双(α-呋喃甲酸)氧钒合成方法的改进及抗癌作用研究  

An improved method for synthesis of bis(α-furancarboxylato)oxovanadium and its anticancer activity

作　　者：李雪 高丽辉 高安丽[1] 姜婧[1] 巨少英 余娟[1] LI Xue;GAO Li-hui;GAO An-li;JIANG Jing;JU Shao-ying;YU Juan(Platinum-Based Drug Lab,Kunming Institute of Precious Metals,Kunming 650106,Yunnan,China;Biomedical Engineering Research Center,Kunming Medical University,Kunming 650500,Yunnan,China)

机构地区：[1]昆明贵金属研究所稀贵金属综合利用新技术国家重点实验室,云南昆明650106 [2]昆明医科大学生物医学工程研究中心,云南昆明650500

出　　处：《云南大学学报（自然科学版）》2021年第1期152-156,共5页Journal of Yunnan University(Natural Sciences Edition)

基　　金：国家自然科学基金(21661018);云南省应用基础研究计划(2018FB012).

摘　　要：通过优化和改进,获得一种合成双(α-呋喃甲酸)氧钒(BFOV)的新方法,产率达93%,w(Ba)<10 mg/kg,元素分析和结构分析与VO(C5H3O3)2·2H2O吻合.运用标准MTT法测试了BFOV分别对A549(人肺癌细胞株)、SKOV3(人卵巢癌细胞株)和耐受顺铂的A549/DPP、SKOV3/DPP生长的抑制活性.此外,还使用MTT法试验了它对Beas-2B(人肺正常上皮细胞株)的毒性以及对小鼠的急性毒性.结果表明,BFOV的水溶性好、水溶液稳定性高,不但对人癌细胞株A549和SKOV3具有很强的抑制作用,IC50小于顺铂或与顺铂相当,且对顺铂耐受的人癌细胞株A549/DPP和SKOV3/DPP具有更强的抑制活性,可以克服顺铂的耐药性.同时,它对人体正常细胞Beas-2B的毒性和对小鼠的急性毒性均小于顺铂.因此,双(α-呋喃甲酸)氧钒可作为抗癌药物,值得进一步研究和评价.A new synthetic method of bis(α-furancarboxylato)oxovanadium(BFOV)was developed with a yield of up to 93%.The content of barium ions remaining in the product was minimized to less than 10 mg/kg.The data of the element analysis and structural measurements were well consistent with the formulae VO(C5H3O3)2·2H2O.The standard MTT assay was used to evaluate anticancer activity of BFOV against several human cancer cell lines,including lung and ovarian cancer cells(A549 and SKOV3)as well as their respective cisplatin-resistant cells(A549/DDP and SKOV3/DDP).Moreover,the effect of BFOV on human normal lung epithelial cells(Beas-2B)was determined also by using MTT assay.Its acute toxicity was also tested on mice.BFOV has a good water-solubility and water-stability.The biological tests reveal that BFOV is able to inhibit the growth of cancer cell A549 and SKOV3 and its anticancer activity is higher than or comparable to that of cisplatin as a control drug.More importanly,BFOV has greater potency on cisplatin-resistant A549/DPP,indicating it can overcome the resistance of these cancer cells to cisplatin.BFOV,a vanadium complex,displays much milder inhibitory effect than cisplatin.Furthermore,the acute toxicity of BFOV on mice,expressed in terms of LD10 and LD50,is also less than that of cisplatin.

关 键 词：双(Α-呋喃甲酸)氧钒 合成 抗癌作用 毒性 

分 类 号：O614.51[理学—无机化学]