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Isolation and characterization at cholinergic nicotinic receptors of a neurotoxin from the venom of the Acanthophis sp. Seram death adder.

Abstract：

:The present study describes the isolation of the first neurotoxin (acantoxin IVa) from Acanthophis sp. Seram death adder venom and an examination of its activity at nicotinic acetylcholine receptor (nAChR) subtypes. Acantoxin IVa (MW 6815; 0.1-1.0 microM) caused concentration-dependent inhibition of indirect twitches (0.1 Hz, 0.2 ms, supramaximal V) and inhibited contractile responses to exogenous nicotinic agonists in the chick biventer cervicis nerve-muscle, confirming that this toxin is a postsynaptic neurotoxin. Acantoxin IVa (1-10 nM) caused pseudo-irreversible antagonism at skeletal muscle nAChR with an estimated pA2 of 8.36+/-0.17. Acantoxin IVa was approximately two-fold less potent than the long-chain (Type II) neurotoxin, alpha-bungarotoxin. With a pKi value of 4.48, acantoxin IVa was approximately 25,000 times less potent than alpha-bungarotoxin at alpha7-type neuronal nAChR. However, in contrast to alpha-bungarotoxin, acantoxin IVa completely inhibited specific [3H]-methyllycaconitine (MLA) binding in rat hippocampus homogenate. Acantoxin IVa had no activity at ganglionic nAChR, alpha4beta2 subtype neuronal nAChR or cytisine-resistant [3H]-epibatidine binding sites. While long-chain neurotoxin resistant [3H]-MLA binding in hippocampus homogenate requires further investigation, we have shown that a short-chain (Type I) neurotoxin is capable of fully inhibiting specific [3H]-MLA binding.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Wickramaratna JC,Fry BG,Loiacono RE,Aguilar MI,Alewood PF,Hodgson WC

doi

10.1016/j.bcp.2004.03.033

subject

Has Abstract

pub_date

2004-07-15 00:00:00

pages

383-94

issue

2

eissn

0006-2952

issn

1873-2968

pii

S0006295204002138

journal_volume

68

pub_type

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