Beales P E, Hawa M, Williams A J, Albertini M C, Giorgini A, Pozzilli P
Department of Diabetes and Metabolism, St. Bartholomew's Hospital, London, UK.
Acta Diabetol. 1995 Mar;32(1):53-6. doi: 10.1007/BF00581047.
Glutamic acid decarboxylase (GAD) is the enzyme responsible for the synthesis of gamma-aminobutyric acid (GABA). GAD has been identified as a 64-kDa antigen expressed in pancreatic beta-cells, to which autoantibodies are generated prior to the onset of type 1 (insulin-dependent) diabetes mellitus. GAD may therefore be an initiating factor in beta-cell destruction. We administered baclofen, a GABA-B receptor agonist, to non-obese diabetic (NOD) mice in an attempt to down-regulate GAD expression and thereby reduce the incidence of diabetes. Twenty-four female NOD mice were given baclofen in their drinking water at a final dose of 50 mg/kg body weight daily from weaning to 30 weeks of age. Twenty-four sex- and litter-matched mice were used as controls. At 30 weeks there was no difference in the incidence of diabetes in the treated group compared with the controls. However, there was a significant delay in the onset of diabetes in the treated group (P < 0.001, parallelism test). The degree of insulitis and the GAD activity in the pancreas per mg of protein were unchanged by baclofen treatment with respect to controls. These results suggest that baclofen may be effective in delaying diabetes onset in NOD mice by stimulating GABA activity, as this neurotransmitter, localised in the islets, may modulate insulin secretion and the antigen expression associated with it.
谷氨酸脱羧酶(GAD)是负责合成γ-氨基丁酸(GABA)的酶。GAD已被鉴定为一种在胰腺β细胞中表达的64 kDa抗原,在1型(胰岛素依赖型)糖尿病发病之前会产生针对该抗原的自身抗体。因此,GAD可能是β细胞破坏的起始因素。我们给非肥胖糖尿病(NOD)小鼠施用了巴氯芬(一种GABA-B受体激动剂),试图下调GAD表达,从而降低糖尿病的发病率。从断奶到30周龄,给24只雌性NOD小鼠饮用含巴氯芬的水,最终剂量为每日50 mg/kg体重。将24只性别和同窝匹配的小鼠用作对照。在30周时,与对照组相比,治疗组的糖尿病发病率没有差异。然而,治疗组的糖尿病发病明显延迟(P < 0.001,平行性检验)。与对照组相比,巴氯芬治疗对每毫克蛋白质胰腺中的胰岛炎程度和GAD活性没有影响。这些结果表明,巴氯芬可能通过刺激GABA活性有效延迟NOD小鼠的糖尿病发病,因为这种位于胰岛中的神经递质可能调节胰岛素分泌及其相关的抗原表达。