ArticlePharmaceutical research2007
Melittin as a permeability enhancer II: in vitro investigations in human mucus secreting intestinal monolayers and rat colonic mucosae.
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 9 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
9 citing papers in PubMed, 31 citations in OpenAlex.
- Recent advances in melittin-based nanoparticles for antitumor treatment: from mechanisms to targeted delivery strategies.Journal of nanobiotechnology · 2023Review
- Stereoisomer-Dependent Membrane Association and Capacity for Insulin Delivery Facilitated by Penetratin.Pharmaceutics · 2023Article
- Applications and evolution of melittin, the quintessential membrane active peptide.Biochemical pharmacology · 2021Review
- Toxicological Risk Assessment of the Accidental Ingestion of a Honeybee (Frontiers in veterinary science · 2020Review
- Transepithelial transport of PAMAM dendrimers across isolated rat jejunal mucosae in ussing chambers.Biomacromolecules · 2014Article
- Effect of melittin on mice stomach.Saudi journal of biological sciences · 2014Article
- In vitro interactions between the oral absorption promoter, sodium caprate (C(10)) and S. typhimurium in rat intestinal ileal mucosae.Pharmaceutical research · 2008Article
- Melittin as an epithelial permeability enhancer I: investigation of its mechanism of action in Caco-2 monolayers.Pharmaceutical research · 2007Article
- Gliclazide reduces MKC intestinal transport in healthy but not diabetic rats.European journal of drug metabolism and pharmacokineticsArticle
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeMelittin has shown potential as a non-cytotoxic absorption enhancer in Caco-2 monolayers. Our objectives were to assess in vitro efficacy and cytotoxicity of melittin in two intestinal permeability models and investigate the potential mechanism by which melittin might enhance gastrointestinal absorption. MATERIALS AND
methodsThe effects of melittin were examined in the mucus-secreting intestinal cell monolayers, HT29-MTX-E12 (E12), using transepithelial electrical resistance (TER), transmission electron microscopy (TEM) and the MTT viability assay. The effects of melittin on TER, permeability and short circuit current (Isc) were also investigated in rat colon mucosae mounted in Ussing chambers. Ion transporting capacity of tissue was measured in response to secretagogues as surrogate markers of cytotoxicity. Melittin stability was examined by a means of a hemolytic assay. The mechanism by which melittin decreases TER across the rat mucosa was examined with a range of enzymatic inhibitors.
resultsApical addition of melittin resulted in a reversible non-cytotoxic concentration-dependent decrease in TER across E12 monolayers, which was independent of the presence of mucus. Apical addition of melittin reduced TER and increased the permeability of [(14)C]-mannitol across rat colonic mucosae. The melittin-induced drop in TER in rat colon was significantly attenuated by W7 suggesting partial mediation by calmodulin.
conclusionsThe rapid and reversible nature of melittin's permeation enhancing properties and its limited cytotoxicity in polarized intestinal epithelia, suggests a potential drug delivery role for the peptide in oral formulations of poorly absorbed drugs.
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Registered trials
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