天然产物研究与开发 ›› 2021, Vol. 33 ›› Issue (4): 535-542.doi: 10.16333/j.1001-6880.2021.4.001

• 研究论文 •    下一篇

柚皮素酰腙类衍生物的合成、体外抗氧化活性以及细胞毒性研究

董家吏1,2，廖岳婷1,2，焦必宁2，苏学素1*   

  1. 1西南大学化学化工学院，重庆 400715；2中国农业科学院柑桔研究所（西南大学柑桔研究所） 农业农村部柑桔产品质量安全风险评估实验室，重庆 400712

  • 出版日期:2021-04-28 发布日期:2021-05-10
  • 基金资助:
    国家重点研发专项（2019YFC1605604-2）；国家现代农业（柑桔）产业技术体系建设专项（CARS-26）；国家农产品质量安全风险评估重大专项（GJFP2019043）

Synthesis,antioxidant activity in vitro and cytotoxicity of naringenin acylhydrazone derivatives

DONG Jia-li1,2,LIAO Yue-ting1,2,JIAO Bi-ning2,SU Xue-su1*   

  1. 1College of Chemistry and Chemical Engineering,Southwest University,Chongqing 400715,China;2Laboratory of Quality and Safety Risk Assessment for Citrus Products,Ministry of Agriculture and Rural Affairs,Citrus Research Institute,Chinese Academy of Agricultural Sciences (Citrus Research Institute of Southwest University),Chongqing 400712,China

  • Online:2021-04-28 Published:2021-05-10

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摘要： 柚皮素具有良好的抗氧化活性，但由于其生物利用率低，导致其应用受限。本文合成得到13种柚皮素的酰腙类衍生物，其中12种未被文献报道。采用ABTS、FRAP、DPPH 3种方法测定了合成衍生物与柚皮素的体外抗氧化活性。结果显示13种化合物的抗氧化活性均强于柚皮素，其中8种衍生物的体外抗氧化活性是柚皮素活性的3到6倍。细胞毒性实验中细胞存活率>90%时，可认为化合物对细胞无抑制。8种化合物对HEK293细胞的细胞毒性实验结果显示，在0~25 μmol/L浓度范围内，衍生物b、g、j、k、l对HEK293细胞存活率大于90%，其中衍生物g、k、l的浓度在0~50 μmol/L时，HEK293细胞的存活率仍大于90%，而衍生物j在浓度高达100 μmol/L时细胞存活率仍大于90%。研究结果为后期的抗氧化食品添加剂及抗氧化药物筛选提供理论依据。


关键词: 柚皮素, 酰腙, 抗氧化活性, 细胞毒性

Abstract:

Naringenin has better antioxidant activity.However,its application is limited due to its low bioavailability.In this article,13 kinds of naringenin acylhydrazone derivatives were synthesized,12 of them have not been reported in the literature.The antioxidant activities in vitro of 13 derivatives were determined by ABTS,FRAP,and DPPH methods.The results show that the antioxidant activity of 13 compounds is stronger than that of naringenin,and the antioxidant activity of 8 derivatives is 3 to 6 times higher than that of naringenin.In the cytotoxicity test,when the cell survival rate is >90%,it is regarded that the compound does not inhibit the cells.When the concentration range of 0-25 mol/L,the survival rate of HEK293 cells treated with derivatives b,g,j,k and l was more than 90%.In addition,when the concentration of derivatives g,k,l is 0-50 μmol/L,the survival rate of HEK293 cells is still more than 90%.Especially when the concentration of derivative j is as high as 100 μmol/L,the cell survival rate was still above 90%.The results provide a theoretical basis for the later screening of antioxidant food additives and antioxidant drugs.

Key words: naringenin, acylhydrazone, antioxidant activity, cytotoxicity

中图分类号:  O629.5

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