title: Synthesis and anti-tumor activity evaluation of rhein-aloe emodin hybrid molecule.
abstract: 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.
authors.affiliation: Guangxi Medical University, Guangxi Nanning 530021, China. yuan_yefei@126.com
authors.forename: Ye-Fei
authors.initials: YF
authors.lastname: Yuan
authors.forename: Xiang-Yu
authors.initials: XY
authors.lastname: Hu
authors.forename: Ying
authors.initials: Y
authors.lastname: He
authors.forename: Jia-Gang
authors.initials: JG
authors.lastname: Deng
mesh_terms: D000880:Anthraquinones / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy; D015394:Molecular Structure
chemical_list: D000880:Anthraquinones; D000970:Antineoplastic Agents; C571557:rhein-aloe-emodin hybrid molecule; C518327:aloe emodin; C020491:rhein