Synthesis and antitumor activity of emodin quaternary ammonium salt derivatives.
Synthesis and antitumor activity of emodin quaternary ammonium salt derivatives.
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DOI：
10.1016/j.ejmech.2012.07.047
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发表时间：
2012-10
影响因子：
6.7
通讯作者：
Jingwei Shao;Fengsen Zhang;Zedong Bai;Conghui Wang;Yaofeng Yuan;Wenfeng Wang
中科院分区：
文献类型：
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作者：
Jingwei Shao;Fengsen Zhang;Zedong Bai;Conghui Wang;Yaofeng Yuan;Wenfeng Wang
合成了一系列新的C-3和C-6位点修饰的大黄素衍生物，并对其体外和体内抗癌活性进行了评价。其中，化合物5g和5h分别对HepG2、BGC-823、AGS癌细胞具有较显著的抗增殖能力，对HELF正常细胞系具有较低的细胞毒性。化合物5g和5h诱导AGS细胞周期阻滞于G0/G1期，并通过激活caspase-3和caspase-9酶诱导凋亡。用H22异种移植物在昆明小鼠体内进行了5g和5h的研究。结果显示，与对照组相比，5g中剂量组（10 mg/kg）和5h高剂量组（25 mg/kg）具有显著的抗肿瘤活性。
A series of new emodin derivatives modified at the C-3 and the C-6 positions were synthesized, and evaluated for their anticancer activities in vitro and in vivo. Among them, Compounds 5g and 5h had more significant antiproliferative ability against HepG2, BGC-823, AGS cancer cell lines and low cytotoxicity to HELF normal cell line, respectively. Compounds 5g and 5h induced AGS cell cycle arrest at G0/G1 phase and induce apoptosis via activation of caspase-3 and caspase-9 enzyme. In vivo studies using H22 xenografts in Kunming mice were conducted with 5g and 5h. The results revealed that the medium dosage group (10 mg/kg) of 5g and the high dosage group (25 mg/kg) of 5h showed significant antitumor activity compared to the control group.