Coleus forskohlii

Forskolin is a diteipene derivative from the plant Coleus forskohlii. It activates all mammalian isozymes of adenylyl cyclase except AC9 and AC 10. 

Some new diterpenoid oxides have been obtained from Eupatorium jhanii. They are jhanol (12) and its 18-acetate together with jhanidiol (13) and its 18-monoacetate and diacetate. Their structures were established by correlation with manoyl oxide and by an examination of their C n.m.r. spectra. 11/3-Hydro-xymanoyl oxide (14) has been isolated from Juniperus oxycedrus ° A group of new 11-oxomanoyl oxide derivatives (15a—e) has been obtained from Coleus forskohlii (Labiatae). Their oxygenation pattern is reminiscent of that of the tricyclic diterpenoids which have beemobtained from other Coleus species. 

The aerial parts of Conyza steudellii (Asteraceae) have given new labdane xylosides, while from the leaves of Conyza trihecatactis, a xylopyranoside of 13-epi-sclareol has been isolated among other labdanes [104,105]. Havardic acids A-F (as methyl esters), have been isolated from another genus of the Asteraceae family, i.e Grindelia havardii [106]. 11-oxo-manoyl oxide derivatives and coleosol, which is also a manoyl oxide derivative, have been obtained from Coleus forskohlii (Labiateae) [107,108] while from another plant of the Labiatae family, Roylea calycina a tumor inhibitory compound, namely precalyone, as well as calyone have been isolated [109]. 

The most important manoyl oxide derivative is forskolin (9), Fig. (7), (7p-acetoxy-8, 13-epoxy-la, 6p, 9a-trihydroxylabd-14-en-ll-one) [151-153]. It belongs to the labdane series of diterpenes and was isolated from the Indian herb Coleus forskohlii (Willd.) Briq. (Labiatae). Since ancient times it has been used in Hindu and Ayurvedic traditional medicine [154]. The plant Coleus forskohlii (Willd.) Briq. has been extensively studied, and from its extracted roots a group of diterpenoids, with the basic skeleton of 11-oxo-manoyl oxide, have been isolated. The main compound, forskolin, presented remarkable chemical and biological properties [155]. Analogues of forskolin were then prepared by semisynthesis [156] or obtained by microbial transformations [157]. New analogues, more soluble than forskolin have shown activities comparable to and even higher than forskolin [158]. 

Most products containing Coleus Forskohlii should be (but rarely actually are) standardized for a 10% forskolin content. An effective dosage of the 10% standardized product has been 165-250 MG, 3-4 times daily. So far there is some existing research that supports the listed effects of Coleus Forskohlii. And anecdotal /personal evaluations are positive thus far. It seems finding an actual standardized source is the most difficult aspect of acquiring favorable results. 

The use of Coleus Forskohlii seems to have possible cardiovascular benefits by acting as a vasodilator (lowers blood pressure), inhibition of platelet aggregation (reduced blood clotting), and positive inotropic activity in the heart (increased contractile force). 

The use of Coleus Forskohlii does not seem to inhibit endogenous TSH production. There is a synergy between this product and beta-andrenergic drugs such as Clenbuterol, ephedrine, synephrine, and norephedrine. 

Some athletes used guggulsterones to regenerate thyroid function after discontinuance of synthetic T-3/T-4 protocols. Those who thought ahead, utilized guggulsterones " synthetic T-3/T-4 thyroid hormone use to prevent thyroid function suppression even temporarily. This usually was initiated 10-14 days prior to synthetic thyroid administration discontinuance. Coleus Forskohlii, the amino acid tyrosine, and iodine also had a noted great deal of value for this purpose. 

T-2 use can create a negative feedback loop at higher dosages and due to prolonged use. The result was often metabolic lag usually for 3-7 days after discontinuance. (See guggulsterones and Coleus Forskohlii for common reported... 

Bhat SV, Bajqwa BS et al (1977) Structures and stereochemistry of new labdane diterpinoids from coleus forskohlii briq. Tetrahedron Lett 18 1669-1672... 

Dideoxyforskolin Coleus forskohlii (Lamiaceae) Inactive as AC activator... 

Forskolin Coleus forskohlii (Lamiaceae) [root] Glc-TR (PM rat adipocyte)... 

Calyone (27) and precalyone (28), the latter showing tumour inhibitory activity, have been isolated from Roylea calycina (Labiatae), and coleosol (29) is a manoyl oxide derivative which has been isolated from another of the Labiatae used in folk medicine. Coleus forskohlii ... 

Forskolin, a labdane diterpenoid, was isolated from the tuberous roots of Coleus forskohlii Briq. (Lami-aceae) [1], C. forskohlii has been used as an important folk medicine in India. Forskolin was found to be an activator of adenylate cyclase [2], leading to an increase of c-AMP, and now a medicine in India, Germany, and Japan. The production of forskolin is completely dependent on the commercial collection of wild and cultivated plants in India. We have already set up the production of monoclonal antibodies (MAbs) against forskolin [3]. The practical application of enzyme-linked immunosorbent assay (ELISA) for the distribution of forskolin contained in clonally propagated plant organs and the quantitative fluctuation of forsko-lin depend on the age of C. forskohlii [4,5]. As an extension of this approach, we present the production of the immunoaffinity column using anti-forskolin MAb and its application [6]. 

Another important use of pure natural substances is as pharmacological or biochemical tools for the study of novel mechanisms of action, or of pathophysiological processes e.g. forskolin is a diterpene in the root of Coleus forskohlii (Lamiaceae), which activates adenylate cyclase and causes an increase in cellular c AMP levels. Phorbol esters (from family Euphorbiaceae) stimulate protein kinase C, and tetrodotoxin in Fu iuspc-cies influences the transport of sodium ions. 

Epothilones A and B are promising anticancer agents that bind to microtubules in the cell in the same way that paclitaxel (Taxol) does and are more potent.410 Paclitaxel was obtained first from the bark of the Pacific yew (Taxus brevifolia).4n Widespread extraction of the compound from this source could have wiped out the species. Fortunately, it can now be extracted from the needles of more common yews or produced in tissue culture. (See Sec II.C on tissue culture.) Forskolin is a diterpene, from the roots of Coleus forskohlii, that lowers blood pressure.412 Him-bacine, from an Australian pine tree, offers a potential treatment for Alzheimer s disease.413 Combretastatin, from the bark of the African bush willow, Combretum caffrum, cuts the flow of blood to tumors, causing 95% of the cancer cells to die in 24 h, but does not harm healthy blood vessels.414... 

FIGURE 52 Forskolin, which is isolated from Coleus forskohlii, stimulates adenylate cyclase. 

Forskolin, which is isolated from Coleus forskohlii, stimulates adenylate cyclase. Choleragen, the secretory product of Vibrio cholerae, can persistently activate adenylate cyclase by catalyzing the transfer of the ADP-ribose moiety of nicotinamide adenine dinucleotide (NAD+) to (see also Figure 52). 

Drim-8-en-l 1-oic acid (158) is a convenient synthon for the preparation of polyfunctional drimanes. This acid has been used as an intermediate in the total synthesis of 1,6,7-tridesoxyforskolin (159), a related compound to forskolin (160), possessing ionotropic, antihypotensive and other activities [106]. Optically active compound (159) was isolated together with forskolin from the plant Coleus forskohlii [107]. 

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