Department of Oral and Maxillofacial Surgery, Tokyo Medical University, Shinjyuku-ku, Tokyo, Japan.
In Vivo. 2010 Jan-Feb;24(1):55-8.
We have previously reported that among 12 major ingredients of Sairei-to, Scutellariae radix inhibited prostaglandin E(2) (PGE(2)) production by lipopolysaccharide (LPS)-activated mouse macrophage-like RAW264.7 cells more efficiently than other ingredients, and wogonin, a major flavonoid from Scutellariae radix, showed greater inhibitory activity and membrane permeability than baicalein and baicalin. Here the effects of six other flavonoids, with similar structures, on membrane permeability and PGE(2) production were investigated. 7-Methoxyflavone inhibited the LPS-stimulated PGE(2) production to the greatest extent, followed by flavone>wogonin (5,7-dihydroxy-8-methoxyflavone)>> 7,8-dimethoxyflavone>chrysin (5,7-dihydroxyflavone)> baicalein (5,6,7-trihydroxyflavone)>>chromone. 7-Methoxyflavone also showed the highest membrane permeability, followed by flavone>chrysin>7,8-dimethoxy-flavone>wogonin>baicalein. When PGE(2) inhibitory activity was expressed per molecule incorporated into the cells, wogonin produced the greatest inhibition, further substantiating its anti-inflammatory potency.
我们之前曾报道过，在清暑益气汤的 12 种主要成分中，黄芩根比其他成分更有效地抑制脂多糖（LPS）激活的鼠巨噬细胞样 RAW264.7 细胞中前列腺素 E2（PGE2）的产生，而黄芩中的主要黄酮类化合物汉黄芩素比黄芩素和黄芩苷具有更大的抑制活性和膜通透性。在这里，研究了其他六种结构相似的黄酮类化合物对膜通透性和 PGE2 产生的影响。7-甲氧基黄酮对 LPS 刺激的 PGE2 产生的抑制作用最大，其次是黄酮>汉黄芩素（5,7-二羟基-8-甲氧基黄酮）>>7,8-二甲氧基黄酮>白杨素（5,7-二羟基黄酮）>黄芩素（5,6,7-三羟基黄酮）>>色酮。7-甲氧基黄酮的膜通透性也最高，其次是黄酮>白杨素>7,8-二甲氧基黄酮>汉黄芩素>黄芩素。当按每个进入细胞的分子表示 PGE2 抑制活性时，汉黄芩素产生的抑制作用最大，进一步证实了其抗炎效力。
