BF211, a derivative of bufalin, enhances the cytocidal effects in multiple myeloma cells by inhibiting the IL-6/JAK2/STAT3 pathway

doi:10.1016/j.intimp.2018.08.016

	BF211, a derivative of bufalin, enhances the cytocidal effects in multiple myeloma cells by inhibiting the IL-6/JAK2/STAT3 pathway
	Wu, Xiao-Yu 2; Tian, Fang 3; Su, Min-Hui 3; Wu, Min 3; Huang, Yue 3; Hu, Li-Hong 4; Jin, Liang 2; Zhu, Xue-Jun 1,3
刊名	International immunopharmacology
	2018-11
卷号	64 页码:24-32
ISSN号	1878-1705
DOI	10.1016/j.intimp.2018.08.016
文献子类	Article
英文摘要	Despite remarkable advances in multiple myeloma (MM) therapy, this condition remains incurable. BF211 is an active compound derived from bufalin, which is isolated from the Traditional Chinese Medicine, Chansu. In this study, we explored the cytotoxicity of BF211 in 20 tumor cell lines and discovered that the MM cell lines, ARP-1 and CAG, exhibited greater sensitivity to BF211. Compared with bufalin, BF211 induced a greater apoptotic effect and lower acute toxicity at nanomolar concentration. The IL-6/JAK2/STAT3 signaling pathway is essential to the progression and development of MM. We showed that exogenous IL-6 promoted MM cell proliferation in a dose-dependent manner and this effect was blocked by BF211. Furthermore, BF211 suppressed the phosphorylation of JAK2 and STAT3 both in vivo and in vitro. In a mouse MM xenograft model, BF211 significantly inhibited tumor growth and did not affect body weight. In conclusion, the anti-MM activity of BF211 is mediated mainly by suppressing the IL-6/JAK2/STAT3 signaling pathway. Thus, we suggest that BF211 warrants further investigation in clinical trials in MM.
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/266820]
专题	中国科学院上海药物研究所
通讯作者	Hu, Li-Hong; Jin, Liang; Zhu, Xue-Jun
作者单位	1.Division of Hematology, Department of Medicine, Jiangsu Provincial Traditional Chinese Medical Hospital, Nanjing, Jiangsu Province, China 2.State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Screening, School of Life Science and Technology, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing, Jiangsu 210009, China; 3.Department of Center Laboratory, Jiangsu Provincial Traditional Chinese Medical Hospital, Nanjing, Jiangsu Province, China; 4.Pharmacy Institute, Nanjing University of Chinese Medicine, Nanjing, Jiangsu Province, China;
推荐引用方式 GB/T 7714	Wu, Xiao-Yu,Tian, Fang,Su, Min-Hui,et al. BF211, a derivative of bufalin, enhances the cytocidal effects in multiple myeloma cells by inhibiting the IL-6/JAK2/STAT3 pathway[J]. International immunopharmacology,2018,64:24-32.
APA	Wu, Xiao-Yu.,Tian, Fang.,Su, Min-Hui.,Wu, Min.,Huang, Yue.,...&Zhu, Xue-Jun.(2018).BF211, a derivative of bufalin, enhances the cytocidal effects in multiple myeloma cells by inhibiting the IL-6/JAK2/STAT3 pathway.International immunopharmacology,64,24-32.
MLA	Wu, Xiao-Yu,et al."BF211, a derivative of bufalin, enhances the cytocidal effects in multiple myeloma cells by inhibiting the IL-6/JAK2/STAT3 pathway".International immunopharmacology 64(2018):24-32.