The antinociceptive and anti-inflammatory activities of caulerpin, a bisindole alkaloid isolated from seaweeds of the genus Caulerpa.
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.
de Souza
Everton Tenório
ET
LaFI-Laboratório de Farmacologia e Imunidade, Instituto de Ciências Biológicas e da Saúde, Universidade Federal de Alagoas, Maceió (AL), Brazil. evertontenorio_al@yahoo.com.br
de Lira
Daysianne Pereira
DP
de Queiroz
Aline Cavalcanti
AC
da Silva
Diogo José Costa
DJ
de Aquino
Anansa Bezerra
AB
Mella
Eliane A Campessato
EA
Lorenzo
Vitor Prates
VP
de Miranda
George Emmanuel C
GE
de Araújo-Júnior
João Xavier
JX
Chaves
Maria Célia de Oliveira
MC
Barbosa-Filho
José Maria
JM
de Athayde-Filho
Petrônio Filgueiras
PF
Santos
Bárbara Viviana de Oliveira
BV
Alexandre-Moreira
Magna Suzana
MS
D000700:Analgesics / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D002211:Capsaicin; D002351:Carrageenan; D046068:Caulerpa / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy*; D005260:Female; D005557:Formaldehyde; D026121:Indole Alkaloids / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D007211:Indoles / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D008297:Male; D051379:Mice; D010146:Pain / Q000139:chemically induced / Q000188:drug therapy*; D010538:Peritonitis / Q000139:chemically induced / Q000188:drug therapy; D012624:Seaweed / Q000737:chemistry*
D000700:Analgesics; D000893:Anti-Inflammatory Agents; D026121:Indole Alkaloids; D007211:Indoles; D005557:Formaldehyde; C000392:caulerpin; D002351:Carrageenan; D002211:Capsaicin