title: Antitumor Effects and Mechanism of Novel Emodin Rhamnoside Derivatives against Human Cancer Cells In Vitro.
abstract: A series of novel anthracene L-rhamnopyranosides compounds were designed and synthesized and their anti-proliferative activities on cancer cell lines were investigated. We found that one derivative S-8 (EM-d-Rha) strongly inhibited cell proliferation of a panel of different human cancer cell lines including A549, HepG2, OVCAR-3, HeLa and K562 and SGC-790 cell lines, and displayed IC50 values in low micro-molar ranges, which are ten folds more effective than emodin. In addition, we found EM-d-Rha (3-(2",3"-Di-O-acetyl-α-L-rhamnopyranosyl-(1→4)-2',3'-di-O-acetyl-α-L-rhamnopyranosyl)-emodin) substantially induced cellular apoptosis of HepG2 and OVCAR-3 cells in the early growth stage. Furthermore, EM-d-Rha led to the decrease of mitochondrial transmembrane potential, and up-regulated the express of cells apoptosis factors in a concentration- and time-dependent manner. The results indicated the EM-d-Rha may inhibit the growth and proliferation of HepG2 cells through the pathway of apoptosis induction, and the possible molecular mechanism may due to the activation of intrinsic apoptotic signal pathway.
authors.affiliation: Department of Pharmaceutical Engineering, South China Agricultural University, Guangzhou, Guangdong, China.
authors.forename: Jie-yu
authors.initials: JY
authors.lastname: Xing
authors.affiliation: Department of Pharmaceutical Engineering, South China Agricultural University, Guangzhou, Guangdong, China.
authors.forename: Gao-peng
authors.initials: GP
authors.lastname: Song
authors.affiliation: Department of Biochemistry and Molecular Biology, Oklahoma State University, Stillwater, Oklahoma, United States of America.
authors.forename: Jun-peng
authors.initials: JP
authors.lastname: Deng
authors.affiliation: College of Life Science, Shenzhen Key Laboratory of Microbial Genetic Engineering, Shenzhen University, Shenzhen, Guangdong, China.
authors.forename: Ling-zhi
authors.initials: LZ
authors.lastname: Jiang
authors.affiliation: Department of Pharmaceutical Engineering, South China Agricultural University, Guangzhou, Guangdong, China.
authors.forename: Ping
authors.initials: P
authors.lastname: Xiong
authors.affiliation: Department of Pharmaceutical Engineering, South China Agricultural University, Guangzhou, Guangdong, China.
authors.forename: Bin-jie
authors.initials: BJ
authors.lastname: Yang
authors.affiliation: Department of Pharmaceutical Engineering, South China Agricultural University, Guangzhou, Guangdong, China.
authors.forename: Shan-shan
authors.initials: SS
authors.lastname: Liu
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D004642:Emodin / Q000031:analogs & derivatives*; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D066298:In Vitro Techniques; D061986:MCF-7 Cells; D053078:Membrane Potential, Mitochondrial / Q000187:drug effects*; D009369:Neoplasms / Q000188:drug therapy / Q000235:genetics / Q000473:pathology*
chemical_list: D000970:Antineoplastic Agents; D004642:Emodin