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Isolation of epi-oleanolic acid from Korean mistletoe and its apoptosis-lnducing activity in tumor cells.

机译:韩国槲寄生中表皮油酸的分离及其在肿瘤细胞中的凋亡诱导活性。

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摘要

A triterpene was isolated as a cytotoxic principle from the dichloromethane extract of Korean mistletoe (KM; Viscum album coloratum) by repeated silica gel chromatography and recrystallization. In in vitro analysis of cytotoxic activity using various human and murine tumor cell lines, the dichloromethane extract of KM was highly cytotoxic against these cells. We isolated the most active compound, referred to VD-3, from the dichloromethane extract of KM. The VD-3 was shown to be less cytotoxic to normal cells (murine splenocytes). From the identification of the chemical structure of VD-3 by spectral data and chemical synthesis, the compound was proven to be epi-oleanolic acid. Tumor cells treated with VD-3 showed a typical pattern of apoptotic cell death, such as apparent morphological changes and DNA fragmentation. These results indicate that epi-oleanolic acid is an important compound responsible for antitumor activity of KM.
机译:通过重复硅胶色谱法和重结晶从韩国槲寄生的二氯甲烷提取物中分离出三萜(KM; Viscum Album coloratum)。在使用各种人类和鼠类肿瘤细胞系进行细胞毒性活性的体外分析中,KM的二氯甲烷提取物对这些细胞具有高度的细胞毒性。我们从KM的二氯甲烷萃取物中分离出活性最高的化合物,称为VD-3。 VD-3被证明对正常细胞(鼠脾细胞)的细胞毒性较小。通过光谱数据和化学合成鉴定VD-3的化学结构,证明该化合物为表油酸。用VD-3处理的肿瘤细胞表现出典型的凋亡细胞死亡模式,例如明显的形态变化和DNA片段化。这些结果表明,表油酸是负责KM的抗肿瘤活性的重要化合物。

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