[The interaction of organosilicon bisammonium compounds with the cholinesterases of Far-Eastern squids and vertebrates. The comparative enzymological, kinetic and conformational aspects].
The research of interaction of cholinesterases from human erythrocytes, horse blood serum, brain of the frog Rana temporaria, optical ganglia of the Pacific squid Todarodes pacificus, as well as optical ganglia of specimens of the Comandor squid Berryteuthis magister from different areas in the Bering sea with 13 organosilicon bis (trimethylammonium) compounds (silane and siloxane rows) as reversible cholinesterase inhibitors have been first studied and generalized. Calculations of the effector structure using the method of theoretical conformational analysis showed higher rigidity of interonium chain of siloxane derivatives and gave grounds to accept the asymmetry of hydrate envelope for these compounds. The data of conformational and kinetic analysis allowed to propose that specificity of antienzymic effect of organosilicon compounds was mainly due to conformational flexibility of interonium chain and the nature of hydration of effector molecule. The new information on the mechanism of catalytic reactions effected by cholinesterases from animals at different evolutionary stages was obtained.
Rozengart
E V
EV
Shestakova
N N
NN
Khovanskikh
A E
AE
Prokator
S O
SO
Kovalev
N N
NN
Epshteĭn
L M
LM
D000818:Animals; D002800:Cholinesterase Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D002802:Cholinesterases / Q000187:drug effects*; D049832:Decapodiformes / Q000201:enzymology*; D004347:Drug Interactions; D004912:Erythrocytes / Q000187:drug effects / Q000201:enzymology; D006736:Horses / Q000097:blood; D006801:Humans; D017646:Organosilicon Compounds / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D000644:Quaternary Ammonium Compounds / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D011896:Rana temporaria / Q000097:blood; D013329:Structure-Activity Relationship; D014714:Vertebrates / Q000097:blood*
D002800:Cholinesterase Inhibitors; D017646:Organosilicon Compounds; D000644:Quaternary Ammonium Compounds; D002802:Cholinesterases
Vzaimodeĭstvie kremniĭorganicheskikh bisammonievykh soedineniĭ s kholinésterazami dal'nevostochnykh kalmarov i nekotorykh pozvonochnykh. Sravnitel'no-énzimologicheskie, kineticheskie i konformatsionnye aspekty.