower had a relaxing yet non-sedating effect on patients in a pre-operative setting.¹¹ The flavonoid constituents have recently been found to exert their activity through modulation of GABA-A receptors (GABA is a relaxing neurotransmitter). These constituents also act as antioxidants to protect cells and tissues from free-radical damage.¹²

Safety: Passion Flower has an excellent safety record; side effects are rare, with only the very occasional individualized allergic-type reaction being reported.¹³ The ESCOP monograph Passiflorae Herba lists no known contraindications, no reported herb/drug interactions, and no reports of overdose toxicity.¹⁴ A recent animal study examining the effects of high-dose, long-term administration of a formula containing Passion Flower, Hawthorne, and Valerian found no signs of toxicity.¹⁵

Our formula contains a small amount of concentrated (4:1) Passion Flower extract to act synergistically along with Wild Oats for an aphrodisiac and trophorestorative effect on the nervous system.

References

1. Cronin J. Passionflower: Reigniting male libido and other potential uses. Alternative & Complementary Therapies. 2003; April:89-92.
2. PMID: 15261959
3. PMID: 12165186
4. PMID: 14690874
5. PMID: 12722149
6. PMID: 12511112
7. Passiflorae Herba. ESCOP Monographs. 2nd Ed. 2003. New York: Thieme. P. 359.
8. PMID: 19216234
9. PMID: 17966676
10. PMID: 19006051
11. PMID: 18499602
12. PMID: 19051605
13. Mills & Bone. The Essential Guide to Herbal Safety. St. Louis, MO: Elsevier Churchill Livingstone. Pp. 526-8.
14. Passiflorae Herba. ESCOP Monographs. 2nd Ed. 2003. New York: Thieme. P. 360.
15. PMID: 19048610

Tribulus (Tribulus terrestris) is an herb used for thousands of years in both Ayurvedic practice (where it is known as Gokshura) and in traditional Chinese medicine (TCM), where it is called Bai Ji Li or Ci Ji Li. Other names for this potent little plant include Bull’s Head and Goat Head. Both Ayurveda and TCM consider it to be a warming systemic tonic that rejuvenates and builds vitality while enhancing male libido. Traditional practice reports that Gokshura has natural androgenic effects while increasing sexual self-confidence, desire, and performance. It has traditionally been used to prolong ejaculation time, enhance erection, and increase sexual satisfaction.¹ Because of its warming nature, Gokshura is also considered to stimulate the circulation and enhance blood flow to the penis. TCM uses it as a vasodilator in clinical practice.² In Ayurveda, Gokshura is classified as a ‘rasayana’ herb; these are reputed to improve the body’s defenses, enhance longevity, and promote both physical and mental health. Today we might think of it as having ‘adaptogenic’ activity, similar to that of Ginseng.

Gokshura contains a complex mixture of constituents known as steroidal saponins. Similar compounds are found in many herbs used as male tonics, adaptogens, and aphrodisiacs (e.g., Ginseng, Eleuthero, and Sarsaparilla). Two of the prominent steroidal saponins in Gokshura are called protodioscin and protogracillin.^3,4,5,6 It also contains phytosterols (e.g., beta-sitosterol, which is in many herbs used to benefit the prostate gland). The concentrated extract used in our formula is standardized to contain 40% total saponins.

A recent study from the National University of Singapore investigated the effects of Gokshura extract on hormonal profiles in different animals. Eight weeks of treatment significantly increased levels of testosterone (up 52%), dihydrotestosterone (up 31%), and DHEA (dehydroepiandrosterone – up 29%) in the primates. Increases were also noted in the other animals. The researchers hypothesized that the activity was due to the content of protodioscin in the extract.⁷

Researchers at the Sungkyunkwan University College of Pharmacy in South Korea investigated a traditional formula known as SA1, which included Gokshura, Red Ginseng, Hawthorne, Goji Berries, and five other herbs. The formula is traditionally used in Korean indigenous medicine as a male sexual vitality and energy tonic. They found that two weeks of oral treatment with SA1 increased successful sexual behavior in animals. It was also noted that the SA1 formula significantly increased blood pressure within the erectile tissues of the penis.⁸

In an investigation on the effects of chronic stress on animals, it was found that an Ayurvedic formula containing Gokshura and four other natural ingredients had significant adaptogenic activity and improved biochemical, physiological, and behavioral responses to stress.⁹

A 2006 animal study found that extracts of Gokshura had significant antihypertensive activity, which the researchers hypothesized was the result of smooth muscle relaxation in the arteries, possibly involving the release of endothelial nitric oxide.¹⁰ Safety: Toxicological studies have found Tribulus to be very safe in animals. Men have used doses of up to 1,500 mg per day without adverse effects, although typically much less is taken. Very large doses of Tribulus may irritate the digestive tract due to the high concentration of saponins. People with coeliac disease, cholestasis, fat malabsorption syndromes, or fat-soluble vitamin malabsorption syndromes should use caution with Tribulus.¹¹ [Mills & Bone, pp. 606-8]

References

1. Green, James. 2007. The Male Herbal. Berkeley, CA: Crossing Press. Pp. 125-6.
2. PMID: 2364467
3. PMID: 12946722
4. PMID: 9397208
5. PMID: 14604238
6. PMID: 19152803
7. PMID: 18068966
8. PMID: 16819173
9. PMID: 11218827
10. PMID: 16289603
11. Mills & Bone. The Essential Guide to Herbal Safety. St. Louis, MO: Elsevier Churchill Livingstone. Pp. 606-8.

Trikatu is a ancient Ayurvedic formula containing three spicy herbs (Piper nigrum [Maricha], Piper longum [Pippali], and Zingiber officinale [Sunthi]). Traditionally known as the "Three Pungents," Trikatu is added to many formulas in order to stimulate the digestion and circulation and to thereby enhance the bioavailability of other ingredients.¹ In Ayurveda, Trikatu is considered to be unsurpassed as a ‘rasayana’ or restorative tonic formula to ‘re-kindle the digestive fire’ and restore the body’s energy. It is also traditionally considered to be an aphrodisiac that warms and stimulates the sexual system.²

There is some scientific evidence to back up the traditional assertion that Trikatu can enhance absorption and potentiate a formula.^3,4 Animal studies have found that piperine, an alkaloid found in both Piper nigrum and P. longum, can stimulate digestion via the pancreatic enzymes,⁵ and can enhance absorption via effects on the intestinal mucosa⁶ and reduction of gastrointestinal transit time. Piperine also has a significant influence on hepatic metabolism via effects on several of the cytochrome p-450 enzymes responsible for metabolizing phytochemicals and drugs. The overall result of these activities is an increase in the bioavailability of certain compounds accompanied by a delay in their breakdown.⁷ This suggests that Trikatu may indeed be able to enhance the activities of other herbs with which it occurs in a formula.

Another constituent of Trikatu, Zingiber, contains numerous physiologically active phytochemicals including essential oils and the pungent resinous principles called gingerols and shogaols. Besides their warming, stimulating effects, animals studies on these compounds have revealed that they are also strongly antioxidant and anti- inflammatory,^8,9,10 have vasodilating effects, and can benefit the circulatory system.^11,12 Another animal study found that Trikatu had beneficial effects on the lipid composition of the blood and suggested that it might help prevent constriction of the blood vessels by discouraging the deposition of plaque.¹³

Our formula features Trikatu as a warming, stimulating carrier to enhance the activities of the other aphrodisiac and adaptogenic herbs, as well as for its beneficial effects on blood flow to the penis.

Our formula features Trikatu as a warming, stimulating carrier to enhance the activities of the other aphrodisiac and adaptogenic herbs, as well as for its beneficial effects on blood flow to the penis.

Safety: Trikatu has been safely used for generations in Ayurveda and TCM. A recent study found that even very high doses (2,000 mg of Trikatu per kilogram of body weight – the rough equivalent of 140,000 mg for a 150-lb. man) had no adverse effects on animals.¹⁴ Animal studies have found varying effects regarding the influence of Trikatu on the bioavailability of different drugs.^15,16,17,18 If you are taking sensitive pharmaceutical medications, consult your health care provider to see if you might need to adjust dosages or take your prescription drugs and supplements at different times of day.

References

1. van Wyk, Ben-Erik and Michael Wink. 2004. Medicinal Plants of the World. Portland, OR: Timber Press. Pp. 244, 349.
2. Puri, H.S. 2003. Rasayana: Ayurvedic Herbs for Longevity and Rejuvenation. New York: Taylor & Francis. P. 312.
3. PMID: 1434692
4. PMID: 7311598
5. PMID: 10702999
6. PMID: 12046863
7. PMID: 17987447
8. PMID: 17950516
9. PMID: 16117603
10. PMID: 18706468
11. PMID: 18037515
12. PMID: 15613983
13. PMID: 15742354
14. PMID: 19182439
15. PMID: 15120451
16. PMID: 18296885
17. PMID: 2401524
18. PMID: 16767797

Wild Oat seed (Avena fatua, A. sativa) has an outstanding historical reputation as a nutritive and trophorestorative tonic for the nervous system with additional supportive activity for sexual function. The old saying ‘to sow your wild oats’ may well be based on empirical observation of this activity. Avena has been, and continues to be, used extensively in Western phytotherapy as a warming, nourishing, and mildly stimulating tonic to repair the effects of stress, over-work, and exhaustion.¹ Oat seed was used extensively by the American Eclectic physicians as a nervine tonic, mild stimulant, antispasmodic, and remedy for fatigue.²

Oats also contain antioxidants including the avenanthramides and a range of polyphenolic compounds (e.g., p-coumaric, caffeic, and ferulic acids).^5,6 Studies have demonstrated that the avenanthramides have anti-inflammatory activity in both human skin⁷ and endothelial cells within the blood vessels.^8,9

There has been relatively little scientific study of Avena seed extracts compared to other botanicals, despite the fact that they are commonly used in phytotherapy and are considered to be one of the best trophorestorative substances in the herbal Materia Medica. Avena extracts have also been used successfully in Germany to reduce tobacco cravings and withdrawal symptoms from addictive drugs.¹⁰

Safety: Avena is very safe and there are no known adverse effects, drug interactions, or contraindications (with the exception of some people having coeliac disease/gluten intolerance who may be sensitive to Oats).¹¹

References

1. Green, James. 2007. The Male Herbal. Berkeley, CA: Crossing Press. Pp. 277-8.
2. Felter, Harvey Wickes and John Uri Lloyd. 1983 (reprint of 1898 original). Avena Sativa Monograph. King’s American Dispensatory. Vol. 1, 18th ed. Sandy, OR: Eclectic Medical Publications.
3. van Wyk, Ben-Erik and Michael Wink. 2004. Medicinal Plants of the World. Portland, OR: Timber Press.
4. PMID: 18301937
5. PMID: 12537428
6. PMID: 10739096
7. PMID: 18461339
8. PMID: 18062932
9. PMID: 17513394
10. Weiss, Rudolf Fritz. 1988. Herbal Medicine. 1st English ed. Gothenburg, Sweden: Beaconsfield Publishers.
11. PMID: 1526282

Korean Red Ginseng (Panax ginseng) has been used for thousands of years and is traditionally thought of as a ‘chi’ tonic for enhancing vitality, virility, sexual vigor, and stamina. It is highly regarded in traditional Chinese medicine (TCM) and is thought of as one of the most potent and effective overall tonics for male health and sexuality. Chinese tradition relates that Ginseng enhances the production of body fluids, rebuilds the vital energy, and promotes health and longevity.¹ Today we understand that Red Ginseng also acts as an adaptogen, helping to build vitality and sustained energy, supporting the adrenals, building the body’s defense mechanisms, and counteracting the effects of stress.² Ginseng also has beneficial effects on the circulatory system and is traditionally considered to ‘benefit the heart chi’ and ‘calm the shen (spirit).’ The steamed form of Ginseng is often preferred because the way it is slowly cooked is believed to help release the active ingredients. Ginseng is often formulated with synergistic herbs including Damiana, Wild Oats, and Goji Berry, along with spicy compounds such as Trikatu.

Several hundred scientific studies have been published on the pharmacology of Ginseng. This respected herb contains a complex, synergistic mixture of constituents including a group of more than 150 different triterpenoid saponins known collectively as the ginsenosides.³ The ginsenosides in particular have demonstrated antioxidant, anti-inflammatory, and immunostimulant properties in several animal studies.⁴ Both in vitro and animal studies also demonstrate that the ginsenosides have neuroprotective effects.^5,6 Immunomodulating polysaccharides,⁷ unique peptides, and some polyphenols are also present in this powerful herb.

A recent meta-analysis of studies on the erection-enhancing effects of Korean Red Ginseng found a number of significant positive results in male volunteers.⁸ A human clinical study performed at the Yonsei University College of Medicine found that the use of Korean Red Ginseng improved penile rigidity and girth, libido, and patient satisfaction.⁹ In addition, a recent review of animal studies found ‘good evidence’ that the ginsenosides could facilitate erection by relaxing the blood vessels in the corpus cavernosa, an effect that was thought to be mediated by nitric oxide released by the vascular endothelium and perivascular nerves.¹⁰

Several studies support the traditional assertion that Ginseng may have benefits for the circulatory system¹¹ and for enhancing the body’s resistance to the effects of stress.¹² In TCM, it has long been thought of as a warming and stimulating tonic for these purposes.

Safety: Ginseng has very low toxicity and an excellent safety record. Large doses given to animals had no adverse activity on physiological function or reproduction.¹³ The ESCOP monograph on Ginseng lists no known contraindications or serious adverse effects when taken at the recommended dosage level.¹⁴ Some people having a very hot constitution (a tendency towards elevated blood pressure, red face, impatient or short-tempered, impulsive or aggressive personality) may find larger doses of Ginseng to be over-stimulating, especially if combined with caffeine or other stimulants. It is traditionally recommended to suspend the use of Ginseng during an acute infection because the body is thought to be in an overheated condition during that time.

Euphallic^™ contains a concentrated extract of Red Ginseng, standardized to contain 10% ginsenosides. In our formula, the Ginseng acts as a synergist for the other aphrodisiac extracts (Gokshura, Damiana, and LJ100^®) as well as for the adaptogens (Rhodiola, Schisandra, and Goji Berry).

References

1. Mills & Bone. 2000. Ginseng. In Principles and Practice of Phytotherapy. New York: Churchill Livingstone. Pp. 418-32.
2. Green, James. 2007. The Male Herbal. Berkeley, CA: Crossing Press. Pp. 257-8.
3. PMID: 18772102
4. PMID: 18567057
5. PMID: 17265697
6. PMID: 15215637
7. PMID: 15180575
8. PMID: 18754850
9. PMID: 8750052
10. PMID: 12076988
11. PMID: 15278009
12. PMID: 15215639
13. Mills & Bone. 2005. Ginseng. In The Essential Guide to Herbal Safety. St. Louis, MO: Elsevier Churchill Livingstone. Pp. 433-6.
14. Ginseng Radix. ESCOP Monographs. 2nd Ed. 2003. New York: Thieme. P. 212.

Rhodiola (Rhodiola rosea), also known as Arctic Root, Golden Root, or Roseroot, is an unusual plant which grows in the Arctic and high-elevation regions of the Northern Hemisphere. Long in use by tribal peoples of Siberia, Scandinavia, and Tibet, its properties as a stimulating adaptogen were ‘discovered’ in the Soviet era and used by athletes, cosmonauts, and the military to enhance strength and endurance, improve both immediate and sustained energy, and increase mental alertness. Rhodiola has been official in the Russian Pharmacopoeia since 1969.¹

Rhodiola is also popular in China, and in fact has been highly regarded as a ‘longevity’ and ‘chi’ tonic for many generations.² This herb is generally considered to be more stimulating compared to most other adaptogens and to have a special affinity for the sexual system. It is thought to have the unusual ability to enhance immediate energy via the ‘sympatho-adrenal system’ or SAS, and to promote sustained energy as well by activity on the ‘hypothalamus-pituitary-adrenal axis’ or HPA.

Rhodiola contains unique phytochemicals which have not been found in any other species. The first of these is a family of monoterpene glycosides called rhodiolosides A- E.³ The other unique compounds in Rhodiola, called the rosavins (rosin, rosarin, and rosavin), are phenylpropanoid glycosides. Another phenolic compound, salidroside (rhodioloside), is also present. Most contemporary concentrated extracts of Rhodiola are standardized to contain 3% rosavins and 1% salidrosides. Flavonoids (rodiolin, rodionin, kaempferol, quercetin, and rutin), essential oil constituents (rosiridol, rosaridin), phytosterols (beta-sitosterol and daucosterol), and steroidal glycosides (creosides I, II, III, IV, & V) are also found in this herb.^4,5

There are several hundred studies published on the pharmacology and physiological activities of Rhodiola, although many of these have not yet been translated into English. However, in the last decade or so, interest in this plant has exploded and more research is being carried out daily. A recent Russian study using a single dose of Rhodiola found that it increased alertness and had a ‘pronounced anti-fatigue effect’ in a trial of 161 volunteers,⁶ and a Swedish review explains that Rhodiola ‘typically generates no side effects, unlike traditional stimulants that possess addiction, tolerance and abuse potential.’⁷ Similarly, a clinical study from a Belgian university found that Rhodiola enhanced endurance and exercise capacity.⁸ These results are typical of the older human and animal studies.

Besides its potency as an energy tonic, Rhodiola is also considered to have benefits for the circulatory system^9,10,11 and to improve libido.^12,13,14 In our formula, it supports the activities of the other herbs (Trikatu, Cayenne, and Hawthorne) that stimulate blood flow to the penis; enhances the libido-stimulating action of the Gokshura, Damiana, Ginseng, and Wild Oats; provides antioxidant protection, enhances well-being, and improves sexual stamina.

Safety: Rhodiola has an excellent safety profile. Extensive Russian toxicological studies (both animal and human) have found no signs of toxicity at high therapeutic dosages.¹⁵ Because of its stimulating nature, very high doses (1,500 mg and above) may cause insomnia and/or irritability in some individuals.

References

1. State Pharmacopoeia of the USSR. Vol. 2. Moscow: Medicina; 1990. Pp. 364-6.
2. Winston, David and Steven Maimes. 2007. Rhodiola. In: Adaptogens: Herbs for Strength, Stamina, and Stress Relief. Rochester, VT: Healing Arts Press. Pp. 191-4.
3. PMID: 16880679
4. van Wyk, Ben-Erik and Michael Wink. 2004. Rhodiola rosea. In Medicinal Plants of the World. Portland, OR: Timber Press. P. 271.
5. PMID: 17637521
6. PMID: 12725561
7. PMID: 16261511
8. PMID: 15256690
9. PMID: 12410627
10. PMID: 18074810
11. PMID: 15252224
12. PMID: 17901042
13. Ramazanov, Zakir. Phytochemistry, pharmacology, and standardization of Rhodiola rosea root extract. 2005. National Bioscience Corporation, Chester, NY.
14. Brown R, P Gerbarg, and Z Ramazanov. Rhodiola rosea: a phytomedicinal overview. Herbal Gram. American Botanical Council. 2002; 56:40-52.
15. Kurkin V and G Zapesochnaya. Chemical composition and pharmacological characteristics of Rhodiola rosea [review]. Journal of Medicinal Plants, Russian Academy of Science, Moscow 1985; 1231-445.

Schisandra (Schisandra chinensis), also known as Gomishi or Wu Wei Zi (Five-flavor Berry), is one of the most valued herbs in the traditional healing systems of China, Korea, and Japan. In traditional Chinese medicine (TCM), it is considered to have a warming and balanced energy which contains all five of the fundamental flavor principles: sweet, sour, pungent, salty, and bitter. TCM regards Schisandra as a mildly stimulating tonic that ‘calms the Shen’ and ‘fortifies the chi’ and can benefit the adrenals (for enhanced energy and stamina), support the liver (aiding detoxification), nourish the lungs (for enhanced oxygenation), relax the nervous system, and support the libido.¹ Contemporary phytotherapy considers it to be antioxidant, anti- inflammatory, adaptogenic, nervine tonic, neuroprotective, and hepatoprotective.² Schisandra is listed in the official Pharmacopoeias of China, Japan, South Korea, and Russia and has been researched extensively in those countries.

Schisandra contains a complex mixture of constituents belonging to the class called lignans. In particular, the schisandrins and the gomisins (schizandrol A & B, schisandrin A & B, schisantherin A & B, and gominsin N) have demonstrated considerable biological activity. Multiple studies on these lignans have found adaptogenic, antioxidant, and hepatoprotective effects.³ This herb also contains OPCs (similar to those in ActiVin^® and Hawthorne) that work synergistically with L-arginine to enhance the release of vasodilating nitric oxide in the blood vessels. In addition, an essential oil, essential fatty acids, phytosterols, antioxidant carotenoids, and tocopherols (including vitamin E) are all found in Schisandra berries.⁴

A recent study investigating the vasodilating effects of Schisandra extract found significant relaxation of isolated vascular tissue. The researchers noted that the results suggest this effect was ‘mediated by not only the endothelium-dependent NO [nitric oxide] pathway but also by a direct effect on vascular smooth muscle cells.’⁵ A Korean investigation found a similar effect⁶ and another study using one of the lignans from Schisandra (gomisin A) also produced similar results.⁷ Many of the herbs traditionally thought of as aphrodisiacs and circulatory system tonics are being found to have effects based on the endothelial nitric oxide system.

Numerous animal studies have noted the activities of Schisandra to include adaptogenic and antioxidant effects on the nervous, endocrine, immune, respiratory, cardiovascular, and gastrointestinal systems. In human clinical studies, Schisandra has been found to enhance endurance and accuracy of movement, mental performance and working capacity, and resistance to the effects of stress.^8,9 This versatile adaptogen has also been found to act via the sympatho-adrenal system (the SAS) to bring about immediate increases in energy and feelings of well-being.¹⁰

Our formula uses a concentrated extract of Schisandra, standardized to contain 5% schisandrins. Although mainly included as a warming adaptogenic energy tonic with relaxing support for the nervous system, this versatile herb also works synergistically with the other aphrodisiacs via the nitric-oxide mediated vasodilation that enhances blood flow to the penis.

Safety: Schisandra has been studied extensively by toxicologists in Asia. It has very low toxicity and in fact can act to protect the liver and other organs against toxic substances. Extremely large doses (2,000 mg/kg) given orally in animal studies had no serious toxic effects.¹¹ Larger therapeutic doses of concentrated Schisandra lignans can increase the oral bioavailability of tacrolimus, an immunosuppressive drug given to transplant patients.¹² Consult with your health care provider if you are taking tacrolimus or other drugs metabolized by P-glycoprotein transporters.

References

1. Green, James. 2007. The Male Herbal. Berkeley, CA: Crossing Press. Pp. 288-9.
2. Winston, David and Steven Maimes. 2007. Schisandra. In: Adaptogens: Herbs for Strength, Stamina, and Stress Relief. Rochester, VT: Healing Arts Press. Pp. 195-8.
3. PMID: 11475889
4. Upton, Roy. Editor. Schisandra berry (Schisandra chinensis): Analytical, quality control and therapeutic monograph. American Herbal Pharmacopoeia and Therapeutic Compendium. Santa Cruz, CA; 1999:1-25.
5. PMID: 18983904
6. PMID: 16704926
7. PMID: 18067062
8. PMID: 18515024
9. PMID: 19188053
10. PMID: 16261511
11. Mills & Bone. 2005. The Essential Guide to Herbal Safety. St. Louis, MO: Elsevier Churchill Livingstone. Pp. 563-5.
12. PMID: 17506780

Goji Berry (Lycium barbarum, L. chinense) or Gou Qi Zi, also known as the Wolfberry, has been used in traditional Chinese medicine (TCM) as both a food and a tonic for thousands of years. TCM considers Goji to be a potent nutritive tonic that enhances vitality, sexual function, male fertility, stamina, and happiness. The berries are a rich source of antioxidant compounds, believed in TCM to support the function of the circulatory system, provide sustained energy, and nourish the liver, kidneys, adrenals, and blood. They are also taken to ‘improve the eyesight.’¹ In TCM, Goji is considered to be a ‘longevity tonic’ and contemporary research from the University of Hong Kong is helping to provide a physiological explanation for the anti-aging mechanisms of the berry extracts.²

Goji berries contain a high concentration of amino acids (including betaine) and numerous flavonoids and carotenoids (e.g., zeaxanthin, beta-cryptoxanthin, and beta- carotene), along with triterpenoid and steroidal saponins, phytosterols, and polysaccharides.^3,4

An animal study from Wuhan University in China found that the polysaccharides from Goji had a protective effect on testicular tissue and improved antioxidant activity in the testes along with increasing the quality and quantity of sperm. In addition, the polysaccharides were noted to improve sexual performance and reproductive function in the animals, enhancing penile erection, increasing the levels of sex hormones, and enlarging the sexual organs.⁵ Another animal study from the Catholic University of Korea found that Goji Berry in a formula with Schisandra and three other herbs increased pressure in the corpus cavernosa of the penis and enhanced nitric-oxide activity in the penile tissues.⁶ Yet another study from Sungkyunkwan University in Korea found that a formula including Goji Berries, Gokshura, Hawthorne, and Red Ginseng stimulated sexual activity and erectile function in animals.⁷

Several studies have found evidence to support the traditional conception of Goji berries as a ‘longevity tonic’ by demonstrating their neuroprotective effects in models of age-related neurodegenerative disease.^8,9,10 A recent clinical trial found that the antioxidant properties of Goji are bioavailable and can protect the body from free radical damage and lipid peroxidation (both of which are important for the health of the circulatory system).¹¹ Another clinical study found that after two weeks of taking a standardized form of Goji juice (as compared to placebo), volunteers reported ‘increased ratings for energy level, athletic performance, quality of sleep, ease of awakening, ability to focus on activities, mental acuity, calmness, and feelings of health, contentment, and happiness’ with reduced perception of fatigue and stress and increased sexual activity.¹²

Our formula uses a concentrated extract of Goji Berry, standardized to 40% polysaccharides. Goji acts synergistically with the other aphrodisiac and adaptogenic herbs to support and stimulate sexual vitality, while helping to relax the penile vasculature and enhance erection via nitric oxide activity.

Safety: Goji berries are widely available in the form of foods and beverages and are considered to be very safe. This herb is a member of the nightshade family, so people with intolerance to nightshade-family vegetables may want to avoid larger doses. There is one case report from 1980 concerning an interaction of Lycium with coumadin (Warfarin^®) where the Lycium was suspected of potentiating the effect of the drug.

References

1. Winston, David and Steven Maimes. 2007. Lycium. In: Adaptogens: Herbs for Strength, Stamina, and Stress Relief. Rochester, VT: Healing Arts Press. Pp. 178-81.
2. PMID: 17710531
3. van Wyk, Ben-Erik and Michael Wink. 2004. Medicinal Plants of the World. Portland, OR: Timber Press. P. 195.
4. PMID: 18486400
5. PMID: 16563441
6. PMID: 18762238
7. PMID: 16819173
8. PMID: 17611646
9. PMID: 16139464
10. PMID: 17568570
11. PMID: 19185773
12. PMID: 18447631
13. Capani F et al. IRCS J Med Sci 1980; 8:661.

L-Arginine is a naturally-occurring amino acid that serves as the precursor for the synthesis of nitric oxide [NO] in the human body. Nitric oxide, generated in the nerve tissue and the vascular endothelium, is a powerful endogenous vasodilator. Pharmaceuticals (e.g., sildenafil) used to enhance erection employ the NO mechanism to relax the smooth muscles in the arteries. This allows vasodilation and enhances blood flow into the corpus cavernosa of the penis.^1,2

A recent clinical study from the Medical University Sofia in Bulgaria found a powerful synergistic action between L-arginine and the phytochemicals known as OPCs. A preparation consisting of these two ingredients was taken by 50 volunteers for one month. The researchers noted a significant up-regulation in the production of nitric oxide (NO) inside the penile vasculature and an increase in testosterone levels.³ Participants in the study reported that, on average, their frequency of intercourse doubled and their erectile function was enhanced.

In our formula, a highly-absorbable form of L-arginine works synergistically with the OPCs in ActiVin^®, Hawthorne, Goji Berry, Rhodiola, and Schisandra. Interestingly, certain aphrodisiac formulas from traditional Chinese medicine (TCM) also contain OPC-rich herbal ingredients. One of these has been found to increase blood flow to the penis and sexual behavior in animals.⁴

Safety: L-Arginine has been used extensively as a nutrient, as well as for a range of therapeutic applications in doses as high as 1,000 to 6,000 mg/day. Even these large amounts are generally well tolerated by healthy adults. Adverse effects are rare at lower dosage levels. Large doses (1,000 mg or more) of L-arginine are theorized to possibly have an additive interaction with ACE Inhibitors, potassium-sparing diuretics, and phosphdiesterse-5 inhibitors (e.g., sildenafil). Consult with your health care provider if you are using these medications.⁵

References

1. PMID: 17637789
2. PMID: 15866322
3. PMID: 17703218
4. PMID: 16819173
5. Stargrove, Treasure, & McKee. 2008. Arginine. In Herb, Nutrient, and Drug Interactions. St Louis, MO: Mosby Elsevier. Pp. 653-60.

Niacin (also known as nicotinic acid or vitamin B3) is a naturally-occurring vitamin found in dietary sources such as meats, dairy, eggs, and wheat germ. Niacin is necessary for the function of NAD and NADP (co-enzymes which are fundamental to mitochondrial energy metabolism), DNA repair, and the production of steroid hormones in the adrenals. Small-to-moderate amounts of niacin can enhance vasodilation.¹ Larger doses have been prescribed by physicians for the management of cardiovascular health. ²

In our formula, a moderate amount of niacin is included to act synergistically with the other circulatory system stimulants and tonics (Capsicum, Trikatu, and Hawthorne). Together, these ingredients encourage relaxation of the blood vessels and enhance blood flow to the penis. Niacin also offers nutritional support.

Safety: Niacin is safe and well tolerated at lower doses. Amounts of 100 mg or more can result in mild itching, prickling, or flushing of the skin. Some sensitive individuals will experience skin flushing (peripheral vasodilation) with even smaller doses of niacin. Sustained use of large amounts of niacin (750 mg/day or more) may be toxic to the liver. Pharmacologic doses of niacin (1,000 mg and up) should be supervised by a physician.³

Zinc is an essential trace element and is often included in male enhancement formulas. Many of the body’s enzymes depend on zinc as a co-factor in biochemical transformations. Zinc is important for the regulation of hormonal activity and the proper functioning of many proteins and cell membranes, as well as for regulation of the immune system. It also contributes to antioxidant protection in the body. In men, zinc is necessary for the proper formation of sperm. In addition, this trace element inhibits the activity of 5-alpha-reductase, which converts testosterone into its metabolite, dihydrotestosterone.⁴ Several animal and clinical studies indicate that supplemental zinc can protect testosterone levels in the body and contribute to performance enhancement and sperm quality.^5,6,7,8

A moderate amount of zinc is included in our formula to act synergistically with Gokshura and Damiana for the general health of the reproductive system and to optimize testosterone metabolism.

Safety: Lower doses of zinc (up to 40 mg/day) are considered to be safe for adults. Mild gastrointestinal distress has been noted with doses of 50 to 150 mg/day and doses of 225 mg or more can cause vomiting. Long-term use of 50 mg/day or more of zinc can cause copper deficiency.⁹

Copper is also an essential trace element and is a companion mineral for zinc. It is necessary for the proper functioning of many enzymes in the body having to do with energy production in the mitochondria, neurotransmitter synthesis and metabolism, and protection from free radical damage. Copper is also necessary for the utilization of iron and the proper formation of red blood cells. Zinc can decrease the body’s ability to absorb copper, so copper is often included in formulas to counter-balance the activity of zinc.¹⁰

Safety: Small doses of copper are considered to be safe. The tolerable upper intake level for copper is 10 mg/day, while the RDA is slightly less than 1 mg/day for adult men. Copper toxicity is rare. Long-term exposure to doses larger than 10 mg/day can cause liver damage.¹¹

1. Higdon, Jane. 2003. Niacin. In: An Evidence-Based Approach to Vitamins and Minerals. New York: Thieme. Pp. 15-22.
2. PMID: 17620858
3. Stargrove, Treasure, & McKee. 2008. Niacin. In Herb, Nutrient, and Drug Interactions. St Louis, MO: Mosby Elsevier. Pp. 281-305. Stargrove, Treasure, & McKee. 2008. Zinc. In Herb, Nutrient, and Drug Interactions. St Louis, MO: Mosby Elsevier. Pp. 618-52.
4. PMID: 17984944
5. PMID: 16648789
6. PMID: 17169313
7. PMID: 16648790
8. Higdon, Jane. 2003. Zinc. In: An Evidence-Based Approach to Vitamins and Minerals. New York: Thieme. Pp. 197-205.
9. Murray, Michael. 1996. Copper. In: Encyclopedia of Nutritional Supplements. New York: Prima Publishing. Pp. 199-203.
10. Higdon, Jane. 2003. Copper. In: An Evidence-Based Approach to Vitamins and Minerals. New York: Thieme. Pp. 116-22.