Zhang Xiaojie, Wang Rubing, Chen Guanglin, Dejean Laurent, Chen Qiao-Hong
Department of Chemistry, California State University, Fresno, CA, U.S.A.
Anticancer Res. 2015 Oct;35(10):5293-8.
To systematically investigate the effects of a class of curcumin-based compounds on cancer cell viability, proliferation, and apoptosis.
Cytotoxicity and anti-proliferative potency were estimated by the trypan blue exclusion assay and WST-1 cell proliferation assay, respectively. Cell death pathways were discriminated according to plasma membrane integrity and lipid asymmetry cell profiles using a F2N12S and CYTOX AADvanced double staining flow cytometry-based assay.
Nine compounds ( 2-10: ) exhibit 13- to 58-fold better cytotoxic and anti-proliferative potencies than curcumin towards HeLa cells. In this cervical cancer cell model, dienone and 1-methylpiperidone serve as the favorable central linkers; 5-methylisoxazol-3-yl and 3-methylisoxazol-5-yl act as the optimal terminal aromatic moiety. Finally, the effects of compounds 6: and 10: on HeLa cells' plasma membrane integrity and lipid asymmetry suggest that the early cytotoxic effect of these compounds is due to a stimulation of apoptosis.
系统研究一类姜黄素基化合物对癌细胞活力、增殖和凋亡的影响。
分别通过台盼蓝排斥试验和WST-1细胞增殖试验评估细胞毒性和抗增殖能力。使用基于F2N12S和CYTOX AADvanced双重染色流式细胞术的检测方法，根据质膜完整性和脂质不对称性细胞图谱区分细胞死亡途径。
九种化合物（2 - 10）对HeLa细胞的细胞毒性和抗增殖能力比姜黄素高13至58倍。在这个子宫颈癌细胞模型中，二烯酮和1-甲基哌啶酮是有利的中心连接基团；5-甲基异恶唑-3-基和3-甲基异恶唑-5-基是最佳的末端芳香基团。最后，化合物6和10对HeLa细胞质膜完整性和脂质不对称性的影响表明，这些化合物的早期细胞毒性作用是由于对凋亡的刺激。
