Suleria Hafiz Ansar Rasul, Hines Barney M, Addepalli Rama, Chen Wei, Masci Paul, Gobe Glenda, Osborne Simone A
School of Medicine, The University of Queensland, Translational Research Institute, Kent Street, Woolloongabba 4102, Australia.
CSIRO Agriculture, 306 Carmody Road, St Lucia 4067, Australia.
Mar Drugs. 2016 Dec 31;15(1):8. doi: 10.3390/md15010008.
Waste generated from the processing of marine organisms for food represents an underutilized resource that has the potential to provide bioactive molecules with pharmaceutical applications. Some of these molecules have known anti-thrombotic and anti-coagulant activities and are being investigated as alternatives to common anti-thrombotic drugs, like heparin and warfarin that have serious side effects. In the current study, extracts prepared from blacklip abalone () processing waste, using food grade enzymes papain and bromelain, were found to contain sulphated polysaccharide with anti-thrombotic activity. Extracts were found to be enriched with sulphated polysaccharides and assessed for anti-thrombotic activity through heparin cofactor-II (HCII)-mediated inhibition of thrombin. More than 60% thrombin inhibition was observed in response to 100 μg/mL sulphated polysaccharides. Anti-thrombotic potential was further assessed as anti-coagulant activity in plasma and blood, using prothrombin time (PT), activated partial thromboplastin time (aPTT), and thromboelastography (TEG). All abalone extracts had significant activity compared with saline control. Anion exchange chromatography was used to separate extracts into fractions with enhanced anti-thrombotic activity, improving HCII-mediated thrombin inhibition, PT and aPTT almost 2-fold. Overall this study identifies an alternative source of anti-thrombotic molecules that can be easily processed offering alternatives to current anti-thrombotic agents like heparin.
将海洋生物加工成食品过程中产生的废物是一种未充分利用的资源，有潜力提供具有药物应用价值的生物活性分子。其中一些分子具有已知的抗血栓和抗凝血活性，正作为常见抗血栓药物（如肝素和华法林，它们有严重副作用）的替代品进行研究。在本研究中，利用食品级酶木瓜蛋白酶和菠萝蛋白酶从黑唇鲍鱼加工废料中制备的提取物，被发现含有具有抗血栓活性的硫酸化多糖。提取物富含硫酸化多糖，并通过肝素辅因子II（HCII）介导的凝血酶抑制作用评估其抗血栓活性。在100μg/mL硫酸化多糖作用下，观察到超过60%的凝血酶抑制率。通过使用凝血酶原时间（PT）、活化部分凝血活酶时间（aPTT）和血栓弹力图（TEG），进一步评估抗血栓潜力作为血浆和血液中的抗凝血活性。与生理盐水对照相比，所有鲍鱼提取物都具有显著活性。使用阴离子交换色谱法将提取物分离成具有增强抗血栓活性的级分，使HCII介导的凝血酶抑制、PT和aPTT提高了近2倍。总体而言，本研究确定了一种抗血栓分子的替代来源，这种来源易于加工，可为肝素等当前抗血栓药物提供替代品。
