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Synthesis, in silico screening and preclinical evaluation studies of a hexapeptide analogue for its antimicrobial efficacy

机译：合成，在硅筛选和六肽类似物中抗微生物疗效的临床前评价研究

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摘要

A novel Trp-Arg rich antimicrobial peptide was designed and the synthesized nonapeptide (hexapeptide analogue AMP) was screened for its antimicrobial and hemolytic activity. In silico studies were performed against a microbial target protein to validate the findings. In vivo studies were carried out for preclinical evaluation of the designed peptide sequence using Tc-99m as the radioisotope. The results obtained from the in vitro studies revealed excellent antibacterial activity against E. coli with low hemolytic activity. The in silico studies with the crystal structure of E. coli Pencillin Binding Protein 1b (PBP1b) glycosyltransferase (PDB ID: 3VMA) show higher electrostatic and hydrophobic interactions than the co-crystallized ligand. The radio labeling yield of the Tc-99m-labeled AMP was found to be >98%. The blood-kinetics in rabbits and the biodistribution studies in mice confirmed rapid renal excretion from systemic circulation. The scintigraphic analysis for the infection and inflammation animal models revealed that the radiolabel was able to discriminate between infection and inflammation in both mice and rats. Furthermore, blocking experiments in scintigraphy were also carried out using cold peptide to confirm the specificity towards the E. coli infection. Based on the above findings, we consider the designed AMP as a novel antimicrobial agent with the ability to image bacterial infection in vivo by using a gamma emitting radioisotope.
机译：设计了一种新型TRP-ARG富抗杀菌肽，并筛选合成的非肽（六肽类似物AMP），用于其抗微生物和溶血活性。在硅研究中进行针对微生物靶蛋白进行的，以验证发现。在体内研究进行了使用TC-99M作为放射性同位素的设计肽序列的临床前评价。从体外研究获得的结果揭示了具有低溶血活性的大肠杆菌的优异抗菌活性。在硅结构的晶体结构中的晶体结构的研究表明，比共结晶的配体显示出更高的静电和疏水相互作用的静电和疏水相互作用。发现TC-99M标记的放大器的无线电标记产率为> 98％。兔子中的血液动力学和小鼠的生物分布研究证实了来自全身循环的快速肾脏排泄。感染和炎症动物模型的闪烁术分析表明，放射性标签能够区分小鼠和大鼠的感染和炎症。此外，还使用冷肽进行闪烁术中的阻断实验，以确认对大肠杆菌感染的特异性。基于上述研究结果，我们认为设计的放大器作为一种新型抗微生物剂，具有通过使用γ发射放射性同位素来成像体内细菌感染的新型抗微生物剂。

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  • 来源
    《RSC Advances》 |2015年第118期|共7页
  • 作者

    Kaul Ankur; Tiwari Anjani K.; Varshney Raunak; Mishra Anil K.;

  • 作者单位

    Inst Nucl Med &

    Allied Sci Div Cyclotron &

    Radiopharmaceut Sci Delhi 110054 India;

    Inst Nucl Med &

    Allied Sci Div Cyclotron &

    Radiopharmaceut Sci Delhi 110054 India;

    Inst Nucl Med &

    Allied Sci Div Cyclotron &

    Radiopharmaceut Sci Delhi 110054 India;

    Inst Nucl Med &

    Allied Sci Div Cyclotron &

    Radiopharmaceut Sci Delhi 110054 India;

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  • 正文语种 eng
  • 中图分类 化学;
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