Min B, Oh S R, Lee H K, Takatsu K, Chang I M, Min K R, Kim Y
College of Pharmacy, Chungbuk National University, Cheongju, Korea.
Planta Med. 1999 Jun;65(5):408-12. doi: 10.1055/s-1999-14016.
Fruits of Sophora japonica L. (Leguminosae) exhibited an inhibitory effect in the IL-5 bioassay of mIL-5-dependent Y16 proliferation. The isoflavonoids of sophoricoside, genistein, orobol, and genistin were isolated as the IL-5 inhibitors from fresh fruits of the plant by activity-guided fractionation. Among the IL-5 inhibitors, sophoricoside exhibited the highest inhibitory effect with 89% inhibition at 12.5 microM, 82% at 6.3 microM, 72% at 3.1 microM, 59% at 1.6 microM, and 24% at 0.8 microM where the 50% inhibition (IC50) was shown at the concentration of 1.5 microM. Oxyphenylbutazone as the positive control exhibited the IC50 value at the concentration of 31.7 microM. In the order of IC50 values the inhibitory potency in the IL-5 bioassay was sophoricoside > orobol (9.8 microM) approximately equal to genistin (10.6 microM) > genistein (51.9 microM). The position of O-glycosylation and number of hydroxy groups in the isoflavonoids seem to play an important role in the inhibitory effect in the IL-5 bioassay.
槐花（豆科）果实对依赖小鼠白细胞介素-5（mIL-5）的Y16细胞增殖的白细胞介素-5生物测定显示出抑制作用。通过活性导向分级分离法从该植物的新鲜果实中分离出槐糖苷、染料木黄酮、刺芒柄花素和染料木苷等异黄酮类作为白细胞介素-5抑制剂。在这些白细胞介素-5抑制剂中，槐糖苷表现出最高的抑制作用，在12.5微摩尔浓度下抑制率为89%，6.3微摩尔浓度下为82%，3.1微摩尔浓度下为72%，1.6微摩尔浓度下为59%，0.8微摩尔浓度下为24%，其50%抑制浓度（IC50）为1.5微摩尔。作为阳性对照的羟基保泰松在31.7微摩尔浓度下显示出IC50值。按照IC50值的顺序，在白细胞介素-5生物测定中的抑制效力为槐糖苷＞刺芒柄花素（9.8微摩尔）≈染料木苷（10.6微摩尔）＞染料木黄酮（51.9微摩尔）。异黄酮类中O-糖基化的位置和羟基的数量似乎在白细胞介素-5生物测定的抑制作用中起重要作用。
