Coluccia M, Fanizzi F P, Giannini G, Giordano D, Intini F P, Lacidogna G, Loseto F, Mariggio M A, Nassi A, Natile G
Istituto di Patologia Generale, Bari, Italy.
Anticancer Res. 1991 Jan-Feb;11(1):281-7.
Platinum complexes with N,N'-bis(1-hydroxybut-2-yl)ethylenediamine, [PtCl2(ethambutol)] were prepared and the biological activity of three isomers [with (-), (+) and (+/-) ethambutol, respectively] investigated. All species interact with the Bam HI and Ava I recognition sequences showing a binding preference for GC rich sequences of DNA. The complex which showed the greatest interaction with adjacent guanines, [PtCl2[+/-)ethambutol)] was also found to be the most mutagenic of the three. On the other hand, only [PtCl2[+)ethambutol)] had a considerable antitumour activity against both P388 leukaemia and Lewis lung carcinoma, and this was not correlated either with restriction enzyme blocking activity or with mutagenicity.
制备了铂与 N,N'-双(1-羟基丁-2-基)乙二胺的配合物[PtCl2(乙胺丁醇)]，并研究了三种异构体[分别与(-)、(+)和(+/-)乙胺丁醇形成的配合物]的生物活性。所有物种均与Bam HI和Ava I识别序列相互作用，对富含GC的DNA序列表现出结合偏好。与相邻鸟嘌呤相互作用最强的配合物[PtCl2[(+/-)乙胺丁醇]]也被发现是三种配合物中诱变活性最强的。另一方面，只有[PtCl2[(+)乙胺丁醇]]对P388白血病和Lewis肺癌都具有相当的抗肿瘤活性，且这与限制酶阻断活性或诱变性均无关联。
