2. Academic Validation
  3. Individual and combined antiparasitic effect of six plant metabolites against Leishmania amazonensis and Trypanosoma cruzi

Individual and combined antiparasitic effect of six plant metabolites against Leishmania amazonensis and Trypanosoma cruzi

  • Bioorg Med Chem Lett. 2016 Apr 1;26(7):1772-5. doi: 10.1016/j.bmcl.2016.02.044.
Louis P Sandjo 1,  Milene H de Moraes 2,  Victor Kuete 3,  Blaise C Kamdoum 4,  Bonaventure T Ngadjui 4,  Mario Steindel 5
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Sciences, CCS, Universidade Federal de Santa Catarina, Florianópolis 88040-900, Santa Catarina, Brazil. Electronic address: p.l.sandjo@ufsc.br.
  • 2 Department of Microbiology, Immunology and Parasitology, Universidade Federal de Santa Catarina, 88040-900 Florianópolis, Santa Catarina, Brazil.
  • 3 Department of Biochemistry, Faculty of Science, University of Dschang, PO Box 67, Dschang, Cameroon.
  • 4 Department of Organic Chemistry, University of Yaoundé 1, PO Box 812, Yaoundé, Cameroon.
  • 5 Department of Microbiology, Immunology and Parasitology, Universidade Federal de Santa Catarina, 88040-900 Florianópolis, Santa Catarina, Brazil. Electronic address: mario.steindel@ufsc.br.
PMID: 26906638 DOI: 10.1016/j.bmcl.2016.02.044
Abstract

Six plant metabolites including isobavachalcone (1), 4-hydroxylonchocarpine (2), and (E)-1-(2,2-dimethyl-2H-chromen-6-yl)-3-(4-hydroxyphenyl)prop-2-en-1-one (3), 6,8-(di-3-methyl-but-2-enyl)eriodictyol (4), damnacanthal (5), and buesgenine (6) were evaluated for their leishmanicidal and trypanocidal activities against intracellular amastigotes of Leishmania amazonensis and Trypanosoma cruzi. Compounds 2-4 and 6 displayed antileishmanial activity while 3 and 5 showed trypanocidal effect. The leishmanicidal activity of 6 was expressed with the lowest IC50 (5.70μg/mL) whereas the most trypanocidal metabolite (5) showed its activity with IC50 at 11.14μg/mL. In addition, antiprotozoal effect of mixtures of 1-6 prepared at different ratios (3:1, 1:1, and 1:3) was also investigated. Interestingly, 1 and 2 initially inactive against T. cruzi, displayed trypanocidal activities when mixed together. This activity increased when 3 (13.63μg/mL) was combined with 1 in ratios 1:1 (10.01μg/mL) and 3:1 (7.78μg/mL). Moreover, the leishmanicidal effect of 4 against L. amazonensis increased in the mixture 6/4 (1:3).

Keywords

Activity in combination; Antiparasitic effect; Secondary metabolites.

Figures