Carmody Jill S, Ahmad Nadia N, Machineni Sriram, Lajoie Scott, Kaplan Lee M
Obesity, Metabolism, and Nutrition Institute and Gastrointestinal Unit (J.S.C., N.N.A., S.M., S.L., L.M.K.), Massachusetts General Hospital, Boston, Massachusetts 02114; and Department of Medicine (J.S.C., N.N.A., S.M., L.M.K.), Harvard Medical School, Boston, Massachusetts 02115.
Endocrinology. 2015 Sep;156(9):3183-91. doi: 10.1210/en.2015-1226. Epub 2015 Jun 11.
Roux-en-Y gastric bypass (RYGB) typically leads to substantial, long-term weight loss (WL) and diabetes remission, although there is a wide variation in response to RYGB among individual patients. Defining the pathways through which RYGB works should aid in the development of less invasive anti-obesity treatments, whereas identifying weight-regulatory pathways unengaged by RYGB could facilitate the development of therapies that complement the beneficial effects of surgery. Activation of serotonin 2C receptors (5-HT2CR) by serotonergic drugs causes WL in humans and animal models. 5-HT2CR are located on neurons that activate the melanocortin-4 receptors, which are essential for WL after RYGB. We therefore sought to determine whether 5-HT2CR signaling is also essential for metabolic effects of RYGB or whether it is a potentially complementary pathway, the activation of which could extend the benefits of RYGB. Diet-induced obese male mice deficient for the 5-HT2CR and their wild-type littermates underwent RYGB or sham operation. Both groups lost similar amounts of weight after RYGB, demonstrating that the improved metabolic phenotype after RYGB is 5-HT2CR independent. Consistent with this hypothesis, wild-type RYGB-treated mice lost additional weight after the administration of the serotonergic drugs fenfluramine and meta-chlorophenylpiperazine but not the nonserotonergic agent topiramate. The fact that RYGB does not depend on 5-HT2CR signaling suggests that there are important WL mechanisms not fully engaged by surgery that could potentially be harnessed for medical treatment. These results suggest a rational basis for designing medical-surgical combination therapies to optimize clinical outcomes by exploiting complementary physiological mechanisms of action.
Roux-en-Y胃旁路术(RYGB)通常会导致显著的长期体重减轻(WL)和糖尿病缓解,尽管个体患者对RYGB的反应存在很大差异。明确RYGB起作用的途径应有助于开发侵入性较小的抗肥胖治疗方法,而识别RYGB未涉及的体重调节途径则可能促进补充手术有益效果的疗法的开发。血清素能药物激活血清素2C受体(5-HT2CR)会导致人类和动物模型体重减轻。5-HT2CR位于激活黑皮质素-4受体的神经元上,而黑皮质素-4受体对于RYGB术后的体重减轻至关重要。因此,我们试图确定5-HT2CR信号传导对于RYGB的代谢作用是否也至关重要,或者它是否是一种潜在的互补途径,激活该途径可能会扩展RYGB的益处。对缺乏5-HT2CR的饮食诱导肥胖雄性小鼠及其野生型同窝小鼠进行RYGB或假手术。两组在RYGB术后体重减轻量相似,表明RYGB术后改善的代谢表型不依赖于5-HT2CR。与这一假设一致,野生型RYGB治疗的小鼠在给予血清素能药物芬氟拉明和间氯苯哌嗪后体重进一步减轻,但给予非血清素能药物托吡酯后体重未减轻。RYGB不依赖于5-HT2CR信号传导这一事实表明,存在手术未充分涉及的重要体重减轻机制,这些机制可能潜在地用于医学治疗。这些结果为设计药物 - 手术联合疗法提供了合理依据,通过利用互补的生理作用机制来优化临床结果。