MMSL 2011, 80(3):129-139 | DOI: 10.31482/mmsl.2011.019

ANATOXIN-A(S): NATURAL ORGANOPHOSPHORUS ANTICHOLINESTERASE AGENTReview article

Jiří Patočka ORCID...1*, Ramesh C. Gupta2, Kamil Kuča ORCID...3
1 Department of Radiology and Toxicology, Faculty of Health and Social Studies, University of South Bohemia České Budějovice, České Budějovice, Czech Republic
2 Breathitt Veterinary Center, Toxicology Department, Murray State University, Hopkinsville, KY, USA
3 Center of Advanced Studies, Faculty of Military Health Sciences, University of Defence, Hradec Králové, Czech Republic

Anatoxin-a(s) is a guanidinemethyl phosphate ester isolated from the freshwater cyanobacterium (blue-green algae) Anabaena flos-aquae strain NRC 525-17. Previous work has shown anatoxin-a(s) to be a potent irreversible inhibitor of electric eel acetylcholinesterase (AChE, EC 3.1.1.7). Anatoxin-a(s) has been shown to be an active site-directed inhibitor of AChE, which is resistant to reactivation by oximes because of the enzyme-oxime adduct formation. In vivo pretreatment with physostigmine and high concentrations of pyridine 2-aldoxime methochloride (2-PAM) were the only effective antagonists against a lethal dose of anatoxin-a(s). Anatoxin-a(s) is very toxic and it is produced by cyanobacteria during its blooms. Purified toxin has an LD50 (i.p) of approximately 20-50 μg/kg body weight in mice. Toxicoses associated with cholinesterase-inhibiting anatoxin-a(s) have been observed in humans, animals, birds and fish. Anatoxin-a(s) induces clinical signs of hypercholinergic preponderance, such as salivation, lacrimation, urinary incontinence, defecation, convulsion, fasciculation, and respiratory arrest.

Keywords: natural organophosphate; anatoxin-a(s); anticholinesterase; chemistry; pharmacology; toxicology; blue-green algae; neurotoxin

Received: July 1, 2011; Revised: August 22, 2011; Published: September 9, 2011  Show citation

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Patočka, J., Gupta, R.C., & Kuča, K. (2011). ANATOXIN-A(S): NATURAL ORGANOPHOSPHORUS ANTICHOLINESTERASE AGENT. MMSL, 80(3), 129-139. doi: 10.31482/mmsl.2011.019
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