- Design, synthesis and biological activities of tetrandrine and fangchinoline derivatives as antitumer agents
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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 (IC50?=?16.06?μM and 25.41?μM). Finally flow cytometry determined that compound 5d could indeed inhibit the proliferation of HepG2 cells via inducing apoptosis.
- Li, Dechao,Liu, Haizheng,Liu, Yufa,Zhang, Qikun,Liu, Chao,Zhao, Shuhua,Jiao, Bo
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- Synthesis and biological evaluation of fangchinoline derivatives as anti-inflammatory agents through inactivation of inflammasome
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Twenty eight 7-substitued fangchinoline analogues, of which twenty two were novel, were synthesized and evaluated for their effect to inhibit lipopolysaccharide/nigericin (LPS/NIG)-induced IL-1β release at both cell and protein levels at the concentration of 5 μM. Among them, compound 6 exhibited promising inhibitory potency against IL-β activation with an IC50 value of 3.7 μM. Preliminary mechanism study revealed that 6 might target NLRP3 protein, and then block ASC pyroptosome formation with-NLRP3, rather than acting on the activation of the NLRP3 inflammasome (NF-κB and MAPK pathways) or caspase-1 protein. Our current study supported the potential role of compound 6 against IL-β activation, and provided powerful information for developing fangchinoline derivatives into a novel class of anti-inflammatory agents.
- Liu, Ting,Zeng, Qingxuan,Zhao, Xiaoqiang,Wei, Wei,Li, Yinghong,Deng, Hongbin,Song, Danqing
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