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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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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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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