Objective： To study the anti-tumor activities of novel estrogen compound 17a α-D-homo-ethynylestradiol-3-acetate in vitro and in vivo. Methods： In vitro anti-tumor activity was assayed in adenoma cells A549 and hum...Objective： To study the anti-tumor activities of novel estrogen compound 17a α-D-homo-ethynylestradiol-3-acetate in vitro and in vivo. Methods： In vitro anti-tumor activity was assayed in adenoma cells A549 and human liver cancer cells Bel-7402 using MTT method, and half-inhibitory concentration （IC50） were observed. In vivo the pulmonary adenoma LA795 cells was selected and the conventional assay method of anti-tumor activity was employed. 5, 7.5, 10 mg/kg of 17a α-D-homo-ethynylestradiol-3-acetate was administered by i.p., and tumor-inhibitory rate, thymus and spleen indexes, bone marrow cells （BMC） were observed. Results： IC50 of 17a α-D-homo-ethynylestradiol-3-acetate in vitro for A549 and Bel-7402 cells were 12.28 μg/ml and 17.79 μg/ml, respectively. In vivo the highest tumor-inhibitory rates for LA795 was 60.0% （P〈0.01）. The drug had hardly any side-effect in spleen indexes, thymus indexes, and BMC compared with control mice. Nevertheless, compared with the positive control drug cyclophosphamide （CY）, thymus and spleen indexes, BMC showed obvious differences （P〈0.01）. Conclusion： 17a α-D-homo-ethynylestradiol-3-acetate has obvious anti-tumor activities in vitro and in vivo with low side-effect, thus worth further investigation.展开更多
基金the grant from Tianjin Nature Science Fund Key Item(No.043802411)
文摘Objective： To study the anti-tumor activities of novel estrogen compound 17a α-D-homo-ethynylestradiol-3-acetate in vitro and in vivo. Methods： In vitro anti-tumor activity was assayed in adenoma cells A549 and human liver cancer cells Bel-7402 using MTT method, and half-inhibitory concentration （IC50） were observed. In vivo the pulmonary adenoma LA795 cells was selected and the conventional assay method of anti-tumor activity was employed. 5, 7.5, 10 mg/kg of 17a α-D-homo-ethynylestradiol-3-acetate was administered by i.p., and tumor-inhibitory rate, thymus and spleen indexes, bone marrow cells （BMC） were observed. Results： IC50 of 17a α-D-homo-ethynylestradiol-3-acetate in vitro for A549 and Bel-7402 cells were 12.28 μg/ml and 17.79 μg/ml, respectively. In vivo the highest tumor-inhibitory rates for LA795 was 60.0% （P〈0.01）. The drug had hardly any side-effect in spleen indexes, thymus indexes, and BMC compared with control mice. Nevertheless, compared with the positive control drug cyclophosphamide （CY）, thymus and spleen indexes, BMC showed obvious differences （P〈0.01）. Conclusion： 17a α-D-homo-ethynylestradiol-3-acetate has obvious anti-tumor activities in vitro and in vivo with low side-effect, thus worth further investigation.
