Department of Pharmaceutical Sciences, State University of Ponta Grossa, General Carlos Cavalcanti Avenue 4748, 84900-030, Ponta Grossa, Paraná, Brazil.
Department of General Biology, State University of Ponta Grossa, General Carlos Cavalcanti Avenue 4748, 84900-030, Ponta Grossa, Paraná, Brazil.
Chem Biodivers. 2020 Sep;17(9):e2000369. doi: 10.1002/cbdv.202000369. Epub 2020 Sep 2.
The current study was carried out by a bioguided fractionation of a hexane extract of the latex of Euphorbia umbellata against leukemic cells. Samples were analyzed by NMR, GC/MS, triterpenes quantification, and MTT reduction assay. Morphological, cell cycle, mitochondrial membrane potential and caspases 3/7 analyses were performed for the dichloromethane and ethanol fractions, and selectivity index for the dichloromethane fraction. NMR analysis presented characteristic signals of terpenes and steroids, data were confirmed by the quantification of triterpenes and GC/MS analysis. MTT reduction assay demonstrated that HL-60 was the most sensitive cell lineage against dichloromethane and ethanol fractions. Compounds of these matrices caused morphological changes compatible with apoptosis induction, altered cell cycle, increment of depolarized population cells and activation of caspases 3/7. Selectivity indices were higher than 22.44. Bioguided-fractionation study showed that samples of the latex of E. umbellata raised the activity of the phytocomplex against leukemic cells, and the cytotoxicity can be associated with an apoptosis pathway.
本研究采用生物导向分级分离法，从大飞扬属乳汁的正己烷提取物中分离出针对白血病细胞的物质。采用 NMR、GC/MS、三萜类定量分析和 MTT 还原测定法对样品进行分析。对二氯甲烷和乙醇馏分进行形态学、细胞周期、线粒体膜电位和半胱天冬酶 3/7 分析，并测定二氯甲烷馏分的选择性指数。NMR 分析呈现萜类和甾体的特征信号，三萜类定量分析和 GC/MS 分析数据得到证实。MTT 还原测定法表明，HL-60 是对二氯甲烷和乙醇馏分最敏感的细胞系。这些基质中的化合物引起与诱导细胞凋亡相符的形态变化，改变细胞周期，增加去极化细胞群，并激活半胱天冬酶 3/7。选择性指数高于 22.44。生物导向分级分离研究表明，大飞扬属乳汁的样品提高了植物复合物对白血病细胞的活性，细胞毒性可能与细胞凋亡途径有关。
