Davies M E, Bondi J V, Grabowski L, Schofield T L, Field A K
Antiviral Res. 1987 Feb;7(2):119-25. doi: 10.1016/0166-3542(87)90027-1.
2'-Nor-2'-deoxyguanosine (2'NDG), previously reported by us to effectively treat acute herpes simplex infections in mice, was used therapeutically to significantly enhance healing of established herpetic corneal lesions and prevent stromal disease in rabbits. Treatment using 0.06% 2'NDG drops (5 times daily) starting 3 days after infection resulted in more rapid healing of corneal epithelial lesions, rapid resolution of conjunctival inflammation, and prevention of stromal clouding compared to placebo-treated animals. In comparative dose-response titrations, the relative potency of 2'NDG to acyclovir was 6.4, which was significant. In addition, soluble ophthalmic inserts were developed for delivery of 2'NDG. Once a day treatment using ophthalmic inserts which released 100 micrograms 2'NDG significantly enhanced corneal and conjunctival healing and prevented stromal disease; 2'NDG eye drops (100 micrograms) delivered once a day were also effective in inhibiting the progression of corneal lesions. These results indicate that 2'NDG may be therapeutically effective in treatment of herpes keratitis, and further suggest that for use as eye drops or in an ophthalmic insert, 2'NDG may be effective even if applied once per day.
2'-去甲-2'-脱氧鸟苷(2'NDG),我们之前报道其可有效治疗小鼠急性单纯疱疹感染,现用于治疗以显著促进兔已形成的疱疹性角膜病变的愈合并预防基质病变。在感染后3天开始使用0.06% 2'NDG滴眼液(每日5次)进行治疗,与安慰剂治疗的动物相比,角膜上皮病变愈合更快,结膜炎症迅速消退,且预防了基质混浊。在比较剂量反应滴定中,2'NDG对阿昔洛韦的相对效价为6.4,具有显著性。此外,还开发了用于递送2'NDG的可溶性眼科插入物。每天使用释放100微克2'NDG的眼科插入物进行一次治疗可显著促进角膜和结膜愈合并预防基质病变;每天递送一次的2'NDG滴眼液(100微克)在抑制角膜病变进展方面也有效。这些结果表明2'NDG在治疗疱疹性角膜炎方面可能具有治疗效果,进一步表明用作滴眼液或眼科插入物时,即使每天应用一次2'NDG也可能有效。