含吲哚环的查尔酮类衍生物的制备及其抗抑郁、抗炎、镇痛活性  

Preparation of Chalcone Derivatives Containing Indole Ring and Study on Their Antidepressant,Anti-inflammatory and Analgesic Activities

作　　者：汤敏 冯雨诺 王秋实 方超华 胡立威 关丽萍 TANG Min;FENG Yunuo;WANG Qiushi;FANG Chaohua;HU Liwei;GUAN Liping(School of Food Science and Pharmacy of Zhejiang Ocean University,Zhoushan 316022,China)

机构地区：[1]浙江海洋大学食品与药学学院,浙江舟山316022

出　　处：《海南师范大学学报(自然科学版)》2025年第1期14-21,共8页Journal of Hainan Normal University(Natural Science)

基　　金：福建省药物新靶点研究重点实验室开放课题(FJ-YW-2023KF04);国家级大学生创新创业训练计划(202310340048);浙江省公益技术应用研究计划(2017C33131)。

摘　　要：设计合成了7个吲哚查尔酮衍生物,并对7个化合物的抗抑郁、抗炎和镇痛活性进行评价。以吲哚-3-甲醛为原料,通过Aldol缩合反应,获得7个吲哚查尔酮化合物,经^(1)H NMR、^(13)C NMR确证结构。采用ICR小鼠的绝望空间诱导的小鼠抑郁模型、二甲苯诱导的小鼠耳肿胀模型以及醋酸诱导的小鼠扭体模型分别测定目标化合物的体内抗抑郁、抗炎、镇痛活性。7个化合物表现出不同的抗抑郁、抗炎、镇痛活性。与对照组相比,3-氟吲哚查尔酮(11f)的抗抑郁活性最高(抑制率为65.98%),2-氟吲哚查尔酮(1e)对炎症的抑制作用最好(抑制率为94.14%),3,4-二甲基吲哚查尔酮(11b)的镇痛效果最佳(抑制率为87.36%)。合成的7个吲哚查尔酮衍生物具有一定的抗抑郁、抗炎、镇痛活性。说明7个化合物对抑郁症及其并发症具有潜在疗效。In this paper,seven indolechalcone derivatives were designed and synthesized.The antidepressant,anti-analgesic and anti-inflammatory activities of these seven compounds were also evaluated.Seven indolechalones were obtained from indole-3-formaldehyde by Aldol condensation reaction.Their structures were confirmed by^(1)H NMR,^(13)C NMR.The in vivo antidepressant,anti-inflammatory and analgesic activities of the target compounds were determined using a despair space induced mouse depression model,a xylene induced mouse ear swelling model and an acetic acid induced pain models in ICR mice,respectively.Seven compounds showed different anti-analgesic,antidepressant and anti-inflammatory activities.Compared with the control group,3-F-indolochalcone(1f)had the highest antidepressant activity(the inhibition rate was 65.98%),2-F-indolochalcone(1e)had the best inhibitory effect on inflammation(the inhibition rate was 94.14%),and 3,4-dimethyl-indolochalcone(1b)had the best analgesic effect(the inhibition rate was 87.36%).The seven synthesized indochalcone derivatives had certain antidepressant,anti-inflammatory and analgesic activities.These results indicated that 7 compounds have potential efficacy on depression and its complications.

关 键 词：吲哚查尔酮衍生物 抗抑郁 镇痛 抗炎 

分 类 号：O621.3[理学—有机化学]