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铂络合物是抗癌药物中近年研制新药。最引人注目的是顺氯氨铂,已用于临床。二价铂与尿嘧啶类形成一类兰色的络合物“铂兰”(Platinum Pyrimi-dine Blues,Platinum Blues),据报告在动物实验中抗癌活性很高,且肾毒性小,溶解度大,认为较有苗头。我们对铂兰的合成、提纯及抗癌活性进行了实验研究,结果摘要报告于后。 合成、提纯:主要原料为铂氯酸钾、氯亚铂酸钾(上海试剂一厂,分析纯),(口由)(口雪)(uracil)(上海试剂二厂,生化试剂)。所用试剂均为分析纯。用醋酸盐法由氯亚铂酸钾制备顺式二氯二氨合铂(PDD),得鲜黄色结晶,在盐酸酸化过的热水中多次重结晶提纯。以提纯的PDD与与(口由)(口雪)采用文献的方法在暗室制备铂兰。PDD与硝酸银按摩尔比1:2混合,加等摩尔(口由)(口雪),在37℃反应5～10天,调pH为6,5～8.5。反应结束时在4℃冷却,过滤,即得铂兰。滤液加等体积乙醇尚可得少量产品。铂兰以黑纸密封避光4℃冷藏。
Platinum complexes are new drugs for the development of anticancer drugs in recent years. Most notable is cisplatin, which has been used clinically. Divalent platinum and uracil form a blue-colored complex, Platinum Pyrimi-dine Blues (Platinum Blues), which has been reported to have high anticancer activity, low nephrotoxicity, and high solubility in animal experiments. , think that there are more signs. We conducted an experimental study on the synthesis, purification and anticancer activity of piranthans, and the results were reported in the final report. Synthesis and purification: The main raw materials are potassium chlorate, potassium chloroplatinate (Shanghai Reagent No. 1 Plant, analytical grade), (mouth) (uraxue) (uracil) (Shanghai Reagent Plant, biochemical reagents). All reagents used were of analytical grade. The cis-dichlorodiammine platinum (PDD) was prepared from potassium chloroplatinate using the acetate method to obtain bright yellow crystals which were repeatedly recrystallized and purified in hot water acidified with hydrochloric acid. Platyline blue was prepared in a dark room with purified PDD and osmolar (Pasimo) using the literature method. PDD and silver nitrate were mixed at a molar ratio of 1:2, and equimolar (mouth) was added. The reaction was carried out at 37° C. for 5 to 10 days and the pH was adjusted to 6, 5 to 8.5. At the end of the reaction, it was cooled at 4[deg.] C. and filtered to give a brilliant blue water. Filtrate plus an equal volume of ethanol is still available in small quantities. Platinum Blue is sealed with dark paper and protected from light at 4°C.