Kuchmerovskaia T M, Parkhomets P K, Donchenko G V, Obrosova I G, Klimenko A P, Kuchmerovskiĭ N A, Pakirbaeva L V, Efimov A S
Institute of Biochemistry, Kiev.
Vopr Med Khim. 1998 Nov-Dec;44(6):559-64.
Streptosotocin-induced diabetes in rats is accompanied by the development of diabetic complications such as neuropathies. [2-14C]serotonin and [U-14C]GABA release from the neurotransmitter pre-loaded synaptosomes showed significant elevation. Aldose reductase inhibitors (AL-1576, sorbinil) administration leads to partial restoration of serotonin and GABA release, while picamilon restored only GABA release. It was shown that Na+,K(+)-ATPase activities decreased in synaptosomes, synaptic membranes and sciatic nerve of diabetic rats compared to control. Administration of AL-1576 normalized Na+, K(+)-ATPase activity, while sorbinil and picamilon less effectively. Sorbitol level are increased in streptozotocin-diabetic rats as compared to control. The picamilon and aldose reductase inhibitors administration to diabetic rats is accompanied by the partial reduction of brain sorbitol level. The findings confirm the important role of picamilon and aldose reductase inhibitors in the prevention and treatment of diabetic neuropathy.
链脲佐菌素诱导的大鼠糖尿病伴有糖尿病并发症的发展，如神经病变。从预先加载神经递质的突触体中释放的[2-¹⁴C]血清素和[U-¹⁴C]γ-氨基丁酸显示出显著升高。给予醛糖还原酶抑制剂（AL-1576、索比尼尔）可使血清素和γ-氨基丁酸的释放部分恢复，而匹卡米隆仅能恢复γ-氨基丁酸的释放。结果表明，与对照组相比，糖尿病大鼠的突触体、突触膜和坐骨神经中的Na⁺，K⁺-ATP酶活性降低。给予AL-1576可使Na⁺，K⁺-ATP酶活性恢复正常，而索比尼尔和匹卡米隆的效果较差。与对照组相比，链脲佐菌素诱导的糖尿病大鼠的山梨醇水平升高。给糖尿病大鼠施用匹卡米隆和醛糖还原酶抑制剂可使脑山梨醇水平部分降低。这些发现证实了匹卡米隆和醛糖还原酶抑制剂在预防和治疗糖尿病神经病变中的重要作用。
