Ohnishi S T, Ohnishi T
Philadelphia Biomedical Research Institute, King of Prussia, PA.
Arzneimittelforschung. 1991 Dec;41(12):1201-5.
A monomeric derivative and several oligomeric derivatives were synthesized from prostaglandin B2. Their lipid solubility was studied by measuring their octanol-water partition coefficients. With EPR spectroscopy, the oligomeric derivatives were shown to have g = 2 signal, indicating these compounds have intrinsic free radicals. Measuring the rate of adenochrome formation, it was shown that these derivatives could scavenge superoxide anions. Using a spin-trapping technique employing DMPO, we found that these oligomers could also scavenge hydroxyl radicals. The calcium chelating activity of these compounds were also studied. In an in vitro rat model, these compounds inhibited lipid peroxidation as measured by the production of thiobarbituric acid reacting substances. Other prostaglandin oligomeric derivatives synthesized from PGE1 were also studied, and their properties were compared with these new compounds. Results suggest that both the water solubility and the chelating activity for calcium ions may not be related to their protective effects in ischemic or traumatic injury.
从前列腺素B2合成了一种单体衍生物和几种低聚物衍生物。通过测量它们的正辛醇 - 水分配系数来研究它们的脂溶性。利用电子顺磁共振光谱法，表明低聚物衍生物具有g = 2信号，表明这些化合物具有内在自由基。通过测量腺色素的形成速率，表明这些衍生物可以清除超氧阴离子。使用采用DMPO的自旋捕获技术，我们发现这些低聚物也可以清除羟基自由基。还研究了这些化合物的钙螯合活性。在体外大鼠模型中，通过硫代巴比妥酸反应物质的产生来测量，这些化合物抑制脂质过氧化。还研究了从PGE1合成的其他前列腺素低聚物衍生物，并将它们的性质与这些新化合物进行了比较。结果表明，水溶性和对钙离子的螯合活性可能都与它们在缺血性或创伤性损伤中的保护作用无关。
