Numerical data concerning the inhibition of mammalian esterases with Bomin-1, 2 and 3.



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TOXINS & ALKALOIDS

Numerical data concerning the inhibition of mammalian esterases with Bomin-1, 2 and 3.
(2-alkoxy-2-oxo-3H-1, 4, 2-benzodioxaphosphorines compounds):






ENZYME Rat liver
CarboxylEsterase		 Human Erythrocytes
AcetylCholineEsterase		 Horse serum
ButyrylChlorineEsterase
INHIBITOR Type of
inhibition		 Ka
(Mx10-7)		 K+2
(min-1)		 KII
(M-1.min-1x106)		 Type of
inhibition		 KII
(M-1.min-1x10)		 Type of
inhibition		 Ki
(Mx10-5)
R=C2H5 : BOMIN-1 Irreversible 5.32 1.33 2.50 Irreversible 4.30 reversible
competitive		 2.22
R=C3H7-n : BOMIN-2 Irreversible 1.26 0.48 3.85 Irreversible 95.11 reversible
mixed-type		 1.42
R=C4H9-n : BOMIN-3 Irreversible 1.58 0.39 2.50 Irreversible 328.00 reversible
mixed-type		 0.83
  • Ka, k+2 and kII for irreversible CarboxylEsterase inhibition were determined according to the following scheme:
    E + l Ka
    		 El k+2
    		 El' with Ka=[E]x[l]/[El] and kII=k+2 / Ka

  • kII for irreversible AChE inhibition were determined according to the following scheme:
    E + l KII
    		 El'

  • Ki for reversible BuChE inhibition were determined from analysis of kinetics data in Lineweaver-Berk plots.
    Ki=[E]x[l]/[El]


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