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目的:从藤黄酸及其衍生物中寻找一种有效的细胞凋亡诱导剂。方法:为了进一步发现潜在的抗肿瘤先导化合物,设计合成了8个新的藤黄酸-NO供体衍生物,并通过体外MTT法测定它们对HT-29,Bel-7402,BGC-823和A549细胞的抑制活性。结果:通过MTT法检测细胞,观察形态学变化,Annexin-V/PI双染色法证实藤黄酸结构中C35被羟基取代的化合物4能诱导SKOV3细胞凋亡。结论:化合物4具有显著的诱导细胞凋亡作用,有望成为抗癌新药物研发中的潜在先导化合物。
OBJECTIVE: To find an effective apoptosis inducer from gambogic acid and its derivatives. METHODS: To further identify potential antitumor lead compounds, eight new derivatives of gambogic acid-NO donor were designed and synthesized and their inhibitory effects on HT-29, Bel-7402, BGC-823 and A549 Cell inhibitory activity. Results: MTT assay was used to observe the morphological changes. Annexin-V / PI double staining confirmed that C35 substituted by hydroxyl group in gambogic acid could induce SKOV3 cell apoptosis. Conclusion: Compound 4 has a significant apoptosis-inducing effect and is expected to become a potential lead compound in the development of new anti-cancer drugs.