The impact of chitooligosaccharides and their derivatives on the in vitro and in vivo antitumor activity: A comprehensive review

Chitooligosaccharides (COS) are the degraded products of chitin or chitosan. COS is water-soluble, non-cytotoxic to organisms, readily absorbed through the intestine, and eliminated primarily through the kidneys. COS possess a wide range of biological activities, including immunomodulation, cholesterol-lowering, and antitumor activity. Although work on COS goes back at least forty years, several aspects remain unclear. This review narrates the recent developments in COS antitumor activities, while paying considerable attention to the impacts of physicochemical properties (such as molecular weight and degrees of deacetylation) and chemical modifications both in vitro and in vivo. COS derivatives not only improve some physicochemical properties, but also expand the range of applications in drug and gene delivery. COS (itself or as a drug carrier) can inhibit tumor cell proliferation and metastasis, which might be attributed to its ability to stimulate the immune response along with its anti-angiogenic activity. Further, an attempt has been made to report limitations and future research. The potential health benefits of COS and its derivatives against cancer may offer a new insight on their applications in food and medical fields. •Chitooligosaccharides (COS) are the degraded products of chitin and chitosan.•The PK of COS with insight into therapeutic dosage formulations is addressed.•The antitumor activities are associated with COS physicochemical properties.•COS (itself or as a drug carrier) suppress tumor proliferation and metastasis.•COS and their derivatives might have the potential health benefits as anticancer.