Douaud F, Le Roch N, Renault J, Havouis R, Vaultier M, Moulinoux J P, Seiler N
UPRES-A CNRS 6027, Institut de Recherche Contre le Cancer, Faculté de Médecine, Université de Rennes I, France.
Anticancer Drug Des. 1997 Dec;12(8):621-33.
Several dimethylsilane tetramines [homologs of spermine with an Si(CH3)2 group in the central carbon chain], a carbon analog of the dimethylsilane tetramines [containing C(CH3)2 instead of Si(CH3)2] and a dimethylsilane hexamine were studied with regard to their cytotoxic activity and their ability to interact with double-stranded DNA. All polyamine analogs exerted cytostatic effects to several cell lines at micromolar concentrations. Their ability to condense DNA was comparable to and their ability to displace ethidium bromide from binding to DNA was superior to that of spermine. Their cytostatic effect was not correlated with the depletion of cellular spermidine concentrations. It is suggested that the new polyamine analogs act mainly by displacing spermidine from binding sites which are essential for the promotion of cell growth.
研究了几种二甲基硅烷四胺（在中心碳链中具有Si(CH3)2基团的精胺同系物）、二甲基硅烷四胺的碳类似物（含有C(CH3)2而非Si(CH3)2）以及一种二甲基硅烷六胺的细胞毒性活性及其与双链DNA相互作用的能力。所有多胺类似物在微摩尔浓度下对几种细胞系都发挥了细胞生长抑制作用。它们凝聚DNA的能力与精胺相当，且从与DNA结合中取代溴化乙锭的能力优于精胺。它们的细胞生长抑制作用与细胞内亚精胺浓度的消耗无关。有人提出，新的多胺类似物主要通过从对促进细胞生长至关重要的结合位点取代亚精胺来发挥作用。
