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Absorption-enhancing mechanism of sodium caprate and decanoylcarnitine in Caco-2 cells.
J Pharmacol Exp Ther. 1995 Feb; 272(2):739-43.JP

Abstract

The mechanism of action of the absorption enhancers such as sodium caprate (C10) and decanoylcarnitine (DC) was examined. Both C10 and DC increased the epithelial permeability of fluorescein isothiocyanate dextran 4000 and decreased the transepithelial electrical resistance in Caco-2 cell monolayer. Irrespective of the presence or absence of mucosal calcium, C10 rapidly increased intracellular calcium levels dose-dependently. Compound 48/80, a phospholipase C inhibitor, prevented the increases of the intracellular calcium level and permeability of fluorescein isothiocyanate dextran 4000 by C10. Furthermore, N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide hydrochloride, a strong calmodulin inhibitor, also significantly decreased the enhancing effect of C10. These results suggest that C10 releases calcium from intracellular stores via activation of phospholipase C in plasma membrane. The increase of the calcium levels was considered to induce the contraction of calmodulin-dependent actin microfilament, followed by dilatation of the paracellular route. Although DC also increased intracellular calcium levels, neither compound 48/80 nor N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide hydrochloride decreased the enhancing effect of DC. The enhancing mechanisms were different for C10 and DC.

Authors+Show Affiliations

Department of Biopharmaceutics, Tokyo College of Pharmacy, Japan.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

7853188

Citation

Tomita, M, et al. "Absorption-enhancing Mechanism of Sodium Caprate and Decanoylcarnitine in Caco-2 Cells." The Journal of Pharmacology and Experimental Therapeutics, vol. 272, no. 2, 1995, pp. 739-43.
Tomita M, Hayashi M, Awazu S. Absorption-enhancing mechanism of sodium caprate and decanoylcarnitine in Caco-2 cells. J Pharmacol Exp Ther. 1995;272(2):739-43.
Tomita, M., Hayashi, M., & Awazu, S. (1995). Absorption-enhancing mechanism of sodium caprate and decanoylcarnitine in Caco-2 cells. The Journal of Pharmacology and Experimental Therapeutics, 272(2), 739-43.
Tomita M, Hayashi M, Awazu S. Absorption-enhancing Mechanism of Sodium Caprate and Decanoylcarnitine in Caco-2 Cells. J Pharmacol Exp Ther. 1995;272(2):739-43. PubMed PMID: 7853188.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Absorption-enhancing mechanism of sodium caprate and decanoylcarnitine in Caco-2 cells. AU - Tomita,M, AU - Hayashi,M, AU - Awazu,S, PY - 1995/2/1/pubmed PY - 1995/2/1/medline PY - 1995/2/1/entrez SP - 739 EP - 43 JF - The Journal of pharmacology and experimental therapeutics JO - J Pharmacol Exp Ther VL - 272 IS - 2 N2 - The mechanism of action of the absorption enhancers such as sodium caprate (C10) and decanoylcarnitine (DC) was examined. Both C10 and DC increased the epithelial permeability of fluorescein isothiocyanate dextran 4000 and decreased the transepithelial electrical resistance in Caco-2 cell monolayer. Irrespective of the presence or absence of mucosal calcium, C10 rapidly increased intracellular calcium levels dose-dependently. Compound 48/80, a phospholipase C inhibitor, prevented the increases of the intracellular calcium level and permeability of fluorescein isothiocyanate dextran 4000 by C10. Furthermore, N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide hydrochloride, a strong calmodulin inhibitor, also significantly decreased the enhancing effect of C10. These results suggest that C10 releases calcium from intracellular stores via activation of phospholipase C in plasma membrane. The increase of the calcium levels was considered to induce the contraction of calmodulin-dependent actin microfilament, followed by dilatation of the paracellular route. Although DC also increased intracellular calcium levels, neither compound 48/80 nor N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide hydrochloride decreased the enhancing effect of DC. The enhancing mechanisms were different for C10 and DC. SN - 0022-3565 UR - https://www.unboundmedicine.com/medline/citation/7853188/Absorption_enhancing_mechanism_of_sodium_caprate_and_decanoylcarnitine_in_Caco_2_cells_ L2 - https://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=7853188 DB - PRIME DP - Unbound Medicine ER -