21,922 results match your criteria species inhibit


Supramolecular polymerization provides non-equilibrium product distributions of imine-linked macrocycles.

Chem Sci 2020 Jan 9;11(7):1957-1963. Epub 2020 Jan 9.

Department of Chemistry, Northwestern University Evanston IL 60208 USA

Supramolecular polymerization of imine-linked macrocycles has been coupled to dynamic imine bond exchange within a series of macrocycles and oligomers. In this way, macrocycle synthesis is driven by supramolecular assembly, either into small aggregates supported by π-π interactions, or high-aspect ratio nanotubes stabilized primarily by electrostatic and solvophobic interactions. For the latter, supramolecular polymerization into nanotubes restricts imine exchange, thereby conferring chemical stability to the assemblies and their constituent macrocycles. Read More

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January 2020

Peptidomimetics prepared by tail-to-side chain one component peptide stapling inhibit Alzheimer's amyloid-β fibrillogenesis.

Chem Sci 2020 Mar 27;11(16):4171-4179. Epub 2020 Mar 27.

Laboratory of Peptide and Amyloid Research, Department of Chemistry, Indian Institute of Technology Guwahati Assam-781039 India

Alzheimer's disease (AD) is the most common form of dementia affecting the elderly population worldwide. Despite enormous efforts and considerable advancement in research, no therapeutic agents have come to light to date. However, many peptide-based and small molecule inhibitors interact efficiently with the amyloid-β (Aβ) peptide and alter its aggregation pathway. Read More

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: where do we stand in our battle against this oral pathogen?

RSC Med Chem 2021 May 26;12(5):666-704. Epub 2021 Feb 26.

College of Pharmacy, Department of Pharmaceutical Sciences, University of Kentucky Lexington KY 40536-0596 USA +1 859 218 1686.

Periodontal diseases, such as gingivitis and periodontitis, are inflammatory diseases triggered by pathogenic bacteria that lead to damage of the soft tissue and bone supporting the teeth. Amongst the identified oral periodontopathogenic bacteria, is able to enhance oral dysbiosis, which is an imbalance in the beneficial commensal and periodontal pathogenic bacteria that induces chronic inflammation. Given the critical role of oral pathogenic bacteria like in the pathogenesis of periodontitis, local and/or systemic antibacterial therapy has been suggested to treat this disease, especially in its severe or refractory forms. Read More

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F1012-2 Induced ROS-Mediated DNA Damage Response through Activation of MAPK Pathway in Triple-Negative Breast Cancer.

Biomed Res Int 2021 1;2021:6650045. Epub 2021 Jun 1.

School of Pharmaceutical Sciences, Zhejiang Chinese Medical University, Hangzhou, Zhejiang 311402, China.

We have previously reported that F1012-2, a sesquiterpene lactone isolated from the Chinese herbal medicine DC., exhibits strong effects against Triple Negative Breast Cancer (TNBC). In this study, we found F1012-2 effectively inhibited cell migration and invasion detected by wound healing and transwell assays. Read More

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Phytochemical composition and bioactive effects of ethyl acetate fraction extract (EAFE) of Glechoma hederacea L.

J Food Biochem 2021 Jun 14:e13815. Epub 2021 Jun 14.

Department of Food and Nutrition, Providence University, Taichung, Taiwan.

Hepatocellular carcinoma (HCC) is a highly malignant cancer that exists worldwide. Herbal medicine plays an important role in the management and treatment of various diseases worldwide. The herbal medicine Glechoma hederacea L. Read More

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Purified antioxidant from the medicinal mushroom Phellinus pini protects rat H9c2 cell against H O -induced oxidative stress.

J Food Biochem 2021 Jun 13:e13818. Epub 2021 Jun 13.

School of Biomedical Sciences, Faculty of Medicine, The Chinese University of Hong Kong, Hong Kong, China.

In this study, through the combination of AB-8 macroporous resin, Sephadex LH-20 column chromatography and semi-preparative HPLC, an antioxidant component was purified from the crude extract of Phellinus pini, thereby evaluating the cardioprotective effect of the fraction. As a result, total phenolic content of the 60% ethanol elution was increased by 4.8-fold after one run treatment on Sephadex LH-20 chromatography with gradient elution. Read More

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Tethered peptide toxins for ion channels.

Methods Enzymol 2021 1;654:203-224. Epub 2021 Apr 1.

Departments of Pediatrics, Physiology & Biophysics, and Pharmaceutical Sciences, Susan and Henry Samueli College of Health Sciences, University of California, Irvine, CA, United States. Electronic address:

In this method paper, we describe protocols for using membrane-tethered peptide toxins (T-toxins) to study the structure/function and biophysics of toxin-channel interactions with two-electrode voltage clamp (TEVC). Here, we show how T-toxins can be used to determine toxin equilibrium affinity, to quantify toxin surface level by enzyme-linked immunosorbent assay (ELISA) and/or single-molecule total internal reflection fluorescence (smTIRF) microscopy, to assess toxin association and dissociations rate, to identify toxin residues critical to binding via scanning mutagenesis, and to study of toxin blocking mechanism. The sea anemone type I (SAK1) toxin HmK and a potassium channel are used to demonstrate the strategies. Read More

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A horizontally acquired Legionella genomic island encoding a LuxR type regulator and effector proteins displays variation in gene content and regulation.

Mol Microbiol 2021 Jun 13. Epub 2021 Jun 13.

The Shmunis School of Biomedicine and Cancer Research, George S. Wise Faculty of Life Sciences, Tel-Aviv University, Tel-Aviv, 6997801, Israel.

The intracellular pathogen Legionella pneumophila translocates >300 effector proteins into host cells, many of which are regulated at the transcriptional level. Here, we describe a novel L. pneumophila genomic island, which undergoes horizontal gene transfer within the Legionella genus. Read More

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Mixing postharvest fungicides and sanitizers results in unpredictable survival of microbes that affect cantaloupes.

Food Microbiol 2021 Oct 2;99:103797. Epub 2021 Apr 2.

ARC Training Centre for Food Safety in the Fresh Produce Industry, School of Life and Environmental Sciences, Sydney Institute of Agriculture, Faculty of Science, The University of Sydney, NSW, 2006, Australia. Electronic address:

Postharvest treatments with sanitizers and fungicides are applied to increase the quality, safety and shelf life of fresh produce including cantaloupes (also known as rockmelons). The primary role of sanitizers during cantaloupe washing is to prevent cross contamination of potentially pathogenic bacteria in washwater. Postharvest fungicide sprays or dips are employed to inhibit spoilage-causing fungi. Read More

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October 2021

The protective effects of 18β-glycyrrhetinic acid against acrylamide-induced cellular damage in diabetic rats.

Environ Sci Pollut Res Int 2021 Jun 11. Epub 2021 Jun 11.

Department of Zoology, College of Science, King Saud University, P.O. Box 2455, Riyadh, 11451, Saudi Arabia.

This study was aimed at elucidating the protective effects of 18β-glycyrrhetinic acid (18βGA) against acrylamide (Acr)-induced cellular damage in diabetic rats. Rats were randomly assigned into eight groups (n = 8) following 12 h of fasting: control group, a single dose of 50 mg/kg streptozotocin (STZ) intraperitoneally (diabetic group), 50 mg/kg 18βGA orally after 2 weeks from STZ injection (18βGA group), 20 mg/kg Acr after 1month from STZ injection (Acr group), STZ plus Acr (STZ-Acr group), STZ plus 18βGA (STZ-18βGA group), Acr plus 18βGA (Acr-18βGA group), or STZ plus Acr plus 18βGA (STZ-Acr-18βGA group). Administration of 18βGA alone increased GSH, GSH-PX, SOD, and CAT in both liver and kidneys. Read More

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Transporter-interfering chemicals inhibit P-glycoprotein of yellowfin tuna (Thunnus albacares).

Comp Biochem Physiol C Toxicol Pharmacol 2021 Jun 8:109101. Epub 2021 Jun 8.

Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography, University of California, San Diego, La Jolla, CA 92093-0202, United States of America. Electronic address:

Marine pollutants bioaccumulate at high trophic levels of marine food webs and are transferred to humans through consumption of apex species. Yellowfin tuna (Thunnus albacares) are marine predators, and one of largest commercial fisheries in the world. Previous studies have shown that yellowfin tuna can accumulate high levels of persistent organic pollutants, including several that are Transporter Interfering Chemicals (TICs) which bind to human xenobiotic transporters and interfere with their function. Read More

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Epigenetic modification cooperates with Zeb1 transcription factor to regulate Bmp4 to promote chicken PGCs formation.

Gene 2021 Jun 8:145760. Epub 2021 Jun 8.

Key Laboratory of Animal Breeding Reproduction and Molecular Design for Jiangsu Province, College of Animal Science and Technology, Yangzhou University, Yangzhou 225009, China; Joint International Research Laboratory of Agriculture and Agri-Product Safety of the Ministry of Education of China, Yangzhou University, China; College of biotechnology, Jiangsu University of science and technology, China. Electronic address:

BMP4 is the critical gene of primordial germ cell formation in mammal, however, the mechanism of PGCs formation in chicken still unknown. In this research, we compared the evolution relationship of different species. Although the protein sequence is highly conservative between mouse, human and chicken, promotors vary among avian and mammal species. Read More

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Ethylenediamine-bound magnetite nanoparticles as dual function colorimetric sensor having charge transfer and nanozyme activity for TNT and tetryl detection.

Mikrochim Acta 2021 Jun 11;188(7):228. Epub 2021 Jun 11.

Engineering Faculty, Chemistry Department, Istanbul University-Cerrahpaşa, Avcilar, Istanbul, Turkey.

A reusable, low-cost, and convenient ethylenediamine (EDA)-bound magnetite nanoparticles (MNPs)-based colorimetric sensor has been developed for dual function colorimetric determination of nitroaromatic explosives such as TNT and tetryl. Colorimetric detection of analytes may occur through two independent routes: (1) nano-FeO- EDA- NH as σ-donor may interact with the σ- and π-acceptor aromatic-poly(NO) groups to produce a colored charge-transfer (CT) complex; (2) nano-FeO-EDA-NH as a Fenton-type nanozyme may generate reactive species that comprise hydroxyl radicals (OH) with HO to oxidize 3,3',5,5'-tetramethylbenzidine (TMB) to a blue-colored diimine (oxTMB-TMB) CT complex, where this color is bleached with TNT/tetryl because of donor-acceptor interactions between the explosive -NO groups and the -NH group of FeO-EDA nanoparticles of restricted nanozyme activity. Both methods can quantify TNT well below the EPA recommended TNT residential screening level in soil, LOD being in the micromolar range. Read More

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Evaluation of antioxidant, antinflammatory and antityrosinase potential of extracts from different aerial parts of Rhanterium suaveolens from Tunisia.

Chem Biodivers 2021 Jun 11. Epub 2021 Jun 11.

University of Messina: Universita degli Studi di Messina, Chemical Biological Pharmaceutical and Environmental Science, Cda Palatucci, Italia, 98168, Messina, ITALY.

The genus Rhanterium (Asteraceae) is a widely distributed medicinal plant throughout western North Africa and some Rhanterium species are used in folk medicine. The aim of research was to investigate methanolic extracts from different parts (flowers, leaves, and stems) of Tunisian Rhanterium suaveolens as potential sources of bioactive products useful for healthy purposes. In particular, were analyzed the phenolic composition of these extracts and their antioxidant, anti-inflammatory, and anti-tyrosinase properties. Read More

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Antimicrobial activity, chemical composition and cytotoxicity of basidiocarp.

Food Funct 2021 Jun 10. Epub 2021 Jun 10.

Paranaense University, Molecular Biology Laboratory, 87502-210, Umuarama, PR, Brazil.

Lentinus crinitus (L.) Fr. (Basidiomycota: Polyporales) is a wild mushroom with several biotechnological applications; however, there are few studies on its chemical composition and antimicrobial activity. Read More

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Neohesperidin Induces Cell Cycle Arrest, Apoptosis, and Autophagy via the ROS/JNK Signaling Pathway in Human Osteosarcoma Cells.

Am J Chin Med 2021 Jun 2:1-24. Epub 2021 Jun 2.

Department of Orthopedic Surgery, Xiang'an Hospital of Xiamen University, No. 2000, Xiang'an East Road, Xiang'an District Xiamen City, Fujian Province, P. R. China.

Neohesperidin has anti-oxidative and anti-inflammatory properties and exerts extensive therapeutic effects on various cancers. In this study, the osteosarcoma cell lines were exposed to different concentrations of neohesperidin. Cell proliferation and viability were assessed by CCK-8 and colony-formation assays. Read More

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Resveratrol activates PI3K/AKT to reduce myocardial cell apoptosis and mitochondrial oxidative damage caused by myocardial ischemia/reperfusion injury.

Acta Histochem 2021 Jun 6;123(5):151739. Epub 2021 Jun 6.

Department of Cardiovascular Surgery, The First Affiliated Hospital of Nanjing Medical University, Nanjing, 210029, China. Electronic address:

Resveratrol is a kind of iPolyphenols widely existing in herbal medicine. Here we aim to investigate whether resveratrol can reduce the degree of myocardial ischemia/reperfusion (IR) injury and inhibit the development of oxidative stress, and elucidate the molecular mechanism of resveratrol in protecting myocardial cells. The primary rat cardiomyocytes were used to establish an ischemia/reperfusion model in vitro, and a series of routine biochemical experiments were conducted to explore the antioxidant and anti-apoptotic effects of resveratrol in myocardial ischemia-reperfusion injury. Read More

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Napabucasin Drug-Drug Interaction Potential, Safety, Tolerability, and Pharmacokinetics Following Oral Dosing in Healthy Adult Volunteers.

Clin Pharmacol Drug Dev 2021 Jun 9. Epub 2021 Jun 9.

Clinical NCA & PK/PD, Nuventra, Inc., Durham, North Carolina, USA.

Napabucasin is an orally administered reactive oxygen species generator that is bioactivated by the intracellular antioxidant nicotinamide adenine dinucleotide phosphate:quinone oxidoreductase 1. Napabucasin induces cell death in cancer cells, including cancer stem cells. This phase 1 study (NCT03411122) evaluated napabucasin drug-drug interaction potential for 7 cytochrome P450 (CYP) enzymes and the breast cancer resistance protein transporter/organic anion transporter 3. Read More

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A Bioengineered Nisin Derivative to Control Biofilms of .

Appl Environ Microbiol 2021 Jun 9:AEM0039121. Epub 2021 Jun 9.

APC Microbiome Ireland, University College Cork, Cork, Ireland.

Antimicrobial peptides are evolving as novel therapeutic options against the increasing problem of multidrug-resistant microorganisms, and nisin is one such avenue. However, some bacteria possess a specific nisin resistance system (NSR) which cleaves the peptide reducing its bactericidal efficacy. NSR-based resistance was identified in strains of , a ubiquitous pathogen that causes mastitis in dairy cattle. Read More

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Comparative phytochemistry of flavaglines (= rocaglamides), a group of highly bioactive flavolignans from species (Meliaceae).

Authors:
Harald Greger

Phytochem Rev 2021 Jun 4:1-40. Epub 2021 Jun 4.

Chemodiversity Research Group, Faculty of Life Sciences, University of Vienna, Rennweg 14, 1030 Wien, Austria.

Flavaglines are formed by cycloaddition of a flavonoid nucleus with a cinnamic acid moiety representing a typical chemical character of the genus of the family Meliaceae. Based on biosynthetic considerations 148 derivatives are grouped together into three skeletal types representing 77 cyclopenta[]benzofurans, 61 cyclopenta[]benzopyrans, and 10 benzo[]oxepines. Apart from different hydroxy, methoxy, and methylenedioxy groups of the aromatic rings, important structural variation is created by different substitutions and stereochemistries of the central cyclopentane ring. Read More

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Comparative transcriptomics analysis reveals differential Cd response processes in roots of two turnip landraces with different Cd accumulation capacities.

Ecotoxicol Environ Saf 2021 Jun 5;220:112392. Epub 2021 Jun 5.

Germplasm Bank of Wild Species, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China; Xishuangbanna Tropical Botanical Garden, Chinese Academy of Sciences, Xishuangbanna 666303, China. Electronic address:

Understanding the molecular mechanisms of cadmium (Cd) tolerance and accumulation in plants is important to address Cd pollution. In the present study, we performed comparative transcriptome analysis to identify the Cd response processes in the roots of two turnip landraces, KTRG-B14 (high-Cd accumulation) and KTRG-B36 (low-Cd accumulation). Two common enhanced processes, glutathione metabolism and antioxidant system, were identified in both landraces. Read More

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Ferrous hemoglobin and hemoglobin-based oxygen carriers acting as a peroxidase can inhibit oxidative damage to endothelial cells caused by hydrogen peroxide.

Artif Organs 2021 Jun 8. Epub 2021 Jun 8.

College of Life Science, Northwest University, Xi'an, P.R. China, 710069.

Oxidative damage caused by the ferryl hemoglobin is one of the major clinical adverse reactions of hemoglobin-based oxygen carriers (HBOCs), while the production of reactive oxygen species in a pathological state can oxidize hemoglobin (HbFe ) to ferryl Hb, which can then enter the pseudoperoxidase cycle, making hemoglobin highly toxic. In this study, we found that ferrous hemoglobin and polymerized porcine hemoglobin (one of the HBOCs) have the peroxidase activity different from the pseudoperoxidase activity of ferric hemoglobin. Ferrous hemoglobin can catalyze the reaction of tyrosine (Tyr) with hydrogen peroxide. Read More

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Light, power, action! Interaction of respiratory energy and blue light induced stomatal movements.

New Phytol 2021 Jun 8. Epub 2021 Jun 8.

School of Life Sciences, University of Essex, Colchester, CO4 3SQ, UK.

Although the signalling pathway of blue light dependent stomatal opening is well characterized, little is known about the interspecific diversity, the role it plays in the regulation of gas exchange and the source of energy used to drive the commonly observed increase in pore aperture. Using a combination of red and blue light under ambient and low [O ] (to inhibit respiration), the interaction between blue light, photosynthesis and respiration in determining stomatal conductance was investigated. These findings were used to develop a novel model to predict the feedback between photosynthesis and stomatal conductance under these conditions. Read More

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A Bacterial Symbiont Protects Honey Bees from Fungal Disease.

mBio 2021 Jun 8:e0050321. Epub 2021 Jun 8.

Department of Biology, Indiana University, Bloomington, Indiana, USA.

Fungal pathogens, among other stressors, negatively impact the productivity and population size of honey bees, one of our most important pollinators (1, 2), in particular their brood (larvae and pupae) (3, 4). Understanding the factors that influence disease incidence and prevalence in brood may help us improve colony health and productivity. Here, we examined the capacity of a honey bee-associated bacterium, Bombella apis, to suppress the growth of fungal pathogens and ultimately protect bee brood from infection. Read More

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Colchicine inhibits ROS generation in response to glycoprotein VI stimulation.

Sci Rep 2021 Jun 7;11(1):11965. Epub 2021 Jun 7.

The ANZAC Research Institute, Concord Repatriation General Hospital, Hospital Road, Concord, NSW, 2139, Australia.

Colchicine inhibits coronary and cerebrovascular events in patients with coronary artery disease (CAD), and although known to have anti-inflammatory properties, its mechanisms of action are incompletely understood. In this study, we investigated the effects of colchicine on platelet activation with a particular focus on its effects on activation via the collagen glycoprotein (GP)VI receptor, P2Y receptor, and procoagulant platelet formation. Therapeutic concentrations of colchicine in vitro (equivalent to plasma levels) significantly decreased platelet aggregation in whole blood and in platelet rich plasma in response to collagen (multiplate aggregometry) and reduced reactive oxygen species (ROS) generation (HDCF-DA, flow cytometry) in response to GPVI stimulation with collagen related peptide-XL (CRP-XL, GPVI specific agonist). Read More

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Tanshinones inhibit NLRP3 inflammasome activation by alleviating mitochondrial damage to protect against septic and gouty inflammation.

Int Immunopharmacol 2021 Jun 3;97:107819. Epub 2021 Jun 3.

The Fifth Affiliated Hospital, Key Laboratory of Molecular Target & Clinical Pharmacology and the State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou 511436, PR China. Electronic address:

Tanshinones, the active ingredients derived from the roots of Salvia miltiorrhiza, have been widely used as traditional medicinal herbs for treating human diseases. Although tanshinones showed anti-inflammatory effects in many studies, large knowledge gaps remain regarding their underlying mechanisms. Here, we identified 15 tanshinones that suppressed the activation of NLRP3 inflammasome and studied their structure-activity relationships. Read More

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4-Chlorophenylthioacetone-derived thiosemicarbazones as potent antitrypanosomal drug candidates: Investigations on the mode of action.

Bioorg Chem 2021 May 25;113:105018. Epub 2021 May 25.

Departamento de Bioquímica e Imunologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, MG, Brazil; Faculdade de Medicina, Programa em Ciências da Saúde: Infectologia e Medicina Tropical, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil. Electronic address:

Chagas disease (ChD), caused by Trypanosoma cruzi, remains a challenge for the medical and scientific fields due to the inefficiency of the therapeutic approaches available for its treatment. Thiosemicarbazones and hydrazones present a wide spectrum of bioactivities and are considered a platform for the design of new anti-T. cruzi drug candidates. Read More

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SiCEP3, a C-terminally encoded peptide from Setaria italica, promotes ABA import and signaling.

J Exp Bot 2021 Jun 7. Epub 2021 Jun 7.

State Key Laboratory of Crop Biology, Engineering center of Saline-alkali soil plant - microbial joint restoration, College of Life Sciences, Shandong Agricultural University, Tai'an Shandong, China.

C-terminally encoded peptides (CEPs) are small peptides, typically post-translationally modified, and highly conserved in many species. CEPs are known to inhibit plant growth and development, but the mechanisms are not well understood. In this study, fourteen CEPs were identified in Setaria italica and were divided into two groups. Read More

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Isolation of a natural product with anti-mitotic activity from a toxic Canadian prairie plant.

Heliyon 2021 May 24;7(5):e07131. Epub 2021 May 24.

Natural Product and Cancer Cell Laboratories, University of Lethbridge, Lethbridge, AB, T1K 3M4 Canada.

We are investigating plants from the prairie ecological zone of Canada to identify natural products that inhibit mitosis in cancer cells. Investigation of plant parts from the Canadian plant species (Asteraceae) revealed that leaf extracts (PP-360A) had anti-mitotic activity on human cancer cell lines. Cells treated with leaf extracts acquired a rounded morphology, similar to that of cells in mitosis. Read More

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A metal-organic framework/polymer derived catalyst containing single-atom nickel species for electrocatalysis.

Chem Sci 2020 Sep 25;11(40):10991-10997. Epub 2020 Sep 25.

Institute of Chemical Sciences and Engineering, École Polytechnique Fédérale de Lausanne (EPFL), EPFL-ISIC-Valais Sion 1950 Switzerland

While metal-organic frameworks (MOF) alone offer a wide range of structural tunability, the formation of composites, through the introduction of other non-native species, like polymers, can further broaden their structure/property spectrum. Here we demonstrate that a polymer, placed inside the MOF pores, can support the collapsible MOF and help inhibit the aggregation of nickel during pyrolysis; this leads to the formation of single atom nickel species in the resulting nitrogen doped carbons, and dramatically improves the activity, CO selectivity and stability in electrochemical CO reduction reaction. Considering the vast number of multifarious MOFs and polymers to choose from, we believe this strategy can open up more possibilities in the field of catalyst design, and further contribute to the already expansive set of MOF applications. Read More

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September 2020