Richmond R C, Simic M G
Br J Cancer Suppl. 1978 Jun;3:20-3.
The radiolysis of cis-dichlorodiammineplatinum (II) (cis-PDD) was studied in order to better understand the mechanisms by which it acts as a radiation sensitizer. The Pt(I) intermediate formed by e- aq reduction of cis-PDD loses both chlorides rapidly, interacts with O2 to form a Pt-oxygen adduct, reacts with the hydroxyl radical adduct of thymine and the peroxy radical of t-butanol, and disproportionates to platinum metal and trans-PDD. The Pt (III) intermediate formed by OH oxidation of cis-PDD likely disproportionates to cis-PDD and Pt(IV) complexes. In a biological model, radiation-induced 3H-thymine base residue release from DNA is found to be inhibited by cis-PDD.
为了更好地理解顺二氯二氨铂(II)(顺铂)作为辐射增敏剂的作用机制,对其辐射分解进行了研究。通过水合电子还原顺铂形成的Pt(I)中间体迅速失去两个氯原子,与O2相互作用形成Pt-氧加合物,与胸腺嘧啶的羟基自由基加合物和叔丁醇的过氧自由基反应,并歧化为铂金属和反式顺铂。通过顺铂的OH氧化形成的Pt(III)中间体可能歧化为顺铂和Pt(IV)配合物。在生物模型中,发现顺铂可抑制辐射诱导的DNA中3H-胸腺嘧啶碱基残基的释放。