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目的:研究灯盏乙素苷元4’-N,N-双取代氨甲基苯甲酸醚类衍生物的合成方法及其对PC12细胞的保护作用。方法:以灯盏乙素苷元为原料,通过缩合反应、酰氯反应等,经乙酰氯/甲醇体系脱去保护基后获得灯盏乙素苷元4’-N,N-双取代氨甲基苯甲酸醚类衍生物(8a~8f);采用MTT及LDH漏出率法研究化合物对PC12细胞的保护作用。结果:合成的化合物能较强抑制PC12细胞所受的氧化损伤,其中化合物8e,8f对PC12细胞的保护作用显著优于阳性对照药维生素E[8e,8f分别为(40.87±1.12),(41.73±0.61),VE为(45.61±0.82),P<0.05],结论:合成方法方便可行,灯盏乙素苷元4’-N,N-双取代氨甲基苯甲酸醚类衍生物有较好的体外活性,具有进一步开发前景。
OBJECTIVE: To study the synthesis of 4’-N, N-disubstituted aminomethyl benzoic acid ethers derivatives of scutellarin and their protective effects on PC12 cells. Methods: The scutellarin glycoside was used as starting material to obtain 4’-N, N-disubstituted aminomethylbenzoic acid of scutellarin by deprotection reaction with acetyl chloride / methanol system through condensation reaction and acid chloride reaction. Ether derivatives (8a ~ 8f). The protective effect of the compounds on PC12 cells was investigated by MTT and LDH leakage rates. Results: The synthesized compounds could significantly inhibit the oxidative damage of PC12 cells. The protective effect of 8e, 8f on PC12 cells was significantly better than that of vitamin E [8e, 8f (40.87 ± 1.12), (41.73 ± 0.61), VE was (45.61 ± 0.82), P <0.05] .Conclusion: The synthesis method is convenient and feasible. 4’-N, N-disubstituted aminomethyl benzoic acid ether derivatives of scutellarin are better In vitro activity, with further development prospects.