CAS: 22888-70-6; (2R,3R)-3,5,7-Trihydroxy-2-((2R,3R)-3-(4-Hydroxy-3-Methoxyphenyl)-2-(Hydroxymethyl)-2,3-Dihydrobenzo[b][1,4]Dioxin-6-yl)Chroman-4-One

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CAS号1220986-69-5 23-O-acetylsilybin A | CAS号871249-25-1 23-O-acetylsilybin | CAS号34482-56-9 silybin dihemis...

23-O-Acetylsilybin A置于candida Antarctica Lipase B,正丁醇体系中,用 甲基叔丁基醚 用作溶剂,化学反应 60.0H,以67%的收率获得水飞蓟宾
参考文献:Enzymatic Kinetic Resolution Of Silybin Diastereoisomers
标题:Enzymatic Kinetic Resolution Of Silybin Diastereoisomers
摘要:In Nature,The Flavonolignan Silybin (1) occurs As A Mixture Of Two Diastereomers,Silybin A And Silybin B,Which In A Number Of Biological Assays Exhibit Different Activities. A Library Of Hydrolases (Lipases,Esterases,And Proteases) Was Tested For Separating The Silybin A And B Diastereomers By Selective Transcsterification Or By Stereoselective Alcoholysis Of 23-O-Acetylsilybin (2). Novozym 435 Proved To Be The Most Suitable Enzyme For The Preparative Production Of Both Optically Pure Silybins A And B By Enzymatic Discrimination. Gram Amounts Of The Optically Pure Substances Can Be Produced Within One Week,And The New Method Is Robust And Readily Scalable To Tens Of Grams.
Doi:10.1021/np900758D

专利信息

专利号:US-7598291-B2
优先权日:2004-09-02
标题 :Methods and compositions for enhancing collagen and proteoglycan synthesis in the skin
发明人：NIMNI MARCEL; HAN BO
权利人:NIMNI MARCEL; HAN BO
摘要:A composition for application to the skin can stimulate the in vivo synthesis of collagen and proteoglycans and improve the appearance of the skin, increasing its elasticity and fullness. In general, a composition according to the present invention comprises: (1) an antioxidant compound in a quantity sufficient to enhance collagen synthesis in the skin; (2) an organic penetrant in which the antioxidant compound is soluble in a sufficient quantity that a concentration of the antioxidant compound sufficient to enhance collagen synthesis can be applied topically and penetrate the skin; (3) a mixture of essential amino acids; (4) a supplemental source of sulfur; and (5) a topical pharmaceutically acceptable carrier. The antioxidant compound can be lipoic acid, a lipoic acid analogue or derivative, a bioflavonoid, a constituent of ginkgo, or an isoflavone. The organic penetrant is preferably benzyl alcohol. Other ingredients, such as esters of tocopherol and ascorbic acid, can be included.

专利号:US-2010160244-A1
优先权日:2004-09-02
标 题 :Methods and compositions for enhancing collagen, proteoglycan, and glutathione synthesis in the skin
发明人：NIMNI MARCEL; HAN BO
权利人:NIMNI MARCEL; HAN BO
摘要:A composition for application to the skin can stimulate the in vivo synthesis of collagen and proteoglycans and improve the appearance of the skin, increasing its elasticity and fullness. In general, a composition according to the present invention comprises: (1) an antioxidant compound in a quantity sufficient to enhance collagen synthesis in the skin; (2) an organic penetrant in which the antioxidant compound is soluble in a sufficient quantity that a concentration of the antioxidant compound sufficient to enhance collagen synthesis can be applied topically and penetrate the skin; (3) a mixture of essential amino acids or hydrolyzed whey protein; (4) a supplemental source of sulfur; and (5) a topical pharmaceutically acceptable carrier. The antioxidant compound can be lipoic acid or a lipoic acid analogue or derivative. The organic penetrant is preferably benzyl alcohol. Other ingredients, such as esters of tocopherol and ascorbic acid, can be included.

专利号:US-RE40849-E
优先权日:1998-04-30
标题:Method of treatment of glutathione deficient mammals
发明人：KELLER ROBERT H; KIRCHENBAUM DAVID W
权利人:VIT IMMUNE L C
摘要:Glutathione (GSH) is a tripeptide of extreme importance as a catalyst, reductan, and reactant. It can be depleted intracellulary either by forming a direct complex with an electrophilic agent (accomplished investigationally by agents such as bromobenzene or diethyl maleate), by way of inhibition of synthesis, or by subjecting cells to oxidant stress. Most cells, except for epithelia cells, do not have a direct transport capacity for intact GSH. Non-epithelial cells must either transport precursor substrates for GSH synthesis or salvage amino acids from circulating GSH for reuse in intracellular resynthesis. Dietary cysteine is a rate limiting substrate for the synthesis of glutathione and also inhibits GSH efflux. Although GSH is synthesized from precursors in virtually all cells, the liver is the main source of plasma GSH. Protection and support of liver function is paramount to elevating GSH levels. The disclosure is also of a unique combination of nutritional supplements including n-acetyl cysteine, vitamin C, l-glucosamine, n-acetyl d-glucosamine, quercitin, sylimarin, Alpha lipoic acid and high protein, low fat whey that are combined to support various bodily systems involved in glutathione synthesis, reutilization and storage; all intended to elevate glutathione concentration in the mammalian cell.

专利号:EP-1721601-A1
优先权日:2005-05-11
标 题 :Use of taurine for enhancing lipid synthesis in the epidermis
发明人：DOERING THOMAS; WALDMANN-LAUE MARIANNE; WADLE ARMIN; ANDERHEGGEN BERND
权利人:HENKEL KGAA
摘要:The present invention is the use of taurine for stimulating the epidermal synthesis of barrier lipids.

专利号:US-7101854-B2
优先权日:2000-10-09
标题:Tetrapeptide stimulating the functional activity of hepatocytes, pharmacological substance on its basis and the method of its application
发明人：KHAVINSON VLADIMIR KHATSKELEVI
权利人:SANKT PETERBURGSKAYA OBSCHESTV
摘要:The invention refers to the field of medicine and may be applied as a substance stimulating the functional activity of hepatocytes, restoring the synthesis of non-specific proteins, normalising metabolism activating the processes of proliferation and differentiation of the liver cells. There is proposed a new compound -tetrapeptide lysyl-glutamyl-aspartyl-alanine of the general formula Lys-Glu-Asp-Ala [SEQ ID NO:1]. There is proposed a pharmaceutical composition capable of stimulating the functional activity of hepatocytes and a pharmaceutical peptide substance containing as its active base a therapeutically effective quantity of tetrapeptide of the formula Lys-Glu-Asp-Ala [SEQ ID NO:1] or one of its salts intended for parenteral administration. There is proposed a method of stimulating the functional activity of hepatocytes including therapeutic administration to a patient of the pharmaceutical peptide substance in doses 0.01–100 μg/kg of the body weight at least once a day during a period required for attaining a therapeutic effect.

专利号:US-8017776-B2
优先权日:2003-07-15
标题 :Methods for synthesis of acyloxyalkyl compounds
发明人：BHAT LAXMINARAYAN; GALLOP MARK A
权利人:XENOPORT INC
摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.