Lin Ping, Shen Nuo, Yin Fan, Guo Shou-Dong
Institute of Lipid Metabolism and Atherosclerosis, Innovative Drug Research Centre, School of Pharmacy, Weifang Medical University, Weifang, China.
Front Pharmacol. 2022 Sep 14;13:1000315. doi: 10.3389/fphar.2022.1000315. eCollection 2022.
Dyslipidemias are disorders of plasma levels of lipids, such as elevated levels of total cholesterol and triglyceride, that are associated with various human diseases including cardiovascular disease (CVD) and non-alcoholic fatty liver disease (NAFLD). Statins are the first-line drugs for treatment of dyslipidemia. However, a substantial proportion of patients cannot reach the recommended LDL-c level even with the highest tolerated doses of statins, and there is no available drug specifically for NAFLD therapy. Sea cucumbers are one of the widely distributed invertebrates, and are an important resource of food and medicine. Sea cucumbers have many valuable nutrients including saponins, fatty acids, phospholipids, cerebrosides, sulfated polysaccharides, as well as proteins and peptides. In recent years, these natural products derived from sea cucumbers have attracted attentions for treatment of CVD and NAFLD because of their lipid-lowering effect and low toxicity. However, the hypolipidemic mechanisms of action and the structure-activity relationship of these bioactive components have not been well-documented in literature. This review article summarizes the signaling pathways and the potential structure-activity relationship of sea cucumber-derived bioactive compounds including saponins, lipids, carbohydrates as well as peptides and proteins. This article will provide information useful for the development of sea cucumber-derived lipid-lowering compounds as well as for investigation of hypolipidemic compounds that are derived from other natural resources.
血脂异常是指血浆脂质水平紊乱,如总胆固醇和甘油三酯水平升高,与包括心血管疾病(CVD)和非酒精性脂肪性肝病(NAFLD)在内的多种人类疾病相关。他汀类药物是治疗血脂异常的一线药物。然而,即使使用最高耐受剂量的他汀类药物,仍有相当一部分患者无法达到推荐的低密度脂蛋白胆固醇(LDL-c)水平,并且目前尚无专门用于治疗NAFLD的药物。海参是广泛分布的无脊椎动物之一,是重要的食物和药物资源。海参含有许多有价值的营养成分,包括皂苷、脂肪酸、磷脂、脑苷脂、硫酸化多糖以及蛋白质和肽。近年来,这些源自海参的天然产物因其降脂作用和低毒性而在治疗CVD和NAFLD方面受到关注。然而,这些生物活性成分的降血脂作用机制和构效关系在文献中尚未得到充分记载。这篇综述文章总结了海参衍生的生物活性化合物(包括皂苷、脂质、碳水化合物以及肽和蛋白质)的信号通路和潜在的构效关系。本文将为开发源自海参的降脂化合物以及研究源自其他自然资源的降血脂化合物提供有用信息。