Human Physiology and Unit of Dietetic and Sports Medicine Section, Department of Experimental Medicine, School of Medicine, University of Campania Luigi Vanvitelli, 80138 Naples, Italy.
Department of Experimental Medicine, Biotechnology and Molecular Biology Section, School of Medicine, University of Campania Luigi Vanvitelli, 80138 Naples, Italy.
Cells. 2021 Feb 16;10(2):403. doi: 10.3390/cells10020403.
Brown-like adipocytes can be induced in white fat depots by a different environmental or drug stimuli, known as "browning" or "beiging". These brite adipocytes express thermogenin UCP1 protein and show different metabolic advantages, such as the ability to acquire a thermogenic phenotype corresponding to standard brown adipocytes that counteracts obesity. In this research, we evaluated the effects of several browning agents during white adipocyte differentiation of bone marrow-derived mesenchymal stromal cells (MSCs). Our in vitro findings identified two compounds that may warrant further in vivo investigation as possible anti-obesity drugs. We found that rosiglitazone and sildenafil are the most promising drug candidates for a browning treatment of obesity. These drugs are already available on the market for treating diabetes and erectile dysfunction, respectively. Thus, their off-label use may be contemplated, but it must be emphasized that some severe side effects are associated with use of these drugs.
棕色样脂肪细胞可以在白色脂肪组织中被不同的环境或药物刺激诱导产生,这种现象被称为“褐色化”或“米色化”。这些 brite 脂肪细胞表达解偶联蛋白 1(UCP1)蛋白,并表现出不同的代谢优势,例如能够获得与标准棕色脂肪细胞相对应的产热表型,从而对抗肥胖。在这项研究中,我们评估了几种褐色化诱导剂在骨髓间充质干细胞(MSCs)向白色脂肪细胞分化过程中的作用。我们的体外研究结果确定了两种可能具有进一步体内研究价值的化合物,它们可能是治疗肥胖症的潜在药物。我们发现罗格列酮和西地那非是治疗肥胖症褐色化的最有前途的药物候选物。这两种药物分别已被批准用于治疗糖尿病和勃起功能障碍。因此,可以考虑将其超适应证使用,但必须强调的是,这些药物的使用可能会带来一些严重的副作用。