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Review
. 2018 Dec 30:2018:2952085.
doi: 10.1155/2018/2952085. eCollection 2018.

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

Affiliations
Review

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

Hari Sharan Adhikari et al. Int J Biomater. .

Abstract

Tailoring of chitosan through the involvement of its amino, acetamido, and hydroxy groups can give derivatives of enhanced solubility and remarkable anticancer activity. The general mechanism of such activity is associated with the disturbances in normal functioning of cell cycle, interference to the central dogma of biological system from DNA to RNA to protein or enzymatic synthesis, and the disruption of hormonal path to biosynthesis to inhibit the growth of cancer cells. Both chitosan and its various derivatives have been reported to selectively permeate through the cancer cell membranes and show anticancer activity through the cellular enzymatic, antiangiogenic, immunoenhancing, antioxidant defense mechanism, and apoptotic pathways. They get sequestered from noncancer cells and provide their enhanced bioavailability in cancer cells in a sustained release manner. This review presents the putative mechanisms of anticancer activity of chitosan and mechanistic approaches of structure activity relation upon the modification of chitosan through functionalization, complex formation, and graft copolymerization to give different derivatives.

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Figures

Scheme 1
Scheme 1
Steps involved in the preparation of chitosan.
Figure 1
Figure 1
Structure of chitosan.
Figure 2
Figure 2
Structure of chitin.
Figure 3
Figure 3
Deacetylation of chitin.
Figure 4
Figure 4
Synthetic route to 2-phenylhydrazine (or hydrazine) thiosemicarbazone chitosan.
Figure 5
Figure 5
Structure of chitosan-metal complex.
Figure 6
Figure 6
Figure 7
Figure 7
Synthetic route of chitosan–thymine conjugate.
Figure 8
Figure 8
Synthetic route of sulfated chitosan (SCS) and sulfated benzaldehyde chitosan (SBCS).
Figure 9
Figure 9
Synthetic route of N-succinyl chitosan.
Figure 10
Figure 10
Synthetic route of glycol chitosan.
Figure 11
Figure 11
Synthetic route to furanoallocolchicinoid chitosan.
Figure 12
Figure 12
Graft copolymerization of polypyrrole-chitosan.
Figure 13
Figure 13
(a) Heparan sulfate (HS). (b) Carboxymethyl benzylamide dextran (CMDB).

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