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Anti-HIV-1 activity and structure-activity-relationship study of a fucosylated glycosaminoglycan from an echinoderm by targeting the conserved CD4 induced epitope
文献类型：期刊论文
| 作者 | Lian W1,2; Wu MY1; Huang N3; Gao N1; Xiao C1,2; Li Z1; Zhang ZG1; Zheng YT[*]3; Peng WL[*]2; Zhao JH[*]1 |
| 刊名 | BIOCHIMICA ET BIOPHYSICA ACTA
 |
| 出版日期 | 2013 |
| 卷号 | 1830期号:10页码:4681-4691 |
| 关键词 | Cluster of Differentiation 4 induced epitope Anti-human immunodeficiency virus activity Envelope glycoprotein 120 Glycosaminoglycan |
| 通讯作者 | zhengyt@mail.kiz.ac.cn ; pengwenlie@21cn.com ; zhaojinhua@yahoo.com |
| 英文摘要 | Background: Fucosylated glycosaminoglycan (FG) is a novel glycosaminoglycan with a chondroitin sulfate-like backbone and fucose sulfate branches. The aim of this study is to investigate the mechanism and structure-activity relationships (SAR) of FG for combating HIV-1 infection. Methods: Anti-HIV activities of FGs were assessed by a cytopathic effect assay and an HIV-1 p24 detection assay. The biomolecule interactions were explored via biolayer interferometry technology. The SAR was established by comparing its anti-HIV-1 activities, conserved CD4 induced (CD4i) epitope-dependent interactions and anticoagulant activities. Results: FG efficiently and selectively inhibited the X4- and R5X4-tropic HIV-1 infections in C8166 cells with little cytotoxicity against C8166 cells and PBMCs. Our data indicated that FG bound to gp120 with nanomolar affinity and may interact with CD4i of gp120. Additionally, the CD4i binding affinity of FG was higher than that of dextran sulfate. SAR studies suggested that the unique sulfated fucose branches account for the anti-HIV-1 activity. The molecular size and present carboxyl groups of FG may also play important roles in various activities. Notably, several FG derivatives showed higher anti-HIV-1 activities and much lower anticoagulant activities than those of heparin. Conclusions: FG exhibits strong activity against X4- and R5X4-tropic HIV-1 infections. The mechanism may be related to targeting CD4i of gp120, which results in inhibition of HIV-1 entry. The carboxyl group substituted derivatives of FG (8.5-12.8 kDa), might display high anti-HIV-1 activity and low anticoagulant activity. General significance: Our data supports further the investigation of FG derivatives as novel HIV-1 entry inhibitors targeting CD4i. |
| 收录类别 | SCI |
| 资助信息 | This work was funded in part by the Yunnan Provincial Science and Technology Department in China (Nos. 2010CI116, 2012BC011 and 2012FB177), National Natural Science Foundation of China (No. 81102372),OutstandingTechnicalTalentFoundationoftheChinese AcademyofSciences andWestLightFoundationoftheChineseAcademy of Sciences. |
| 语种 | 英语 |
| WOS记录号 | WOS:000323854900031 |
| 公开日期 | 2014-10-17 |
| 源URL | [http://159.226.149.42:8088/handle/152453/8078]  |
| 专题 | 昆明动物研究所_分子免疫药理学 昆明动物研究所_动物模型与人类重大疾病机理重点实验室 |
| 作者单位 | 1.State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, Yunnan 650201, China 2.School of Life Sciences, Sun Yat-sen University, Guangzhou, Guangdong 510275, China 3.Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Science and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, China |
| 推荐引用方式 GB/T 7714 | Lian W,Wu MY,Huang N,et al. Anti-HIV-1 activity and structure-activity-relationship study of a fucosylated glycosaminoglycan from an echinoderm by targeting the conserved CD4 induced epitope[J]. BIOCHIMICA ET BIOPHYSICA ACTA,2013,1830(10):4681-4691. |
| APA | Lian W.,Wu MY.,Huang N.,Gao N.,Xiao C.,...&Zhao JH[*].(2013).Anti-HIV-1 activity and structure-activity-relationship study of a fucosylated glycosaminoglycan from an echinoderm by targeting the conserved CD4 induced epitope.BIOCHIMICA ET BIOPHYSICA ACTA,1830(10),4681-4691. |
| MLA | Lian W,et al."Anti-HIV-1 activity and structure-activity-relationship study of a fucosylated glycosaminoglycan from an echinoderm by targeting the conserved CD4 induced epitope".BIOCHIMICA ET BIOPHYSICA ACTA 1830.10(2013):4681-4691. |
入库方式： OAI收割
来源：昆明动物研究所
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