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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

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Received: 22 May 2013; in revised form: 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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

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.

AMA Style

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. International Journal of Molecular Sciences. 2013; 14(6):12873-12892.

Chicago/Turabian Style

Li, Yuling; Duan, Zhijun; Tian, Yan; Liu, Zhen; Wang, Qiuming. 2013. "A Novel Perspective and Approach to Intestinal Octreotide Absorption: Sinomenine-Mediated Reversible Tight Junction Opening and Its Molecular Mechanism." Int. J. Mol. Sci. 14, no. 6: 12873-12892.


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