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Mar. Drugs 2013, 11(5), 1553-1564; doi:10.3390/md11051553
Article

Spasmolytic Effect of Caulerpine Involves Blockade of Ca2+ Influx on Guinea Pig Ileum

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1 Laboratory of Pharmacology and Immunity, Institute of Biological Sciences and Health, Federal University of Alagoas, Maceió 57020-720, AL, Brazil 2 Postgraduate Program in Natural Products and Synthetic Bioactive, Federal University of Paraíba, João Pessoa 58051-900, PB, Brazil 3 Department of Pharmaceutical Sciences, Federal University of Paraíba, João Pessoa 58051-900, PB, Brazil 4 Laboratory of Marine Algae, Department of Systematics and Ecology, Federal University of Paraíba, João Pessoa 58051-900, PB, Brazil 5 Department of Physiology and Pathology, Federal University of Paraíba, João Pessoa 58051-900, PB, Brazil
* Authors to whom correspondence should be addressed.
Received: 25 February 2013 / Revised: 16 April 2013 / Accepted: 26 April 2013 / Published: 13 May 2013
(This article belongs to the Special Issue Marine Algae)
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Abstract

In this work, we investigated the spasmolytic effect of caulerpine, a bisindole alkaloid isolated from marine algae of the Caulerpa genus, on guinea pig ileum. Our findings indicated that caulerpine inhibited phasic contractions induced by carbachol (IC50 = 7.0 ± 1.9 × 10−5 M), histamine (IC50 = 1.3 ± 0.3 × 10−4 M) and serotonin (IC50 = 8.0 ± 1.4 × 10−5 M) in a non-selective manner. Furthermore, caulerpine concentration-dependently inhibited serotonin-induced cumulative contractions (pD′2 = 4.48 ± 0.08), shifting the curves to the right with Emax reduction and slope of 2.44 ± 0.21, suggesting a noncompetitive antagonism pseudo-irreversible. The alkaloid also relaxed the ileum pre-contracted by KCl (EC50 = 9.0 ± 0.9 × 10−5 M) and carbachol (EC50 = 4.6 ± 0.7 × 10−5 M) in a concentration-dependent manner. This effect was probably due to inhibition of Ca2+ influx through voltage-gated calcium channels (CaV), since caulerpine slightly inhibited the CaCl2-induced contractions in depolarizing medium without Ca2+, shifting the curves to the right and with Emax reduction. According to these results, the spasmolytic effect of caulerpine on guinea pig ileum seems to involve inhibition of Ca2+ influx through CaV. However, other mechanisms are not discarded.
Keywords: caulerpine; guinea pig ileum; spasmolytic effect; Ca2+ channel caulerpine; guinea pig ileum; spasmolytic effect; Ca2+ channel
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Cavalcante-Silva, L.H.A.; de Carvalho Correia, A.C.; Barbosa-Filho, J.M.; da Silva, B.A.; de Oliveira Santos, B.V.; de Lira, D.P.; Sousa, J.C.F.; de Miranda, G.E.C.; de Andrade Cavalcante, F.; Alexandre-Moreira, M.S. Spasmolytic Effect of Caulerpine Involves Blockade of Ca2+ Influx on Guinea Pig Ileum. Mar. Drugs 2013, 11, 1553-1564.

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