The in vitro leishmanicidal effect of (3S)-16,17-didehydrofalcarinol (1) isolated from Tridax procumbens whole plant against Leishmania mexicana, the causative agent of cutaneous leishmaniasis (chiclero's ulcer) in the New World, was investigated. This oxylipin showed significant in vitro activity against promastigotes and intracellular amastigotes of L. mexicana. Its inhibitory effect on amastigotes was not due to activation of NO in recombinant gamma-interferon-stimulated macrophages, since the production of NO was decreased in presence of the oxylipin. This is the first report on the leishmanicidal activity against the intracellular stage (amastigote) of the oxylipin (3S)-16,17-didehydrofalcarinol.
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http://dx.doi.org/10.1002/ptr.3052 | DOI Listing |
Mol Biochem Parasitol
January 2025
Post-graduate Program in Pharmaceutical Sciences, Federal University of Ceará, Fortaleza - CE, Brazil; Fundação Oswaldo Cruz, Fiocruz, Fiocruz Ceará, Eusébio - CE, Brazil; Northeast Network of Biotechnology (RENORBIO), State University of Ceará (UECE), Fortaleza - CE, Brazil.
Globally, an estimated 1 billion people reside in endemic areas, and over 12 million individuals are infected with leishmaniasis. Despite its prevalence, leishmaniasis continues to be a neglected disease, mainly affecting underdeveloped countries. In Brazil, the available treatments are pentavalent antimonials and Amphotericin B, which are outdated, toxic, require prolonged parenteral administration and have limited efficacy.
View Article and Find Full Text PDFExp Parasitol
January 2025
Grupo de Química Orgánica de Productos Naturales, Instituto de Química, Universidad de Antioquia-UdeA. Calle 70 # 52-21, Medellín, Colombia. Electronic address:
Cutaneous Leishmaniasis and Chagas disease are neglected tropical diseases that affect millions worldwide. Despite the high morbidity associated with these infections, current treatments are often highly toxic and are showing diminishing efficacy. Thus, new therapeutic options are urgently needed.
View Article and Find Full Text PDFMolecules
January 2025
Department of Biochemistry and Organic Chemistry, Institute of Chemistry, São Paulo State University (UNESP), Araraquara 14800-060, SP, Brazil.
Leishmaniasis is a neglected tropical disease caused by a protozoan of the genus Leishmania, which has visceral and cutaneous forms. The symptoms of leishmaniasis include high fever and weakness, and the cutaneous infection also causes lesions under the skin. The drugs used to treat leishmaniasis have become less effective due to the resistance mechanisms of the protozoa.
View Article and Find Full Text PDFBiomedicines
January 2025
Department of Biotechnology, Abdul Wali Khan University Mardan, Mardan 23200, Pakistan.
Thiadiazine thione (THTT) has gained significant interest owing to its pharmacological potentials, particularly its antiparasitic and anti-inflammatory properties. Leishmaniasis is a clinical syndrome caused by infection with species and is associated with an inflammatory response and nociception. The available treatments against leishmaniasis are inadequate, as they are associated with high cost, toxicity, and increased resistance.
View Article and Find Full Text PDFMar Drugs
December 2024
Faculty of Pharmaceutical Sciences, Tokyo University of Science, Noda, Chiba 278-8510, Japan.
Leishmaniasis is a major public health problem, especially affecting vulnerable populations in tropical and subtropical regions. The disease is endemic in 90 countries, and with millions of people at risk, it is seen as one of the ten most neglected tropical diseases. Current treatments face challenges such as high toxicity, side effects, cost, and growing drug resistance.
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