Comoglio A, Leonarduzzi G, Carini R, Busolin D, Basaga H, Albano E, Tomasi A, Poli G, Morazzoni P, Magistretti M J
Department of Experimental Medicine and Oncology, University of Turin, Italy.
Free Radic Res Commun. 1990;11(1-3):109-15. doi: 10.3109/10715769009109673.
Silybin has been complexed in 1:1 ratio with phosphatidyl choline to give IdB 1016 in order to increase its bioavailability. The antioxidant and free radical scavenger action of this new form of silybin has been evaluated. One hour after the intragastric administration to rats of IdB 1016 (1.5 g/kg b.wt.) the concentration of silybin in the liver microsomes was estimated to be around 2.5 micrograms/mg protein corresponding to a final concentration in the microsomal suspension used of about 10 microM. At these levels IdB decreased by about 40% the lipid peroxidation induced in microsomes by NADPH, CCl4 and cumene hydroperoxide, probably by acting on lipid derived radicals. Spin trapping experiments showed, in fact, that the complexed form of silybin was able to scavenge lipid dienyl radicals generated in the microsomal membranes. In addition, IdB 1016 was also found to interact with free radical intermediates produced during the metabolic activation of carbon tetrachloride and methylhydrazine. These effects indicate IdB 1016 as a potentially protective agent against free radical-mediated toxic damage.
水飞蓟宾已与磷脂酰胆碱按1:1的比例络合生成IdB 1016，以提高其生物利用度。这种新型水飞蓟宾的抗氧化和自由基清除作用已得到评估。给大鼠灌胃IdB 1016（1.5 g/kg体重）1小时后，肝脏微粒体中水飞蓟宾的浓度估计约为2.5微克/毫克蛋白质，相当于所用微粒体悬浮液中的最终浓度约为10微摩尔。在这些水平下，IdB使由NADPH、四氯化碳和氢过氧化异丙苯诱导的微粒体脂质过氧化降低了约40%，这可能是通过作用于脂质衍生的自由基实现的。自旋捕获实验表明，事实上，水飞蓟宾的络合形式能够清除微粒体膜中产生的脂质二烯基自由基。此外，还发现IdB 1016与四氯化碳和甲基肼代谢活化过程中产生的自由基中间体相互作用。这些作用表明IdB 1016是一种潜在的抗自由基介导的毒性损伤保护剂。
