新型二硫杂环戊烯硫酮化合物的合成及其对谷氨酸诱导损伤HT22细胞的保护作用

Synthesis of Novel 3H-1,2-dithiole-3-thione Compounds and Their Protective Effects on Glutamic Acid-induced Damage of HT22 Cells

在保留ADT-OH的3H-1,2-二硫杂环戊烯-3-硫酮结构的基础上,用芳乙烯基替换4-羟基苯环,设计并合成了6个二硫杂环戊烯硫酮化合物(L_1~L_6,其中L_2,L_3,L_5和L_6为新化合物),其结构经~1H NMR,^(13)C NMR和HR-MS(ESI)表征。采用MTT法研究了L_1~L_6对谷氨酸诱导损伤的海马神经元HT22细胞的影响。药理初筛结果表明:给药浓度为10~100μmol·L^(-1)时,L_1,L_2,L_4和L_6均能提高受损HT22细胞的存活率(P<0.01);给药浓度为1μmol·L^(-1)时,L_3和L_5均可提高损伤HT22细胞的存活率(P<0.01)。

The structure of ADT-OH was modified by replacing 4-OH phenyl with aryl vinyl, based on retaining its 3H-1,2-dithiocyclopentene-3-thione. Six 3H-1,2-dithiole-3-thione compounds （ L1 - L6 ） were designed and synthesized. Among them, L2, L3, L5 and L6 were novel compounds. The structures were characterized by IH NMR, 13C NMR and HR-MS（ESI）. Effects of L1- L6 on glutamic acid-in- duced damage of HT22 cells were investigated by MTY method. The primary pharmacological results dis- played that L1, L2, L4 and L6 significantly improved the survival rates of damaged HT22 cells at the con- centration of 10 - 100 μmol L-1 （P 〈0.01 ）, L3 and L5 increased the survival rates of damaged HT22 cells at the concentration of 1 μmol L- 1 （p 〈 0. O1 ）.