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Effect of Novel 7β-Derivatives of Forskolin upon Human Platelet Adenylate Cyclase System

Edward B. Seguin, N. Ferry, Jacques Hanoune, Max Koch

Open publisher page 6 citations

Abstract

We have synthesized different 7β-derivatives of the diterpene forskolin, which are presumably more hydrophilic than the parent compound. Their activity was tested on the adenylate cyclase system of human platelet membranes. The 7β-glyceryl and 7β-dimethylacryloyl derivatives were as potent as native forskolin while 7-deacetylforskolin was 10 fold less active. Pyranosyl derivatives were unable to stimulate adenylate cyclase although they displayed a weak antagonistic effect against forskolin activation.

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What this paper is about

We have synthesized different 7β-derivatives of the diterpene forskolin, which are presumably more hydrophilic than the parent compound. Their activity was tested on the adenylate cyclase system of human platelet membranes. The 7β-glyceryl and 7β-dimethylacryloyl derivatives were as potent as native forskolin while 7-deacetylforskolin was 10 fold less active. Pyranosyl derivatives were unable to stimulate adenylate cyclase although they displayed a weak antagonistic effect against forskolin activation.

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Available abstract

We have synthesized different 7β-derivatives of the diterpene forskolin, which are presumably more hydrophilic than the parent compound. Their activity was tested on the adenylate cyclase system of human platelet membranes. The 7β-glyceryl and 7β-dimethylacryloyl derivatives were as potent as native forskolin while 7-deacetylforskolin was 10 fold less active. Pyranosyl derivatives were unable to stimulate adenylate cyclase although they displayed a weak antagonistic effect against forskolin activation.

Key concepts: Forskolin, Adenylate kinase, Cyclase, Chemistry, Platelet, ADCY9, Biochemistry, Internal medicine

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