Abstract

Perilla (Perilla frutescens L.) leaves have shown therapeutic efficacy in the treatment of inflammatory disorders, allergies, bronchial asthma, and systemic damage due to free radicals. In the present study we analyzed the active constituents in perilla leaves using high-performance liquid chromatography (HPLC) and isolated luteolin, a polyphenolic flavonoid. We investigated the anti-inflammatory and antipruritic properties of luteolin. Luteolin inhibited the secretion of inflammatory cytokines such as interleukin-1β (IL-1 β) and tumor necrosis factor-α (TNF-α) from human mast cells (HMC-1) stimulated with phorbol myristate acetate plus calcium ionophore A23187 in a dose-dependent manner. Luteolin also significantly reduced the histamine release from rat peritoneal mast cells stimulated by compound 48/80, a potent histamine liberator. Furthermore, the administration of luteolin markedly inhibited the scratching behavior and vascular permeability induced by pruritogens, such as compound 48/80 or serotonin, in ICR mice. These results suggested that luteolin has potential as a therapeutic agent against inflammation and itch-related skin diseases.

Highlights

  • Inflammation is a protective aspect of the body’s response to injury or infection and induces release of various chemicals that stimulate nerve endings

  • In the present study we focused on luteolin, a flavonoid extracted from perilla leaves and investigated its anti-inflammatory and antipruritic effects on human mast cells (HMC-1), rat peritoneal mast cells (RPMCs) and ICR mice

  • Luteolin isolated from the Lonicera japonica flowers was shown to inhibit pro-inflammatory cytokine and inflammatory mediator production by HMC-1 cells activated with phorbol 12-myristate 13-acetate (PMA) plus A23187, and suppress inflammation-associated gene expression by blocking the NF-κB pathway [21,22,23]

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Summary

Introduction

Inflammation is a protective aspect of the body’s response to injury or infection and induces release of various chemicals that stimulate nerve endings. IgE-FcεRI on the cell surface, they release histamine and mast cell granule proteins as well as a wide variety of pro-inflammatory mediators such as interleukin (IL)-1, IL-6, IL-8, and tumor necrosis factor (TNF)-α, which may exacerbate allergic diseases [5,6]. These mediators affect nerve, muscle, and endothelial cells and induce itching, contraction, vasodilation and edema. Perilla leaves have long been used to treat various diseases, including depression, tumors, bacterial and fungal infections, allergies and some intestinal disorders They inhibit Th2-cytokine production, anti-DNP IgE production and IgA nephropathy [13,14]. In the present study we focused on luteolin, a flavonoid extracted from perilla leaves and investigated its anti-inflammatory and antipruritic effects on human mast cells (HMC-1), rat peritoneal mast cells (RPMCs) and ICR mice

The Chemical Structure and Effect of Luteolin on Cell Survival
Inhibition of TNF-α and IL-1β Production by Luteolin
Inhibition of Histamine Release by Luteolin
Effects of Luteolin on Scratching Behavior and Vascular Permeability
Chemicals
Perilla Leaves and Luteolin Isolation
Animals
Cell Culture and Stimulation
MTT Assay
Histamine Assay
Cytokine ELISA
Scratching Behavior
3.10. Skin Vascular Permeability
Conclusions
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