Abstract：
:With the aim of determining selectivity and the possible target(s) of nitroheteroaryl-1,3,4-thiadiazoles considered as possible leads for the development of anti-leishmanial agents, we studied 5-nitroimidazole, 5-nitrofuran and 5-nitrothiophene analogs of N-substituted-piperazinyl-1,3,4-thiadiazoles. We investigated 21 representative compounds 1-3(a-g) for the following properties: selectivity and efficiency against different Leishmania wild type species and intracellular parasite, toxicity against host cells and inhibition of topoisomerases I and II. Our results indicate that the nitroimidazole analogs 1a and 1f, and nitrofuran derivatives 2a, 2b, 2c, 2f, and 2g exhibited low toxicity against the host cells (IC(50)> or =80 microM), but high selectivity against intracellular amastigotes (selectivity index>12). Leishmania topoisomerases revealed impressive sensitivity to the agents (%inhibition >50 at IC(50) doses of compounds against Leishmania). Our findings showed that at least part of leishmaniacidal effect of the compounds could be attributed to disruption DNA-relaxed activities of topoisomerases I and II, and cleavable-complex formation.
journal_name
Exp Parasitoljournal_title
Experimental parasitologyauthors
Poorrajab F,Ardestani SK,Foroumadi A,Emami S,Kariminia A,Behrouzi-Fardmoghadam M,Shafiee Adoi
10.1016/j.exppara.2008.12.004subject
Has Abstractpub_date
2009-04-01 00:00:00pages
323-30issue
4eissn
0014-4894issn
1090-2449pii
S0014-4894(08)00321-4journal_volume
121pub_type
杂志文章abstract：:Five-month-old beagle dogs were experimentally infected with amastigotes of Leishmania infantum and kept for 14 months. Infection course was monitored by clinical examination, serum protein variations, and levels of specific antibodies against Leishmania estimated by indirect immunofluorescence test and Western blotti...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1006/expr.1996.0018
更新日期：1996-03-01 00:00:00
abstract：:An NADP-linked glutamate dehydrogenase (EC 1.4.1.4) was found in the soluble fraction of Trichomonas vaginalis. Its molecular weight was about 230,000 (gel filtration). The enzyme, partially purified by diafiltration and hydroxyapatite column chromatography, was heat stable (1 hr at 57 C). It catalyzed both the aminat...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/0014-4894(88)90007-0
更新日期：1988-10-01 00:00:00
abstract：:The expression and activity of topoisomerase I (PfTopoI) has been examined during the intraerythrocytic stages of the Plasmodium falciparum life cycle. The promoter is inactive during the early ring stage and becomes active only during the later trophozoite and schizont stages. The PfTOP1 transcript starts to accumula...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1006/expr.1998.4362
更新日期：1999-02-01 00:00:00
abstract：:Giardia lamblia is a protozoan pathogen with distinct cytoskeletal structures, including median bodies and eight flagella. In this study, we examined components comprising G. lamblia flagella. Crude flagellar extracts were prepared from G. lamblia trophozoites, and analyzed by two-dimensional (2-D) gel electrophoresis...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/j.exppara.2013.07.010
更新日期：2013-10-01 00:00:00
abstract：:In Trypanosoma brucei the GPI-anchored variant surface glycoprotein (VSG) represents approximately 90% of cell surface protein and a major proportion of endoplasmic reticulum (ER) biosynthetic output. We identified four trypanosomatid-specific genes encoding candidate ER-resident proteins; all were required for normal...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/j.exppara.2010.01.015
更新日期：2010-07-01 00:00:00
abstract：:We probed DNA from all trypanosomatid genera by slot blot hybridization with an oligonucleotide (SL3') complementary to a sequence of the Phytomonas spliced-leader or mini-exon RNA. The 19-nucleotide probe target site was previously shown to be highly conserved among a limited number of Phytomonas isolates, but diverg...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1006/expr.1996.0119
更新日期：1996-12-01 00:00:00
abstract：:Factors which control the expression of the refractory or susceptible condition to infection with Dirofilaria immitis in the mosquito. Aedes aegypti, were investigated using three protocols. (1) Microfilariae and prelarvae were injected into the hemocoel of susceptible A. aegypti. Some microfilariae and prelarvae deve...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/0014-4894(88)90057-4
更新日期：1988-06-01 00:00:00
abstract：:According to the World Health Organization, lymphatic filariasis (LF), a mosquito-borne neglected tropical disease (NTD), should be eliminated as a public health concern by the end of 2020. To this end, the goals of the Global Programme to Eliminate Lymphatic Filariasis (GPELF) include interrupting transmission throug...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/j.exppara.2020.107918
更新日期：2020-08-01 00:00:00
abstract：:Previous results from our laboratory using pharmacological approaches suggested a role for nitric oxide (NO) in the host defense against the human filarial parasite, Brugia malayi. We sought to determine whether a complementary genetic approach, using mice homozygous for a targeted mutation in the gene encoding induci...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1006/expr.2001.4611
更新日期：2001-05-01 00:00:00
abstract：:Previous studies showed that Echinococcus granulosus infection reduces allergic airway inflammation in experimentally infected hosts and the cystic fluid of E. granulosus is known to activate regulatory T (CD4+CD25+Foxp3+T, Treg) cells. To evaluate the effects of cystic fluid of E. granulosus on allergic airway inflam...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/j.exppara.2019.02.003
更新日期：2019-03-01 00:00:00
abstract：:Isospora suis is an intestinal protozoan parasite in pigs. The 2-3 weeks old piglets are most often infected by I. suis because their immune system is not fully developed. The infection exhibits clinical features such as diarrhea and dehydration and seriously affects the economic interests of farmers. The traditional ...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/j.exppara.2016.03.001
更新日期：2016-06-01 00:00:00
abstract：:Entamoeba histolytica infection is associated with considerable morbidity and mortality in the form of intestinal and extraintestinal amoebiasis. No vaccine is yet available for amoebiasis. Heparan Sulphate Binding Proteins (HSBPs) from E. histolytica were evaluated for immunogenicity and protective efficacy in a Guin...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/j.exppara.2013.08.011
更新日期：2013-11-01 00:00:00
abstract：:Transforming growth factor-β (TGF-β) signaling pathway is documented to participate in liver fibrosis via multifactorial mechanisms. microRNA Let-7b (Let-7b) has been proved to alleviate cell fibrosis through regulating TGF-β receptor I (TβRI), but whether it is involved in Schistosomiasis liver fibrosis (SLF) has not...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/j.exppara.2017.09.024
更新日期：2017-11-01 00:00:00
abstract：:In this paper, the lytic activity of two variants of Serratia marcescens against promastigotes of Leishmania braziliensis was studied. In vitro assays showed that S. marcescens variant SM365 lyses L. braziliensis promastigotes, while the variant DB11 did not. Scanning electron microscopy (SEM) revealed that S. marcesc...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/j.exppara.2009.03.004
更新日期：2009-06-01 00:00:00
abstract：:Two different diets for the host and three drug dosage regimens were used to select lines resistant to sulfadoxine and pyrimethamine from the parent strain of the rodent malaria parasite Plasmodium berghei [the N (K173) strain]. A higher yield of resistance was obtained when a high parasitemia was present at the begin...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/0014-4894(83)90034-6
更新日期：1983-06-01 00:00:00
abstract：:Using nucleotide variation in the first internal transcribed spacer of nuclear ribosomal DNA, five different genotypes (designated G1-G5) have been identified and the preponderance of genotype G1 in humans and of genotype G3 in pigs led to the proposal that parasites bearing the two genotypes have an affinity for a pa...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/j.exppara.2012.03.006
更新日期：2012-05-01 00:00:00
abstract：:Infectivity of the multicellular pathogen Schistosoma mansoni for the human host is dependent upon the ability of free-living cercariae to transform rapidly into parasitic schistosomula. The biochemical pathways that regulate this transitional period are unknown. The role of protein phosphorylation was investigated by...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/0014-4894(91)90024-q
更新日期：1991-08-01 00:00:00
abstract：:The risk of human hookworm infections from land application of wastewater matrices could be high in regions with high hookworm prevalence. A rapid, sensitive and specific hookworm detection method from wastewater matrices is required in order to assess human health risks. Currently available methods used to identify h...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/j.exppara.2015.08.009
更新日期：2015-12-01 00:00:00
abstract：:Strongyloidiasis is a parasitosis that represents a public health problem, in tropical regions. The present study aimed to investigate the anthelmintic effects of several extracts of Argemone mexicana, as well as its main component berberine (Ber) against the third-stage larvae (L3) of Strongyloides venezuelensis in-v...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/j.exppara.2020.108043
更新日期：2021-01-01 00:00:00
abstract：:Amphotericin B (Amp) has been well-successfully used to treat against Leishmania infection, although high toxicity has been found in patients. In the present study, Amp was administered in Leishmania infantum-infected BALB/c mice by three distinct delivery systems aiming to compare their efficacy against challenge inf...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/j.exppara.2018.02.003
更新日期：2018-03-01 00:00:00
abstract：:Mitochondria from a rodent malarial parasite (Plasmodium berghei) were successfully purified by differential centrifugation and 22% Percoll density gradient separation. The purified mitochondria from the erythrocytic stages of the parasite had a density of 1.05 and were found to be heterogeneous by transmission electr...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1006/expr.1993.1070
更新日期：1993-09-01 00:00:00
abstract：:Murine malarial parasites have long been characterized by their requirement for either antibody-mediated immunity (AMI) or cell-mediated immunity (CMI) for suppression of acute parasitemia, with Plasmodium yoelii reportedly requiring AMI for suppression and P. chabaudi requiring CMI. To assess this characterization in...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1006/expr.1996.4132
更新日期：1997-02-01 00:00:00
abstract：:Isocitrate lyase (EC 4.1.3.1) from mixed larval populations of Caenorhabditis elegans was stabilized in crude extracts by centrifugation over a 0.2-0.6 M sucrose gradient for 2.5 hr in a vertical rotor (VTi 50) at 210,000g. The peak fractions from this sucrose gradient showed a half-life of 33 hr at 30 C and 225 hr at...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/0014-4894(85)90089-x
更新日期：1985-06-01 00:00:00
abstract：:A cell-free culture system for Cryptosporidium parvum was analysed using scanning electron microscopy (SEM) to characterise life cycle stages and compare gene expression in cell-free culture and cell culture using HCT-8 cells. Cryptosporidium parvum samples were harvested at 2 h, 8 h, 14 h, 26 h, 50 h, 74 h, 98 h, 122...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/j.exppara.2015.03.002
更新日期：2015-06-01 00:00:00
abstract：:A murine model system was developed to study the induction and mechanism of protective immunity to L3 of Strongyloides stercoralis. L3 were implanted in BALB/cByJ mice in diffusion chambers constructed with 0.1- or 2.0-microns-pore-size membranes. Parasites survived equally well regardless or membrane type for 7 days,...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1006/expr.1995.1036
更新日期：1995-03-01 00:00:00
abstract：:Non-invasive small animal in vivo imaging is an essential tool in a broad variety of biomedical sciences and enables continuous monitoring of disease progression in order to develop and improve diagnostic, therapeutic and preventive measures. Imaging parasites non-invasively in live animals allows efficient parasite d...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/j.exppara.2020.107905
更新日期：2020-07-01 00:00:00
abstract：:Many methods have been proposed for removing contaminating host cells from mouse peritoneal exudates infected with Toxoplasma gondii tachyzoites. Of these, eight established methods were compared. They were density gradients, sonication and trypsin digestion, differential centrifugation, haemolysin digestion, filtrati...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/0014-4894(84)90080-8
更新日期：1984-04-01 00:00:00
abstract：:Plasma butyrylcholinesterase (BChE) hydrolyzes ester-containing compounds such as succinylcholine, as well as acting as a scavenger against neurotoxic organophosphates (OPs). We previously found that Nippostrongylus brasiliensis infection makes rats more susceptible to OP toxicity by decreasing serum paraoxonase-1 (PO...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/j.exppara.2009.02.009
更新日期：2009-06-01 00:00:00
abstract：:In 1912 Blastocystis hominis was identified as a new species and classified as a yeast (Brumpt 1912). In the early 1920s several groups confirmed its classification as a yeast, specifically a member of the genus Schizosaccharomyces (discussed by Zierdt et al. 1967). Apart from an occasional case report, the classifica...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/0014-4894(89)90110-0
更新日期：1989-04-01 00:00:00
abstract：:Living Leishmania amazonensis amastigotes were incubated with radioiodinated N-benzyloxycarbonyl-L-tyrosyl-L-alanyl diazomethane (Z-Tyr-AlaCHN2), an irreversible inhibitor of mammalian cathepsins B and L. Parasite lysates were subjected to electrophoresis in gelatin-containing sodium dodecyl sulfate-acrylamide gels to...
journal_title：Experimental parasitology
pub_type： 杂志文章
doi：10.1016/0014-4894(91)90066-6
更新日期：1991-11-01 00:00:00
