State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College and Beijing Key Laboratory of Drug Target and Screening Research, Beijing 100050, China.
Beijing Obstetrics and Gynecology Hospital, Capital Medical University, Beijing 100026, China.
Chin J Nat Med. 2020 Nov;18(11):803-817. doi: 10.1016/S1875-5364(20)60021-8.
Excess accumulation of white adipose tissue (WAT) causes obesity which is an imbalance between energy intake and energy expenditure. Obesity is a serious concern because it has been the leading causes of death worldwide, including diabetes, stroke, heart disease and cancer. Therefore, uncovering the mechanism of obesity and discovering anti-obesity drugs are crucial to prevent obesity and its complications. Browning, inducing white adipose tissue to brown or beige (brite) fat which is brown-like fat emerging in WAT, becomes an appealing therapeutic strategy for obesity and metabolic disorders. Due to lack of efficacy or intolerable side-effects, the clinical trials that promote brown adipose tissue (BAT) thermogenesis and browning of WAT have not been successful in humans. Obviously, more specific means still need to be developed to activate browning of white adipose tissue. In this review, we summarized seven kinds of natural products (alkaloids, flavonoids, terpenoids, long chain fatty acids, phenolic acids, else and extract) promoting white adipose tissue browning which can ameliorate the metabolic disorders, including obesity, dislipidemia, insulin resistance and diabetes. Since natural products are important drug sources and the browning property plays a significant role in not only obesity treatment but also in type 2 diabetes (T2DM) improvement, natural products of inducing browning may be an irreplaceable drug discovery orientation for obesity, diabetes and even other metabolic disorders.
白色脂肪组织（WAT）过度积累会导致肥胖，这是能量摄入和消耗之间的失衡。肥胖是一个严重的问题，因为它是全球死亡的主要原因，包括糖尿病、中风、心脏病和癌症。因此，揭示肥胖的机制和发现抗肥胖药物对于预防肥胖及其并发症至关重要。脂肪褐变，诱导白色脂肪组织向棕色或米色（brite）脂肪转化，即 WAT 中出现的棕色样脂肪，成为肥胖和代谢紊乱的一种有吸引力的治疗策略。由于缺乏疗效或不可耐受的副作用，促进棕色脂肪组织（BAT）产热和 WAT 褐变的临床试验在人类中并未成功。显然，仍需要开发更具体的手段来激活白色脂肪组织的褐变。在这篇综述中，我们总结了七种促进白色脂肪组织褐变的天然产物（生物碱、类黄酮、萜类、长链脂肪酸、酚酸、其他和提取物），它们可以改善代谢紊乱，包括肥胖、血脂异常、胰岛素抵抗和糖尿病。由于天然产物是重要的药物来源，褐变特性不仅在肥胖治疗中而且在 2 型糖尿病（T2DM）改善中都起着重要作用，因此诱导褐变的天然产物可能是肥胖、糖尿病甚至其他代谢紊乱的不可替代的药物发现方向。
