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Res Disclosure_Tinogards as Skin Active Disclosure Number: IPCOM000130489D
Publication Date: 2005-Oct-25

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The Prior Art Database


Certain hindered phenols such as glycerides of ß-(3,5-di-tert.butyl-4-hydroxyphenyl) propanoic acid and fatty acids, 1,1-bis(2-hydroxy-3,5-di-tert.butylphenyl)-ethane, 3-(3-[3,5-di-tert.butyl-4-hydroxyphenyl]-propionamidyl)phenylsulfonate, pentaerythritol-tetrakis¬(3-[3',5'-di-tert.¬butyl-4'-hydroxy¬phenyl]-propionate), certain benzofuranones such as 5,7-di-tert.butyl-3-(dimethylphenyl)-(9d)-2(3H)-benzofuranone, and certain hindered nitroxyl, hydroxylamine and hydroxylamine salt compounds such as 2,2,6,6-tetramethyl-1,4-dihydroxypiperidinium citrate have antioxidant and antiradical effects and exhibit marked antiinflammatory action in personal care formulations, e.g. when used in skin-care preparations, bath preparations, make-ups, deodorants or antiperspirants, light-protective preparations, such as sun milks, lotions, creams or oils, pre-tanning preparations, after-sun preparations, depigmenting preparations, medicated bar soaps, antifungals, anti bacterials, insect-repellents, shaving preparations, fragrance preparations, hair-treatment preparations.

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Everyday harmful environment influences are surrounding the human skin; UV radiation, air pollutants, chemical oxidants...The results of that is conducting to the generation on skin of Radical Oxygen Species (ROS), highly reactive intermediates derived from atmospheric molecular oxygen, which are mostly represented by free radical species (OH°, NO° and O2

-°) or by singlet oxgen (1O2), Hydrogen Peroxide (H2O2) or Lipid

Hydroperoxide (LOOH) and else.

Ref. J.F Nicolay (Exsymol SA), Pollution and Ageing: Antioxidants for skin, C&T vol.116, N°8-2001, p37-44
Those ROS oxidize lipids, break down enzymes and matrix proteins, affect the DNA and are leading to the premature ageing of the skin with drying effect, loss of elasticity, strong irritation and promoting the destruction of constituents inside skin.

Photo-oxidation, generated by UV radiation, causes depletion of cellular antioxidants, initiates DNA damage leading to the formation of Thymidine dimmers, activates systems leading to immuno-suppression, releases of inflammatory mediators from variety of skin cells. Ref.S.Pillai & al, UV radiation and skin ageing: roles of ROS...-a review, Int.Journal of Cosm.Science 2005, 27, p17-34

The inflammatory and ROS generation activate the matrix metalloproteinases (MMP) but also cause oxidative damage to cellular proteins, lipids and carbohydrates.

MMPs are a group of Zinc-dependent endopeptidases capable of degrading Extra Cellular Matrix (ECM) components such as collagen, elastin, fibronectin, gelatine, laminin....leading to photo-aged skin with wrinkle lines and dyspigmentation reactions.

To prevent skin from such damages, we can "boost" the endogeneous antioxidant defense system which include both enzymatic and non enzymatic components:

- enzymatic such as Glutathione peroxidase, Catalase, Superoxide dismutase,

    Methallothionein... - non enzymatic such as Glutathione, vitamin E, Vitamin C, Ubiquinol, β-carotene... We can also use specific ingredients such as:

- anti-inflammatory compounds; cyclooxygenase inhibitors, inhibitors of cytokine generation... - scavengers and quenchers of ROS - inhibitors of MMP expression and activity - inhibitors of elastase involved in te formation of skin wrinkles - promoting agent of collagen biosynthesis

Substances having antioxidant and antiradical effects reside in their capability of local reducing of the active oxygen form in the immediate surrounding of the application to the skin, protecting against the oxidation of tissue components and their modification by secondary products of lipid oxidation. After the application to the skin, the antioxidants and antiradicals can protect intercellular lipids, cell membranes, low molecular compounds, such as amino acids with thiol group and glutathione, and further macromolecules, such as proteins and glycosamin glycanes against direct oxidation. Reactive forms of oxygen affect the lipids, which results, in the final phase, in reactive aldehydes that can irrevers...