| Novel Broad-Spectrum Antimicrobial Peptide Derived from Anoplin and Its Activity on Bacterial Pneumonia in Mice | |
| Gou, Sanhu1,2; Li, Beibei1; Ouyang, Xu1; Ba, Zufang1; Zhong, Chao1,3; Zhang, Tianyue1; Chang, LinLin1,3; Zhu, Yuewen1; Zhang, Jingying1,3; Zhu, Ningyi1; Zhang, Yun1; Liu, Hui1; Ni, Jingman1,3 | |
| 2021-08-12 | |
| Online publication date | 2021-06 |
| Source Publication | JOURNAL OF MEDICINAL CHEMISTRY Impact Factor & Quartile |
| ISSN | 0022-2623 |
| EISSN | 1520-4804 |
| Volume | 64Issue:15Pages:11247-11266 |
| page numbers | 20 |
| Abstract | The emergence of multidrug-resistant bacteria has major issues for treating bacterial pneumonia. Currently, anoplin (GLLKRIKTLL-NH2) is a natural antimicrobial candidate derived from wasp venom. In this study, a series of new antimicrobial peptide (AMP) anoplin analogues were designed and synthesized. The relationship between their biological activities and their positive charge, hydrophobicity, amphipathicity, and secondary structure are described. The characteristic shared by these peptides is that positively charged amino acids and hydrophobic amino acids are severally arranged on the hydrophilic and hydrophobic surface of the a-helix to form a completely amphiphilic structure. To achieve ideal AMPs, below the range of the threshold of the cytotoxicity and hemolytic activity, their charges and hydrophobicity were increased as much. Among the new analogues, A-21 (KWWKKWKKWW-NH2) exhibited the greatest antimicrobial activity (geometric mean of minimum inhibitory concentrations = 4.76 mu M) against all the tested bacterial strains, high bacterial cell selectivity in vitro, high effectiveness against bacterial pneumonia in mice infected with Klebsiella pneumoniae, and low toxicity in mice (LD50 = 82.01 mg/kg). A-21 exhibited a potent bacterial membrane-damaging mechanism and lipopolysaccharide-binding ability. These data provide evidence that A-21 is a promising antimicrobial candidate for the treatment of bacterial pneumonia. |
| Publisher | AMER CHEMICAL SOC |
| DOI | 10.1021/acs.jmedchem.1c00614 |
| Indexed By | SCOPUS ; SCIE ; IC |
| Language | 英语 |
| WOS Research Area | Pharmacology & Pharmacy |
| WOS Subject | Chemistry, Medicinal |
| WOS ID | WOS:000685644300041 |
| Original Document Type | Article |
| PMID | 3418067 |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | https://ir.lzu.edu.cn/handle/262010/471069 |
| Collection | 兰州大学 |
| Corresponding Author | Ni, Jingman |
| Affiliation | 1.Lanzhou Univ, Sch Pharm, Inst Pharmaceut, Lanzhou 730000, Peoples R China; 2.Lanzhou Univ, Sch Life Sci, Inst Biochem & Mol Biol, Lanzhou 730000, Peoples R China; 3.Lanzhou Univ, Sch Basic Med Sci, Key Lab Preclin Study New Drugs Gansu Prov, Lanzhou 730000, Peoples R China |
| Recommended Citation GB/T 7714 | Gou, Sanhu,Li, Beibei,Ouyang, Xu,et al. Novel Broad-Spectrum Antimicrobial Peptide Derived from Anoplin and Its Activity on Bacterial Pneumonia in Mice[J]. JOURNAL OF MEDICINAL CHEMISTRY,2021,64(15):11247-11266. |
| APA | Gou, Sanhu.,Li, Beibei.,Ouyang, Xu.,Ba, Zufang.,Zhong, Chao.,...&Ni, Jingman.(2021).Novel Broad-Spectrum Antimicrobial Peptide Derived from Anoplin and Its Activity on Bacterial Pneumonia in Mice.JOURNAL OF MEDICINAL CHEMISTRY,64(15),11247-11266. |
| MLA | Gou, Sanhu,et al."Novel Broad-Spectrum Antimicrobial Peptide Derived from Anoplin and Its Activity on Bacterial Pneumonia in Mice".JOURNAL OF MEDICINAL CHEMISTRY 64.15(2021):11247-11266. |
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