双活性中心抗肿瘤仲钨酸-B化合物的合成及体外药理活性研究

Synthesis and in vitro antitumor activities of paradodecatungstate-B compound with bi-active center

采用常规水溶液法合成了一种新型过渡金属锌修饰的仲钨酸-B化合物(H_(3)O)_(6)[Zn(H_(2)O)_(6)]_(6){Zn_6)(C_(5)H_(11)NO)_(6)(H_(2)O)_(6)[H_(2)W_(12)O_(42)]_(3)}·4H_(2)O(简写为ZnW_(12)),用X-射线单晶衍射、红外光谱和热重分析对化合物结构进行了表征.在化合物ZnW_(12)中,多阴离子通过锌的桥连形成了二维层状结构,其中容纳着游离的配阳离子[Zn(H_(2)O)_(6)]^(2+).用MTT法对化合物进行了体外抗肿瘤活性研究,结果表明:ZnW_(12)对HeLa(宫颈癌)、SKOV-3(卵巢癌)、HepG2(肝癌)和SHY5Y(神经胶质瘤细胞)4种肿瘤细胞的增殖均有抑制作用,IC_(50)分别为90.2,17.6,0.46和7.66μmol/L,远远小于未经锌修饰的母体多酸,说明双活性中心的存在极大地提高了仲钨酸的药理活性.

A novel paradodecatungstate-B compound decorated by transition metal zinc,(H_(3)O)_(6)[Zn(H_(2)O)_(6)]_(6){Zn_6)(C_(5)H_(11)NO)_(6)(H_(2)O)_(6)[H_(2)W_(12)O_(42)]_(3)}·4H_(2)O(abbreviated from ZnW_(12)),has been synthesized by convenient aqueous solution method and structurally characterized by single crystal X-ray diffraction,IR spectrum and TG.In compound ZnW_(12),polyanions were linked by Zn atom to form two-dimensional layers,in which contains the free[Zn(H_(2)O)_(6)]^(2+)cation.The experiment of antitumor activities was measured by MTT assay,the result shows that ZnW_(12) has remarkable inhibitory actions on human cervical carcinoma HeLa cells,ovarian carcinoma SKOV-3 cells,hepatoma HepG2 cells and neuroblastoma SHY5Y cells in vitro.The IC_(50)is respectively of 90.2,17.6,0.46 and 7.66μmol/L,much smaller than the parent polyoxometalate without decorated by zinc,indicating that existence of bi-active center has greatly improved the antitumor activities of paradodecatungstate-B.