摘要
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细胞、人子宫内膜癌HEC_1细胞、人卵巢透明细胞癌SHIN3及HOC_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100μmol/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。
OBJECTIVE： Three sesquiterpone lactones 1-O-acetylbritannilactone, isoalantolactone and britannilactone were isolated from the roots of Inula helenium and the flowers of Inula japonica. The antitumor activities of the three sesquiterpenoids in the cell fines 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 cytometry. 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 100μmol/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.
出处
《癌变．畸变．突变》
CAS
CSCD
2010年第1期28-31,共4页
Carcinogenesis,Teratogenesis & Mutagenesis
基金
河北省引进留学人员基金(2008-2010)
河北省自然科学基金(08B032)
河北省卫生厅医学科学研究重点课题计划(20090151)
关键词
菊科植物
倍半萜类
妇科肿瘤
增殖抑制活性
细胞凋亡
haplopappns gracillis
sesquiterpenes
gynecologic neoplasms
anti-proliferative activity
apoptosis
