氨基硫脲基Ru配合物对生物大分子催化活性的研究及对抗癌机理的新认识

项目名称： 氨基硫脲基Ru配合物对生物大分子催化活性的研究及对抗癌机理的新认识

项目编号： No.21463009

项目类型： 地区科学基金项目

立项/批准年度： 2015

项目学科： 数理科学和化学

项目作者： 杨晶

作者单位： 南宁师范大学

项目金额： 48万元

中文摘要： 癌症是严重危害人类健康的主要疾病之一，为攻克这一难题，寻找药效高、抗癌谱广、毒性低的抗癌药物一直是医学家、化学家共同关注的课题。金属芳基Ru配合物由于具有低毒、易排泄、易被肿瘤组织吸收等特点，而受到人们的广泛关注。本项目以前期工作中合成的具有高抗肿瘤特性的金属芳基Ru氨基硫脲配合物为基础，选取生物大分子---蛋白质和DNA为靶分子，将催化概念应用于生物及医学领域中，通过研究氨基硫脲基金属Ru配合物对DNA及氨基酸（蛋白质的主要组成部分）可能发生的水解、氢转移、氧化还原等反应的催化活性，将活性数据与抗癌性能对比，从而从催化角度上探索该系列金属Ru配合物具有抗癌性能的可能原因，在研究思想及研究方式上有创新。本项目有利于从分子水平上阐明癌症等疾病的致病机制，从而使通过药物体外筛选寻找有效治疗和诊断药物成为可能。

中文关键词： 氨基硫脲；Ru配合物；生物大分子；催化活性；抗癌机理

英文摘要： Cancer is one of the serious diseases endangering human life and health.In order to overcome this problem, looking for the anticancer drugs with high efficacy，broad spectrum and low toxicity have always been the issues of common concerns for pharmacologists and chemists. Owing to the features of low toxicity, easy to be excreted and absorbed by tumor，Ru compounds have cut a conspicuous figure in the anti-cancer battle and displaced the traditional anti-cancer drugs cisplatin and carboplatin gradually. A series of Ru complexes with thiosemicarbazide ligand have been synthesised and presented high anti-cancer properties. Based on the previous research work, the concept of catalysis is applied to the biological and medical fields, DNA and protein were chosen as the target molecules,the catalytic activity of different reactions of DNA and protein catalysed by Ru complex were discussed and the catalytic mechanism of anti-cancer properties for the Ru complexes are studied in the point of catalysis. This project has innovation on the study ideas and means, which lay the foundation of selecting drugs in vitro, provide theoretical basis for designing and developing anti-cancer drugs and make it possible for elucidating the carcinogenesis and overcoming the problem of cancer.

英文关键词： thiosemicarbazone;complex of Ru;biomacromolecules;catalytic acitivity;anticancer mechanism