Yuan Ye-Fei, Hu Xiang-Yu, He Ying, Deng Jia-Gang
Guangxi Medical University, Guangxi Nanning 530021, China.
Nat Prod Commun. 2012 Feb;7(2):207-10.
To improve the anti-tumor effects of rhein and aloe-emodin, a rhein-aloe-emodin hybrid molecule (RH-AE) was synthesized from rhein and aloe-emodin in the presence of dicyclohexylcarbodiimide (DCC) and 4-dimethylaminopyridine (DMAP). Chemical and spectroscopic methods, such as 1H and 13C NMR spectroscopy, and HR-ESIMS were used for the structure identification of RH-AE. Using the cell counting kit-8 (CCK-8) assay, the in vitro anti-tumor effects were compared between RH-AE, rhein and aloe-emodin on human hepatoma HepG2, human nasopharyngeal carcinoma CNE, human lung cancer NCI-H460, human ovarian cancer SK-OV-3, and human cervical cancer Hela cells. The results showed that the half inhibitory concentration (IC50) of RH-AE on HepG2, CNE, NCI-H460, SK-OV-3, and Hela cells were significantly lower than those of rhein and aloe-emodin. This showed that RH-AE has a better in vitro anti-tumor effect than rhein and aloe-emodin.
为提高大黄酸和芦荟大黄素的抗肿瘤效果，在二环己基碳二亚胺（DCC）和4-二甲氨基吡啶（DMAP）存在的条件下，由大黄酸和芦荟大黄素合成了一种大黄酸-芦荟大黄素杂合分子（RH-AE）。采用1H和13C核磁共振光谱、高分辨电喷雾电离质谱等化学和光谱方法对RH-AE进行结构鉴定。使用细胞计数试剂盒-8（CCK-8）检测法，比较了RH-AE、大黄酸和芦荟大黄素对人肝癌HepG2细胞、人鼻咽癌CNE细胞、人肺癌NCI-H460细胞、人卵巢癌SK-OV-3细胞和人宫颈癌Hela细胞的体外抗肿瘤效果。结果显示，RH-AE对HepG2、CNE、NCI-H460、SK-OV-3和Hela细胞的半数抑制浓度（IC50）显著低于大黄酸和芦荟大黄素。这表明，RH-AE在体外具有比大黄酸和芦荟大黄素更好的抗肿瘤效果。
