柳珊瑚酸对乙酰胆碱酯酶的抑制作用(英文)

Inhibitory effect of suberogorgin on acetylcholinesterase

目的:研究柳珊瑚酸(suberogorgin,Sub)抗乙酰胆碱酯酶(AChE)作用的选择性、可逆性和动力学。方法:制备大鼠和人红细胞膜、大鼠脑和蚯蚓背肌提取液作为AChE组织样品,人血浆为丁酰胆碱酯酶(BuChE)样品;比色法测酶活力。结果:Sub明显抑制上述样品的AChE活力,其pl_(50)各为4.03,4.92,3.82和4.67,对BuChE无抑制作用。Sub与AChE一起孵温后,酶活力在3min内降至最低,而且离心洗涤可使酶活力恢复。不同浓度的Sub对AChE抑制作用的动力学曲线为平行线。结论:Sub是选择性和可逆性的AChE抑制剂,它与AChE的结合点在AChE的外周阴离子部位。

AIM: TO study the selection, reversibility, and kinetics of suberogorgin (Sub) on acetylcholines-terase (AChE). METHODS: The human plasma was used as butyrylcholinesterase (BuChE). The activity of ChE was determined with colorimetry. RESULTS: Sub obviously inhibited the AChE in vitro with pl50 4.03, 4.92, 3.82, and 4.67 in RBC membranes (of rat and human) and tissue extracts (of rat brain and earthworm dorsal muscle), respectively. No inhibition on BuChE was observed. The inhibition of Sub on AChE was far lower than that of physostigmine, but was close to that of galanthamine. Sub decreased the AChE activity to the lowest within 3 min after it was incubated with AChE. Centrifugalization washing reactivated the AChE which had been inhibited by Sub. The double-reciprocal plots of different concentrations of Sub on AChE showed parallel lines. CONCLUSION: Sub was a selective, reversible, and contra-competetive inhibitor of AChE at the binding site on the peripheral anion region of AChE.