Antileishmanial activity of neo-clerodane diterpenes from Croton echioides
| Autor: | Rodolfo Bento Balbinot, Maria Helena Sarragiotto, Cláudio Roberto Novello, Celso Vataru Nakamura, João Carlos Palazzo de Mello, Elisangela Düsman, Jéssica Carreira de Paula |
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| Rok vydání: | 2022 |
| Předmět: |
Leishmania amazonensis
Stem bark biology Traditional medicine 010405 organic chemistry Chemistry Organic Chemistry Euphorbiaceae Plant Science biology.organism_classification 01 natural sciences Biochemistry 0104 chemical sciences Analytical Chemistry Bioguided fractionation 010404 medicinal & biomolecular chemistry Clerodane Diterpenes Croton echioides |
| DOI: | 10.6084/m9.figshare.13297743.v2 |
| Popis: | Nowadays, new leishmanicidal drugs are needed and natural products arise as a promising alternative source. Therefore, bioguided fractionation of a hydroethanolic extract from the stem bark of Croton echioides Baill. were conducted based on its antileishmanial activity. Two novel neo-clerodane diterpenoids methyl-15,16-epoxy-3,13(16),14-neo-clerodatrien-17,18-dicarboxylate (1) and dimethyl-3-oxo-15,16-epoxy-13(16),14-neo-clerodadien-17,18-dicarboxylate (2) were isolated, as well as four known compounds (3–6) and lupeol, from the hexane fraction. Their structures were established by NMR analysis. The crude extract, fractions and the compounds (1 and 3–6) were evaluated for their in vitro antileishmanial activity and cytotoxicity against macrophages J774A.1. The selectivity index (SI) were calculated. The most active compound against promastigote forms of L. amazonensis was the clerodane diterpene 4, with IC50 values of 8.3 µM and SI value of 80.9. Our results highlighted stem bark of Croton echioides Baill. as a promising source for the development of a new chemotherapeutic agent to combat leishmaniasis. |
| Databáze: | OpenAIRE |
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