目的 對黃槿中6種天然倍半萜類成分進(jìn)行衍生化改造,并對所得衍生物進(jìn)行體外抗腫瘤活性評價,分析其構(gòu)效關(guān)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(jìn)行席夫堿修飾,采用噻唑藍(lán)(MTT)法考察合成的目標(biāo)化合物對HeLa、HepG2和MCG-803細(xì)胞的體外抗增殖活性。結(jié)果 衍生改造了19個不同的倍半萜類衍生物,結(jié)合¹H-NMR、¹³C-NMR、HR-MS確定其結(jié)構(gòu),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(tuán)對此類骨架化合物的結(jié)構(gòu)修飾能夠較好地提高其抗腫瘤活性。結(jié)論 部分衍生物表現(xiàn)出良好的抗腫瘤活性,特別對HepG2細(xì)胞活性有較大的提高,化合物12、22、23具有進(jìn)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(xué)基金面上項目（219MS101）；中國醫(yī)學(xué)科學(xué)院醫(yī)學(xué)與健康科技創(chuàng)新工程（重大協(xié)同創(chuàng)新項目）（2021-I2M-1-032）