AvaliaÃÃo da atividade esquistossomicida do FZ4 encapsulado em lipossomas

AUTOR(ES)

Cinthia Meireles Batista

DATA DE PUBLICAÇÃO

2006

RESUMO

The goal of this study is to report the antischistosomal activity of liposomes containing 3-(4-chloro-benzyl)-5-(4-nitro-benzylidene)-imidazolidine-2,4-dione (FZ4-LPSF). The solubility of FZ4 at different pH values was evaluated. Liposomes containing FZ4 (Lipo-FZ4) were obtained through lipid thin film method. The antischistosomal activity was investigated in Swiss mice infected with Schistosoma mansoni. The treatment of animals was performed 49 days after infection with daily dose of 50, 125, 200 mg/kg (i.p.) for 5 days. Animals were killed 64 days post-treatment and the hepatic and portal mesenteric vessels were perfused to recover adult worms. Qualitative oogram patterns were evaluated in small intestine, in which the developmental stages of the eggs were classified. FZ4 is more soluble at pH 12 (14.52 μg/mL) than pH 7.4 (0.53 μg/mL). The two carboxylic groups presented at the imidazolic ring of FZ4 are electron acceptors, which confer a Lewis acid character to FZ4. Similar effects are observed for the p-chloride placed in the benzyl ring and the p-nitro at the benzylidene radical, both presenting positive σp electroattractor effects of 0.24 e 0.78, respectively. The entrapment efficiency of FZ4 into liposomes (1.0 mg/ml) was 95.9% (Â1.4). Remarkable reductions in worm burden (24,65% and 42,4%) were observed with free FZ4 and lipo-FZ4 (50 mg/kg) treatments, respectively. According to the oogram there was an interruption of the ovoposition in all the mice treated. The treatment of animals infected with S. mansoni with lipo-FZ4 evidenced the antischistosomal effect of the FZ4

ASSUNTO(S)

farmacia fz4 schistosoma mansoni lipossomes fz4 esquistossomose schistosomiasis schistosoma mansoni lipossomas

Documentos Relacionados

• AvaliaÃÃo da atividade esquistossomicida do 3 - (4-clorobenzil)-5-(4-nitrobenzilideno)-imidazolidina-2,4-diona (FZ-4) e do Praziquantel frente a Schistosoma mansoni (cepa BH)
• ObtenÃÃo de derivados da Primina: avaliaÃÃo do perfil de atividade biolÃgica
• AvaliaÃÃo da atividade antitumoral em extrato de Indigofera suffruticosa Mill
• SÃntese e avaliaÃÃo da atividade antiinflamatÃria de 5-Benzilideno-3-(4-Clorobenzil)-tiazolidina-2,4-dionas
• Protocolo para avaliaÃÃo do efeito da radiaÃÃo ionizante na atividade da glicoproteÃna -P