从姜黄中发现可保护细胞免受β-淀粉样蛋白损伤的天然产物：一项针对阿尔茨海默病的药物研发工作。
Discovery of natural products from Curcuma longa that protect cells from beta-amyloid insult: a drug discovery effort against Alzheimer's disease.
作者信息
Park So-Young, Kim Darrick S H L
机构信息
Program for Collaborative Research in Pharmaceutical Sciences and Department of Medicinal Chemistry and Pharmacognosy (m/c 877), College of Pharmacy, University of Illinois at Chicago, 60612, USA.
出版信息
J Nat Prod. 2002 Sep;65(9):1227-31. doi: 10.1021/np010039x.
From Curcuma longa, two novel compounds, 4' '-(3' "-methoxy-4' "-hydroxyphenyl)-2' '-oxo-3' '-enebutanyl 3-(3'-methoxy-4'hydroxyphenyl)propenoate (calebin-A, 1) and 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,4,6-heptatrien-3-one (2), and seven known compounds, 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione (curcumin, 3), 1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl)-1,6-heptadiene-3,5-dione (demethoxycurcumin, 4), 1,7-bis(4-hydroxyphenyl)-1,6-heptadiene-3,5-dione (bisdemethoxycurcumin, 5), 1-hydroxy-1,7-bis(4-hydroxy-3-methoxyphenyl)-6-heptene-3,5-dione (6), 1,7-bis(4-hydroxyphenyl)-1-heptene-3,5-dione (7), 1,7-bis(4-hydroxyphenyl)-1,4,6-heptatrien-3-one (8), and 1,5-bis(4-hydroxy-3-methoxyphenyl)-1,4-pentadien-3-one (9), were isolated following a bioassay-guided fractionation scheme utilizing an assay to detect protection of PC12 cells from beta-amyloid insult. Compounds 1, 3-5, and 7 were found to more effectively protect PC12 cells from betaA insult (ED(50) = 0.5-10 microg/mL) than Congo red (10) (ED(50) = 37-39 microg/mL).
从姜黄中，通过生物活性导向的分离方案，利用检测PC12细胞免受β-淀粉样蛋白损伤的保护作用的测定法，分离出两种新型化合物，4''-(3''-甲氧基-4''-羟基苯基)-2''-氧代-3''-烯丁基3-(3'-甲氧基-4'-羟基苯基)丙烯酸酯（姜黄素A，1）和1,7-双(4-羟基-3-甲氧基苯基)-1,4,6-庚三烯-3-酮（2），以及七种已知化合物，1,7-双(4-羟基-3-甲氧基苯基)-1,6-庚二烯-3,5-二酮（姜黄素，3）、1-(4-羟基-3-甲氧基苯基)-7-(4-羟基苯基)-1,6-庚二烯-3,5-二酮（去甲氧基姜黄素，4）、1,7-双(4-羟基苯基)-1,6-庚二烯-3,5-二酮（双去甲氧基姜黄素，5）、1-羟基-1,7-双(4-羟基-3-甲氧基苯基)-6-庚烯-3,5-二酮（6）、1,7-双(4-羟基苯基)-1-庚烯-3,5-二酮（7）、1,7-双(4-羟基苯基)-1,4,6-庚三烯-3-酮（8）和1,5-双(4-羟基-3-甲氧基苯基)-1,4-戊二烯-3-酮（9）。发现化合物1、3 - 5和7比刚果红（10）（ED(50)=37 - 39μg/mL）更有效地保护PC12细胞免受β-淀粉样蛋白损伤（ED(50)=0.5 - 10μg/mL）。
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