Deng J Z, Starck S R, Hecht S M
Department of Chemistry, University of Virginia, Charlottesville, Virginia 22901, USA.
J Nat Prod. 1999 Mar;62(3):477-80. doi: 10.1021/np980522g.
Bioassay-guided fractionation of Panopsis rubescens, using an assay to detect DNA polymerase beta inhibition, led to the isolation of two new bis-5-alkylresorcinols (1 and 2), in addition to one known bis-5-alkylresorcinol (3). The structures of 1-3 were established as 1,3-dihydroxy-5-[14'-(3' ',5' '-dihydroxyphenyl)-cis-4'-tetradecenyl]benzene (1), 1, 3-dihydroxy-5-[14'-(3' ',5' '-dihydroxyphenyl)-cis-7'-tetradecenyl]benzene (2), and 1, 3-dihydroxy-5-[14'-(3' ',5' '-dihydroxyphenyl)tetradecenyl]benzene (3), respectively, by spectroscopic and chemical analyses. Compounds 1-3 exhibited potent inhibition of calf thymus DNA polymerase beta, with IC50 values of 7.5, 6.5, and 5.8 microM, respectively.
利用检测DNA聚合酶β抑制活性的生物测定法对毛药红淡进行生物测定导向的分离，除了得到一种已知的双-5-烷基间苯二酚（3）外，还分离出两种新的双-5-烷基间苯二酚（1和2）。通过光谱和化学分析确定1-3的结构分别为1,3-二羟基-5-[14'-(3'',5''-二羟基苯基)-顺式-4'-十四碳烯基]苯（1）、1,3-二羟基-5-[14'-(3'',5''-二羟基苯基)-顺式-7'-十四碳烯基]苯（2）和1,3-二羟基-5-[14'-(3'',5''-二羟基苯基)十四碳烯基]苯（3）。化合物1-3对小牛胸腺DNA聚合酶β表现出强效抑制作用，IC50值分别为7.5、6.5和5.8微摩尔。
