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目的:研究2-(3,5-二甲氧基苯甲撑基)-环戊酮(IV)的合成方法及其对抗炎和抗肿瘤活性的影响。方法:环7戊酮与吗啡啉脱水反应得到烯胺,然后与3,5-二甲氧基苯甲醛进行缩合反应,生成目标化合物IV7。采用人胆囊收缩素/缩胆囊素八肽(CCK-8)法评价IV7对Hela细胞株增殖的影响;应用二甲苯致小鼠耳肿胀模型评价IV7的抗炎活性。结果:IV7与阴性对照药CMC-Na组相比,抗炎活性的差异有统计学意义(P<0.05)。IV7抑制Hela细胞增殖的作用较弱,在培养48h时IC50为76.0靘ol/L。结论:IV7具有较好的抗炎活性。
Objective: To study the synthesis of 2- (3,5-dimethoxybenzyl) -cyclopentanone (IV) and its effect on anti-inflammatory and anti-tumor activity. Methods: Cyclopentene 7 was dehydrated with morpholine to give enamine. Then condensation reaction with 3,5-dimethoxybenzaldehyde was carried out to produce the target compound IV7. The effect of IV7 on the proliferation of Hela cell line was evaluated by human cholecystokinin / cholecystokinin-octapeptide (CCK-8) assay. The anti-inflammatory activity of IV7 was evaluated by xylene-induced mouse ear swelling model. Results: The difference of anti-inflammatory activity between IV7 and CMC-Na negative control group was statistically significant (P <0.05). The inhibitory effect of IV7 on Hela cell proliferation was weak, with an IC50 of 76.0 μg / L at 48 h. Conclusion: IV7 has good anti-inflammatory activity.