| Autor: |
Araújo-Vilges, Keline Medeiros de, Oliveira, Stefan Vilges de, Couto, Shirley Claudino Pereira, Fokoue, Harold Hilarion, Romero, Gustavo Adolfo Sierra, Kato, Massuo Jorge, Romeiro, Luiz Antonio Soares, Leite, José Roberto Souza Almeida, Kuckelhaus, Selma Aparecida Souza |
| Předmět: |
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| Zdroj: |
Pharmaceutical Biology; Dec2017, Vol. 55 Issue 1, p1601-1607, 7p |
| Abstrakt: |
Context:Plants of the Piperaceae family produce piplartine that was used to synthesize the cinnamides. Objective:To assess the effects of piplartine (1) and cinnamides (2–5) against the protozoa responsible for malaria and leishmaniasis, and peritoneal cells of Swiss mice. Materials and methods:Cultures ofLeishmania amazonensis,Plasmodium falciparum-infected erythrocytes, and peritoneal cells were incubated, in triplicate, with different concentrations of the compounds (0 to 256 μg/mL). The inhibitory concentration (IC50) inL. amazonensisand cytotoxic concentration (CC50) in peritoneal cell were assessed by the MTT method after 6 h of incubation, while the IC50forP. falciparum-infected erythrocytes was determined by optical microscopy after 48 or 72 h of incubation; the Selectivity Index (SI) was calculated by CC50/IC50. Results:All compounds inhibited the growth of microorganisms, being more effective againstP. falciparumafter 72 h of incubation, especially for the compounds1(IC50 = 3.2 μg/mL) and5(IC50 = 6.6 μg/mL), than toL. amazonensis(compound1 = 179.0 μg/mL; compound5 = 106.0 μg/mL). Despite all compounds reducing the viability of peritoneal cells, the SI were <10 toL. amazonensis, whereas in the cultures ofP. falciparumthe SI >10 for the piplartine (>37.4) and cinnamides4(>10.7) and5(= 38.4). Discussion and conclusion:The potential of piplartine and cinnamides4and5in the treatment of malaria suggest further pre-clinical studies to evaluate their effects in murine malaria and to determine their mechanisms in cells of the immune system. [ABSTRACT FROM PUBLISHER] |
| Databáze: |
Complementary Index |
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