Antiparasitic Activity of Diterpenoids Against Trypanosoma cruzi.
Twenty-seven diterpenes, including abietanes, labdanes, abeoabietanes, halimanes, and pimaranes, have been evaluated against epimastigote and intracellular amastigote forms ofTrypanosoma cruziand also against LC5 and NCTC cell lines. Royleanones (3, 4, and5) and a further abietane (12), obtained by purification ofPlectranthusspp. extracts, were the most active compounds on epimastigotes, showing IC50values similar (1.73 µg/mL,12) or even lower (0.39, 0.99, and 1.20 µg/mL,3, 4, and5respectively) than the positive control nifurtimox (2.3 µg/mL). On intracellular amastigotes, abietanes3, 4, and5showed a significant activity with IC50values of 0.83, < 0.31, and 0.62 µg/mL, respectively, but were less potent than the positive control nifurtimox (IC50< 0.16 µg/mL). Compounds3, 4, and5were not cytotoxic to LC5 and NCTC 929 cells at 1 µg/mL.
Instituto de Ciencias Agrarias, Consejo Superior de Investigaciones Científicas, Madrid, Spain.
Sergio
S
Alegre-Gómez
Instituto de Ciencias Agrarias, Consejo Superior de Investigaciones Científicas, Madrid, Spain.
Paula
P
Sainz
Universidade Lusófona Research Center for Biosciences & Health Technologies (CBIOS), Campo Grande, Lisboa, Portugal.
M Fátima
MF
Simões
Universidade Lusófona Research Center for Biosciences & Health Technologies (CBIOS), Campo Grande, Lisboa, Portugal.
Patrícia
P
Rijo
Centro de Química e Bioquímica, Faculdade de Ciências, Universidade de Lisboa, Campo Grande, Lisboa, Portugal.
Cristina
C
Moiteiro
Instituto de Ciencias Agrarias, Consejo Superior de Investigaciones Científicas, Madrid, Spain.
Azucena
A
González-Coloma
Departamento de Medicina Preventiva, Salud Pública y Microbiología, Facultad de Medicina, Universidad Autónoma de Madrid, Madrid, Spain.
Rafael A
RA
Martínez-Díaz
D000818:Animals; D000977:Antiparasitic Agents / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D004224:Diterpenes / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D031346:Plectranthus / Q000737:chemistry; D014349:Trypanosoma cruzi / Q000187:drug effects*
D000977:Antiparasitic Agents; D004224:Diterpenes; D010936:Plant Extracts