Garay Ricardo P, Hannaert Patrick, Chiavaroli Carlo
Equipe d'Accueil EA2381, Laboratoire Pharmacologie Transports Ioniques Membranaires, Université Paris 7, Paris, France.
Treat Endocrinol. 2005;4(4):221-32. doi: 10.2165/00024677-200504040-00003.
The incidence of diabetic retinopathy is still increasing in developed countries. Tight glycemic control and laser therapy reduce vision loss and blindness, but do not reverse existing ocular damage and only slow the progression of the disease. New pharmacologic agents that are currently under development and are specifically directed against clearly defined biochemical targets (i.e. aldose reductase inhibitors and protein kinase C-beta inhibitors) have failed to demonstrate significant efficacy in the treatment of diabetic retinopathy in clinical trials. In contrast, calcium dobesilate (2,5-dihydroxybenzenesulfonate), which was discovered more than 40 years ago and is registered for the treatment of diabetic retinopathy in more than 20 countries remains, to our knowledge, the only angioprotective agent that reduces the progression of this disease. An overall review of published studies involving calcium dobesilate (CLS 2210) depicts a rather 'non-specific' compound acting moderately, but significantly, on the various and complex disorders that contribute to diabetic retinopathy. Recent studies have shown that calcium dobesilate is a potent antioxidant, particularly against the highly damaging hydroxyl radical. In addition, it improves diabetic endothelial dysfunction, reduces apoptosis, and slows vascular cell proliferation.
在发达国家,糖尿病视网膜病变的发病率仍在上升。严格的血糖控制和激光治疗可减少视力丧失和失明,但无法逆转已有的眼部损伤,只能减缓疾病的进展。目前正在研发的、专门针对明确生化靶点的新型药物(如醛糖还原酶抑制剂和蛋白激酶C-β抑制剂)在临床试验中未能证明对糖尿病视网膜病变有显著疗效。相比之下,40多年前就已发现、在20多个国家注册用于治疗糖尿病视网膜病变的羟苯磺酸钙(2,5 - 二羟基苯磺酸)据我们所知仍是唯一能减缓该疾病进展的血管保护剂。对涉及羟苯磺酸钙(CLS 2210)的已发表研究的全面综述表明,这是一种相当“非特异性”的化合物,对导致糖尿病视网膜病变的各种复杂病症有适度但显著的作用。最近的研究表明,羟苯磺酸钙是一种有效的抗氧化剂,尤其能对抗极具破坏性的羟自由基。此外,它还能改善糖尿病性内皮功能障碍、减少细胞凋亡并减缓血管细胞增殖。