Kumari K, Umar S, Bansal V, Sahib M K
Division of Biochemistry, Central Drug Research Institute, Lucknow, India.
Diabetes. 1991 Aug;40(8):1079-84. doi: 10.2337/diab.40.8.1079.
Mono- and diaminoguanidine inhibited ambient glucose-induced glycosylated end product formation of albumin and collagen 125I-labeled albumin covalent binding in vitro. Diaminoguanidine was a stronger inhibitor than monoaminoguanidine. These compounds also inhibited rat eye lens aldose reductase activity in vitro noncompetitively with respect to NADPH with Ki = 30.6 mM for monoaminoguanidine and Ki = 12.5 mM for diaminoguanidine. When administered daily for 98 days at a dose of 25 mg/kg body wt i.p., both compounds lowered eye lens sorbitol and aldose reductase activity in normoglycemic and alloxan-induced diabetic rats. Again, diaminoguanidine was a better inhibitor. Daily long-term administration of mono- and diaminoguanidine (25 mg/kg body wt i.p.) inhibited and prevented experimental diabetes-induced lens opacity in rats, respectively. It appears that diaminoguanidine has a better therapeutic potential in controlling diabetic complications.
单氨基胍和二氨基胍在体外抑制环境葡萄糖诱导的白蛋白糖基化终产物形成以及125I标记的白蛋白与胶原蛋白的共价结合。二氨基胍是比单氨基胍更强的抑制剂。这些化合物在体外对大鼠眼晶状体醛糖还原酶活性也有抑制作用，对NADPH呈非竞争性抑制，单氨基胍的Ki = 30.6 mM，二氨基胍的Ki = 12.5 mM。当以25 mg/kg体重腹腔注射给药98天时，这两种化合物均可降低正常血糖和四氧嘧啶诱导的糖尿病大鼠眼晶状体山梨醇和醛糖还原酶活性。同样，二氨基胍是更好的抑制剂。每日长期腹腔注射单氨基胍和二氨基胍（25 mg/kg体重）分别抑制并预防了实验性糖尿病诱导的大鼠晶状体混浊。看来二氨基胍在控制糖尿病并发症方面具有更好的治疗潜力。
