Classification of Therapeutic and Experimental Drugs for Brown Adipose Tissue Activation: Potential Treatment Strategies for Diabetes and Obesity.
Classification of Therapeutic and Experimental Drugs for Brown Adipose Tissue Activation: Potential Treatment Strategies for Diabetes and Obesity.
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DOI：
10.2174/1573399812666160517115450
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发表时间：
2016
影响因子：
3.3
通讯作者：
Schade KN
中科院分区：
文献类型：
--
作者：
Mukherjee J;Baranwal A;Schade KN
在动物和人类中，褐色脂肪组织（BAT）的药理激活在治疗肥胖和糖尿病方面的潜在应用正在不断增加。我们和其他人已经报道了一些使用实验性或治疗性药物的动物研究。现在有人正在努力将这些发现转化为人类研究。本综述的目的是评估目前使用的具有BAT激活潜力的各种药物。根据药物的作用机制将其分为4类。第一类药物包括β3肾上腺素能受体激动剂用于BAT激活。第二类药物包括影响去甲肾上腺素水平和激活BAT的药物，具有减少肥胖的潜力。第3类包括过氧化物酶体增殖体激活受体-γ的激活剂，用于降血糖、减肥和糖尿病；最后4类包括天然产物和其他新兴药物，但关于BAT激活及其对糖尿病和减肥的影响的信息有限。第1类药物是高BAT激活剂，其次是第2类和第3类。其中一些药物现已扩展到糖尿病和肥胖动物模型以及人类BAT研究中。第3类药物在临床上用于治疗2型糖尿病，但BAT的参与程度尚不清楚。进一步研究这些药物对糖尿病的疗效，并利用无创成像技术测量其对BAT激活的影响，将有助于确立BAT的临床作用。
Increasing efforts are being made towards pharmacologic activation of brown adipose tissue (BAT) in animals and humans for potential use in the treatment of obesity and diabetes. We and others have reported a number of animal studies using either experimental or therapeutic drugs. There are now efforts to translate these findings to human studies. The goal of this review is to evaluate the various drugs currently being used that have the potential for BAT activation. Drugs were classified into 4 classes based on their mechanism of action. Class 1 drugs include the use of β3 adrenoceptor agonists for BAT activation. Class 2 drugs include drugs that affect norepinephrine levels and activate BAT with the potential of reducing obesity. Class 3 includes activators of peroxisome proliferator-activated receptor-γ in pursuit of lowering blood sugar, weight loss and diabetes and finally Class 4 includes natural products and other emerging drugs with limited information on BAT activation and their effects on diabetes and weight loss. Class 1 drugs are high BAT activators followed by Class 2 and 3. Some of these drugs have now been extended to diabetes and obesity animal models and human BAT studies. Drugs in Class 3 are used clinically for Type 2 diabetes, but the extent of BAT involvement is unclear. Further studies on the efficacy of these drugs in diabetes and measuring their effects on BAT activation using noninvasive imaging will help in establishing a clinical role of BAT.