Cationic amphipathic triazines with potent anti-bacterial, anti-inflammatory and anti-atopic dermatitis properties

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dc.contributor.authorP Gunasekaran-
dc.contributor.authorG Rajasekaran-
dc.contributor.authorE H Han-
dc.contributor.authorY H Chung-
dc.contributor.authorY J Choi-
dc.contributor.authorY J Yang-
dc.contributor.authorJ E Lee-
dc.contributor.authorH N Kim-
dc.contributor.authorKiram Lee-
dc.contributor.authorJin Seok Kim-
dc.contributor.authorHyun-Jun Lee-
dc.contributor.authorE J Choi-
dc.contributor.authorE K Kim-
dc.contributor.authorS Y Shin-
dc.contributor.authorJ K Bang-
dc.date.accessioned2019-04-09T16:30:10Z-
dc.date.available2019-04-09T16:30:10Z-
dc.date.issued2019-
dc.identifier.issn2045-2322-
dc.identifier.uri10.1038/s41598-018-37785-zko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/18421-
dc.description.abstractThe emergence of multi-drug resistant bacteria forces the therapeutic world into a position, where the development of new and alternative kind of antibiotics is highly important. Herein, we report the development of triazine-based amphiphilic small molecular antibacterial agents as mimics of lysine- and arginine-based cationic peptide antibiotics (CPAs). These compounds were screened against a panel of both Gram-positive and Gram-negative bacterial strains. Further, anti-inflammatory evaluation of these compounds led to the identification of four efficient compounds, DG-5, DG-6, DL-5, and DL-6. These compounds displayed significant potency against drug-resistant bacteria, including methicillin-resistant S. aureus (MRSA), multidrug-resistant P. aeruginosa (MDRPA), and vancomycin-resistant E. faecium (VREF). Mechanistic studies, including cytoplasmic membrane depolarization, confocal imaging and flow cytometry suggest that DG-5, DG-6, and DL-5 kill bacteria by targeting bacterial membrane, while DL-6 follows intracellular targeting mechanism. We also demonstrate that these molecules have therapeutic potential by showing the efficiency of DG-5 in preventing the lung inflammation of lipopolysaccharide (LPS)-induced acute lung injury (ALI) mouse model. More interestingly, DL-6 exhibited impressive potency on atopic dermatitis (AD)-like skin lesions in BALB/c mice model by suppressing pro-inflammatory cytokines. Collectively, these results suggest that they can serve a new class of antimicrobial, anti-inflammatory and anti-atopic agents with promising therapeutic potential.-
dc.publisherSpringer-Nature Pub Group-
dc.titleCationic amphipathic triazines with potent anti-bacterial, anti-inflammatory and anti-atopic dermatitis properties-
dc.title.alternativeCationic amphipathic triazines with potent anti-bacterial, anti-inflammatory and anti-atopic dermatitis properties-
dc.typeArticle-
dc.citation.titleScientific Reports-
dc.citation.number0-
dc.citation.endPage1292-
dc.citation.startPage1292-
dc.citation.volume9-
dc.contributor.affiliatedAuthorKiram Lee-
dc.contributor.affiliatedAuthorJin Seok Kim-
dc.contributor.affiliatedAuthorHyun-Jun Lee-
dc.contributor.alternativeNameGunasekaran-
dc.contributor.alternativeNameRajasekaran-
dc.contributor.alternativeName한은희-
dc.contributor.alternativeName정영호-
dc.contributor.alternativeName최영진-
dc.contributor.alternativeName양유진-
dc.contributor.alternativeName이지은-
dc.contributor.alternativeName김학남-
dc.contributor.alternativeName이기람-
dc.contributor.alternativeName김진석-
dc.contributor.alternativeName이현준-
dc.contributor.alternativeName최은주-
dc.contributor.alternativeName김은경-
dc.contributor.alternativeName신송엽-
dc.contributor.alternativeName방정규-
dc.identifier.bibliographicCitationScientific Reports, vol. 9, pp. 1292-1292-
dc.identifier.doi10.1038/s41598-018-37785-z-
dc.description.journalClassY-
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Ochang Branch Institute > Natural Product Research Center > 1. Journal Articles
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