CAJ | 학술논문

目的检测土木香中纯化的五种倍半萜化合物抑制肿瘤增殖的活性,并探讨化合物结构与活性之间的关系.方法应用MTT法测定五种倍半萜类化合物对体外培养人肿瘤细胞增殖的影响;应用小鼠移植性肝癌模型测定了异土木香内酯的抗肿瘤活性.结果化合物1(异土木香内酯)对U251SP细胞、HLE细胞和MM1-CB细胞的增殖显示较强的抑制活性;化合物2～5对各种实验用肿瘤细胞的增殖不显示抑制活性;化合物1对移植性肿瘤(肝癌H22)具有明显的抑制作用,并呈现较好的剂量依赖关系.结论异土木香内酯具有较强的肿瘤抑制活性;化合物2～5对肿瘤细胞增殖抑制活性丧失可能由于A-环和B-环之间的键裂开,形成一个大10元环,改变了原来的构象所致.
목적 검측토목향중순화적오충배반첩화합물억제종류증식적활성,병탐토화합물결구여활성지간적관계.방법 응용MTT법측정오충배반첩류화합물대체외배양인종류세포증식적영향;응용소서이식성간암모형측정료이토목향내지적항종류활성.결과 화합물1(이토목향내지)대U251SP세포、HLE세포화MM1-CB세포적증식현시교강적억제활성;화합물2～5대각충실험용종류세포적증식불현시억제활성;화합물1대이식성종류(간암H22)구유명현적억제작용,병정현교호적제량의뢰관계.결론 이토목향내지구유교강적종류억제활성;화합물2～5대종류세포증식억제활성상실가능유우A-배화B-배지간적건렬개,형성일개대10원배,개변료원래적구상소치.
Aim To detect the antitumor activities of five sesquiterpene lactones from the roots of Inula helenium.Method Using MTT assay to evaluate the antitumor activities of five sesquiterpene lactones to the cell lines of U251SP,T-98,HLE,MM1-CB,HMV-1 and KT,and to explore the relationship between structure and activities.Results Isoalantolactone exhibited significant anti-growth activities to U251SP,HLE and MM1-CB,while other compounds demonstrated weak or moderate anti-growth activities to cell lines even in the 50% inhibition concentration≤100 μmol·L~(-1).Conclusion Isoalantolactone exhibits significant anti-growth activities to three cell lines and its anti-tumor activitiesve close relationship with the structures,α,β-unsaturated five-membered lactone ring is necessary for the activities,and saturated lactone or 5,10-seco and A,B-ring become a ten-membered macro-ring leading to the loss or decrease of anti-growth activity.