358,812 results match your criteria inhibition activity


Screening and verification of CYP3A4 inhibitors from Bushen-Yizhi formula to enhance the bioavailability of osthole in rat plasma.

J Ethnopharmacol 2021 Sep 14:114643. Epub 2021 Sep 14.

Science and Technology Innovation Center, Guangzhou University of Chinese Medicine, Guangzhou, 510405, China; Institute of Clinical Pharmacology, Guangzhou University of Chinese Medicine, Guangzhou, 510405, China. Electronic address:

Ethnopharmacological Relevance: With the features of multiple-components and targets as well as multifunction, traditional Chinese medicine (TCM) has been widely used in the prevention and treatment of various diseases for a long time. During the application of TCM, the researches about bioavailability enhancement of the bioactive constituents in formula are flourishing. Bushen-Yizhi formula (BSYZ), a TCM prescription with osthole (OST) as one of the main bioactive ingredients, have been widely used to treat kidney deficiency, mental retardation and Alzheimer's disease. Read More

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September 2021

Enhanced antibacterial activity of lysozyme loaded quaternary ammonium chitosan nanoparticles functionalized with cellulose nanocrystals.

Int J Biol Macromol 2021 Sep 14. Epub 2021 Sep 14.

School of Agriculture and Biology, Shanghai Jiao Tong University, Shanghai 200240, China; Shanghai Veterinary Bio-tech Key Laboratory, Shanghai 200240, China. Electronic address:

In this study, cellulose nanocrystals (CNC) as functional cross-linker and Pickering emulsifier was used to stabilize Lysozyme (Lys) encapsulated in quaternary ammonium chitosan nanoparticles (QC NPs) via ionic gelation method. Physicochemical, structural, and antibacterial properties of the CNC stabilized Lys loaded QC NPs were also evaluated. Particle size, particle size distribution, Zeta potential (ZP), and spectroscopic analyses showed the successful encapsulation of Lys. Read More

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September 2021

A comparative study based on activity, conformation and computational analysis on the inhibition of human salivary aldehyde dehydrogenase by phthalate plasticizers: Implications in assessing the safety of packaged food items.

Toxicology 2021 Sep 14:152947. Epub 2021 Sep 14.

Interdisciplinary Biotechnology Unit, Faculty of Life Sciences, Aligarh Muslim University, Aligarh, 202002, India. Electronic address:

Phthalate plasticizers are commonly used in various consumer-end products. Human salivary aldehyde dehydrogenase (hsALDH) is a detoxifying enzyme which defends us from the toxic aldehydes. Here, the effect of phthalates [Di-2-ethylhexyl phthalate (DEHP), Diethyl phthalate (DEP) and Dibutyl phthalate (DBP)] on hsALDH has been investigated. Read More

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September 2021

Inhibition of huntingtin aggregation by its N-terminal 17-residue peptide and its analogs.

Arch Biochem Biophys 2021 Sep 14:109033. Epub 2021 Sep 14.

Department of Biosciences and Bioengineering, Indian Institute of Technology Guwahati, Guwahati, 781 039, India. Electronic address:

The N-terminal 17-residue stretch of huntingtin (htt) folds into an amphipathic α-helix. The htt-harboring polyQ peptides form oligomers that are mediated via the assembly of the htt α-helices. The oligomerization results in higher local concentration of the polyglutamine (polyQ) region, thereby facilitating amyloid formation. Read More

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September 2021

7-[[(4-methyl-2-pyridinyl)amino](2-pyridinyl)methyl]-8-quinolinol (compound 30666) inhibits enhancer activity and reduces B-cell lymphoma growth - A question of specificity.

Eur J Pharmacol 2021 Sep 14;910:174505. Epub 2021 Sep 14.

Institute of Human Genetics, Polish Academy of Sciences, Poznań, Poland. Electronic address:

B-cell non-Hodgkin lymphoma (NHL) is among the ten most common malignancies. Survival rates range from very poor to over 90% and highly depend on the stage and subtype. Characteristic features of NHL are recurrent translocations juxtaposing an oncogene (e. Read More

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September 2021

Thromboxane A2 synthase inhibition ameliorates endothelial dysfunction, memory deficits, oxidative stress and neuroinflammation in rat model of streptozotocin diabetes induced dementia.

Physiol Behav 2021 Sep 14:113592. Epub 2021 Sep 14.

Pharmacology division, Department of Pharmaceutical Sciences and Drug Research, Faculty of Medicine, Punjabi university, Patiala- 147002, Punjab, India. Electronic address:

Rationale: Vascular dementia (VaD) is the second leading cause of dementia worldwide. It is very important to find the possible pharmacological agents which may be useful in management and therapy of VaD.

Objectives: The present study investigates the effect of ozagrel, a selective thromboxane A2 (TXA2) synthase inhibitor, in a rat model of VaD. Read More

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September 2021

Break Away: FKBP12 sequestration as a target for increasing BMP activity.

Cell Chem Biol 2021 Sep;28(9):1253-1255

Department of Chemistry and Biochemistry, Clemens-Schöpf-Institute, Technical University Darmstadt, Alarich-Weiss Strasse 4, 64287 Darmstadt, Germany. Electronic address:

Bone morphogenetic protein (BMP) signaling contributes to acute kidney injury (AKI), a common disease without adequate treatment options. In this issue of Cell Chemical Biology, Larraufie, Gao and colleagues (Larraufie et al., 2021) show that FKBP12 inhibition can be a target for treatment of AKI via activation of BMP signaling. Read More

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September 2021

RAS induced senescence of skin keratinocytes is mediated through Rho-associated protein kinase (ROCK).

Mol Carcinog 2021 Sep 17. Epub 2021 Sep 17.

Laboratory of Cancer Biology and Genetics, Center for Cancer Research, National Cancer Institute, Bethesda, Maryland, USA.

Cellular senescence is a well-documented response to oncogene activation in many tissues. Multiple pathways are invoked to achieve senescence indicating its importance to counteract the transforming activities of oncogenic stimulation. We now report that the Rho-associated protein kinase (ROCK) signaling pathway is a critical regulator of oncogene-induced senescence in skin carcinogenesis. Read More

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September 2021

pH-Responsive Smart Wettability Surface with Dual Bactericidal and Releasing Properties.

ACS Appl Mater Interfaces 2021 Sep 17. Epub 2021 Sep 17.

School of Food and Biological Engineering, Jiangsu University, Zhenjiang 212013, Jiangsu, P. R. China.

Biomaterial-associated infections caused by pathogenic bacteria have important implications on human health. This study presents the design and preparation of a smart surface with pH-responsive wettability. The smart surface exhibited synergistic antibacterial function, with high liquid repellency against bacterial adhesion and highly effective bactericidal activity. Read More

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September 2021

The impact of regular activity and exercise intensity on the acute effects of resistance exercise on cognitive function.

Scand J Med Sci Sports 2021 Sep 17. Epub 2021 Sep 17.

Institute of Sports Science, Department of Sports Medicine and Exercise Physiology, Goethe University, Frankfurt am Main, Germany.

Beneficial acute effects of resistance exercise on cognitive functions may be modified by exercise intensity or by habitual physical activity. Twenty-six participants (9 female, 17 male; 25.5±3. Read More

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September 2021

Effect of silver nanoparticles on the antibacterial activity of Levofloxacin against methicillin-resistant Staphylococcus aureus.

Authors:
M J Saadh

Eur Rev Med Pharmacol Sci 2021 Sep;25(17):5507-5510

Faculty of Pharmacy, Middle East University, Amman, Jordan.

Objective: The paper presents the antibacterial activity of silver nanoparticles (AgNPs) when conjugated with Levofloxacin. The AgNPs used in this study were synthesized from silver nitrate using sodium borohydride as a reducing agent.

Materials And Methods: Levofloxacin activity was determined by minimum inhibitory concentrations (MICs) and also the erythrocyte hemolytic assay determined the capability of conjugation to cause hemolysis in human erythrocyte. Read More

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September 2021

Preparation, characterization, and antibacterial properties of hybrid nanofibrous scaffolds for cutaneous tissue engineering.

Hum Cell 2021 Sep 17. Epub 2021 Sep 17.

Stem Cell Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.

Since polymeric nanofibrous scaffolds have been widely used in tissue regeneration, the risk of bacterial infections should not be neglected. In the present work, poly-caprolactone-silk fibroin-soluble eggshell membrane-silver nanoparticles (PCL-SF-SESM-AgNPs) and caprolactone-silk fibroin-soluble eggshell membrane-chitosan (PCL-SF-SESM-CS) scaffolds were fabricated via the electrospinning method for cutaneous regeneration. The composition, morphology, hydrophilicity, and mechanical features of prepared scaffolds were evaluated using Fourier transform infrared (FT-IR), scanning electron microscope (SEM), tensile, and water contact angle tests. Read More

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September 2021

Prolyl Hydroxylase Inhibitors: a New Opportunity in Renal and Myocardial Protection.

Cardiovasc Drugs Ther 2021 Sep 17. Epub 2021 Sep 17.

Atherothrombosis Research Unit, Icahn School of Medicine At Mount Sinai, One Gustave L. Levy Pl, New York, NY, 10029-0310, USA.

Hypoxia, via the activity of hypoxia-inducible factors (HIFs), plays a crucial role in fibrosis, inflammation, and oxidative injury, processes which are associated with progression of cardiovascular and kidney diseases. HIFs are key transcription heterodimers consisting of regulatory α-subunits (HIF-1α, HIF-2α, HIF-3α) and a constitutive β-subunit (HIF-β). The stability of HIFs is regulated by the prolyl hydroxylases (PHDs). Read More

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September 2021

Cyclophilin A: a possible host modulator in Chandipura virus infection.

Arch Virol 2021 Sep 17. Epub 2021 Sep 17.

ICMR-National Institute of Virology, 130/1 Sus Road, Pashan, Pune, 411021, India.

Chandipura virus (CHPV), belonging to the genus Vesiculovirus of the family Rhabdoviridae, has been identified as one of the causes of pediatric encephalitis in India. Currently, neither vaccines nor therapeutic drugs are available against this agent. Considering that the disease progresses very fast with a high mortality rate, working towards the development of potential therapeutics against it will have a public health impact. Read More

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September 2021

Flunarizine suppresses Mycobacterium tuberculosis growth via calmodulin-dependent phagosome maturation.

J Leukoc Biol 2021 Sep 17. Epub 2021 Sep 17.

Guangdong Provincial Key Laboratory of Regional Immunity and Diseases, Department of Pathogen Biology, School of Medicine, Shenzhen University, Shenzhen, China.

Tuberculosis (TB), an infectious bacterial disease caused by Mycobacterium tuberculosis (Mtb), is a major cause of death worldwide. Multidrug-resistant TB remains a public health crisis and thus novel effective treatments, such as host-directed therapies (HDTs), are urgently required to overcome the challenges of TB infection. In this study, we evaluated 4 calcium modulators for their effects on Mtb growth in macrophages. Read More

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September 2021

CREB regulates the expression of Type 1 Inositol 1,4,5-trisphosphate receptors.

J Cell Sci 2021 Sep 17. Epub 2021 Sep 17.

Department of Pharmacology and Physiology, University of Rochester, Rochester, NY, 14642, USA.

Inositol 1,4,5-trisphosphate (IP3) receptors (IP3Rs) play a central role in regulating intracellular calcium signals in response to a variety of internal/external cues. Dysregulation of IP3R signaling is the underlying cause for numerous pathological conditions. It is well established that the activities of IP3Rs are governed by several post-translational modifications including phosphorylation by protein kinase A (PKA). Read More

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September 2021

Arjunetin as a promising drug candidate against SARS-CoV-2: molecular dynamics simulation studies.

J Biomol Struct Dyn 2021 Sep 17:1-22. Epub 2021 Sep 17.

Department of Biotechnology, Bhupat and Jyoti Mehta School of Biosciences, Applied and Industrial Microbiology Laboratory, Indian Institute of Technology Madras, Chennai, India.

Stem and bark of the tree Wight & Arn. (Combretaceae) has been documented to exhibit therapeutic properties like cardiotonic, anticancer, antiviral, antibacterial, antifungal, hypercholesterolemia, hypolipidemic, and anti-coagulant. Our previous studies have shown that, ethanolic extract of bark exhibits radical scavenging anti-oxidant activity and also effectively inhibited catalase activity. Read More

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September 2021

Characterization of a Novel Shewanella algae Arginine Decarboxylase Expressed in Escherichia coli.

Mol Biotechnol 2021 Sep 16. Epub 2021 Sep 16.

College of Light Industry and Food Engineering, Guangxi University, Nanning, 530004, People's Republic of China.

Arginine decarboxylase (ADC) catalyzes the decarboxylation of arginine to form agmatine, an important physiological and pharmacological amine, and attracts attention to the enzymatic production of agmatine. In this study, we for the first time overexpressed and characterized the marine Shewanella algae ADC (SaADC) in Escherichia coli. The recombinant SaADC showed the maximum activity at pH 7. Read More

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September 2021

Vitamin C reduces vancomycin-related nephrotoxicity through the inhibition of oxidative stress, apoptosis, and inflammation in mice.

Ann Transl Med 2021 Aug;9(16):1319

Department of Pharmacy, Ruijin Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, China.

Background: Vancomycin (VCM) is an antibiotic widely used to treat a range of serious bacterial infections; however, it is associated with nephrotoxicity. Vitamin C (VC) is a classical antioxidant that can alleviate various organ injuries and inflammatory responses by reducing inflammation and oxidative stress. This study aimed to examine the effect of VC on VCM-related nephrotoxicity in mice. Read More

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Effects of ligustrazine on the expression of neurotransmitters in the trigeminal ganglion of a rat migraine model.

Ann Transl Med 2021 Aug;9(16):1318

Department of Traditional Chinese Medicine, Guangzhou Red Cross Hospital, Jinan University, Guangzhou, China.

Background: Migraine is one of the most common neurological diseases which has been treated by active substances from traditional Chinese medicine (TCM), such as ligustrazine, an extract of the Chinese herb Chuanxiong. However, the pathogenesis of migraine and the curative mechanisms of ligustrazine have remained unclear. The genes , , , and have been implicated to play a role. Read More

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Ozone induces BEL7402 cell apoptosis by increasing reactive oxygen species production and activating JNK.

Ann Transl Med 2021 Aug;9(15):1257

Division of Vascular and Interventional Radiology, Department of General Surgery, Nanfang Hospital, Southern Medical University, Guangzhou, China.

Background: Oxidative stress is an important factor in the modulation of both tumorigenesis and anticancer responses. Ozone (O) is a strong oxidant that causes redox reactions and exerts anticancer effects in various types of cancer cells. However, the pathways involved in O-induced cell death are not well understood. Read More

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L. bark: an untapped bioactive source harbouring therapeutic properties for the treatment of Alzheimer's disease.

In Silico Pharmacol 2021 26;9(1):51. Epub 2021 Aug 26.

ICMR-National Institute of Traditional Medicine, Belagavi, Karnataka 590010 India.

A critical approach for target identification to detect the significant molecular mechanism of lead molecules via computational methods combined with in vitro procedures defines the modern strategy to combat untreatable diseases. Hence, the present investigation dealt to determine the effect of L. bark extract/fraction(s) over acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity followed by target identification and docking analysis of prime phytoconstituents. Read More

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Tumor NLRP3-Derived IL-1β Drives the IL-6/STAT3 Axis Resulting in Sustained MDSC-Mediated Immunosuppression.

Front Immunol 2021 31;12:661323. Epub 2021 Aug 31.

Department of Medicine, University of Colorado Denver, Aurora, CO, United States.

Tumors evade the immune system by inducing inflammation. In melanoma, tumor-derived IL-1β drives inflammation and the expansion of highly immunosuppressive myeloid-derived suppressor cells (MDSCs). Similar in many tumors, melanoma is also linked to the downstream IL-6/STAT3 axis. Read More

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Identifying transcriptional programs underlying cancer drug response with TraCe-seq.

Nat Biotechnol 2021 Sep 16. Epub 2021 Sep 16.

Department of Discovery Oncology, Genentech Inc., South San Francisco, CA, USA.

Genetic and non-genetic heterogeneity within cancer cell populations represent major challenges to anticancer therapies. We currently lack robust methods to determine how preexisting and adaptive features affect cellular responses to therapies. Here, by conducting clonal fitness mapping and transcriptional characterization using expressed barcodes and single-cell RNA sequencing (scRNA-seq), we have developed tracking differential clonal response by scRNA-seq (TraCe-seq). Read More

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September 2021

Shouting strengthens maximal voluntary force and is associated with augmented pupillary dilation.

Sci Rep 2021 Sep 16;11(1):18419. Epub 2021 Sep 16.

Graduate School of Education, The University of Tokyo, Tokyo, 113-0033, Japan.

Previous research has demonstrated that human maximal voluntary force is generally limited by neural inhibition. Producing a shout during maximal exertion effort enhances the force levels of maximal voluntary contraction. However, the mechanisms underlying this enhancement effect on force production remain unclear. Read More

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September 2021

A forward genetic screen identifies modifiers of rocaglate responsiveness.

Sci Rep 2021 Sep 16;11(1):18516. Epub 2021 Sep 16.

Department of Biochemistry, McGill University, Montreal, QC, H3G 1Y6, Canada.

Rocaglates are a class of eukaryotic translation initiation inhibitors that are being explored as chemotherapeutic agents. They function by targeting eukaryotic initiation factor (eIF) 4A, an RNA helicase critical for recruitment of the 40S ribosome (and associated factors) to mRNA templates. Rocaglates perturb eIF4A activity by imparting a gain-of-function activity to eIF4A and mediating clamping to RNA. Read More

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September 2021

A bioluminescent and homogeneous SARS-CoV-2 spike RBD and hACE2 interaction assay for antiviral screening and monitoring patient neutralizing antibody levels.

Sci Rep 2021 Sep 16;11(1):18428. Epub 2021 Sep 16.

R&D Department, Promega Corporation, Madison, WI, USA.

Here we describe a homogeneous bioluminescent immunoassay based on the interaction between Fc-tagged SARS-CoV-2 Spike RBD and human ACE2, and its detection by secondary antibodies labeled with NanoLuc luciferase fragments LgBit and SmBit. The assay utility for the discovery of novel inhibitors was demonstrated with a panel of anti-RBD antibodies, ACE2-derived miniproteins and soluble ACE2. Studying the effect of RBD mutations on ACE2 binding showed that the N501Y mutation increased RBD apparent affinity toward ACE2 tenfold that resulted in escaping inhibition by some anti-RBD antibodies. Read More

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September 2021

Bicc1 and Dicer regulate left-right patterning through post-transcriptional control of the Nodal inhibitor Dand5.

Nat Commun 2021 Sep 16;12(1):5482. Epub 2021 Sep 16.

University of Hohenheim, Institute of Biology, Department of Zoology, Stuttgart, Germany.

Rotating cilia at the vertebrate left-right organizer (LRO) generate an asymmetric leftward flow, which is sensed by cells at the left LRO margin. Ciliary activity of the calcium channel Pkd2 is crucial for flow sensing. How this flow signal is further processed and relayed to the laterality-determining Nodal cascade in the left lateral plate mesoderm (LPM) is largely unknown. Read More

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September 2021

PRMT5 regulates cell pyroptosis by silencing CASP1 in multiple myeloma.

Cell Death Dis 2021 Sep 16;12(10):851. Epub 2021 Sep 16.

Department of Hematology, The Affiliated Drum Tower Hospital of Nanjing University Medical School, Nanjing, 210008, Jiangsu, People's Republic of China.

Protein arginine methyltransferase 5 (PRMT5), a histone methyltransferase responsible for the symmetric dimethylation of histone H4 on Arg 3 (H4R3me2s), is an enzyme that participates in tumor cell progression in a variety of hematological malignancies. However, the biological functions of PRMT5 in multiple myeloma (MM) and the underlying molecular mechanisms remain unclear. In this study, we conducted a bioinformatics analysis and found that PRMT5 expression was significantly upregulated in MM. Read More

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September 2021

A Novel Selective PKR Inhibitor Restores Cognitive Deficits and Neurodegeneration in Alzheimer Disease Experimental Models.

J Pharmacol Exp Ther 2021 Sep 16;378(3):262-275. Epub 2021 Jun 16.

Neurodegeneration Cluster, Rare and Neurologic Disease Research TA (M.L.-G., N.M., E.G., C.V., V.R., D.I., L.P., V.T.), Integrated Drug Discovery (P.B., J.-F.S., D.M.), and DMPK (A.K.), Sanofi R&D, Chilly-Mazarin, France

In Alzheimer disease (AD), the double-strand RNA-dependent kinase protein kinase R (PKR )/EIF2AK2 is activated in brain with increased phosphorylation of its substrate eukaryotic initiation factor 2 (eIF2). AD risk-promoting factors, such as ApoE4 allele or the accumulation of neurotoxic amyloid- oligomers (AOs), have been associated with activation of PKR-dependent signaling. Here, we report the discovery of a novel potent and selective PKR inhibitor (SAR439883) and demonstrate its neuroprotective pharmacological activity in AD experimental models. Read More

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September 2021