O -geranylchalcones: synthesis and metabolic inhibition against Leishmania mexicana and Trypanosoma cruzi

AbstractIn this paper, twelve substitutedO-geranylchalcones were synthesized and evaluated for their leishmanicidal and trypanocidal activity. All the synthesized compounds showed selective activity againstL. mexicana strain in comparison toT. cruzi strain.O-geranyl chalcone5j substituted with ameta-NO2 group in B ring, showed the highest selectivity (IS  = 21.46). Cytotoxicity studies using murine macrophages J774.A1 showed that F and Cl substituents on thepara position on the B ring, displayed the less toxicity as in compounds5f and5i. Calculated ADME properties indicated that the obtained chalcones presented a good skin permeability, making them adequate candidates for local treatment of cutaneous leishmaniasis.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research

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by Malgorzata A. Domagalska, Hideo Imamura, Mandy Sanders, Frederik Van den Broeck, Narayan Raj Bhattarai, Manu Vanaerschot, Ilse Maes, Erika D ’Haenens, Keshav Rai, Suman Rijal, Matthew Berriman, James A. Cotton, Jean-Claude Dujardin Whole genome sequencing (WGS) is increasingly used for molecular diagnosis and epidemiology of infectious diseases. CurrentLeishmania genomic studies rely on DNA extracted from cultured parasites, which might introduce sampling and biological biases into the subsequent analyses. Up to now, direct analysis ofLeishmania genome in clinical samples is hampered by high levels of human DNA a...
Source: PLoS Neglected Tropical Diseases - Category: Tropical Medicine Authors: Source Type: research
Leishmaniosis, a disease caused by pathogenic Leishmania parasites, remains an unresolved health problem in the New World and the Old World. It is well known that lizards can be infected by a subgenus of Leishman...
Source: BMC Veterinary Research - Category: Veterinary Research Authors: Tags: Research article Source Type: research
This study assessed the potential role of the Sub-Saharan rodents Arvicanthis neumanni, A. niloticus and Mastomys natalensis as hosts of L. donovani and L. sp. from Ghana, based on experimental infections of animals and xenodiagnoses. The distribution and load of parasites were determined post mortem using qPCR from the blood, skin and viscera samples. The attractiveness of Arvicanthis and Mastomys to Phlebotomus orientalis was tested by pair-wise comparisons. None of the animals inoculated with L. donovani were infectious to P. orientalis females, although, in some animals, parasites were detected by PCR even 30 weeks pos...
Source: International Journal for Parasitology: Parasites and Wildlife - Category: Parasitology Source Type: research
Conclusion: Leishmania major is responsible for the most common CL in southern Iran. In addition, in two patients with L. major and L. tropica, mix infection with Crithidia was confirmed. The potential role of Crithidia as the main factor for CL and the probability of this parasite to have synergistic effects on Leishmania, as a hypothesis, requires more comprehensive researches on the ambiguity of this protozoon. PMID: 31803781 [PubMed]
Source: Iranian Journal of Arthropod-Borne Diseases - Category: Infectious Diseases Tags: J Arthropod Borne Dis Source Type: research
Conclusion: We reported a new point mutation of G562A in AQP1 gene involved in molecular mechanism in resistant isolates. PMID: 31803775 [PubMed]
Source: Iranian Journal of Arthropod-Borne Diseases - Category: Infectious Diseases Tags: J Arthropod Borne Dis Source Type: research
Analytical ChemistryDOI: 10.1021/acs.analchem.9b03735
Source: Analytical Chemistry - Category: Chemistry Authors: Source Type: research
Canine leishmaniosis (CanL) caused by Leishmania infantum can have several dermatological manifestations. The type of immune response elicited against the parasite appears to be at the basis for such clinical var...
Source: Parasites and Vectors - Category: Microbiology Authors: Tags: Research Source Type: research
Abstract A series of bis-naphthoquinone derivatives prepared by condensation of aryl aldehydes with lawsone was tested for anti-parasitic activities against Toxoplasma gondii and Trypanosoma brucei parasites. Monofluorophenyl derivative 1a , 3,4-difluorophenyl analog 1c and furyl compound 1l exhibited significant activity against T. gondii cells and appear to be new promising drug candidates against this parasite. The 3,4,5-trifluorophenyl derivative 1g and the isovanillyl derivative 1j displayed selective activity against Leishmania major amastigotes. PMID: 31804031 [PubMed - as supplied by publisher]
Source: Chemistry and Biodiversity - Category: Biochemistry Authors: Tags: Chem Biodivers Source Type: research
Leishmaniases are widespread neglected diseases with an incidence of 1.6 million new cases and 40 thousand deaths per year. Leishmania parasites may show distinct, species-specific patterns of virulence that lead to different clinical manifestations. It is well known that successive in vitro passages (SIVP) lead to the attenuation of virulence, but neither the metabolism nor the pathways involved in these processes are well understood. Herein, promastigotes of a virulent L. amazonensis strain recently isolated from mice was compared to SIVP derived and attenuated promastigotes, submitted to 10, 40, and 60 axenic passages a...
Source: Frontiers in cellular and infection microbiology - Category: Microbiology Source Type: research
CONCLUSIONS: These data suggest that annexin A1 is assisting macrophages in the phagocytosis process of patients with exudative cellular reaction lesion type.
Source: Revista da Sociedade Brasileira de Medicina Tropical - Category: Tropical Medicine Source Type: research
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