The Influence of Capsaicin on the Integrity of Microvascular Endothelial Cell Monolayers.

Mathias Kaiser,Carola Förster,Frauke Lankamp,Steffi Ketelhut,Malgorzata Burek,Francisco Goycoolea,Christian Gorzelanny,Stefan Britz,Björn Kemper

doi:10.3390/ijms20010122

Abstract

Microvascular endothelial cells are an essential part of many biological barriers, such as the blood–brain barrier (BBB) and the endothelium of the arteries and veins. A reversible opening strategy to increase the permeability of drugs across the BBB could lead to improved therapies due to enhanced drug bioavailability. Vanilloids, such as capsaicin, are known to reversibly open tight junctions of epithelial and endothelial cells. In this study, we used several in vitro assays with the murine endothelial capillary brain cells (line cEND) as a BBB model to characterize the interaction between capsaicin and endothelial tight junctions.

Highlights

Capsaicin occurs in chili peppers as the main compound responsible for pungency [1]
We investigated the response of murine microvascular endothelial cells to capsaicin and its synthetic analogue, nonivamide, using
Quantified Impact of Vanilloids on the Viability of cEND Cells Using MTT Assays changes in the endothelial cells that affected the actin skeleton as well as the tight junctions by means assess theofmetabolic cellsand upon treatment with capsaicin of theTo dislocation claudin 5competence proteins for of cEND

Summary

Introduction

Capsaicin occurs in chili peppers as the main compound responsible for pungency [1]. Capsaicin is known to ease chronic pain, change body temperature, and reduce obesity [2,3] among other known bioactivities. It was found that capsaicin is able to reversibly open tight junctions [4], a protein network interconnecting epithelial cell layers [5]. We have previously exploited this effect to enhance the permeability of macromolecules by designing a nanocapsule formulation comprising an oil core coated with chitosan, a pseudo-natural aminopolysaccharide [6,7]. The impact of capsaicin derivatives on epithtlial tight junctions was investigated [8]. We investigated whether capsaicin is able to reversibly open endothelial cell monolayers.

Methods

Results

Conclusion