Application of L-2-oxathiaazalane-4-carboxylic acid and ester derivative thereof in cosmeceutical product
A technology of thiazepine and pentane, applied in the field of application of L-2-oxothiazelane-4-carboxylic acid and its ester derivatives as skin cosmeceuticals, can solve the problem Scientific data support and other issues to achieve the effect of restoring skin vitality, improving aging, and improving flexibility
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Embodiment 1
[0067] Embodiment 1: Preparation of L-2-oxothiazepine-4-carboxylate derivatives
[0068] The preparation of OTC chloride is carried out by OTC and oxalyl chloride (Oxalyl Chloride) or thionyl chloride (Thionyl Chloride) under the reaction condition of 50 ℃ in equimolar ratio. OTC esters can be composed of OTC chlorides and corresponding alcohols, such as straight chain C 1 -C 18 Alcohol is obtained by adding triethylamine (TEA) and dimethylaminopyridine (DMAP) in acetonitrile solvent. Another preparation method can be obtained by passing OTC and corresponding alcohol compounds in a dry reaction solvent and passing through dry HCI gas. The reaction mixture can be separated and purified on a silica gel column with ethyl acetate, n-hexane mixture, or other traditional normal phase eluents. Earned OTC C 1 -C 18 Ester derivatives by time-flight mass spectrometry, 1 The structure was confirmed by H-NMR, and its purity was determined to be 99% by HPLC-ESI / MS (product of Agilent...
Embodiment 2
[0069] Embodiment 2: subcutaneous animal model
[0070] Female hairless mice (6-8 weeks) were caged with sterilized chow, water, and in a 14 / 10 hr light / dark environment. [6- 13 C] OTC and [6- 13 C] OTC C 1 -C 18 Ester derivative dissolved in 200 mg commercially available Vanicream Lite TM Medium mixing (for Parmacentical Specialties, Inc company product, wherein contains purified water, white petroleum jelly (white petrolatum), cetearethalcohol, ceteareth-20, propylene glycol (propylene glycol, CH 3 CHOHCH 2 OH), sorbitol monostearate, polyethylene glycol monostearate, sorbic acid and BHT. And the concentration of OTC and OTC ester compound is 20% (weight ratio). The formulated paste was applied to the skin of the mice every day for a week. Control mice were treated with 200 mg of Vanicream Lite without OTC and OTC esters TM . After the mice in the experimental group and the control group died painlessly by intracardiac injection of pentobarbital, the skin was colle...
Embodiment 3
[0073] Example 3: General Rules for Cosmeceuticals
[0074] The obtained skin tissue was homogenized in 5% trichloroacetic acid (trichoroacetic acid) for 10 seconds and then centrifuged at 4°C (10,000xg). After 15 minutes of centrifugation, the supernatant was taken out and DTT was added to make it in the solution The final concentration in is 20mM. Leave at room temperature for 2 hours to reduce any possible oxidized glutathione, subcutaneous glutathione 13 C / 12 C isotopic abundance values and gas chromatography-mass spectrometry conditions were performed as described above. The role of traditional antioxidants is to quench free radicals in the skin to protect the skin from environmental harmful substances. Such antioxidant groups include, for example, vitamin C containing phenolic hydroxyl and ester derivatives beta-carotene, catechin, carcumin, and ferulic acid. Ferulic acid derivations, gillic acid derivations, lycopene, reductive acid, rosemarinic acid, tannic acid...
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