Kv1.2 potassium channel inhibitors from Chukrasia tabularis.
Eighteen new limonoids, chubularisins A-R (1-18), along with eleven known analogues, were isolated from the stem bark of Chukrasia tabularis. The structures of 1-18 were elucidated on the basis of spectroscopic data and chemical evidence. Compound 1 represented the first example of 8,9,12-orthoester of phragmalin limonoids. Interestingly, compounds 4, 8, and 22 exhibited potent and selective inhibition against the delayed rectifier (I(K)) K(+) current with IC(50) values of 0.61, 2.03, and 2.15 μM, respectively.
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park, Shanghai, 201203, People's Republic of China.
Hong-Bing
HB
Liu
Hua
H
Zhang
Ping
P
Li
Yan
Y
Wu
Zhao-Bing
ZB
Gao
Jian-Min
JM
Yue
D051663:Kv1.2 Potassium Channel / Q000037:antagonists & inhibitors* / Q000737:chemistry; D036701:Limonins / Q000737:chemistry / Q000494:pharmacology*; D024301:Plant Bark / Q000737:chemistry*
D051663:Kv1.2 Potassium Channel; D036701:Limonins