Leishmaniasis and bioinorganic compounds containing Au(I) and Pd(II): antileishmanial activities, mechanims of action and putative new drug targets

• Grant number: 13/08248-1
• Support Opportunities: Regular Research Grants
• Start date: April 01, 2014
• End date: September 30, 2016
• Field of knowledge: Biological Sciences - Parasitology - Protozoology of Parasites
• Principal Investigator: Marcia Aparecida Silva Graminha
• Grantee: Marcia Aparecida Silva Graminha
• Host Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil

Abstract

The World Health Organization (WHO) estimates that more than one billion people suffer from neglected tropical diseases. Leishmaniasis is a widespread disease, affecting 12 million people around the world with about 1-2 million estimated new cases occurring every year. For more than 60 years, pentavalent antimonials, Sb (V) compounds, have been the first-line chemotherapy against leishmaniasis, but the emergence of resistant strains has limited their usefulness. Alternatively, amphotericin B, pentamidine isethionate, miltefosine and paramomycin are available, but their use is limited due to toxicity or high cost of treatment. The main goal of this proposal is to evaluate in vitro and in vivo leishmanicidal activities of bioinorganics compounds containing gold(I) or palladium(II). Besides, investigate possible mechanisms of action of such compounds through proteomics, metalomics and genetics approaches are also been considered. (AU)

Scientific publications

(5)

(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)

LOPERA, A. A.; VELASQUEZ, A. M. A.; CLEMENTINO, L. C.; ROBLEDO, S.; MONTOYA, A.; DE FREITAS, L. M.; BEZZON, V. D. N.; FONTANA, C. R.; GARCIA, C.; GRAMINHA, M. A. S.. Solution-combustion synthesis of doped TiO2 compounds and its potential antileishmanial activity mediated by photodynamic therapy. JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY B-BIOLOGY, v. 183, p. 64-74, JUN 2018. (17/03552-5, 16/05345-4, 16/19289-9, 14/24581-5, 13/08248-1)

DO ESPIRITO SANTO, RAFAEL DIAS; ARENAS VELASQUEZ, ANGELA MARIA; GUSHIKEN PASSIANOTO, LUANA VITORINO; LOPERA SEPULVEDA, ALEX ARBEY; CLEMENTINO, LEANDRO DA COSTA; ASSIS, RENATA PIRES; BAVIERA, AMANDA MARTINS; KALABA, PREDRAG; DOS SANTOS, FABIO NEVES; EBERLIN, MARCOS NOGUEIRA; et al. N, N ', N ''-trisubstituted guanidines: Synthesis, characterization and evaluation of their leishmanicidal activity. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v. 171, p. 13-pg., 2019-06-01. (13/24487-6, 17/03552-5, 13/08248-1, 16/19289-9)

DO ESPIRITO SANTO, RAFAEL DIAS; ARENAS VELASQUEZ, ANGELA MARIA; GUSHIKEN PASSIANOTO, LUANA VITORINO; LOPERA SEPULVEDA, ALEX ARBEY; CLEMENTINO, LEANDRO DA COSTA; ASSIS, RENATA PIRES; BAVIERA, AMANDA MARTINS; KALABA, PREDRAG; DOS SANTOS, FABIO NEVES; EBERLIN, MARCOS NOGUEIRA; et al. N, N `, N `'-trisubstituted guanidines: Synthesis, characterization and evaluation of their leishmanicidal activity. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v. 171, p. 116-128, JUN 1 2019. (13/24487-6, 17/03552-5, 16/19289-9, 13/08248-1)

DE ALMEIDA, LETICIA; PASSALACQUA, THAIS GABAN; DUTRA, LUIZ ANTONIO; VARONEZ DA FONSECA, JESSICA N.; QUEIROZ NASCIMENTO, RHAYANNE F.; IMAMURA, KELY BRAGA; DE ANDRADE, CLEVERTON ROBERTO; DOS SANTOS, JEAN LEANDRO; GRAMINHA, MARCIA A. S.. In vivo antileishmanial activity and histopathological evaluation in Leishmania infantum infected hamsters after treatment with a furoxan derivative. BIOMEDICINE & PHARMACOTHERAPY, v. 95, p. 536-547, NOV 2017. (17/03552-5, 13/08248-1)

ARENAS VELASQUEZ, ANGELA MARIA; RIBEIRO, WILLIAN CAMPOS; VENN, VUTEY; CASTELLI, SILVIA; DE CAMARGO, MARIANA SANTORO; DE ASSIS, RENATA PIRES; DE SOUZA, RODRIGO ALVES; RIBEIRO, ALINE RIMOLDI; PASSALACQUA, THAIS GABAN; DA ROSA, JOAO ARISTEU; et al. Efficacy of a Binuclear Cyclopalladated Compound Therapy for Cutaneous Leishmaniasis in the Murine Model of Infection with Leishmania amazonensis and Its Inhibitory Effect on Topoisomerase 1B. Antimicrobial Agents and Chemotherapy, v. 61, n. 8, AUG 2017. (13/08248-1)