Takano-Ishikawa Y, Goto M, Yamaki K
National Food Research Institute, Kannondai, Tsukuba, Ibaraki, Japan.
Phytomedicine. 2006 May;13(5):310-7. doi: 10.1016/j.phymed.2005.01.016. Epub 2005 Oct 10.
A study of the structure-activity relations of the inhibitory effect of flavonoids on lipopolysaccharide (LPS)-induced prostaglandin production was carried out via a comparative examination of 39 flavonoids and related compounds. A comparison of the subclasses showed that flavones were most effective, followed by flavanones. Flavonols were less effective than those two groups. These results suggest that the C2-C3 double-bond and 4-oxo functional group of the C-ring are important factors for the high inhibition activities. Flavonoids showed the strongest inhibitory effect on the expression of Cox-2 protein. These results help to explain part of the reason for the pharmacological efficacy of flavonoids as anti-inflammatory compounds.
通过对39种黄酮类化合物及相关化合物进行比较研究，开展了黄酮类化合物对脂多糖（LPS）诱导的前列腺素生成抑制作用的构效关系研究。各亚类比较结果显示，黄酮类最为有效，其次是黄烷酮类。黄酮醇类的效果不如这两组。这些结果表明，C环的C2-C3双键和4-氧代官能团是具有高抑制活性的重要因素。黄酮类化合物对Cox-2蛋白的表达显示出最强的抑制作用。这些结果有助于解释黄酮类化合物作为抗炎化合物药理功效的部分原因。
