RESUMO

Calophyllum species are sources of calanolides, which inhibit human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT). The hexane extract of the leaves from C. brasiliense collected in Soconusco, State of Chiapas, Mexico, analyzed by HPLC showed to contain apetalic acid, calanolides B, and C. It showed potent anti-HIV-1 RT inhibition (IC(50)=20.2 µg/ml), but was not toxic in mice (LD(50)=1.99 g/kg). The histological study of the mice treated at the highest dose revealed no alteration on hepatocytes, and an increase in the number of spleen megakaryocytes. These results suggest this extract is suitable to continue studies for developing a phytodrug against HIV-1.

Assuntos

Calophyllum/química , Transcriptase Reversa do HIV/antagonistas & inibidores , Isoflavonas/farmacologia , Fitoterapia , Extratos Vegetais/farmacologia , Piranocumarinas/farmacologia , Inibidores da Transcriptase Reversa/farmacologia , Animais , Calophyllum/efeitos adversos , Infecções por HIV/tratamento farmacológico , Infecções por HIV/virologia , HIV-1/enzimologia , Hepatócitos/efeitos dos fármacos , Humanos , Isoflavonas/efeitos adversos , Isoflavonas/análise , Masculino , Megacariócitos/efeitos dos fármacos , México , Camundongos , Extratos Vegetais/efeitos adversos , Extratos Vegetais/química , Folhas de Planta , Piranocumarinas/efeitos adversos , Piranocumarinas/análise , Inibidores da Transcriptase Reversa/efeitos adversos , Inibidores da Transcriptase Reversa/análise , Baço/efeitos dos fármacos