Chemical composition, antileishmanial and antioxidant activity of Eugenia moraviana (Myrtaceae) fruit extract

Medicinal Chemistry Research(2020)

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摘要
Leishmaniasis is a severe disease caused by protozoa of the genus Leishmania . The disease affects millions of people. Treatment is limited to only a few drugs that cause severe side effects. The identification of new compounds to treat leishmaniasis remains a challenge. This study aimed to determine the chemical composition of Eugenia moraviana fruit extract ( Em CE) and to investigate its effect on the promastigote and amastigote forms of Leishmania amazonensis , the ultrastructural changes induced by it, its cytotoxicity, and antioxidant effect. Liquid chromatography–high-resolution mass spectrometry was used to identify Em CE components. Amastigote forms (IC 50 0.6 µg mL −1 ) were more sensitive to Em CE treatment than promastigote forms (IC 50 77.2 µg mL −1 ). The cytotoxicity concentration 50% was 187.8 µg mL −1 for J774.A1 macrophages and 190.0 µg mL −1 for murine macrophages, with selectivity index of 313 and 316.7, respectively. Em CE induced 14.7% hemolysis. Promastigotes exposed to Em CE experienced drastic ultrastructural changes, such as intense cytoplasm vacuolization and mitochondrial swelling. The antioxidant activity IC 50 for DPPH was 0.78 µg mL −1 , inhibition of lipid peroxidation was 56.4%, FRAP assays with 1.19 µM ferrous sulfate/mg sample, and total phenolic acid equivalent was 76.1 µg gallic acid/mg sample. Em CE was not cytotoxic, was highly selective for protozoans, and caused intracellular death of the parasite. The results indicated the potential value of Em CE in the treatment of leishmaniasis. These results are the first report of antileishmanial activity and chemical composition for E. moraviana fruits extract.
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关键词
Leishmaniasis,Antileishmanial agents,Cambuí,Myrtaceae,Chemical characterization
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