Institute of Marine Drugs, Guangxi University of Chinese Medicine, Nanning 530200, China.
Guangxi Key Laboratory of Marine Drugs, Guangxi University of Chinese Medicine, Nanning 530200, China.
Mar Drugs. 2023 Feb 24;21(3):148. doi: 10.3390/md21030148.
Echinoderms have been attracting increasing attention for their polysaccharides, with unique chemical structure and enormous potential for preparing drugs to treat diseases. In this study, a glucan (TPG) was obtained from the brittle star . Its structure was elucidated by physicochemical analysis and by analyzing its low-molecular-weight products as degraded by mild acid hydrolysis. The TPG sulfate (TPGS) was prepared, and its anticoagulant activity was investigated for potential development of anticoagulants. Results showed that TPG consisted of a consecutive α1,4-linked D-glucopyranose (D-Glc) backbone together with a α1,4-linked D-Glc disaccharide side chain linked through C-1 to C-6 of the main chain. The TPGS was successfully prepared with a degree of sulfation of 1.57. Anticoagulant activity results showed that TPGS significantly prolonged activated partial thromboplastin time, thrombin time, and prothrombin time. Furthermore, TPGS obviously inhibited intrinsic tenase, with an EC value of 77.15 ng/mL, which was comparable with that of low-molecular-weight heparin (LMWH) (69.82 ng/mL). TPGS showed no AT-dependent anti-FIIa and anti-FXa activities. These results suggest that the sulfate group and sulfated disaccharide side chains play a crucial role in the anticoagulant activity of TPGS. These findings may provide some information for the development and utilization of brittle star resources.
棘皮动物因其多糖而受到越来越多的关注,其具有独特的化学结构,在制备治疗疾病的药物方面具有巨大的潜力。在本研究中,从脆星星体中获得了一种葡聚糖(TPG)。通过物理化学分析和分析其通过温和酸水解降解的低分子量产物来阐明其结构。制备了 TPG 硫酸盐(TPGS),并研究了其抗凝活性,以开发潜在的抗凝剂。结果表明,TPG 由连续的α1,4-连接的 D-葡萄糖(D-Glc)主链和通过主链的 C-1 至 C-6 连接的α1,4-连接的 D-Glc 二糖侧链组成。成功制备了硫酸化度为 1.57 的 TPGS。抗凝活性结果表明,TPGS 显著延长了激活部分凝血活酶时间、凝血酶时间和凝血酶原时间。此外,TPGS 明显抑制内源性凝血酶,EC 值为 77.15ng/mL,与低分子量肝素(LMWH)(69.82ng/mL)相当。TPGS 没有 AT 依赖性抗 FIIa 和抗 FXa 活性。这些结果表明硫酸基团和硫酸化二糖侧链在 TPGS 的抗凝活性中起关键作用。这些发现可能为脆星星体资源的开发和利用提供一些信息。