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[具有抗疟活性的光茄标准化提取物的细胞毒性作用及遗传损伤评估]

[Evaluation of cytotoxic effect and genetic damage of standardized extracts of Solanum nudum with antiplasmodial activity].

作者信息

García-Huertas Paola, Pabón Adriana, Arias Carlos, Blair Silvia

机构信息

Grupo Malaria, Sede de Investigación Universitaria, Universidad de Antioquia, Medellín, Colombia.

出版信息

Biomedica. 2013 Jan-Mar;33(1):78-87. doi: 10.1590/S0120-41572013000100010.

Abstract

INTRODUCTION

The plant Solanum nudum (Solanaceae) is extensively used for the treatment of malaria-related symptoms in traditional medicine practices in the Colombian Pacific. Recently, it has become a significant source of promising new molecules for developing a pharmaceutical malaria treatment.

OBJECTIVE

This research aimed to evaluate the cytotoxic effect and the genetic damage of standardized extracts of S. nudumon different cells.

MATERIALS AND METHODS

Sixty six standardized S. nudum extracts were used, evaluating cytotoxicity in U937 and HepG2 cells and the antiplasmodial activity using both a chloroquine-sensitive (NF54) and a chloroquine-resistant (FCB2) strain. The hemolytic effect on healthy O + erythrocytes, the mutagenic effect on S.Typhimurium TA98 and TA100 strains and the genotoxic effect on U937 cells were evaluated. The extracts that displayed both antiplasmodial activity and low toxicity were selected.

RESULTS

Five extracts were selected: 28MA1, 29MA1, 51MA1, 55MA1 and 61MA1. These extracts were active against P. falciparum with IC 50 between 9.8 and 54.8 µg/ml and selectivity indexes were calculated between 0.9 and 4.4, the latter for 29MA1. Also, no hemolytic effects in healthy O + erythrocytes were shown at a concentration of 250 µg/ml, nor did they cause mutations in the TA98 and TA100 strains or generate genotoxic effects in U937cells.

CONCLUSION

The use of standardized extracts of S. nudum could contribute to the body of work aimed at developing a new pharmaceutical treatment for malaria using natural products.

摘要

引言

光茄(茄科)在哥伦比亚太平洋地区的传统医学实践中被广泛用于治疗疟疾相关症状。最近,它已成为开发疟疾药物治疗的有前景新分子的重要来源。

目的

本研究旨在评估光茄标准化提取物对不同细胞的细胞毒性作用和遗传损伤。

材料与方法

使用了66种光茄标准化提取物,评估其对U937和HepG2细胞的细胞毒性以及对氯喹敏感(NF54)和氯喹耐药(FCB2)菌株的抗疟原虫活性。评估了对健康O+红细胞的溶血作用、对鼠伤寒沙门氏菌TA98和TA100菌株的诱变作用以及对U937细胞的遗传毒性作用。选择了具有抗疟原虫活性且毒性低的提取物。

结果

选择了5种提取物:28MA1、29MA1、51MA1、55MA1和61MA1。这些提取物对恶性疟原虫有活性,IC50在9.8至54.8μg/ml之间,计算出的选择性指数在0.9至4.4之间,后者是29MA1的。此外,在250μg/ml的浓度下,对健康O+红细胞未显示溶血作用,对TA98和TA100菌株也未引起突变,对U937细胞也未产生遗传毒性作用。

结论

使用光茄标准化提取物有助于开展旨在利用天然产物开发疟疾新药物治疗的工作。

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