Resveratrol analogues present effective antileishmanial activity against promastigotes and amastigotes from distinct Leishmania species by multitarget action in the parasites

AbstractObjectivesThein vitro antileishmanial effect of analogues of resveratrol (AR) present in the N ‐aryl imines and N‐aryl hydrazones series was investigated. In addition, possible parasite targets were evaluated.MethodsAntipromastigote activity ofLeishmania amazonensis,L. braziliensis andL. infantum, as well as the cytotoxicity on macrophages was determined by MTT assay andL.  braziliensis‐infected macrophages effect by Giemsa stain. After staining, effects on the parasite targets were analysed by flow cytometry or by fluorescence microscopy.Key ‐findingsAmong the tested compounds, the derivativeAR26 showed the best effect against promastigotes of allLeishmania species (IC50 
Source: Journal of Pharmacy and Pharmacology - Category: Drugs & Pharmacology Authors: Tags: Research Paper Source Type: research

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Abstract Sri Lanka reports a large epidemic of cutaneous leishmaniasis (CL) caused by an atypical L. donovani while regional leishmaniasis elimination drive aims at achieving its targets in 2020. Visceralization, mucotrophism, and CL associated poor treatment response were recently reported. Long-term clinico-epidemiological trends (2001-2013) in this focus were examined for the first time. Both constant and changing features were observed. Sociodemographic patient characteristics that differ significantly from those of country profile, microchanges within CL profile, spatial expansion, constant biannual seasonal ...
Source: Biomed Res - Category: Research Authors: Tags: Biomed Res Int Source Type: research
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Source: Prostaglandins and Other Lipid Mediators - Category: Lipidology Source Type: research
Authors: Çulha G, Kaya T, Gülbol Duran G, Urhan Küçük M, Doğramacı AÇ, Tiyekli Çelik D Abstract Leishmaniasis is a parasitic disease that is transmitted to humans by the bites of infected female phlebotomine sandflies. In the diagnosis of cutaneous leishmaniasis (CL), in the smear samples, the demonstration of the parasite by microscope remains a gold standard method. However, it becomes difficult to diagnose the parasite since the number of amastigotes in chronic cases with a lesion of one year or longer is very low. Due to many factor such as patients primarily do not ...
Source: Mikrobiyoloji Bulteni - Category: Microbiology Tags: Mikrobiyol Bul Source Type: research
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Source: Veterinary Parasitology - Category: Veterinary Research Source Type: research
by Megan A. Sloan, Karen Brooks, Thomas D. Otto, Mandy J. Sanders, James A. Cotton, Petros Ligoxygakis Trypanosomatid parasites are causative agents of important human and animal diseases such as sleeping sickness and leishmaniasis. Most trypanosomatids are transmitted to their mammalian hosts by insects, often belonging to Diptera (or true flies). These are called dixenous trypanosomatids since th ey infect two different hosts, in contrast to those that infect just insects (monoxenous). However, it is still unclear whether dixenous and monoxenous trypanosomatids interact similarly with their insect host, as fly-monoxenou...
Source: PLoS Genetics - Category: Genetics & Stem Cells Authors: Source Type: research
Abstract Folates are essential biomolecules required to carry out many crucial processes in leishmania parasite. Dihydrofolate reductase-thymidylate synthase (DHFR-TS) and pteridine reductase 1 (PTR1) involved in folate biosynthesis in leishmania have been established as suitable targets for development of chemotherapy against leishmaniasis. In the present study, various computational tools such as homology modelling, pharmacophore modelling, docking, molecular dynamics and molecular mechanics have been employed to design dual DHFR-TS and PTR1 inhibitors. Two designed molecules, i.e. 2-(4-((4-nitrobenzyl)oxy)pheny...
Source: SAR and QSAR in Environmental Research - Category: Environmental Health Authors: Tags: SAR QSAR Environ Res Source Type: research
The main clinical forms of leishmaniasis in Bangladesh are visceral leishmaniasis and post-kala-azar dermal leishmaniasis, which are caused by Leishmania donovani. Imported cutaneous leishmaniasis (CL) is emergin...
Source: Parasites and Vectors - Category: Microbiology Authors: Tags: Short report Source Type: research
by Chukwunonso O. Nzelu, Hirotomo Kato, Nathan C. Peters Leishmaniasis, caused by protozoan parasites of theLeishmania genus, represents an important health problem in many regions of the world. Lack of effective point-of-care (POC) diagnostic tests applicable in resources-limited endemic areas is a critical barrier to effective treatment and control of leishmaniasis. The development of the loop-mediated isothermal amplification (LAMP) assay has provided a new tool towards the development of a POC diagnostic test based on the amplification of pathogen DNA. LAMP does not require a thermocycler, is relatively inexpensive, a...
Source: PLoS Neglected Tropical Diseases - Category: Tropical Medicine Authors: Source Type: research
h B Abstract Protozoal infections are still a global health problem, threatening the lives of millions of people around the world, mainly in impoverished tropical and sub-tropical regions. Thus, in view of the lack of efficient therapies and increasing resistances against existing drugs, this study describes the antiprotozoal potential of synthetic cinnamate ester analogs and their structure-activity relationships. In general, Leishmania donovani and Trypanosoma brucei were quite susceptible to the compounds in a structure-dependent manner. Detailed analysis revealed a key role of the substitution pattern on the a...
Source: ChemMedChem - Category: Chemistry Authors: Tags: ChemMedChem Source Type: research
In this study, we evaluated cellular and humoral immune responses induced by our newly designed multi-epitope vaccine in BALB/c mice. Four antigenic proteins, including histone H1, sterol 24-c-methyltransferase (SMT),Leishmania-specific hypothetical protein (LiHy), andLeishmania-specific antigenic protein (LSAP) were chosen for the prediction of potential immunodominant epitopes. Moreover, to enhance vaccine immunogenicity, two toll-like receptors 4  (TLR4) agonists, resuscitation-promoting factors ofMycobacterium tuberculosis (RpfE and RpfB), were employed as the built-in adjuvants. Immunization with the designed mul...
Source: Medical Microbiology and Immunology - Category: Microbiology Source Type: research
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