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肥胖症:代谢性疾病,药物发现与天然产物研究进展

Obesity: The Metabolic Disease, Advances on Drug Discovery and Natural Product Research.

作者信息

Castro Mafalda, Preto Marco, Vasconcelos Vitor, Urbatzka Ralph

机构信息

Interdisciplinary Centre of Marine and Environmental Research (CIIMAR/CIMAR), Rua dos Bragas 289, 4050-123 Porto, Portugal.

出版信息

Curr Top Med Chem. 2016;16(23):2577-604. doi: 10.2174/1568026616666160415155644.

DOI:10.2174/1568026616666160415155644
PMID:27086785
Abstract

Obesity is a global health threat. OECD reported that more than half (52%) of the adult population in the European Union is overweight or obese. Obesity and obesity-related co-morbidities have deep negative effects on morbidity, mortality, professional and personal quality of life. Healthcare costs represent a negative impact of this disease, with an associated economic cost of 100 billion US$ per year in the United States. The most prescribed drugs for obesity treatment worldwide are orlistat, and phentermine/topiramate extended release, while the major prescribed drug for the same disease in the US are exenatide and dapagliflozin. The so far developed drugs, targeting weight loss, have a long history of malignant secondary effects. There is still a lack of efficient and safe drugs to treat obesity and related metabolic complications since in many cases cure cannot be reached by bariatric surgery or healthy lifestyle habits. Terrestrial and aquatic organisms are a promising source of valuable, bioactive compounds, often with interest for human health. Some of the natural compounds or organisms have been used for centuries by humans as traditional medicine foods. In this review, we give insights into the adipose tissue function and development, and the progress in traditional anti-obesity pharmacotherapy. A major focus is to highlight the state of the art of natural compounds with anti-obesity properties and their potential as candidates for drug development; an overview is given about natural compounds derived from different marine animal sources, cyanobacteria, marine phytoplankton, fungus or plants.

摘要

肥胖是一种全球性的健康威胁。经济合作与发展组织(OECD)报告称,欧盟超过一半(52%)的成年人口超重或肥胖。肥胖及与肥胖相关的合并症对发病率、死亡率、职业和个人生活质量都有严重的负面影响。医疗成本是这种疾病的一个负面影响,在美国,其相关经济成本每年达1000亿美元。全球最常被处方用于治疗肥胖的药物是奥利司他以及缓释型苯丁胺/托吡酯,而在美国,治疗同一疾病最常被处方的药物是艾塞那肽和达格列净。迄今为止研发的旨在减肥的药物,长期以来都有恶性副作用的历史。由于在许多情况下,减肥手术或健康的生活方式习惯无法实现治愈,因此仍然缺乏有效且安全的药物来治疗肥胖及相关代谢并发症。陆地和水生生物是有价值的生物活性化合物的一个有前景的来源,这些化合物通常对人类健康有益。一些天然化合物或生物已被人类用作传统药用食物达几个世纪之久。在本综述中,我们深入探讨了脂肪组织的功能与发育,以及传统抗肥胖药物治疗的进展。一个主要重点是突出具有抗肥胖特性的天然化合物的最新研究状况及其作为药物开发候选物的潜力;概述了源自不同海洋动物来源、蓝细菌、海洋浮游植物、真菌或植物的天然化合物。

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