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依据药物与DNA发生相互作用能抑制DNA的复制、合成和增殖且这种作用在体内与在体外的一致性,用荧光探剂溴化乙锭(EB,EthBr)示踪药物/DNA作用而提出了荧光筛选新方法。该法具有可靠性强、灵敏度高、操作简便、耗费很小、周期较短等特点,适合于抗癌药物的初步筛选。以所合成的Schiff碱非铂抗癌络合物为例,考察了方法的可行性,并进一步确定了Schiff碱络合物与DNA的结合常数K_M,发现其大小与抗癌活性顺序相一致。这一结果为解释络合物抗癌作用的生化基础提供了初步依据,同时还说明络合有利于抗癌并以载体或整体起作用。
Based on the interaction of drug and DNA, the DNA replication, synthesis and proliferation can be inhibited and the in vitro and in vivo consistency of this effect is demonstrated by the fluorescent / ethidium bromide (EB, EthBr) tracing drug / DNA interaction Fluorescent screening of new methods. The method has the characteristics of strong reliability, high sensitivity, easy operation, low cost and short cycle, and is suitable for the preliminary screening of anticancer drugs. Taking the synthesized Schiff base non-platinum anticancer complex as an example, the feasibility of the method was investigated and the binding constant K_M between the Schiff base complex and DNA was further confirmed, which was consistent with the order of anticancer activity. This result provides a preliminary basis for explaining the biochemical basis of the anticancer effect of the complex and at the same time shows that complexation is good for anticancer and acts as a carrier or an integral body.