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Synthesis, in vitro screening and molecular docking of isoquinolinium-5-carbaldoximes as acetylcholinesterase and butyrylcholinesterase reactivators.

David Malinak, Rafael Dolezal, Vendula Hepnarova, Miroslava Hozova, Rudolf Andrys, Petr Bzonek, Veronika Racakova, Jan Korabecny, Lukas Gorecki, Eva Mezeiova, Miroslav Psotka, Daniel Jun, Kamil Kuca, Kamil Musilek,

The series of symmetrical and unsymmetrical isoquinolinium-5-carbaldoximes was designed and prepared for cholinesterase reactivation purposes. The novel compounds were evaluated for intrinsic acetylcholinesterase (AChE) or butyrylcholinesterase (BChE) inhibition, when the majority of novel compounds resulted with high inhibition of both enzymes and only weak inhibitors were selected for reactivation experiments ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):478-488]

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Evaluation of the paraoxonase-1 kinetic parameters of the lactonase activity by nonlinear fit of progress curves.

Marko Goličnik, Aljoša Bavec,

Although paraoxonase-1 (PON1) activity has been demonstrated to be a reliable biomarker of various diseases, clinical studies have been based only on relative comparison of specific enzyme activities, which capture differences mainly due to (usually unknown) PON1 concentration. Hence, the aim of this report is to present for the first ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):261-264]

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Effects of Brominated and Organophosphate Ester Flame Retardants on Male Reproduction.

Barbara F Hales, Bernard Robaire,

BACKGROUND:Environmental chemicals that interfere with the production and/or action of hormones may have adverse effects on male reproduction. This review focuses on the possible impact of exposure to flame retardant chemicals on male reproduction. Flame retardants are added to a wide variety of combustible materials to prevent fires from starting, ... Read more >>

Andrology (Andrology)
[2020, :]

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Effects of several organophosphates on hepatic cytochrome P450 activities in rats.

Rania H Abdou, Mohamed Elbadawy, Waleed F Khalil, Tatsuya Usui, Kazuaki Sasaki, Minoru Shimoda,

Four commonly used organophosphates (fenitrothion, dichlorvos, chlorpyrifos, and trichlorfon) were orally administered to male Sprague-Dawley rats for five days in order to explore their effects on the activities of liver cytochrome P450 (CYP). In addition, Michaelis-Menten kinetics of the metabolic reactions catalyzed by liver CYPs were analyzed following the addition ... Read more >>

J. Vet. Med. Sci. (The Journal of veterinary medical science)
[2020, :]

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A Retrospective Study of Acute Poisoning Cases and Their Management at Emergency Department of Dessie Referral Hospital, Northeast Ethiopia.

Abebe Getie, Yaschilal Muche Belayneh,

Background:Poisoning causes significant patient morbidity and mortality worldwide. It is a common reason for emergency department visits and hospitalizations. Acute poisoning needs immediate effective management to prevent patient mortality or sequela. This study was carried out to determine the pattern of acute poisoning cases and their management at the emergency ... Read more >>

Drug Healthc Patient Saf (Drug, healthcare and patient safety)
[2020, 12:41-48]

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Performance of pirimiphos-methyl based Indoor Residual Spraying on entomological parameters of malaria transmission in the pyrethroid resistance region of Koulikoro, Mali.

Moussa KEITA, Nafomon SOGOBA, Boïssé Traoré, Fousseyni Kané, Boubacar Coulibaly, Sekou Fantamady Traoré, Seydou Doumbia,

<title>Abstract</title> <p> Background: Following mosquito vector resistance to both pyrethroid and carbamates, organophosphate (pirimiphos-methyl) was used for the Indoor Residual Spray campaigns performed in 2015 to 2016 in the district of Koulikoro. In this context, we assessed the effect of IRS on malaria transmission by comparing entomological indices ... Read more >>

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Studies of Emission Processes of Polymer Additives into Water Using Quartz Crystal Microbalance-A Case Study on Organophosphate Esters.

Linhong Xiao, Ziye Zheng, Knut Irgum, Patrik L Andersson,

Plastic materials contain various additives, which can be released during the entire lifespan of plastics and pose a threat to the environment and human health. Despite our knowledge on leakage of additives from products, accurate and rapid approaches to study emission kinetics are largely lacking, in particular, methodologies that can ... Read more >>

Environ. Sci. Technol. (Environmental science & technology)
[2020, :]

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Trends in the Recent Patent Literature on Cholinesterase Reactivators (2016-2019).

Alexandre A de Castro, Letícia C Assis, Flávia V Soares, Kamil Kuca, Daniel A Polisel, Elaine F F da Cunha, Teodorico C Ramalho,

Acetylcholinesterase (AChE) is the key enzyme responsible for deactivating the ACh neurotransmitter. Irreversible or prolonged inhibition of AChE, therefore, elevates synaptic ACh leading to serious central and peripheral adverse effects which fall under the cholinergic syndrome spectra. To combat the toxic effects of some AChEI, such as organophosphorus (OP) nerve ... Read more >>

Biomolecules (Biomolecules)
[2020, 10(3):]

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Tracing the occurrence of organophosphate ester along the river flow path and textile wastewater treatment processes by using dissolved organic matters as an indicator.

Lingfang Fu, Liying Bin, Jiao Cui, Dieudonne Nyobe, Ping Li, Shaosong Huang, Fenglian Fu, Bing Tang,

Organophosphate esters (OPEs) are frequently detected in wastewater and receiving river, but their occurrence is hard to be quickly and effectively responded. In this study, the relevant OPEs and dissolved organic matters (DOMs) data were obtained from two textile wastewater treatment plants (WWTPs) with different processes and a 15 km stretch ... Read more >>

Sci. Total Environ. (The Science of the total environment)
[2020, 722:137895]

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The dominant malaria vector, Anopheles funestus from rural south-eastern Tanzania, is more strongly resistant to insecticides than Anopheles arabiensis

Polius Gerazi Pinda, Fredros Okumu, Claudia Eichenberger, Halfan Ngowo, Dickson Msaky, Said Abbasi, Japhet Kihonda, Hamis Bwanaly,

<title>Abstract</title> <p> Background: Long-lasting insecticide-treated nets (LLINs) and indoor residual spraying (IRS) have greatly reduced malaria transmission in sub-Saharan Africa, but are threatened by insecticide resistance in dominant malaria vectors. In south-eastern Tanzania, pyrethroid-resistant Anopheles funestus now transmit more than 80% of malaria infections even in villages where ... Read more >>

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Enhanced pulmonary systemic delivery of protein drugs via zwitterionic polymer conjugation.

Caroline Tsao, Zhefan Yuan, Peng Zhang, Erik Liu, Patrick McMullen, Kan Wu, Hsiang-Chieh Hung, Shaoyi Jiang,

Pulmonary delivery of protein drugs into the systemic circulation is highly desirable as the lung provides a large absorption surface area and a more favorable environment for biologics compared to other delivery routes. However, pulmonary systemic delivery of proteins presents several challenges such as poor protein stability and limited bioavailability, ... Read more >>

J Control Release (Journal of controlled release : official journal of the Controlled Release Society)
[2020, 322:170-176]

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The pro-convulsant effects of diazinon low dose in male rats under amygdala kindling.

Fatemeh Saberi, Farideh Bahrami, Mehdi Saberi, Mahdi Mashhadi Akbar Boojar,

Organophosphates can damage the brain in systemic intoxication. In this study, the effects of a minimum toxic dose (MTD) of diazinon (DZ) on amygdala afterdischarge threshold (ADT), kindling acquisition and kindled seizure parameters were evaluated. Intact male rats were stereotactically implanted with a tripolar and two monopolar electrodes in the ... Read more >>

Drug Chem Toxicol (Drug and chemical toxicology)
[2020, :1-8]

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Detection of organophosphorus pesticides with liquid crystals supported on the surface deposited with polyoxometalate-based acetylcholinesterase-responsive supramolecular spheres.

Lubin Qi, Wenli Wu, Qi Kang, Qiongzheng Hu, Li Yu,

Here, we demonstrate use of acetylcholinesterase (AChE)-responsive polyoxometalate (POM)/surfactant supramolecular spheres to build a liquid crystal (LC)-based sensing platform for detection of organophosphorus pesticides. The self-assembled spheres are composed of hybrid materials of a POM, sodium dodecatungstophosphate (PW12), and a surfactant, myristoylcholine (Myr). It displays dark appearance when the aqueous ... Read more >>

Food Chem (Food chemistry)
[2020, 320:126683]

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Prenatal Exposure to Organophosphate Flame Retardants and the Risk of Low Birth Weight: A Nested Case-Control Study in China.

Dan Luo, Wenyu Liu, Yun Tao, Limei Wang, Meng Yu, Liqin Hu, Aifen Zhou, Adrian Covaci, Wei Xia, Yuanyuan Li, Shunqing Xu, Surong Mei,

Organophosphate flame retardants (OPFRs), used as flame retardants and plasticizers, have been suggested to impair fetal growth and development in toxicological studies, but epidemiological data are extremely limited. This study was designed to explore whether prenatal exposure to OPFRs was associated with an increased risk of low birth weight (LBW) ... Read more >>

Environ. Sci. Technol. (Environmental science & technology)
[2020, 54(6):3375-3385]

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Assessment of human exposure to selected pesticides in Norway by wastewater analysis.

Nikolaos I Rousis, Emma Gracia-Lor, Malcolm J Reid, Jose Antonio Baz-Lomba, Yeonsuk Ryu, Ettore Zuccato, Kevin V Thomas, Sara Castiglioni,

Pesticides offer many benefits for humanity and agriculture, but at the same time pose a potential risk to human health because of their widespread use and high biological activity. Human biomonitoring (HBM) studies are the main tool to investigate human exposure to pesticides and other chemicals, but face limitations such ... Read more >>

Sci. Total Environ. (The Science of the total environment)
[2020, 723:138132]

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Development of a practical prediction scoring system for severe acute organophosphate poisoning.

Ning Dong, Junlan Liu, Zhihao Wang, Nan Gao, Li Pang, Jihong Xing,

Acute organophosphorus poisoning (AOPP) is a serious public health issue, especially in the rural areas. This study was designed to establish a scoring system to assess the risk of cases with severe AOPP. A retrospective cohort study was conducted at two independent hospitals. The derivation cohort included 444 patients with ... Read more >>

J Appl Toxicol (Journal of applied toxicology : JAT)
[2020, :]

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Investigation of the effects of dichlorvos poisoning on AMPK signaling pathway in chicken brain tissues.

Yanyu Xiao, Xibang Zheng, Guyue Li, Changming Zhou, Cong Wu, Zheng Xu, Guoliang Hu, Xiaoquan Guo, Lin Li, Huabin Cao, Vincent Latigo, Ping Liu,

Dichlorvos is a common crop insecticide widely used by people which causes extensive and serious environmental pollution. However, it has been shown that organophosphorus poisoning causes energy metabolism and neural disorders. The overall purpose of this study was to investigate the damage to brain tissue and the changes in AMPK ... Read more >>

Environ. Pollut. (Environmental pollution (Barking, Essex : 1987))
[2020, 261:114109]

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Compact reaction-module on a pad for scalable flow-production of organophosphates as drug scaffolds.

Se Jun Yim, Bandaru T Ramanjaneyulu, Shinde Vidyacharan, Yu Dong Yang, In Seok Kang, Dong-Pyo Kim,

Continuous pharmaceutical manufacturing receives intense attention as an alternative way to meet flexible market needs with the assurance of higher safety and quality control. Here, we report a compact reaction-module on a pad (CRP, 170 × 170 × 1.2 mm) for scale-up production of drug precursors in a continuous-flow. The ... Read more >>

Lab Chip (Lab on a chip)
[2020, 20(5):973-978]

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Glacial Melt Inputs of Organophosphate Ester Flame Retardants to the Largest High Arctic Lake.

Yuxin Sun, Amila O De Silva, Kyra A St Pierre, Derek C G Muir, Christine Spencer, Igor Lehnherr, John J MacInnis,

Organophosphate esters (OPEs) have been detected in the Arctic environment, but the influence of glacial melt on the environmental behavior of OPEs in recipient Arctic aquatic ecosystems is still unknown. In this study, water samples were collected from Lake Hazen (LH) and its tributaries to investigate the distribution of 14 ... Read more >>

Environ. Sci. Technol. (Environmental science & technology)
[2020, 54(5):2734-2743]

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Co-occurrence and distribution of organophosphate tri- and di-esters in indoor dust from different indoor environments in Guangzhou and their potential human health risk.

Qiongpu Hu, Liang Xu, Yi Liu, Xiangying Zeng, Zhiqiang Yu,

In this study, 45 indoor dust samples and four particulate samples from air-conditioner filters were collected from four different indoor environments in Guangzhou, China, and the concentration and composition of organophosphate tri-esters (OPEs) and organophosphate di-esters (Di-OPs) were determined. Eight of the 10 target OPEs were detected in indoor dust ... Read more >>

Environ. Pollut. (Environmental pollution (Barking, Essex : 1987))
[2020, 262:114311]

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Resistance status of Anopheles gambiae (s.l.) to four commonly used insecticides for malaria vector control in South-East Nigeria.

Okechukwu Chukwuekezie, Emmanuel Nwosu, Udoka Nwangwu, Festus Dogunro, Cosmas Onwude, Nneka Agashi, Ebuka Ezihe, Clementina Anioke, Stephen Anokwu, Emelda Eloy, Peter Attah, Francis Orizu, Sylvester Ewo, Angela Okoronkwo, Anumba Joseph, Ijeoma Ikeakor, Sylvester Haruna, Virgile Gnanguenon,

BACKGROUND:Progress made in the control of malaria vectors globally is largely due to the use of insecticides. However, success in the fight against malaria has slowed down or even stalled due to a host of factors including insecticide resistance. The greatest burden of the disease is felt in Africa, particularly ... Read more >>

Parasit Vectors (Parasites & vectors)
[2020, 13(1):152]

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Indoor residual spraying for malaria control in Sub-Saharan Africa 1997 to 2017; an adjusted retrospective analysis

Julie-Anne Tangena, Chantal M.J. Hendriks, Maria Devine, Meghan Tammaro, Anna Trett, Ignatius Williams, Adilson José DePina, Achamylesh Sisay, Ramandimbiarijaona Herizo, Hmooda Toto Kafy, Elizabeth Chizema, Allan Were, Jennifer Rozier, Michael Coleman, Catherine Moyes,

<title>Abstract</title> <p> Background: Indoor residual spraying (IRS) is a key tool for controlling and eliminating malaria by targeting vectors. To support the development of effective intervention strategies it is important to understand the impact of vector control tools on malaria incidence and on the spread of insecticide resistance. ... Read more >>

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Occurrence, phase distribution, and bioaccumulation of organophosphate esters (OPEs) in mariculture farms of the Beibu Gulf, China: A health risk assessment through seafood consumption.

Ruijie Zhang, Kefu Yu, An Li, Weibin Zeng, Tian Lin, Yinghui Wang,

As emerging pollutants, the occurrence and risks of organophosphate esters (OPEs) in mariculture farms should be concerned; however, information is limited. Beibu Gulf is one of the essential mariculture zones in China. This study aimed to investigate the occurrence of OPEs in mariculture farms of the Beibu Gulf, their phase ... Read more >>

Environ. Pollut. (Environmental pollution (Barking, Essex : 1987))
[2020, 263(Pt B):114426]

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Ecotoxicity of malathion pesticide and its genotoxic effects over the biomarker comet assay in Daphnia magna.

Luís F O Knapik, Wanessa Ramsdorf,

Malathion is a highly toxic organophosphate insecticide, being one of the most widely used in the world and is generally used for insect control in food production. Thus, ecotoxicological studies have been used to verify its toxic effects on aquatic organisms, such as Daphnia magna and biomarkers, as the comet ... Read more >>

Environ Monit Assess (Environmental monitoring and assessment)
[2020, 192(5):264]

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Evaluation of Resistance Management for the Oriental Fruit Moth (Lepidoptera: Tortricidae) to Insecticides in Brazilian Apple Orchards.

Lino Bittencourt Monteiro, Luis Gustavo Witt, Izonete Cristina Guiloski, Regis Silvori Silva Dos Santos, Helena C Silva de Assis,

The oriental fruit moth, Grapholita molesta (Busk, 1916), is one of the most important pests in apple orchards in southern Brazil. Chemical control is still the most commonly used strategy for pest control. The aim of this study was to determine the resistance evolution of seven South Brazilian populations to ... Read more >>

J. Econ. Entomol. (Journal of economic entomology)
[2020, :]

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