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
  • 1. Department of Pharmaceutical Sciences, CCS, Universidade Federal de Santa Catarina, Florianópolis 88040-900, Santa Catarina, Brazil. Electronic address: [email protected].
  • 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: [email protected].
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.