Chlorogenic Acid Isomers Isolated from Artemisia lavandulaefolia Exhibit Anti-Rosacea Effects In Vitro

Rosacea is a chronic inflammatory disease affecting facial skin. It is associated with immune and vascular dysfunction mediated via increased expression and activity of cathelicidin and kallikrein 5 (KLK5), a serine protease of stratum corneum. Therefore, KLK5 inhibitors are considered as therapeuti...

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Published in:Biomedicines 2022-02, Vol.10 (2), p.463
Main Authors: Roh, Kyung-Baeg, Jang, Youngsu, Cho, Eunae, Park, Deokhoon, Kweon, Dae-Hyuk, Jung, Eunsun
Format: Article
Language:English
Subjects:
Acids
Angiogenesis
Artemisia lavandulaefolia
Bioactive compounds
cathelicidin
Cell culture
Cell proliferation
Chemokines
Chlorogenic acid
chlorogenic acid isomers
Cytokines
Endothelial cells
Erythema
Immune response
Inflammation
Inflammatory diseases
Isomers
Kallikrein
kallikrein 5
Leukocyte migration
Macrophages
Mast cells
Metabolites
Molecular modelling
Pathophysiology
Peptides
Proteins
Rosacea
Serine proteinase
Skin
Skin diseases
Stratum corneum
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Summary:Rosacea is a chronic inflammatory disease affecting facial skin. It is associated with immune and vascular dysfunction mediated via increased expression and activity of cathelicidin and kallikrein 5 (KLK5), a serine protease of stratum corneum. Therefore, KLK5 inhibitors are considered as therapeutic agents for improving the underlying pathophysiology and clinical manifestation of rosacea. Here, we isolated the active constituents of ( ) and investigated their inhibitory effect on KLK5 protease activity. Using bioassay-guided isolation, two bioactive compounds including chlorogenic acid isomers, 3,5-dicaffeoylquinic acid (isochlorogenic acid A) (1), and 4,5-dicaffeoylquinic acid (isochlorogenic acid C) (2) were isolated from . In this study, we evaluated the effects of isochlorogenic acids A and C on dysregulation of vascular and immune responses to rosacea, and elucidated their molecular mechanisms of action. The two chlorogenic acid isomers inhibit KLK5 protease activity, leading to reduced conversion of inactive cathelicidin into active LL-37. This inhibition of LL-37 production by isochlorogenic acids A and C reveals the efficacy of suppressing the expression of inflammatory mediators induced by LL-37 in immune cells such as macrophages and mast cells. In addition, both isomers of chlorogenic acid directly inhibited the proliferation and migration of vascular endothelial cells induced by LL-37.
ISSN:2227-9059
2227-9059
DOI:10.3390/biomedicines10020463