目的合成14-N-(3-乙酰基苯)-氨基粉防己碱,并考察其体外抗肿瘤活性。方法本研究以粉防己碱为原料,依次经硝化、还原和Chan-Lam-Evans偶联共计三步反应,合成了一种双苄基异喹啉衍生物,新合成的化合物的结构经核磁共振氢谱(^(1)H-nuclear ...目的合成14-N-(3-乙酰基苯)-氨基粉防己碱,并考察其体外抗肿瘤活性。方法本研究以粉防己碱为原料,依次经硝化、还原和Chan-Lam-Evans偶联共计三步反应,合成了一种双苄基异喹啉衍生物,新合成的化合物的结构经核磁共振氢谱(^(1)H-nuclear magnetic resonance,^(1)H-NMR)、核磁共振碳谱(^(13)C-nuclear magnetic resonance,^(13)C-NMR)和高分辨质谱(high resolution mass spectrometer,HRMS)确证。采用MTT法将所得衍生物14-N-(3-乙酰基苯)粉防己碱对人肝癌细胞HepG2和人正常肝细胞HL7702的体外抑制活性进行了初步评价;通过设计细胞划痕、侵袭实验探究化合物对HepG2细胞迁移和侵袭能力影响。结果MTT实验结果表明,该化合物可以剂量依赖性地抑制HepG2细胞增殖,其IC_(50)值为4.61μmol/L。细胞划痕、侵袭实验表明该化合物明显抑制HepG2细胞迁移和侵袭能力,且呈剂量依赖性,差异具有统计学意义(P<0.005)。结论结果表明,14-N-(3-乙酰基苯)-氨基粉防己碱可作为一种潜在的抗肝癌药物。展开更多
The resin of Ferula sinkiangensis has been traditionally utilized for treating gastrointestinal disorders,inflammation,tumors,various cancers,and alopecia areata.The primary bioactive constituents,sesquiterpene coumar...The resin of Ferula sinkiangensis has been traditionally utilized for treating gastrointestinal disorders,inflammation,tumors,various cancers,and alopecia areata.The primary bioactive constituents,sesquiterpene coumarins,have demonstrated notable therapeutic potential against neuroinflammation.In this study,a structure-guided fractionation method was used to isolate nine novel sesquiterpene coumarins from the resin of F.sinkiangensis.These compounds were characterized and structurally elucidated using comprehensive physicochemical and spectroscopic techniques,including calculated electronic circular dichroism(ECD).Anti-neuroinflammatory assays revealed that compounds 2,3,and 6 significantly inhibited nitric oxide(NO)production in lipopolysaccharide(LPS)-stimulated BV2 microglial cells,with IC_(50)values ranging from 1.63 to 12.25μmol·L^(−1).展开更多
文摘目的合成14-N-(3-乙酰基苯)-氨基粉防己碱,并考察其体外抗肿瘤活性。方法本研究以粉防己碱为原料,依次经硝化、还原和Chan-Lam-Evans偶联共计三步反应,合成了一种双苄基异喹啉衍生物,新合成的化合物的结构经核磁共振氢谱(^(1)H-nuclear magnetic resonance,^(1)H-NMR)、核磁共振碳谱(^(13)C-nuclear magnetic resonance,^(13)C-NMR)和高分辨质谱(high resolution mass spectrometer,HRMS)确证。采用MTT法将所得衍生物14-N-(3-乙酰基苯)粉防己碱对人肝癌细胞HepG2和人正常肝细胞HL7702的体外抑制活性进行了初步评价;通过设计细胞划痕、侵袭实验探究化合物对HepG2细胞迁移和侵袭能力影响。结果MTT实验结果表明,该化合物可以剂量依赖性地抑制HepG2细胞增殖,其IC_(50)值为4.61μmol/L。细胞划痕、侵袭实验表明该化合物明显抑制HepG2细胞迁移和侵袭能力,且呈剂量依赖性,差异具有统计学意义(P<0.005)。结论结果表明,14-N-(3-乙酰基苯)-氨基粉防己碱可作为一种潜在的抗肝癌药物。
基金supported by the National Natural Science Foundation of China(No.U1903122)the Scientific Research Fund of Liaoning Province Education Department(No.LJKZ0945)the Natural Science Foundation of Liaoning Province(No.2022-MS-242).
文摘The resin of Ferula sinkiangensis has been traditionally utilized for treating gastrointestinal disorders,inflammation,tumors,various cancers,and alopecia areata.The primary bioactive constituents,sesquiterpene coumarins,have demonstrated notable therapeutic potential against neuroinflammation.In this study,a structure-guided fractionation method was used to isolate nine novel sesquiterpene coumarins from the resin of F.sinkiangensis.These compounds were characterized and structurally elucidated using comprehensive physicochemical and spectroscopic techniques,including calculated electronic circular dichroism(ECD).Anti-neuroinflammatory assays revealed that compounds 2,3,and 6 significantly inhibited nitric oxide(NO)production in lipopolysaccharide(LPS)-stimulated BV2 microglial cells,with IC_(50)values ranging from 1.63 to 12.25μmol·L^(−1).
