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
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)