Holder G M, Tierney B, Bresnick E
Cancer Res. 1981 Nov;41(11 Pt 1):4408-14.
The binding of [3H]benzo(a)pyrene to proteins of rat liver cytosol, the nuclear uptake of cytosolic protein-bound [3H]-benzo(a)pyrene, and the subsequent nuclear metabolism of the polycyclic hydrocarbon were investigated. The binding of [3H]benzo(a)pyrene to cytosol had a saturable high affinity component with a Kd of 2.54 nM and a capacity of 530 fmol/mg protein. Specific binding of [3H]benzo(a)pyrene to cytosol was also assayed using sucrose density gradient analysis. Nuclear uptake of protein-bound [3H]benzo(a)pyrene was demonstrated both directly and by sucrose density gradient analysis. The nuclear benzo(a)pyrene was readily converted to metabolites which were qualitatively and quantitatively no different from nuclear metabolites of exogenously (not protein associated) added [3H]benzo(a)pyrene.
研究了[3H]苯并(a)芘与大鼠肝脏胞质溶胶蛋白质的结合、胞质溶胶中蛋白质结合的[3H]苯并(a)芘的核摄取以及随后多环烃的核代谢。[3H]苯并(a)芘与胞质溶胶的结合具有一个可饱和的高亲和力成分,解离常数(Kd)为2.54 nM,结合容量为530 fmol/mg蛋白质。还使用蔗糖密度梯度分析测定了[3H]苯并(a)芘与胞质溶胶的特异性结合。通过直接和蔗糖密度梯度分析均证实了蛋白质结合的[3H]苯并(a)芘的核摄取。核中的苯并(a)芘很容易转化为代谢产物,这些代谢产物在定性和定量上与外源添加(未与蛋白质结合)的[3H]苯并(a)芘的核代谢产物没有差异。