Activity of synthetic chalcones in hamsters experimentally infected with Leishmania (Viannia) braziliensis

Abstract

The purpose of this study is to evaluate the toxicity of synthetic chalcones 1 and 2 in uninfected hamsters and anti-Leishmania activity of synthetic chalcones 1 and 2 in hamsters infected with Leishmania (Viannia) braziliensis. For the toxicity test, uninfected animals were treated with chalcones 1 and 2, and clinical and biochemical parameters and histological aspects of the liver and kidneys were assessed. Chalcones 1 and 2 were then intraperitoneally or topically administered (10 mg/kg body weight) three times per week in animals infected with promastigotes of L. (V.) braziliensis. We monitored the thickness of the infected footpads, determined parasitic load, performed histological analysis, and detected apoptosis in situ. The results were analyzed using Student's t test and Mann-Whitney test at a significance level of 5%. Neither of the chalcones showed toxicity. Chalcone 2 administered intraperitoneally significantly reduced the thickness of the infected footpad compared with the beginning of treatment. The parasite load of the lymph node and spleen was reduced in the groups treated with chalcones 1 (topical) and 2 (intraperitoneal). Chalcone 2 (topical) reduced parasite burden only in the lymph node. The histological analysis revealed reconstitution of the tissue and reductions of inflammation and apoptosis in the infected footpad in these groups. The synthetic chalcones 1 (topical) and 2 (intraperitoneal and topical) at a dose of 10 mg/kg showed anti-Leishmania activity in vivo, no renal or hepatic toxicity, and a reduction of apoptosis of the cells in the lesions. These chalcones may have substantial potential for the treatment of cutaneous leishmaniasis.

Photodynamic Therapy for the Treatment of American Tegumentary Leishmaniasis: Evaluation of Therapies Association in Experimentally Infected Mice With Leishmania (Leishmania) amazonensis

“…The doses, number of injections and route of administration used are similar to those used in other studies that have achieved therapeutic success. 30,33,34 However, the total number of PDT sessions was only 8 in the first cycle of treatment and 12 in the second cycle, which differed from the other experiments, which performed a total of 36 irradiation sessions, in addition to using hamsters and not mice as in this study. 16,30 Thus, we believe that a longer treatment with PDT may contribute to a greater reduction in the volume and thickness of the lesions.…”

Evaluación de la toxicidad de chalconas sintéticas con potencial anti-Leishmania en ratones BALB/c

“…Según el modelo in vivo de leishmaniosis, la vía de administración, el esquema del tratamiento y el efecto biológico pueden diferir. De Mello et al determinaron la no toxicidad de dos chalconas sintéticas (por vía intralesional y por vía IP) evaluadas hasta una dosis de 10 mg/kg de peso corporal administradas tres veces por semana durante cuatro semanas y la actividad antiparasitaria de las mismas contra Leishmania braziliensis en hámsteres dorados (16) . Aponte et al observaron una alta actividad in vivo de las chalconas 42 y 43 (administradas por vía intralesional) en el modelo murino infectado por Leishmania amazonensis en la almohadilla plantar (9) .…”

Monocristais de 1-(2'-hidroxifenil)-3-hidroxi-3-(4-metoxifenil)-propan-1-ona: Síntese, estrutura e propriedades vibracionais

“…Todas estas substâncias têm sido amplamente investigadas recentemente. Todas elas são muito promissoras por suas propriedades ópticas não lineares (NLO) (Fichou, 1988) e também por suas atividades biológicas, como anticancerígena (Bertl, 2004), antileishmania (Mello, 2015), antituberculose (Gupta, 2013), antimicrobiana (Gupta, 2010;Sahu, 2012), antimalárica (Narender, 2005), antifúngica (Boeck, 2005) e anti-inflamatória (Kontogiorgis, 2008;Batovska, 2010). Muito esforço tem sido dedicado ao entendimento e descrição de suas propriedades, bem como, na busca do controle da síntese desses materiais.…”