title: Chitosan derivatives inhibit cell proliferation and induce apoptosis in breast cancer cells.
abstract: OBJECTIVE
  Both the sulfated and non-sulfated derivatives (e.g. carboxymethyl benzylamide dextrans) of heparan sulfate were reported to have anticancer activity. On this basis, we introduced sulfates and phenyls in carboxymethyl benzylamide dextrans into chitosan, which is easily modified by different functional groups in any given position and then evaluated anticancer activity in breast cancer cells.
  
  
  METHODS
  Chitosan derivatives were synthesized by introducing sulfate and phenyl groups into chitosan. Cell proliferation and apoptosis were assessed by (3)H-thymidine incorporation and fluorescence activated cell sorter analysis. Activation of Ras/MAPK signaling pathway downstream of fibroblast growth factor-2 (FGF-2) was analyzed by Western blot.
  
  
  RESULTS
  The sulfated chitosan (SCS) and the sulfated benzaldehyde chitosan (SBCS) significantly inhibited cell proliferation, induced apoptosis and blocked the FGF-2-induced phosphorylation of ERK in MCF-7 cells, SBCS had better inhibitory effects and a lower IC(50) compared to SCS.
  
  
  CONCLUSIONS
  The sulfated and benzaldehyde chitosans seem to be good potential compounds for anticancer drug design.
authors.affiliation: Huazhong University of Science and Technology, Wuhan, Hubei, China.
authors.forename: Ming
authors.initials: M
authors.lastname: Jiang
authors.forename: Handong
authors.initials: H
authors.lastname: Ouyang
authors.forename: Pin
authors.initials: P
authors.lastname: Ruan
authors.forename: Han
authors.initials: H
authors.lastname: Zhao
authors.forename: Zhenjun
authors.initials: Z
authors.lastname: Pi
authors.forename: Siluo
authors.initials: S
authors.lastname: Huang
authors.forename: Ping
authors.initials: P
authors.lastname: Yi
authors.forename: Michel
authors.initials: M
authors.lastname: Crepin
mesh_terms: D017209:Apoptosis / Q000187:drug effects*; D015153:Blotting, Western; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D049109:Cell Proliferation / Q000187:drug effects*; D048271:Chitosan / Q000737:chemistry* / Q000494:pharmacology*; D005260:Female; D016222:Fibroblast Growth Factor 2 / Q000378:metabolism; D006801:Humans; D020928:Mitogen-Activated Protein Kinases / Q000378:metabolism; D015398:Signal Transduction; D014407:Tumor Cells, Cultured; D018631:ras Proteins / Q000378:metabolism
chemical_list: D016222:Fibroblast Growth Factor 2; D048271:Chitosan; D020928:Mitogen-Activated Protein Kinases; D018631:ras Proteins