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Int. J. Mol. Sci. 2013, 14(6), 12873-12892; doi:10.3390/ijms140612873
Article

A Novel Perspective and Approach to Intestinal Octreotide Absorption: Sinomenine-Mediated Reversible Tight Junction Opening and Its Molecular Mechanism

1
,
1,* , 2
,
1
 and
1
1 Department of Gastroenterology, First Affiliated Hospital of Dalian Medical University, Dalian 116011, China 2 College of Pharmacy, Dalian Medical University, Dalian 116011, China
* Author to whom correspondence should be addressed.
Received: 22 May 2013 / Revised: 5 June 2013 / Accepted: 7 June 2013 / Published: 20 June 2013
(This article belongs to the Section Biochemistry, Molecular Biology and Biophysics)
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Abstract

In this work, we assessed the effects of sinomenine (SN) on intestinal octreotide (OCT) absorption both in Caco-2 cell monolayers and in rats. We also investigated the molecular mechanisms of tight junction (TJ) disruption and recovery by SN-mediated changes in the claudin-1 and protein kinase C (PKC) signaling pathway. The data showed that exposure to SN resulted in a significant decrease in the expression of claudin-1, which represented TJ weakening and paracellular permeability enhancement. Then, the recovery of TJ after SN removal required an increase in claudin-1, which demonstrated the transient and reversible opening for TJ. Meanwhile, the SN-mediated translocation of PKC-α from the cytosol to the membrane was found to prove PKC activation. Finally, SN significantly improved the absolute OCT bioavailability in rats and the transport rate in Caco-2 cell monolayers. We conclude that SN has the ability to enhance intestinal OCT absorption and that these mechanisms are related at least in part to the important role of claudin-1 in SN-mediated, reversible TJ opening via PKC activation.
Keywords: octreotide; sinomenine; intestinal absorption; tight junction octreotide; sinomenine; intestinal absorption; tight junction
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Li, Y.; Duan, Z.; Tian, Y.; Liu, Z.; Wang, Q. A Novel Perspective and Approach to Intestinal Octreotide Absorption: Sinomenine-Mediated Reversible Tight Junction Opening and Its Molecular Mechanism. Int. J. Mol. Sci. 2013, 14, 12873-12892.

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