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Absorption-enhancing mechanism of EDTA, caprate, and decanoylcarnitine in Caco-2 cells.
J Pharm Sci. 1996 Jun; 85(6):608-11.JP

Abstract

The mechanism of paracellular expansion by absorption enhancers, e.g., EDTA, sodium caprate (C10), and decanoylcarnitine (DC), was studied, the focus being on the process of actin microfilament contraction in the tight junction. The effects of various inhibitors such as KN-62 (a specific inhibitor of Ca2+/calmodulin dependent protein kinase), H7 (a protein kinase C (PKC) inhibitor), and W7 (a calmodulin antagonist) were examined on the paracellular expansion by the enhancers in Caco-2 cells. From the experimental results, the following mechanisms were suggested. EDTA activates PKC by depletion of extracellular calcium via chelation resulting in expansion of the paracellular route. C10 increases the intracellular calcium level by an interaction with the cell membrane independent of cell polarity resulting in contraction with actin microfilament. DC interacts specifically with the apical membrane to increase the intracellular calcium level, but the mechanistic details subsequent to the increase of calcium are not clear.

Authors+Show Affiliations

Department of Biopharmaceutics, Tokyo University of Pharmacy and Life Science, Japan.No affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

8773957

Citation

Tomita, M, et al. "Absorption-enhancing Mechanism of EDTA, Caprate, and Decanoylcarnitine in Caco-2 Cells." Journal of Pharmaceutical Sciences, vol. 85, no. 6, 1996, pp. 608-11.
Tomita M, Hayashi M, Awazu S. Absorption-enhancing mechanism of EDTA, caprate, and decanoylcarnitine in Caco-2 cells. J Pharm Sci. 1996;85(6):608-11.
Tomita, M., Hayashi, M., & Awazu, S. (1996). Absorption-enhancing mechanism of EDTA, caprate, and decanoylcarnitine in Caco-2 cells. Journal of Pharmaceutical Sciences, 85(6), 608-11.
Tomita M, Hayashi M, Awazu S. Absorption-enhancing Mechanism of EDTA, Caprate, and Decanoylcarnitine in Caco-2 Cells. J Pharm Sci. 1996;85(6):608-11. PubMed PMID: 8773957.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Absorption-enhancing mechanism of EDTA, caprate, and decanoylcarnitine in Caco-2 cells. AU - Tomita,M, AU - Hayashi,M, AU - Awazu,S, PY - 1996/6/1/pubmed PY - 2000/7/19/medline PY - 1996/6/1/entrez SP - 608 EP - 11 JF - Journal of pharmaceutical sciences JO - J Pharm Sci VL - 85 IS - 6 N2 - The mechanism of paracellular expansion by absorption enhancers, e.g., EDTA, sodium caprate (C10), and decanoylcarnitine (DC), was studied, the focus being on the process of actin microfilament contraction in the tight junction. The effects of various inhibitors such as KN-62 (a specific inhibitor of Ca2+/calmodulin dependent protein kinase), H7 (a protein kinase C (PKC) inhibitor), and W7 (a calmodulin antagonist) were examined on the paracellular expansion by the enhancers in Caco-2 cells. From the experimental results, the following mechanisms were suggested. EDTA activates PKC by depletion of extracellular calcium via chelation resulting in expansion of the paracellular route. C10 increases the intracellular calcium level by an interaction with the cell membrane independent of cell polarity resulting in contraction with actin microfilament. DC interacts specifically with the apical membrane to increase the intracellular calcium level, but the mechanistic details subsequent to the increase of calcium are not clear. SN - 0022-3549 UR - https://www.unboundmedicine.com/medline/citation/8773957/Absorption_enhancing_mechanism_of_EDTA_caprate_and_decanoylcarnitine_in_Caco_2_cells_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0022-3549(15)50084-1 DB - PRIME DP - Unbound Medicine ER -