Ontology type: schema:ScholarlyArticle Open Access: True
2019-12
AUTHORSPethaiah Gunasekaran, Ganesan Rajasekaran, Eun Hee Han, Young-Ho Chung, Young-Jin Choi, Yu Jin Yang, Ji Eun Lee, Hak Nam Kim, Kiram Lee, Jin-Seok Kim, Hyun-Jun Lee, Eun-Ju Choi, Eun-Kyung Kim, Song Yub Shin, Jeong Kyu Bang
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. More... »
PAGES1292
http://scigraph.springernature.com/pub.10.1038/s41598-018-37785-z
DOIhttp://dx.doi.org/10.1038/s41598-018-37785-z
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PUBMEDhttps://www.ncbi.nlm.nih.gov/pubmed/30718691
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]Download the RDF metadata as: json-ld nt turtle xml License info
JSON-LD is a popular format for linked data which is fully compatible with JSON.
curl -H 'Accept: application/ld+json' 'https://scigraph.springernature.com/pub.10.1038/s41598-018-37785-z'
N-Triples is a line-based linked data format ideal for batch operations.
curl -H 'Accept: application/n-triples' 'https://scigraph.springernature.com/pub.10.1038/s41598-018-37785-z'
Turtle is a human-readable linked data format.
curl -H 'Accept: text/turtle' 'https://scigraph.springernature.com/pub.10.1038/s41598-018-37785-z'
RDF/XML is a standard XML format for linked data.
curl -H 'Accept: application/rdf+xml' 'https://scigraph.springernature.com/pub.10.1038/s41598-018-37785-z'
This table displays all metadata directly associated to this object as RDF triples.
331 TRIPLES
21 PREDICATES
80 URIs
21 LITERALS
9 BLANK NODES