Ricci G L, Baldassarre V, Longo G, Zanninelli G
Arzneimittelforschung. 1986 Apr;36(4):691-4.
The apparent maximal transport capacity (Tm) of the liver for bilirubin was studied in rats after oral treatment for two weeks with the two flavonoids (+)-cyanidanol-3 and palmitoyl-catechin in order to investigate a possible mechanism of action on jaundice described in humans. (+)-Cyanidanol-3 produces no changes in bilirubin-Tm, and the analysis of bilirubin and its conjugates in the different compartments reveals a decreased amount of the whole bilirubin taken up by the liver. Palmitoyl-catechin, a more lipophilic derivative of catechin, produces a slight increase in bilirubin-Tm. This appears related to the increased conjugation rate demonstrated in vitro for bilirubin. A multicompartimental analysis shows a different distribution of bilirubins as compared to controls. It is likely that physicochemical changes of the membrane environment, where the enzyme is buried, have modified the capacity of the hepatocyte to dispose bilirubin.
为了研究两种黄酮类化合物(+)-氰定醇-3和棕榈酰儿茶素对人体黄疸可能的作用机制,对大鼠进行了为期两周的口服治疗,之后研究了肝脏对胆红素的表观最大转运能力(Tm)。(+)-氰定醇-3对胆红素-Tm没有影响,对不同区室中胆红素及其结合物的分析显示,肝脏摄取的总胆红素量减少。棕榈酰儿茶素是儿茶素的一种亲脂性更强的衍生物,可使胆红素-Tm略有增加。这似乎与体外证实的胆红素结合率增加有关。多区室分析显示,与对照组相比,胆红素的分布有所不同。很可能是酶所在的膜环境的物理化学变化改变了肝细胞处理胆红素的能力。