中草药来源的Ⅰ类HDAC抑制剂筛选

doi:10.16333/j.1001-6880.2018.7.001

天然产物研究与开发 ›› 2018, Vol. 30 ›› Issue (7): 1099-1104.doi: 10.16333/j.1001-6880.2018.7.001

• 研究论文 • 下一篇

中草药来源的Ⅰ类HDAC抑制剂筛选

姚晓辉，黎欢，胡阳亮，胡英杰，符林春，沈小玲*

广州中医药大学热带医学研究所中药新药发现实验室，广州，510405

出版日期:2018-08-08 发布日期:2018-08-08
基金资助:
国家重大科技专项（2014ZX10005002）

Screening of Class I HDAC Inhibitors from Traditional Chinese Medicine

YAO Xiao-hui,LI Huan,HU Yang-liang,HU Ying-jie,FU Lin-chun,SHEN Xiao-ling*

Laboratory of New Herbal Drug Discovery,Tropical Medicine Institute,Guangzhou University of Chinese Medicine,Guangzhou 510405,China

Online:2018-08-08 Published:2018-08-08

摘要/Abstract

摘要： 为从中药来源的化合物中筛选Ⅰ类组蛋白去乙酰化酶（HDAC）抑制剂，采用HDAC抑制剂筛选试剂盒从60个化合物中筛选出对HDAC活性抑制作用较强的化合物，再用HDAC3/8抑制剂筛选试剂盒进一步评价其HDAC抑制，同时Western-blot法检测其对人宫颈癌细胞株（HeLa）Ⅰ类HDAC表达的影响。结果显示:血根碱、胡椒碱、异甘草素、丹酚酸C对HDAC抑制活性较强；异甘草素和异甘草苷显著抑制HDAC3/8活性；血根碱对HeLa细胞有明显的增殖抑制作用，对Ⅰ类HDAC的表达有明显的抑制作用。本研究提示血根碱、异甘草素和异甘草苷是Ⅰ类HDAC的抑制剂，其中血根碱值得进一步深入研究。

关键词: Ⅰ类HDAC抑制剂筛选, 天然化合物, 血根碱, 异甘草素, 异甘草苷

Abstract: To screen class Ⅰ HDAC inhibitors of natural origin,in total 60 compounds from traditional Chinese medicine were evaluated the HDAC inhibitory effect by employment of HDAC inhibitor screening kits.Compounds exhibiting higher activity to inhibit HDAC were further investigated the effect on inhibiting HDAC3/8 activity by using HDAC3/8 inhibitor screening kits,and the effect on protein expression of class Ⅰ HDACs in HeLa cells by Western-blotting.It was found that,Sanguinarine，Piperine,Isoliquiritigenin,Isoliquiritin,Salvianolic acid C were more active than others to inhibit HDAC activity;Isoliquiritigenin and Isoliquiritin significantly inhibited HDAC3/8 activity;In addition,Sanguinarine strongly inhibited cell proliferation and cellular expression of class Ⅰ HDACs in HeLa cells.Our results showed that Isoliquiritigenin,Isoliquiritin and Sanguinarine are potential inhibitors of class Ⅰ HDACs.Among them Sanguinarine is worth further studying.

Key words: screening of ClassⅠHDAC inhibitors, natural compounds, sanguinarine, isoliquiritigenin, isoliquiritin

中图分类号:

R965.1

姚晓辉，黎欢，胡阳亮，胡英杰，符林春，沈小玲*. 中草药来源的Ⅰ类HDAC抑制剂筛选[J]. 天然产物研究与开发, 2018, 30(7): 1099-1104.

YAO Xiao-hui,LI Huan,HU Yang-liang,HU Ying-jie,FU Lin-chun,SHEN Xiao-ling*. Screening of Class I HDAC Inhibitors from Traditional Chinese Medicine[J]. NATURAL PRODUCT RESEARCH AND DEVELOPMENT, 2018, 30(7): 1099-1104.

[1]	陈玉甫1,2，张学俊1,2*，王明力1,2，贺扬洁1,2，张萌萌3，陶菡1,2，胡川渝3. 不同方法提取杜仲中桃叶珊瑚苷等4种高活性成分的比较研究[J]. 天然产物研究与开发, 2019, 31(1): 10-15.
[2]	覃月穆1,2，姜泽群1,2，马艳霞2，张旭1,2*. 异甘草素对人肺癌细胞株 H460 增殖、凋亡及NF-κB信号通路的影响[J]. 天然产物研究与开发, 2018, 30(5): 847-855.
[3]	殷晓芹1，王新杨2*，徐新1，王静1，袁浩亮3. 四种中药单体选择性抑制环氧合酶-2活性的评价[J]. 天然产物研究与开发, 2018, 30(10): 1769-1775.
[4]	王妍妍，张琴，冷天艳，杨丽华*. 血根碱通过下调TGF-β1/Smad通路抑制紫杉醇耐药卵巢癌细胞生长[J]. 天然产物研究与开发, 2017, 29(7): 1127-1131.
[5]	朱中海1,3,刘丹丽1,3,徐航超1,3,韩悦1,3,厉云2,韩蓓1,3*. 铅中毒及排铅天然化合物研究进展[J]. 天然产物研究与开发, 2014, 26(Suppl1): 159-162.

中草药来源的Ⅰ类HDAC抑制剂筛选

Screening of Class I HDAC Inhibitors from Traditional Chinese Medicine

PDF (PC)

可视化

摘要/Abstract

引用本文

使用本文

参考文献

相关文章 5

编辑推荐

Metrics

本文评价