墨西哥落羽杉中三个活性双黄酮研究

Three Bioactive Biflavones Isolated from Taxodium mucronatum

从墨西哥落羽杉 (Taxodiummucronatum)枝叶中分离得到 3个化合物 ,通过MS、1DNMR、 2DNMR以及与参考文献比较的方法鉴定它们分别为 3个已知双黄酮 ,即 :a mentoflavone (1) ,podocarpusflavoneA (2 ) ,4′ ,7 dimethylamentoflavone (3)。本文还对文献中amentoflavone的C - 2 和C - 6 的碳谱数据归属进行了修正。体外生物活性筛选结果表明 ,这 3个双黄酮均为组织蛋白酶B的抑制剂 ,其IC50 值分别为 1 75、 1 6 8和 0 5 5 μmol/L ;这 3个双黄酮均显示一定的细胞毒活性 ,其中化合物 1对肿瘤细胞株BGC 82 3的IC50 值为 3 5 1μmol/L ,化合物 2对肿瘤细胞株HT 2 9的IC50 值为 11 16 μmol/L ,化合物 3对肿瘤细胞株A5 49、BEL 74 0 2、DU14 5、HT 2 9的IC50 值分别为 7 74、 17 16、 12 4 2、 14 5 4μmol/L。

Biflavones amentoflavone (1),podocarpusflavone A (2),and 4′,7-dimethylamentoflavone (3) were isolated and identified from leaves and branches of Taxodium mucronatum .In vitro bioassay screening,the results indicated that amentoflavone (1),podocarpusflavone A (2) and 4′,7-dimethylamentoflavone (3) showed significant inhibitory activities on cathepsin B with IC_(50) values of 1.75,1.68 and 0.55?μmol/L,respectively,which were new natural inhibitors of cathepsin B.1 showed cytotoxicity on cancer cell line BGC-823 with IC_(50) value of 3.51?μmol/L.2 showed cytotoxicity on cancer cell line HT-29 with IC_(50) value of 11.16?μmol/L.3 showed cytotoxicities on cancer cell lines A549,BEL-7402,DU145 and HT-29 with IC_(50) values of 7.74,17.16,12.42 and 14.54?μmol/L,respectively.