目的 對黃槿中6種天然倍半萜類成分進行衍生化改造,并對所得衍生物進行體外抗腫瘤活性評價,分析其構效關系。方法 選取各種芳胺對黃槿中發(fā)現(xiàn)的6種倍半萜成分進行席夫堿修飾,采用噻唑藍(MTT)法考察合成的目標化合物對HeLa、HepG2和MCG-803細胞的體外抗增殖活性。結果 衍生改造了19個不同的倍半萜類衍生物,結合¹H-NMR、¹³C-NMR、HR-MS確定其結構,其中17個衍生物首次得到。部分衍生物表現(xiàn)出良好的抗腫瘤活性,芐胺基團對此類骨架化合物的結構修飾能夠較好地提高其抗腫瘤活性。結論 部分衍生物表現(xiàn)出良好的抗腫瘤活性,特別對HepG2細胞活性有較大的提高,化合物12、22、23具有進一步研究價值。

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

海南省自然科學基金面上項目（219MS101）；中國醫(yī)學科學院醫(yī)學與健康科技創(chuàng)新工程（重大協(xié)同創(chuàng)新項目）（2021-I2M-1-032）