中山大学学报（自然科学版）（中英文）2025，Vol.64Issue(3)：26-35,10.DOI:10.13471/j.cnki.acta.snus.ZR20240362
α-倒捻子素C3和C6位衍生物的合成及其抑制磷酸二酯酶4活性
Synthesis of α-mangostin derivatives at C3 and C6 positions and their inhibitory activity against phosphodiesterase 4
摘要
Abstract
Based on α-mangostin as the lead compound,and using the primary methods including alkylation and hydrolysis reactions for modifying C-3 and C-6 positions,eighteen novel derivatives with different chain length of carboxylic acid ester,carboxylic acid,and amide substituents in the C-3,C-6 phenolic hydroxyl group of α-mangostin were designed and synthesized.The in vitro evaluation of these compounds'ability to inhibit PDE4 was conducted using the[³H]liquid scintillation counting technique.The experimental results showed that five compound(2a-6a)had the stronger inhibitory activity on PDE4 than α-mangostin.Among them,carboxylic acid derivative of seven carbon chain lengths 5a exhibited the best potential PDE4 inhibitory activity with the IC50 values of 319 nmol/L.关键词
α-倒捻子素/衍生物/磷酸二酯酶4Key words
α-mangostin/derivatives/phosphodiesterase 4(PDE4)分类
药学引用本文复制引用
陈思竹,王雪,吴银飞,黄尚瑛,于思,黄仪有,曹影影,何细新..α-倒捻子素C3和C6位衍生物的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(3):26-35,10.基金项目
广东省教育厅创新强校特色项目(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）
