Japan Tobacco, Central Pharmaceutical Research Institute, Biological/Pharmacological Research Laboratories, 1-1 Murasaki-cho, Takatsuki,Osaka, Japan.
Diabetes Obes Metab. 2009 Nov;11(11):1084-7. doi: 10.1111/j.1463-1326.2009.01082.x. Epub 2009 Jul 13.
Spontaneously Diabetic Torii (SDT) rat shows severe ocular complications such as tractional retinal detachment. In the present study, effect of protein kinase C beta (PKCbeta) inhibitor JTT-010 was evaluated to clarify the involvement of PKCbeta in complications of SDT rat. SDT rats were administered JTT-010 (10 or 50 mg/kg/day) for 48 weeks. SDT rats showed delayed oscillatory potentials in electroretinogram. Delayed motor nerve conduction velocity, decreased coefficients of variation of R-R intervals in electrocardiogram and thermal hypoalgesia were also observed. These functional disorders were prevented by administration of JTT-010. Abnormal retinal vascular was formed and the optic disc was protruded in SDT rat; however, JTT-010 did not prevent these hyperglycaemia-induced retinal abnormalities. These findings indicate that PKCbeta is intimately involved in diabetic complications; however, it seems that other factor(s) are primary contributors to histopathological abnormalities in retina. Therefore, PKCbeta inhibitors require concurrent administration of antihyperglycaemic drugs to achieve maximum effect on diabetic complications.
自发性糖尿病 Torii (SDT) 大鼠表现出严重的眼部并发症,如牵引性视网膜脱离。在本研究中,评估了蛋白激酶 Cβ(PKCβ)抑制剂 JTT-010 的作用,以阐明 PKCβ在 SDT 大鼠并发症中的作用。SDT 大鼠给予 JTT-010(10 或 50mg/kg/天)48 周。SDT 大鼠在视网膜电图中表现出延迟的振荡电位。运动神经传导速度延迟、心电图 R-R 间期变异系数降低和热痛觉减退也观察到。这些功能障碍通过 JTT-010 的给药得到预防。SDT 大鼠形成异常的视网膜血管,视盘突出;然而,JTT-010 并不能预防这些高血糖引起的视网膜异常。这些发现表明 PKCβ 密切参与糖尿病并发症;然而,似乎其他因素是视网膜组织病理学异常的主要原因。因此,PKCβ 抑制剂需要与抗高血糖药物联合使用,以达到对糖尿病并发症的最大效果。