硼钨酸嘧啶盐的抗肿瘤活性

目的：观察硼钨酸嘧啶盐(PBT)体内、体外抗肿瘤活性及毒性作用。 方法：采用MTT法检测PBT对人肝癌SMMC-7721细胞、人胃癌SGC-7901细胞、人宫颈癌HeLa细胞的体外抑瘤活性，及对人羊膜FL细胞的毒性；建立小鼠H₂₂实体瘤模型，测定PBT体内抑瘤效应；经口急性毒性实验方法，计算半数致死剂量（LD₅₀）。 结果：体外实验显示，PBT对上述3种人癌细胞的半数抑制浓度(IC₅₀)分别为57、209和193 mg?L^-1；实验浓度PBT对人羊膜FL细胞生长的最高抑制率小于50%；体内实验结果显示，PBT低、中、高3个剂量对荷瘤小鼠荷瘤生长的抑制率分别为20.32%、33.15%和52.94%，PBT高剂量组小鼠瘤重与5-Fu组比较差异无显著性（P>0.05）；急性毒性实验LD₅₀为1 117.38 mg?kg^-1，LD₅₀ 95%可信限为911.59～1 369.65 mg?kg^-1。 结论：PBT对体外生长的3种人癌细胞均有较好的抑制作用，对人肝癌SMMC-7721细胞抑制作用尤为明显，体内能明显抑制荷瘤小鼠荷瘤的生长，且属于低毒物质。

Anti-tumor activity of pyrimidine borotungstate in vivo and in vitro

Objective To study the anti-tumor activity and the acute toxicity of (PBT) in vivo and in vitro. Methods MTT method was used to examine the inhibitory effects of PBT against several kinds of human cancer cells and the toxicity against the normal cells; H 22 tumor-bearing mice were used to set up animal models to measure the inhibitory effects of PBT in vivo; the conventional acute toxicity experiment of mice by gastric infusion were used to calculate the value of LD 50 . Results The values of IC 50 of PBT against several kinds of human cancer cells (SMMC-7721, SGC-7901, HeLa) were 57, 209, and 193 mg·L -1 , respectively. The highest inhibitory rate (IR) of PBT against FL cells was lower than 50%. The IR in the low, middle, and high dose groups of PBT in H 22 tumor-bearing mice were 20.32%, 33.15%, and 52.94%, respectively. The weight of tumor in high dose group had not significant difference with that in 5-Fu group (P>0.05). The median lethal dose (LD 50 ) of PBT in mice was 1 117.38 mg·kg -1 ,and the range of 95% confidence limit was 911.59-1 369.65 mg·kg -1 . Conclusion PBT could inhibit the growth and proliferation of human cancer cells mentioned above in vitro. Furthermore it is able to kill SMMC-7721 cell significantly. PBT could obviously inhibit the increase of tumor weight in tumor mice. PBT belongs to a kind of low toxic material.