scholarly journals AVALIAÇÃO DA TERAPIA FOTODINÂMICA COM AZUL DE METILENO EM Leishmania major e Leishmania braziliensis: ESTUDO in vitro

2017 ◽  
Vol 22 (40) ◽  
pp. 649
Author(s):  
Danielle El Atra Coelho ◽  
Letícia Corrêa Fontana ◽  
Juliana Guerra Pinto ◽  
Juliana Ferreira-Strixino
Keyword(s):  
Leishmania Major ◽  
Leishmania Braziliensis

A Leishmaníase é uma doença crônica causada pelo protozoário do gênero Leishmania, cujo tratamento é agressivo. A Terapia Fotodinâmica (TFD) é uma alternativa promissora que combina luz, fotossensibilizador (FS) e oxigênio molecular, para causar a morte celular. O objetivo desse trabalho foi avaliar, in vitro, a ação da TFD com Azul de metileno (AM) em promastigotas de Leishmania, por teste de MTT, curva de crescimento e morfologia do parasito. O teste de MTT demonstrou alteração de ambas as espécies após interação com o AM no escuro e após TFD. A análise das curvas demonstrou que a TFD influenciou o crescimento das espécies. A análise morfológica revelou que o AM no escuro não causou alterações expressivas como a TFD, sendo a cepa de L. braziliensis mais afetada que a cepa de L. major. Pode-se concluir que a TFD com AM foi promissora contra promastigotas de Leishmania, pois foi capaz de diminuir o crescimento e alterar a morfologia dos parasitos em cultura.

In vitro evaluation of photodynamic therapy using curcumin on Leishmania major and Leishmania braziliensis

2016 ◽  
Vol 31 (5) ◽  
pp. 883-890 ◽  
Author(s):  
Juliana Guerra Pinto ◽  
Letícia Correa Fontana ◽  
Marco Antonio de Oliveira ◽  
Cristina Kurachi ◽  
Leandro José Raniero ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
Leishmania Major ◽  
Leishmania Braziliensis ◽  
In Vitro Evaluation

Evaluating the Effect of Cinnarizine on Promastigotes and Amastigotes forms of Leishmania major

2020 ◽  
Vol 20 (4) ◽  
pp. 550-555 ◽  
Author(s):  
Lima Asgharpour Sarouey ◽  
Parvaneh Rahimi-Moghaddam ◽  
Fatemeh Tabatabaie ◽  
Khadijeh Khanaliha
Keyword(s):  
Flow Cytometry ◽  
Cutaneous Leishmaniasis ◽  
Leishmania Major ◽  
Inhibitory Effect ◽  
Control Group ◽  
Secondary Infections ◽  
Ic50 Values ◽  
J774 Cells ◽  
Mtt Assays

: As an important global disease, cutaneous leishmaniasis is associated with complications such as secondary infections and atrophic scars. The first line treatment with antimonials is expensive and reported to have serious side effects and enhance resistance development. The main objective of this study was to evaluate the effect of Cinnarizine on standard strains of Leishmania major because of paucity of information on this subject. Methods: In this experimental study, four concentrations of the drug (5, 10, 15 and 20 μg/ml) were added to Leishmania major cultures at 24, 48 and 72 hours intervals. MTT assays were performed to determine parasite viability and drug toxicity. Leishmania major promastigotes were augmented to the in vitro cultured macrophages (J774 cells) and then incubated for 72 hours. Half maximal inhibitory concentration (IC50) was ascertained by counting parasites. The inhibitory effect of the drug was compared with that of Glucantime. Flow-cytometry was performed to investigate apoptosis. Each test was repeated thrice. Results: The IC50 values of Cinnarizine after 72 hours were calculated to be 34.76 μg/ml and 23.73 μg/ml for promastigotes and amastigotes, respectively. The results of MTT assays showed 48 % promastigote viability after 72 hour-exposure to Cinnarizine at 20 μg/ml concentration. Programmed cell death in promastigote- and amastigote-infected macrophages was quantified to be 13.66 % and 98.7 %, respectively. Flow- cytometry analysis indicated that Cinnarizine induced early and late apoptosis in parasites. All treatments produced results which differed significantly from control group (P<0.05). Conclusion: Cinnarizine showed low toxicity with anti-leishmanial and apoptosis effects on both promastigote and intracellular amastigote forms. Therefore, we may suggest further assessment on animal models of this drug as candidates for cutaneous leishmaniasis therapy.

scholarly journals In Vitro Evaluation of the Potential Pharmacological Activity and Molecular Targets of New Benzimidazole-Based Schiff Base Metal Complexes

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 728
Author(s):  
Alberto Aragón-Muriel ◽  
Yamil Liscano ◽  
Yulieth Upegui ◽  
Sara M. Robledo ◽  
María Teresa Ramírez-Apan ◽  
...  
Keyword(s):  
Schiff Base ◽  
Molecular Docking ◽  
Lanthanide Complexes ◽  
Human Tumor ◽  
Model Membranes ◽  
Leishmania Braziliensis ◽  
Cytotoxic Activities ◽  
Schiff Base Ligands ◽  
Major Interest

Metal-based drugs, including lanthanide complexes, have been extremely effective in clinical treatments against various diseases and have raised major interest in recent decades. Hence, in this work, a series of lanthanum (III) and cerium (III) complexes, including Schiff base ligands derived from (1H-benzimidazol-2-yl)aniline, salicylaldehyde, and 2,4-dihydroxybenzaldehyde were synthesized and characterized using different spectroscopic methods. Besides their cytotoxic activities, they were examined in human U-937 cells, primate kidney non-cancerous COS-7, and six other, different human tumor cell lines: U251, PC-3, K562, HCT-15, MCF-7, and SK-LU-1. In addition, the synthesized compounds were screened for in vitro antiparasitic activity against Leishmania braziliensis, Plasmodium falciparum, and Trypanosoma cruzi. Additionally, antibacterial activities were examined against two Gram-positive strains (S. aureus ATCC® 25923, L. monocytogenes ATCC® 19115) and two Gram-negative strains (E. coli ATCC® 25922, P. aeruginosa ATCC® 27583) using the microdilution method. The lanthanide complexes generally exhibited increased biological activity compared with the free Schiff base ligands. Interactions between the tested compounds and model membranes were examined using differential scanning calorimetry (DSC), and interactions with calf thymus DNA (CT-DNA) were investigated by ultraviolet (UV) absorption. Molecular docking studies were performed using leishmanin (1LML), cruzain (4PI3), P. falciparum alpha-tubulin (GenBank sequence CAA34101 [453 aa]), and S.aureus penicillin-binding protein 2a (PBP2A; 5M18) as the protein receptors. The results lead to the conclusion that the synthesized compounds exhibited a notable effect on model membranes imitating mammalian and bacterial membranes and rolled along DNA strands through groove interactions. Interactions between the compounds and studied receptors depended primarily on ligand structures in the molecular docking study.

scholarly journals EAPB0503: an imiquimod analog with potent in vitro activity against cutaneous leishmaniasis caused by Leishmania major and Leishmania tropica

2020 ◽  
Vol 13 (12) ◽  
pp. 2112
Author(s):  
Rana El Hajj ◽  
Hanady Bou Youness ◽  
Laurence Lachaud ◽  
Patrick Bastien ◽  
Carine Masquefa ◽  
...  
Keyword(s):  
Cutaneous Leishmaniasis ◽  
Leishmania Major ◽  
Vitro Activity ◽  
Leishmania Tropica ◽  
In Vitro Activity

Efficacy of biogenic selenium nanoparticles against Leishmania major: In vitro and in vivo studies

2013 ◽  
Vol 27 (3) ◽  
pp. 203-207 ◽  
Author(s):  
Nasibeh Beheshti ◽  
Saied Soflaei ◽  
Mojtaba Shakibaie ◽  
Mohammad Hossein Yazdi ◽  
Fatemeh Ghaffarifar ◽  
...  
Keyword(s):  
Leishmania Major ◽  
Selenium Nanoparticles ◽  
In Vivo Studies ◽  
Biogenic Selenium Nanoparticles

Inhibition by Dications of In Vitro Growth of Leishmania major and Leishmania tropica: Causative Agents of Old World Cutaneous Leishmaniasis

2008 ◽  
Vol 94 (3) ◽  
pp. 743-749 ◽  
Author(s):  
Alexa C. Rosypal ◽  
Karl A. Werbovetz ◽  
Manar Salem ◽  
Chad E. Stephens ◽  
Arvind Kumar ◽  
...  
Keyword(s):  
Cutaneous Leishmaniasis ◽  
Leishmania Major ◽  
Leishmania Tropica ◽  
In Vitro Growth ◽  
Old World ◽  
Causative Agents

scholarly journals Characterization and selective inhibition of myristoyl-CoA:protein N-myristoyltransferase from Trypanosoma brucei and Leishmania major

2006 ◽  
Vol 396 (2) ◽  
pp. 277-285 ◽  
Author(s):  
Chrysoula Panethymitaki ◽  
Paul W. Bowyer ◽  
Helen P. Price ◽  
Robin J. Leatherbarrow ◽  
Katherine A. Brown ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
Leishmania Major ◽  
Homo Sapiens ◽  
Selective Inhibition ◽  
Fungal Species ◽  
Chemotherapeutic Agents ◽  
Human Pathogens ◽  
Ic50 Values

The eukaryotic enzyme NMT (myristoyl-CoA:protein N-myristoyltransferase) has been characterized in a range of species from Saccharomyces cerevisiae to Homo sapiens. NMT is essential for viability in a number of human pathogens, including the fungi Candida albicans and Cryptococcus neoformans, and the parasitic protozoa Leishmania major and Trypanosoma brucei. We have purified the Leishmania and T. brucei NMTs as active recombinant proteins and carried out kinetic analyses with their essential fatty acid donor, myristoyl-CoA and specific peptide substrates. A number of inhibitory compounds that target NMT in fungal species have been tested against the parasite enzymes in vitro and against live parasites in vivo. Two of these compounds inhibit TbNMT with IC50 values of <1 μM and are also active against mammalian parasite stages, with ED50 (the effective dose that allows 50% cell growth) values of 16–66 μM and low toxicity to murine macrophages. These results suggest that targeting NMT could be a valid approach for the development of chemotherapeutic agents against infectious diseases including African sleeping sickness and Nagana.

scholarly journals Achievement of constitutive fluorescent pLEXSY-egfp Leishmania braziliensis and its application as an alternative method for drug screening in vitro

2017 ◽  
Vol 112 (2) ◽  
pp. 155-159 ◽  
Author(s):  
Matheus Silva e Bastos ◽  
◽  
Luciana Ângelo de Souza ◽  
Thiago Souza Onofre ◽  
Abelardo Silva Júnior ◽  
...  
Keyword(s):  
Drug Screening ◽  
Leishmania Braziliensis ◽  
Alternative Method ◽  
Screening In Vitro

scholarly journals EAPB0503: An Imiquimod analog with potent in vitro activity against cutaneous leishmaniasis caused by Leishmania major and Leishmania tropica

2018 ◽  
Vol 12 (11) ◽  
pp. e0006854 ◽  
Author(s):  
Rana El Hajj ◽  
Hanady Bou Youness ◽  
Laurence Lachaud ◽  
Patrick Bastien ◽  
Carine Masquefa ◽  
...  
Keyword(s):  
Cutaneous Leishmaniasis ◽  
Leishmania Major ◽  
Vitro Activity ◽  
Leishmania Tropica ◽  
In Vitro Activity

scholarly journals In Vitro Antileishmanial Activity of Nicotinamide

2005 ◽  
Vol 49 (2) ◽  
pp. 808-812 ◽  
Author(s):  
D. Sereno ◽  
A. Monte Alegre ◽  
R. Silvestre ◽  
B. Vergnes ◽  
A. Ouaissi
Keyword(s):  
Leishmania Major ◽  
Growth Arrest ◽  
Antileishmanial Activity ◽  
Vitamin B ◽  
Wild Type ◽  
Intracellular Growth ◽  
Cell Growth Arrest ◽  
Transgenic Parasites

ABSTRACT Our study represents the first report demonstrating the antileishmanial activity of nicotinamide (NAm), a form of vitamin B3. A 5 mM concentration of NAm significantly inhibited the intracellular growth of Leishmania amastigotes and the NAD-dependent deacetylase activity carried by parasites overexpressing Leishmania major SIR2 (LmSIR2). However, the transgenic parasites were as susceptible as the wild-type parasites to NAm-induced cell growth arrest. Therefore, we conclude that NAm inhibits leishmanial growth and that overexpression of LmSIR2 does not overcome this inhibition. The mechanism of the inhibition is not defined but may include other in vivo targets. NAm may thus represent a new antileishmanial agent which could potentially be used in combination with other drugs during therapy.

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