Cryptolepis sanguinolenta: Antimuscarinic Properties of Cryptolepine and the Alkaloid Fraction at M1, M2 and M3 Receptors

Hans W. Rauwald; Martin Kober; Ernst Mutschler; Günter Lambrecht

doi:10.1055/s-2006-961531

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Planta Med 1992; 58(6): 486-488
DOI: 10.1055/s-2006-961531

Papers

Cryptolepis sanguinolenta: Antimuscarinic Properties of Cryptolepine and the Alkaloid Fraction at M1, M2 and M3 Receptors

Hans W. Rauwald¹ , Martin Kober¹ , Ernst Mutschler² , Günter Lambrecht²

¹Institute of Pharmaceutical Biology, University of Frankfurt, Georg-Voigt-Str. 16, D(W)-6000 Frankfurt/M. 11, Federal Republic of Germany
²Department of Pharmacology, University of Frankfurt, Theodor-Stern-Kai 7, Geb. 75A, D(W)-6000 Frankfurt/M., Federal Republic of Germany

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Publikationsverlauf

1991

Publikationsdatum:
05. Januar 2007 (online)

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Abstract

From an ethanol extract of the roots of Cryptolepis sanguinolenta the alkaloid fraction and its main constituent cryptolepine were isolated by partitioning at pH 11 and column chromatography using silica gel and chloroform/methanol as eluent. Cryptolepine was identified mainly by EI-MS and ¹H/¹³C-NMR spectroscopy. Cryptolepine (3-30 μM) and the alkaloid fraction of Cryptolepis sanguinolenta (3-10 μg/ml) antagonized muscarinic effects at M1 receptors in rabbit vas deferens, M2 receptors in guinea-pig atria, and M3 receptors in guinea-pig ileum. The experiments, using N-methylatropine as reference drug, showed a significant antimuscarinic activity for both cryptolepine and the alkaloid fraction, but no appreciable receptor subtype selectivity (pA₂ = 5.00-5.73). Cryptolepine was determined as the antimuscarinic principle of Cryptolepis sanguinolenta. At higher concentrations both materials displayed negative inotropic effects.

Key words

Cryptolepis sanguinolenta (Lindley) Schlechter - Periplocaceae - cryptolepine - alkaloids - antimuscarinic properties - muscarinic receptor subtypes - N-methylatropine.