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Coleus Forskohlii Extract
Coleus Forskohlii Extract
Synonyms--- Plectranthus barbatus, Indian Coleus, C. barbatus Benth., Plectranthus forskohlii Willd., and P. comosus Willemse
Chemical Name:(3R,4aR,5S,6S,6aS,10S,10aR,10bS) -6,10,10b-trihydroxy-3,4a,7,7,10a- pentamethyl-1-oxo-3-vinyldodecahydro-1H-benzo[f]chromen-5-yl acetate
Molecular Formula: C22H34O7
Mol. Wt.:410.5 g/mol
Plectranthus barbatus, or more commonly known as Coleus forskohlii and Indian Coleus (other synonyms: C. barbatus Benth., Plectranthus forskohlii Willd., and P. comosus Willemse), , a member of the mint family, is a tropical perennial plant related to the typical coleus species. This species is a perennial herb with fleshy, fibrous roots that grows wild in the warm subtropical temperate areas in India, Burma, Thailand, and South-West China (Yunnan Province). In India, it is cultivated for use as a condiment. Coleus forskohlii is an important traditional Ayurvedic herb that has been a part of Indian medicine for centuries. For centuries, in Ayurvedic medicine, Coleus species have been used to treat various diseases such as hypothyroidism, heart disease, respiratory disorders (asthma), convulsions, spasmodic pain and painful urination.
In recent years, Coleus forskohlii has gained recognition as the only known plant source of the diterpene, forskohlin (Forlean as its patented name), and it is interesting from a scientific and medicinal standpoint because it produces forskolin. In the 1970s researchers isolated a unique chemically active extract from the Coleus forskohlii roots and called it forskolin, which is a labdane diterpene. In addition to forskolin, this herb has labdane diterpene glycosides forskoditerpenosides A, B, C, D, and E. Additional compounds include 14-deoxycoleon U, coleonol, alpha-amyrin, demethylcryptojaponol, betulic acid, alpha-cedrol and beta-sitosterol. Now available in supplement form, coleus forskohlii extract has been tested in a number of conditions.
Forskohlin is valued as an adenylate cyclase activator. Adenylate cyclase is the enzyme involved in the production of Cyclic Adenosine Monophosphate (cAMP), (a significant biochemical agent involved in metabolic processes), from the high energy molecule, ATP (Adenosine triphosphate). Nicknamed in literature as a "second messenger," cyclic AMP facilitates the action of "primary messengers" or various hormonal and bioactive substances in the body. The role of cyclic AMP is indispensable to many body functions. Cyclic AMP induces a chain of biochemical events that trigger metabolic processes and diet induced thermogenesis3, thereby providing the means to maintain a healthy body composition and lean body mass levels.
Forskolin has been extensively researched in the medical field for use in the treatment of allergies, respiratory problems, cardiovascular diseases, glaucoma, psoriasis, hypothyroidism and weight loss. Forskolin increases Cyclic AMP and appears to have additional actions that are due to its ability to alter a number of membrane transport proteins.
The Coleus forskohlii Extract used in dietary supplements is derived from the roots of the plant Coleus forskohlii (Willd.) Briq.
Effects on Cyclic AMP: Increased cellular cyclic AMP results in inhibition of platelet activation, decreased likelihood of blood clots, reduced release of histamine, decreased allergy symptoms, increased force of contraction of the heart, relaxation of the arteries and other smooth muscles, increased thyroid function, increased fat metabolism, increased energy and possibly weight loss. Cyclic AMP and the chemicals it activates comprise a second messenger system that is responsible for carrying out the complex and powerful effects of hormones in the body. In addition, asthma, eczema, psoriasis, angina, obesity and hypertension are believed to be associated with decreased Cyclic AMP.
Treat Glaucoma: Glaucoma is a condition in which the pressure in the eye is too high, due to an imbalance between the formation of aqueous humor in the eye and its absorption in or drainage out of the eye. Eventually, as the pressure builds up, the blood vessels nourishing the optic nerve are constricted, resulting in irreversible damage to the nerve and impaired vision culminating in blindness, if left untreated. There are several treatments that may be beneficial and coleus is one of them. Clinical studies have shown that topical application of one percent forskolin eye drops resulted in significant decreases in intraocular pressure for up to five hours. Limited clinical experience suggests that oral forskolin appears to offer significant potential for sufferers of glaucoma. An Indian pharmaceutical company is currently engaged in clinical trials of a forskolin eye drop product.
Anti-Depression Effects:Depression is believed to be associated with an imbalance of neurotransmitters in the brain, serotonin and dopamine primarily. Where there is a shortage of serotonin, the supplements 5-HTP or tryptophan or the SSRI drugs like prozac or Zoloft may be beneficial. If the catecholamine neurotransmitters (epinephrine, norephinephrine) are deficient the amino acids L-Phenylalanine or L-Tyrosine, or monoamine oxidase inhibitors like GeroVital (GH3) or Deprenyl are may be helpful. Recent research has also been evaluating drugs that increase Cyclic AMP as a means of elevating the catecholamines. Since forskolin elevates Cyclic AMP, it may improve neurotransmitter function and thereby relieve depression. Clinical trials using coleus to treat depression have not been done.
Benefit Asthma and Allergies: Coleus is an effective smooth muscle relaxer, resulting in bronchodilation, decreased airway resistance, increased vital capacity and increased forced expiratory volume. This action is the result of the increase in Cyclic AMP caused by coleus. Many asthma medications increase Cyclic AMP by inhibiting the enzymes that cause its breakdown. Thus, coleus and the traditional asthma drugs are likely to act synergistically. Therefore, one should consult their physician before combining them.
Weight Loss Effects:It stimulates fat metabolism. It can increase lean body mass, and promote favorable changes in body composition. Researchers have found that many obese people have lower than normal Cyclic AMP production. Because of these considerations, coleus may, theoretically, be a weight loss agent, especially for those with reduced Cyclic AMP production. In a recent study, six overweight women took 25 mg of coleus (250 mg capsules of 10% standardized forskolin extract) twice daily for eight weeks. At the end of the eight-week trial, the participants lost a mean of ten pounds, and reduced their percentage of body fat by nearly 8%. Blood pressure levels also trended lower during the trial.
Anti-Hypothyroidism: It increases thyroid hormone production and stimulate thyroid hormone release.
Anti-Cancer-Metastases:Forskolin act to be a potent inhibitor of tumor colonization, to prevent or inhibit tumor metastases. Applied with rolipram, forskolin provides a route to inhibition of colon cancer cell growth and survival. These two drugs also work together to induce long-term potentiation in neuronal populations.
Immune Enhancement Effects:exhibit potent immune system enhancement by activating macrophages and lymphocytes.
Treat Psoriasis:In psoriasis, cells divide about 1,000 times faster than normal. Coleus helps to alleviate psoriasis by normalizing the cAMP /cGMP ratio.
Cardiovascular Effects, Reduce Blood pressure, Anti-hypertension: Forskolin is a vasodilator. It reduces blood pressure and improve heart function in people with cardiomyopathy. Coleus forskohlii has traditionally been used to treat hypertension, congestive heart failure, and angina. Coleus's basic cardiovascular action is to lower blood pressure, while simultaneously increasing the contractility of the heart. This is believed to be due to forskolin's Cyclic AMP-elevating ability, which results in relaxation of the arteries, and increased force of contraction of the heart muscle. A preliminary trial found that coleus reduced blood pressure and improved heart function in people with cardiomyopathy. Coleus also increases cerebral blood flow, indicating that it may be beneficial in cerebral vascular insufficiency, and in enhancing post-stroke recovery. The platelet aggregation-inhibiting effects of coleus also adds to its value in cardiovascular disorders.
Anti-virus and Anti HIV activity
Increase skin's natural resistance to burning under UV light.It stimulates a tanning response when applied topically.
Reduce urinary tract infections and enhance the ability of antibiotics to kill bacteria that normally survive.
Forskolin can also be used to promote nerve repair by increasing cAMP concentrations. Forskolin can activate or upregulate the proliferation of Schwann cells in culture, together with Fibroblast growth factor or Transforming Growth Factor-Beta. Various experimental studies are underway in using Forskolin as an adjuvant in treatment for diseases such as Parkinsons and/or nerve damage caused by trauma/accident.
Mechanism of action
Forskolin is a diterpene from the roots of Coleus forskohli. In the study and research of cell physiology, it directly activates the enzyme adenylate cyclase and raisesthe intracellular levels of cyclic Adenosine Monophosphate (cyclic AMP or cAMP) in a variety of tissues. Cyclic AMP is an important signal carrier or cell regulating compound necessary for the proper biological response of cells to hormones and other extracellular signals. It is required for cell communication in the hypothalamus/pituitary gland axis and for the feedback control of hormones. It acts by activating protein kinase A.
Once formed, cAMP activates many other enzymes involved in diverse cellular functions. Under normal situations cAMP is formed when a stimulatory hormone (e.g., epinephrine) binds to a receptor site on the cell membrane and stimulates the activation of adenylate cyclase. This enzyme is incorporated into all cellular membranes and only the specificity of the receptor determines which hormone will activate it in a particular cell. Forskolin appears to bypass this need for direct hormonal activation of adenylate cyclase. As a result of this direct activation of adenylate cyclase, intracellular cAMP levels rise. The physiological and biochemical effects of a raised intracellular cAMP level include: inhibition of platelet activation; inhibition of mast cell degranulation and histamine release; increased force of contraction of heart muscle; relaxation of the arteries and other smooth muscles; increased insulin secretion; and increased thyroid function.
Coleus Forskohlii Extract is safe, no side effects have been reported to date, but relying on this type of treatment alone, and avoiding conventional medical care, may have serious health consequences.
• The typical dose is 500-1000mg (10% forsklin) per day (usually in 2-3 doses throughout the day).
• Consult physicians for different condition specifics.
GNI’s Coleus Forskohlii Features and Benefits:
Coleu forskohlii Extract is one of GNI's most competitive products, with many advantages as list in the following, produced as our patent-pending process and know-how technology from Coleus Forskohlii roots.
• Produced with pure water only
• High purity: over 98%
• NO solvent - residual free
• Yellow in appearance
• High solubility in water
• High anti-bacteria, and longer shelf life
10%, 20%, 40%, 98% Forskolin HPLC