scholarly journals In vitro trypanocidal activity of DB745B and other novel arylimidamides against Trypanosoma cruzi

2011 ◽  
Vol 66 (6) ◽  
pp. 1295-1297 ◽  
Author(s):  
Cristiane França Da Silva ◽  
Angela Junqueira ◽  
Marli Maria Lima ◽  
Alvaro José Romanha ◽  
Policarpo Ademar Sales Junior ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Trypanocidal Activity

scholarly journals In vitro trypanocidal activity of the Egyptian plant Schinopsis lorentizii against trypomastigote and amastigote forms of Trypanosoma cruzi

2016 ◽  
pp. 055-060 ◽  
Author(s):  
Khaled Rashed ◽  
Daniele Ferreira ◽  
Viviane Esperandim ◽  
Maria Marcal ◽  
Breno Sequeira ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Trypanocidal Activity

scholarly journals Structure-Based Virtual Screening and In Vitro Evaluation of New Trypanosoma cruzi Cruzain Inhibitors

2019 ◽  
Vol 20 (7) ◽  
pp. 1742 ◽  
Author(s):  
Verónica Herrera-Mayorga ◽  
Edgar Lara-Ramírez ◽  
Karla Chacón-Vargas ◽  
Charmina Aguirre-Alvarado ◽  
Lorena Rodríguez-Páez ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Trypanosoma Cruzi ◽  
Selection Process ◽  
Chronic Phase ◽  
Inhibitory Effect ◽  
Pharmacological Treatments ◽  
Trypanocidal Activity ◽  
Trypanocidal Drugs ◽  
Cruzain Inhibitors

Chagas disease (CD), or American trypanosomiasis, causes more than 10,000 deaths per year in the Americas. Current medical therapy for CD has low efficacy in the chronic phase of the disease and serious adverse effects; therefore, it is necessary to search for new pharmacological treatments. In this work, the ZINC15 database was filtered using the N-acylhydrazone moiety and a subsequent structure-based virtual screening was performed using the cruzain enzyme of Trypanosoma cruzi to predict new potential cruzain inhibitors. After a rational selection process, four compounds, Z2 (ZINC9873043), Z3 (ZINC9870651), Z5 (ZINC9715287), and Z6 (ZINC9861447), were chosen to evaluate their in vitro trypanocidal activity and enzyme inhibition. Compound Z5 showed the best trypanocidal activity against epimatigote (IC50 = 36.26 ± 9.9 μM) and trypomastigote (IC50 = 166.21 ± 14.5 μM and 185.1 ± 8.5 μM on NINOA and INC-5 strains, respectively) forms of Trypanosoma cruzi. In addition, Z5 showed a better inhibitory effect on Trypanosoma cruzi proteases than S1 (STK552090, 8-chloro-N-(3-morpholinopropyl)-5H-pyrimido[5,4-b]-indol-4-amine), a known cruzain inhibitor. This study encourages the use of computational tools for the rational search for trypanocidal drugs.

scholarly journals In Vitro and In Vivo Studies of the Trypanocidal Activity of Four Terpenoid Derivatives against Trypanosoma cruzi

2012 ◽  
Vol 87 (3) ◽  
pp. 481-488 ◽  
Author(s):  
Inmaculada Ramírez-Macías ◽  
Manuel Sánchez-Moreno ◽  
Enrique Alvarez-Manzaneda ◽  
Ramón Gutierrez-Sánchez ◽  
María José Rosales ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
In Vivo Studies ◽  
Trypanocidal Activity

scholarly journals Synthesis and “in Vitro” Trypanocidal Activity Evaluation of Some Organo-iron Compounds.

2002 ◽  
Vol 8 (6) ◽  
pp. 329-332 ◽  
Author(s):  
Máfircio L. A. e Silva ◽  
Alberto F. Neto ◽  
Silvia A. Cardoso ◽  
Sérgio Albuquerque ◽  
Joseph Miller
Keyword(s):  
Trypanosoma Cruzi ◽  
Chagas Disease ◽  
In Vitro Assay ◽  
In Vitro Assays ◽  
Ferrocene Derivatives ◽  
Iron Compounds ◽  
Vitro Assay ◽  
Trypanocidal Activity ◽  
Activity Evaluation

Eight organo-iron ferrocene derivatives and arenocenium salts were prepared and evaluated by “in vitro” assay against one strain of Trypanosoma cruzi (Y). Six of the eight organo-iron compounds assayed, piperazinium diferrocenoate 1, η6-(o-xylene)-η5-(cyclopentadienyl) Iron(II) hexafluorophosphate 3, η6 -(mesitylene)-η5 -(cyclopentadienyl) iron(II) hexafluorphosphate 5, η6 -(durene)-η5 -(cyclopentadienyl) iron(II) hexafluorphosphate 6, η6 -(ρ-chlorotoluene)-η5 -(cyclopentadienyl) Iron(II) hexafluorphosphate 7 and η6 -(chlorobenzene)-η5 -(cyclopentadienyl) iron(II) picrate 8 , were poorly active in the “in vitro” assays. Only two compounds 1,1'–(N-pyperidinocarbonyl) ferrocene 2(IC50=2.4    μg/mL) and η6-(o-xylene)-η5(cyclopentadienyl) iron(II) picrate 4(IC50=12.08    μg/mL), were more active. Thus, some of the compounds are promising to be used against Chagas' disease as a prophylactic agents.

In Vitro Trypanocidal Activity of Tetraethylthiuram Disulfide and Sodium Diethylamine-N-Carbodithioate on Trypanosoma cruzi

1996 ◽  
Vol 55 (3) ◽  
pp. 263-266 ◽  
Author(s):  
Joshua E. Lane ◽  
Clint E. Carter ◽  
Rodrigo Ribeiro-Rodrigues ◽  
Burton J. Bogitsh ◽  
Pramod K. Singh ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Trypanocidal Activity ◽  
Tetraethylthiuram Disulfide

scholarly journals Trypanosoma cruzi: modification of macrophage function during infection.

1977 ◽  
Vol 146 (1) ◽  
pp. 157-171 ◽  
Author(s):  
N Nogueira ◽  
S Gordon ◽  
Z Cohn
Keyword(s):  
Trypanosoma Cruzi ◽  
Plasminogen Activator ◽  
Macrophage Activation ◽  
Specific Antigen ◽  
Peritoneal Macrophages ◽  
Complement Receptor ◽  
Trypanocidal Activity ◽  
Immunological Specificity ◽  
Mycobacterial Antigens

Infection of mice with Trypanosoma cruzi and subsequent intraperitoneal challenge with heat-killed trypanosomes elicits peritoneal macrophages which display in vitro microbicidal activity against trypomastigotes of T. cruzi. These cells also display other activated properties including rapid spreading, intense membrane activity, secretion of high levels of plasminogen activator, and ingestion mediated by the C3 receptor. An intravenous infection with BCG, followed by an intraperitoneal challenge with mycobacterial antigens brings about macrophages with similar properties. These criteria of macrophage activation were compared in normal and BCG- or T. cruzi-immune mice, with or without an intraperitoneal challenge with specific or unrelated antigens. Trypanocidal activity is displayed by both BCG- and T. cruzi-immune macrophages after intraperitoneal challenge with either antigen. Resident-immune macrophages from both T. cruzi- and BCG-infected mice show a trypanostatic, rather than trypanocidal activity. Macrophages from noninfected mice, challenged with the same antigens, show neither trypanostatic nor trypanocidal activity. Increased secretion of plasminogen activator shows a definite immunological specificity. Challenge with the specific antigen induces the appearance of macrophages secreting high levels of plasminogen activator, while unrelated antigens induce much smaller levels. Noninfected mice challenged with the same antigens do not display any enchancement in secretion. In contrast, increased spreading and phagocytosis mediated by the complement receptor are also displayed by cells from noninfected mice challenged with any of the agents tested.

scholarly journals Chemical Composition and Anti-Trypanosoma cruzi Activity of Essential Oils Obtained from Leaves of Xylopia frutescens and X. laevigata (Annonaceae)

2013 ◽  
Vol 8 (3) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Thanany Brasil da Silva ◽  
Leociley Rocha Alencar Menezes ◽  
Marília Fernanda Chaves Sampaio ◽  
Cássio Santana Meira ◽  
Elisalva Teixeira Guimarães ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Trypanosoma Cruzi ◽  
Essential Oils ◽  
Trypanocidal Activity ◽  
Germacrene D ◽  
Main Components ◽  
Type Apparatus

Essential oils from leaves of Xylopia frutescens (XFMJ) and two specimens of Xylopia laevigata (XLMC and XLSI) were obtained by hydrodistillation using a Clevenger-type apparatus, and analyzed by GC-MS and GC-FID. Sesquiterpenes dominated the essential oils. The main constituents of XFMJ were ( E)-caryophyllene (24.8%), bicyclogermacrene (20.8%), germacrene D (17.0%), β-elemene (7.9%), and ( E)-β-ocimene (6.8%). XLMC contained significant quantities of germacrene D (18.9%), bicyclogermacrene (18.4%), β-elemene (9.5%), 5-selinene (9.2%), ( E)-caryophyllene (8.5%), germacrene B (5.7%) and γ-muurolene (5.7%), while germacrene D (27.0%), bicyclogermacrene (12.8%), ( E)-caryophyllene (8.6%), γ-muurolene (8.6%), 5-cadinene (6.8%), and germacrene B (6.0%) were the main components of XLSI. The essential oils had trypanocidal activity against the Y strain of Trypanosoma cruzi. with IC50 values lower than 30 μg.mL−1 and 15 μg.mL−1 against epimastigote and trypomastigote forms of T. cruzi. respectively, and were also able to reduce the percentage in vitro of T. cruzi-infected macrophages and the intracellular number of amastigotes at concentrations that were non-cytotoxic to macrophages.

scholarly journals Trypanosoma cruzi: in vitro induction of macrophage microbicidal activity.

1978 ◽  
Vol 148 (1) ◽  
pp. 288-300 ◽  
Author(s):  
N Nogueira ◽  
Z A Cohn
Keyword(s):  
Trypanosoma Cruzi ◽  
Spleen Cell ◽  
Peritoneal Macrophages ◽  
Complete Disappearance ◽  
Microbicidal Activity ◽  
Trypanocidal Activity ◽  
Intracellular Parasites ◽  
Normal Spleen

Normal, resident and inflammatory mouse peritoneal macrophages can be induced to display microbicidal activity against trypomastigotes of Trypanosoma cruzi by exposure to products from antigen-pulsed, sensitized spleen cell populations. Optimal macrophage microbicidal activity was achieved by constant exposure and daily renewal of the spleen cell factors. Macrophages obtained after an intraperitoneal injection of mild inflammatory agents were rapidly induced, displaying trypanocidal activity 24 h after exposure to the active spleen cell factor(s), and by 48 h, parasites were no longer observed. Resident peritoneal macrophages required 24 h longer for activation. Removal of the factor(s) before achieving complete disappearance of intracellular parasites led to resumed growth of the surviving organisms. The spleen cell factor(s) is effective when added either before or after exposure of the macrophages to trypomastigotes, and does not itself alter parasite viability. Dilution of the factor(s) up to 1:16 still results in significant trypanocidal activity. In vivo activated cells, obtained after a specific secondary challenge of animals infected with T. cruzi or Bacille Calmette-Guérin, lose their trypanocidal activity under in vitro conditions. This loss of activity can be prevented or restored by the addition of the active spleen cell factor(s). Induction of trypanocidal activity is also obtained with products from Concanavalin A- or lipopolysaccharide-stimulated normal spleen cells.

scholarly journals Trypanocidal activity and selectivity in vitro of aromatic amidine compounds upon bloodstream and intracellular forms of Trypanosoma cruzi

2011 ◽  
Vol 127 (2) ◽  
pp. 429-435 ◽  
Author(s):  
E.M. De Souza ◽  
P.B. da Silva ◽  
A.S.G. Nefertiti ◽  
M.A. Ismail ◽  
R.K. Arafa ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Trypanocidal Activity

IN VITRO and IN VIVO TRYPANOCIDAL ACTIVITY OF A BENZOFUROXAN DERIVATIVE AGAINST Trypanosoma cruzi

2021 ◽  
pp. 108125
Author(s):  
Letícia dos Santos Petry ◽  
João Cândido Pillar Mayer ◽  
Marjorie de Giacommeti ◽  
Dionatan Teixeira de Oliveira ◽  
Litiérria Razia Garzon ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Trypanocidal Activity
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