Organic Ursolic Acid 100G 35%...
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You may mix it into an organic apple sauce. Mix it very well and then allow to sit for a few minutes, and then repeat one more time. This will help it to become absorbed into the apple sauce (or a similar item), because it is a very fine powder. If this does not work for you- then you can put the powder into 4 to 6 ounces of your favorite juice and use a mixer or blender to get it into solution.
It is also suggested to take this item between meals (at least 1 - 2 hours separate from the main meals of the day) whenever it is possible.
(This protocol has been provided to us by the courtesy of American Metabolic Laboratories and is ONLY to be used under the strict guidance and supervision of your physician or your health care professional.)
PHI (Phosphohexose isomerase/glucose phosphate Isomerase or GPI) is the Human Autocrine Motility Facto (AMF), the regulator of anaerobic sugar metabolism by the Warburg type of glycolysis. It is the facilitator of the metastatic spreading of cancer and most likely any circulating tumor cells (CTC). According to current knowledge, cancer cells will migrate from a tumor to a different site (or organ) by either the presence of PHI, or via the mechanical dislodging of cells from an existing tumor.
PHI (GPI) is anaerobic. Many efforts have been made to inhibit the enzyme by various oxygen-enriching modalities; such as Hyperbaric Oxygen Therapy, Ozone Therapy, H2O2, Vitamin C, Yoga and Aerobic Exercise.
A relatively recent discovery, published in biomedical literature encouragingly demonstrated the use of Ursolic Acid for the inhibition of AMF in a Cancer, Supression of AMF/PGI-mediated tumorogenic activity by Ursolic Acid by Shin WL, et al. Mol Carcinog. 2013 Oct;52(10):800-12.
Ursolic Acid is a botanical product and has already been used with success in humans for weight reduction and lean muscle creation and preservation.
The highest potency available of 35% extract is now available here from BioNewGenics.
*An initial PHI evaluation performed along with the Cancer Profile (available only from American Metabolic Laboratories) is suggested, and a repeat of the PHI test is highly advisable around the 5th week of supplementation with this potent, botanical food supplement.
According to research, the general suggested dose for Athletics and Weight Control is:
10 mg/kg, i.e. 10 mg/2.2 lb.of body weight.
*SPECS FOR MEASURING: 1 GRAM = APPROXIMATELY 3/4 TEASPOON
This is a nutritional, non-medicinal formula, not yet evaluated by the FDA. You MUST consult with a physician for proper guidance during your therapy!
The protocol above provided courtesy of ©American Metabolic Laboratories, 1/2016.
Ursolic acid (also known as Ursol, Prunol, Malol or Apple Peel Extract) is a substance found in many plants and fruits. It comes from a family of chemicals known as the Pentacyclic Triterpenes, which have recently become the subject of very important scientific research.
INHIBITON OF TUMOR PROMOTON IN SKIN
Ursolic acid (UA) and oleanolic acid (OA), isolated from Glechoma hederacea, inhibited Epstein-Barr virus activation induced by 12-O-tetradecanoylphorbol 13-acetate (TPA) in mouse skin. The inhibitory effects were evaluated for 20 weeks. Continuous application of UA and OA (41 nmol of each) before TPA-treatment (4.1 nmol) delayed the formation of papillomas in mouse skin and reduced the rate (%) of papilloma bearing mice. Both UA and OA exhibited remarkable inhibitory activity against tumor promotion, which is comparable to the known tumor inhibitor, retinoic acid (RA). Compared to either RA or OA, ursolic acid inhibited tumor more effectively after a single application before initial TPA-treatment as shown in Figure 1. This suggests that the role of tumor inhibition by UA differs from that of either RA or OA. It is suggested that pretreatment of skin with UA may inhibit the first dramatic cellular event in tumor promotion caused by TPA17.
Topical application of ursolic acid derived from rosemary extract inhibited TPA-induced tumor initiation and promotion, inflammation, and ornithine decarboxylase activity in mouse skin. Ursolic acid exhibited strong anti-inflammatory activity. It is even more active than of 1 or 2 mmol of ursolic acid along with 5 nmol of TPA for TPA for 20 weeks inhibited the formation of skin tumors per mouse by 45 or 61% respectively.
Lower doses (0.1 or 0.3 mmol) of ursolic acid had a similar inhibitory effect as the higher doses. Twice weekly topical application of 0.1, 0.3, 1, or 2 mmol of ursolic acid along with 5 nmol TPA for 8,12, and 18 weeks reduced the number of skin tumors per mouse by 52-86%, 49-63%, and 44-61%, respectively18.
Ursolic acid and its isomer, oleanolic acid have been recommended for skin cancer therapy in Japan19. Topical cosmetic preparations containing ursolic acid/ oleanolic acid have been patented in Japan for the prevention of topical skin cancer20. An ursolic acid/ oleanolic acid ointment inhibited 7,12-dimethylbenz [a] anthracene (DMBA)-induced skin cancer in mice. Reportedly, 0% and 3% of mice developed cancer in 15 weeks and 30 weeks, respectively compared to 50% and 90% for the control mice20.
THE CHEMISTRY OF URSOLIC ACID
Ursolic acid [(3b)-3-Hydroxyurs-12-en-28-oic acid] rarely occurs without its isomer oleanolic acid [(3b)-3-Hydroxyolean-12-en-28-oic acid] They may occur in their free acid form, as shown in Figure 1, or as aglycones for triterpenoid saponins which are comprised of a triterpenoid aglycone linked to one or more sugar moieties. Ursolic and oleanolic acids are similar in pharmacological activity1.
Several ursolic acid derivatives, both natural and synthetic, have been reported. Novel ursolic acid derivatives, including ursane-type triterpenoid saponins, naturally occur as secondary metabolites through complex metabolic processes in different parts of the plants5,8-12. Synthetic derivatives obtained from ursolic acid have been reported and evaluated for their pharmacological action 3,13-16
HAIR GROWTH STIMULANT
Ursolic acid and its isomer, oleanolic acid, have been used in to nics to enhance hair growth and prevent scalp irritation26,27. Both triterpenoid compounds encourage hair growth by stimulating the peripheral blood flow in the scalp and activating the hair mother cells. They also furnish alopecia-preventing and dandruff-preventing effects27.
Ursolic acid (triterpenoid sapogenin from the ursan group) inhibited the growth of several strains of staphylococci28. Numerous ursolic acid containing plants from the Lamiaceae family exhibited antibacterial/ fungal activity29. The minimal inhibitory concentration of Rosmarinus officinalis, Origanum majorana, and Lavandula officinalis were 500, 250, and 500 mg/cm3, respectively29. Ursolic acid also inhibited the growth of Microsporium lenosum and Candida albicans at 250 mg/mL30.
Ursolic acid is a potent anti-inflammatory agent. Thus, it has been recommended for use in burn ointments4. It not only inhibits human leucocyte elastase(HLE), but also 5-lipoxygenase and cyclooxygenase activity21, 22. Ursolic acid (1.0 mg/ear) inhibited TPA-induced mouse ear edema by 72.4%23. Hirota and coworkers24 determined that 200 mg and 50 mg applications of ursolic acid inhibited 12-O-hexadecanoyl-16-hydroxyphorbol-13-acetate (HPPA) - induced inflammation by 49% and 33%, respectively. In addition, it inhibited concanavalin A (Con A) induced histamine release, which can cause severe inflammation, by 95% at a concentration of 0.001 M25.
Ursolic acid treatment improves the health of skin and hair. Ursolic acid and its derivatives form oil-resistant barriers on the skin and hair as they do in the waxy coating of fruits6. Ursolic acid has been used to treat photoaged skin because it prevents and improves the appearance of wrinkles and age spots by restoring the skin's collagen bundle structures and its elasticity31. Concentrations of ursolic acid ranging from 0.01 to 50 mg have been reported for inclusion in skin treatment preparations 32-33.
Like most triterpenoids, ursolic acid is ubiquitous in the plant kingdom5. Ursolic acid and its derivatives are constituents of numerous plants which are having diversified phylogenetic origin and taxonomic position. It has been isolated from the protective wax-like coatings of apples, pears, cranberries, prunes, and other fruits6. Seaweed’s are rich in ursolic acid derivatives6. Some of the more commonly known medicinal plants containing ursolic acid are shown in Table 16,7.
Table 1. Partial List of Medicinal Plants Containing Ursolic Acid
|Common Name||Botanical Name||Family|
|Holy Basil (Tulsi)||Ocimum sanctum L.||Lamiaceae|
|Bilberry||Vaccinum myrtillus L.||Vacciniaceae|
|Devil's Claw||Harpagophytum procumbens DC||Pedaliaceae|
|Elder Flowers (European Variety)||Sambucus nigra L.||Caprifoliaceae|
|Peppermint leaves||Mentha piperita L.||Lamiaceae|
|Periwinkle||Vinca minor L.||Apocynaceae|
|Lavender||Lavandula augustifolia Mill.||Lamiaceae|
|Oregano||Origanum vulgare L.||Lamiaceae|
|Thyme||Thymus vulgaris L.||Lamiaceae|
|Hawthorn||Crataegus laevigata (Poir) DC||Rosaceae|
|Cherry laurel leaves||Prunus laurocerasus L.||Rosaceae|
Liu, J. (1995) Pharmacology of oleanolic and ursolic acid. J. Ethnopharmacology 49, 57-68.
The Merck Index (1996) 12th edition, Merck Research Laboratories, Whitehouse Station, NJ. 1686-1687.
Mezzetti, T., Orzalesi, G., and Bellavita, V. (1971) Chemistry of ursolic acid. Planta Medica 20(3), 244-252.
Harry, R.G. (1963) Cosmetic Materials. Their Origin, Characteristics, Uses, and Dermatological Action. Chemical Publishing Co., Inc., New York, NY.
Price, K.R., Johnson, I.T., and Fenwick, G.R. (1987) The chemistry and biological significance of saponins in foods and feedingstuffs. CRC Critical Reviews in Food Science and Nutrition 20(1), 27-135.
D'Amelio, F.S. (1999) Botanicals - A Phytocosmetic Desk Reference. CRC Press, Boca Raton, FI.
Leung, A.Y. and Foster, s. (1996) 2nd edition encyclopedia of common Natural Ingredients Used in Food, Drugs, and Cosmetics. John Wiley and Sons Inc. New York, NY.
Kraemer, K.H., Taketa, A.T., Schenkel, E.P., Gosmann, G., and Guillaume, D. (1996) Matesaponin 5, a highly polar saponin from Ilex paraguariensis. Phytochemistry 42(4), 1119-1122.
Miyase, T., Melek, F.R., El-Gindi, O.D., Abdel-Khalik, S.M., El-Gindi, M.R., Haggag, M.Y., and Hilal, S.H. (1996) Saponins from Fagonia arabica. Phytochemistry 41(4). 1175-1179.
Miyase, T., Shiokawa, K.I., Zhang, D.M., Ueno, A. (1996) Arliasaponins I-XI, triterpene saponins from the roots of Aralia decaisneana. Phytochemistry 41 (5), 1411-1418.
Nakanishi, T., Tanaka, K., Murata, H., Somekawa, M., and Inada, A. (1993) Phytochemical studies of seeds of medicinal plants III. Ursolic acid and oleanolic acid glycosides from seeds of Patrinia scabiosaefolia Fischer. Chem. Pharm. Bull. (Tokyo) 41 (1), 183-186.
De Tommasi, N., De Simone, F., and Pizza, C. (1992) constituents of Eriobotrya japonica. A study of their antiviral properties. J. Nat. Prod. 55 (8), 1067-1073.
Finlay, H., Honda, T., Gribble, G.W., Benoit, N.E., Suh, N., and Sporn, M.B. (1997) Novel A-Ring cleaved analogs of oleanolic and ursolic acids which affect growth regulation in NRP. 152 prostate cells. Bioorganic and Medicinal Chemistry Letters 7, 1769.
Finlay, H., Honda, T., Gribble, G.W., Suh. N., and Sporn, M.B. (1997) New enone derivatives of oleanolic and ursolic acid as inhibitors of nitric oxide production in mouse macrophages. Bioorganic and Medicinal Chemistry Letters 7, 163.
Lee, K., Lin, Y., Wu, T., Zhang, D., Yamagishi, T., Hayashi, T., Hall, I.H., Chang. J., Wu, R.; Yang, T. (1988) The cytotoxic principles of Prunella vulgaris, Psychotria serpens, and Hyptis capitata: ursolic acid and related derivatives. Planta Medica 54, 308-311.
Takechi, M., Uno, C., and Tanaka, Y. (1996) Structure-activity relationships of synthetic saponins. Phytochemistry 41 (1), 121-123.
Tokuda, H., Ohigashi, H., Koshimizu, K., and Ito, Y. (1986) Inhibitory effects of ursolic and oleanolic acid on skin tumor promotion by 12-O-tetradecanoylphorbol-13-acetate. Cancer Letters 33, 279-285.
Huang, M., Ho, C., Wang, z., Ferraro, T., Lou, Y., Stauber, K., Ma, W., Georgiadis, C., Laskin, J., and Conney, A. (1994) Inhibition of skin tumorigenesis by rosemary and its constituents carnosol and ursolic acid. Cancer Res. 54, 701-708.
Muto, Y., Ninomiya, M., and Fujiki, H. (1990) Present status research on cancer chemoprevention in Japan. Japanese J. of Clinical Oncology 20, 219-224.
Ishida, M., Okubo, T., Koshimizu, K., Daito, H., Tokuda, H., Kin, T., Yamamoto, T., and Yamazaki, N. (1990) Topical preparations containing ursolic acid and/ or oleanolic acid for prevention of skin cancer. Chemical Abstract 113, 12173y.
Safayhi, H., Rall, B., Sailer, E., and Ammon, H. (1997) Inhibition of boswellic acids of human leucocyte elastase. J. of Pharmacology and Experimental Therapeutics 281 (10), 460-463.
Najid, A., Simon, A., Cook, J., Chable-Rabinovitch, H., Delage, C., Chulia, A., and Riguad, M. (1992) Characterization of ursolic acid as a lipoxygenase and cyclooxygenase inhibitor using macrophages, platelets and differentiated HL60 leukemic cells. FEBS 299(3), 213-217.
Reico, M.C, Giner, R., Terencio, M., Sanz, M., and Rios, J. (1991) Anti-inflammatory activity of Helichrysum stoechas. Planta Medica 57(2), A56-A57.
Hirota, M., Mori, T., Yoshida, M., Iriye, R. (1990) Suppression of tumor promoter-induced inflammation of mouse ear by ursolic acid and 4,4-dimethylcholestane derivatives. Agric. Biol. Chem. 54(4), 1073-1075.
Tsuruga, T., Chun, Y., Ebizuka, Y., and Sankawa, U. (1991) Biologically active constituents of Melaleuca leucadendron: inhibitors of induced histamine release from rat mast cells. Chem Pharm. Bull 39 (12), 3276-3278.
Okazaki, T., Suetsugu, M.; and Yoshida, T. (1987) Hair tonics containing oleanolic derivatives. Chemical Abstracts 107, P161369V.
Kikuko, T., Shigemi, S., Masahiro, S., and Tatsu, M. (1993) Hair-raising cosmetic. Japanese Patent, no. 05286835.
Kowalewski, Z., Kortus, M., Ediza, W.; and Koniar, H. (1976) Antibiotic action of beta-ursolic acid. Arch. Immunol. Ther. Exp. (Warsz) 24 (1), 115-119.
Sattar, a., Bankova, V., Kujumgiev, a., Galabov, A., Ignatova, A., Todorova, C., and Popov, S. (1995) Chemical composition and biological activity of leaf exudates from some Lamiaceae plants. Pharmazie 50, 62-65.
Zaletova, N., Shchavlinskii, A., Tolkachev, O., Vichkanova, S., Fateeva, T., Krutikova, N.; Yartseva, I., and Klyuev, N. (1987) Preparation of some derivatives of ursolic acid and their antimicrobial activity. Chemical Abstracts 106, 18867e.
The IFSCC in Cannes. (1998) Manufacturing Chemist 61-62.
Granger, S. and Scott, I. (1998) Skin care compositions containing a polycyclic triterpene carboxylic acid and a retenol. Unites States Patent no. 5,723, 139.
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Ursolic acid has been put under scientific scrutiny to investigate a number of proposed effects, using cell lines or animal models. Ursolic Acid and its derivatives have shown promise in fighting cancer, due to an ability to suppress the growth of new blood vessels, which some types of cancer require to grow and spread, and by helping to stop cell division (1).
Ursolic acid may be beneficial to in treating diabetes via a number of mechanisms. Of particular interest is its suspected ability to enhance the effects of insulin on sugar uptake (2). There is much hope, but so far evidence for a role in promoting cardiovascular health is conflicting and under-studied (3). Studies in mice have identified promise for Ursolic acid both in preventing muscle wasting, and encouraging the growth of skeletal muscle. It may also be able to affect the way fat is accumulated in the body, and prevent obesity (4,5). Lastly, Ursolic acid is thought to possess weak anti-aromatase activity (6).
The properties of Ursolic acid have generated a lot of interest within the bodybuilding community. Insulin, apart from regulating the levels of sugar in the blood, has powerful anabolic effects. Ursolic acid has been shown to behave in quite a similar way to insulin, reducing circulating blood sugar, and stimulating muscle growth. In one study researchers saw an increase in the amount of IGF-1, a powerful anabolic substance stimulated by human growth hormone, produced by the skeletal muscles (4).
Ursolic acid has also shown promise in weight control. In mice fed a high fat diet, those supplemented with Ursolic acid ate more and gained less weight – the differences were shown to be due to a lower accumulation of fat. This shows a lot of promise for Ursolic acid as a fat burner (5). Aromatase is the enzyme in the body that converts testosterone to oestrogen. Minimising this reaction with an aromatase inhibitor means maximising the effects of the body's own testosterone production, which is important to anyone trying to bulk up (6).
Ursolic acid can be stacked with anything, but stacking with fat burners or testosterone boosters may enhance its effects or the purpose of body-building and weight loss.
(1)Ma CM, Cai SQ, Cui JR, Wang RQ, Tu PF, Hattori M. Daneshtalab, M (2005). "The cytotoxic activity of ursolic acid derivatives". Eur. J. Med. Chem 40 (6): 582–589
(2) Zhang W, et al. Ursolic acid and its derivative inhibit protein tyrosine phosphatase 1B, enhancing insulin receptor phosphorylation and stimulating glucose uptake. Biochim Biophys Acta. (2006)
(3) Tannock LR. Ursolic acid effect on atherosclerosis: apples and apples, or apples and oranges. Atherosclerosis. (2011)
(4) Kunkel, S. D.; Suneja, M.; Ebert, S. M.; Bongers, K. S.; Fox, D. K.; Malmberg, S. E.; Alipour, F.; Shields, R. K.; Adams, C. M. (2011). "MRNA Expression Signatures of Human Skeletal Muscle Atrophy Identify a Natural Compound that Increases Muscle Mass". Cell Metabolism 13 (6): 627–638.
(5) Kunkel SD, Elmore CJ, Bongers KS, Ebert SM, Fox DK, et al. (2012) Ursolic Acid Increases Skeletal Muscle and Brown Fat and Decreases Diet-Induced Obesity, Glucose Intolerance and Fatty Liver Disease
(6) Gnoatto, SC; Dassonville-Klimpt, A; Da Nascimento, S; Galéra, P; Boumediene, K; Gosmann, G; Sonnet, P; Moslemi, S (2008). "Evaluation of ursolic acid isolated from Ilex paraguariensis and derivatives on aromatase inhibition". European journal of medicinal chemistry 43(9): 1865–77.
(7) Liao Q, et al. LC-MS determination and pharmacokinetic studies of ursolic acid in rat plasma after administration of the traditional chinese medicinal preparation Lu-Ying extract.Yakugaku Zasshi. (2005)
(8) Chattopadhyay D, et al. A potent sperm motility-inhibiting activity of bioflavonoids from an ethnomedicine of Onge, Alstonia macrophylla Wall ex A. DC, leaf extract. Contraception. (2005).
(9) Messner B, et al. Ursolic acid causes DNA-damage, p53-mediated, mitochondria- and caspase-dependent human endothelial cell apoptosis, and accelerates atherosclerotic plaque formation in vivo. Atherosclerosis. (2011)
**Always consult with a physician prior to adding any nutritional supplement to your regimen to ensure that there are no contraindications.
*FDA disclaimer: These statements have not been evaluated or approved by the FDA. This product is not intended to treat, cure or prevent any disease or illness.
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