HPLC Analysis of HI‐6 Dichloride and Dimethanesulfonate—Antidotes against Nerve Agents and Organophosphorus Pesticides

2007 ◽  
Vol 40 (14) ◽  
pp. 2783-2787 ◽  
Author(s):  
Daniel Jun ◽  
Kamil Kuca ◽  
Petr Stodulka ◽  
Vit Koleckar ◽  
Bohuslav Dolezal ◽  
...  
Keyword(s):  
Hplc Analysis ◽  
Organophosphorus Pesticides ◽  
Nerve Agents ◽  
Hi 6

scholarly journals Evaluation of Potency of Known Oximes (Pralidoxime, Trimedoxime, HI-6, Methoxime, Obidoxime) to in vitro Reactivate Acetylcholinesterase Inhibited by Pesticides (Chlorpyrifos and Methylchlorpyrifos and Nerve Agent (Russian VX)

2007 ◽  
Vol 50 (3) ◽  
pp. 203-206 ◽  
Author(s):  
Kamil Musílek ◽  
Kamil Kuča ◽  
Daniel Jun
Keyword(s):  
Organophosphorus Pesticides ◽  
Nerve Agents ◽  
Nerve Agent ◽  
Hi 6 ◽  
Acetylcholinesterase Reactivators

Nerve agents and pesticides belong to the group of organophosphates. They are able to inhibit irreversibly the enzyme acetylcholinesterase (AChE). Acetylcholinesterase reactivators were designed for the treatment of nerve agent intoxications. Their potency to reactivate pesticide-inhibited AChE was many times evaluated. In this study, five commonly used AChE reactivators (pralidoxime, methoxime, HI-6, obidoxime, trimedoxime) for the reactivation of AChE inhibited by two pesticides (chlorpyrifos and methylchlorpyrifos) were used. Russian VX (nerve agent) as a member of nerve agents’ family was taken for comparison. Obtained results show that oximes developed against nerve agent intoxication are less effective for intoxication with organophosphorus pesticides. Especially, methylchlorpyrifos-inhibited AChE was found to be poorly reactivated by the compounds used.

scholarly journals Comparative determination of the efficacy of bispyridinium oximes in paraoxon poisoning / Usporedno određivanje učinkovitosti bispiridinijevih oksima pri trovanju paraoksonom

2015 ◽  
Vol 66 (2) ◽  
pp. 129-134 ◽  
Author(s):  
Suzana Žunec ◽  
Božica Radić ◽  
Kamil Kuča ◽  
Kamil Musilek ◽  
Ana Lucić Vrdoljak
Keyword(s):  
Therapeutic Efficacy ◽  
Standard Therapy ◽  
Organophosphorus Compounds ◽  
Nerve Agents ◽  
Therapeutic Efficiency ◽  
Hi 6 ◽  
Comparative Determination

Abstract The inability of standard therapy to provide adequate protection against poisoning by organophosphorus compounds (pesticides and nerve agents) motivated us to search for new, more effective oximes. We investigated the pharmacotoxicological properties of six experimental K-oximes (K027, K033, K048, K074, K075, and K203) in vivo. The therapeutic efficacy of K-oximes (at doses of 5 or 25 % of their LD50) combined with atropine was assessed in paraoxon-poisoned mice and compared with conventionally used oximes HI-6 and TMB-4. The bisoxime K074 was the most toxic (LD50=21.4 mg kg-1) to mice, while monoxime K027 was the least toxic (LD50=672.8 mg kg-1). With the exception of K033, all of the tested K-oximes showed better therapeutic efficiency than HI-6 and TMB-4. K027 and K048 stood out by demonstrating low acute toxicities and ensuring protective indices ranging from 60.0 to 100.0 LD50 of paraoxon. Taking into account that these two oximes showed a similar therapeutic efficacy regardless of the applied doses, our results suggest that K027 and K048 could be antidotes for paraoxon intoxication.

scholarly journals Catalytic Degradation of Nerve Agents

Catalysts ◽  
2020 ◽  
Vol 10 (8) ◽  
pp. 881
Author(s):  
Agatino Zammataro ◽  
Rossella Santonocito ◽  
Andrea Pappalardo ◽  
Giuseppe Trusso Sfrazzetto
Keyword(s):  
World War Ii ◽  
Acute Toxicity ◽  
Organophosphorus Compounds ◽  
Organophosphorus Pesticides ◽  
Lethal Effect ◽  
Nerve Agents ◽  
Catalytic Degradation ◽  
World War ◽  
Degradation Reactions ◽  
Chemical Hydrolysis

Nerve agents (NAs) are a group of highly toxic organophosphorus compounds developed before World War II. They are related to organophosphorus pesticides, although they have much higher human acute toxicity than commonly used pesticides. After the detection of the presence of NAs, the critical step is the fast decontamination of the environment in order to avoid the lethal effect of these organophosphorus compounds on exposed humans. This review collects the catalytic degradation reactions of NAs, in particular focusing our attention on chemical hydrolysis. These reactions are catalyzed by different catalyst categories (metal-based, polymeric, heterogeneous, enzymatic and MOFs), all of them described in this review.

scholarly journals Enzymatic Degradation of Organophosphorus Pesticides and Nerve Agents by EC: 3.1.8.2

Catalysts ◽  
2020 ◽  
Vol 10 (12) ◽  
pp. 1365
Author(s):  
Marek Matula ◽  
Tomas Kucera ◽  
Ondrej Soukup ◽  
Jaroslav Pejchal
Keyword(s):  
Catalytic Activity ◽  
Organophosphorus Compounds ◽  
Organophosphorus Pesticides ◽  
Chemical Warfare Agents ◽  
Enzyme Commission Number ◽  
Nerve Agents ◽  
Organophosphorus Acid Anhydrolase ◽  
Warfare Agents ◽  
Heavy Burden ◽  
Medical Countermeasures

The organophosphorus substances, including pesticides and nerve agents (NAs), represent highly toxic compounds. Standard decontamination procedures place a heavy burden on the environment. Given their continued utilization or existence, considerable efforts are being made to develop environmentally friendly methods of decontamination and medical countermeasures against their intoxication. Enzymes can offer both environmental and medical applications. One of the most promising enzymes cleaving organophosphorus compounds is the enzyme with enzyme commission number (EC): 3.1.8.2, called diisopropyl fluorophosphatase (DFPase) or organophosphorus acid anhydrolase from Loligo Vulgaris or Alteromonas sp. JD6.5, respectively. Structure, mechanisms of action and substrate profiles are described for both enzymes. Wild-type (WT) enzymes have a catalytic activity against organophosphorus compounds, including G-type nerve agents. Their stereochemical preference aims their activity towards less toxic enantiomers of the chiral phosphorus center found in most chemical warfare agents. Site-direct mutagenesis has systematically improved the active site of the enzyme. These efforts have resulted in the improvement of catalytic activity and have led to the identification of variants that are more effective at detoxifying both G-type and V-type nerve agents. Some of these variants have become part of commercially available decontamination mixtures.

Diagnoses of Pathological States Based on Acetylcholinesterase and Butyrylcholinesterase

2020 ◽  
Vol 27 (18) ◽  
pp. 2994-3011 ◽  
Author(s):  
Miroslav Pohanka
Keyword(s):  
Oxidative Stress ◽  
Secondary Metabolites ◽  
Myasthenia Gravis ◽  
Neurodegenerative Disorders ◽  
Crucial Role ◽  
Biochemical Markers ◽  
Organophosphorus Pesticides ◽  
Nerve Agents ◽  
Specific Function

Two cholinesterases exist: Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). While AChE plays a crucial role in neurotransmissions, BChE has no specific function apart from the detoxification of some drugs and secondary metabolites from plants. Thus, both AChE and BChE can serve as biochemical markers of various pathologies. Poisoning by nerve agents like sarin, soman, tabun, VX, novichok and overdosing by drugs used in some neurodegenerative disorders like Alzheimer´s disease and myasthenia gravis, as well as poisoning by organophosphorus pesticides are relevant to this issue. But it appears that changes in these enzymes take place in other processes including oxidative stress, inflammation, some types of cancer and genetically conditioned diseases. In this review, the cholinesterases are introduced, the mechanism of inhibitors action is explained and the relations between the cholinesterases and pathologies are explained.

Prophylaxis and Post-exposure Treatment of Intoxications Caused by Nerve Agents and Organophosphorus Pesticides

2013 ◽  
Vol 13 (14) ◽  
pp. 2102-2115 ◽  
Author(s):  
Kamil Kuca ◽  
Daniel Jun ◽  
Kamil Musilek ◽  
Miroslav Pohanka ◽  
Jana Karasova ◽  
...  
Keyword(s):  
Organophosphorus Pesticides ◽  
Nerve Agents ◽  
Exposure Treatment ◽  
Post Exposure

Oxime K033-Reactivation Activity of Cholinesterases Inhibited by Various Nerve Agents and Organophosphorus Pesticides

2018 ◽  
Vol 15 (11) ◽  
pp. 1124-1130 ◽  
Author(s):  
Kamil Kuca ◽  
Kamil Musilek ◽  
Daniel Jun ◽  
Jaroslav Pejchal ◽  
Ondrej Krejcar ◽  
...  
Keyword(s):  
Organophosphorus Pesticides ◽  
Nerve Agents
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