title: Novel Synthetic Mono-triazole Glycosides Induce G0/G1 Cell-cycle Arrest and Apoptosis in Cholangiocarcinoma Cells.
abstract: The treatment of cholangiocarcinoma (CCA) is still ineffective and the search for a novel treatment is needed. In this study, eight novel mono-triazole glycosides (W1-W8) were synthesized and tested for their anticancer activities in CCA cell lines.
  
  
  
  The anti-proliferation effect and the underlying mechanisms of the triazole glycosides were explored. Viable cells were determined using the MTT test.
  
  
  
  Among glycosides tested, W4 and W5 exhibited the most potent anticancer activity in a dose- and time-dependent fashion. Flow cytometry and wstern blot analysis revealed that W4 and W5 induced G0/G1phase cell-cycle arrest through down-regulation of cyclin D1, cyclin E and induction of cyclin-dependent kinase inhibitors, p27 and p21 protein expression. Annexin V/propidium iodide (PI) staining demonstrated that W4 and W5 also induced apoptotic cells in a dose-dependent manner via caspase signaling cascade.
  
  
  
  Together, these findings imply that the novel synthetic glycosides might be a promising anticancer agent for CCA.
authors: Department of Biochemistry, Liver Fluke and Cholangiocarcinoma Research Center, Faculty of Medicine, Khon Kaen University, Khon Kaen, Thailand.
authors: Sumalee
authors: S
authors: Obchoei
authors: Department of Chemistry and Center for Innovation in Chemistry, Faculty of Science, Burapha University, Chonburi, Thailand.
authors: Rungnapha
authors: R
authors: Saeeng
authors: Department of Biochemistry, Liver Fluke and Cholangiocarcinoma Research Center, Faculty of Medicine, Khon Kaen University, Khon Kaen, Thailand.
authors: Chaisiri
authors: C
authors: Wongkham
authors: Department of Biochemistry, Liver Fluke and Cholangiocarcinoma Research Center, Faculty of Medicine, Khon Kaen University, Khon Kaen, Thailand sopit@kku.ac.th.
authors: Sopit
authors: S
authors: Wongkham
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D002453:Cell Cycle / Q000187:drug effects*; D045744:Cell Line, Tumor; D018281:Cholangiocarcinoma / Q000473:pathology*; D006027:Glycosides / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D006027:Glycosides; D014230:Triazoles
keywords: G0/G1 arrest; Glycoside; cell apoptosis; cell growth; cholangiocarcinoma