Leth T, Søndergaard H
Int J Vitam Nutr Res. 1983;53(3):297-311.
The biological activity of 2 R, 4' R, 8' R-(RRR)-a-tocopherol and all-rac-a-tocopherol has been determined by 3 different bioassays: Resorption-gestation test, red blood cell hemolysis test and rat liver storage test. Expressed in relation to all-rac-a-tocopheryl acetate is found by the resorption-gestation test with the doses given in vegetable oil potency ratios of 0.79 for all-rac-a-tocopherol and 1.06 for RRR-a-tocopherol, by the red blood cell hemolysis test ratios of 0.85 for all-rac-a-tocopherol and 1.13 for RRR-a-tocopherol and by the rat liver storage test ratios of 1.03 for all-rac-a-tocopherol and 1.32 for RRR-a-tocopherol. Furthermore is by the resorption-gestation test found a potency ratio of 0.90 between RRR-a-tocopheryl succinate and all-rac-a-tocopheryl acetate. By the evaluation of these figures, most weight must be added to the results from the resorption-gestation test, as it involves the most complex biological mechanism of the 3 methods. The potency ratios found in this investigation are significantly lower than the currently accepted potency ratios of 1.10 between all-rac-a-tocopherol and all-rac-a-tocopheryl acetate, 1.49 between RRR-a-tocopherol and all-rac-a-tocopheryl acetate and 1.21 between RRR-a-tocopheryl succinate and all-rac-a-tocopheryl acetate (all values calculated from their corresponding acetate by multiplication with the ratio of the molecular weight), but the potency ratio between RRR-a-tocopherol and all-rac-a-tocopherol calculated from the 3 different bioassays does not deviate significantly from the currently accepted value of 1.36. It seems necessary to reconsider the biological activity of all-rac-a-tocopherol and RRR-a-tocopherol, and it is suggested to use a potency ratio of 0.80 between all-rac-a-tocopherol and all-rac-a-tocopheryl acetate and 1.0 between RRR-a-tocopherol and all-rac-a-tocopheryl acetate.
通过三种不同的生物测定法测定了2R,4'R,8'R-(RRR)-α-生育酚和消旋-α-生育酚的生物活性：着床-妊娠试验、红细胞溶血试验和大鼠肝脏储存试验。以消旋-α-生育酚醋酸酯为参照，在着床-妊娠试验中，按植物油效价比给药时，消旋-α-生育酚的效价比为0.79，RRR-α-生育酚为1.06；在红细胞溶血试验中，消旋-α-生育酚的效价比为0.85，RRR-α-生育酚为1.13；在大鼠肝脏储存试验中，消旋-α-生育酚的效价比为1.03，RRR-α-生育酚为1.32。此外，在着床-妊娠试验中发现RRR-α-生育酚琥珀酸酯与消旋-α-生育酚醋酸酯的效价比为0.90。通过对这些数据的评估，必须对着床-妊娠试验的结果给予最大权重，因为它涉及这三种方法中最复杂的生物学机制。本研究中发现的效价比显著低于目前公认的消旋-α-生育酚与消旋-α-生育酚醋酸酯之间的效价比1.10、RRR-α-生育酚与消旋-α-生育酚醋酸酯之间的效价比1.49以及RRR-α-生育酚琥珀酸酯与消旋-α-生育酚醋酸酯之间的效价比1.21（所有数值均通过将其相应醋酸酯乘以分子量比计算得出），但从三种不同生物测定法计算得出的RRR-α-生育酚与消旋-α-生育酚之间的效价比与目前公认的1.36值无显著偏差。似乎有必要重新考虑消旋-α-生育酚和RRR-α-生育酚的生物活性，建议消旋-α-生育酚与消旋-α-生育酚醋酸酯之间的效价比为0.80，RRR-α-生育酚与消旋-α-生育酚醋酸酯之间的效价比为1.0。
