Abstract

Alkaloids, polyphenols, cyanogenic glycosides and saponins are among the main chemical compounds synthesized by plants but not considered essential for their basic metabolism. These compounds have different functions in plants, and have been recognized with medicinal and pharmacological properties. In this research, concentrations of the mentioned secondary metabolites were determined in the medicinal plants Artemisia absinthium, Cnidoscolus aconitifolius, Parthenium hysterophorus, Piper carpunya and Taraxacum officinale, from Ecuador, and related with cytotoxic effects against Artemia salina. Alcoholic and aqueous extracts from leaves of these selected plants were prepared at different concentrations. To assess cytotoxicity of these extracts, different bioassays with A. salina were undertaken, and the mortality rates and LC50 were obtained. Besides, concentrations of alkaloids, cyanogenic glycosides, phenols, tannins and saponins were determined by spectrophotometric methods; this constituted the first report of quantification of secondary metabolites in the selected plants from Ecuador. T. officinale had the highest concentration of total phenols (22.30 ± 0.23 mg/g) and tannins (11.70 ± 0.10 mg/g), C. aconitifolius of cyanogenic glycosides (5.02 ± 0.37 µg/g) and P. hysterophorus of saponins (6.12 ± 0.02 mg/g). Tannins values obtained were not adverse to their consumption. Alcoholic and aqueous extracts of selected plants had hemolytic activity depending on the concentration of saponins. Although the values of cyanogenic glycosides were permissible, it was necessary to monitor the presence of this metabolite in plants to minimize health problems. LC50 values ranged from extremely toxic (3.37 µg/mL) to highly toxic (274.34 μg/mL), in P. carpunya and T. officinale, respectively. From correlation analysis, it was observed that increase values of alkaloids concentrations had highly significant (p<0.001) acute toxicity against A. salina, while at a higher polyphenol concentration the level of plants cytotoxicity decreased significantly (p<0.001). The results of principal component analysis showed that saponins apparently were in synergy with polyphenols to decrease cytotoxicity, but antagonize with alkaloids and cyanogenic glycosides, indicating that these secondary metabolites present variability in the mechanisms of action against A. salina, as cytotoxic compounds. These results also demonstrate that polyphenols and saponins can be lethal at low concentrations, demonstrating the potential of brine shrimp bioassay as a model to evaluate plant extracts containing low concentrations of chemical compounds with high polarities. The significant positive correlation between cytotoxicity and concentration of alkaloids confirmed by the bioassay of brine shrimp can be useful to identify promising sources of antitumor compounds, and to evaluate tolerable limits not affecting other benign cells. Contents of secondary metabolites found in the selected plants confer them great pharmacologic values.

Highlights

  • Las plantas con propiedades medicinales han estado relacionadas estrechamente con el surgimiento y desarrollo de la civilización humana en diferentes zonas geográficas y han sido reconocidas por la Organización Mundial para la Salud (OMS, 2002) para el tratamiento de diversas enfermedades

  • Con los resultados observados de correlaciones y del análisis de componentes principales, se puede inferir que las plantas medicinales evaluadas en este estudio contienen glucósidos cianógenicos, con una tendencia de toxicidad a nivel celular no significativa y totalmente independiente a los polifenoles, saponinas y a los alcaloides

  • Estos resultados demuestran que las saponinas y los polifenoles pueden ser letales para A. salina a bajas concentraciones, evidenciando que este bioensayo permite evaluar extractos vegetales que contengan bajas concentraciones de compuestos con altas polaridades

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Summary

Introduction

Las plantas con propiedades medicinales han estado relacionadas estrechamente con el surgimiento y desarrollo de la civilización humana en diferentes zonas geográficas y han sido reconocidas por la Organización Mundial para la Salud (OMS, 2002) para el tratamiento de diversas enfermedades. Al considerar que los enfoques de las investigaciones acerca de los metabolitos secundarios presentes en las plantas son hacia la búsqueda de nuevas sustancias con propiedades antitumorales, esta investigación tuvo como objetivo determinar las concentraciones de alcaloides, fenoles totales, taninos, glucósidos cianogénicos y saponinas, y correlacionarlas con el efecto citotóxico, a través del bioensayo contra el crustáceo Artemia salina.

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