Effect of piplartine and cinnamides on Leishmania amazonensis, Plasmodium falciparum and on peritoneal cells of Swiss mice. (1st January 2017)

• Record Type: Journal Article
• Authors: 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
• Is Part Of: Pharmaceutical biology. Volume 55:Number 1(2017)
• Page Start: 1601
• Page End: 1607
• Publication Date: 2017-01-01
• Subjects: Piperlongumine -- selectivity index -- malaria -- Leishmaniasis; Piperaceae; Pharmacognosy -- Periodicals; Materia medica, Vegetable -- Periodicals; 615.321
• DOI: 10.1080/13880209.2017.1313870
• Languages: English
• ISSNs: 1388-0209

Abstract

Abstract: 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 of Leishmania 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 ) in L. amazonensis and cytotoxic concentration (CC50 ) in peritoneal cell were assessed by the MTT method after 6 h of incubation, while the IC50 for P. 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 against P. falciparum after 72 h of incubation, especially for the compounds 1 (IC50 = 3.2 μg/mL) and 5 (IC50 = 6.6 μg/mL), than to L. amazonensis (compound 1 = 179.0 μg/mL; compound 5 = 106.0 μg/mL). Despite all compounds reducing the viability of peritoneal cells, the SI were <10 to L. amazonensis, whereas in the cultures of P. falciparum the SI >10 for the piplartine (>37.4) and cinnamides 4 (>10.7) and 5 (= 38.4). Discussion and conclusion: The potential of piplartine and cinnamides 4 and 5 in 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.