中山大学学报（自然科学版）（中英文）2025，Vol.64Issue(4)：79-90,12.DOI:10.13471/j.cnki.acta.snus.ZR20240361
芒果苷元衍生物的设计合成及其抑制磷酸二酯酶4活性
Design and synthesis of norathyriol derivatives and their inhibition of phosphodiesterase 4 activity
摘要
Abstract
Derivatives of Norathyriol were designed and synthesized in this study,and their phosphodi-esterase4(PDE4)inhibitory activities were evaluated in vitro.Mangiferin was used as the starting ma-terial for structural modification,and sixteen derivatives were prepared through 2-deglycosylation,2,3-cyclic synthesis,and 6,7-substitution reactions and other methods.The PDE4 inhibitory activities of these compounds were evaluated in vitro by[3H]liquid scintillation counting method.Among these compounds,derivative 4 has the highest inhibitory activity(IC50=358 nmol/L).The docking display structure showed that the pyran ring could form hydrogen bonds with Gln-369,and the 6-methyl cyclo-propane could form hydrophobic interactions with surrounding hydrophobic amino acids.关键词
芒果苷元/衍生物/磷酸二酯酶4/抑制剂Key words
norathyriol/derivatives/phosphodiesterase 4/inhibitor分类
医药卫生引用本文复制引用
黄尚瑛,刘兴福,陈思竹,刘昊柏,张国强,黄仪有,曹影影,何细新..芒果苷元衍生物的设计合成及其抑制磷酸二酯酶4活性[J].中山大学学报（自然科学版）（中英文）,2025,64(4):79-90,12.基金项目
广东省教育厅特色类创新项目(2022KTSCX029) （2022KTSCX029）
广东省教育厅重点领域项目(2024ZDZX2044) （2024ZDZX2044）
国家自然科学基金(22277019) （22277019）
