Obsah souboru
<?xml version="1.0" encoding="utf-8"?>
<!DOCTYPE Publisher PUBLIC "-//MetaPress//DTD MetaPress 2.0//EN" "http://public.metapress.com/dtd/MPRESS/MetaPressv2.dtd">
<Publisher>
<PublisherInfo>
<PublisherName>University of South Bohemia, Ceske Budejovice and Versita, Warsaw</PublisherName>
</PublisherInfo>
<Journal>
<JournalInfo JournalType="Journals">
<JournalPrintISSN>1214-021X</JournalPrintISSN>
<JournalElectronicISSN>1214-0287</JournalElectronicISSN>
<JournalTitle>Journal of Applied Biomedicine</JournalTitle>
<JournalCode>JAB</JournalCode>
<JournalID>121649</JournalID>
<JournalURL>http://versita.metapress.com/link.asp?target=journal&id=121649</JournalURL>
</JournalInfo>
<Volume>
<VolumeInfo>
<VolumeNumber>8</VolumeNumber>
</VolumeInfo>
<Issue>
<IssueInfo IssueType="Regular">
<IssueNumberBegin>2</IssueNumberBegin>
<IssueNumberEnd>2</IssueNumberEnd>
<IssueSupplement>0</IssueSupplement>
<IssuePartStart>0</IssuePartStart>
<IssuePartEnd>0</IssuePartEnd>
<IssueSequence>000008000220100601</IssueSequence>
<IssuePublicationDate>
<CoverDate Year="2010" Month="6" Day="1"/>
<CoverDisplay>Number 2 / June 2010</CoverDisplay>
</IssuePublicationDate>
<IssueID>LR323T458627</IssueID>
<IssueURL>http://versita.metapress.com/link.asp?target=issue&id=LR323T458627</IssueURL>
</IssueInfo>
<Article ArticleType="Original">
<ArticleInfo Free="No" ESM="No">
<ArticleDOI>10.2478/v10136-009-0008-6</ArticleDOI>
<ArticlePII>1NJ2NH18173J888J</ArticlePII>
<ArticleSequenceNumber>6</ArticleSequenceNumber>
<ArticleTitle Language="En">The effect of trimedoxime on acetylcholinesterase and on the cholinergic system of the rat bladder</ArticleTitle>
<ArticleFirstPage>87</ArticleFirstPage>
<ArticleLastPage>92</ArticleLastPage>
<ArticleHistory>
<RegistrationDate>20100524</RegistrationDate>
<ReceivedDate>20100524</ReceivedDate>
<Accepted>20100524</Accepted>
<OnlineDate>20100524</OnlineDate>
</ArticleHistory>
<FullTextFileName>1NJ2NH18173J888J.pdf</FullTextFileName>
<FullTextURL>http://versita.metapress.com/link.asp?target=contribution&id=1NJ2NH18173J888J</FullTextURL>
<Composite>2</Composite>
</ArticleInfo>
<ArticleHeader>
<AuthorGroup>
<Author AffiliationID="A1">
<GivenName>Ondřej</GivenName>
<Initials/>
<FamilyName>Soukup</FamilyName>
<Degrees/>
<Roles/>
</Author>
<Author AffiliationID="A3">
<GivenName>Ondřej</GivenName>
<Initials/>
<FamilyName>Holas</FamilyName>
<Degrees/>
<Roles/>
</Author>
<Author AffiliationID="A3">
<GivenName>Jiří</GivenName>
<Initials/>
<FamilyName>Binder</FamilyName>
<Degrees/>
<Roles/>
</Author>
<Author AffiliationID="A4">
<GivenName>Kumar</GivenName>
<Initials/>
<FamilyName>Killy</FamilyName>
<Degrees/>
<Roles/>
</Author>
<Author AffiliationID="A4">
<GivenName>Gunnar</GivenName>
<Initials/>
<FamilyName>Tobin</FamilyName>
<Degrees/>
<Roles/>
</Author>
<Author AffiliationID="A1 A2">
<GivenName>Daniel</GivenName>
<Initials/>
<FamilyName>Jun</FamilyName>
<Degrees/>
<Roles/>
</Author>
<Author AffiliationID="A1">
<GivenName>Josef</GivenName>
<Initials/>
<FamilyName>Fusek</FamilyName>
<Degrees/>
<Roles/>
</Author>
<Author AffiliationID="A1 A2 A5">
<GivenName>Kamil</GivenName>
<Initials/>
<FamilyName>Kuča</FamilyName>
<Degrees/>
<Roles/>
</Author>
<Affiliation AFFID="A1">
<OrgDivision/>
<OrgName>Department of Toxicology, University of Defence, Hradec Králové, Czech Republic</OrgName>
<OrgAddress/>
</Affiliation>
<Affiliation AFFID="A2">
<OrgDivision/>
<OrgName>Center of Advanced Studies, Faculty of Military Health Sciences, University of Defence, Hradec Králové, Czech Republic</OrgName>
<OrgAddress/>
</Affiliation>
<Affiliation AFFID="A3">
<OrgDivision/>
<OrgName>Department of Pharmaceutical Chemistry and Drug Control, Faculty of Pharmacy in Hradec Králové, Charles University in Prague, Hradec Králové, Czech Republic</OrgName>
<OrgAddress/>
</Affiliation>
<Affiliation AFFID="A4">
<OrgDivision/>
<OrgName>Institute of Neuroscience and Physiology, Department of Pharmacology, the Sahlgrenska Academy, Goteborg University, Sweden</OrgName>
<OrgAddress/>
</Affiliation>
<Affiliation AFFID="A5">
<OrgDivision/>
<OrgName>Department of Chemistry, Faculty of Sciences, J. E. Purkinje University, Ústí nad Labem, Czech Republic</OrgName>
<OrgAddress/>
</Affiliation>
</AuthorGroup>
<Abstract Language="En">Trimedoxime is a bisquaternary oxime that is widely used in the treatment of organophosphorous poisoning caused by tabun and paraoxon. We tested its affinity to acetylcholinesterase (AChE), its mechanism of interaction and effect on the cholinergic system of the rat bladder. The half maximal inhibitory concentration (IC<sub>50</sub>) of trimedoxime to recombinant AChE was found to be 82.0 mM ± 30.1 mM. This represents a weak inhibition. Its interaction with AChE seems to be very similar to obidoxime - one aromatic nucleus interacts with the peripheral anionic site and the other with the residues TYR337 and TYR341 inside the cavity. Also the oxime moiety is moving towards the catalytic triade ready for the reactivation of the inhibited AChE. In the organ bath experiment no significant effect of trimedoxime was observed on the contraction of the detrusor caused by the muscarinic agonist metacholine.</Abstract>
<KeywordGroup Language="En">
<Keyword>acetylcholinesterase</Keyword>
</KeywordGroup>
<KeywordGroup Language="En">
<Keyword>trimedoxime</Keyword>
</KeywordGroup>
<KeywordGroup Language="En">
<Keyword>antidote</Keyword>
</KeywordGroup>
<KeywordGroup Language="En">
<Keyword>muscarinic receptors</Keyword>
</KeywordGroup>
<KeywordGroup Language="En">
<Keyword>reactivation</Keyword>
</KeywordGroup>
<biblist>
<bib-other>
<bibtext seqNum="1"> Abrams P, Andersson KE, Buccafusco JJ, Chapple C, de Groat WC, Fryer AD, Kay G, Laties A, Nathanson NM, Pasricha PJ, Wein AJ: Muscarinic receptors: their distribution and function in body systems, and the implications for treating overactive bladder. <i>Br J Pharmacol</i> 148:565-578, 2006.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="2"> Antonijević B, Stojiljković MP.: Unequal efficacy of pyridinium oximes in acute organophosphate poisoning. <i>Clin Med Res</i> 5:71-82, 2006.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="3"> Bajgar J: Organophosphates/nerve agent poisoning: mechanism of action, diagnosis, prophylaxis, and treatment. <i>Adv Clin Chem</i> 38:151-216, 2004.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="4"> Cabal J, Kuča K, Kassa J: Specification of the structure of oximes able to reactivate tabun-inhibited acetylcholinesterase. <i>Basic Clin Pharmacol Toxicol</i> 95:81-86, 2004.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="5"> Collins SM, Crankshaw DJ: Dissociation of contraction and muscarinic receptor binding to isolated smooth muscle cells. <i>Am J Physiol</i> 251:G546-552, 1986.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="6"> Ekström F, Pang YP, Boman M, Artursson E, Akfur C, Börjegren S: Crystal structures of acetylcholinesterase in complex with HI-6, Ortho-7 and obidoxime: Structural basis for differences in the ability to reactivate tabun conjugates. <i>Biochem Pharmacol</i> 72:597-607, 2006.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="7"> Ellman GL, Courtney KD, Andres V, Featherstone RM: A new and rapid colorimetric determination of acetylcholinesterase activity. <i>Biochem Pharmacol</i> 7:88-95, 1961.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="8"> Giglio D, Aronsson P, Eriksson L, Tobin G: <i>In vitro</i> characterization of parasympathetic and sympathetic responses in cyclophosphamide-induced cystitis in the rat. <i>Basic Clin Pharmacol Toxicol</i> 100:96-108, 2007.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="9"> Giniatullin RA, Shabunova IA, Nikolskii EN, Bukharaeva EA: Reactivating and cholinolytic action of trimedoxime bromide at the neuromuscular-junction of warm-blooded animals. <i>Neurophysiology</i> 20:256-260, 1988.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="10"> Hamilton MG, Lundy PM: HI-6 therapy of soman and tabun poisoning in primates and rodents. <i>Arch Toxicol</i> 63:144-149, 1989.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="11"> Jun D, Musilová L, Kuča K, Kassa J, Bajgar J: Potency of several oximes to reactivate human acetylcholinesterase and butyrylcholinesterase inhibited by paraoxon <i>in vitro. Chem Biol Interact</i> 175:421-424, 2008.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="12"> Kassa J: Review of oximes in the antidotal treatment of poisoning by organophosphorus nerve agents. <i>J Toxicol Clin Toxicol</i> 40:803-816, 2002.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="13"> Kassa J, Kuča K, Cabal J: Comparison of the efficacy of currently available oximes against tabun in rats. <i>Biologia (Bratisl)</i> 60:77-79, 2005.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="14"> Kassa J, Kuča K, Cabal J, Paar M: A comparison of the efficacy of new asymmetric bispyridinium oximes (K027, K048) with currently available oximes against tabun by <i>in vivo</i> methods. <i>J Toxicol Environ Health A</i> 69:1875-1882, 2006.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="15"> Kassa J, Žďárová Karasová J, Tesařová S.: Evaluation of the neuroprotective efficacy of individual oxime (HI-6) and oxime mixtures (HI-6 + trimedoxime, HI-6 + K203) in tabun-poisoned rats. <i>J Appl Biomed</i> 7:189-199, 2009.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="16"> Kuča K, Jun D, Bajgar J: Currently used cholinesterase reactivators against nerve agent intoxication: Comparison of their effectivity <i>in vitro. Drug Chem Toxicol</i> 30:31-40, 2007.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="17"> Kuča K, Musílek K, Jun D, Pohanka M, Žďárová Karasová J, Novotný L, Musilová L.: Could oxime HI-6 really be considered as "broad-spectrum" antidote? <i>J Appl Biomed</i> 7:143-149, 2009.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="18"> Marrs TC: Organophosphate poisoning. <i>Pharmacol Ther</i> 58:51-66, 1993.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="19"> Morris GM, Goodsell DS, Halliday RS, Huey R, Hart WE, Belew RK, Olson AJ: Automated docking using a Lamarckian genetic algorithm and an empirical binding free energy function. <i>J Comput Chem</i> 19:1639-1662, 1998.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="20"> Ogura H, Kosasa T, Kuriya Y, Yamanishi Y: Comparison of inhibitory activities of donepezil and other cholinesterase inhibitors on acetylcholinesterase and butyrylcholinesterase <i>in vitro. Methods Find Exp Clin Pharmacol</i> 22:609-613, 2000.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="21"> Soukup O, Pohanka M, Tobin G, Jun D, Fusek J, Musílek K, Marek J, Kassa J, Kuča K: The effect of HI-6 on cholinesterases and on the cholinergic system of the rat bladder. <i>Neuro Endocrinol Lett</i> 29:759-762, 2008.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="22"> Tattersall JE: Ion channel blockade by oximes and recovery of diaphragm muscle from soman poisoning <i>in vitro. Br J Pharmacol</i> 108:1006-1015, 1993.</bibtext>
</bib-other>
<bib-other>
<bibtext seqNum="23"> Žďárová Karasová J, Bajgar J, Novotný L, Kuča K: Is a high dose of Huperzine A really suitable for pretreatment against high doses of soman? <i>J Appl Biomed</i> 7:93-99, 2009.</bibtext>
</bib-other>
</biblist>
</ArticleHeader>
</Article>
</Issue>
</Volume>
</Journal>
</Publisher>
soukup.xml