Chen Jianjun, Chang Hyeun Wook, Kim Hyun Pyo, Park Haeil
College of Pharmacy, Kangwon National University, Chunchon 200-701, Republic of Korea.
Bioorg Med Chem Lett. 2006 May 1;16(9):2373-5. doi: 10.1016/j.bmcl.2006.01.117. Epub 2006 Feb 28.
A series of C-C biflavones was designed to investigate the relationship between structural array of different flavone-flavone subunit linkage and the inhibitory activity against phospholipase A2 (PLA2). Among six classes of C-C biflavones designed, four classes of C-C biflavones, which have flavone-flavone subunit linkages at A ring-A ring, A ring-B ring, B ring-B ring, and B ring-C ring, were synthesized. The synthetic biflavones exhibited somewhat different inhibitory activities against sPLA2-IIA. Among them, the biflavone a having a C-C 4'-4' linkage showed comparable inhibitory activity with that of the natural biflavonoid, ochnaflavone, and 7-fold stronger activity than that of amentoflavone. Further chemical modification is being carried out in order to obtain the chemically optimized biflavonoids.
设计了一系列C-C双黄酮，以研究不同黄酮-黄酮亚基连接的结构阵列与对磷脂酶A2（PLA2）的抑制活性之间的关系。在所设计的六类C-C双黄酮中，合成了四类在A环-A环、A环-B环、B环-B环和B环-C环具有黄酮-黄酮亚基连接的C-C双黄酮。合成的双黄酮对分泌型磷脂酶A2-IIA表现出略有不同的抑制活性。其中，具有C-C 4'-4'连接的双黄酮a表现出与天然双黄酮奥氏黄酮相当的抑制活性，且活性比穗花杉双黄酮强7倍。为了获得化学优化的双黄酮，正在进行进一步的化学修饰。
