| 汤 敏†
，冯雨诺†
，王秋实，方超华，胡立威，关丽萍*.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[J].海南师范大学学报自科版,2025,38(1):14-21 |
| 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 |
| |
| DOI：10.12051/j.issn.1674-4942.2025.01.003 |
| 中文关键词: 吲哚查尔酮衍生物 抗抑郁 镇痛 抗炎 |
| 英文关键词: indolechalcone derivatives analgesia anti-inflammatory anti-depressive disorder |
| 基金项目: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） |
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| 摘要点击次数: 469 |
| 全文下载次数: 191 |
| 中文摘要: |
| 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、13C 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（1f）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
（1b）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。 |
| 英文摘要: |
| In this paper, seven indolechalcone derivatives were designed and synthesized. The antidepressant, anti-an⁃
algesic and anti-inflammatory activities of these seven compounds were also evaluated. Seven indolechalones were ob⁃
tained from indole-3-formaldehyde by Aldol condensation reaction. Their structures were confirmed by 1
H NMR, 13C
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 in⁃
hibition 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. |
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