title: Inhibitory effect of synthetic C-C biflavones on various phospholipase A(2)s activity.
abstract: Several prototypes of C-C biflavones (a-f) were synthesized and evaluated their inhibitory activity against phospholipase A(2)s (PLA(2)s) activity. The synthetic C-C biflavones (a-f) showed rather different inhibitory activity against various PLA(2)s. Most synthetic C-C biflavonoids exhibited potent and broad inhibitory activity against various sPLA(2)s and cPLA(2) tested regardless of their structural array. In particular, of natural and synthetic biflavonoids tested, the synthetic C-C biflavonoid (d) only showed inhibitory activity against sPLA(2) X. None of the natural and synthetic biflavonoids tested showed inhibitory activity against sPLA(2) IB. Further chemical modification of these basic structures will be carried out in order to investigate the synthetic C-C biflavones which possess more selective inhibitory activity against isozymes of PLA(2).
authors.affiliation: College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Republic of Korea.
authors.forename: Tae Chul
authors.initials: TC
authors.lastname: Moon
authors.forename: Zhejiu
authors.initials: Z
authors.lastname: Quan
authors.forename: Jeongsoo
authors.initials: J
authors.lastname: Kim
authors.forename: Hyun Pyo
authors.initials: HP
authors.lastname: Kim
authors.forename: Ichiro
authors.initials: I
authors.lastname: Kudo
authors.forename: Makodo
authors.initials: M
authors.lastname: Murakami
authors.forename: Haeil
authors.initials: H
authors.lastname: Park
authors.forename: Hyeun Wook
authors.initials: HW
authors.lastname: Chang
mesh_terms: D004789:Enzyme Activation / Q000187:drug effects; D047309:Flavones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007527:Isoenzymes / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D064801:Phospholipase A2 Inhibitors; D013237:Stereoisomerism; D013329:Structure-Activity Relationship