2-(3,5-二甲氧基苯甲撑基)-环戊酮的合成及其抗感染与抗肿瘤活性的研究  

Studies on Synthesis of 2-(3,5-dimethoxybenzylidene)-cyclopentanone & Its Activities in Anti-inflammation and Anti-tumor

作　　者：靳宗达[1] 曹毅[1] 候丙波[1] 绪广林[2] 郑丽玲[1] 敖桂珍[1] 

机构地区：[1]苏州大学医学部药学院,江苏苏州215123 [2]南京师范大学生命科学院新药研究中心,南京210097

出　　处：《抗感染药学》2010年第4期243-245,共3页Anti-infection Pharmacy

摘　　要：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 method of 2-（3,5-dimethoxy-benzylidene）-cyclopentanone（IV7） and its activities of anti-inflammation and anti-tumor.Methods：The target compound（IV7） was synthesized from the cyclopentanone,morpholine and 3,5-dimethoxybenzaldehyde.Its anti-tumor activity was assessed by CCK-8 in Hela carcinoma cell line,and its anti-inflammatory activity was evaluated with model of xylene-induced ear edema in mice.Results：IV7 exerted significant anti-inflammatory activity comparable with CMC-Na（P0.05）.CKK-8 results revealed that IV7 could inhibit weakly the proliferation of Hela cells（IC50 = 76.0μmol/L at 48 h）.Conclusion：Preliminary pharmacological tests showed that IV7 exhibited the potent anti-inflammation.

关 键 词：2-(3 5-二甲氧基苯甲撑基)-环戊酮 合成 抗炎 抗肿瘤 

分 类 号：R965[医药卫生—药理学]