Direct inhibition of elastase and matrixmetalloproteinases and stimulation of biosynthesis of fibrillar collagens, elastin, and fibrillins by xanthohumol Journal Article


Authors: Philips, N.; Samuel, M.; Arena, R.; Chen, Y. J.; Conte, J.; Natrajan, P.; Haas, G.; Gonzalez, S.
Article Title: Direct inhibition of elastase and matrixmetalloproteinases and stimulation of biosynthesis of fibrillar collagens, elastin, and fibrillins by xanthohumol
Abstract: In skin aging there is deterioration of the extracellular matrix's collagen and elastin fibers, from its reduced biosynthesis and increased degradation by elastase and matrixmetalloproteinases (MMPs). Xanthohumol is a flavonoid isolated from the hop plant Humulus lupulus L., with anti-microbial, antioxidant, anti-inflammatory, and anti-carcinogenic properties. The goal of this research was to investigate xanthohumol as an anti-skin- aging agent via its beneficial regulation of the extracellular matrix. To this purpose, we examined the direct effect of xanthohumol on the activities of elastase and MMPs (MMPs 1, 2, and 9) and its effect on the expression (protein and/or transcription levels) of collagens (types I, III, and V), elastin, and fibrillins (1 and 2) in dermal fibroblasts. Xanthohumol significantly inhibited elastase and MMP-9 activities from its lowest concentration, and MMP-1 and MMP-2 at its higher concentrations, which implies a greater protective effect on elastin. It dramatically increased the expression of types I, III, and V collagens, and elastin, fibrillin-1, and fibrillin-2 in dermal fibroblasts. The effects were similar to those of ascorbic acid. This is the first report identifying xanthohumol's potential to improve skin structure and firmness: it simultaneously inhibits the activities of elastase/MMPs and stimulates the biosynthesis of fibrillar collagens, elastin, and fibrillins.
Keywords: cytology; metabolism; drug effect; enzymology; enzyme inhibitor; microfilament proteins; enzyme linked immunosorbent assay; skin; biosynthesis; chemistry; drug antagonism; enzyme inhibitors; matrix metalloproteinase; collagen; fibroblast; fibroblasts; flavonoid; flavonoids; actin binding protein; enzyme-linked immunosorbent assay; isolation and purification; matrix metalloproteinases; elastin; fibrillin; pancreatic elastase; propiophenone derivative; xanthohumol; humulus; propiophenones
Journal Title: Journal of Cosmetic Science
Volume: 61
Issue: 2
ISSN: 1525-7886
Publisher: Soc Cosmetic Chemists  
Date Published: 2010-03-01
Start Page: 125
End Page: 132
Language: English
PUBMED: 20447364
PROVIDER: scopus
DOI/URL:
Notes: --- - "Export Date: 20 April 2011" - "Source: Scopus"
Citation Impact
MSK Authors
  1. Salvador Gonzalez Rodriguez
    203 Rodriguez