Tjälve H, Olsson S, Andersson A
Acta Pharmacol Toxicol (Copenh). 1980 Jul;47(1):38-44. doi: 10.1111/j.1600-0773.1980.tb02022.x.
The uptake of 14C-chloroquine by isolated mouse pancreatic islets in vitro was investigated. The islets were found to have a very high capacity to accumulate the substance. The uptake of 14C-chloroquine in the islets was a saturable process. Metabolic inhibitors, ouabain, anaerobic conditions and absence of glucose did not inhibit the uptake of 14C-chloroquine in the islets, suggesting that the substance is accumulated by some means other than energy-dependent active transport or pinocytosis. The uptake of 14C-chloroquine was inhibited by low temperature and low pH and in the presence of mepacrine, chlorpromazine, imipramine and desmethylimipramine. Only a small part of the 14C-chloroquine which had been taken up in the islets left the cells during 45 min. incubation in non-radioactive media. Two possible mechanisms for the uptake of 14C-chloroquine in the islets are considered: (1) The accumulation may be due to a binding of the substance to cellular constituents. (2) Chloroquine may be trapped by protonation within lysosomes or other membrane-surrounded organelles with low pH.
研究了体外分离的小鼠胰岛对14C-氯喹的摄取。发现胰岛具有非常高的积累该物质的能力。胰岛中14C-氯喹的摄取是一个可饱和的过程。代谢抑制剂、哇巴因、无氧条件和无葡萄糖均不抑制胰岛对14C-氯喹的摄取，这表明该物质是通过能量依赖性主动转运或胞饮作用以外的某种方式积累的。低温、低pH以及在存在米帕林、氯丙嗪、丙咪嗪和去甲丙咪嗪的情况下，14C-氯喹的摄取受到抑制。在非放射性培养基中孵育45分钟期间，胰岛中摄取的14C-氯喹只有一小部分离开细胞。考虑了胰岛中14C-氯喹摄取的两种可能机制：(1)积累可能是由于该物质与细胞成分结合。(2)氯喹可能通过质子化被困在溶酶体或其他低pH的膜包围细胞器内。
