Ischemic retinopathy and age-related macular degeneration are the leading ocular diseases that cause blindness. The etiology of these diseases is due in part to the reduction of blood flow in the retina and/or choroid. Crocin analogs isolated from Crocus sativus L. were found to significantly increase the blood flow in the retina and choroid and to facilitate retinal function recovery. Increased blood flow due to vasodilation presumably improves oxygenation and nutrient supply of retinal structures. These results indicated that crocin analogs could be used to treat ischemic retinopathy and/or age-related macular degeneration. It was noted that disaccharide analogs of crocin, such as crocin-1 and crocin-2, were less potent than monosaccharide analogs of crocin, such as crocin-3 and crocin-4, constituting an interesting structure-activity relationship.
Ischemic retinopathy and, particularly, age-related macular degeneration (AMD) are difficult eye diseases to treat. Since the etiology of these diseases is inadequate blood circulation in the retina and choroid, drugs which can improve blood circulation to these tissues should be beneficial to these diseases. Since fovea is avascular, AMD is closely related to choroidal vascular abnormalities, and drugs which show strong effects to increase choroidal blood flow would be particularly useful. Puerarin and all its derivatives, except ET (puerarin disubstituted with -CH2CH2OH), showed marked increase of choroidal blood flow at various time periods. Even ET showed a tendency to increase choroidal blood flow, though it was not statistically significant. As for b wave recovery, all puerarin analogs showed strong recovery of retinal function after ischemic insult for 30 min. These results indicate that puerarin analogs could be used for the treatment of ischemic retinopathy, and AMD in particular.
Because of the discovery of potent interleukin-1 (IL-1) blocking effects by CK-103A (4,6-dihydropyridazino[4,5-c]pyridazin-5 (1H)-ones) on rat uveitis induced by IL-1, numerous derivatives of CK-103A have been synthesized and their efficacies on the same animal model studied. The uveitis was induced by injection of 1 ng IL-1/10 microliters intravitreally. The inflammation reached peak at 12 hr after the injection of IL-1. The prevention/blockade of IL-1-induced uveitis was measured at this peak inflammation time point. It was found that 8 out of 12 CK-analogs studied produced an effective blockade of IL-1-induced uveitis. Most of them were at least equipotent or even more potent than prednisolone in blocking IL-1-induced uveitis. It is concluded that most dihydropyridazinopyridazin derivatives are effective anti-uveitis compounds. Some could be found to be safe and useful for the treatment of this dreadful disease.
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