Review Article

Anticancer Activity of Chitosan, Chitosan Derivatives, and Their Mechanism of Action

Table 3

Anticancer mechanism of action of HCT as a precursor of chitosan thiosemicarbazone and chitosan derivatives in some potential target cells.

Compounds Target cellsMechanism of actionTestOutcomeYearRef.

HCTL1210Inhibition of RR activityIn vitroAntineoplastic effect1956-89[119126]

Chitosan copper(II) complex293 and HeLa cellsCheckpoint-controlled progression of cell proliferation at S phaseIn vitroInhibition of cellular proliferation2006 
2000
[42] 
[138]

Copper loaded chitosan nano particlesOsteocarcinomanano particles mediated enhanced permeation and retention (EPR) effect, increase in ROS level, DNA fragmentation and apoptosisIn vitro  and in vivoInhibition of tumor growth2017 
2009 
2013 
2009
[96] 
[139] 
[140] 
[141]

CMCS HUVECs Inhibition of extracellular matrix degradation and transformation of malignant cells In vitro  
Suppression of angiogenesis, decrease in VEGF and increase in TIMP1 levels  
2015 
2009 
2007 
2007 
[45] 
[82] 
[95] 
[106]   
H-22Necrosis due to cell distortion and disintegration of nucleiIn vivoInhibition of tumor growth2015[45]
Solid tumorEnhancement in IFN- γ and TNF- α levels, regulation of immune-related cytokines induction and immunoenhancementIn vivo  mice modelIncrease in thymus index, tumor growth inhibition2015[45]

Chitosan thymine conjugateHepG2Inhibition of DNA synthesis, mRNA transcription and translation of the cancer-causing geneIn vitroInhibition of tumor growth2012[46]

SCS and SBCSMCF-7 cellsInduction of apoptosis and blockade of the FGF-2-induced phosphorylation of ERKIn vitroInhibition of cells proliferation2011[47]

G-Chi- MMC and N-Suc-Chi -MMC conjugateSolid tumors, leukemia, metastatic liver cancerSustained release of drug from conjugateIn vitro and in vivoHigher antitumor effect and less side effects2005[48]

Furanoallocolchicinoid- chitosan conjugateWnt-1 breast tumor bearing miceTubulin reorganization, cell cycle arrest, sequestering of colchicine molecules.In vivoInhibition of tumor cell proliferation and less side effects.2016 
2015
[49] 
[75]

3-Amino-2-phenyl-4(3H)-quinazolinone PPC-silver chloride nano compositeEAC and MCF-7Sequestering of molecules from noncancer cells and sustained release to cancer cells with zero order kineticsIn vitroTarget delivery of nano particles2017[50, 51]