Folmer Florence, Harrison William T A, Tabudravu Jioji N, Jaspars Marcel, Aalbersberg William, Feussner Klaus, Wright Anthony D, Dicato Mario, Diederich Marc
Department of Chemistry, University of Aberdeen, Old Aberdeen, UK.
J Nat Prod. 2008 Jan;71(1):106-11. doi: 10.1021/np070290y. Epub 2007 Dec 19.
The two naphthopyrones 6-methoxycomaparvin (1) and 6-methoxycomaparvin 5-methyl ether (2) were isolated from a bioactive methanol-soluble extract of the Fijian echinoderm Comanthus parvicirrus. Their structures were assigned on the basis of spectroscopic methods. X-ray diffraction analysis was used to confirm the structure of 1. Both compounds were tested for their potential to inhibit the activation of the transcription factor NF-kappaB, which plays an important role in cancer development and inflammation, and the mechanism of action of the two compounds was investigated. Both naphthopyrones 1 and 2 completely inhibit TNF-alpha-induced NF-kappaB activation at a concentration of 300 microM by inhibiting the enzymatic activity of the kinase IKKbeta.
从斐济棘皮动物小环辐肛参的具有生物活性的甲醇可溶提取物中分离出了两种萘并吡喃酮，即6-甲氧基柯玛帕文（1）和6-甲氧基柯玛帕文5-甲基醚（2）。它们的结构是通过光谱方法确定的。采用X射线衍射分析来确认1的结构。对这两种化合物抑制转录因子NF-κB激活的潜力进行了测试，NF-κB在癌症发展和炎症中起重要作用，并对这两种化合物的作用机制进行了研究。两种萘并吡喃酮1和2在浓度为300微摩尔时通过抑制激酶IKKβ的酶活性完全抑制肿瘤坏死因子-α诱导的NF-κB激活。
