Insecticidal activity
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Bacillus thuringiensis (Bt) is known for its Cry and Vip3A pesticidal proteins with high selectivity to target pests. Here, we assessed the potential of a novel neotropical Bt strain (UFT038) against six lepidopteran pests, including two Cry-resistant populations of fall armyworm, Spodoptera frugiperda. We also sequenced and analyzed the genome of Bt UFT038 to identify genes involved in insecticidal activities or encoding other virulence factors. In toxicological bioassays, Bt UFT038 killed and inhibited the neonate growth in a concentration-dependent manner. Bt UFT038 and HD-1 were equally toxic against S. cosmioides, S. frugiperda (S_Bt and R_Cry1 + 2Ab populations), Helicoverpa zea, and H. armigera. However, larval growth inhibition results indicated that Bt UFT038 was more toxic than HD-1 to S. cosmioides, while HD-1 was more active against Chrysodeixis includens. The draft genome of Bt UFT038 showed the cry1Aa8, cry1Ac11, cry1Ia44, cry2Aa9, cry2Ab35, and vip3Af5 genes. Besides this, genes encoding the virulence factors (inhA, plcA, piplC, sph, and chi1-2) and toxins (alo, cytK, hlyIII, hblA-D, and nheA-C) were also identified. Collectively, our findings reveal the potential of the Bt UFT038 strain as a source of insecticidal genes against lepidopteran pests, including S. cosmioides and S. frugiperda.
- MeSH
- Bacillus thuringiensis * genetika metabolismus MeSH
- bakteriální proteiny genetika metabolismus MeSH
- biologická kontrola škůdců MeSH
- endotoxiny metabolismus MeSH
- faktory virulence metabolismus MeSH
- Glycine max MeSH
- hemolyziny genetika metabolismus farmakologie MeSH
- insekticidy * farmakologie metabolismus MeSH
- larva MeSH
- lidé MeSH
- můry * MeSH
- novorozenec MeSH
- Spodoptera metabolismus MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- novorozenec MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- MeSH
- antibakteriální látky aplikace a dávkování terapeutické užití MeSH
- dítě MeSH
- dostupnost zdravotnických služeb * MeSH
- infekční nemoci diagnóza farmakoterapie MeSH
- insekticidy toxicita MeSH
- ivermektin aplikace a dávkování terapeutické užití MeSH
- lidé MeSH
- mladiství MeSH
- otrava diagnóza etiologie terapie MeSH
- perinatální péče MeSH
- porod MeSH
- rozvojové země MeSH
- služby preventivní péče MeSH
- svrab diagnóza terapie MeSH
- vakcinace MeSH
- Check Tag
- dítě MeSH
- lidé MeSH
- mladiství MeSH
- mužské pohlaví MeSH
- Publikační typ
- kazuistiky MeSH
- Geografické názvy
- východní Afrika MeSH
Oxidative stress status, as a disruption of redox homeostasis, in the blood sera of Wistar rats caused by repeated application of selected acetylcholinesterase reactivators - asoxime, obidoxime, K027, K048, K074, and K075 were evaluated. Throughout this study, each oxime in a dose of 0.1 of LD50/kg im was given 2x/week for 4 weeks. Then, seven days after the last oximes' application, markers of lipid peroxidation (malondialdehyde, MDA), and protein oxidation (advanced oxidation protein products, AOPP), as well as the activity of antioxidant enzymes (catalase, CAT, superoxide dismutase, SOD, reduced glutathione, GSH, and oxidized glutathione, GSSG), were determined. Oxidative stress parameters, MDA and AOPP were significantly highest in the K048-, K074- and K075-treated groups (p < 0.001). The activity of CAT was significantly elevated in the obidoxime-treated group (p < 0.05), while treatment with K027, K048, and K074 induced high elevation in SOD levels (p < 0.01, p < 0.001). Interestingly, the activity of GSH in each oxime-treated group was significantly elevated. Unlike, treatment with obidoxime caused elevation in GSSG levels (p < 0.01). As a continuation of our previously published data, these results assure that applied oximes following subacute treatment ameliorated the oxidative status and further adverse systemic toxic effects in rats.
- MeSH
- antioxidancia metabolismus farmakologie MeSH
- biologické markery * krev MeSH
- glutathion * krev metabolismus MeSH
- katalasa metabolismus krev MeSH
- krysa rodu rattus MeSH
- malondialdehyd krev metabolismus MeSH
- oxidační stres * účinky léků MeSH
- oximy * farmakologie MeSH
- peroxidace lipidů účinky léků MeSH
- potkani Wistar * MeSH
- produkty pokročilé oxidace proteinů krev MeSH
- reaktivátory cholinesterasy farmakologie MeSH
- superoxiddismutasa metabolismus krev MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
In this review, the current progress in the research and development of butyrylcholinesterase (BChE) reactivators is summarised and the advantages or disadvantages of these reactivators are critically discussed. Organophosphorus compounds such as nerve agents (sarin, tabun, VX) or pesticides (chlorpyrifos, diazinon) cause irreversible inhibition of acetylcholinesterase (AChE) and BChE in the human body. While AChE inhibition can be life threatening due to cholinergic overstimulation and crisis, selective BChE inhibition has presumably no adverse effects. Because BChE is mostly found in plasma, its activity is important for the scavenging of organophosphates before they can reach AChE in the central nervous system. Therefore, this enzyme in combination with its reactivator can be used as a pseudo-catalytic scavenger of organophosphates. Three structural types of BChE reactivators were found, i.e. bisquaternary salts, monoquaternary salts and uncharged compounds. Although the reviewed reactivators have certain limitations, the promising candidates for BChE reactivation were found in each structural group.
- MeSH
- acetylcholinesterasa metabolismus chemie MeSH
- butyrylcholinesterasa * metabolismus chemie MeSH
- cholinesterasové inhibitory * chemie farmakologie chemická syntéza MeSH
- lidé MeSH
- molekulární struktura MeSH
- organofosforové sloučeniny * chemie farmakologie MeSH
- reaktivátory cholinesterasy farmakologie chemie chemická syntéza MeSH
- vztahy mezi strukturou a aktivitou MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
Solanum viarum, a perennial shrub, belongs to the family Solanaceae known for its therapeutic value worldwide. As a beneficial remedial plant, it is used for treating several disorders like dysentery, diabetes, inflammation, and respiratory disorders. Phytochemistry studies of this plant have shown the presence of steroidal glycoside alkaloids, including solasonine, solasodine, and solamargine. It also has flavonoids, saponins, minerals, and other substances. S. viarum extracts and compounds possess a variety of pharmacological effects, including antipyretic, antioxidant, antibacterial, insecticidal, analgesic, and anticancer activity. Most of the heavy metals accumulate in the aerial sections of the plant which is considered a potential phytoremediation, a highly effective method for the treatment of metal-polluted soils. We emphasize the forgoing outline of S. viarum, as well as its ethnomedicinal and ethnopharmacological applications, the chemistry of its secondary metabolites, and heavy metal toxicity. In addition to describing the antitumor activity of compounds and their mechanisms of action isolated from S. viarum, liabilities are also explained and illustrated, including any significant chemical or metabolic stability and toxicity risks. A comprehensive list of information was compiled from Science Direct, PubMed, Google Scholar, and Web of Science using different key phrases (traditional use, ethnomedicinal plants, western Himalaya, Himachal Pradesh, S viarum, and biological activity). According to the findings of this study, we hope that this review will inspire further studies along the drug discovery pathway of the chemicals extracted from the plant of S. viarum. Further, this review shows that ethnopharmacological information from ethnomedicinal plants can be a promising approach to drug discovery for cancer and diabetes.
- MeSH
- biodegradace * MeSH
- etnofarmakologie * MeSH
- fytonutrienty farmakologie izolace a purifikace MeSH
- fytoterapie MeSH
- lidé MeSH
- rostlinné extrakty * farmakologie chemie izolace a purifikace MeSH
- Solanum * chemie MeSH
- tradiční lékařství * metody MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
A-series agent A-234 belongs to a new generation of nerve agents. The poisoning of a former Russian spy Sergei Skripal and his daughter in Salisbury, England, in March 2018 led to the inclusion of A-234 and other A-series agents into the Chemical Weapons Convention. Even though five years have already passed, there is still very little information on its chemical properties, biological activities, and treatment options with established antidotes. In this article, we first assessed A-234 stability in neutral pH for subsequent experiments. Then, we determined its inhibitory potential towards human recombinant acetylcholinesterase (HssAChE; EC 3.1.1.7) and butyrylcholinesterase (HssBChE; EC 3.1.1.8), the ability of HI-6, obidoxime, pralidoxime, methoxime, and trimedoxime to reactivate inhibited cholinesterases (ChEs), its toxicity in rats and therapeutic effects of different antidotal approaches. Finally, we utilized molecular dynamics to explain our findings. The results of spontaneous A-234 hydrolysis showed a slow process with a reaction rate displaying a triphasic course during the first 72 h (the residual concentration 86.2%). A-234 was found to be a potent inhibitor of both human ChEs (HssAChE IC50 = 0.101 ± 0.003 μM and HssBChE IC50 = 0.036 ± 0.002 μM), whereas the five marketed oximes have negligible reactivation ability toward A-234-inhibited HssAChE and HssBChE. The acute toxicity of A-234 is comparable to that of VX and in the context of therapy, atropine and diazepam effectively mitigate A-234 lethality. Even though oxime administration may induce minor improvements, selected oximes (HI-6 and methoxime) do not reactivate ChEs in vivo. Molecular dynamics implies that all marketed oximes are weak nucleophiles, which may explain the failure to reactivate the A-234 phosphorus-serine oxygen bond characterized by low partial charge, in particular, HI-6 and trimedoxime oxime oxygen may not be able to effectively approach the A-234 phosphorus, while pralidoxime displayed low interaction energy. This study is the first to provide essential experimental preclinical data on the A-234 compound.
- MeSH
- acetylcholinesterasa MeSH
- antidota farmakologie MeSH
- butyrylcholinesterasa MeSH
- cholinesterasové inhibitory toxicita MeSH
- fosfor MeSH
- krysa rodu rattus MeSH
- kyslík MeSH
- lidé MeSH
- oximy farmakologie MeSH
- pralidoximové sloučeniny * MeSH
- pyridinové sloučeniny farmakologie MeSH
- reaktivátory cholinesterasy * farmakologie MeSH
- taurin analogy a deriváty MeSH
- trimedoxim farmakologie MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
Článek popisuje strom azadirachtu indickou, zvaný neem, a výrobky z něj. Tyto výrobky se používají v tradiční medicíně, jako agrochemikálie, zdroj biologicky aktivních látek, ale i jako součást potravy. Článek popisuje hlavní chemické složky, jmenovitě azadirachtin.
The article deals with the Azadirachta indica tree, called neem, which, as well as its products, is used in traditional medicine, agrochemicals, as a source of biologically active substances, but also as part of food. It describes the main chemical components, namely azadirachtin.
- MeSH
- agrochemikálie chemie MeSH
- Azadirachta * chemie fyziologie MeSH
- fytoterapie MeSH
- insekticidy MeSH
- léčivé rostliny chemie MeSH
- lidé MeSH
- Check Tag
- lidé MeSH
The article deals with the Azadirachta indica tree, called neem, which, as well as its products, is used in traditional medicine, agrochemicals, as a source of biologically active substances, but also as part of food. It describes the main chemical components, namely azadirachtin.
- MeSH
- agrochemikálie chemie MeSH
- Azadirachta * chemie fyziologie MeSH
- fytoterapie MeSH
- insekticidy MeSH
- léčivé rostliny chemie MeSH
- lidé MeSH
- Check Tag
- lidé MeSH
Pesticide residues are an important topic in many environmental studies, but little is known about the effects of pesticide residues of different ages on beneficial arthropods. Therefore, in this study the activity of residues of three different ages of several commonly used insecticides on the behaviour and mortality of European earwigs was evaluated in the laboratory and the effect of the insecticides was verified in the field. All residues of the biorational SpinTor® (spinosad), Radiant SC (spinetoram), and the conventional Steward® (indoxacarb) showed significantly faster mortality progression compared to the control in the laboratory. All the Steward® residues caused a significant wave of erratic behaviour as the earwigs went through a deep and relatively long moribund stage and resurrected. We verified the effects of SpinTor® and Steward® on changes in earwig abundance and their behaviour in the orchard. Earwigs abundance was significantly lower 16 days after application of biorational SpinTor® and conventional Steward® which had a significantly more pronounced and longer lasting effect. The earwig population stabilised by day 53 after the insecticide applications. Field applications of insecticides had no effect on earwig behaviour and sex ratio. Our results show that older residues have a negative effect on European earwigs equal to that of fresh residues, although their degradation should occur. It is interesting to note that biorational insecticides may not be safer than chemical insecticides.
- MeSH
- Auricularia MeSH
- hmyz MeSH
- insekticidy * toxicita MeSH
- predátorské chování MeSH
- rezidua pesticidů * toxicita MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
During production of γ-hexachlorocyclohexane (γ-HCH), thousands of tons of other isomers were synthesized as byproducts, and after dumping represent sources of contamination for the environment. Several microbes have the potential for aerobic and anaerobic degradation of HCHs, and zero-valent iron is an effective remediation agent for abiotic dechlorination of HCHs, whereas the combination of the processes has not yet been explored. In this study, a sequence of anoxic/oxic chemico-biological treatments for the degradation of HCHs in a real extremely contaminated soil (10-30 g/kg) was applied. Approximately 1500 kg of the soil was employed, and various combinations of reducing and oxygen-releasing chemicals were used for setting up the aerobic and anaerobic phases. The best results were obtained with mZVI/nZVI, grass cuttings, and oxygen-releasing compounds. In this case, 80 % removal of HCHs was achieved in 129 days, and 98 % degradation was achieved after 1106 days. The analysis of HCHs and their transformation products proved active degradation when slight accumulation of the transformation product during the anaerobic phase was followed by aerobic degradation. The results document that switching between aerobic and anaerobic phases, together with the addition of grass, also created suitable conditions for the biodegradation of HCHs and monochlorobenzene/benzene by microbes.
