Levin B E, Dunn-Meynell A A
Neurology Service, Department of Veterans Affairs New Jersey Health Care System, East Orange 07018, USA.
Am J Physiol Regul Integr Comp Physiol. 2000 Dec;279(6):R2222-8. doi: 10.1152/ajpregu.2000.279.6.R2222.
Chronic administration of sibutramine lowers body weight, presumably by altering brain monoamine metabolism. Here the effect of sibutramine on sympathoadrenal function (24-h urine norepinephrine and epinephrine levels) and arcuate nucleus (ARC) neuropeptide Y (NPY) and proopiomelanocortin (POMC) expression was assessed in diet-induced obese rats fed a low-fat diet. Chronic (10 wk) sibutramine [5 mg. kg(-1). day(-1) ip; rats fed ad libitum and injected with sibutramine (AS)] lowered body weight by 15% but only transiently (3-4 wk) reduced intake compared with vehicle-treated controls [rats fed chow ad libitum and injected with vehicle daily (AV)]. Other rats food restricted (RS) to 90% of the weight of AS rats and then given sibutramine restored their body weights to the level of AS rats when allowed libitum food intake. After reequilibration, RS rats were again energy restricted to reduce their weight to 90% of AS rats, and additional vehicle-treated rats (RV) were restricted to keep their body weights at the level of AS rats for 3 wk more. Terminally, total adipose depot weights and leptin levels paralleled body weights (AV > AS = RV > RS), although AS rats had heavier abdominal and lighter peripheral depots than RV rats of comparable body weights. Sibutramine treatment increased sympathetic activity, attenuated the increased ARC NPY, and decreased POMC mRNA levels induced by energy restriction in RV rats. Thus sibutramine lowered the defended body weight in association with compensatory changes in those central pathways involved in energy homeostasis.
西布曲明的长期给药可降低体重,可能是通过改变脑单胺代谢实现的。在此,我们评估了西布曲明对低脂饮食喂养的饮食诱导肥胖大鼠交感肾上腺功能(24小时尿去甲肾上腺素和肾上腺素水平)以及弓状核(ARC)神经肽Y(NPY)和阿黑皮素原(POMC)表达的影响。慢性(10周)给予西布曲明[5毫克·千克⁻¹·天⁻¹,腹腔注射;自由进食并注射西布曲明的大鼠(AS)]可使体重降低15%,但与给予赋形剂处理的对照组[自由进食并每日注射赋形剂的大鼠(AV)]相比,仅短暂(3 - 4周)减少了摄入量。其他大鼠食物限制(RS)至AS大鼠体重的90%,然后给予西布曲明,当允许自由进食时,其体重恢复到AS大鼠的水平。重新平衡后,RS大鼠再次进行能量限制以将体重降至AS大鼠的90%,另外给予赋形剂处理的大鼠(RV)进行限制,使其体重在3周内保持在AS大鼠的水平。最终,尽管体重相当的AS大鼠比RV大鼠腹部脂肪库更重、外周脂肪库更轻,但总脂肪库重量和瘦素水平与体重平行(AV > AS = RV > RS)。西布曲明治疗增加了交感神经活动,减弱了RV大鼠能量限制诱导的ARC NPY增加,并降低了POMC mRNA水平。因此,西布曲明降低了防御体重,并伴有能量稳态相关中枢通路的代偿性变化。