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徐学清实验室在J Med Chem上发表研究论文

 

    徐学清授课题组于近日在J Med Chem上发表了题为“Functional characterization of A Novel Lipopolysaccharide-binding Antimicrobial and Anti-inflammatory Peptide in vitro and in vivo”的研究论文。
    抗菌肽是脊椎动物防御病原微生物侵入的重要组分,是研发新型抗菌药物的希望。该论文报道了从沼水蛙(Hylarana guentheri)皮肤中鉴定的新抗菌肽Esculentin-1GNEsculentin-1GN 的氨基酸序列为GLFSKKGGKGGKSWIKGVFKGIKGIGKEVGGDVIRTGIEIAACKIKGEC,其在水溶液中具有双亲性α螺旋结构,能通过破坏细菌细胞膜杀死细菌,也能抑制脂多糖诱导的炎性因子NOIL-1βIL-6TNF-α的分泌却促进IL-10的表达。Esculentin-1GN还能结合D-(+)-半乳糖醛酸和脂多糖,抑制脂多糖激活的炎性通路。最后论文通过体内实验证实,该肽在体内能抑制甲叉菜胶诱导的急性炎症。因此,具有脂多糖结合、抗菌和抗炎活性的Esculentin-1GN将是研发新型抗感染药物的优良模板。

    此论文受到国家自然科学基金面上项目、南方医科大学杰青培育计划等基金资助。2015级硕士研究生曾白霜为本论文的第一作者,徐学清教授为该论文的通讯作者。J Med Chem为大类:医学 2区;小类: 药物化学 1区,IF=6.253

Zeng B, Chai J, Deng Z, Ye T, Chen W, Li D, Chen X, Chen M, Xu X. Functional characterization of A Novel Lipopolysaccharide-binding Antimicrobial and Anti-inflammatory Peptide in vitro and in vivo. J Med Chem. 2018 Nov 14. doi: 10.1021/acs.jmedchem.8b01358. [Epub ahead of print]
Abstract
Antimicrobial peptides (AMPs) are key components of host immune defense of vertebrates against microbial invasions. Here, we report a new AMP (Esculentin-1GN) characterized from the skin of the frog Hylarana guentheri. Esculentin-1GN (GLFSKKGGKGGKSWIKGVFKGIK
GIGKEVGGDVIRTGIEIAACKIKGEC) with high amphipathic α-helical structure in membrane-mimetic environments has the microbial-killing activity by destruction of the cell membrane. Moreover, Esculentin-1GN inhibits LPS-induced expression of pro-inflammatory nitric oxide, interleukin-1β, interleukin-6 and tumor necrosis factor while enhances expression of interleukin-10. Furthermore, Esculentin-1GN can bind to D-(+)-Galacturonic acid and LPS. Meanwhile, Esculentin-1GN suppresses the activation of inflammatory response pathway induced by LPS. In addition, Esculentin-1GN significantly reduces acute inflammation in carrageenan-induced mice paw. Taken together, the novel LPS-binding Esculentin-1GN with antimicrobial and anti-inflammatory activities will be an excellent temple designing new antibiotic formulations.

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文章链接:https://www.ncbi.nlm.nih.gov/pubmed/?term=Functional+characterization+of+A+Novel+Lipopolysaccharide-binding+Antimicrobial+and+Anti-inflammatory+Peptide+in+vitro+and+in+vivo+