ArticlePharmaceutical research2007
Melittin as an epithelial permeability enhancer I: investigation of its mechanism of action in Caco-2 monolayers.
Article in Pharmaceutical research, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 38 citations in OpenAlex.
- A high-throughput gut-on-chip platform to study the epithelial responses to enterotoxins.Scientific reports · 2024Article
- Applications and evolution of melittin, the quintessential membrane active peptide.Biochemical pharmacology · 2021Review
- Antimicrobial Peptides in Gut Health: A Review.Frontiers in nutrition · 2021Review
- Dual Action of the PN159/KLAL/MAP Peptide: Increase of Drug Penetration across Caco-2 Intestinal Barrier Model by Modulation of Tight Junctions and Plasma Membrane Permeability.Pharmaceutics · 2019Article
- The In Vitro Protective Role of Bovine Lactoferrin on Intestinal Epithelial Barrier.Molecules (Basel, Switzerland) · 2019Article
- Candida albicans-Induced Epithelial Damage Mediates Translocation through Intestinal Barriers.mBio · 2018Article
- Production of antibacterial peptide from bee venom via a new strategy for heterologous expression.Molecular biology reports · 2014Article
- Fucoidan enhances intestinal barrier function by upregulating the expression of claudin-1.World journal of gastroenterology · 2013Article
- CriticalSorb™ promotes permeation of flux markers across isolated rat intestinal mucosae and Caco-2 monolayers.Pharmaceutical research · 2012Article
- Melittin modulates keratinocyte function through P2 receptor-dependent ADAM activation.The Journal of biological chemistry · 2012Article
- Omeprazole induces gastric transmucosal permeability to the peptide bradykinin.World journal of gastroenterology · 2010Article
- Mechanistic analysis of chemical permeation enhancers for oral drug delivery.Pharmaceutical research · 2008Article
- Melittin as a permeability enhancer II: in vitro investigations in human mucus secreting intestinal monolayers and rat colonic mucosae.Pharmaceutical research · 2007Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeMelittin is an amphipathic antimicrobial peptide which has been shown to enhance the permeability of mannitol and reduce transepithelial electrical resistance (TER) across Caco-2 monolayers. The aim of this work was to further examine the potential of melittin as a paracellular permeability enhancer and to investigate the mechanism of interaction with tight junction proteins in Caco-2. MATERIALS AND
methodsThe permeability of a range of fluorescent markers of differing molecular weights across monolayers was examined and immunofluorescence and western blotting analysis of tight junction proteins were also carried out. The mechanism of TER reduction was also examined using cell signalling inhibitors.
resultsApical but not basolateral addition of melittin increased the permeability of a range FITC-dextrans (4-70 kDa) across monolayers. Melittin effects were reversible and no cytotoxicity was evident in polarized Caco-2 epithelia at the concentrations used. Altered expression of ZO-1, E-cadherin and F-actin was also detected. The phospholipase A2 inhibitors, aristolochic acid and indomethacin and the cyclooxygenase inhibitor, piroxicam, partially attenuated melittin-induced TER reduction, suggesting that part of the mechanism by which melittin opens tight junctions involves prostaglandin signalling.
conclusionsApically-added melittin opens tight junctions, causing dramatic TER reductions with significant increases in flux of dextrans. These effects appear mediated in part via PLA2 and involve alterations in specific tight junction proteins.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.