Bravo-Nuevo Arturo, Marcy Alice, Huang Minzhou, Kappler Frank, Mulgrew Jennifer, Laury-Kleintop Lisa, Reichman Melvin, Tobia Annette, Prendergast George C
Lankenau Institute for Medical Research (LIMR), Wynnewood, Pennsylvania, United States of America.
Dynamis Pharmaceuticals Co. Inc., Jenkintown, Pennsylvania, United States of America.
PLoS One. 2014 Feb 27;9(2):e90031. doi: 10.1371/journal.pone.0090031. eCollection 2014.
Metabolic syndrome, diabetes and diabetes complications pose a growing medical challenge worldwide, accentuating the need of safe and effective strategies for their clinical management. Here we present preclinical evidence that the sorbitol derivative meglumine (N-methyl-D-glucamine) can safely protect against several features of metabolic syndrome and diabetes, as well as elicit enhancement in muscle stamina. Meglumine is a compound routinely used as an approved excipient to improve drug absorption that has not been ascribed any direct biological effects in vivo. Normal mice (SV129) administered 18 mM meglumine orally for six weeks did not display any gastrointestinal or other observable adverse effects, but had a marked effect on enhancing muscle stamina and at longer times in limiting weight gain. In the established KK.Cg-Ay/J model of non-insulin dependent diabetes, oral administration of meglumine significantly improved glycemic control and significantly lowered levels of plasma and liver triglycerides. Compared to untreated control animals, meglumine reduced apparent diabetic nephropathy. Sorbitol can improve blood glucose uptake by liver and muscle in a manner associated with upregulation of the AMPK-related enzyme SNARK, but with undesirable gastrointestinal side effects not seen with meglumine. In murine myoblasts, we found that meglumine increased steady-state SNARK levels in a dose-dependent manner more potently than sorbitol. Taken together, these findings provide support for the clinical evaluation of meglumine as a low-cost, safe supplement offering the potential to improve muscle function, limit metabolic syndrome and reduce diabetic complications.
代谢综合征、糖尿病及糖尿病并发症在全球范围内对医学构成了日益严峻的挑战,凸显了对其进行临床管理的安全有效策略的需求。在此,我们提供临床前证据表明,山梨醇衍生物葡甲胺(N-甲基-D-葡糖胺)可安全预防代谢综合征和糖尿病的多种特征,并能增强肌肉耐力。葡甲胺是一种常用的经批准的辅料,用于改善药物吸收,在体内尚未发现有任何直接的生物学效应。正常小鼠(SV129)口服18 mM葡甲胺六周后未出现任何胃肠道或其他可观察到的不良反应,但对增强肌肉耐力有显著作用,且在较长时间内可限制体重增加。在已建立的非胰岛素依赖型糖尿病KK.Cg-Ay/J模型中,口服葡甲胺可显著改善血糖控制,并显著降低血浆和肝脏甘油三酯水平。与未治疗的对照动物相比,葡甲胺可减轻明显的糖尿病肾病。山梨醇可通过上调与AMPK相关的酶SNARK的方式改善肝脏和肌肉对血糖的摄取,但会产生葡甲胺未出现的不良胃肠道副作用。在小鼠成肌细胞中,我们发现葡甲胺比山梨醇更有效地以剂量依赖方式增加稳态SNARK水平。综上所述,这些发现为葡甲胺作为一种低成本、安全的补充剂进行临床评估提供了支持,它有可能改善肌肉功能、限制代谢综合征并减少糖尿病并发症。