对苯二酚单烷基醚的合成及其抗脂质过氧化活性
Synthesis and anti lipid-peroxidation activity of hydroquinone monoalkyl ethers.
作者信息
Nihro Y, Furukawa H, Sogawa S, Wang T C, Miyataka H, Matsumoto H, Miki T, Satoh T
机构信息
Faculty of Pharmaceutical Sciences, Tokushima Bunri University, Japan.
出版信息
Chem Pharm Bull (Tokyo). 1994 Mar;42(3):576-9. doi: 10.1248/cpb.42.576.
A series of hydroquinone monoalkyl ethers was synthesized and evaluated for anti lipid-peroxidation activity in rat liver microsomes. 4-Hexyloxy-2,3,6-trimethylphenol (9), having a low redox potential, as well as ascorbic acid exhibited the strongest anti lipid-peroxidation activity (IC50 = 4.2 x 10(-7) M). Structure-activity relationship studies demonstrated that the inhibitory effect of hydroquinone monoalkyl ethers on lipid peroxidation was increased by the acquisition of an optimum hydrophobicity and decreased by an insufficient or excessive hydrophobicity.
合成了一系列对苯二酚单烷基醚，并在大鼠肝微粒体中评估了它们的抗脂质过氧化活性。具有低氧化还原电位的4-己氧基-2,3,6-三甲基苯酚（9）以及抗坏血酸表现出最强的抗脂质过氧化活性（IC50 = 4.2×10⁻⁷ M）。构效关系研究表明，对苯二酚单烷基醚对脂质过氧化的抑制作用会因获得最佳疏水性而增强，因疏水性不足或过大而减弱。
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