Hasmeda M, Polya G M
School of Biochemistry, La Trobe University, Bundoora, Victoria, Australia.
Phytochemistry. 1996 Jun;42(3):599-605. doi: 10.1016/0031-9422(96)00091-x.
Curcumin [diferuloylmethane; 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione], a major bioactive secondary metabolite found in the rhizomes of turmeric (Curcuma longa), is an inhibitor of Ca(2+)- and phospholipid-dependent protein kinase C (PKC) and of the catalytic subunit (cAK) of cyclic AMP-dependent protein kinase (IC50 values 15 and 4.8 microM, respectively). Curcumin inhibits plant Ca(2+)-dependent protein kinase (CDPK) (IC50 41 microM), but does not inhibit myosin light chain kinase or a high affinity 3',5'-cyclic AMP-binding phosphatase. Curcumin inhibits cAK, PKC and CDPK in a fashion that is competitive with respect to both ATP and the synthetic peptide substrate employed. The IC50 values for inhibition of cAK by curcumin are very similar when measured with kemptide (LRRASLG) (in the presence or absence of ovalbumin) or with casein or histone III-S as substrates. However, the presence of bovine serum albumin (0.8 mg ml-1) largely overcomes inhibition of cAK by curcumin.
姜黄素[二阿魏酰甲烷；1,7 - 双(4 - 羟基 - 3 - 甲氧基苯基)-1,6 - 庚二烯 - 3,5 - 二酮]是在姜黄（Curcuma longa）根茎中发现的一种主要的生物活性次生代谢产物，它是钙（2 +）和磷脂依赖性蛋白激酶C（PKC）以及环磷酸腺苷依赖性蛋白激酶催化亚基（cAK）的抑制剂（IC50值分别为15和4.8 microM）。姜黄素抑制植物钙（2 +）依赖性蛋白激酶（CDPK）（IC50为41 microM），但不抑制肌球蛋白轻链激酶或高亲和力的3',5'-环磷酸腺苷结合磷酸酶。姜黄素以对ATP和所用合成肽底物均具有竞争性的方式抑制cAK、PKC和CDPK。当用kemptide（LRRASLG）（在有或没有卵清蛋白的情况下）或酪蛋白或组蛋白III - S作为底物测量时，姜黄素抑制cAK的IC50值非常相似。然而，牛血清白蛋白（0.8 mg ml-1）的存在在很大程度上克服了姜黄素对cAK的抑制作用。
