Antiparasitic Activities of Acridone Alkaloids from Swinglea glutinosa (Bl.) Merr
نویسندگان
چکیده
Onze alcalóides acridônicos isolados de Swinglea glutinosa (Bl.) Merr. foram avaliados para suas atividades in vitro contra linhagens de Plasmodium falciparum sensíveis a cloroquina 3D7, Trypanosoma brucei rhodesiense STIB9000 e Leishmania donovani L82. Ensaios com células KB foram também executados com o objetivo de se determinar o grau de toxicidade das substâncias ativas contra os parasitas. Nove dos compostos apresentaram IC 50 entre 0,3 e 11,6 μM contra P. falciparum. Em contraste, um pequeno número de compostos mostrou atividade significativa contra T. brucei rhodesiense e nenhum apresentou atividade contra L. donovani. Entre os alcalóides três tiveram IC 50 < 1,0 μM contra P. falciparum, enquanto que contra T. b. rhodesiense cinco mostraram IC 50 < 10 μM. A caracterização dos alcalóides, 1,3,5-triidróxi-4-metóxi-10-metil-2,8bis(3-metilbut-2-enil)acridin-9(10H)-ona (1), 2,3-diidro-4,9-diidróxi-2-(2-hidróxipropan-2-il)11-metóxi-10-metilfuro[3,2-b]acridin-5(10H)-ona (2) e 3,4-diidro-3,5,8-triidróxi-6-metóxi-2,2,7trimetil-2H-pirano[2,3-a]acridin-12(7H)-ona (3), é aqui discutida. Discute-se também a relação estrutura-atividade para todos os compostos ensaiados. O isolamento e dados espectrais para os alcalóides 1-3 estão sendo aqui descritos pela primeira vez, embora em trabalho anterior tenham sido relatadas as suas atividades citotóxicas.
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