期刊
PLANTA MEDICA
卷 88, 期 13, 页码 1163-1174出版社
GEORG THIEME VERLAG KG
DOI: 10.1055/a-1708-2081
关键词
leishmanicidal activity; cytotoxic activity; Leishmania amazonensis; pimaranes; Aldama arenaria (syn; Viguiera arenaria ); Asteraceae
资金
- CNPq [010216/2012-0]
- FAPESP [2010/51454-3]
- Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES) [1481071]
- Fundacao de Amparo a Pesquisa do Estado do Amazonas (FAPEAM) [002/2015]
- CAPES-Demanda Social Scholarship
Two pimarane analogues and their derivatives isolated from Aldama arenaria exhibited moderate cytotoxic activity and leishmanicidal activity. Compound 4 showed the strongest cytotoxic activity, while derivative 5 showed the most promising leishmanicidal activity.
Two pimaranes ent -pimara-8(14),15-dien-19-oic acid ( 1 ) and ent -8(14),15-pimaradien-3 beta -ol ( 2 ), isolated from Aldama arenaria , and six semi-synthetic derivatives methyl ester of the ent -pimara-8(14),15-dien-19-oic acid ( 3 ), ent -pimara-8(14),15-dien-19-ol ( 4 ), acetate of ent -pimara-8(14),15-dien-19-ol ( 5 ), ent -pimara-8(14),15-dien-19-ol succinic acid ( 6 ), acetate of ent -8(14),15-pimaradien-3 beta -ol ( 7 ), ent -8(14),15-pimaradien-3 beta -ol succinic acid ( 8 ) were evaluated in vitro for their cytotoxic activities to childhood leukemia cell lines and leishmanicidal activity against the parasite Leishmania amazonensis. Among these compounds, 1 to 6 presented moderate cytotoxic activity, with compound 4 being the most active (GI (50) of 2.6 mu M for the HL60 line) and the derivatives 7 and 8 being inactive. Against the parasite Leishmania amazonensis , the most promising derivative was the acetate of ent -pimara-8(14),15-dien-19-ol ( 5 ), with EC (50) of 20.1 mu M, selectivity index of 14.5, and significant reduction in the parasite load. Pimarane analogues 1 , ent -pimara-8(14),15-dien-19-oic acid, and 2 , ent -8(14),15-pimaradien-3 beta -ol, presented different activities, corroborating the application of such molecules as prototypes for the design of other derivatives that have greater cytotoxic or leishmanicidal potential.
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