Pu G A, Anderson R E
Invest Ophthalmol Vis Sci. 1983 Mar;24(3):288-93.
The choline analog hemicholinium-3 causes selective degeneration of the cones and rods in the rabbit retina. These experiments examine some biochemical effects of hemicholinium-3 on metabolic pathways involved in choline metabolism. No effect of the drug on several important photoreceptor biosynthetic functions was found: leucine incorporation into TCA-precipitable material, glycerol incorporation into phospholipids, and phosphatidylcholine formation by either base exchange or choline phosphotransferase activity. However, hemicholinium-3 does selectively affect free choline use: high-affinity uptake, phosphorylation and subsequent incorporation into lipid. In each instance, hemicholinium-3 causes a significant inhibition of control activity at a concentration of 30 microM, a dosage that causes complete photoreceptor outer segment degeneration in mammalian retinas. Thus, it seems that the enormous synthetic requirements for phosphatidylcholine leave the photoreceptor cell in fragile metabolic balance, and transient alteration of this balance may destroy the outer segment.
胆碱类似物半胱氨酸-3会导致兔视网膜中的视锥细胞和视杆细胞发生选择性退化。这些实验研究了半胱氨酸-3对胆碱代谢相关代谢途径的一些生化影响。未发现该药物对几种重要的光感受器生物合成功能有影响:亮氨酸掺入三羧酸循环可沉淀物质、甘油掺入磷脂以及通过碱基交换或胆碱磷酸转移酶活性形成磷脂酰胆碱。然而,半胱氨酸-3确实会选择性地影响游离胆碱的利用:高亲和力摄取、磷酸化以及随后掺入脂质。在每种情况下,半胱氨酸-3在30微摩尔浓度时会导致对照活性显著抑制,该剂量会导致哺乳动物视网膜中的光感受器外段完全退化。因此,似乎对磷脂酰胆碱的巨大合成需求使光感受器细胞处于脆弱的代谢平衡中,而这种平衡的短暂改变可能会破坏外段。