Zimmermann W A, Hartmann G R
Eur J Biochem. 1981 Aug;118(1):143-50. doi: 10.1111/j.1432-1033.1981.tb05497.x.
When the potent immunosuppressive sesquiterpene ovalicin is added to lymphocyte cultures one first observes a preferential inhibition of uridine incorporation into rRNA. The uptake of the nucleoside, its conversion into the triphosphate or the polymerizing activity itself are not affected. A longer period of incubation with the drug results in a marked decrease in the number of ribosomes, with a concomitant reduction of the rate of leucine incorporation into all cellular proteins. After extended periods of time, the incorporation of thymidine into DNA in stimulated lymphocytes as well as in SV49.1 lymphoma cells is inhibited by 1 nM ovalicin or less, although part of the incorporation seems to be resistant to the drug even at much higher concentrations. A similar affect is observed with 3T6 mouse fibroblasts or HeLa cells. Here, however, a much longer incubation with the drug is required. This observation explains the selective effect of ovalicin on lymphocytes observed in vivo.
当将强效免疫抑制倍半萜烯椭圆玫瑰树碱添加到淋巴细胞培养物中时，首先观察到尿苷掺入rRNA受到优先抑制。核苷的摄取、其转化为三磷酸酯或聚合活性本身均未受影响。用该药物孵育更长时间会导致核糖体数量显著减少，同时亮氨酸掺入所有细胞蛋白质的速率也会降低。经过较长时间后，1 nM或更低浓度的椭圆玫瑰树碱会抑制刺激的淋巴细胞以及SV49.1淋巴瘤细胞中胸苷掺入DNA，尽管即使在更高浓度下，部分掺入似乎对该药物具有抗性。在3T6小鼠成纤维细胞或HeLa细胞中也观察到类似的效应。然而，在这里需要用该药物孵育更长时间。这一观察结果解释了椭圆玫瑰树碱在体内对淋巴细胞的选择性作用。
