Cizmáriková R, Kráĺová K, Sersen F
Katedra chemickej teórie lieciv Farmaceutickej fakulty Univerzity Komenského, Bratislava.
Ceska Slov Farm. 2000 Jan;49(1):45-7.
The effect of 18 compounds of the aryloxyaminopropanol type--potential beta-adrenolytics (differing each from other by modifications in the hydrophilic and lipophilic part of the molecule) on the inhibition of oxygen evolution rate in spinach chloroplasts has been investigated. The compounds with n-octyloxymethyl and n-nonyloxymethyl group in position 3 of aromatic ring were found to exhibit the highest inhibitory activity (IC50 = 67, resp. 120 mumol dm-3). The compounds containing a heterocycle or the dimethylamino group in the hydrophilic part of the molecule and with propoxymethyl group on the aromatic ring were not active. Using EPR spectroscopy it was found that the studied compounds interact with Z+/D+ intermediates, i.e. tyrosine radicals TyrZ and TyrD situated in D1 and D2 proteins on the donor side of photosystem 2. Higher concentrations of the studied inhibitors cause release of Mn2+ ions from the oxygen evolving complex which is situated in photosystem 2. The interaction of the tested compounds with chlorophyll occurring in the photosynthetic centres has been confirmed by fluorescence measurements as well.
研究了18种芳氧基氨基丙醇类化合物——潜在的β-肾上腺素能阻滞剂(分子的亲水和疏水部分的修饰各不相同)对菠菜叶绿体中氧释放速率的抑制作用。发现芳环3位带有正辛氧基甲基和正壬氧基甲基的化合物表现出最高的抑制活性(IC50分别为67和120 μmol dm-3)。分子亲水部分含有杂环或二甲基氨基且芳环上带有丙氧基甲基的化合物没有活性。利用电子顺磁共振光谱发现,所研究的化合物与Z+/D+中间体相互作用,即位于光系统2供体侧D1和D2蛋白中的酪氨酸自由基TyrZ和TyrD。较高浓度的所研究抑制剂会导致位于光系统2中的放氧复合体释放Mn2+离子。荧光测量也证实了所测试化合物与光合中心中叶绿素的相互作用。