Table 1.
A summary of anti-cancer activities of chitosan and its derivatives
| CS/CS-derived products | In vitro/in vivo | Reported results | MW/DA | References | Year |
|---|---|---|---|---|---|
| COS | MDA-MB-231 (in vitro) | Reduction in MMP-9 secretion and activities | 1 kDa < MW < 3 kDa | Kyung et al. [196] | 2009 |
| COS |
LLC (in vitro) HepG2 (in vivo) |
Inhibition of MMP-9 secretion Inhibition of the tumor growth |
MW = 23.99 kDa | Shen et al. [103] | 2009 |
| COS | PC-3, A549 (in vitro) | Suppression of cancer cell growth |
DD = 85–100% MW = 360–2625 m/z |
Park et al. [25] | 2011 |
| CSO–SA | MCF-7, A549, Bel-7402 (in vitro) | Discovered anti-cancer activities of podophyllotoxin loaded on CSO–SA micelles |
DD = 95% MW = 15.0 kDa |
Huang et al. [197] | 2012 |
| Sulfated polysaccharide | SKOV3 and ECV304 cells (in vitro) | Inhibition of MMP-2 expression | MW = 11.3 kDa | Zong et al. [198] | 2013 |
| O-Carboxymethyl-chitosan | Human normal liver cell L02, human hepatoma cell Bel-7402, human gastric cancer cell SGC-7901 and human cervical carcinoma cell Hela | Cytokine levels were compatible in vitro. In vivo, nontoxic to body and enhanced body immune response, serum levels of IL-2 and TNF-α in sarcoma-180-bearing mouse |
DD = 78.0% MW = 340 kDa |
Zheng et al. [199] | 2011 |
| CSOSA-g-PEI | Hela and MCF-7 | Comparable transfection efficiency level of CSOSA-g-PEI to lipofectamine 2000 |
DD = 95.0% MW = 17.5 kDa |
Hu et al. [200] | 2013 |
| CSOAA (conjugate for doxorubicin (DOX) delivery) | FaDu cells (in vitro) and FaDu tumor xenografted mouse model (in vivo) | Control drug release profile. In addition, cellular uptake |
DD = > 90% MW = 5 kDa |
Termsarasab et al. [201] | 2013 |
| FA–PEG–COL | BALB/c mice bearing OVK18 #2 tumor xenograft (in vivo) | Showing much potential for effective ovarian cancer treatment via gene therapy |
DD = > 90% MW = 3–5 kDa |
Li et al. [202] | 2014 |
| CTS | RT112 bladder cancer cell lines (In vitro) | CS exhibited a remarkable reduction in proliferation of RT112 cell line. CTS with lower MW found to be more effective than higher MW ones |
DD = 70–90% MW = 5800 and 19,800 g/mol |
Younes et al. [203] | 2014 |
| CTS (LMWC) | Ca922 cells (in vitro) | G1/S cell cycle arrest subtle increases of caspase activity |
DD = 75–85% MW = 50–190 kDa |
Wimardhani et al. [98] | 2014 |
| CS | Bladder carcinoma cells (RT112 and RT112cp) |
Cytotoxic effect of chitosan increased with increasing DA and decreasing pH MW had no effect on toxicity of CS |
DD = 39–98% MW = 75,000–110,000 g/mol |
Younes et al. [96] | 2015 |
| CS | IMR 32/Hep G2 cells (in vitro) | Moderate anti-proliferative effect |
DD = 90.2–93.3% MW = 382.73–423.43 kDa 212.93–548.75 kDa |
Chien et al. [204] | 2016 |
| COS |
10 tumor cell lines (In vitro) S180-bearing mice (in vivo) |
HCT-116 cells were the least sensitive to COS MCF-7 cells were the most sensitive to COS Stimulation of M1 type macrophage and production of TNF-α |
DD = 90–93% MW = 1–2 kDa |
Zou et al. [97] | 2016 |
| COS | HeLa cells (in vitro) | At concentration of 40 mg/ml, an abnormal morphology was found in HeLa cells |
DD = 80% MW = 1.44 kDa |
Chokradjaroen et al. [205] | 2017 |
| CS | Ovarian cancer cell line—PA-1 (in vitro) | 100% growth suppression of the of PA-1 tumor cells at low concentration at 10 µg/ml | Not reported | Srinivasan et al. [206] | 2018 |
COS chitosan oligosaccharide, CS chitosan, CSO–SA stearic acid-g-chitosan oligosaccharide, CSOSA-g-PEI polyethylenimine-conjugated stearic acid-g-chitosan oligosaccharide micelles, FA–PEG–COL folic acid–poly(ethylene glycol)–chitosan oligosaccharide lactate, CSOAA chitosan oligosaccharide–arachidic acid, LMWC low molecular weight chitosan, MMP matrix metalloproteinase, DA degree of acetylation