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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: To observe the effects of three sesquiterpene compounds, such as isocorhinol, 1_oxyacetylgalacturonan and grandifloral lactone, isolated from the composites of Compositae, on the growth of human cervical carcinoma HeLa cells, human endometrial carcinoma HEC_1 cells, human ovarian clear cell carcinoma SHIN3 and HOC_21 cells and human ovarian cystadenocarcinoma HAC_2 cells proliferation, the three sesquiterpene compounds in vitro inhibition of tumor cell proliferation and its structure And the activity of the structure-activity relationship, and then explore the three sesquiterpene compounds inhibit the possible mechanism of tumor cell proliferation in vitro. Methods: HeLa, HEC_1, SHIN3, HOC_21 and HAC_2 cells were used as research objects. The inhibitory effects of three sesquiterpenoids on the proliferation of the above five kinds of gynecological tumor cells were detected by MTT colorimetric assay. Flow cytometry Effect of Isomeratril on HeLa Cell Apoptosis. Results: Isohumuylolactone significantly inhibited the proliferation of the above 5 kinds of tumor cells. Even with the high concentration of 100μmol / L, , The proliferation of five kinds of gynecologic tumor cells showed no inhibitory activity. Flow cytometry revealed apoptosis of HeLa cells treated with isoflurane. CONCLUSION: It suggests that the open loop of A_ ring may be the reason that the eucalyptol sesquiterpene lactone inhibits the proliferation of tumor cells disappear or weakened in vitro. Isoxtrin inhibits the proliferation of tumor cells possibly by inducing tumor cells Apoptosis mechanism and achieve.