CAJ | 학술논문

目的:观察菊科植物中分离出的3种倍半萜化合物异土木香内酯、1-氧-乙酰大花旋覆花内酯和大花旋覆花内酯对体外培养的人子宫颈癌HeLa丑细胞、人子宫内膜癌HEC-1细胞、人卵巢透明细胞癌SHIN3及HOG-21细胞和人卵巢囊腺癌HAC-2细胞增殖的影响,研究这3种倍半萜化合物的体外抑制肿瘤细胞增殖作用及其结构与活性之间的构效关系,进而探讨3种倍半萜化合物的体外抑制肿瘤细胞增殖的可能机制.方法:以HeLa、HEC-1、SHIN3、HOC-21和HAC-2细胞为研究对象,利用四唑盐(MTT)比色法检测3种倍半萜化合物对上述5种妇科肿瘤细胞增殖的抑制作用;利用流式细胞术检测异土木香内脂对HeLa细胞凋亡的影响.结果:异土木香内酯对上述5种肿瘤细胞的增殖均有明显的抑制作用,1-氧-乙酰大花旋覆花内酯和大花旋覆花内酯即使在100 μmol/L的高浓度下,对5种妇科肿瘤细胞的增殖不显示抑制活性;流式细胞学检查发现异土木香内脂处理后的HeLa细胞出现凋亡现象.结论:提示A-环开环可能是导致桉叶烷型倍半萜内酯的体外抑制肿瘤细胞增殖作用消失或减弱的原因;异土木香内酯抑制肿瘤细胞增殖作用有可能是通过诱导肿瘤细胞凋亡机制而实现的.
목적:관찰국과식물중분리출적3충배반첩화합물이토목향내지、1-양-을선대화선복화내지화대화선복화내지대체외배양적인자궁경암HeLa축세포、인자궁내막암HEC-1세포、인란소투명세포암SHIN3급HOG-21세포화인란소낭선암HAC-2세포증식적영향,연구저3충배반첩화합물적체외억제종류세포증식작용급기결구여활성지간적구효관계,진이탐토3충배반첩화합물적체외억제종류세포증식적가능궤제.방법:이HeLa、HEC-1、SHIN3、HOC-21화HAC-2세포위연구대상,이용사서염(MTT)비색법검측3충배반첩화합물대상술5충부과종류세포증식적억제작용;이용류식세포술검측이토목향내지대HeLa세포조망적영향.결과:이토목향내지대상술5충종류세포적증식균유명현적억제작용,1-양-을선대화선복화내지화대화선복화내지즉사재100 μmol/L적고농도하,대5충부과종류세포적증식불현시억제활성;류식세포학검사발현이토목향내지처리후적HeLa세포출현조망현상.결론:제시A-배개배가능시도치안협완형배반첩내지적체외억제종류세포증식작용소실혹감약적원인;이토목향내지억제종류세포증식작용유가능시통과유도종류세포조망궤제이실현적.
OBJECTIVE: Three sesquiterpene lactones 1-O-acetylbritannilactone, isoalantolactone and britannilactone were isolated from the roots of lnula helenium and the flowers of Inula japonica. The antitumor activities of the three sesquiterpenoids in the cell lines of HeLa, HEC-1, SHIN3, HOC-21 and HAC-2 were measured, and the relationship between structure and activity and the possible mechanisms were explored. METHODS: The effect of three sesquiterpene lactones on five cell lines was measured by MTT assay in vitro. The apoptosis induced by isoalantolactone was examined by flow eytometry. RESULTS: Isoalantolactone exhibited excellent anti-proliferative activities on HeLa, SHIN3 and HOC-21 and HAC-2 cell lines, while 1-O-acetylbritannilactone and britannilactone demonstrated weak anti-proliferative activities on HeLa, SHIN3, HOAC-21 and HAC-2 cell lines even at the concentration of 100 μmol/L. The apoptotic rate in isoalantolactone group with the concentration of 12.5 μmol/L was higher than that in PBS group. CONCLUSION: MTT assay indicated that anti-proliferative activities in HeLa, SHIN3, HOAC-21 and HAC-2 cell lines were closely related to structure, 1, 10-seco of eudesmane sesquiterpene lactone resulted in reduced anti-proliferative activity. The anti-tumor activity of isoalantolactone was probably achieved by inducing HeLa cell apoptosis.