Authors: Risako Onodera Keiichi Motoyama Hidetoshi Arima
Publish Date: 2010/08/21
Volume: 70, Issue: 3-4, Pages: 321-326
Abstract
Methylβcyclodextrin MβCyD is widely used as a raft disrupting agent through extraction of cholesterol from lipid rafts which are highly expressed in cell membranes of tumor cells but it does not have tumor cellselective action Meanwhile the widespread use of folic acid FA as a tumortargeting ligand has been known because folate receptor FR overexpresses in various kinds of epithelial tumor cells In the present study in order to obtain more tumor cellselectivity and antitumor activity of MβCyD we designed folateappended MβCyD FAMβCyD and evaluated its physicochemical properties and antitumor activity The 1HNMR study demonstrated that FAMβCyD having average degree of substitution of FA DSF of 10 was prepared In addition FAMβCyD DSF 10 was found to be amorphous in a solid state and surfaceactive Importantly FAMβCyD DSF 10 had potent cytotoxicity compared to MβCyD in KB cells but not in A549 cells These results suggest that FAMβCyD DSF 10 has the potential as a novel antitumor agent
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