Department of Biomolecular Sciences, School of Pharmacy, University of Mississippi, Oxford, MS 38677-1848, USA.
Research Institute of Pharmaceutical Sciences, School of Pharmacy, University of Mississippi, Oxford, MS 38677-1848, USA.
Molecules. 2019 Aug 1;24(15):2803. doi: 10.3390/molecules24152803.
Galactosaminoglycans (GalAGs) are sulfated glycans composed of alternating -acetylgalactosamine and uronic acid units. Uronic acid epimerization, sulfation patterns and fucosylation are modifications observed on these molecules. GalAGs have been extensively studied and exploited because of their multiple biomedical functions. Chondroitin sulfates (CSs), the main representative family of GalAGs, have been used in alternative therapy of joint pain/inflammation and osteoarthritis. The relatively novel fucosylated chondroitin sulfate (FCS), commonly found in sea cucumbers, has been screened in multiple systems in addition to its widely studied anticoagulant action. Biomedical properties of GalAGs are directly dependent on the sugar composition, presence or lack of fucose branches, as well as sulfation patterns. Although research interest in GalAGs has increased considerably over the three last decades, perhaps motivated by the parallel progress of glycomics, serious questions concerning the effectiveness and potential side effects of GalAGs have recently been raised. Doubts have centered particularly on the beneficial functions of CS-based therapeutic supplements and the potential harmful effects of FCS as similarly observed for oversulfated chondroitin sulfate, as a contaminant of heparin. Unexpected components were also detected in CS-based pharmaceutical preparations. This review therefore aims to offer a discussion on (1) the current and potential therapeutic applications of GalAGs, including those of unique features extracted from marine sources, and (2) the potential drawbacks of this class of molecules when applied to medicine.
半乳糖胺聚糖（GalAGs）是由交替的乙酰半乳糖胺和糖醛酸单元组成的硫酸化聚糖。在这些分子上观察到糖醛酸差向异构化、硫酸化模式和岩藻糖基化修饰。GalAGs 因其多种生物医学功能而被广泛研究和利用。硫酸软骨素（CSs）是 GalAGs 的主要代表家族，已被用于关节疼痛/炎症和骨关节炎的替代疗法。相对较新的岩藻糖基硫酸软骨素（FCS），常见于海参中，除了广泛研究的抗凝作用外，还在多个系统中进行了筛选。GalAGs 的生物医学特性直接取决于糖组成、是否存在岩藻糖支链以及硫酸化模式。尽管过去三十年来对 GalAGs 的研究兴趣显著增加，或许是受到糖组学的平行进展的推动，但最近对 GalAGs 的有效性和潜在副作用提出了严重质疑。人们的疑虑主要集中在基于 CS 的治疗性补充剂的有益功能以及 FCS 的潜在有害作用上，就像观察到肝素污染物过度硫酸化的软骨素一样。在基于 CS 的药物制剂中也检测到了意想不到的成分。因此，本综述旨在讨论（1）GalAGs 的当前和潜在治疗应用，包括从海洋来源提取的独特特征，以及（2）当将此类分子应用于医学时的潜在缺点。
