The antinociceptive and anti-inflammatory activities of caulerpin, a bisindole alkaloid isolated from seaweeds of the genus Caulerpa.

Abstract

The antinociceptive and anti-inflammatory activity of caulerpin was investigated. This bisindole alkaloid was isolated from the lipoid extract of Caulerpa racemosa and its structure was identified by spectroscopic methods, including IR and NMR techniques. The pharmacological assays used were the writhing and the hot plate tests, the formalin-induced pain, the capsaicin-induced ear edema and the carrageenan-induced peritonitis. Caulerpin was given orally at a concentration of 100 micromol/kg. In the abdominal constriction test caulerpin showed reduction in the acetic acid-induced nociception at 0.0945 micromol (0.0103-1.0984) and for dypirone it was 0.0426 micromol (0.0092-0.1972). In the hot plate test in vivo the inhibition of nociception by caulerpin (100 micromol/kg, p.o.) was also favorable. This result suggests that this compound exhibits a central activity, without changing the motor activity (seen in the rotarod test). Caulerpin (100 micromol/kg, p.o.) reduced the formalin effects in both phases by 35.4% and 45.6%, respectively. The possible anti-inflammatory activity observed in the second phase in the formalin test of caulerpin (100 micromol/kg, p.o.) was confirmed on the capsaicin-induced ear edema model, where an inhibition of 55.8% was presented. Indeed, it was also observed in the carrageenan-induced peritonitis that caulerpin (100 micromol/kg, p.o.) exhibited anti-inflammatory activity, reducing significantly the number of recruit cells by 48.3%. Pharmacological studies are continuing in order to characterize the mechanism(s) responsible for the antinociceptive and anti-inflammatory actions and also to identify other active principles present in Caulerpa racemosa.

• Authors: Everton Tenório de Souza, Daysianne Pereira de Lira, Aline Cavalcanti de Queiroz, Diogo José Costa da Silva, Anansa Bezerra de Aquino, Eliane A Campessato Mella, Vitor Prates Lorenzo, George Emmanuel C de Miranda, João Xavier de Araújo-Júnior, Maria Célia de Oliveira Chaves, José Maria Barbosa-Filho, Petrônio Filgueiras de Athayde-Filho, Bárbara Viviana de Oliveira Santos, Magna Suzana Alexandre-Moreira
• Journal: Marine drugs (Mar Drugs) Vol. 7 Issue 4 Pg. 689-704 (Nov 26 2009) ISSN: 1660-3397 [Electronic] Switzerland
• PMID: 20098607 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Analgesics
• Anti-Inflammatory Agents
• Indole Alkaloids
• Indoles
• Formaldehyde
• caulerpin
• Carrageenan
• Capsaicin

Topics

• Analgesics (isolation & purification, pharmacology, therapeutic use)
• Animals
• Anti-Inflammatory Agents (isolation & purification, pharmacology, therapeutic use)
• Capsaicin
• Carrageenan
• Caulerpa (chemistry)
• Dose-Response Relationship, Drug
• Edema (chemically induced, drug therapy)
• Female
• Formaldehyde
• Indole Alkaloids (isolation & purification, pharmacology, therapeutic use)
• Indoles (isolation & purification, pharmacology, therapeutic use)
• Male
• Mice
• Pain (chemically induced, drug therapy)
• Peritonitis (chemically induced, drug therapy)
• Seaweed (chemistry)