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-skinaging 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.
authors.affiliation: School of Natural Sciences, Fairleigh Dickinson University, Teaneck, NJ, USA.
authors.forename: Neena
authors.initials: N
authors.lastname: Philips
authors.forename: Mathew
authors.initials: M
authors.lastname: Samuel
authors.forename: Rosemarie
authors.initials: R
authors.lastname: Arena
authors.forename: Yu-Jun
authors.initials: YJ
authors.lastname: Chen
authors.forename: Jennifer
authors.initials: J
authors.lastname: Conte
authors.forename: Prashanthi
authors.initials: P
authors.lastname: Natarajan
authors.forename: Prashanti
authors.initials: P
authors.lastname: Natrajan
authors.forename: Gerhard
authors.initials: G
authors.lastname: Haas
authors.forename: Salvador
authors.initials: S
authors.lastname: Gonzalez
mesh_terms: D003094:Collagen / Q000096:biosynthesis*; D004549:Elastin / Q000096:biosynthesis*; D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D004797:Enzyme-Linked Immunosorbent Assay; D000071837:Fibrillins; D005347:Fibroblasts / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism; D005419:Flavonoids / Q000302:isolation & purification / Q000494:pharmacology*; D027582:Humulus / Q000737:chemistry; D061965:Matrix Metalloproteinase Inhibitors; D008840:Microfilament Proteins / Q000096:biosynthesis*; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors*; D011427:Propiophenones / Q000302:isolation & purification / Q000494:pharmacology*; D012867:Skin / Q000166:cytology / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D000071837:Fibrillins; D005419:Flavonoids; D061965:Matrix Metalloproteinase Inhibitors; D008840:Microfilament Proteins; D011427:Propiophenones; D003094:Collagen; D004549:Elastin; D010196:Pancreatic Elastase; C104536:xanthohumol