Study on the development of anti-diabetic-complications having anti-glycation and antioxidant activities

具有抗糖化和抗氧化活性的抗糖尿病并发症的研究进展

• 批准号: 13672312
• 负责人: MIWA Ichitomo
• 金额: $ 2.3万
• 依托单位: Meijo University
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 2001
• 资助国家: 日本
• 起止时间: 2001 至 2003
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-13672312/
• 关键词: pyridoxal-aminoguanidine adduct; aminoguanidine; diabetic complication; diabetic nephropathy; diabetic neuropathy; diabetic cataract; antioxidant activity; 非酵素的糖化; 糖尿病合併症治療薬; 糖尿病治療薬

1.We compared the inhibitory effect of PL-AG, pyridoxal-aminoguanidine Schiff base, developed by us on nephropathy of diabetic mice with that of aminoguanidine (AG) known as a promising candidate for anti-diabetic-complications. Various parameters such as urinary albumin excretion rate, urine volume, and mesangial volume were improved more markedly by PL-AG than by AG, indicating that PL-AG is superior to AG in preventing diabetic nephropathy.2.PL-AG was more potent than other compounds such as AG, pyridoxamine, and pyridoxal in in vitro antioxidant activity. In vivo antioxidant activity of PL-AG in diabetic rats was also greater than that of AG. PL-AG was found to act as an antioxidant by reacting with reactive oxygen species to yield a stable oxidized form of PL-AG and by chelating Axansition metal ions.4.PL-AG did not show any ameliorating effect on the development of diabetes in Goto-Kakizaki rats, a model rat of type 2 diabetes.

1.比较了吡哆醛-氨基胍Schiff碱（PL-AG）和氨基胍（AG）对糖尿病小鼠肾病的抑制作用。PL-AG对尿白蛋白排泄率、尿量和系膜体积等各项参数的改善作用均优于AG，表明PL-AG在预防糖尿病肾病方面上级AG。2.PL-AG的体外抗氧化活性优于AG、吡多胺和吡多醛等其他化合物。PL-AG在糖尿病大鼠体内的抗氧化活性也大于AG。PL-AG通过与活性氧反应生成稳定的氧化型PL-AG和螯合金属离子而发挥抗氧化作用。4.PL-AG对2型糖尿病模型大鼠Goto-Kakizaki大鼠的糖尿病发展没有任何改善作用。

项目成果

H.Miyoshi, T.Taguchi et al.: "Aminoguanidine pyridoxal adduct is superior to aminoguanidine for preventing diabetic nephropathy in mice"Horm.Metab.Res.. 34. 371-377 (2002)

H.Miyoshi、T.Taguchi 等人：“氨基胍吡哆醛加合物在预防小鼠糖尿病肾病方面优于氨基胍”Horm.Metab.Res.. 34. 371-377 (2002)

A.-S.Chen, T.Taguchi et al.: "Pyridoxal-aminoguanidine adduct is more effective than aminoguanidine in preventing neuropathy and cataract in diabetic rats"Horm.Metab.Res.. 36. 183-187 (2004)

A.-S.Chen、T.Taguchi 等人：“吡哆醛-氨基胍加合物在预防糖尿病大鼠的神经病变和白内障方面比氨基胍更有效”Horm.Metab.Res.. 36. 183-187 (2004)

H.Miyoshi, T.Taguchi, I.Miwa, T.Koike その他: "Aminoguanidine Pyridoxal Adduct is Superior to Aminoguanidine for Preventing Diabetic Nephropathy in Mice"Hormone & Metabolic Research. 34. 371-377 (2002)

H.Miyoshi、T.Taguchi、I.Miwa、T.Koike 等人：“氨基胍吡哆醛加合物在预防小鼠糖尿病肾病方面优于氨基胍”《激素与代谢研究》34. 371-377 (2002)。