Rational Design of a Potent Antimicrobial Peptide Based on the Active Region of a Gecko Cathelicidin
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Le résumé fourni par la source
The emergence of multidrug-resistant (MDR) bacteria presents a significant challenge to public health, increasing the risk of infections that are resistant to current antibiotic treatment. Antimicrobial peptides (AMPs) offer a promising alternative to conventional antibiotics in the prevention of MDR bacterial infections. In the present study, we identified a novel cathelicidin AMP from Gekko japonicus, which exhibited broad-spectrum antibacterial activity against both Gram-negative and Gram-positive bacteria, with minimal inhibitory concentrations ranging from 2.34 to 4.69 μg/mL. To improve its potential therapeutic application, a series of peptides was synthesized based on the active region of the gecko-derived cathelicidin. The lead peptide (RH-16) showed an antimicrobial activity comparable to that of the parent peptide. Structural characterization revealed that RH-16 adopted an amphipathic α-helical conformation. Furthermore, RH-16 demonstrated neither hemolytic nor cytotoxic activity but effectively killed a wide range of clinically isolated, drug-resistant bacteria. The antimicrobial activity of RH-16 was attributed to the nonspecific targeting of bacterial membranes, leading to rapid bacterial membrane permeabilization and rupture. RH-16 also retained its antibacterial activity in plasma and exhibited mild toxicity in vivo . Notably, RH-16 offered robust protection against skin infection in a murine model. Therefore, this newly identified cathelicidin AMP may be a strong candidate for future pharmacological development targeting multidrug resistance. The use of a rational design approach for isolating the minimal antimicrobial unit may accelerate the transition of natural AMPs to clinically applicable antibacterial agents.
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Le contrôle bibliographique ouvert
DOI retrouvé dans Crossref DOI retrouvé ; titre concordant.
- Titre Crossref
- Rational Design of a Potent Antimicrobial Peptide Based on the Active Region of a Gecko Cathelicidin
- Date Crossref
- 05/02/2024
- Éditeur
- American Chemical Society (ACS)
- Type
- journal-article
Ce recoupement confirme des métadonnées liées au DOI. Il ne confirme ni la méthode ni les conclusions de l’étude, et il ne compte pas comme une seconde source scientifique indépendante.
Où se fait cette recherche
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Chinese Academy of Medical Sciences & Peking Union Medical College pays non établi dans la noticeUniversité ou école supérieure
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Kunming Medical University Third Department of Breast Surgery pays non établi dans la noticeUniversité ou école supérieure
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First Affiliated Hospital of Kunming Medical University pays non établi dans la noticeÉtablissement de santé
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Kunming Institute of Botany pays non établi dans la noticeStructure de recherche
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Chinese Academy of Sciences pays non établi dans la noticeOrganisme public
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Chinese Academy of Medical Sciences and Peking Union Medical College Institute of Medical Biology pays non établi dans la noticeUniversité ou école supérieure
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State Key Laboratory of Phytochemistry and Plant Resources in West China pays non établi dans la noticeStructure de recherche
Chinese Academy of Medical Sciences & Peking Union Medical College, Third Department of Breast Surgery — Kunming Medical University et First Affiliated Hospital of Kunming Medical University, avec 4 autres affiliations.
Une affiliation ne permet pas de déduire la nationalité d’un auteur.