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Effects of (1E,4E)-2-Methyl-1,5-bis(4-nitrophenyl)penta-1,4-dien-3-one on Trypanosoma cruzi and Its Combinational Effect with Benznidazole, Ketoconazole, or Fluconazole
Joint Authors
Ueda-Nakamura, Tânia
Nakamura, Celso Vataru
Peron, Francieli
Lazarin-Bidóia, Danielle
Ud Din, Zia
Rodrigues-Filho, Edson
Silva, Sueli de Oliveira
Source
Issue
Vol. 2017, Issue 2017 (31 Dec. 2017), pp.1-11, 11 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2017-05-23
Country of Publication
Egypt
No. of Pages
11
Main Subjects
Abstract EN
This study reports the activity induced by (1E,4E)-2-methyl-1,5-bis(4-nitrophenyl)penta-1,4-dien-3-one (A3K2A3) against Trypanosoma cruzi.
This compound showed trypanocidal activity against the multiplicative epimastigote and amastigote forms of this protozoan, with IC50 values of 1.99±0.17 and 1.20±0.16 μM, respectively, and EC50 value of 15.57±0.34 μM against trypomastigotes.
The combination of A3K2A3 with benznidazole or ketoconazole demonstrated strong synergism, increasing effectiveness against trypomastigotes or epimastigotes of T.
cruzi.
In addition, the drug combination of A3K2A3 with benznidazole or ketoconazole on LLCMK2 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.
A3K2A3 might be a promising compound against T.
cruzi.
American Psychological Association (APA)
Peron, Francieli& Lazarin-Bidóia, Danielle& Ud Din, Zia& Rodrigues-Filho, Edson& Ueda-Nakamura, Tânia& Silva, Sueli de Oliveira…[et al.]. 2017. Effects of (1E,4E)-2-Methyl-1,5-bis(4-nitrophenyl)penta-1,4-dien-3-one on Trypanosoma cruzi and Its Combinational Effect with Benznidazole, Ketoconazole, or Fluconazole. BioMed Research International،Vol. 2017, no. 2017, pp.1-11.
https://search.emarefa.net/detail/BIM-1138476
Modern Language Association (MLA)
Peron, Francieli…[et al.]. Effects of (1E,4E)-2-Methyl-1,5-bis(4-nitrophenyl)penta-1,4-dien-3-one on Trypanosoma cruzi and Its Combinational Effect with Benznidazole, Ketoconazole, or Fluconazole. BioMed Research International No. 2017 (2017), pp.1-11.
https://search.emarefa.net/detail/BIM-1138476
American Medical Association (AMA)
Peron, Francieli& Lazarin-Bidóia, Danielle& Ud Din, Zia& Rodrigues-Filho, Edson& Ueda-Nakamura, Tânia& Silva, Sueli de Oliveira…[et al.]. Effects of (1E,4E)-2-Methyl-1,5-bis(4-nitrophenyl)penta-1,4-dien-3-one on Trypanosoma cruzi and Its Combinational Effect with Benznidazole, Ketoconazole, or Fluconazole. BioMed Research International. 2017. Vol. 2017, no. 2017, pp.1-11.
https://search.emarefa.net/detail/BIM-1138476
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1138476