scholarly journals Novel Arsenic Nanoparticles Are More Effective and Less Toxic than As (III) to Inhibit Extracellular and Intracellular Proliferation ofLeishmania donovani

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Sudipta Chakraborty ◽  
Kaushik Bhar ◽  
Sandip Saha ◽  
Rajarshi Chakrabarti ◽  
Anjali Pal ◽  
...  
Keyword(s):  
Leishmania Donovani ◽  
Protozoan Parasite ◽  
Antileishmanial Activity ◽  
Macrophage Cell Line ◽  
Macrophage Cell ◽  
Vector Borne ◽  
First Time ◽  
Intracellular Proliferation ◽  
Mouse Macrophage Cell Line

Visceral leishmaniasis, a vector-borne tropical disease that is threatening about 350 million people worldwide, is caused by the protozoan parasiteLeishmania donovani. Metalloids like arsenic and antimony have been used to treat diseases like leishmaniasis caused by the kinetoplastid parasites. Arsenic (III) at a relatively higher concentration (30 μg/mL) has been shown to have antileishmanial activity, but this concentration is reported to be toxic in several experimental mammalian systems. Nanosized metal (0) particles have been shown to be more effective than their higher oxidation state forms. There is no information so far regarding arsenic nanoparticles (As-NPs) as an antileishmanial agent. We have tested the antileishmanial properties of the As-NPs, developed for the first time in our laboratory. As-NPs inhibited thein vitrogrowth, oxygen consumption, infectivity, and intramacrophage proliferation ofL. donovaniparasites at a concentration which is about several fold lower than that of As (III). Moreover, this antileishmanial activity has comparatively less cytotoxic effect on the mouse macrophage cell line. It is evident from our findings that As-NPs have more potential than As (III) to be used as an antileishmanial agent.

scholarly journals Antileishmanial Activities of Several Classes of Aromatic Dications

2002 ◽  
Vol 46 (3) ◽  
pp. 797-807 ◽  
Author(s):  
James J. Brendle ◽  
Abram Outlaw ◽  
Arvind Kumar ◽  
David W. Boykin ◽  
Donald A. Patrick ◽  
...  
Keyword(s):  
Cell Line ◽  
Leishmania Donovani ◽  
Pneumocystis Carinii ◽  
Antileishmanial Activity ◽  
Microbial Pathogens ◽  
Mouse Macrophage ◽  
Macrophage Cell Line ◽  
Macrophage Cell ◽  
Mouse Macrophage Cell Line

ABSTRACT Aromatic dicationic molecules possess impressive activity against a broad spectrum of microbial pathogens, including Pneumocystis carinii, Cryptosporidium parvum, and Candida albicans. In this work, 58 aromatic cations were examined for inhibitory activity against axenic amastigote-like Leishmania donovani parasites. In general, the most potent of the compounds were substituted diphenyl furan and thiophene dications. 2,5-Bis-(4-amidinophenyl)thiophene was the most active compound. This agent displayed a 50% inhibitory concentration (IC50) of 0.42 ± 0.08 μM against L. donovani and an in vitro antileishmanial potency 6.2-fold greater than that of the clinical antileishmanial dication pentamidine and was 155-fold more toxic to the parasites than to a mouse macrophage cell line. 2,4-Bis-(4-amidinopheny)furan was twice as active as pentamidine (IC50, 1.30 ± 0.21 μM), while 2,5-bis-(4-amidinopheny)furan and pentamidine were essentially equipotent in our in vitro antileishmanial assay. Carbazoles, dibenzofurans, dibenzothiophenes, and benzimidazoles containing amidine or substituted amidine groups were generally less active than the diphenyl furans and thiophenes. In all cases, aromatic dications possessing strong antileishmanial activity were severalfold more toxic to the parasites than to a cultured mouse macrophage cell line. These structure-activity relationships demonstrate the potent antileishmanial activity of several aromatic dications and provide valuable information for the future design and synthesis of more potent antiparasitic agents.

Novel azoles with potent antileishmanial activity

2021 ◽  
Author(s):  
Tarun Mathur ◽  
Manoj Kumar ◽  
Tarani K Barman ◽  
V Samuel Raj ◽  
Dilip J Upadhyay ◽  
...  
Keyword(s):  
Tissue Culture ◽  
Visceral Leishmaniasis ◽  
Leishmania Donovani ◽  
Antileishmanial Activity ◽  
In Vitro Activity ◽  
Macrophage Cell Line ◽  
Macrophage Cell ◽  
Starting Point ◽  
Good Starting Point

Aim: To investigate the antileishmanial activity of novel azole compounds against Leishmania donovani, which causes deadly visceral leishmaniasis disease. Materials & methods: A focused azole-based library was screened against both promastigotes and amastigotes forms of L. donovani strains in flat-bottomed 96-well tissue-culture plates and J774A.1 macrophage cell-line infected with L. donovani. The comprehensive screening of azole-based library against L. donovani strains provided novel hits, which can serve as a good starting point to initiate hit to lead optimization campaign. Results: Hits identified from azole-based library exhibited potent in vitro activity against promastigotes and amastigotes of L. donovani. Conclusion: These potent novel azole hits could be a good starting point to carry out for further medicinal chemistry exploration for antileishmania program.

Construction of novel in vitro epithelioid cell granuloma model from mouse macrophage cell line

2007 ◽  
Vol 299 (8) ◽  
pp. 399-403 ◽  
Author(s):  
Takeshi Yanagishita ◽  
Daisuke Watanabe ◽  
Yoichi Akita ◽  
Aki Nakano ◽  
Yuichiro Ohshima ◽  
...  
Keyword(s):  
Cell Line ◽  
Epithelioid Cell ◽  
Mouse Macrophage ◽  
Macrophage Cell Line ◽  
Macrophage Cell ◽  
Epithelioid Cell Granuloma ◽  
Mouse Macrophage Cell Line

In vitro differentiation of the murine macrophage cell line BDM-1 into osteoclast-like cells.

Endocrinology ◽  
1995 ◽  
Vol 136 (10) ◽  
pp. 4285-4292 ◽  
Author(s):  
J H Shin ◽  
A Kukita ◽  
K Ohki ◽  
T Katsuki ◽  
O Kohashi
Keyword(s):  
Cell Line ◽  
Murine Macrophage ◽  
In Vitro Differentiation ◽  
Macrophage Cell Line ◽  
Macrophage Cell ◽  
Murine Macrophage Cell Line

Identification of tyrosine 706 in the kinase insert as the major colony-stimulating factor 1 (CSF-1)-stimulated autophosphorylation site in the CSF-1 receptor in a murine macrophage cell line

1990 ◽  
Vol 10 (6) ◽  
pp. 2991-3002
Author(s):  
P van der Geer ◽  
T Hunter
Keyword(s):  
Cell Line ◽  
Murine Macrophage ◽  
Colony Stimulating Factor ◽  
Macrophage Cell Line ◽  
Macrophage Cell ◽  
Major Site ◽  
Murine Macrophage Cell Line ◽  
Stimulating Factor

The receptor for colony-stimulating factor 1 (CSF-1) is a ligand-activated protein-tyrosine kinase. It has been shown previously that the CSF-1 receptor is phosphorylated on serine in vivo and that phosphorylation on tyrosine can be induced by stimulation with CSF-1. We studied the phosphorylation of the CSF-1 receptor by using the BAC1.2F5 murine macrophage cell line, which naturally expresses CSF-1 receptors. Two-dimensional tryptic phosphopeptide mapping showed that the CSF-1 receptor is phosphorylated on several different serine residues in vivo. Stimulation with CSF-1 at 37 degrees C resulted in rapid phosphorylation on tyrosine at one major site and one or two minor sites. We identified the major site as Tyr-706. The identity of Tyr-706 was confirmed by mutagenesis. This residue is located within the kinase insert domain. There was no evidence that Tyr-973 (equivalent to Tyr-969 in the human CSF-1 receptor) was phosphorylated following CSF-1 stimulation. When cells were stimulated with CSF-1 at 4 degrees C, additional phosphotyrosine-containing phosphopeptides were detected and the level of phosphorylation of the individual phosphotyrosine-containing phosphopeptides was substantially increased. In addition, we show that CSF-1 receptors are capable of autophosphorylation at six to eight major sites in vitro.

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