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Leishmaniasis is a group of infectious diseases transmitted to humans during vector bites and caused by protozoans of the genus . Conventional therapies face challenges due to their serious side effects, prompting research into new anti-leishmania agents. In this context, we investigated the effectiveness of morolic acid, a pentacyclic triterpene, on promastigotes and amastigotes. The present study employed the MTT assay, cytokine analysis using optEIATM kits, an HDCFDA test, and nitric oxide dosage involving nitrite production and Griess reagent. Morolic acid inhibited promastigote and axenic amastigote growth forms at IC values of 1.13 µM and 2.74 µM, respectively. For cytotoxicity to macrophages and VERO cells, morolic acid obtained respective CC values of 68.61 µM and 82.94 µM. The compound causes damage to the parasite membrane, leading to cellular leakage. In the infection assay, there was a decrease in parasite load, resulting in a CI of 2.56 µM. This effect was associated with immunomodulatory activity, altering macrophage structural and cellular parasite elimination mechanisms. Morolic acid proved to be an effective and selective natural compound, making it a strong candidate for future in vivo studies in cutaneous leishmaniasis.
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11279160 | PMC |
http://dx.doi.org/10.3390/microorganisms12071392 | DOI Listing |
RSC Med Chem
October 2024
Institute of Experimental Botany of the Czech Academy of Sciences, Isotope Laboratory Vídeňská 1083 14220 Prague 4 Czech Republic
A series of amides of selected plant triterpenoids, moronic acid and morolic acid, with the tripeptides MAG and GAM, was designed and synthesized. Two required tripeptides 5 and 10 were synthesized by a step-wise chain elongation of the ethyl esters of either glycine or l-methionine at their N-terminus using Boc-protected amino acids in each step. The tripeptides 5 and 10 were used for the synthesis of 13-23, the derivatives of moronic acid (11) and morolic acid (12), to get a series of amide derivatives of the less frequently studied triterpenoids 11 and 12.
View Article and Find Full Text PDFChemMedChem
October 2024
Programa de Pós-Graduação de Produtos Naturais e Sintéticos Bioativos, Universidade federal da Paraíba, 58051-900, João Pessoa - PB, Brazil.
Leishmaniasis, caused by Leishmania parasites, presents a major global health challenge due to limitations of existing treatments, including toxicity, side effects, drug resistance, and high costs. This study utilized the MuDRA (Multi-Descriptor Read Across) model for virtual screening to identify potential anti-Leishmania infantum compounds. A set of 15 terpenes and steroids was screened, leading to the identification of four promising candidates-lupeol, xylodiol, morolic acid, and trachyloban-18-oic acid.
View Article and Find Full Text PDFMicroorganisms
July 2024
Infectious Disease Laboratory, Campus Ministro Reis Velloso, Federal University Delta of Parnaiba, Parnaíba 64202-020, PI, Brazil.
Leishmaniasis is a group of infectious diseases transmitted to humans during vector bites and caused by protozoans of the genus . Conventional therapies face challenges due to their serious side effects, prompting research into new anti-leishmania agents. In this context, we investigated the effectiveness of morolic acid, a pentacyclic triterpene, on promastigotes and amastigotes.
View Article and Find Full Text PDFSoft Matter
October 2023
Institute of Experimental Botany of the Czech Academy of Sciences, Isotope Laboratory, Vídeňská 1083, CZ-14220 Prague, Czech Republic.
Moronic acid and morolic acid, less frequently studied plant triterpenoids, were subjected to derivation with several structural modifiers, namely, piperazine-, pyrazine-, 1-indole- and L-methionine-based compounds. Derivation was targeted to design and prepare novel compounds capable of nano-assembling and/or displaying cytotoxicity. Formation of nanostructures has been proven for several novel target compounds that formed different types of nanostructures, either in chloroform or in water.
View Article and Find Full Text PDFMolecules
December 2020
School of Pharmacy, Sungkyunkwan University, Suwon 16419, Korea.
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