The efficacy of novel arylimidamides against Trypanosoma cruzi in vitro

Cristiane Frana Da Silva, Anissa Daliry, Patrcia Bernardino Da Silva, Senol Akay, Moloy Banerjee, Abdelbasset A. Farahat, Mary K. Fisher, Laixing Hu, Arvind Kumar, Zongying Liu, Chad E. Stephens, David W. Boykin, Maria De Nazar Correia Soeiro

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

The present study aimed to determine the in vitro biological efficacy and selectivity of 7 novel AIAs upon bloodstream trypomastigotes and intracellular amastigotes of Trypanosoma cruzi. The biological activity of these aromatic compounds was assayed for 48 and 24 h against intracellular parasites and bloodstream forms of T. cruzi (Y strain), respectively. Additional assays were also performed to determine their potential use in blood banks by treating the bloodstream parasites with the compounds diluted in mouse blood for 24 h at 4C. Toxicity against mammalian cells was evaluated using primary cultures of cardiac cells incubated for 24 and 48 h with the AIAs and then cellular death rates were determined by MTT colorimetric assays. Our data demonstrated the outstanding trypanocidal effect of AIAs against T. cruzi, especially DB1853, DB1862, DB1867 and DB1868, giving IC50 values ranging between 16 and 70 nanomolar against both parasite forms. All AIAs presented superior efficacy to benznidazole and some, such as DB1868, also demonstrated promising activity as a candidate agent for blood prophylaxis. The excellent anti-trypanosomal efficacy of these novel AIAs against T. cruzi stimulates further in vivo studies and justifies the screening of new analogues with the goal of establishing a useful alternative therapy for Chagas disease.

Original languageEnglish (US)
Pages (from-to)1863-1869
Number of pages7
JournalParasitology
Volume138
Issue number14
DOIs
StatePublished - Dec 1 2011

Fingerprint

Trypanosoma cruzi
Parasites
parasites
blood flow
blood
bloodstream forms
trypomastigotes
amastigotes
Blood Banks
alternative medicine
Chagas disease
Primary Cell Culture
Chagas Disease
assays
Complementary Therapies
in vivo studies
Inhibitory Concentration 50
aromatic compounds
inhibitory concentration 50
bioactive properties

Keywords

  • Chagas disease
  • Trypanosoma cruzi
  • arylimidamides
  • chemotherapy

ASJC Scopus subject areas

  • Parasitology
  • Animal Science and Zoology
  • Infectious Diseases

Cite this

Da Silva, C. F., Daliry, A., Da Silva, P. B., Akay, S., Banerjee, M., Farahat, A. A., ... Correia Soeiro, M. D. N. (2011). The efficacy of novel arylimidamides against Trypanosoma cruzi in vitro. Parasitology, 138(14), 1863-1869. https://doi.org/10.1017/S0031182011001429

The efficacy of novel arylimidamides against Trypanosoma cruzi in vitro. / Da Silva, Cristiane Frana; Daliry, Anissa; Da Silva, Patrcia Bernardino; Akay, Senol; Banerjee, Moloy; Farahat, Abdelbasset A.; Fisher, Mary K.; Hu, Laixing; Kumar, Arvind; Liu, Zongying; Stephens, Chad E.; Boykin, David W.; Correia Soeiro, Maria De Nazar.

In: Parasitology, Vol. 138, No. 14, 01.12.2011, p. 1863-1869.

Research output: Contribution to journalArticle

Da Silva, CF, Daliry, A, Da Silva, PB, Akay, S, Banerjee, M, Farahat, AA, Fisher, MK, Hu, L, Kumar, A, Liu, Z, Stephens, CE, Boykin, DW & Correia Soeiro, MDN 2011, 'The efficacy of novel arylimidamides against Trypanosoma cruzi in vitro', Parasitology, vol. 138, no. 14, pp. 1863-1869. https://doi.org/10.1017/S0031182011001429
Da Silva CF, Daliry A, Da Silva PB, Akay S, Banerjee M, Farahat AA et al. The efficacy of novel arylimidamides against Trypanosoma cruzi in vitro. Parasitology. 2011 Dec 1;138(14):1863-1869. https://doi.org/10.1017/S0031182011001429
Da Silva, Cristiane Frana ; Daliry, Anissa ; Da Silva, Patrcia Bernardino ; Akay, Senol ; Banerjee, Moloy ; Farahat, Abdelbasset A. ; Fisher, Mary K. ; Hu, Laixing ; Kumar, Arvind ; Liu, Zongying ; Stephens, Chad E. ; Boykin, David W. ; Correia Soeiro, Maria De Nazar. / The efficacy of novel arylimidamides against Trypanosoma cruzi in vitro. In: Parasitology. 2011 ; Vol. 138, No. 14. pp. 1863-1869.
@article{c76c5763d0394a6daf497b3893f2882f,
title = "The efficacy of novel arylimidamides against Trypanosoma cruzi in vitro",
abstract = "The present study aimed to determine the in vitro biological efficacy and selectivity of 7 novel AIAs upon bloodstream trypomastigotes and intracellular amastigotes of Trypanosoma cruzi. The biological activity of these aromatic compounds was assayed for 48 and 24 h against intracellular parasites and bloodstream forms of T. cruzi (Y strain), respectively. Additional assays were also performed to determine their potential use in blood banks by treating the bloodstream parasites with the compounds diluted in mouse blood for 24 h at 4C. Toxicity against mammalian cells was evaluated using primary cultures of cardiac cells incubated for 24 and 48 h with the AIAs and then cellular death rates were determined by MTT colorimetric assays. Our data demonstrated the outstanding trypanocidal effect of AIAs against T. cruzi, especially DB1853, DB1862, DB1867 and DB1868, giving IC50 values ranging between 16 and 70 nanomolar against both parasite forms. All AIAs presented superior efficacy to benznidazole and some, such as DB1868, also demonstrated promising activity as a candidate agent for blood prophylaxis. The excellent anti-trypanosomal efficacy of these novel AIAs against T. cruzi stimulates further in vivo studies and justifies the screening of new analogues with the goal of establishing a useful alternative therapy for Chagas disease.",
keywords = "Chagas disease, Trypanosoma cruzi, arylimidamides, chemotherapy",
author = "{Da Silva}, {Cristiane Frana} and Anissa Daliry and {Da Silva}, {Patrcia Bernardino} and Senol Akay and Moloy Banerjee and Farahat, {Abdelbasset A.} and Fisher, {Mary K.} and Laixing Hu and Arvind Kumar and Zongying Liu and Stephens, {Chad E.} and Boykin, {David W.} and {Correia Soeiro}, {Maria De Nazar}",
year = "2011",
month = "12",
day = "1",
doi = "10.1017/S0031182011001429",
language = "English (US)",
volume = "138",
pages = "1863--1869",
journal = "Parasitology",
issn = "0031-1820",
publisher = "Cambridge University Press",
number = "14",

}

TY - JOUR

T1 - The efficacy of novel arylimidamides against Trypanosoma cruzi in vitro

AU - Da Silva, Cristiane Frana

AU - Daliry, Anissa

AU - Da Silva, Patrcia Bernardino

AU - Akay, Senol

AU - Banerjee, Moloy

AU - Farahat, Abdelbasset A.

AU - Fisher, Mary K.

AU - Hu, Laixing

AU - Kumar, Arvind

AU - Liu, Zongying

AU - Stephens, Chad E.

AU - Boykin, David W.

AU - Correia Soeiro, Maria De Nazar

PY - 2011/12/1

Y1 - 2011/12/1

N2 - The present study aimed to determine the in vitro biological efficacy and selectivity of 7 novel AIAs upon bloodstream trypomastigotes and intracellular amastigotes of Trypanosoma cruzi. The biological activity of these aromatic compounds was assayed for 48 and 24 h against intracellular parasites and bloodstream forms of T. cruzi (Y strain), respectively. Additional assays were also performed to determine their potential use in blood banks by treating the bloodstream parasites with the compounds diluted in mouse blood for 24 h at 4C. Toxicity against mammalian cells was evaluated using primary cultures of cardiac cells incubated for 24 and 48 h with the AIAs and then cellular death rates were determined by MTT colorimetric assays. Our data demonstrated the outstanding trypanocidal effect of AIAs against T. cruzi, especially DB1853, DB1862, DB1867 and DB1868, giving IC50 values ranging between 16 and 70 nanomolar against both parasite forms. All AIAs presented superior efficacy to benznidazole and some, such as DB1868, also demonstrated promising activity as a candidate agent for blood prophylaxis. The excellent anti-trypanosomal efficacy of these novel AIAs against T. cruzi stimulates further in vivo studies and justifies the screening of new analogues with the goal of establishing a useful alternative therapy for Chagas disease.

AB - The present study aimed to determine the in vitro biological efficacy and selectivity of 7 novel AIAs upon bloodstream trypomastigotes and intracellular amastigotes of Trypanosoma cruzi. The biological activity of these aromatic compounds was assayed for 48 and 24 h against intracellular parasites and bloodstream forms of T. cruzi (Y strain), respectively. Additional assays were also performed to determine their potential use in blood banks by treating the bloodstream parasites with the compounds diluted in mouse blood for 24 h at 4C. Toxicity against mammalian cells was evaluated using primary cultures of cardiac cells incubated for 24 and 48 h with the AIAs and then cellular death rates were determined by MTT colorimetric assays. Our data demonstrated the outstanding trypanocidal effect of AIAs against T. cruzi, especially DB1853, DB1862, DB1867 and DB1868, giving IC50 values ranging between 16 and 70 nanomolar against both parasite forms. All AIAs presented superior efficacy to benznidazole and some, such as DB1868, also demonstrated promising activity as a candidate agent for blood prophylaxis. The excellent anti-trypanosomal efficacy of these novel AIAs against T. cruzi stimulates further in vivo studies and justifies the screening of new analogues with the goal of establishing a useful alternative therapy for Chagas disease.

KW - Chagas disease

KW - Trypanosoma cruzi

KW - arylimidamides

KW - chemotherapy

UR - http://www.scopus.com/inward/record.url?scp=84862530700&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84862530700&partnerID=8YFLogxK

U2 - 10.1017/S0031182011001429

DO - 10.1017/S0031182011001429

M3 - Article

C2 - 21902869

AN - SCOPUS:84862530700

VL - 138

SP - 1863

EP - 1869

JO - Parasitology

JF - Parasitology

SN - 0031-1820

IS - 14

ER -