Publications
| Title | Abstract | Year Filter | PMID(sorted ascending) Filter |
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| improved anticancer and antiparasitic activity of new lawsone mannich bases. | substituted lawsone mannich bases 2a-e, 3a-e and 4a-e were prepared and tested for their biological activities. the new fatty alkyl substituted compounds 2a-c exhibited strong and selective growth inhibitory activities in the low one-digit micromolar and sub-micromolar range against a panel of human cancer cell lines associated with ros formation. in addition, compounds 2a-c revealed sub-micromolar anti-trypanosomal activities against parasitic trypanosoma brucei brucei cells via deformation of ... | 2017 | 27912173 |
| how do the alkaloids emetine and homoharringtonine kill trypanosomes? an insight into their molecular modes of action. | although trypanosoma brucei causes deadly sleeping sickness, the number of the registered medications is rather limited. some plant alkaloids are potent trypanocidal agents. | 2016 | 27912879 |
| immunomodulatory activity of buchholzia coriacea seed methanol extract on trypanosoma brucei brucei infected mice. | the seeds of buchholzia coriacea engler (capparaceae) are used in eastern nigeria to treat feverish conditions, and to treat malaria and sleeping sickness that cause fever. | 2017 | 27951754 |
| trypanosoma brucei invasion and t-cell infiltration of the brain parenchyma in experimental sleeping sickness: timing and correlation with functional changes. | the timing of trypanosoma brucei entry into the brain parenchyma to initiate the second, meningoencephalitic stage of human african trypanosomiasis or sleeping sickness is currently debated and even parasite invasion of the neuropil has been recently questioned. furthermore, the relationship between neurological features and disease stage are unclear, despite the important diagnostic and therapeutic implications. | 2016 | 28002454 |
| trypanosoma brucei brucei traverses different biological barriers differently and may modify the host plasma membrane in the process. | trypanosoma brucei are extracellular hemoflagellate protozoan parasites and one of the causative agents of a devastating zoonotic disease called african trypanosomiasis. in humans, the disease is caused by trypanosoma brucei rhodensiense and trypanosoma brucei gambiense, which cross the blood brain barrier (bbb) causing neurological disorders which culminate in death if untreated. in some domestic animals and laboratory rodents, trypanosoma brucei brucei causes a disease similar to that in human ... | 2017 | 28011167 |
| igm, lgg and il-6 profiles in the trypanosoma brucei brucei monkey model of human african trypanosomiasis. | human african trypanosomiasis (hat) patients manifest immunological profiles, whose variations over time can be used to indicate disease progression. however, monitoring of these biomarkers in human patients is beset by several limitations which can be offset by using chronic animal models. a recent improved monkey model of hat using a trypanosoma brucei brucei isolate has been developed but the immunological profile has not been elucidated. the objectives of the current study was to determine t ... | 2017 | 28099874 |
| conjugates of 2,4-dihydroxybenzoate and salicylhydroxamate and lipocations display potent antiparasite effects by efficiently targeting the trypanosoma brucei and trypanosoma congolense mitochondrion. | we investigated a chemical strategy to boost the trypanocidal activity of 2,4-dihydroxybenzoic acid (2,4-dhba)- and salicylhydroxamic acid (sham)-based trypanocides with triphenylphosphonium and quinolinium lipophilic cations (lc). three series of lc conjugates were synthesized that were active in the submicromolar (5a-d and 10d-f) to low nanomolar (6a-f) range against wild-type and multidrug resistant strains of african trypanosomes (trypanosoma brucei brucei and t. congolense). this represente ... | 2017 | 28112515 |
| proline metabolism is essential for trypanosoma brucei brucei survival in the tsetse vector. | adaptation to different nutritional environments is essential for life cycle completion by all trypanosoma brucei sub-species. in the tsetse fly vector, l-proline is among the most abundant amino acids and is mainly used by the fly for lactation and to fuel flight muscle. the procyclic (insect) stage of t. b. brucei uses l-proline as its main carbon source, relying on an efficient catabolic pathway to convert it to glutamate, and then to succinate, acetate and alanine as the main secreted end pr ... | 2017 | 28114403 |
| genetic and structural study of dna-directed rna polymerase ii of trypanosoma brucei, towards the designing of novel antiparasitic agents. | trypanosoma brucei brucei (tbb) belongs to the unicellular parasitic protozoa organisms, specifically to the trypanosoma genus of the trypanosomatidae class. a variety of different vertebrate species can be infected by tbb, including humans and animals. under particular conditions, the tbb can be hosted by wild and domestic animals; therefore, an important reservoir of infection always remains available to transmit through tsetse flies. although the tbb parasite is one of the leading causes of d ... | 2017 | 28265521 |
| synthesis and biological evaluation of selective tubulin inhibitors as anti-trypanosomal agents. | african trypanosomiasis is still a threat to human health due to the severe side-effects of current drugs. we identified selective tubulin inhibitors that showed the promise to the treatment of this disease, which was based on the tubulin protein structural difference between mammalian and trypanosome cells. further lead optimization was performed in the current study to improve the efficiency of the drug candidates. we used trypanosoma brucei brucei cells as the parasite model, and human normal ... | 2017 | 28428042 |
| genome-wide snp analysis reveals distinct origins of trypanosoma evansi and trypanosoma equiperdum. | trypanosomes cause a variety of diseases in man and domestic animals in africa, latin america and asia. in the trypanozoon subgenus, trypanosoma brucei gambiense and t. b. rhodesiense cause human african trypanosomiasis, while t. b. brucei, t. evansi and t. equiperdum are responsible for nagana, surra and dourine in domestic animals, respectively. the genetic relationships between t. evansi and t. equiperdum and other trypanozoon species remain unclear because the majority of phylogenetic analys ... | 2017 | 28541535 |
| expression, purification, and crystallization of type 1 isocitrate dehydrogenase from trypanosoma brucei brucei. | isocitrate dehydrogenases (idhs) are metabolic enzymes that catalyze the oxidative decarboxylation of isocitrate to α-ketoglutarate. depending on the electron acceptor and subcellular localization, these enzymes are classified as nadp(+)-dependent idh1 in the cytosol or peroxisomes, nadp(+)-dependent idh2 and nad(+)-dependent idh3 in mitochondria. trypanosoma brucei is a protozoan parasite that causes african sleeping sickness in humans and nagana disease in animals. here, for the first time, a ... | 2017 | 28642005 |
| oral administration of azithromycin ameliorates trypanosomosis in trypanosoma congolense-infected mice. | animal trypanosomosis is a devastating parasitic disease that is of economic importance to livestock production. the infection includes animal african trypanosomosis, surra, and dourine. the treatment is based solely on few compounds that were discovered decades ago and which are associated with severe toxicity. furthermore, it is likely that the parasite has developed resistance towards them. thus, there is an urgent need for new, accessible, and less toxic drugs. azithromycin is an antibiotic ... | 2017 | 28674747 |
| development of novel peptide-based michael acceptors targeting rhodesain and falcipain-2 for the treatment of neglected tropical diseases (ntds). | this paper describes the development of a class of peptide-based inhibitors as novel antitrypanosomal and antimalarial agents. the inhibitors are based on a characteristic peptide sequence for the inhibition of the cysteine proteases rhodesain of trypanosoma brucei rhodesiense and falcipain-2 of plasmodium falciparum. we exploited the reactivity of novel unsaturated electrophilic functions such as vinyl-sulfones, -ketones, -esters, and -nitriles. the michael acceptors inhibited both rhodesain an ... | 2017 | 28763614 |
| expression of interferon-inducible chemokines and sleep/wake changes during early encephalitis in experimental african trypanosomiasis. | human african trypanosomiasis or sleeping sickness, caused by the parasite trypanosoma brucei, leads to neuroinflammation and characteristic sleep/wake alterations. the relationship between the onset of these alterations and the development of neuroinflammation is of high translational relevance, but remains unclear. this study investigates the expression of interferon (ifn)-γ and ifn-inducible chemokine genes in the brain, and the levels of cxcl10 in the serum and cerebrospinal fluid prior to a ... | 2017 | 28821016 |
| trypanosoma infection favors brucella elimination via il-12/ifnγ-dependent pathways. | this study develops an original co-infection model in mice using brucella melitensis, the most frequent cause of human brucellosis, and trypanosoma brucei, the agent of african trypanosomiasis. although the immunosuppressive effects of t. brucei in natural hosts and mice models are well established, we observed that the injection of t. brucei in mice chronically infected with b. melitensis induces a drastic reduction in the number of b. melitensis in the spleen, the main reservoir of the infecti ... | 2017 | 28824630 |
| rodent-free cyclical transmission of trypanosoma brucei brucei. | we provide a simple protocol enabling cyclical transmission of trypanosoma brucei brucei to be performed without the need for mammals. these procedures have two advantages: they are in line with 3r principles of animal use - replace, refine, reduce - and may enable more laboratories to study the complete life cycle. | 2017 | 28843782 |
| apols with low ph dependence can kill all african trypanosomes. | the primate-specific serum protein apolipoprotein l1 (apol1) is the only secreted member of a family of cell death promoting proteins 1-4 . apol1 kills the bloodstream parasite trypanosoma brucei brucei, but not the human sleeping sickness agents t.b. rhodesiense and t.b. gambiense 3 . we considered the possibility that intracellular members of the apol1 family, against which extracellular trypanosomes could not have evolved resistance, could kill pathogenic t. brucei subspecies. here we show th ... | 2017 | 28924146 |
| screening a natural product-based library against kinetoplastid parasites. | kinetoplastid parasites cause vector-borne parasitic diseases including leishmaniasis, human african trypanosomiasis (hat) and chagas disease. these neglected tropical diseases (ntds) impact on some of the world's lowest socioeconomic communities. current treatments for these diseases cause severe toxicity and have limited efficacy, highlighting the need to identify new treatments. in this study, the davis open access natural product-based library was screened against kinetoplastids (leishmania ... | 2017 | 29023425 |
| biological and phytochemical investigations on caesalpinia benthamiana, a plant traditionally used as antimalarial in guinea. | caesalpinia benthamiana is widely used as antimalarial in guinean traditional medicine. leaf extracts of the plant were tested for their in vitro antiprotozoal activity against trypanosoma brucei brucei and t. cruzi and the chloroquine-sensitive ghana strain of plasmodium falciparum along with their cytotoxicity on mrc-5 cells. the methanolic extract showed the strongest antiprotozoal activity against p. falciparum (ic50 4 μg/ml), a good activity against t. brucei (ic50 13 μg/ml), and a moderate ... | 2017 | 29081823 |
| improving anti-trypanosomal activity of alkamides isolated from achillea fragrantissima. | in previous studies the aerial parts of achillea fragrantissima were found to have substantial antileishmanial and antitrypanosomal activity. a bioassay-guided fractionation of a dichloromethane extract yielded the isolation of the essential anti-trypanosomal compounds of the plant. seven sesquiterpene lactones (including achillolide-a), two flavonoids, chrysosplenol-d and chrysosplenetine, and four alkamides (including pellitorine) were identified. this is the first report for the isolation of ... | 2017 | 29108932 |
| apol1 nephrotoxicity: what does ion transport have to do with it? | apolipoprotein l1 (apol1) protein is the human serum factor that protect human beings against trypanosoma brucei brucei, the cause of trypanosomiasis. subspecies of t b brucei that cause human sleeping sickness-t b gambiense and t b rhodesiense evolved molecular mechanisms that enabled them to evade killing by apol1. sequence changes (termed g1 and g2) in the apol1 gene that restored its ability to kill t b rhodesiense also increase the risk of developing glomerular diseases and accelerate progr ... | 2017 | 29110762 |
| intracellular diminazene aceturate content and adenosine incorporation in diminazene aceturate-resistant babesia gibsoni isolate in vitro. | the mechanism of the development of diminazene aceturate (da) resistance in babesia gibsoni is still unknown even though da-resistant b. gibsoni isolate was previously developed in vitro. to clarify the mechanisms of da-resistance in b. gibsoni, we initially examined the intracellular da content in the da-resistant isolate using high-performance liquid chromatography, and compared it with that in the wild-type. as a result, the intracellular da content in the da-resistant isolate was significant ... | 2017 | 29122576 |
| antimicrobial and antiparasitic activities of three algae from the northwest coast of algeria. | the objective of this study was to investigate the biological activities of algerian algae, sargassum vulgare, cladostephus hirsutus and rissoella verruculosa. antimicrobial activity of the crude extracts and their fractions was assessed using the disc diffusion assay, the minimum inhibitory concentration and the minimum bactericidal concentration. antiparasitic activity was studied in vitro against the blood stream forms of trypanosoma brucei brucei and the intraerythrocytic stages of plasmodiu ... | 2017 | 29166772 |
| tsetse fly (glossina pallidipes) midgut responses to trypanosoma brucei challenge. | tsetse flies (glossina spp.) are the prominent vector of african trypanosome parasites (trypanosoma spp.) in sub-saharan africa, and glossina pallidipes is the most widely distributed species in kenya. this species displays strong resistance to infection by parasites, which are typically eliminated in the midgut shortly after acquisition from the mammalian host. although extensive molecular information on immunity for the related species glossina morsitans morsitans exists, similar information i ... | 2017 | 29258576 |
| design, synthesis, and antiprotozoal evaluation of new 2,9-bis[(substituted-aminomethyl)phenyl]-1,10-phenanthroline derivatives. | a series of new 2,9-bis[(substituted-aminomethyl)phenyl]-1,10-phenanthroline derivatives was synthesized, and the compounds were screened in vitro against three protozoan parasites (plasmodium falciparum, leishmania donovani, and trypanosoma brucei brucei). biological results showed antiparasitic activity with ic50 values in the μm range. the in vitro cytotoxicity of these molecules was assessed by incubation with human hepg2 cells; for some derivatives, cytotoxicity was observed at significantl ... | 2017 | 29266861 |
| a new chimeric triple reporter fusion protein as a tool for in vitro and in vivo multimodal imaging to monitor the development of african trypanosomes and leishmania parasites. | trypanosomiases and leishmaniases, caused by a group of related protist parasites, are neglected tropical diseases currently threatening >500 million people worldwide. reporter proteins have revolutionised the research on infectious diseases and have opened up new advances in the understanding of trypanosomatid-borne diseases in terms of both biology, pathogenesis and drug development. here, we describe the generation and some applications of a new chimeric triple reporter fusion protein combini ... | 2018 | 29339220 |