ISOLATION OF POTENTIAL CANCER CHEMOPREVENTIVE AGENTS FROM ERIODICTYON-CALIFORNICUM
ISOLATION OF POTENTIAL CANCER CHEMOPREVENTIVE AGENTS FROM ERIODICTYON-CALIFORNICUM
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DOI：
10.1021/np50081a012
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发表时间：
1992-03-01
影响因子：
5.1
通讯作者：
BAIRD, WM
中科院分区：
文献类型：
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作者：
LIU, YL;HO, DK;BAIRD, WM
以活性为基础的分级分离Eriodictyon californicum，分离出12种黄酮类化合物，这些黄酮类化合物抑制组织培养中仓鼠胚胎细胞对致癌物苯并[a]芘的代谢。 其中一个化合物经光谱分析和碱解鉴定为新的黄烷酮化合物3 '-甲基-4'-异丁酰基圣草酚[1]。 其他7种活性黄烷酮被鉴定为圣草酚[2]、高圣草酚[3]、5，4 '-二羟基-6，7-二甲氧基黄烷酮[4]、松属素[5]、樱花素[6]、5，7，4'-三羟基-6，3 '-二甲氧基黄烷酮[7]和柚皮素4'-甲醚[8]。 四种活性黄酮也被分离出来：小蓟素[9]、黄毛菊醇[10]、hispidulin [11]和白杨素[12]。 在浓度仅为10 μ g/ml时，蓟素和chrysoeriol对苯并[a]芘代谢的高度抑制和苯并[a]芘对最终致癌DNA结合代谢物的活化表明这些黄酮作为潜在的化学预防剂值得在体内进一步研究。
Activity-based fractionation of Eriodictyon californicum resulted in the isolation of 12 flavonoids that inhibit the metabolism of the carcinogen benzo[a]pyrene by hamster embryo cells in tissue culture. One was identified as a new flavanone, 3'-methyl-4'-isobutyryleriodictyol [1], on the basis of spectroscopic analysis and alkaline hydrolysis. The seven other active flavanones were identified as eriodictyol [2], homoeriodictyol [3], 5,4'-dihydroxy-6,7-dimethoxyflavanone [4], pinocembrin [5], sakuranetin [6], 5,7,4'-trihydroxy-6,3'-dimethoxyflavanone [7], and naringenin 4'-methyl ether [8]. Four active flavones were also isolated: cirsimaritin [9], chrysoeriol [10], hispidulin [11], and chrysin [12]. The high inhibition of benzo[a]pyrene metabolism and the activation of benzo[a]pyrene to ultimate carcinogenic DNA-binding metabolites by cirsimaritin and chrysoeriol at a concentration of only 10-mu-g/ml indicates that these flavones warrant further investigation in vivo as potential chemopreventive agents.