苦皮藤中新骨架生物碱1,3-氧氮杂环已烷化合物的抗癌活性

摘要

从杀虫植物苦皮藤中分离得到两个新骨架生物碱,被命名为1,3-氧氮杂环已烷化合物A、B.它们的生物活性被美国国际卫生和抗癌研究中心(NCI)筛选.通过体外定向肿瘤筛选,9个不同种类的60个细胞株毒理实验结果表明,化合物生物碱B显示温和的细胞抗癌活性,抗非小细胞肺癌(NCI-H23),抑癌细胞生长率GI50=3.0×10-5 m(9.6μg/mL).生物碱A的细胞毒理正在筛选中.%Two new alkaloids A, B identified as 1,3-oxazacyclohexane skeleton were isolated from the seeds of Celastrus angulatus. Previous studies were focus on the sesquiterpene poloyol esters and sesquiterpene alkaloids from this family plants, which we have reported the separation and structural elucidation of two new alkaloids A, B from the same plant in recent days. Their structures were respectivily identified as 2α-(2'-pyrrolyl)-4α-methoxycarbony1-1, 3-oxazacyclohexane (A) and 2α-(2'-pyrrolyl)-4α-methoxycarbonyl-5β-[(2"-methyl)-hepty1]-1, 3-oxazacyclohexane (B). The compound B demonstrated moderate cytotoxicity against non-small lung cancer (NCL-H23) cell line by the National Cancer Institute in vitro cytotoxicity screen.