Inhibitory efficacy of bufadienolides on Na,K-pump activity versus cell proliferation

doi:10.1016/j.bbrep.2016.03.015

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	Inhibitory efficacy of bufadienolides on Na,K-pump activity versus cell proliferation
	Xu, Yinfang 2; Liu, Xuan 1; Schwarz, Silvia 2; Hu, Lihong 1; Guo, Dean1 ; Gu, Quanbao 2; Schwarz, Wolfgang 2
刊名	Biochemistry and biophysics reports
	2016-07
卷号	6 页码:158-164
ISSN号	2405-5808
DOI	10.1016/j.bbrep.2016.03.015
文献子类	Article
英文摘要	Bufadienolides are cytotoxic drugs that may form the basis for anticancer agents. Due to structural and functional similarity to cardiotonic glycosides, application is restricted. We, therefore, investigated correlation of their putative anticancer effects with inhibition of Na,Kpumps. The natural bufalin and three derivatives were tested. The anticancer effects of the drugs were checked by observing their inhibitory effects on proliferation of rat liver cancer cells using MTT assay. Inhibition of Na,K-pump was determined by measuring pump-mediated current of rat α1/β1 and α2/β1 Na,Kpumps expressed in oocytes. All tested bufadienolides inhibited cell proliferation and Na,Kpump activity. An activity coefficient =100x/IC was used to describe drug effectivity as anticancer drug. Natural bufalin exhibited lowest effectivity on cell proliferation, and also the value for rat α1 isoform was the lowest (0.08), the α2 isoform was much less sensitive (=1.00). The highest values were obtained for the BF238 derivative with =0.88 and 2.64 for the α1 and α2 isoforms, respectively. Therefore, we suggest that search for bufalin derivatives with high anticancer effect and low affinity for both Na,Kpump isoforms may be a promising strategy for development of anticancer drugs.
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/266317]
专题	上海中药现代化研究中心
作者单位	1.Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China 2.Shanghai Research Center of Acupuncture and Meridians, Shanghai, China;
推荐引用方式 GB/T 7714	Xu, Yinfang,Liu, Xuan,Schwarz, Silvia,et al. Inhibitory efficacy of bufadienolides on Na,K-pump activity versus cell proliferation[J]. Biochemistry and biophysics reports,2016,6:158-164.
APA	Xu, Yinfang.,Liu, Xuan.,Schwarz, Silvia.,Hu, Lihong.,Guo, Dean.,...&Schwarz, Wolfgang.(2016).Inhibitory efficacy of bufadienolides on Na,K-pump activity versus cell proliferation.Biochemistry and biophysics reports,6,158-164.
MLA	Xu, Yinfang,et al."Inhibitory efficacy of bufadienolides on Na,K-pump activity versus cell proliferation".Biochemistry and biophysics reports 6(2016):158-164.