凋亡性查耳酮类似物在人肝癌HepG2细胞中的合成。
Synthesis of apoptotic chalcone analogues in HepG2 human hepatocellular carcinoma cells.
作者信息
Park Cheon-Soo, Ahn Yongchel, Lee Dahae, Moon Sung Won, Kim Ki Hyun, Yamabe Noriko, Hwang Gwi Seo, Jang Hyuk Jai, Lee Heesu, Kang Ki Sung, Lee Jae Wook
机构信息
Department of Surgery, Gangneung Asan Hospital, University of Ulsan College of Medicine, Gangneung 210-711, Republic of Korea.
Department of Hematology and Oncology, Gangneung Asan Hospital, University of Ulsan College of Medicine, Gangneung 210-711, Republic of Korea.
出版信息
Bioorg Med Chem Lett. 2015 Dec 15;25(24):5705-7. doi: 10.1016/j.bmcl.2015.10.093. Epub 2015 Oct 31.
Eight chalcone analogues were prepared and evaluated for their cytotoxic effects in human hepatoma HepG2 cells. Compound 5 had a potent cytotoxic effect. The percentage of apoptotic cells was significantly higher in compound 5-treated cells than in control cells. Exposure to compound 5 for 24h induced cleavage of caspase-8 and -3, and poly (ADP-ribose) polymerase (PARP). Our findings suggest that compound 5 is the active chalcone analogue that contributes to cell death in HepG2 cells via the extrinsic apoptotic pathway.
制备了八种查尔酮类似物，并评估了它们对人肝癌HepG2细胞的细胞毒性作用。化合物5具有强大的细胞毒性作用。化合物5处理的细胞中凋亡细胞的百分比明显高于对照细胞。用化合物5处理24小时可诱导半胱天冬酶-8和-3以及聚（ADP-核糖）聚合酶（PARP）的裂解。我们的研究结果表明，化合物5是一种活性查尔酮类似物，它通过外源性凋亡途径导致HepG2细胞死亡。
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