2-(甲氧基甲氧基)苯硼酸置于盐酸,Bis-Triphenylphosphine-Palladium(II) Chloride,三氟化硼乙醚,Potassium Carbonate,甲基磺酰氯体系中,用 甲醇 作为反应溶剂,化学反应 39.0H,反应生成 大豆异黄酮 参考文献:Palladium-Catalyzed Carbonylative Cross-Coupling Reaction Of Arylboronic Acids With Aryl Electrophiles: Synthesis Of Biaryl Ketones 标题:Palladium-Catalyzed Carbonylative Cross-Coupling Reaction Of Arylboronic Acids With Aryl Electrophiles: Synthesis Of Biaryl Ketones 摘要:The Carbonylative Cross-Coupling Reaction Of Arylboronic Acids With Aryl Electrophiles (Ari,Arbr,And Arotf) To Yield Unsymmetrical Biaryl Ketones Was Carried Out In Anisole At 80 Degrees C In The Presence Of A Palladium Catalyst And A Base; The Reaction Selectively Proceeded Under An Atmospheric Pressure Of Carbon Monoxide When Pdcl2(Pph3)(2)(3 Mol %)/k2Co3 (3 Equiv) Were Used For Aryl Iodides And Pdcl2(Dppf) (3 Mol %)/k2Co3 (3 Equiv)/ki (3 Equiv) For The Bromides Or The Triflates. The Carbonylation Of Arylboronic Acids With Benzyl Halides Gave Aryl Benzyl Ketones. DOI:10.1021/jo980417B
专利号:WO-2012004653-A8 优先权日:2010-07-07 标 题:Method for inhibition of nf-kb gene expression 发明人:BHATTACHARYA SUSHMITA; DASGUPTA SUMAN; BARMA POMY; BISWAS ANINDITA; PAL BIKASH CHANDRA; BHATTACHARYA SHELLEY; BHATTACHARYA SAMIR; BORDOLOI MANOBJYOTI; BARUA NABIN CHANDRA; RAO PARUCHURI GANGADHAR 权利人:COUNCIL SCIENT IND RES; VISVA BHARATI SCHOOL OF LIFE SCIENCES; BHATTACHARYA SUSHMITA; DASGUPTA SUMAN; BARMA POMY; BISWAS ANINDITA; PAL BIKASH CHANDRA; BHATTACHARYA SHELLEY; BHATTACHARYA SAMIR; BORDOLOI MANOBJYOTI; BARUA NABIN CHANDRA; RAO PARUCHURI GANGADHAR 摘要:The present invention discloses a method of inhibition of synthesis of NF- kB by inhibiting its gene expression using isoflavones Daidzein and Daidzin. Daidzein, a non toxic dietary supplement isoflavone of the structure (1) and 7-O-ϵ-glucopyranosyl daidzein of the structure (2) are novel inhibitors of NF- kB which blocks the synthesis of NF- kB by inhibiting its gene expression and have no toxic effect. Both daidzein of the structure (1) and daidzin of the structure (2) ameliorate palmitate induced overexpression of NF- kB in skeletal muscle cells by eliminating the inhibition of NF- kB on insulin stimulated glucose uptake. Daidzein inhibits NF- kB expression in prostate and breast cancer cells that increased mortality of these cancer cells. Daidzin of the structure (2) has very good bioavailibility over daidzein of structure (1). Daidzein of the structure (1) is not absorbed when orally fed to mice as it is eliminated from the gut through glucuronidation process catalyzed by UGT1. Daidzin of the structure (2) is glucosylated daidzein and is protected from UGT1 mediated degradation and is hydrolysed to daidzein which is absorbed and remains for more than 4 hours in blood and is expected to be distributed to different tissues and organs. Daidzein of the structure (1) and daidzin of the structure (2) reduce palmitate stimulated increased synthesis of NF- kB significantly. Daidzein inhibits formation of NF- kB -DNA complex stimulated by palmitate and both daidzein and daidzin inhibited NF- kB expression which leads to reduction of its DNA binding. Daidzein of the structure(1) was obtained from soy leaves through chromatography and both natural and synthetic daidzein and daidzin have same biological activities.
专利号:WO-2025081225-A1 优先权日:2023-10-17 标 题 :Synthesis of polyphenols 发明人:TURLAND CADE LACHLAN; GROLMAN DAVID; BEHRENDORFF JAMES BRUCE YARNTON HAYCOCK; MORADI SHAYLI VARASTEH; THOMSON RAINE ELIZABETH STURT 权利人:Delica Therapeutics Pty Ltd 摘要:The present disclosure relates to polyphenols, including flavonoids, flavones and cannflavins, and methods of synthesising polyphenols. The present disclosure provides methods, enzymes and compositions that may be useful in the synthesis of polyphenols.
专利号:US-2012003164-A1 优先权日:1998-12-30 标题 :Cosmetic or dermatological composition containing an active agent which stimulates synthesis of the protein hsp 32 in the skin 发明人:NIZARD CARINE; MOREAU MARIELLE; BONTE FREDERIC 权利人:NIZARD CARINE; MOREAU MARIELLE; BONTE FREDERIC; DIOR CHRISTIAN PARFUMS 摘要:A dermatological or cosmetological composition for an external topical administration, included together with pharmaceutically and/or cosmetologically acceptable excipients: at least one UVA-stabilizing and/or UVB-stabilizing screening agent, at least one compound capable of activating the endogenous synthesis of Heat Shock Protein (HSP) 32 or a functional peptide fragment of such a protein, and forskolin or any extract containing it.
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-2004101523-A1 优先权日:1989-07-27 标题:Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension 发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J 权利人:SEARLE & CO 摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.
专利号:WO-9101724-A1 优先权日:1989-07-27 标题 :Renal-selective prodrugs for the treatment of hypertension 发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J 权利人:SEARLE & CO 摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as depa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitors compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-Y-glutamyl fusaric acid is preferred.
参考文献:10.1080/01635580903285015 摘要:Messina M, Hilakivi-Clarke L. Early Intake Appears to Be the Key to the Proposed Protective Effects of Soy Intake Against Breast Cancer. Nutrition and Cancer. 2009 Nov 10;61(6):792–8. doi: 10.1080/01635580903285015. 参考文献:10.1080/01635580903285163 摘要:Sahin K, Akdemir F, Tuzcu M, Sahin N, Onderci M, Ozercan R, Ilhan N, Kilic E, Seren S, Kucuk O. Genistein Suppresses Spontaneous Oviduct Tumorigenesis in Quail. Nutrition and Cancer. 2009 Nov 10;61(6):799–806. doi: 10.1080/01635580903285163. 参考文献:10.1021/np900588q 摘要:Zhang H, Yang F, Qi J, Song XC, Hu ZF, Zhu DN, Yu BY. Homoisoflavonoids from the fibrous roots of Polygonatum odoratum with glucose uptake-stimulatory activity in 3T3-L1 adipocytes. J Nat Prod. 2010 Apr 23;73(4):548–52. doi: 10.1021/np900588q. 参考文献:10.1021/jf903796c 摘要:Xu B, Chang SK, Liu Z, Yuan S, Zou Y, Tan Y. Comparative studies on the chemical and cell-based antioxidant activities and antitumor cell proliferation properties of soy milk manufactured by conventional and commercial UHT methods. J Agric Food Chem. 2010 Mar 24;58(6):3558–66. doi: 10.1021/jf903796c. 参考文献:10.1186/1475-2891-10-73 摘要:Bojić M, Debeljak Ž, Tomičić M, Medić-Šarić M, Tomić S. Evaluation of antiaggregatory activity of flavonoid aglycone series. Nutrition Journal. 2011 Jul 11;10(1):73. doi: 10.1186/1475-2891-10-73.