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Planta Med 2017; 83(03/04): 306-311
DOI: 10.1055/s-0042-115646
Natural Product Chemistry and Analytical Studies
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Antiparasitic Activity of Diterpenoids Against Trypanosoma cruzi

Sergio Alegre-Gómez
1   Instituto de Ciencias Agrarias, Consejo Superior de Investigaciones Científicas, Madrid, Spain
,
Paula Sainz
1   Instituto de Ciencias Agrarias, Consejo Superior de Investigaciones Científicas, Madrid, Spain
,
M. Fátima Simões
2   Universidade Lusófona Research Center for Biosciences & Health Technologies (CBIOS), Campo Grande, Lisboa, Portugal
3   Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia da Universidade de Lisboa, Lisboa Portugal
,
Patrícia Rijo
2   Universidade Lusófona Research Center for Biosciences & Health Technologies (CBIOS), Campo Grande, Lisboa, Portugal
3   Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia da Universidade de Lisboa, Lisboa Portugal
,
Cristina Moiteiro
4   Centro de Química e Bioquímica, Faculdade de Ciências, Universidade de Lisboa, Campo Grande, Lisboa, Portugal
,
Azucena González-Coloma
1   Instituto de Ciencias Agrarias, Consejo Superior de Investigaciones Científicas, Madrid, Spain
,
Rafael A. Martínez-Díaz
5   Departamento de Medicina Preventiva, Salud Pública y Microbiología, Facultad de Medicina, Universidad Autónoma de Madrid, Madrid, Spain
› Author Affiliations
Further Information

Publication History

received 11 April 2017
revised 08 August 2016

accepted 16 August 2016

Publication Date:
06 September 2016 (online)

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Abstract

Twenty-seven diterpenes, including abietanes, labdanes, abeoabietanes, halimanes, and pimaranes, have been evaluated against epimastigote and intracellular amastigote forms of Trypanosoma cruzi and also against LC5 and NCTC cell lines. Royleanones (3, 4, and 5) and a further abietane (12), obtained by purification of Plectranthus spp. extracts, were the most active compounds on epimastigotes, showing IC50 values similar (1.73 µg/mL, 12) or even lower (0.39, 0.99, and 1.20 µg/mL, 3, 4, and 5 respectively) than the positive control nifurtimox (2.3 µg/mL). On intracellular amastigotes, abietanes 3, 4, and 5 showed a significant activity with IC50 values 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). Compounds 3, 4, and 5 were not cytotoxic to LC5 and NCTC 929 cells at 1 µg/mL.

Key words

Plectranthus spp. - Aeollanthus rydingianus - Lamiaceae - diterpenoids - antitrypanosomal activity - intracellular amastigotes

Supporting Information

 

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