Mar. Drugs 2022, 20(12), 784; https://doi.org/10.3390/md20120784
Antidiabetic Properties of Chitosan and Its Derivatives
Diabetes mellitus is a chronic metabolic disorder. In addition to taking medication, adjusting the composition of the diet is also considered one of the effective methods to control the levels of blood glucose. Chitosan and its derivatives are natural and versatile biomaterials with health benefits. Chitosan has the potential to alleviate diabetic hyperglycemia by reducing hepatic gluconeogenesis and increasing skeletal muscle glucose uptake and utility. Scientists also focus on the glucoselowering effect of chitosan oligosaccharide (COS). COS supplementation has the potential to alleviate abnormal glucose metabolism in diabetic rats by inhibiting gluconeogenesis and lipid peroxidation in the liver. Both high and low molecular weight chitosan feeding reduced insulin resistance by inhibiting lipid accumulation in the liver and adipose tissue and ameliorating chronic inflammation in diabetic rats. COS can reduce insulin resistance but has less ability to reduce hepatic lipids in diabetic rats.
Application of Chitosan and Its Derivatives in Clinical Trials
|
MW and DD of Chitosan/COS 1 |
Experimental Species |
Routes of Administration |
Doses and Durations |
Antidiabetic Effects |
|
Average MW 20 kDa 2 |
Obese diabetic KK-Ay mice |
In drinking water |
0.05%, 0.2% or 0.8% for 11 weeks |
Anti-hyperglycemia; anti-hyperinsulinemia; anti-hypertriglyceridemia |
|
Average MW 1.5 kDa; DD = 86.5% |
High-energy diet/streptozotocin-induced diabetic Sprague Dawley rats; in vitro β-cells |
Oral |
500 and 1000 mg/kg for 8 weeks |
Anti-hyperglycemia; improvement of glucose tolerance; protecting β-cells |
|
Average MW < 1000 Da (GO2KA1) |
db/db diabetic mice |
In diet |
4% for 42 days |
Reduction in blood glucose and HbA1c; inhibition of carbohydrate hydrolysis enzymes |
|
Average MW = 380 kDa; DD = 89.8% |
High-fructose diet-fed Sprague Dawley rats |
In diet |
5% for 21 weeks |
Improvement of impairment in glucose and lipid metabolism |
|
Average MW < 1000 Da (GO2KA1) 2 |
In vitro |
Culture medium |
1 and 10 mg/mL |
Inhibiting intestinal glucose digestion and transport; enhancing glucose uptake |
|
Average MW < 1000 Da (GO2KA1) 2 |
Human subjects with prediabetes |
Oral |
1500 mg per day for 12 weeks |
Help control postprandial glucose |
1 MW: molecular weight; DD: degree of deacetylation. 2 In these literature reports, information on the DD was not shown.
Anti-Diabetic Effect and Mechanism of Chitosan and Its Derivatives
Conclusions
Chitosan and its derivatives have been shown to improve glucose and lipid homeostasis in diabetic rodents, which may provide a new option for diabetic intervention. Nevertheless, more scientific evidence is urgently needed from both animal studies and clinical trials to further understand its glucose regulating effects and safety.