SUMMARY
Daphnia magna is a freshwater microcrustacean which is often used for acute and chronic toxicity testing
in aquatic ecotoxicology. Recently, tests with daphnids have been used to prescreen the toxicity of newly
synthesized acetylcholinesterase reactivators (oximes), which appear as weak inhibitors of
acetylcholinesterase (AChE). In our study we investigated and compared the toxicity of five reversible
acetylcholinesterase inhibitors, two of them non ionic (tacrine and 7-MEOTA) and three ionic (berberine
chloride, 1-methyltacridium iodide and ethidium bromide). Tests were carried out according to the
methodology described in the standard EN ISO 6341. EC50 values as well as dose-response curves were
calculated for all tested inhibitors. In general, non ionic substances were found to be less toxic than ionic
substances. Estimated EC50 values in tests taking respectively 24 h and 48 h were as follows: tacrine 3000
resp. 1515 micro g.l-1, 7-MEOTA 3606 resp. 707.2 micro g.l-1, berberine chloride 903.6 resp. 822.4 micro g.l-1, 1-methylacridinium iodide 714.3 resp. 233.5 micro g.l-1 and ethidium bromide 644.3 resp. 291.1 micro g.l-1. The higher
toxicity of 7-MEOTA in time compared to tacrine and the similar toxicity of berberine chloride in both
tests are explained as a consequence of their metabolism in the daphnid's body.
KEY WORDS
antidotes; cholinesterase; crustacean; inhibition; tacrine; toxicity
REFERENCES
Adema DMM: Daphnia magna as a test animal in
acute and chronic toxicity tests. Hydrobiologia
59:125-134, 1978.
Baird DJ, Barber I, Bradley M et al.: The
Daphnia bioassay: a critique. Hydrobiologia
188/189:403-406, 1989.
Benzie JAH: Cladocera: The Genus Daphnia
(including Daphniopsis). Guides to the identification of the microinvertebrates of the
continental waters of the world. Vol. 21,
Kenobi Prod., Ghent 2005.
Berger J: Why do circadian biorythms age?
J Appl Biomed 1:77-84, 2003.
Cooney JD: Freshwater tests. In Rand GM (ed.):
Fundamentals of aquatic toxicology, Taylor
and Francis, New York 2003, pp. 71-102.
De Bosschere H, Baert K, Ducatelle R, De
Backer P: The use of a Daphnia magna
bioassay for rapid screening of acute
intoxications with insecticides in dogs and
cats. Vet Res Commun 25:421-427, 2001.
Dejmek L: 7-MEOTA. Drugs Future 15:126-129, 1990.
Diamantino TC, Almeida E, Soares AMVM,
Guilhermino L: Characterization of
cholinesterases from Daphnia magna Straus
and their inhibition by zinc. Bull Environ
Contam Toxicol 71:219-225, 2003.
Eddleston M, Eyer P, Worek F et al.: Differences
between organophosphorus insecticides in
human self-poisoning: a prospective cohort
study. Lancet 366 (9495):1452-1459, 2005.
EN ISO. Water quality - Determination of the
inhibition of the mobility of Daphnia magna
Straus (Cladocera, Crustacea) - Acute toxicity
test, EN ISO 6341:1996/AC 1998. European
Committee for Standardization, Brussels 1998.
Guilhermino L, Lopes MC, Carvalho P, Soares
AMVM: Inhibition of acetylcholinesterase
activity as effect criterion in acute tests with
juvenile Daphnia magna. Chemosphere
32:727-738, 1996.
Kuca K, Cabal J, Patocka J, Dohnal V:
Quaternary heteroarenium salts as the
competitive inhibitors of the brain
acetylcholinesterase. Lett Drug Des Discov
1:97-100, 2004.
Motulsky HJ, Christopoulos A: Fitting Models to
Biological Data using Linear and Nonlinear
Regression. A practical guide to curve fitting.
GraphPad Software Inc, San Diego 2003.
Newman C: Quantitative Methods in Aquatic
Toxicology. Lewis Publishers, Florida 1995.
Passmore P, Patterson C: Acetylcholinesterase
inhibitors: Cognition and function. CPD Bull
Old Age Psychiatry 2:63-70, 2001.
Peters RH: Metabolism in Daphnia. In Peters
RH, De Bernardi R (eds.): Daphnia,
Memorie Dell'istituto Italiano di Idrobiologia
45:193-243, 1987.
Pope C, Karanth S, Liu J: Pharmacology and
toxicology of cholinesterase inhibitors: uses
and misuses of common mechanism of action.
Environ Toxicol Pharmacol 19:433-446, 2005.
Postmes ThJ, Prick R, Brorens I: The declaration
of the heart frequency in the water flea
Daphnia magna by adrenoreceptor agonists
and antagonists. Hydrobiologia 171:141-148, 1989.
Printes LB, Callaghan A: A comparative study on
the relationship between acetylcholinesterase
activity and acute toxicity in Daphnia magna
exposed to anticholinesterase insecticides.
Environ Toxicol Chem 23:1241-1247, 2004.
Skrinjaric-Spoljar M, Burger N, Lovric J:
Inhibition of acetylcholinesterase by three new
pyridinium compounds and their effect on
phosphonylation of the enzyme. J Enzyme
Inhib Med Chem 14:331-341, 1999.
Tsai PL, Tsai TH: Hepatobiliary excretion of
berberine. Drug Metab Dispos 32:405-412, 2004.
Vesela S, Ondruska V, Kuca K, Patocka J: Tests
with Daphnia magna: A new approach to
prescreen toxicity of newly synthesized
acetylcholinesterase reactivators. J Enzyme
Inhib Med Chem in press, 2006.
Villegas-Navarro A, Esperanza Rosas L, Reyes
JL: The heart of Daphnia magna: effect of
four cardioactive drugs. Comp Biochem
Physiol C, Pharmacol Toxicol Endocrinol
136:127-134, 2003.
|
CITED
Novackova M, Halaska MJ, Robova H, Mala I, Pluta M, Chmel R, Rob L. A Prospective Study in Detection of Lower-Limb Lymphedema and Evaluation of Quality of Life After Vulvar Cancer Surgery. Int J Gynecol Cancer. 22: 1081-1088, 2012.
Halaska MJ, Novackova M, Mala I, Mala I, Pluta M, Chmel R, Stankusova H, Robova H, Rob L. A Prospective Study of Postoperative Lymphedema After Surgery for Cervical Cancer. Int J Gynecol Can. 20: 900-904, 2010.
Berger J. Preclinical testing on insects predicts human haematotoxic potentials. Lab Anim. 43: 328-332, 2009.
Pohanka M, Kuca K, Kassa J. New performance of biosensor technology for Alzheimer's disease drugs: in vitro comparison of tacrine and 7-methoxytacrine. Neuroendocrinology Lett. 29: 755-758, 2008.
Vesela S, Kuca K, Jun D. Efficacy and dosing of antidotes applied to Daphnia intoxicated by nerve agent tabun. Environ Toxicol Pharmacol. 26: 283-289, 2008.
Vesela S, Kuca K, Jun D. Daphnia intoxicated by nerve agent tabun can be treated using human antidotes. Environ Toxicol Pharmacol. 25: 329-333, 2008.
Vesela S, Vijverberg J. Effect of body size on toxicity of zinc in neonates of four differently sized Daphnia species. Aquat Ecol. 41: 67-73, 2007.
|
