Anti-wrinkle agent and adam inhibitor
An anti-wrinkle and inhibitor technology, which is applied in the field of new ADAM inhibitors and anti-wrinkle agents for fine wrinkles, can solve the problems of not being able to fully prevent/improve fine wrinkles, and achieve the goal of inhibiting hypertrophy, improving wrinkles, and preventing or improving wrinkles Effect
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[0045] Alkyl glucosides and salts thereof can be produced according to known production methods.
[0046] In addition, the anti-wrinkle agent of the present invention basically consists of an alkyl glucoside or a salt thereof, but may contain other components. By blending this anti-wrinkle agent with a skin external preparation base, a skin external preparation can be provided.
[0047] The compounding amount of the alkyl glucoside or its salt in the above-mentioned skin external preparation varies depending on the form of use, the form of the product, etc., and is not particularly limited. For example, based on the total amount of the skin external preparation, the compounding amount is preferably 0.001 to 10 mass %, more preferably 0.005 to 5% by mass, still more preferably 0.01 to 1% by mass.
[0048] In this specification, the "external skin preparation" includes cosmetics, pharmaceuticals, quasi-drugs, and the like. Similarly, its dosage forms include aqueous solution, ...
Embodiment
[0073] The present invention will be further described in detail below through examples. The present invention is not limited to these Examples. The compounding quantity here is mass %.
[0074] 1. Exploration of new ADAM inhibitors
[0075] The inhibitory effect of ADAM activity was evaluated as follows: TNF-α excised and released from the membrane of human lymphoma-derived U937 cells under the action of ADAM was used as an index to evaluate the inhibitory effect of TNF-α released by the drug. Use this method to screen various compounds to find new ADAM inhibitors.
[0076] The U937 cells derived from human lymphoma were inoculated into 48-well plates, and the number of cells was adjusted to 1×10 5 cells / 0.25ml and cultured overnight at 37°C. A medium containing 30 μm / ml of alkyl glucoside was added and incubated at 37° C. for 30 minutes for pretreatment. Thereafter, 10 nM PMA (phorbol ester: 12-O-tetradecanoylphorbol acetate; Sigma P8139) was added, and cultured at 37° ...
preparation example 1
[0102] Formulation Example 1: Emulsion
[0103] (formula) mass%
[0104] Stearic acid 2.5
[0105] Cetyl Alcohol 1.5
[0106] Vaseline 5.0
[0107] Liquid Paraffin 5.0
[0108] Polyoxyethylene (10mol) monooleate 2.0
[0109] Polyethylene glycol 1500 3.0
[0110] Triethanolamine 1.0
[0111] Carboxyvinyl polymer 0.05
[0112] Decyl beta-D-glucoside 2.0
[0113] Sodium bisulfite 0.01
[0114] Ethyl p-hydroxybenzoate 0.2
[0115] Appropriate amount of spices
[0116] Purified water balance
[0117] (preparation method)
[0118] The carboxyvinyl polymer was dissolved in a small amount of purified water (Phase A). Add polyethylene glycol 1500, triethanolamine, and decyl β-D-glucoside to the remaining purified water, heat to dissolve, and keep at 70°C (aqueous phase). The other ingredients were mixed, heated and melted, and kept at 70°C (oil phase). Add the oil phase to the water phase for pre-emulsification, add phase A, uniformly emulsify with a homomixer, and cool ...
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