Nakamura H, Ishikawa M
Hokkaido Igaku Zasshi. 1975 Sep;50(5):476-84.
Animal experiments using mice were conducted to determine the difference of cholesterol metabolism, if any, between a group of mice administered with dl-alpha-tocopheryl linolate (EL) and another group administered with a mixture of dl-alpha-tocopheryl acetate (E), and ethyllinolate (L) (E+L) that were combined in such a way as to have the same composition as EL. The following results were obtained. 1. While no difference in cholesterol biosynthesis was seen in, in vitro liver homogenate to which agent were added, in liver from animals orally administered with agents in vivo, a decrease in biosynthesis of liver cholesterol in the EL group compared against the E+L group was seen, where-as opposite results were obtained when the agents were injected. 2. Absorption of cholesterol was studied. Cholesterol-4-14C was intubated into the stomach of mice fed with the agents. From the cholesterol radioactivity appearing in blood, it was seen that the inhibition of cholesterol absorption in the small intestine was higher in the EL group than in the E+L group. At the same time the excretion of the sterol-14C coming from the intubated cholesterol-14C into the feces was considerably higher in the EL group as compared with the E+L group. However, when a mixture of the agents and cholesterol-4-14C was intubated into the stomach of normally fed mice, no differences in absorption was seen and results opposite to the above were seen in the excretion of sterol-14C into the feces. 3. Following cholesterol-4-14C injection, when the mice were fed on agent added feed, the EL group showed an increased excretion of sterol-14C and sterol into feces as compared with the E+L group. 4. Regarding the disappearance of injected cholesterol-4-14C from the tissue, no difference was seen between the EL group and the E+L group, when the agents were injected or fed. 5. With regard to in vivo biosynthesis of fatty acid in the group administered orally with the agents, liver fatty acid biosynthesis showed to decrease in the EL group compared with the E+L group, while opposite results were seen in the injected groups. Based on the above, when viewed from cholesterol metabolism, oral administration of agents in the EL group showed a superior effect as a cholesterol-lowering agents compared against the E+L group and the writer is of the opinion that this may well be used for clinical purposes.
进行了以小鼠为对象的动物实验,以确定给予dl-α-生育酚亚油酸酯(EL)的小鼠组与给予dl-α-生育酚醋酸酯(E)和亚油酸乙酯(L)的混合物(E+L,其组合方式使得成分与EL相同)的另一组小鼠之间胆固醇代谢的差异(若有)。获得了以下结果。1. 虽然在添加试剂的体外肝脏匀浆中未观察到胆固醇生物合成的差异,但在体内经口给予试剂的动物肝脏中,与E+L组相比,EL组肝脏胆固醇生物合成减少,而当注射试剂时则获得相反结果。2. 研究了胆固醇的吸收。将胆固醇-4-¹⁴C插管到喂食试剂的小鼠胃中。从血液中出现的胆固醇放射性可知,EL组小肠中胆固醇吸收的抑制作用高于E+L组。同时,与E+L组相比,EL组中来自插管的胆固醇-¹⁴C的甾醇-¹⁴C向粪便中的排泄显著更高。然而,当将试剂与胆固醇-4-¹⁴C的混合物插管到正常喂食小鼠的胃中时,未观察到吸收差异,且在甾醇-¹⁴C向粪便中的排泄方面出现了与上述相反的结果。3. 在注射胆固醇-4-¹⁴C后,当给小鼠喂食添加了试剂的饲料时,与E+L组相比,EL组中甾醇-¹⁴C和甾醇向粪便中的排泄增加。4. 关于注射的胆固醇-4-¹⁴C从组织中的消失情况,当注射或喂食试剂时,EL组和E+L组之间未观察到差异。5. 关于经口给予试剂的组中脂肪酸的体内生物合成,与E+L组相比,EL组肝脏脂肪酸生物合成减少,而在注射组中观察到相反结果。基于上述情况,从胆固醇代谢的角度来看,EL组经口给予试剂作为降胆固醇剂显示出比E+L组更好的效果,作者认为这很可能可用于临床目的。