Han Xiang Hua, Hong Seong Su, Lee Dongho, Lee Jung Joon, Lee Moon Soon, Moon Dong-Cheul, Han Kun, Oh Ki-Wan, Lee Myung Koo, Ro Jai Seup, Hwang Bang Yeon
College of Pharmacy, Chungbuk National University, Cheongju, Korea.
Arch Pharm Res. 2007 Apr;30(4):397-401. doi: 10.1007/BF02980210.
1-Methyl-2-undecyl-4(1H)-quinolone (1) was previously isolated as a selective MAO-B inhibitor from the Evodiae Fructus. Further bioassay-guided purification led to the identification of five known quinolone alkaloids, 1-methyl-2-nonyl-4(1H)-quinolone (2), 1-methyl-2-[(Z)-6-undecenyl]-4(1H)-quinolone (3), evocarpine (4), 1-methyl-2-[(6Z,9Z)-6,9-pentadecadienyl]-4(1H)-quinolone (5), and dihydroevocarpine (6). All the isolates showed more potent inhibitory effects against MAO-B compared to MAO-A. The most MAO-B selective compound 5 among the isolates inhibited MAO-B in a competitive manner, according to kinetic analyses by Lineweaver-Burk reciprocal plots.
1-甲基-2-十一烷基-4(1H)-喹诺酮（1）先前是从吴茱萸果实中作为一种选择性单胺氧化酶B（MAO-B）抑制剂分离得到的。进一步的生物活性导向纯化导致鉴定出5种已知的喹诺酮生物碱，即1-甲基-2-壬基-4(1H)-喹诺酮（2）、1-甲基-2-[(Z)-6-十一碳烯基]-4(1H)-喹诺酮（3）、吴茱萸次碱（4）、1-甲基-2-[(6Z,9Z)-6,9-十五碳二烯基]-4(1H)-喹诺酮（5）和二氢吴茱萸次碱（6）。与单胺氧化酶A（MAO-A）相比，所有分离物对MAO-B均表现出更强的抑制作用。根据Lineweaver-Burk双倒数作图法进行的动力学分析，分离物中对MAO-B选择性最高的化合物5以竞争性方式抑制MAO-B。
