A novel analog of antimicrobial peptide Polybia-MPI, with thioamide bond substitution, exhibits increased therapeutic efficacy against cancer and diminished toxicity in mice

doi:10.1016/j.peptides.2010.06.019

CORC > 兰州大学 > 兰州大学 > 基础医学院 > 期刊论文

	A novel analog of antimicrobial peptide Polybia-MPI, with thioamide bond substitution, exhibits increased therapeutic efficacy against cancer and diminished toxicity in mice
	Zhang, W; Li, J; Liu, LW; Wang, KR; Song, JJ; Yan, JX; Li, ZY; Zhang, BZ; Wang, R; Zhang, BZ (reprint author), Lanzhou Univ, Inst Biochem & Mol Biol, Sch Basic Med Sci, Key Lab Preclin Study New Drugs Gansu Prov, 222 Tian Shui S Rd, Lanzhou 730000, Gansu, Peoples R China.
刊名	PEPTIDES
	2010-10
卷号	31 期号:10 页码:1832-1838
关键词	Antimicrobial peptide Anticancer Thioamide Enzymatic stability Toxicity
ISSN号	0196-9781
DOI	10.1016/j.peptides.2010.06.019
文献子类	Article
英文摘要	Polybia-MPI (MPI), a short cationic alpha-helical antimicrobial peptide, exhibited excellent anticancer activity and selectivity in vitro in our previous studies. To improve its in vivo application, we synthesized an analog (MPI-1) of MPI by replacing the C terminal amide -[CO-NH2] with thioamide -psi[CS-NH2]. Although there is just one atom difference, the MPI-1 exhibited some surprising properties. In vitro studies revealed that MPI-1 exhibited relatively high lytic activity over MPI, whereas its stability to enzymatic degradation in serum was improved remarkably. Despite the enhanced toxicity in vitro, MPI-1 exhibited significantly lower mortality to mice than MPI at 75 mg/kg. Importantly, in vivo anticancer activity study indicated that MPI-1 could remarkably suppress the growth of sarcoma xenograft tumors more efficiently than MPI. Therefore, the significantly improved anticancer activity and predominantly lower in vivo toxicity might allow MPI-1 to be a good candidate for future anticancer treatment. (C) 2010 Elsevier Inc. All rights reserved.
学科主题	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
出版地	NEW YORK
资助项目	国家自然科学基金项目 ; 国家科技重大专项
项目编号	National Natural Science Foundation of China [20932003, 90813012] ; Ministry of Science and Technology of China [2009ZX09503-017, 2007AA02Z321]
语种	英语
WOS记录号	WOS:000282617200006
资助机构	NSFC ; MOST
内容类型	期刊论文
源URL	[http://ir.lzu.edu.cn/handle/262010/121461]
专题	基础医学院_期刊论文
通讯作者	Zhang, BZ (reprint author), Lanzhou Univ, Inst Biochem & Mol Biol, Sch Basic Med Sci, Key Lab Preclin Study New Drugs Gansu Prov, 222 Tian Shui S Rd, Lanzhou 730000, Gansu, Peoples R China.
推荐引用方式 GB/T 7714	Zhang, W,Li, J,Liu, LW,et al. A novel analog of antimicrobial peptide Polybia-MPI, with thioamide bond substitution, exhibits increased therapeutic efficacy against cancer and diminished toxicity in mice[J]. PEPTIDES,2010,31(10):1832-1838.
APA	Zhang, W.,Li, J.,Liu, LW.,Wang, KR.,Song, JJ.,...&Zhang, BZ .(2010).A novel analog of antimicrobial peptide Polybia-MPI, with thioamide bond substitution, exhibits increased therapeutic efficacy against cancer and diminished toxicity in mice.PEPTIDES,31(10),1832-1838.
MLA	Zhang, W,et al."A novel analog of antimicrobial peptide Polybia-MPI, with thioamide bond substitution, exhibits increased therapeutic efficacy against cancer and diminished toxicity in mice".PEPTIDES 31.10(2010):1832-1838.