Issue 7, 2012
From the journal:

Organic & Biomolecular Chemistry

Kv1.2 potassium channelinhibitors from Chukrasia tabularis†

Hong-Bing Liu,a   Hua Zhang,a   Ping Li,a   Yan Wu,a   Zhao-Bing Gaoa  and  Jian-Min Yue*a  

* Corresponding authors

a 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, People's Republic of China
E-mail: jmyue@mail.shcnc.ac.cn
Fax: +86-21-50806718
Tel: +86-21-50806718

Abstract

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 (IK) K+ current with IC50 values of 0.61, 2.03, and 2.15 μM, respectively.

Graphical abstract: Kv1.2 potassium channel inhibitors from Chukrasia tabularis

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Article information

DOI
https://doi.org/10.1039/C1OB06666H
Article type
Paper
Submitted
02 Oct 2011
Accepted
14 Nov 2011
First published
16 Nov 2011

Org. Biomol. Chem., 2012,10, 1448-1458

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Kv1.2 potassium channel inhibitors from Chukrasia tabularis

H. Liu, H. Zhang, P. Li, Y. Wu, Z. Gao and J. Yue, Org. Biomol. Chem., 2012, 10, 1448 DOI: 10.1039/C1OB06666H

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