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Methanol Toxicity

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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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Biological exploration of a novel 1,2,4-triazole-indole hybrid molecule as antifungal agent.

Fabrice Pagniez, Nicolas Lebouvier, Young Min Na, Isabelle Ourliac-Garnier, Carine Picot, Marc Le Borgne, Patrice Le Pape,

(2-(2,4-Dichlorophenyl)-3-(1H-indol-1-yl)-1-(1,2,4-1H-triazol-1-yl)propan-2-ol (8 g), a new 1,2,4-triazole-indole hybrid molecule, showed a broad-spectrum activity against Candida, particularly against low fluconazole-susceptible species. Its activity was higher than fluconazole and similar to voriconazole on C. glabrata (MIC90 = 0.25, 64 and 1 µg/mL, respectively), C. krusei (MIC90 = 0.125, 64 and 0.125 µg/mL, respectively) and C. albicans ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):398-403]

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Design, synthesis, in vitro inhibition and toxicological evaluation of human carbonic anhydrases I, II and IX inhibitors in 5-nitroimidazole series.

Ashok Aspatwar, Nanda Kumar Parvathaneni, Harlan Barker, Emilie Anduran, Claudiu T Supuran, Ludwig Dubois, Philippe Lambin, Seppo Parkkila, Jean-Yves Winum,

With the aim to obtain novel compounds possessing both strong affinity against human carbonic anhydrases and low toxicity, we synthesised novel thiourea and sulphonamide derivatives 3, 4 and 10, and studied their in vitro inhibitory properties against human CA I, CA II and CA IX. We also evaluated the toxicity of ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):109-117]

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Novel CDKs inhibitors for the treatment of solid tumour by simultaneously regulating the cell cycle and transcription control.

Xin Wang, Kaiyuan Deng, Cheng Wang, Yao Li, Tianqi Wang, Zhi Huang, Yakun Ma, Peiqing Sun, Yi Shi, Shengyong Yang, Yan Fan, Rong Xiang,

A novel series of cyclin-dependent kinases (CDKs) inhibitors, which play critical roles in the cell cycle control and regulation of cell transcription, were synthesised. A systematic study of enzymatic and cellular assays led to the identification of compound X22 with a nanomolar potency against CDK4 and CDK9 and potent antiproliferative ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):414-423]

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A potentiated cooperation of carbonic anhydrase IX and histone deacetylase inhibitors against cancer.

Jessica Ruzzolini, Anna Laurenzana, Elena Andreucci, Silvia Peppicelli, Francesca Bianchini, Fabrizio Carta, Claudiu T Supuran, Maria Novella Romanelli, Chiara Nediani, Lido Calorini,

The emergence of tumour recurrence and resistance limits the survival rate for most tumour-bearing patients. Only, combination therapies targeting pathways involved in the induction and in the maintenance of cancer growth and progression might potentially result in an enhanced therapeutic efficacy. Herein, we provided a prospective combination treatment that includes ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):391-397]

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Synthesis of novel, DNA binding heterocyclic dehydroabietylamine derivatives as potential antiproliferative and apoptosis-inducing agents.

Fengyi Zhao, Xu Sun, Wen Lu, Li Xu, Jiuzhou Shi, Shilong Yang, Mengyi Zhou, Fan Su, Feng Lin, Fuliang Cao,

Several dehydroabietylamine derivatives containing heterocyclic moieties such as thiophene and pyrazine ring were successfully synthesized. The antiproliferative activities of these thiophene-based Schiff-bases, thiophene amides, and pyrazine amides were investigated in vitro against Hela (cervix), MCF-7 (breast), A549 (lung), HepG2 (liver), and HUVEC (umbilical vein) cells by MTT assay. The toxicity of ... Read more >>

Drug Deliv (Drug delivery)
[2020, 27(1):216-227]

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Formation of inclusion complex of enrofloxacin with 2-hydroxypropyl-β-cyclodextrin.

Yili Ding, Yuchang Pang, Chamakura V N S Vara Prasad, Bingyun Wang,

Enrofloxacin, a third-generation fluoroquinolone, is a broad-spectrum antimicrobial drug against a lot of veterinary bacterial diseases. However, bactericidal activity of enrofloxacin is concentration-dependent and its poor aqueous solubility and bitter taste limit its development and application. Meanwhile, 2-hydroxypropyl-β-cyclodextrin (HP-β-CD), a widely used cyclodextrin analog, is a safe and an effective ... Read more >>

Drug Deliv (Drug delivery)
[2020, 27(1):334-343]

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Design, synthesis, in vitro and in vivo evaluation of benzylpiperidine-linked 1,3-dimethylbenzimidazolinones as cholinesterase inhibitors against Alzheimer's disease.

Jun Mo, Tingkai Chen, Hongyu Yang, Yan Guo, Qi Li, Yuting Qiao, Hongzhi Lin, Feng Feng, Wenyuan Liu, Yao Chen, Zongliang Liu, Haopeng Sun,

Cholinesterase inhibitor plays an important role in the treatment of patients with Alzheimer's disease (AD). Herein, we report the medicinal chemistry efforts leading to a new series of 1,3-dimethylbenzimidazolinone derivatives. Among the synthesised compounds, 15b and 15j showed submicromolar IC50 values (15b, eeAChE IC50 = 0.39 ± 0.11 µM; 15j, eqBChE IC50 = 0.16 ± 0.04 µM) towards acetylcholinesterase (AChE) ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):330-343]

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Antimalarial Activity of Aqueous and 80% Methanol Crude Seed Extracts and Solvent Fractions of Schinus molle Linnaeus (Anacardiaceae) in Plasmodium berghei-Infected Mice.

Getu Habte, Teshome Nedi, Solomon Assefa,

Background:Malaria is among the leading causes of mortality and morbidity. Moreover, the emergence of resistance to antimalarial drugs is a major problem in controlling the disease. This makes the development of novel antimalarial drugs a necessity. Medicinal plants are important sources in discovering antimalarial drugs. Schinus molle is claimed for ... Read more >>

J Trop Med (Journal of tropical medicine)
[2020, 2020:9473250]

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Toxic assessment, growth disrupting and neurotoxic effects of red seaweeds' botanicals against the dengue vector mosquito Aedes aegypti L.

Rabia Bibi, Rajput Muhammad Tariq, Munawwer Rasheed,

Application of synthetic pesticides over decades to control insects, pests, and disease vectors has resulted in negative impacts on environment and health. The current study assessed the toxicological effects of 12 botanicals obtained from 4 different red seaweeds against the dengue vector mosquito Aedes aegypti L. (Diptera: Culicidae). Four species ... Read more >>

Ecotoxicol. Environ. Saf. (Ecotoxicology and environmental safety)
[2020, 195:110451]

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Thioproline formation as a driver of formaldehyde toxicity in Escherichia coli

Jenelle Patterson, Hai He, Jacob Folz, Qiang Li, Mark Wilson, Oliver Fiehn, Steven Bruner, Arren Bar-Even, Andrew Hanson,

ABSTRACT Formaldehyde (HCHO) is a reactive carbonyl compound that formylates and cross-links proteins, DNA, and small molecules. It is of specific concern as a toxic intermediate in the design of engineered pathways involving methanol oxidation or formate reduction. The high interest in engineering these pathways is not, however, matched by ... Read more >>

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Comparing passive dosing and solvent spiking methods to determine the acute toxic effect of pentachlorophenol on Daphnia magna.

Hyun-Ah Kwon, Yoonah Jeong, Hyun Pyo Jeon, Sanghun Kim,

Pentachlorophenol (PCP) is a widespread and persistent hydrophobic organic pollutant in the environment despite its restricted public use. Risk assessment of such hydrophobic organic compounds (HOCs) is challenging because sorption and volatilization issues during toxicity test often lead to inconsistent exposure concentration. Considering the hydrophobicity of the PCP, in this ... Read more >>

Ecotoxicology (Ecotoxicology (London, England))
[2020, 29(3):286-294]

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Statins interfere with the attachment of S. cerevisiae mtDNA to the inner mitochondrial membrane.

Angela Cirigliano, Antonia Amelina, Beatrice Biferali, Alberto Macone, Chiara Mozzetta, Michele Maria Bianchi, Mattia Mori, Bruno Botta, Elah Pick, Rodolfo Negri, Teresa Rinaldi,

The 3-hydroxy-3-methylglutaryl-CoA reductase, a key enzyme of the mevalonate pathway for the synthesis of cholesterol in mammals (ergosterol in fungi), is inhibited by statins, a class of cholesterol lowering drugs. Indeed, statins are in a wide medical use, yet statins treatment could induce side effects as hepatotoxicity and myopathy in ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):129-137]

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Novel sulphonamides incorporating triazene moieties show powerful carbonic anhydrase I and II inhibitory properties.

Sinan Bilginer, Baris Gonder, Halise Inci Gul, Ruya Kaya, Ilhami Gulcin, Baris Anil, Claudiu T Supuran,

A series of compounds incorporating 3-(3-(2/3/4-substituted phenyl)triaz-1-en-1-yl) benzenesulfonamide moieties were synthesised and their chemical structure was confirmed by physico-chemical methods. Carbonic anhydrase (CA, EC 4.2.1.1) inhibitory effects of the compounds were evaluated against human isoforms hCA I and II. KI values of these sulphonamides were in the range of 21 ± 4-72 ± 2 nM ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):325-329]

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Data on the relationship between acetone, ethylene glycol, isopropanol, methanol, and propylene glycol serum/plasma concentrations and osmolal gaps in patients at an academic medical center.

Heather R Greene, Matthew D Krasowski,

Ingestion of toxic alcohols other than ethanol (ethylene glycol, methanol, isopropanol, and propylene glycol) can cause life-threatening complications including altered level of consciousness, respiratory depression, and organ damage from metabolites. Many hospitals lack the ability to specifically analyze these compounds using gas chromatography, gas chromatography/mass spectrometry, or by enzymatic assays ... Read more >>

Data Brief (Data in brief)
[2020, 29:105189]

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In Vivo Antimalarial Activity of 80% Methanol and Aqueous Bark Extracts of Terminalia brownii Fresen. (Combretaceae) against Plasmodium berghei in Mice.

Hana Biruk, Biruk Sentayehu, Yonatan Alebachew, Wondmagegn Tamiru, Abebe Ejigu, Solomon Assefa,

Background:Despite a substantial scientific progress over the past two decades, malaria continues to be a worldwide burden. Evergrowing resistance towards the currently available antimalarial drugs is a challenge to combat malaria. Medicinal plants are a promising source of new drugs to tackle this problem. Thus, the present study aimed at ... Read more >>

Biochem Res Int (Biochemistry research international)
[2020, 2020:9749410]

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Antimalarial Activity of Meriandra dianthera Leaf Extracts in Plasmodium berghei-Infected Mice.

Kalay Hagazy, Gereziher G Sibhat, Aman Karim, Gebretsadkan H Tekulu, Gomathi Periasamy, Mebrahtom G Hiben,

Objective:To evaluate the antimalarial effect of aqueous methanolic extract and solvent fractions of Meriandra dianthera leaves against Plasmodium berghei in mice model. Method:M. dianthera leaves were extracted with 80% methanol and dried. The dried crude extract was then defatted and further fractionated with chloroform, ethyl acetate, and butanol. Acute oral ... Read more >>

Evid Based Complement Alternat Med (Evidence-based complementary and alternative medicine : eCAM)
[2020, 2020:8980212]

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The in vitro cytotoxic, genotoxic and oxidative damage potentials of the oral artificial sweetener aspartame on cultured human blood cells.

Kenan Çadirci, Özlem Özdemir Tozlu, Hasan Türkez, Adil Mardinoğlu,

BACKGROUND/AIM:Aspartame (APM, L-aspartyl-L-phenylalanine methylester) is a low-calorie, non-saccharide artificial sweetener widely used in foods and beverages. When metabolized by the body, APM is broken down into aspartic acid, phenylalanine amino acids, and a third substance, methanol. Since the amino acid phenylalanine serves as a neurotransmitter building block affecting the brain, ... Read more >>

Turk J Med Sci (Turkish journal of medical sciences)
[2020, :]

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Acute and Subacute Toxicity Profiles of the Methanol Extract of Lycopersicon esculentum L. Leaves (Tomato), a Botanical with Promising In Vitro Anticancer Potential.

Gaëlle S Nguenang, Arsène S M Ntyam, Victor Kuete,

Lycopersicon esculentum (tomato) is a plant widely used in Africa like food and to solve many health problems. The methanol crude extract of tomato recently demonstrated a good antiproliferative effect on many human cancer cell lines. The aim of this research was to evaluate the acute toxicity and subacute oral ... Read more >>

Evid Based Complement Alternat Med (Evidence-based Complementary and Alternative Medicine : eCAM)
[2020, 2020:8935897]

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Iron as electron donor for denitrification: The efficiency, toxicity and mechanism.

Ru Wang, Shao-Yi Xu, Meng Zhang, Abbas Ghulam, Chen-Lin Dai, Ping Zheng,

For the treatment of low C/N wastewaters, methanol or acetate is usually dosed as electron donor for denitrification but such organics makes the process costly. To decrease the cost, iron which is the fourth most abundant element in lithosphere is suggested as the substitution of methanol and acetate. The peak ... Read more >>

Ecotoxicol. Environ. Saf. (Ecotoxicology and environmental safety)
[2020, 194:110343]

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Influence of Polymer Charge on the Localization and Dark- and Photo-Induced Toxicity of a Potential Type I Photosensitizer in Cancer Cell Models.

Mikael Lindgren, Odrun A Gederaas, Monica Siksjø, Tom A Hansen, Lena Chen, Bastien Mettra, Chantal Andraud, Cyrille Monnereau,

A current trend within photo-dynamic therapy (PDT) is the development of molecular systems targeting hypoxic tumors. Thus, type I PDT sensitizers could here overcome traditional type II molecular systems that rely on the photo-initiated production of toxic singlet oxygen. Here, we investigate the cell localization properties and toxicity of two ... Read more >>

Molecules (Molecules (Basel, Switzerland))
[2020, 25(5):]

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Anti-inflammatory effect of Acalypha australis L. via suppression of NF-κB signaling in LPS-stimulated RAW 264.7 macrophages and LPS-induced septic mice.

Hyo-Jung Kim, Hae-In Joe, Zhiyun Zhang, Sang Woo Lee, Kyou-Young Lee, Yoon-Bum Kook, Hyo-Jin An,

We evaluated the anti-inflammatory activity of methanol extracts of Chinese medicinal plants from Beijing and determined which extract was the most effective. We found the methanol extract of Acalypha australis L. (AAL) to be the most effective. AAL has been used for clearing heat, toxic material, and hemostasia in Chinese ... Read more >>

Mol. Immunol. (Molecular immunology)
[2020, 119:123-131]

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Educational Case: Ethylene Glycol Poisoning.

Matthew D Krasowski,

The following fictional case is intended as a learning tool within the Pathology Competencies for Medical Education (PCME), a set of national standards for teaching pathology. These are divided into three basic competencies: Disease Mechanisms and Processes, Organ System Pathology, and Diagnostic Medicine and Therapeutic Pathology. For additional information, and ... Read more >>

Acad Pathol (Academic pathology)
[2020, 7:2374289519900330]

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Effect of Ozone and Electron Beam Irradiation on Degradation of Zearalenone and Ochratoxin A.

Kai Yang, Ke Li, Lihong Pan, Xiaohu Luo, Jiali Xing, Jing Wang, Li Wang, Ren Wang, Yuheng Zhai, Zhengxing Chen,

Zearalenone (ZEN) and ochratoxin A (OTA) are key concerns of the food industry because of their toxicity and pollution scope. This study investigated the effects of ozone and electron beam irradiation (EBI) on the degradation of ZEN and OTA. Results demonstrated that 2 mL of 50 μg/mL ZEN was completely ... Read more >>

Toxins (Basel) (Toxins)
[2020, 12(2):]

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Phytochemical investigation, in vitro and in vivo antioxidant properties of aqueous and organic extracts of toxic plant: Atractylis gummifera L.

Khadija Bouabid, Fatima Lamchouri, Hamid Toufik, My El Abbes Faouzi,

ETHNOPHARMACOLOGICAL RELEVANCE:Atractylis gummifera is a toxic plant widely used in Mediterranean traditional medicine against colds, dizziness, and headaches, as an antisyphilitic, against boils, as a purgative, emetic and deworming. All studies reported on this plant have been carried out either on the plant and its traditional uses, or on cases ... Read more >>

J Ethnopharmacol (Journal of ethnopharmacology)
[2020, 253:112640]

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