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磺酰胺类槟榔碱衍生物的合成及其缓解心肌肥大活性评价

杜新宇 杨壮壮 张焱蕾 刘仔翔 任展宏 曾志刚

湖北科技学院学报(医学版)2026,Vol.40Issue(4):306-310,315,6.
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湖北科技学院学报(医学版)2026,Vol.40Issue(4):306-310,315,6.DOI:10.16751/j.cnki.2095-4646.2026030101

磺酰胺类槟榔碱衍生物的合成及其缓解心肌肥大活性评价

Synthesis of Sulfonamide Arecoline Derivatives and Their Activity Evaluation in Alleviating Myocardial Hypertrophy

杜新宇 1杨壮壮 1张焱蕾 2刘仔翔 2任展宏 3曾志刚2

作者信息

  • 1. 湖北科技学院医学部药学院,湖北 咸宁 437100
  • 2. 湖北科技学院核技术与化学生物学院
  • 3. 湖北科技学院医学部基础医学院
  • 折叠

摘要

Abstract

Objective To investigate the inhibitory effects of newly synthesized sulfonamide arecoline derivatives on palmitic acid(PA)-induced cardiomyocyte hypertrophy.Methods Twenty-six novel sulfonamide arecoline derivatives(D1-D26)were synthesized starting from arecoline hydrobromide and structurally characterized.An H9c2 cardiomyocyte hypertrophy model was established to screen for the lead compound via CCK-8 assay.Furthermore,the expression of hypertrophy markers(Nppa,Nppb,and Myh7)were detected by RT-qPCR,and potential targets were explored via molecular docking.Results Compound D24 significantly inhibited PA-induced cardiomyocyte hypertrophy and down-regulated the expression of hypertrophic marker genes(Nppa,Nppb and Myh7).Molecular docking analysis revealed that D24 possessed favorable binding affinity to the Nrf2 protein.Conclusion A novel sulfonamide arecoline derivative,D24,was synthesized and found to inhibit PA-induced cardiomyocyte hypertrophy.

关键词

槟榔碱/磺酰胺/合成/棕榈酸/心肌细胞肥大

Key words

Arecoline/Sulfonamide/Synthesis/Palmitic acid/Cardiomyocyte hypertrophy

分类

医药卫生

引用本文复制引用

杜新宇,杨壮壮,张焱蕾,刘仔翔,任展宏,曾志刚..磺酰胺类槟榔碱衍生物的合成及其缓解心肌肥大活性评价[J].湖北科技学院学报(医学版),2026,40(4):306-310,315,6.

基金项目

项目基金:湖北省科技计划项目(2025CDB024) (2025CDB024)

湖北省自然科学基金-咸宁联合资助项目(2025AFD407) (2025AFD407)

咸宁市科技计划项目(2024RCFW004) (2024RCFW004)

咸宁市自然科学基金"大健康专项"(2025DJK07) (2025DJK07)

湖北科技学院学报(医学版)

2095-4646

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