Systems Biology and Medicine Center for Complex Diseases, Affiliated Hospital of Qingdao University, Qingdao, China.
Systems Biology and Medicine Center for Complex Diseases, Affiliated Hospital of Qingdao University, Qingdao, China.
Prog Mol Biol Transl Sci. 2019;163:113-134. doi: 10.1016/bs.pmbts.2019.02.006. Epub 2019 Mar 26.
A large proportion of all life on Earth lives in the ocean. Marine life includes microscopic life, plants, algae, invertebrates, fungi, and vertebrates. Due to the high salinity, high pressure, hypoxic and low temperature of the marine environment, the polysaccharides or glycans synthesized by marine life have diverse structures and unique biological activities that are not found in glycans in terrestrial life. Moreover, the glycans are the most abundant biopolymers made by the marine life. The reported activities of marine glycans include but not limit to anticoagulant, antithrombotic, antitumor, antioxidant, antiviral, and antibacterial activities. Published reports on marine glycans have increased more than threefold during the past decade. Meanwhile, several pharmaceutical companies in different countries have invested in the research and development of marine glycan-based drugs. Propylene glycol alginate sodium sulfate (PSS), the first marine glycan-based drug developed in China approved by the Chinese FDA, has been used in the treatment of cardiovascular and other diseases for more than 30 years. In this chapter, the structural characteristics, pharmacological activities and clinical applications of three Chinese FDA approved and commercially available marine glycan-based drugs (PSS, PGMS, and FPS) and five marine glycan-based drugs at different stages of clinical studies (GV971, 911, PGS, PS916, and HS203) in China will be reviewed and discussed. Understanding the marine glycan-based drugs at structure and function level would be needed to comprehend their clinical efficacy. Such knowledge will provide molecular basis for the future research and development of marine glycan-based drugs world widely.
地球上很大一部分生命都生活在海洋中。海洋生物包括微生物、植物、藻类、无脊椎动物、真菌和脊椎动物。由于海洋环境的高盐度、高压、缺氧和低温，海洋生物合成的多糖或糖胺聚糖具有不同的结构和独特的生物活性，这些活性在陆地生物的糖胺聚糖中是找不到的。此外，糖胺聚糖是海洋生物中最丰富的生物聚合物。已报道的海洋糖胺聚糖的活性包括但不限于抗凝、抗血栓、抗肿瘤、抗氧化、抗病毒和抗菌活性。在过去十年中，关于海洋糖胺聚糖的报道增加了两倍多。与此同时，不同国家的几家制药公司已经投资于海洋糖基药物的研究和开发。藻酸丙二醇酯磺酸钠（PSS）是中国第一个获得中国 FDA 批准的基于海洋糖的药物，已用于治疗心血管等疾病 30 多年。在本章中，将对三种已获中国 FDA 批准并商业化的基于海洋糖的药物（PSS、PGMS 和 FPS）和五种处于不同临床研究阶段的基于海洋糖的药物（GV971、911、PGS、PS916 和 HS203）的结构特征、药理活性和临床应用进行综述和讨论。了解基于海洋糖的药物的结构和功能水平将有助于理解其临床疗效。这些知识将为未来全球海洋糖基药物的研究和开发提供分子基础。
