Banerjee D, Redman C M
Biochim Biophys Acta. 1977 Nov 7;500(1):49-60. doi: 10.1016/0304-4165(77)90045-9.
The effects of some local anesthetics on plasma protein secretion by rat liver slices have been studied and have been compared with those of colchicine. Rat liver slices were pulse-labelled with L-[14C]leucine for 9 min at 37 degrees C, collected on filter paper, washed with non-radioactive leucine and reincubated in the presence or absence of the drug to be tested. The radioactive plasma proteins produced were obtained by immunoprecipitation from either the chase medium or from the washed slices. Chlorpromazine, (3.10(-5) M), dibucaine (10(-5) M), lidocaine (10(-3) M) and procaine (5.10(-5) M) inhibited both the synthesis and secretion of plasma protein but did not affect the uptake of L-leucine into the slices nor the incorporation of phosphate into intracellular nucleotide phosphates or into phospholipids. The inhibition of secretion elicited by these drugs is probably not due to the inhibition of protein synthesis since cycloheximide, when added to the chase medium at a concentration which completely inhibits protein synthesis, did not inhibit plasma protein secretion, while cycloheximide plus procaine did inhibit secretion and also caused a retention of non-secreted plasma proteins within the slices. Unlike colchicine, however, procaine did not cause the retained plasma proteins to accumulate in Golgi-derived secretory vesicles, but showed a more general effect causing a distribution among several cell fractions.
已研究了某些局部麻醉药对大鼠肝切片血浆蛋白分泌的影响，并与秋水仙碱的影响进行了比较。大鼠肝切片在37℃下用L-[14C]亮氨酸脉冲标记9分钟，收集在滤纸上，用非放射性亮氨酸洗涤，然后在有或无待测药物的情况下再孵育。产生的放射性血浆蛋白通过免疫沉淀从追踪培养基或洗涤后的切片中获得。氯丙嗪（3.10（-5）M）、丁卡因（10（-5）M）、利多卡因（10（-3）M）和普鲁卡因（5.10（-5）M）抑制血浆蛋白的合成和分泌，但不影响L-亮氨酸进入切片的摄取，也不影响磷酸盐掺入细胞内核苷酸磷酸或磷脂。这些药物引起的分泌抑制可能不是由于蛋白质合成的抑制，因为当以完全抑制蛋白质合成的浓度加入追踪培养基时，环己酰亚胺不抑制血浆蛋白分泌，而环己酰亚胺加普鲁卡因确实抑制分泌，并且还导致未分泌的血浆蛋白在切片内潴留。然而，与秋水仙碱不同，普鲁卡因不会使潴留的血浆蛋白在高尔基体衍生的分泌小泡中积累，而是表现出更普遍的作用，导致其在几个细胞组分中分布。
