Coleus forskohlii forskoline from

Diterpenes tend to be most abundant in the Lamiaceae family, for example Salvia officinalis, or common sage, which has antiviral diterpenes (Tada et al. 1994) and forskolin from Coleus forskohlii. Forskolin has demonstrated a range of activities, including vasodil-atory, antihypertensive, bronchodilatory, positive inotropic action on... 

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

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]. 

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]. 

Methods of Isolation and Analysis of Forskolin from Coleus forskohlii... 

Saleem AM, Dhasan PB, Rafiullah MRM (2005) Isolation of forskolin from stem of Coleus forskohlii. Pharmacogn Mag 1(3) 89... 

Mishra SP, Gaikar VG (2009) Hydrotropic extraction process for recovery of forskolin from Coleus Forskohlii roots. Ind Eng Chem Res 48(17) 8083-8090. doi 10.1021/ie801728d... 

Malathy S, Pai J (1999) Monitoring of forskolin produedion from roots and callus by HPTLC in Coleus forskohlii Briq. J Spices Aromat Crop 8 153-157... 

Forskolin is a well-known activator of adenylyl cyclase, obtained from the roots of Coleus forskohlii. Several methods were reported for the isolation of pure forskolin from the roots of C. forskohlii. The various methods of isolation, the purity, and yield of isolated forskolin are described. The methods included column chromatography, vacuum liquid chromatography, charcoal... 

An unusual glycoside, wedeloside (96), from Wedelia asperrima (Asteraceae), inhibits mitochondrial ADP/ATP carrier protein and has the ability to protect animals against the toxic effects of aflatoxin Bi (Croteau and Johnson, 1985 Node et al., 1982). Uie diterpene forskolin (97), from Coleus barbatus and C. forskohlii (Lamiaceae), is an activator of adenylate cyclase, and is an active inhibitor of the action of brefeldin A (a fungal metabolite with pronounced effects on protein trafficking in cells) (De Sousa and Shah, 1988 Schreiber, 1992 Valdes et al., 1987 Wagner, 1988). This compound also is of interest as an antihypertensive agent (Alcaraz and Rios, 1991 Hanson, 1991). 

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