当前位置: X-MOL 学术Eur. J. Med. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
DMXAA-pyranoxanthone hybrids enhance inhibition activities against human cancer cells with multi-target functions
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2017-10-31 , DOI: 10.1016/j.ejmech.2017.10.074
Jie Liu , Fan Zhou , Lei Zhang , Huailing Wang , Jianrun Zhang , Cao Zhang , Zhenlei Jiang , Yanbing Li , Zhijun Liu , Heru Chen

Four 5,6-dimethylxanthone-4-acetic acid (D) and pyranoxanthone (P) hybrids (D-P-n) were design-synthesized based on multi-target-addressed strategy. D-P-4 was confirmed as the most active agent against HepG-2 cell line growth with an IC50 of 0.216 ± 0.031 μM. Apoptosis analysis indicated different contributions of early/late apoptosis/necrosis to cell death for both monomers, the combination (D + P in 1:1 mol ratio) and D-P-4. They all arrested more cells on S phase. Western Blot implied that D-P-4 regulated p53/MDM2 to a better healthy state. Moreover, it improved Bax/Bcl-2 signaling pathway to increase cancer cell apoptosis. In all cases studied, D-P-4 showed the best activity and synergistic effect. All the evidences support that D-P-4 is a better anti-cancer therapy with multi-target functions.



中文翻译:

DMXAA-吡喃并蒽酮杂化物可增强对具有多靶标功能的人类癌细胞的抑制活性

基于多目标寻址策略设计合成了4个5,6-二甲基黄酮-4-乙酸(D)和吡喃酮(P)杂化物(DPn)。证实DP-4是对抗HepG-2细胞系生长的最具活性的药物,IC 50为0.216±0.031μM。凋亡分析表明,两种单体(D  +  P 1:1摩尔比)和DP-4两种单体的早期/晚期凋亡/坏死对细胞死亡的不同贡献。他们都在S期逮捕了更多的细胞。Western Blot暗示DP-4调节p53 / MDM2使其达到更好的健康状态。此外,它改善了Bax / Bcl-2信号传导途径,以增加癌细胞的凋亡。在所有研究的案例中,DP-4表现出最佳的活性和协同作用。所有证据都支持DP-4是一种具有多目标功能的更好的抗癌疗法。

更新日期:2017-10-31
down
wechat
bug