Institute of Chemistry, Komi Scientific Centre, Ural Branch of the Russian Academy of Sciences, 48, Pervomayskaya St., 167000, Syktyvkar, Komi Republic, Russian Federation.
Institute of Biology, Komi Scientific Centre, Ural Branch of the Russian Academy of Sciences, 28, Kommunisticheskaya St., 167982, Syktyvkar, Komi Republic, Russian Federation.
Eur J Med Chem. 2018 May 25;152:10-20. doi: 10.1016/j.ejmech.2018.04.022. Epub 2018 Apr 13.
A series of new C-4- and C-4/C-5-aminomethyl derivatives were synthesized on the basis of α- and γ-mangostins. A comparative evaluation of their chelating ability, radical scavenging activity and hemolytic activity, as well as antioxidant and membrane-protective properties, was carried out on the model of HO-induced hemolysis of mammalian red blood cells. It was shown that γ-mangostin and its C-4/C-5-derivatives were superior to α-mangostin and its derivatives in all the investigated parameters characterizing the antioxidant activity in the test systems used. Most of the synthesized Mannich bases at low concentrations were superior to the original α- and γ-mangostins in the ability to protect mammalian red blood cells under HO-induced oxidative stress conditions.
基于 α-和 γ-倒捻子素，合成了一系列新的 C-4-和 C-4/C-5-氨甲基衍生物。在 HO 诱导的哺乳动物红细胞溶血模型上，对它们的螯合能力、清除自由基活性和溶血活性以及抗氧化和膜保护特性进行了比较评价。结果表明，γ-倒捻子素及其 C-4/C-5-衍生物在所有研究参数上均优于 α-倒捻子素及其衍生物，表明其在所用测试系统中具有抗氧化活性。在所研究的低浓度下，大多数合成的曼尼希碱在 HO 诱导的氧化应激条件下保护哺乳动物红细胞的能力优于原始的 α-和 γ-倒捻子素。
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