This study reports the activity induced by (1,4)-2-methyl-1,5-bis(4-nitrophenyl)penta-1,4-dien-3-one against This compound showed trypanocidal activity against the multiplicative epimastigote and amastigote forms of this protozoan, with IC values of 1.99 ± 0.17 and 1.20 ± 0.16 M, respectively, and EC value of 15.57 ± 0.34 M against trypomastigotes. The combination of with benznidazole or ketoconazole demonstrated strong synergism, increasing effectiveness against trypomastigotes or epimastigotes of . In addition, the drug combination of with benznidazole or ketoconazole on LLCMK cells demonstrated an antagonist effect, which resulted in greater protection of the cells from drug damage. The combination of the compound with fluconazole was not effective. Transmission and scanning electron micrographs showed changes on parasites, mainly in the cytoplasmatic membrane, nucleus, mitochondrion, and Golgi complex, and a large increase in the number of autophagosome-like structures and lipid-storage bodies, accompanied by volume reduction and rounding of the parasite. might be a promising compound against .
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http://dx.doi.org/10.1155/2017/7254193 | DOI Listing |
Acta Trop
August 2024
Laboratorio de Sintese de Farmacos -LASFAR, Instituto de Tecnologia em Farmacos - Farmanguinhos, Fundação Oswaldo Cruz, Rio de Janeiro, RJ 21041-250, Brazil. Electronic address:
Chagas disease (CD), caused by the flagellated protozoan Trypanosoma cruzi (T. cruzi), affects approximately 7 million people worldwide and is endemic in Latin America, especially among socioeconomically disadvantaged populations. Since the 1960s, only two drugs have been commercially available for treating this illness: nifurtimox (NFX) and benznidazole (BZN).
View Article and Find Full Text PDFRev Soc Bras Med Trop
October 2022
Fundação Oswaldo Cruz, Instituto Nacional de Infectologia Evandro Chagas, Rio de Janeiro, RJ, Brasil.
Background: The recent urbanization of Chagas disease (CD) has contributed to a greater risk of coexistence with human immunodeficiency virus (HIV) and AIDS.
Methods: This retrospective observational study included patients who were followed at INI-Fiocruz between July 1986 and October 2021. All patients underwent an assessment protocol that included sociodemographic profile, epidemiological history, and clinical evaluation.
Biomed Res Int
March 2018
Programa de Pós-Graduação em Ciências Biológicas, Universidade Estadual de Maringá, Av. Colombo 5790, 87020-900 Maringá, PR, Brazil.
This study reports the activity induced by (1,4)-2-methyl-1,5-bis(4-nitrophenyl)penta-1,4-dien-3-one against This compound showed trypanocidal activity against the multiplicative epimastigote and amastigote forms of this protozoan, with IC values of 1.99 ± 0.17 and 1.
View Article and Find Full Text PDFAntimicrob Agents Chemother
January 2012
Programa de Pós-Graduação em Microbiologia, Universidade Estadual de Londrina, Londrina, Paraná, Brazil.
American trypanosomiasis, or Chagas' disease, is caused by Trypanosoma cruzi and affects around 15 million people throughout the American continent. The available treatment is based on two nitroheterocyclic drugs, nifurtimox and benznidazole, both only partially effective and toxic. In this context, new drugs must be found.
View Article and Find Full Text PDFMem Inst Oswaldo Cruz
July 2009
Laboratório de Doenças Parasitárias, Instituto Oswaldo Cruz, Fiocruz, Rio de Janeiro 21040-360, Brasil.
Treatments for Chagas disease have been administered since the first attempts by Mayer & Rocha Lima (1912, 1914) and up to the drugs currently in use (nifurtimox and benznidazole), along with potential drugs such as allopurinol and first, second and third-generation antifungal agents (imidazoles and triazoles), in separate form. Several diseases such as tuberculosis, leprosy and AIDS only came under control after they were treated with associations of drugs with different mechanisms of action. This not only boosts the action of the different compounds, but also may avoid the development of parasite resistance .
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