双过氧钒化合物NH4[OV(O2)2(C8H7N3)]·4H2O抗肿瘤活性研究

Antitumor Activity of a New Complex of Diperoxovanadate NH_4[OV(O_2)_2(C_8H_7N_3)]·4H_2O

在细胞和动物实验水平上,研究了双过氧钒化合物NH4[OV(O2)2(C8H7N3)]×4H2O(简写bpV(Imi-Py))对癌细胞的增殖作用,碱性磷酸酶的活性抑制和体内抗肿瘤作用.研究结果显示bpV(Imi-Py)对胃癌细胞株MGC-803、肺癌细胞株95D和L342的IC50值分别为8.27、26.37和9.54μmol/L,而对人正常肾胚胎细胞HEK293的IC50值达6 642μmol/L,表明该化合物对肿瘤细胞具有特异杀伤作用.研究还表明bpV(Imi-Py)对MGC-803细胞提取液的碱性磷酸酶(ALP)也有明显抑制作用,呈现量效关系.动物体内抗肿瘤实验发现bpV(Imi-Py)能抑制肝癌细胞生长,肿瘤体积实验组较对照组下降35.6%,表明bpV(Imi-Py)有较好的抗肿瘤活性.另外,小鼠急性毒性实验的LD50为147.2mg.kg-1,说明bpV(Imi-Py)是一种中等毒性的抗肿瘤化合物.图4,表1,参15.

A diperoxovanadate complex NH4[OV （O2） 2{2-（ 2＇-pyridyl ）-imidazole}]×4H20, bpV （ Imi-Py ） for short, was investigated at the level of cell and animal based on its proliferation on cancer cells, inhibition on alkaline phosphatase and anti-tumor in animal experiments. The results showed that the IC50 values of bpV （Imi-Py） for gastric cancer cell line MGC-803, lung cancer cell line 95D and L342 were 8.27, 26.37, and 9.54 μmol/L, respectively. However, its IC50 value for normal human embryonic kidney cell cultures HEK293 is 6642 μ mol/L, indicating that cancer cells can be selectively inhibited by bpV （Imi-Py）. The inhibition of bpV （Imi-Py） on alkaline phosphatase is also obvious, and showed the dose-response relationship. At the same time, animal tumor trail showed that bpV （Imi-Py） inhibited hepatocarcinoma cells. The volume of tumor was reduced by about 35.6% relative to control. It suggests that bpV （Imi-py） has good anti-tumor activity. In addition, the LD50 of bpV （Imi-Py） is 147.2 mg· kg^-1 intravenously in mice, indicating its moderate toxicity. In conclusion, bpV （Imi-Py） is one kind of anti-tumor complex with ：moderate toxicity.