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[吡啶鎓、硫代吡啶鎓和硒代吡啶鎓衍生物盐对胆碱酯酶的可逆抑制作用]

[Reversible inhibition of cholinesterases by salts of pyrilium, thiopyrilium and selenopyrilium derivatives].

作者信息

Brestkin A P, Dmitrieva E N, Zhukovskiĭ Iu G, Safonova A A, Sedavkina V A

出版信息

Ukr Biokhim Zh (1978). 1988 Mar-Apr;60(2):35-40.

PMID:3394173
Abstract

Salts of pyrilium, thiopyrilium and selenopyrilium derivatives at pH 7.5 and temperature of 25 degrees C are studied for their effect on the catalytic activity of acetyl cholinesterase (EC 3.1.1.7) of human blood erythrocytes and butyryl cholinesterase (EC 3.1.1.8) of horse blood serum which is measured by the method of potentiometric titration. All enumerated salts are established to be strong reversible inhibitors of mixed-type cholinesterases, that is testified by small values of the inhibitory constants: competitive Ki, noncompetitive K'i and generalized K epsilon. Pyrilium and selenopyrilium salts inhibit acetyl cholinesterase of human blood erythrocytes to a higher extent than butyryl cholinesterase of horse blood serum, and thiopyrilium salts inhibit the latter to the highest extent. By the value of the inhibitory effect on acetyl cholinesterase of human blood erythrocytes thiopyrilium salts exceed the analogous pyrilium salts, whereas in experiments with butyl cholinesterase of horse blood serum there is an opposite dependence.

摘要

在pH值为7.5、温度为25摄氏度的条件下,研究了吡喃鎓盐、硫代吡喃鎓盐和硒代吡喃鎓盐衍生物对人血红细胞乙酰胆碱酯酶(EC 3.1.1.7)和马血清丁酰胆碱酯酶(EC 3.1.1.8)催化活性的影响,采用电位滴定法进行测定。所有列举的盐均被确定为混合型胆碱酯酶的强可逆抑制剂,这通过抑制常数的小数值得到证明:竞争性Ki、非竞争性K'i和广义Kε。吡喃鎓盐和硒代吡喃鎓盐对人血红细胞乙酰胆碱酯酶的抑制程度高于马血清丁酰胆碱酯酶,而硫代吡喃鎓盐对后者的抑制程度最高。就对人血红细胞乙酰胆碱酯酶的抑制作用而言,硫代吡喃鎓盐超过了类似的吡喃鎓盐,而在马血清丁酰胆碱酯酶的实验中则存在相反的依赖性。

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