ABSTRACT
Glycation is an ageing reaction of naturally occurring sugars with dermal proteins, with clinical signs appearing in vivo around age 30, and increasing steadily/regularly with age. The suppleness of the dermis is affected by the formation of bridges between proteins and sugars (Maillard's reaction). The accumulation of advanced glycation end products (AGEs) in skin plays a very important role in skin ageing. Therefore, natural compounds or extracts that possess antiglycation activities may have great anti-ageing potential. In the present study, Silybum marianum flower extract (SMFE) was demonstrated to possess antiglycation activity. We found that SMFE inhibits glycation reaction between BSA and glucose. In addition, antiglycation activity of SMFE was confirmed in a human skin explants model. SMFE reduced Nε-(carboxymethyl) lysine (CML) expression, whereas SMFE stimulated fibrillin-1 expression compared to treatment with methyglyoxal. An active ingredient contributing to the observed activities was identified as silibinin. The antiglycation activity of silibinin was dose-dependent. The beneficial effects of silibinin may be applied to prevention or management of AGE-mediated pathologies, targeting in a pleiotropic and complementary way the biochemical and cellular bases of skin aging.
Subject(s)
Antioxidants/pharmacology , Flowers/chemistry , Glycosylation/drug effects , Phenols/pharmacology , Plant Extracts/pharmacology , Silybum marianum/chemistry , Skin/drug effects , Adult , Chromatography, High Pressure Liquid , Female , Fibrillin-1 , Fibrillins , Flavonoids/pharmacology , Glycation End Products, Advanced/metabolism , Humans , In Vitro Techniques , Microfilament Proteins/metabolism , Middle Aged , Silybin , Silymarin/metabolism , Skin Irritancy Tests/methodsABSTRACT
The phenolic compound phloretin is a prominent member of the chemical class of dihydrochalcones. Phloretin is specifically found in apple and apple juice and known for its biological properties. We were particularly interested in its potential dermo-cosmetic applications. However, practical limitations of phloretin do exist due to its poor water-solubility. Phloretin was sulfonated with sulfuric acid (98%, wt) and mixed with saturated salt water to produce phloretin 3',3-disulfonate in order to increase its water-solubility. Here we reported the photoprotective effect of phloretin 3',3-disulfonate (PS), a new semi-synthetic derivative of phloretin. Results showed that PS attenuated cyclobutane pyrimidine dimer (CPDs) formation, glutathione (GSH) depletion and apoptosis induced by ultraviolet B (UVB). The photoprotective effect of PS is tightly correlated to the enhancement of nucleotide excision repair (NER) gene expression. Furthemore, PS had inhibitory effects on UVB-induced release of the inflammatory mediators, such as IL-6 and prostaglandin-E2. We also confirmed the safety and clinical efficacy of PS on human skin. Overall, the results demonstrated significant benefits of PS on the protection of keratinocytes against UVB-induced injuries and suggested its potential use in skin photoprotection.
Subject(s)
Keratinocytes/drug effects , Keratinocytes/radiation effects , Phloretin/analogs & derivatives , Phloretin/pharmacology , Sunscreening Agents/chemistry , Sunscreening Agents/pharmacology , Apoptosis/drug effects , Apoptosis/radiation effects , Cell Line , DNA Repair/drug effects , Gene Expression Regulation/drug effects , Glutathione/metabolism , Humans , Keratinocytes/metabolism , Skin Irritancy Tests , Ultraviolet RaysABSTRACT
A white rot fungus Phlebia tremellosa produced lignin degrading enzymes, which showed degrading activity against various recalcitrant compounds. However, manganese peroxidase (MnP) activity, one of lignin degrading enzymes, was very low in this fungus under various culture conditions. An expression vector that carried both the laccase and MnP genes was constructed using laccase genomic DNA of P. tremellosa and MnP cDNA from Polyporus brumalis. P. tremellosa was genetically transformed using the expression vector to obtain fungal transformants showing increased laccase and MnP activity. Many transformants showed highly increased laccase and MnP activity at the same time in liquid medium, and three of them were used to degrade endocrine disrupting chemicals. The transformant not only degraded bisphenol A and nonylphenol more rapidly but also removed the estrogenic activities of the chemicals faster than the wild type strain.
Subject(s)
Basidiomycota/genetics , Basidiomycota/metabolism , Endocrine Disruptors/metabolism , Metabolic Networks and Pathways/genetics , Organisms, Genetically Modified , Benzhydryl Compounds , Biotransformation , Cloning, Molecular , Gene Expression , Genetic Vectors , Laccase/genetics , Laccase/metabolism , Lignin/metabolism , Peroxidases/genetics , Peroxidases/metabolism , Phenols/metabolism , Transformation, GeneticABSTRACT
Irpex lacteus was genetically transformed using an laccase expression vector to get increased laccase producing strains. Stable integration of the vector was confirmed by PCR using the vector-specific primers, and the transformants showed increased laccase activities. When the transformants were grown with several endocrine disrupting chemicals, laccase activity of each transformant was induced up to six times higher than that of the wild type. They showed increased degrading activities against EDCs as well as increased removal rates of estrogenic activities generated by the EDCs than the wild type, and the laccase expression was increased during the degradations of the EDCs.
