目的 对黄槿中6种天然倍半萜类成分进行衍生化改造,并对所得衍生物进行体外抗肿瘤活性评价,分析其构效关系。方法 选取各种芳胺对黄槿中发现的6种倍半萜成分进行席夫碱修饰,采用噻唑蓝(MTT)法考察合成的目标化合物对HeLa、HepG2和MCG-803细胞的体外抗增殖活性。结果 衍生改造了19个不同的倍半萜类衍生物,结合¹H-NMR、¹³C-NMR、HR-MS确定其结构,其中17个衍生物首次得到。部分衍生物表现出良好的抗肿瘤活性,苄胺基团对此类骨架化合物的结构修饰能够较好地提高其抗肿瘤活性。结论 部分衍生物表现出良好的抗肿瘤活性,特别对HepG2细胞活性有较大的提高,化合物12、22、23具有进一步研究价值。

Objective To modify derivatives of 6 natural sesquiterpenoids from Hibiscus tiliaceus Linn., evaluate their in vitro antitumor activities, and reveal the structure-activity relationship. Methods A series of amines from H. tiliaceus were used to synthesize the gossypol Schiff base of the 6 sesquiterpenoids. Their antitumor activities in vitro were evaluated for HeLa, HepG2, and MCG-803 by MTT assay. Results Nineteen derivatives were synthesized, seventeen of which was reported for the first time, and their structures were characterized by ¹H-NMR, ¹³C-NMR, and HR-MS. MTT assay showed some sesquiterpenoid derivatives exhibited good antitumor activity against HeLa, HepG2, and MCG-803 cell, and benzylamine modification could enhance antitumor activity of these sesquiterpenoid skeletons. Conclusion Some derivatives show promising antitumor activities, especially for the HepG2 cell lines, and compound 12, 22, and 23 are worth further studying.

R284.2；R966

海南省自然科学基金面上项目（219MS101）；中国医学科学院医学与健康科技创新工程（重大协同创新项目）（2021-I2M-1-032）