Biocatalyzed cross-coupling of sinomenine and 1,2-dihydroxybenzene by Coriolus unicolor
Biocatalyzed cross-coupling of sinomenine and 1,2-dihydroxybenzene by Coriolus unicolor
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云芝生物催化青藤碱与1,2-二羟基苯的交叉偶联
DOI：
10.1016/j.cclet.2012.01.004
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发表时间：
2012-03-01
影响因子：
9.1
通讯作者：
Wang, Jun Zhi
中科院分区：
文献类型：
--
作者：
Deng, Zhang Shuang;Zhao, Dan;Wang, Jun Zhi
青藤碱是一种治疗类风湿性关节炎（RA）的临床可用药物。在不断寻找具有较好生物活性的青藤碱衍生物的研究中，青藤碱与1,2-二羟基苯在真菌Coriolus unicolor催化下发生交叉偶联反应，得到了独特的C - C交叉偶联化合物2，并与(S)-disinomenine和(R)-disinomenine结合。用质谱和核磁共振谱对2的结构进行了鉴定。化合物2对SW982细胞IL-6过量产生的抑制活性进一步测定，与(S)-disinomenine和青藤碱（分别抑制17%和12%）相比，化合物2对IL-6的抑制活性更强（抑制96%）。(C) 2012张爽邓。由Elsevier B.V.代表中国化学会出版。版权所有。
Sinomenine is a clinically available drug for the treatment of rheumatoid arthritis (RA). In a continuous research aiming at discovery of sinomenine derivates with better bioactivity, a cross-coupling reaction of sinomenine and 1,2-dihydroxybenzene catalyzed by a fungus Coriolus unicolor afforded an unique C C cross-coupled compound 2, together with (S)-disinomenine and (R)-disinomenine. The structure of 2 was elucidated by MS and NMR spectroscopy. Compound 2 was further assayed for the inhibitory activity on IL-6 overproduction in SW982 cells and exhibited a much more potent activity on IL-6 (96% inhibition) compared with those of (S)-disinomenine and sinomenine (17% and 12% inhibition, respectively). (C) 2012 Zhang Shuang Deng. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.