8,703 results match your criteria additive inhibition

Untargeted and targeted analysis of sarin poisoning biomarkers in rat urine by liquid chromatography and tandem mass spectrometry.

Anal Bioanal Chem 2021 Sep 21. Epub 2021 Sep 21.

Department of Chemistry, Lomonosov Moscow State University, 119991, Moscow, Russia.

Chemical warfare agents continue to pose a real threat to humanity, despite their prohibition under the Chemical Weapons Convention. Sarin is one of the most toxic and lethal representatives of nerve agents. The methodology for the targeted analysis of known sarin metabolites has reached great heights, but little attention has been paid to the untargeted analysis of biological samples of victims exposed to this deadly poisonous substance. Read More

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September 2021

Dual BET/HDAC inhibition to relieve neuropathic pain: recent advances, perspectives, and future opportunities.

Pharmacol Res 2021 Sep 18:105901. Epub 2021 Sep 18.

Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy; Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Section of Pharmacology and Toxicology, University of Florence, Viale G. Pieraccini 6, 50139 Florence, Italy. Electronic address:

Despite the intense research on developing new therapies for neuropathic pain states, available treatments have limited efficacy and unfavorable safety profiles. Epigenetic alterations have a great influence on the development of cancer and neurological diseases, as well as neuropathic pain. Histone acetylation has prevailed as one of the well investigated epigenetic modifications in these diseases. Read More

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September 2021

Anti-Vibrio dibutyl phthalate from marine-derived Streptomyces sp. S073.

Res Vet Sci 2021 Sep 8;140:198-202. Epub 2021 Sep 8.

Department of Ecology, Institute of Hydrobiology, School of Life Science and Technology, Key Laboratory of Eutrophication and Red Tide Prevention of Guangdong Higher Education Institutes, Engineering Research Center of Tropical and Subtropical Aquatic Ecological Engineering, Ministry of Education, Jinan University, Guangzhou 510632, PR China. Electronic address:

Marine Streptomyces S073 was previously shown to have strong anti-Vibrio activity, and its antibacterial mechanism was proposed to be associated with siderophore-mediated iron competition and other antagonistic agents. In this study, anti-Vibrio compounds produced by S073 were isolated by bioassay-guided fractionation using column chromatography and HPLC, and the target compound in the most active fraction was identified as dibutyl phthalate (DBP) by various spectroscopic analyses, including EI-MS, H NMR and C NMR. The DBP-producing capacity of S073 was 2. Read More

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September 2021

An assessment of the growth inhibition profiles of L. extracts against and spp.

J Tradit Complement Med 2021 Sep 1;11(5):457-465. Epub 2021 Apr 1.

School of Environment and Science, Nathan Campus, Griffith University, Australia.

Staphylococcal and streptococcal species trigger a wide variety of infections involving epithelial tissues. Virginian witch hazel (WH; L.; family: Hamamelidaceae) is a plant that has been used traditionally by Native Americans to treat a variety of skin conditions. Read More

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September 2021

Regorafenib enhances anti-PD1 immunotherapy efficacy in murine colorectal cancers and their combination prevents tumor regrowth.

J Exp Clin Cancer Res 2021 Sep 13;40(1):288. Epub 2021 Sep 13.

Institute for Experimental Molecular Imaging, Medical Faculty, RWTH Aachen University, Aachen, Germany.

Background: Patients with advanced colorectal cancer (CRC) have a poor prognosis. Combinations of immunotherapies and anti-angiogenic agents are currently being evaluated in clinical trials. In this study, the multikinase inhibitor regorafenib (REG) was combined with an anti-programmed cell death protein 1 (aPD1) antibody in syngeneic murine microsatellite-stable (MSS) CT26 and hypermutated MC38 colon cancer models to gain mechanistic insights into potential drug synergism. Read More

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September 2021

REV1-Polζ maintains the viability of homologous recombination-deficient cancer cells through mutagenic repair of PRIMPOL-dependent ssDNA gaps.

Mol Cell 2021 Sep 7. Epub 2021 Sep 7.

Department of Genetics and Development, Herbert Irving Comprehensive Cancer Center, Columbia University Irving Medical Center, New York, NY, USA. Electronic address:

BRCA1/2 mutant tumor cells display an elevated mutation burden, the etiology of which remains unclear. Here, we report that these cells accumulate ssDNA gaps and spontaneous mutations during unperturbed DNA replication due to repriming by the DNA primase-polymerase PRIMPOL. Gap accumulation requires the DNA glycosylase SMUG1 and is exacerbated by depletion of the translesion synthesis (TLS) factor RAD18 or inhibition of the error-prone TLS polymerase complex REV1-Polζ by the small molecule JH-RE-06. Read More

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September 2021

PIM Kinases in Multiple Myeloma.

Cancers (Basel) 2021 Aug 26;13(17). Epub 2021 Aug 26.

Division of Hematologic Malignancies and Cellular Therapy, Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA.

Multiple myeloma (MM) remains an incurable disease and novel therapeutic agents/approaches are urgently needed. The PIM (Proviral insertion in murine malignancies) serine/threonine kinases have 3 isoforms: PIM1, PIM2, and PIM3. PIM kinases are engaged with an expansive scope of biological activities including cell growth, apoptosis, drug resistance, and immune response. Read More

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Silver-sepiolite (Ag-Sep) hybrid reinforced active gelatin/date waste extract (DSWE) blend composite films for food packaging application.

Food Chem 2021 Aug 30;369:130983. Epub 2021 Aug 30.

Department of Chemical Engineering, SAN Campus, Khalifa University, Abu Dhabi, United Arab Emirates. Electronic address:

In this study, date syrup waste extract (DSWE) (15 wt%) and different content of silver doped sepiolite hybrid (Ag-Sep, 0.25-3 wt%) were incorporated into gelatin matrix to develop a series of active composite packaging films. Incorporating 2 wt% of Ag-Sep increased the modulus of blend film by 98% compared to unmodified gelatin/DSWE blend film. Read More

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Cinnamic acid inhibits cell viability, invasion, and glycolysis in primary endometrial stromal cells by suppressing NF-κB-induced transcription of PKM2.

Biosci Rep 2021 Sep 9. Epub 2021 Sep 9.

Gynecology of Traditional Chinese Medicine, Shanghai Municipal Hospital of Traditional Chinese Medicine Affiliated to Shanghai TCM University, Shanghai, China.

Background:   Endometriosis is a painful disorder characterized by the growth of endometrial tissue outside the uterine cavity. Here, we investigated the effects of the cinnamic acid isolated from the Chinese medicinal plant Cinnamomum cassia Presl on primary endometrial stromal cells.

Methods:   Immunohistochemistry was used to examine protein expression and cell purity. Read More

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September 2021

Role of medicinal plants from North Western Himalayas as an efflux pump inhibitor against MDR AcrAB-TolC Salmonella enterica serovar typhimurium: In vitro and In silico studies.

J Ethnopharmacol 2021 Sep 4:114589. Epub 2021 Sep 4.

Faculty of Applied Sciences and Biotechnology, Shoolini University of Biotechnology and Management Sciences, Bajhol, PO Sultanpur, District Solan, 173229, Himachal Pradesh, India. Electronic address:

Ethnopharmacological Relevance: Zingiber officinale Roscoe has been utilized traditionally to cure various diseases like cold, cough, diarrhoea, nausea, asthma, vomiting, toothache, stomach upset, respiratory disorders, joint pain, and throat infection. It is also consumed as spices and ginger tea.

Aim Of The Study: The current study was aimed to identify the phytocompounds of traditional medicinal plants of North-Western Himalaya that could inhibit the AcrAB-TolC efflux pump activity of Salmonella typhimurium and become sensitive to antibiotic killing at reduced dosage. Read More

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September 2021

Endochin-like quinolones (ELQs) and bumped kinase inhibitors (BKIs): Synergistic and additive effects of combined treatments against Neospora caninum infection in vitro and in vivo.

Int J Parasitol Drugs Drug Resist 2021 Aug 28;17:92-106. Epub 2021 Aug 28.

Institute of Parasitology, Vetsuisse Faculty, University of Bern, Switzerland. Electronic address:

The apicomplexan parasite Neospora caninum is an important causative agent of congenital neosporosis, resulting in abortion, birth of weak offspring and neuromuscular disorders in cattle, sheep, and many other species. Among several compound classes that are currently being developed, two have been reported to limit the effects of congenital neosporosis: (i) bumped kinase inhibitors (BKIs) target calcium dependent protein kinase 1 (CDPK1), an enzyme that is encoded by an apicoplast-derived gene and found only in apicomplexans and plants. CDPK1 is essential for host cell invasion and egress; (ii) endochin-like quinolones (ELQs) are inhibitors of the cytochrome bc complex of the mitochondrial electron transport chain and thus inhibit oxidative phosphorylation. Read More

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Identification of coagulation factor IX variants with enhanced activity through ancestral sequence reconstruction.

Blood Adv 2021 09;5(17):3333-3343

Cell and Gene Therapy Program, Department of Pediatrics, Aflac Cancer and Blood Disorders Center, Children's Healthcare of Atlanta and Emory University, Atlanta, GA.

Orthologous proteins contain sequence disparity guided by natural selection. In certain cases, species-specific protein functionality predicts pharmacological enhancement, such as greater specific activity or stability. However, immunological barriers generally preclude use of nonhuman proteins as therapeutics, and difficulty exists in the identification of individual sequence determinants among the overall sequence disparity. Read More

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September 2021

Response to combined peptide receptor radionuclide therapy and checkpoint immunotherapy with ipilimumab plus nivolumab in metastatic Merkel cell carcinoma.

J Nucl Med 2021 Sep 2. Epub 2021 Sep 2.

University Hospital Essen, Germany.

Merkel cell carcinoma (MCC) is a highly aggressive neuroendocrine cancer of the skin. For patients who are refractory to immune checkpoint inhibition (ICI), treatment options are limited. Few cases of MCCs with high somatostatin receptor (SSTR) expression were reported to show responses upon SSTR-directed peptide receptor radionuclide therapy (PRRT). Read More

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September 2021

Ferric ammonium citrate (FAC)-induced inhibition of osteoblast proliferation/differentiation and its reversal by soybean-derived peptides (SDP).

Food Chem Toxicol 2021 Oct 28;156:112527. Epub 2021 Aug 28.

College of Food Science and Engineering/Collaborative Innovation Center for Modern Grain Circulation and Safety/Key Laboratory of Grains and Oils Quality Control and Processing, Nanjing University of Finance and Economics, Nanjing, 210023, China. Electronic address:

Ferric citrate has been used to treat hyperphosphatemia, a prevalent symptom in patients with chronic kidney disease while ferric ammonium citrate (FAC), a more dissolvable format, is widely used as food additive. However, excess iron is associated with osteoporosis. Dietary soybean products have been shown to prevent the progression of osteoporosis. Read More

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October 2021

Targeting ADCC: A different approach to HER2 breast cancer in the immunotherapy era.

Breast 2021 Aug 19;60:15-25. Epub 2021 Aug 19.

Centro de Investigaciones Oncológicas, Fundación Cáncer, Ciudad Autónoma de Buenos Aires, Argentina.

The clinical outcome of patients with human epidermal growth factor receptor 2 (HER2) amplified breast carcinoma (BC) has improved with the development of anti-HER2 targeted therapies. However, patients can experience disease recurrence after curative intent and disease progression in the metastatic setting. In the current era of evolving immunotherapy agents, the understanding of the immune response against HER2 tumor cells developed by anti-HER2 antibodies (Abs) is rapidly evolving. Read More

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Assessing the Single and Combined Toxicity of the Bioinsecticide Spear and Cry3Bb1 Protein Against Susceptible and Resistant Western Corn Rootworm Larvae (Coleoptera: Chrysomelidae).

J Econ Entomol 2021 Aug 28. Epub 2021 Aug 28.

Plant Genetics Research Unit, USDA/ARS, Columbia, MO, USA.

The western corn rootworm (WCR), Diabrotica virgifera virgifera LeConte (Coleoptera: Chrysomelidae), poses a serious threat to maize (Zea mays L.) growers in the U.S. Read More

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A Fully Human Monoclonal Antibody Targeting cKIT Is a Potent Inhibitor of Pathological Choroidal Neovascularization in Mice.

Pharmaceutics 2021 Aug 20;13(8). Epub 2021 Aug 20.

Department of Global Innovative Drug, Graduate School of Chung-Ang University, Seoul 06974, Korea.

Stem cell factor (SCF) and its receptor, cKIT, are novel regulators of pathological neovascularization in the eye, which suggests that inhibition of SCF/cKIT signaling may be a novel pharmacological strategy for treating neovascular age-related macular degeneration (AMD). This study evaluated the therapeutic potential of a newly developed fully human monoclonal antibody targeting cKIT, NN2101, in a murine model of neovascular AMD. In hypoxic human endothelial cells, NN2101 substantially inhibited the SCF-induced increase in angiogenesis and activation of the cKIT signaling pathway. Read More

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Expandable Graphite for Flame Retardant PA6 Applications.

Polymers (Basel) 2021 Aug 15;13(16). Epub 2021 Aug 15.

Institute of Polymer Technology, Friedrich-Alexander-University Erlangen-Nuremberg, Am Weichselgarten 9, 91058 Erlangen, Germany.

A new expandable graphite (EG) type was studied as a flame retardant additive in Polyamide 6 (PA6). The fire behavior was characterized by a cone calorimeter using external heat fluxes of 35, 50 and 65 kW/m, limiting the oxygen index (LOI) and UL-94 burning tests. Additionally, electric and thermal conductivity as well as rheological properties were characterized to provide a general property overview. Read More

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Antibiotics Combinations and Chitosan Nanoparticles for Combating Multidrug Resistance .

Infect Drug Resist 2021 20;14:3327-3339. Epub 2021 Aug 20.

Department of Microbiology and Immunology, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.

Background: Successful treatment of -associated infection is complicated by the emergence of multidrug resistance (MDR), particularly in clinical settings. This urges searching for new alternatives to encounter such health problem.

Aim: This study aimed to evaluate certain antibiotic combinations and CNPs either alone or in combination of some selected antibiotics for the purpose of combating MDR clinical isolates. Read More

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Effects of the Autophagy-Inhibiting Agent Chloroquine on Acute Myeloid Leukemia Cells; Characterization of Patient Heterogeneity.

J Pers Med 2021 Aug 10;11(8). Epub 2021 Aug 10.

Department of Clinical Science, University of Bergen, N-5021 Bergen, Norway.

Autophagy is a highly conserved cellular degradation process that prevents cell damage and promotes cell survival, and clinical efforts have exploited autophagy inhibition as a therapeutic strategy in cancer. Chloroquine is a well-known antimalarial agent that inhibits late-stage autophagy. We evaluated the effects of chloroquine on cell viability and proliferation of acute myeloid leukemia acute myeloid leukemia (AML) cells derived from 81 AML patients. Read More

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Linking the Phytochemicals and the α-Glucosidase and α-Amylase Enzyme Inhibitory Effects of Seed Extracts.

Foods 2021 Aug 6;10(8). Epub 2021 Aug 6.

Laboratory of Applied Chemistry and Environment (LCAE), Faculty of Sciences Oujda (FSO), University Mohammed First (UMP), Oujda 60000, Morocco.

L. (), commonly referred to as black seeds or black cumin, is used in popular medicine (herbal) all over the world for the treatment and prevention of several diseases, including diabetes. This study aims to investigate the inhibitory effect of extracts and fractions against the activities of intestinal α-glucosidase and pancreatic α-amylase in vitro, and to explain the inhibitory effect of these fractions against these enzymes by identifying their active compounds responsible for this effect and determine their modes of inhibition. Read More

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Clinical Effects of Immersive Multimodal BCI-VR Training after Bilateral Neuromodulation with rTMS on Upper Limb Motor Recovery after Stroke. A Study Protocol for a Randomized Controlled Trial.

Medicina (Kaunas) 2021 Jul 21;57(8). Epub 2021 Jul 21.

Facultad de Ciencias Experimentales, Universidad Francisco de Vitoria, 28223 Pozuelo de Alarcón, Spain.

The motor sequelae after a stroke are frequently persistent and cause a high degree of disability. Cortical ischemic or hemorrhagic strokes affecting the cortico-spinal pathways are known to cause a reduction of cortical excitability in the lesioned area not only for the local connectivity impairment but also due to a contralateral hemisphere inhibitory action. Non-invasive brain stimulation using high frequency repetitive magnetic transcranial stimulation (rTMS) over the lesioned hemisphere and contralateral cortical inhibition using low-frequency rTMS have been shown to increase the excitability of the lesioned hemisphere. Read More

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Transcriptional Regulation of Isoforms and by Metformin and Simvastatin through Analyzing Nascent RNA Synthesis in a Human Brain Cell Line.

Biomolecules 2021 08 22;11(8). Epub 2021 Aug 22.

Department of Biochemistry and Medical Genetics, Rady Faculty of Health Sciences, Max Rady College of Medicine, University of Manitoba, Winnipeg, MB R3E 0J9, Canada.

Methyl CpG binding protein 2 (MeCP2) is the main DNA methyl-binding protein in the brain that binds to 5-methylcytosine and 5-hydroxymethyl cytosine. gene mutations are the main origin of Rett Syndrome (RTT), a neurodevelopmental disorder in young females. The disease has no existing cure, however, metabolic drugs such as metformin and statins have recently emerged as potential therapeutic candidates. Read More

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Considering syntrophic acetate oxidation and ionic strength improves the performance of models for food waste anaerobic digestion.

Bioresour Technol 2021 Aug 19;341:125802. Epub 2021 Aug 19.

Department of Chemical Engineering, Universitat de València, Avinguda de la Universitat s/n, 46100 Burjassot, València, Spain. Electronic address:

Current mechanistic anaerobic digestion (AD) models cannot accurately represent the underlying processes occurring during food waste (FW) AD. This work presents an update of the Anaerobic Digestion Model no. 1 (ADM1) to provide accurate estimations of free ammonia concentrations and related inhibition thresholds, and model syntrophic acetate oxidation as acetate-consuming pathway. Read More

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Accelerated Weathering Increases the Release of Toxic Leachates from Microplastic Particles as Demonstrated through Altered Toxicity to the Green Algae .

Toxics 2021 Aug 5;9(8). Epub 2021 Aug 5.

Department of the Built Environment, Aalborg University, Thomas Manns vej 23, 9220 Aalborg, Denmark.

Studies that evaluate the impact of microplastic particles (MPs) often apply particles of pristine material. However, MPs are affected by various abiotic and biotic processes in the environment that possibly modify their physical and chemical characteristics, which might then result in their altered toxic effect. This study evaluated the consequence of weathering on the release of toxic leachates from microplastics. Read More

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Griffithsin and Carrageenan Combination Results in Antiviral Synergy against SARS-CoV-1 and 2 in a Pseudoviral Model.

Mar Drugs 2021 Jul 26;19(8). Epub 2021 Jul 26.

Population Council, New York, NY 10065, USA.

Over 182 million confirmed cases of COVID-19 and more than 4 million deaths have been reported to date around the world. It is essential to identify broad-spectrum antiviral agents that may prevent or treat infections by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) but also by other coronaviruses that may jump the species barrier in the future. We evaluated the antiviral selectivity of griffithsin and sulfated and non-sulfated polysaccharides against SARS-CoV-1 and SARS-CoV-2 using a cytotoxicity assay and a cell-based pseudoviral model. Read More

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Anticancer activity of RAPTA-EA1 in triple-negative BRCA1 proficient breast cancer cells: single and combined treatment with the PARP inhibitor olaparib.

Heliyon 2021 Aug 10;7(8):e07749. Epub 2021 Aug 10.

Laboratory of Pharmaceutical Biotechnology, Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand.

RAPTA-EA1 is a promising glutathione transferase (GSTP-1) inhibitor that has previously been shown to inhibit the growth of various breast cancer cells. We studied the anticancer activity of RAPTA-EA1 on triple-negative BRCA1 competent breast cancer MDA-MB-231 cells. MDA-MB-231 cells are significantly more sensitive to RAPTA-EA1 than MCF-7 cells. Read More

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CuCl-catalyzed inexpensive, faster and ligand/additive free synthesis of isoquinolin-1(2H)-one derivatives via the coupling-cyclization strategy: Evaluation of a new class of compounds as potential PDE4 inhibitors.

Bioorg Chem 2021 Oct 13;115:105265. Epub 2021 Aug 13.

Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500 046, India. Electronic address:

In spite of possessing a wide range of pharmacological properties the anti-inflammatory activities of isoquinolin-1(2H)-ones were rarely known or explored earlier. PDE4 inhibitors on the other hand in addition to their usefulness in treating inflammatory diseases have been suggested to attenuate the cytokine storm in COVID-19 especially TNF-α. In our effort, a new class of isoquinolin-1(2H)-ones derivatives containing an aminosulfonyl moiety were designed and explored as potential inhibitors of PDE4. Read More

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October 2021

O/N/P-doped biochar induced to enhance adsorption of sulfonamide with coexisting Cu/ Cr (VI) by air pre-oxidation.

Bioresour Technol 2021 Aug 18;341:125794. Epub 2021 Aug 18.

State Key Laboratory of Biogeology and Environmental Geology, China University of Geosciences, Beijing 100083, PR China; School of Earth Sciences and Resources, China University of Geosciences, Beijing 100083, PR China. Electronic address:

The aim of this work to study the effectiveness of newly synthesized O/N/P-doped biochar for the removal of antibiotics with coexisting heavy metals. This study developed a low-dose additive agent with air pre-oxidation (APO) to obtain O/N/P-doped biochar (ONPBC) at 650/350 °C pyrolysis temperature with adsorption amount of 76.99 mg·g (ONPBC650) and 62. Read More

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Effects of co-formulants on the absorption and secretion of active substances in plant protection products in vitro.

Arch Toxicol 2021 Oct 20;95(10):3205-3221. Epub 2021 Aug 20.

Department of Pesticides Safety, German Federal Institute for Risk Assessment, Max-Dohrn-Straße 8-10, 10589, Berlin, Germany.

Currently, the authorisation process for plant protection products (PPPs) relies on the testing of acute and topological toxicity only. Contrastingly, the evaluation of active substances includes a more comprehensive set of toxicity studies. Nevertheless, mixture effects of active ingredients and co-formulants may result in increased toxicity. Read More

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October 2021