Intraocular pressure-lowering activity of phenolic antioxidants in normotensive rabbits

Intraocular pressure-lowering activity of phenolic antioxidants in normotensive rabbits
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DOI:
10.1076/ceyr.19.3.234.5320
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发表时间:
1999-09-01
影响因子:
2
通讯作者:
Green, K
Green, K
中科院分区:
医学4区
文献类型:
--
作者:
Hodges, LC;Kearse, EC;Green, K

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目的.本研究的目的是确定酚类抗氧化剂静脉注射到正常血压的兔眼内压(IOP)降低活动。测试了属于以下类别的抗氧化剂:肉桂酸;黄酮醇;黄烷醇;花青素;异黄酮;和单宁酸。将测试化合物溶解于作为媒介物的水或油/盐水中,并静脉内注射到血压正常的兔中。注射后每小时监测IOP,并表示为相对于注射前值的百分比。仅使用溶媒进行对照。对每只眼睛的IOP取平均值,以提供每只家兔的一个值。对于在1 mg时显示出活性的化合物,收集从0.01 mg-2 mg剂量开始的剂量-反应数据。表没食子儿茶素、表没食子儿茶素没食子酸酯和杨梅素在1 mg剂量下使IOP降低至对照水平以下。单宁酸是最有效的,在200 μ g剂量下降低IOP超过30%。只有含有连苯三酚B环系统和非芳香族C环的酚类抗氧化剂(表没食子儿茶素、表没食子儿茶素没食子酸酯和杨梅素)或鞣酸中发现的可能的没食子酰葡糖苷在降低IOP中具有活性,鞣酸的活性最高。其他抗氧化剂在该系统中没有活性,这表明与适当的眼部系统相互作用的更具体的结构要求。这些分子的蛋白质或蛋白聚糖结合特性在该活性中也可能是重要的。
Purpose. The purpose of this study was to determine the intraocular pressure (IOP)-lowering activity of phenolic antioxidants injected intravenously into normotensive rabbits. Antioxidants belonging to the following classes were tested: cinnamic acids; flavonols; flavanols; anthocyanidins; isoflavones: and tannic acid.Methods. Test compounds were dissolved in either water or oil/saline as vehicle and injected intravenously into normotensive rabbits. IOP was monitored hourly after injection and expressed as a percent relative to preinjection values. Controls were conducted using vehicle alone. IOP from each eye was averaged to provide one value per rabbit. Dose-response data beginning at 0.01 mg-2 mg doses were collected for compounds shown to be active at 1 mg.Results. Epigallocatechin, epigallocatechin gallate and myricetin lowered IOP below control levels at doses of 1 mg. Tannic acid was the most active, lowering IOP more than 30% at doses of 200 mu g.Conclusion. Only phenolic antioxidants containing a pyrogallol B-ring system and nonaromatic C-ring (epigallocatechin, epigallocatechin gallate and myricetin) or possible galloyl glucosides as found in tannic acid were active in lowering IOP, with tannic acid being the most active. Other antioxidants were not active in this system suggesting a more specific structural requirement for interacting with appropriate ocular systems. The protein or proteoglycan-binding properties of these molecules may also be important in this activity.