Urechites andrieuxii Muell.-Arg. (Apocynaceae) is widely used in the Yucatan Peninsula for the treatment of cutaneous leishmaniasis. The influence of the environment in the variability of the leishmanicidal activity of the plant was evaluated using crude methanol extracts of roots from individuals belonging to four natural populations growing in the Yucatan Peninsula. The results of the growth inhibition test using three Leishmania spp. promastigotes showed a stronger leishmanicidal activity in populations of U. andrieuxii growing in more humid environments. Further evaluation against four human cancer cell lines and in the brine shrimp bioassay of both extracts from various parts of the plant and from the most active methanol root extracts, suggested that while the leaf extract appears to have selective toxicity against Leishmania parasites, the strong leishmanicidal activity detected in the root extracts of the plant might be due to its cytotoxicity.
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http://dx.doi.org/10.1016/s0378-8741(03)00011-4 | DOI Listing |
Bioorg Chem
December 2024
Universidad de Buenos Aires, CONICET, Cátedra de Química Orgánica II, Departamento de Ciencias Químicas, Facultad de Farmacia y Bioquímica, Junín 956, 1113 Buenos Aires, Argentina. Electronic address:
This work describes the synthesis and biological evaluation of hitherto unknown N-arylspermidine derivatives 3. Compounds 3 were efficiently prepared from cyclic amidines through a novel synthetic approach comprising alkylation with ω-halonitriles followed by reduction. The cyclic N-arylamidine directs the alkylation to the unsubstituted nitrogen and also provides the N-benzyl group present in the triamine after simultaneous reduction of the resulting quaternary salt 2 and the cyano group.
View Article and Find Full Text PDFArch Biochem Biophys
December 2024
Department of Biochemistry and Immunology, Ribeirão Preto Medical School, University of São Paulo, Ribeirão Preto, Brazil. Electronic address:
UBC13 is an orthologue of Homo sapiens ubiquitin-conjugation E2 enzymes described in Leishmania mexicana, a null mutant lacking this gene cannot be produced, suggesting essential functions in this parasite. Leishmania infantum is an etiological agent of visceral leishmaniasis, the most severe type of disease that is potentially fatal if untreated. The ubiquitination process has been targeted for leishmanicidal compounds, indicating its essential function in parasite homeostasis.
View Article and Find Full Text PDFInt J Biol Macromol
December 2024
Department of Animal Morphology and Physiology, Federal Rural University of Pernambuco - UFRPE, Dom Manoel de Medeiros Avenue, 52171-900 Recife, PE, Brazil. Electronic address:
New leishmanicidal products are needed for the treatment to be effective, since current drugs are toxic to healthy human/animal cells and have low efficacy against the parasite. Bioactive compounds from microalgae, such as lectins, can be explored as new anti-Leishmania candidates. This study aimed to evaluate the cytotoxic and anti-Leishmania action of the cell extract (CE) and lectin (CVU) from Chlorella vulgaris biomass.
View Article and Find Full Text PDFJ Nat Prod
December 2024
Instituto de Biologia, Universidade Estadual de Campinas, Campinas 13083-862, SP, Brazil.
Leishmaniasis is a worldwide disease caused by more than 20 species of parasites. and are among the main causative agents of cutaneous leishmaniasis, presenting a broad spectrum of clinical forms. As these pathologies lead to unsatisfactory treatment outcomes, the discovery of alternative chemotherapeutic options is urgently required.
View Article and Find Full Text PDFJ Asian Nat Prod Res
November 2024
Laboratory of Cell and Molecular Biology, Department of Botany, Centre of Advanced Study, University of Calcutta, Kolkata, India.
Visceral leishmaniasis still remains a leading cause of parasitic deaths, with modern pentavalent antimonials showing limited efficacy and health risks. The methanolic bark extract of the Northeastern Indian plant, , demonstrated potent leishmanicidal effects against the parasite , demonstrating IC values of 20-36 µg/ml, with selective toxicity for parasites over healthy cells. It induced parasite death through elevated oxidative and nitrosative stress elements, reduced arginase activity, nuclear fragmentation, cell cycle arrest, and apoptosis.
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