Excellent Center for Drug Discovery and Department of Physiology, Faculty of Science, Mahidol University, Rama VI Road, Ratchathewi, Bangkok 10400, Thailand.
Excellent Center for Drug Discovery and Department of Physiology, Faculty of Science, Mahidol University, Rama VI Road, Ratchathewi, Bangkok 10400, Thailand.
Pharmacol Ther. 2017 Feb;170:80-97. doi: 10.1016/j.pharmthera.2016.10.013. Epub 2016 Oct 20.
Chitosan oligosaccharide (COS) is an oligomer of β-(1➔4)-linked d-glucosamine. COS can be prepared from the deacetylation and hydrolysis of chitin, which is commonly found in the exoskeletons of arthropods and insects and the cell walls of fungi. COS is water soluble, non-cytotoxic, readily absorbed through the intestine and mainly excreted in the urine. Of particular importance, COS and its derivatives have been demonstrated to possess several biological activities including anti-inflammation, immunostimulation, anti-tumor, anti-obesity, anti-hypertension, anti-Alzheimer's disease, tissue regeneration promotion, drug and DNA delivery enhancement, anti-microbial, anti-oxidation and calcium-absorption enhancement. The mechanisms of actions of COS have been found to involve the modulation of several important pathways including the suppression of nuclear factor kappa B (NF-κB) and mitogen-activated protein kinases (MAPK) and the activation of AMP-activated protein kinase (AMPK). This review summarizes the current knowledge of the preparation methods, pharmacokinetic profiles, biological activities, potential therapeutic applications and safety profiles of COS and its derivatives. In addition, future research directions are discussed.
壳寡糖（COS）是β-（1→4）-连接的 D-葡萄糖胺的低聚物。COS 可通过甲壳素的脱乙酰化和水解制备，甲壳素普遍存在于节肢动物和昆虫的外骨骼以及真菌的细胞壁中。COS 水溶性好，无细胞毒性，可通过肠道吸收，主要通过尿液排泄。特别重要的是，COS 及其衍生物已被证明具有多种生物活性，包括抗炎、免疫刺激、抗肿瘤、抗肥胖、降血压、抗阿尔茨海默病、促进组织再生、增强药物和 DNA 传递、抗菌、抗氧化和促进钙吸收。COS 的作用机制涉及调节几个重要途径，包括抑制核因子 κB（NF-κB）和丝裂原活化蛋白激酶（MAPK）以及激活 AMP 激活蛋白激酶（AMPK）。本综述总结了 COS 及其衍生物的制备方法、药代动力学特征、生物活性、潜在治疗应用和安全性的最新知识。此外，还讨论了未来的研究方向。
