دورية أكاديمية
أعرض في EDS

Repurposing the scorpion venom peptide VmCT1 into an active peptide against Gram-negative ESKAPE pathogens.

التفاصيل البيبلوغرافية
العنوان: Repurposing the scorpion venom peptide VmCT1 into an active peptide against Gram-negative ESKAPE pathogens.
المؤلفون: Pedron CN; Universidade Federal do ABC, Centro de Ciências Naturais e Humanas, 5001 Avenida dos Estados, Santo André, 09210580 SP, Brazil., Araújo I; Universidade Federal do ABC, Centro de Ciências Naturais e Humanas, 5001 Avenida dos Estados, Santo André, 09210580 SP, Brazil., da Silva Junior PI; Instituto Butantan, Laboratório Especial de Toxinologia Aplicada, 1500 Avenida Vital Brasil, 05503900 São Paulo, SP, Brazil., Dias da Silva F; Universidade Federal do ABC, Centro de Ciências Naturais e Humanas, 5001 Avenida dos Estados, Santo André, 09210580 SP, Brazil., Torres MT; Departments of Psychiatry and Microbiology, Perelman School of Medicine, University of Pennsylvania, Philadelphia 19104, PA, United States; Department of Bioengineering, University of Pennsylvania, Philadelphia 19104, PA, United States. Electronic address: marcelot@pennmedicine.upenn.edu., Oliveira Junior VX; Universidade Federal do ABC, Centro de Ciências Naturais e Humanas, 5001 Avenida dos Estados, Santo André, 09210580 SP, Brazil; Universidade Federal de São Paulo, 100 Rua 3 de Maio, 04044020 São Paulo, SP, Brazil. Electronic address: vani.junior@ufabc.edu.br.
المصدر: Bioorganic chemistry [Bioorg Chem] 2019 Sep; Vol. 90, pp. 103038. Date of Electronic Publication: 2019 Jun 08.
نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't
اللغة: English
بيانات الدورية: Publisher: Elsevier Country of Publication: United States NLM ID: 1303703 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1090-2120 (Electronic) Linking ISSN: 00452068 NLM ISO Abbreviation: Bioorg Chem Subsets: MEDLINE
أسماء مطبوعة: Publication: Amsterdam : Elsevier
Original Publication: New York, London, Academic Press.
مواضيع طبية MeSH: Anti-Bacterial Agents/*pharmacology , Antifungal Agents/*pharmacology , Antimicrobial Cationic Peptides/*pharmacology , Scorpion Venoms/*pharmacology, Amino Acid Substitution ; Anti-Bacterial Agents/chemistry ; Anti-Bacterial Agents/toxicity ; Antifungal Agents/chemistry ; Antifungal Agents/toxicity ; Antimicrobial Cationic Peptides/chemistry ; Antimicrobial Cationic Peptides/toxicity ; Candida albicans/drug effects ; Candida tropicalis/drug effects ; Drug Design ; Erythrocytes/drug effects ; Gram-Negative Bacteria/drug effects ; Gram-Positive Bacteria/drug effects ; Hemolysis/drug effects ; Humans ; Microbial Sensitivity Tests ; Molecular Structure ; Scorpion Venoms/chemistry ; Scorpion Venoms/toxicity ; Structure-Activity Relationship
مستخلص: VmCT1 is a cationic antimicrobial peptide (AMP) from the venom of the scorpion Vaejovis mexicanus. VmCT1 and analogs were designed with single substitutions for verifying the influence of changes in physicochemical features described as important for AMPs antimicrobial and hemolytic activities, as well as their effect on VmCT1 analogs resistance against proteases action. The increase of the net positive charge by the introduction of an arginine residue in positions of the hydrophilic face of the helical structure affected directly the antimicrobial activity. Arg-substituted analogs presented activity against Gram-negative bacteria from the ESKAPE list of pathogens that were not observed for VmCT1. Additionally, peptides with higher net positive charge presented increased antimicrobial activity with values ranging from 0.39 to 12.5 μmol L -1 against Gram-positive and Gram-negative bacteria and fungi. The phenylalanine substitution by glycine (position 1), and the valine substitution by a proline residue (position 8) led to analogs with lower hemolytic activity (at concentrations 50 and 100 μmol L -1 , respectively). These results revealed that it is possible to modulate the biological activities of VmCT1 derivatives by designing single substituted-analogs as prospective therapeutics against bacteria and fungi.
(Copyright © 2019 Elsevier Inc. All rights reserved.)
فهرسة مساهمة: Keywords: Antimicrobial peptide; Scorpion venom peptide; Structure-activity relationship; VmCT1
المشرفين على المادة: 0 (Anti-Bacterial Agents)
0 (Antifungal Agents)
0 (Antimicrobial Cationic Peptides)
0 (Scorpion Venoms)
0 (VmCT1 peptide, Vaejovis mexicanus)
تواريخ الأحداث: Date Created: 20190619 Date Completed: 20201019 Latest Revision: 20210120
رمز التحديث: 20231215
DOI: 10.1016/j.bioorg.2019.103038
PMID: 31212183
قاعدة البيانات: MEDLINE
الوصف
تدمد:1090-2120
DOI:10.1016/j.bioorg.2019.103038