Structure-function relationship of king cobra cathelicidin
文献类型：期刊论文
| 作者 | Zhang Y1,3; Zhao H2; Lee WH[*]1; Zhang Y1; Yu GY1,3,4; Liu XD2; Shen JH[*]2 |
| 刊名 | PEPTIDES
 |
| 出版日期 | 2010 |
| 卷号 | 31期号:8页码:1488-1493 |
| 关键词 | Antimicrobial peptide Cathelicidin King cobra Pexiganan |
| 通讯作者 | kmsjh99@yahoo.com.cn ; leewh@mail.kiz.ac.cn |
| 合作状况 | 其它 |
| 英文摘要 | King cobra cathelicidin (OH-CATH) is composed of 34 amino acid residues having strong antibacterial and very weak hemolytic activities as reported by us recently. OH-CATH can be served as a valuable template to develop novel therapeutic drugs. In this study, OH-CATH and six of its analogs were synthesized to explore their structure-function relationships based on their bactericidal and hemolytic activities. Experimental results of OH-CATH(3-34) and OH-CATH(5-34) indicated that the N-terminal 4 amino acid residues of OH-CATH played an important role on its hemolytic activity but had weak effects on its bactericidal activity. Among OH-CATH and its analogs, OH-CATH(5-34) had the lowest hemolytic activity while maintained strong antimicrobial activity. To evaluate its potential usage, the biological activities of OH-CATH(5-34) were compared with those of pexiganan. The bactericidal activity of OH-CATH(5-34) against 5 different species (11 laboratory strains) was 2-4 times stronger than that of pexiganan (4-16 mu g/ml vs 8-32 mu g/ml). Hemolytic activity of OH-CATH(5-34) against human erythrocytes was 0.69% while that of pexiganan was 16.5% at the dosage of 200 mu g/ml. OH-CATH(5-34) showed very weak cytotoxic activities against primary rabbit ventricular endothelial cells and four human cancer cell lines whereas pexiganan showed strong cytotoxic activity against these five cell lines (IC(50)=20-90 mu g/ml). The intravenous LD(50) value of OH-CATH(5-34) on mice was 7-fold higher than that of pexiganan (175 mg/kg vs 25 mg/kg). Taken together, our results suggested that OH-CATH(5-34) should be considered as an excellent candidate for developing therapeutic drugs. |
| 收录类别 | SCI |
| 资助信息 | This work was supported by grants from National Basic Research Program of China (973 Program, 2010CB529800), National Sci- ence & Technology Major Project (2009ZX09103-147), the Chinese National Natural Science Foundation (30630014, 30960384), the Chinese Academy of Sciences “Key Research Direction” (KSCX2- YW-R-088,KSCX2-YW-R-212)and Yunnan Science and Technology Commission (2005PY01-23). |
| 语种 | 英语 |
| 源URL | [http://159.226.149.26:8080/handle/152453/9608]  |
| 专题 | 昆明动物研究所_动物活性蛋白多肽组学 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.Key Laboratory of Animal Models and Human Disease Mechanisms of The Chinese Academy of Sciences & Yunnan Province, Kunming Institute of Zoology, The Chinese Academy of Sciences, Kunming, Yunnan 650223, China 2.Department of Urology, The First Affiliated Hospital of Kunming Medical College, Kunming, Yunnan 650032, China 3.Graduate School of The Chinese Academy of Science, Beijing 100049, China 4.Biochemistry Section of Kunming Medical College, Kunming, Yunnan 650031, China |
| 推荐引用方式 GB/T 7714 | Zhang Y,Zhao H,Lee WH[*],et al. Structure-function relationship of king cobra cathelicidin[J]. PEPTIDES,2010,31(8):1488-1493. |
| APA | Zhang Y.,Zhao H.,Lee WH[*].,Zhang Y.,Yu GY.,...&Shen JH[*].(2010).Structure-function relationship of king cobra cathelicidin.PEPTIDES,31(8),1488-1493. |
| MLA | Zhang Y,et al."Structure-function relationship of king cobra cathelicidin".PEPTIDES 31.8(2010):1488-1493. |
入库方式： OAI收割
来源：昆明动物研究所
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