Sino-France Laboratory for Drug Screening, Key Laboratory of Molecular Biophysics of Ministry of Education, School of Life Science and Technology, Huazhong University of Science and Technology, 430074 Wuhan, Hubei, China. slhuang@mail.hust.edu.cn, pingy@mail.hust.edu.cn.
Anticancer Res. 2011 Apr; 31(4):1321-8.
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.
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.
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.
The sulfated and benzaldehyde chitosans seem to be good potential compounds for anticancer drug design.
PMID: 21508382 [PubMed - in process] Source: National Library of Medicine.
