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目的:合成木犀草素Mannich碱衍生物并考察其抗癌活性。方法:室温下木犀草素与甲醛、胺经Mannich反应得到8种Mannich碱衍生物。采用MTT法,以5氟-尿嘧啶(5-Fu)为阳性对照药,通过人宫颈癌细胞(Hela)、人胃癌细胞(SGC-7901)、人结肠癌细胞(HCT-116)、人白血病细胞(K562)、人乳腺癌细胞(MCF-7)、人前列腺癌细胞(DU-145)等6种肿瘤细胞进行体外抗癌活性评价,以正常人胚肾上皮细胞(HEK-293)为毒性对照;对化合物8h进行抗癌分子机制研究。结果:合成的8种化合物结构经1H-NMR、13C-NMR和MS确证。体外抗癌活性试验表明部分化合物显示出比木犀草素更好的抗癌活性。结论:化合物8h可能通过线粒体途径抑制SGC-7901细胞增殖,从而诱导细胞凋亡。
Objective: To synthesize Lignans Mannich base derivatives and investigate their anticancer activity. Methods: Eight kinds of Mannich base derivatives were obtained by Mannich reaction between luteolin and formaldehyde and amines at room temperature. MTT assay was used to detect the expression of 5-fluorouracil (5-Fu) in human gastric cancer cells (Hela), human gastric cancer cells (SGC-7901), human colon cancer cells (HCT-116) Six kinds of tumor cells such as K562, MCF-7 and DU-145 were evaluated in vitro for their anticancer activity, and normal human embryonic kidney epithelial cells (HEK-293) Control; 8h anti-cancer compounds on the molecular mechanism. Results: The structures of the 8 compounds were confirmed by 1H-NMR, 13C-NMR and MS. In vitro antitumor activity tests showed that some of the compounds showed better anticancer activity than luteolin. Conclusion: Compound 8h may inhibit the proliferation of SGC-7901 cells through mitochondrial pathway and induce apoptosis.