Un dépsido antiplasmodial de un liquen nigeriano dirinaria picta, epífito en la palma de aceite Elaeis Guineense
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Rev. Bol. Quim
Abstract
Este estudio investigo los potenciales anti-plasmodiales y citotoxicos de los extractos de cloroformo (LCE) y etanol (LEE) de liquenes foliosos Dirinaria picta con el objetivo de aislar el (los) compuesto (s) principal (es) del farmaco antipaludico. Los ensayos in vitro anti-plasmodial y de citotoxicidad se realizaron usando el ensayo de deshidrogenasa plasmodium lactato y las lineas celulares humanas HeLa cervica, respectivamente. La estructura del compuesto aislado se elucido usando tecnicas espectroscopicas. El LCE produjo un nuevo depsido antiplasmodial 1 (antiplasmodial IC50 ≈ 37 μg / ml; citotoxicidad (IC50 > 100 μg / ml; Indice de selectividad> 2,7) y una fraccion impura LC2 (antiplasmodial IC50≈ 79 μg / ml; citotoxicidad (IC50> 100) μg / mL; Indice de selectividad <1.3). El LEE (IC50 antiplasmodial ≈ 17 μg / mL; citotoxicidad (IC50 ≈ 62 μg / mL; Indice de selectividad ≈ 3.7) mostro una actividad antiplamodial significativamente mejor (p <0.05) aunque fue mas citotoxico en comparacion con depsido 1 y LC2. El depsido 1, LC2 y LEE fueron menos citotoxicos en comparacion con emetina (citotoxicidad (IC50 = 0.02 μM ≈ 0.013 μg / mL) aunque no tan activos como los medicamentos de referenda chloroquine (antiplasmodial IC50 = 0.031 μM = 0.016 μg / mL). Este es el primer informe sobre el potencial antipaludico de los liquenes nigerianos y el aislamiento de un nuevo depsido antiplamodial 1.
This study investigated the anti-plasmodial and cytotoxic potentials of the chloroform (LCE) and ethanol (LEE) extracts from the foliose lichen Dirinaria picta with the view of isolating anti-malarial drug lead compound(s). In vitro anti-plasmodial and cytotoxicity assays were done using the plasmodium lactate dehydrogenase assay and human HeLa cervica cell lines respectively. The structure of the isolated compound was elucidated using spectroscopic techniques. The LCE yielded a novel antiplasmodial depside 1 (antiplasmodial IC50≈37 (μg/mL; cytotoxicity (IC50 >100 μg/mL; Selectivity index >2.7) and an impure fraction LC2 (antiplasmodial IC50 ≈ 79 μg/mL; cytotoxicity (IC50 >100 μg/mL; Selectivity index <1.3). The LEE (antiplasmodial IC50 ≈ 17 μg/mL; cytotoxicity (IC50 ≈ 62 μg/mL; Selectivity index ≈ 3.7) showed a significantly (p < 0.05) better anti-plasmodial activity though more cytotoxic compared to depside 1 and LC2.The depside 1, LC2 and LEE were less cytotoxic compared to emetine (cytotoxicity (IC50 = 0.02 μM ≈ 0.013 μg/mL) though not as active as the reference drugs chloroquine (antiplasmodial IC50 = 0.031 μM ≈ 0.016 μg/mL). This is the first time report on the anti-malarial potential of Nigerian lichens and the isolation of a novel anti-plasmodial depside 1.
This study investigated the anti-plasmodial and cytotoxic potentials of the chloroform (LCE) and ethanol (LEE) extracts from the foliose lichen Dirinaria picta with the view of isolating anti-malarial drug lead compound(s). In vitro anti-plasmodial and cytotoxicity assays were done using the plasmodium lactate dehydrogenase assay and human HeLa cervica cell lines respectively. The structure of the isolated compound was elucidated using spectroscopic techniques. The LCE yielded a novel antiplasmodial depside 1 (antiplasmodial IC50≈37 (μg/mL; cytotoxicity (IC50 >100 μg/mL; Selectivity index >2.7) and an impure fraction LC2 (antiplasmodial IC50 ≈ 79 μg/mL; cytotoxicity (IC50 >100 μg/mL; Selectivity index <1.3). The LEE (antiplasmodial IC50 ≈ 17 μg/mL; cytotoxicity (IC50 ≈ 62 μg/mL; Selectivity index ≈ 3.7) showed a significantly (p < 0.05) better anti-plasmodial activity though more cytotoxic compared to depside 1 and LC2.The depside 1, LC2 and LEE were less cytotoxic compared to emetine (cytotoxicity (IC50 = 0.02 μM ≈ 0.013 μg/mL) though not as active as the reference drugs chloroquine (antiplasmodial IC50 = 0.031 μM ≈ 0.016 μg/mL). This is the first time report on the anti-malarial potential of Nigerian lichens and the isolation of a novel anti-plasmodial depside 1.
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Vol. 35, No. 1