A novel phosphoramide compound, DCZ0805, shows potent anti-myeloma activity via the NF-kappa B pathway

doi:10.1186/s12935-021-01973-1

	A novel phosphoramide compound, DCZ0805, shows potent anti-myeloma activity via the NF-kappa B pathway
	Gao, Xuejie 1; Li, Bo 2; Ye, Anqi 3; Wang, Houcai 1; Xie, Yongsheng 1; Yu, Dandan 1; Xu, Zhijian 2; Shi, Bingqing 1; Zhang, Hui 1; Feng, Qilin 1
刊名	CANCER CELL INTERNATIONAL
	2021-05-30
卷号	21 期号:1 页码:10
关键词	Multiple myeloma Anti-tumor activity NF-kappa B
DOI	10.1186/s12935-021-01973-1
通讯作者	Shi, Jumei(shijumei@tongji.edu.cn) ; Zhu, Weiliang(wlzhu@simm.ac.cn)
英文摘要	Background: Multiple myeloma (MM) is a highly aggressive and incurable clonal plasma cell disease with a high rate of recurrence. Thus, the development of new therapies is urgently needed. DCZ0805, a novel compound synthesized from osalmide and pterostilbene, has few observed side effects. In the current study, we intend to investigate the therapeutic effects of DCZ0805 in MM cells and elucidate the molecular mechanism underlying its anti-myeloma activity. Methods: We used the Cell Counting Kit-8 assay, immunofluorescence staining, cell cycle assessment, apoptosis assay, western blot analysis, dual-luciferase reporter assay and a tumor xenograft mouse model to investigate the effect of DCZ0805 treatment both in vivo and in vitro. Results: The results showed that DCZ0805 treatment arrested the cell at the G0/G1 phase and suppressed MM cells survival by inducing apoptosis via extrinsic and intrinsic pathways. DCZ0805 suppressed the NF-kappa B signaling pathway activation, which may have contributed to the inhibition of cell proliferation. DCZ0805 treatment remarkably reduced the tumor burden in the immunocompromised xenograft mouse model, with no obvious toxicity observed. Conclusion: The findings of this study indicate that DCZ0805 can serve as a novel therapeutic agent for the treatment of MM.
资助项目	National Natural Science Foundation of China[81870158] ; National Natural Science Foundation of China[81900212] ; National Natural Science Foundation of China[81670194] ; National Science &Technology Major Project Key New Drug Creation and Manufacturing Program, China[2018ZX09711002]
WOS关键词	MULTIPLE-MYELOMA ; CELL-CYCLE ; CANCER ; APOPTOSIS ; INFLAMMATION ; REVEALS
WOS研究方向	Oncology
语种	英语
出版者	BMC
WOS记录号	WOS:000656075800001
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/297241]
专题	中国科学院上海药物研究所
通讯作者	Shi, Jumei; Zhu, Weiliang
作者单位	1.Tongji Univ, Shanghai Peoples Hosp 10, Dept Hematol, Sch Med, 301 Yanchang Rd, Shanghai 200072, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Drug Discovery & Design Ctr, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 3.Shanghai Jiao Tong Univ, Shanghai Childrens Med Ctr, Sch Med, Shanghai, Peoples R China
推荐引用方式 GB/T 7714	Gao, Xuejie,Li, Bo,Ye, Anqi,et al. A novel phosphoramide compound, DCZ0805, shows potent anti-myeloma activity via the NF-kappa B pathway[J]. CANCER CELL INTERNATIONAL,2021,21(1):10.
APA	Gao, Xuejie.,Li, Bo.,Ye, Anqi.,Wang, Houcai.,Xie, Yongsheng.,...&Zhu, Weiliang.(2021).A novel phosphoramide compound, DCZ0805, shows potent anti-myeloma activity via the NF-kappa B pathway.CANCER CELL INTERNATIONAL,21(1),10.
MLA	Gao, Xuejie,et al."A novel phosphoramide compound, DCZ0805, shows potent anti-myeloma activity via the NF-kappa B pathway".CANCER CELL INTERNATIONAL 21.1(2021):10.