Abstract
A class of unimolecular channels formed by pillararene-gramicidin hybrid molecules are presented. The charge status of the peptide domain in these channels has a significant impact on their ion transport and antimicrobial activity. These channels exhibited different membrane-association abilities between microbial cells and mammalian cells. One of the channels displayed a higher antimicrobial activity towards S. aureus (IC50 = 0.55 μM) and negligible hemolytic toxicity, showing potential to serve as a systemic antibiotic.
MeSH terms
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Animals
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology*
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Bacillus subtilis / drug effects*
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Calixarenes / chemistry
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Calixarenes / pharmacology*
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Dose-Response Relationship, Drug
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Erythrocytes / drug effects
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Gramicidin / chemistry
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Gramicidin / pharmacology*
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Ion Channels / antagonists & inhibitors*
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Ion Channels / metabolism
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Ion Transport / drug effects
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Microbial Sensitivity Tests
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Molecular Structure
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Rats
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Staphylococcus aureus / drug effects*
Substances
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Anti-Bacterial Agents
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Ion Channels
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Calixarenes
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Gramicidin