{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,6,24]],"date-time":"2026-06-24T16:14:09Z","timestamp":1782317649162,"version":"3.54.5"},"reference-count":51,"publisher":"MDPI AG","issue":"5","license":[{"start":{"date-parts":[[2013,5,13]],"date-time":"2013-05-13T00:00:00Z","timestamp":1368403200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/3.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Marine Drugs"],"abstract":"<jats:p>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 \u00b1 1.9 \u00d7 10\u22125 M), histamine (IC50 = 1.3 \u00b1 0.3 \u00d7 10\u22124 M) and  serotonin (IC50 = 8.0 \u00b1 1.4 \u00d7 10\u22125 M) in a non-selective manner. Furthermore,  caulerpine concentration-dependently inhibited serotonin-induced cumulative contractions  (pD\u20322 = 4.48 \u00b1 0.08), shifting the curves to the right with Emax reduction and slope of  2.44 \u00b1 0.21, suggesting a noncompetitive antagonism pseudo-irreversible. The alkaloid also relaxed the ileum pre-contracted by KCl (EC50 = 9.0 \u00b1 0.9 \u00d7 10\u22125 M) and carbachol (EC50 = 4.6 \u00b1 0.7 \u00d7 10\u22125 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.<\/jats:p>","DOI":"10.3390\/md11051553","type":"journal-article","created":{"date-parts":[[2013,5,13]],"date-time":"2013-05-13T12:17:01Z","timestamp":1368447421000},"page":"1553-1564","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":26,"title":["Spasmolytic Effect of Caulerpine Involves Blockade of Ca2+ Influx on Guinea Pig Ileum"],"prefix":"10.3390","volume":"11","author":[{"given":"Luiz","family":"Cavalcante-Silva","sequence":"first","affiliation":[{"name":"Laboratory of Pharmacology and Immunity, Institute of Biological Sciences and Health, Federal University of Alagoas, Macei\u00f3 57020-720, AL, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ana","family":"De Carvalho Correia","sequence":"additional","affiliation":[{"name":"Postgraduate Program in Natural Products and Synthetic Bioactive, Federal University of Para\u00edba,  Jo\u00e3o Pessoa 58051-900, PB, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jos\u00e9","family":"Barbosa-Filho","sequence":"additional","affiliation":[{"name":"Postgraduate Program in Natural Products and Synthetic Bioactive, Federal University of Para\u00edba,  Jo\u00e3o Pessoa 58051-900, PB, Brazil"},{"name":"Department of Pharmaceutical Sciences, Federal University of Para\u00edba, Jo\u00e3o Pessoa  58051-900, PB, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Bagn\u00f3lia","family":"Da Silva","sequence":"additional","affiliation":[{"name":"Postgraduate Program in Natural Products and Synthetic Bioactive, Federal University of Para\u00edba,  Jo\u00e3o Pessoa 58051-900, PB, Brazil"},{"name":"Department of Pharmaceutical Sciences, Federal University of Para\u00edba, Jo\u00e3o Pessoa  58051-900, PB, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"B\u00e1rbara","family":"De Oliveira Santos","sequence":"additional","affiliation":[{"name":"Postgraduate Program in Natural Products and Synthetic Bioactive, Federal University of Para\u00edba,  Jo\u00e3o Pessoa 58051-900, PB, Brazil"},{"name":"Department of Pharmaceutical Sciences, Federal University of Para\u00edba, Jo\u00e3o Pessoa  58051-900, PB, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Daysianne","family":"De Lira","sequence":"additional","affiliation":[{"name":"Postgraduate Program in Natural Products and Synthetic Bioactive, Federal University of Para\u00edba,  Jo\u00e3o Pessoa 58051-900, PB, Brazil"},{"name":"Department of Pharmaceutical Sciences, Federal University of Para\u00edba, Jo\u00e3o Pessoa  58051-900, PB, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"J\u00e9ssica","family":"Sousa","sequence":"additional","affiliation":[{"name":"Postgraduate Program in Natural Products and Synthetic Bioactive, Federal University of Para\u00edba,  Jo\u00e3o Pessoa 58051-900, PB, Brazil"},{"name":"Department of Pharmaceutical Sciences, Federal University of Para\u00edba, Jo\u00e3o Pessoa  58051-900, PB, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"George","family":"De Miranda","sequence":"additional","affiliation":[{"name":"Laboratory of Marine Algae, Department of Systematics and Ecology, Federal University of Para\u00edba, Jo\u00e3o Pessoa 58051-900, PB, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Fabiana","family":"De Andrade Cavalcante","sequence":"additional","affiliation":[{"name":"Department of Physiology and Pathology, Federal University of Para\u00edba, Jo\u00e3o Pessoa 58051-900, PB, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Magna","family":"Alexandre-Moreira","sequence":"additional","affiliation":[{"name":"Laboratory of Pharmacology and Immunity, Institute of Biological Sciences and Health, Federal University of Alagoas, Macei\u00f3 57020-720, AL, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2013,5,13]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"894","DOI":"10.1016\/j.drudis.2008.07.004","article-title":"Natural products in drug discovery","volume":"13","author":"Harvey","year":"2008","journal-title":"Drug Discov. 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