粉防己碱和防己诺林碱衍生物作为抗肿瘤药物的设计、合成及生物活性
Design, synthesis and biological activities of tetrandrine and fangchinoline derivatives as antitumer agents.
作者信息
Li Dechao, Liu Haizheng, Liu Yufa, Zhang Qikun, Liu Chao, Zhao Shuhua, Jiao Bo
机构信息
College of Chemistry, Chemical Engineering and Materials Science, Collaborative Innovation Center of Functionalized Probes for Chemical Imaging in Universities of Shandong, Key Laboratory of Molecular and Nano Probes, Ministry of Education, Shandong Provincial Key Laboratory of Clean Production of Fine Chemicals, Shandong Normal University, 88 East Wenhua Road, Jinan 250014, PR China.
College of Chemistry, Chemical Engineering and Materials Science, Collaborative Innovation Center of Functionalized Probes for Chemical Imaging in Universities of Shandong, Key Laboratory of Molecular and Nano Probes, Ministry of Education, Shandong Provincial Key Laboratory of Clean Production of Fine Chemicals, Shandong Normal University, 88 East Wenhua Road, Jinan 250014, PR China.
出版信息
Bioorg Med Chem Lett. 2017 Feb 1;27(3):533-536. doi: 10.1016/j.bmcl.2016.12.029. Epub 2016 Dec 23.
The isolation and modification of natural products is always a very important resources to anti-tumor drugs. Therefore, a novel series of tetrandrine and fangchinoline derivatives were designed and synthesized, and their antiproliferative activities against HepG2, MCF-7 cells were evaluated and described. From the activity result obtained, high to very high activity in vitro has been found, one of the tested compounds (compound 5d) exhibited the most significant cytotoxic effects. Compound 5d increased 29.2, 7.37 times anti-proliferative activity for HepG2 cells and MCF-7 cells compared to sunitinib (IC=16.06μM and 25.41μM). Finally flow cytometry determined that compound 5d could indeed inhibit the proliferation of HepG2 cells via inducing apoptosis.
天然产物的分离与修饰一直是抗肿瘤药物的重要资源。因此，设计并合成了一系列新型粉防己碱和防己诺林碱衍生物，并对其对HepG2、MCF-7细胞的抗增殖活性进行了评估和描述。从获得的活性结果来看，体外活性高至非常高，其中一种受试化合物（化合物5d）表现出最显著的细胞毒性作用。与舒尼替尼（IC=16.06μM和25.41μM）相比，化合物5d对HepG2细胞和MCF-7细胞的抗增殖活性分别提高了29.2倍和7.37倍。最后，流式细胞术确定化合物5d确实可以通过诱导凋亡来抑制HepG2细胞的增殖。
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