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背景与目的:从野鸦椿(euscaphis japonica kanitz)枝叶的甲醇提取物分离纯化得到3种酯类化合物7-hydroxy-2-octen-5-olide(1),methyl 5,7-dihydroxy-2(Z)-octenoate(2)和3,7-dihydroxy-5-octanolide(3),对这3种酯类化合物的抗肿瘤细胞增殖作用及其机制进行研究。材料与方法:利用四唑盐(MTT)比色法测定这3种酯类化合物对HeLa细胞增殖的抑制作用;采用流式细胞术检测化合物1对HeLa细胞的凋亡和P53蛋白表达的影响;利用电镜观察化合物1引起HeLa细胞的形态学改变。结果:化合物1和化合物2对体外培养的HeLa细胞的增殖均具有明显地抑制作用,并有较好量效关系,对HeLa细胞增殖的半数抑制浓度分别为49.34μmol/L和24.53μmol/L;流式细胞学检查发现化合物1处理后的HeLa细胞发生凋亡,且P53蛋白表达增加,与对照组比较差异有统计学意义(P<0.01);电镜下可见化合物1引起HeLa细胞凋亡的形态学改变。结论:野鸦椿的提取物7-hydroxy-2-octen-5-olide(1)和methyl 5,7-dihydroxy-2(Z)-octenoate(2)能抑制体外培养的HeLa细胞的增殖,其作用机制可能与调节HeLa细胞P53蛋白表达及诱导HeLa细胞的凋亡有关。
BACKGROUND & AIM: To isolate and purify 3 kinds of ester compounds, 7-hydroxy-2-octen-5-olide(1), methyl 5,7-dihydroxy-2, from the methanol extract of Euscaphis japonica kanitz. Z)-octenoate (2) and 3,7-dihydroxy-5-octanolide (3) studied the anti-tumor cell proliferation and mechanism of these three ester compounds. MATERIALS AND METHODS: The inhibitory effect of these three ester compounds on the proliferation of HeLa cells was measured by tetrazolium (MTT) colorimetric assay. The effect of compound 1 on HeLa cells apoptosis and P53 protein expression was detected by flow cytometry. The morphological changes of HeLa cells induced by compound 1 were observed by electron microscope. RESULTS: Compound 1 and compound 2 had significant inhibitory effect on the proliferation of HeLa cells cultured in vitro and had a good dose-effect relationship. The half inhibition concentrations of HeLa cells proliferation were 49.34 μmol/L and 24.53 μmol/L, respectively. Flow cytometry revealed that apoptosis of HeLa cells was observed after treatment with Compound 1, and the expression of P53 protein was increased. There was statistically significant difference compared with the control group (P<0.01). Under electron microscope, the apoptosis of HeLa cells induced by compound 1 was observed. Learn to change. CONCLUSION: The extract of 7-hydroxy-2-octen-5-olide(1) and methyl 5,7-dihydroxy-2(Z)-octenoate(2) can inhibit the proliferation of HeLa cells cultured in vitro. The mechanism may be related to regulating the expression of P53 protein in HeLa cells and inducing the apoptosis of HeLa cells.