194,136 results match your criteria inhibitory activity

Matairesinol, an active constituent of HC9 polyherbal formulation, exhibits HDAC8 inhibitory and anticancer activity.

Biophys Chem 2021 Apr 2;273:106588. Epub 2021 Apr 2.

Cancer Research Lab., Interactive Research School for Health Affairs (IRSHA), Bharati Vidyapeeth Deemed to be University, Pune-Satara Road, Pune 411043, Maharashtra, India. Electronic address:

Histone deacetylase 8 (HDAC8) has emerged as a promising drug target for cancer therapeutics development. HDAC8 has been reported to regulate cancer cell proliferation, invasion and promote metastasis through modulation of cell cycle associated proteins. Of late, phytocompounds have been demonstrated to exhibit anticancer and anti-HDAC8 activity. Read More

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Antimicrobial and anticancer properties of Carica papaya leaves derived di-methyl flubendazole mediated silver nanoparticles.

J Infect Public Health 2021 Feb 20;14(5):577-587. Epub 2021 Feb 20.

Department of Biotechnology, Prathyusha Engineering College, Chennai 602025, India. Electronic address:

Background: In this study, a biologically active molecule, di-methyl flubendazole isolated from the extract of Carica papaya leaves confirmed by using GC-MS, H NMR, and C NMR analysis was applied to synthesize silver nanoparticles (AgNPs). The AgNPs with plant sources an alternative therapeutic agent for synthetic compound used in cancer chemotherapy.

Methods: The AgNPs were characterized using UV, FT-IR, XRD, FESEM with EDX and TEM. Read More

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February 2021

Dysiscalarones A-E, scalarane sesterterpenoids with nitric oxide production inhibitory activity from marine sponge Dysidea granulosa.

Bioorg Chem 2021 Mar 5;111:104791. Epub 2021 Mar 5.

Research Center for Marine Drugs, State Key Laboratory of Oncogenes and Related Genes, Department of Pharmacy, Ren Ji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200127, China. Electronic address:

Dysiscalarones A-E (1-5), five new scalarane-type bishomoscalarane sesterterpenoids, were isolated from marine sponge Dysidea granulosa collected from the South China Sea, together with two known ones, honulactone A (6) and phyllofolactone I (7). The new structures were determined by extensive spectroscopic analysis including HR-ESI-MS and 1D and 2D NMR data, and their absolute configurations were assigned by single crystal X-ray diffraction analyses. The inhibitory activity of all the seven isolates on the production of nitric oxide (NO) stimulated by lipopolysaccharide (LPS) in mouse RAW 264. Read More

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Evaluation of antioxidant and inhibitory properties of Citrus aurantium L. on the acetylcholinesterase activity and the production of amyloid nano-bio fibrils.

Int J Biol Macromol 2021 Apr 10. Epub 2021 Apr 10.

Department of Biology, Rasht Branch, Islamic Azad University, Rasht, Iran. Electronic address:

The blossoms of Citrus aurantium are considered for the treatment of Alzheimer's disease because of their fragrant essential oils. The aim of this study was to investigate the antioxidant and inhibitory effects of Citrus aurantium extract on the acetylcholinesterase and production of amyloid nanobiofibrils from bovine serum albumin (BSA). The Citrus aurantium petals were harvested from Rasht city in northern IRAN. Read More

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Multidimensional population activity in an electrically coupled inhibitory circuit in the cerebellar cortex.

Neuron 2021 Apr 9. Epub 2021 Apr 9.

Department of Neuroscience, Physiology, and Pharmacology, University College London, London WC1E 6BT, UK. Electronic address:

Inhibitory neurons orchestrate the activity of excitatory neurons and play key roles in circuit function. Although individual interneurons have been studied extensively, little is known about their properties at the population level. Using random-access 3D two-photon microscopy, we imaged local populations of cerebellar Golgi cells (GoCs), which deliver inhibition to granule cells. Read More

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Study of the effect of light on follicular development in laying hens.

Anim Biosci 2021 Apr 13. Epub 2021 Apr 13.

Institute of Animal Husbandry and Veterinary, Hubei Academy of Agricultural Science, Wuhan, 430064, P. R. China.

Objective: The oxidative stress status and changes of chicken ovary tissue after shading were studied, to determine the mechanism of the effect of shading on follicular development.

Methods: Twenty healthy laying hens (40 weeks old) with uniform body weight and the same laying rate were randomly divided into two groups (the shading group and normal light group). In the shading group, the cage was covered to reduce the light intensity inside the cage to 0 without affecting ventilation or food intake. Read More

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The Natural Alkaloid Berberine Can Reduce the Number of Tolerant Cells.

J Nat Prod 2021 Apr 13. Epub 2021 Apr 13.

Department of Life and Environmental Sciences, Polytechnic University of Marche, Ancona 60131, Italy.

The eradication of recurrent (PA) lung infection in cystic fibrosis (CF) patients may be hampered by the development of persistent bacterial forms, which can tolerate antibiotics through efflux pump overexpression. After demonstrating the efflux pump inhibitory effect of the alkaloid berberine on the PA MexXY-OprM efflux pump, in this study, we tested its ability (80/320 μg/mL) to enhance tobramycin (20xMIC/1000xMIC) activity against PA planktonic/biofilm cultures. Preliminary investigations of the involvement of MexY in PA tolerance to tobramycin treatment, performed on the isogenic pair PA K767 (wild type)/K1525 (Δ) growing in planktonic and biofilm cultures, demonstrated that the Δ mutant K1525 produced a lower (100 and 10 000 times, respectively) amount of tolerant cells than that of the wild type. Read More

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Mechanisms of deoxynivalenol-induced endocytosis and degradation of tight junction proteins in jejunal IPEC-J2 cells involve selective activation of the MAPK pathways.

Arch Toxicol 2021 Apr 13. Epub 2021 Apr 13.

Department of Animal Sciences, Purdue University, 270 S. Russell St., West Lafayette, IN, 47907-2041, USA.

Mycotoxin contamination in foods is a major risk factor for human and animal health due to its prevalence in cereals and their by-products. Deoxynivalenol (DON), mainly produced by Fusarium genera, is the most common mycotoxin detected in cereal products. Deoxynivalenol disrupts intestinal barrier function and decreases protein levels of tight junction proteins (TJP). Read More

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Synthesis, α-glucosidase and α-amylase inhibitory activities, acute toxicity and molecular docking studies of thiazolidine-2,4-diones derivatives.

J Biomol Struct Dyn 2021 Apr 13:1-12. Epub 2021 Apr 13.

Laboratory of Pharmacology and Toxicology, Biopharmaceutical and Toxicological Analysis Research Team, Faculty of Medicine and Pharmacy, Mohammed V University in Rabat, Rabat, Morocco.

In the present study, a series of thiazolidine-2,4-diones derivatives () and () were synthesized and characterized by H NMR, C NMR and ESI-MS spectrometry. All compounds were screened for their α-glucosidase and α-amylase inhibitory activities. biological investigations revealed that most of compounds were active against α-glucosidase with IC values in the range of 43. Read More

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Potential antiviral activity of isorhamnetin against SARS-CoV-2 spike pseudotyped virus in vitro.

Drug Dev Res 2021 Apr 13. Epub 2021 Apr 13.

School of Pharmacy, Xi'an Jiaotong University, Xi'an, China.

Coronavirus Disease 2019 (COVID-19) cases and deaths are still rising worldwide, there is currently no effective treatment for severe inflammation and acute lung injury caused by new coronavirus (SARS-COV-2) infection. Therapies to prevent or treat COVID-19, including antiviral drug and several vaccines, are still being development. Human angiotensin-converting enzyme 2 (ACE2), expressing in lung, has been confirmed to be a receptor for SARS-COV-2 infection, interventions for attachment of spike protein of SARS-CoV-2 to ACE2 may be a potential approach to prevent viral infections and it is considered as a potential target for drug development. Read More

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Pan-coronavirus fusion inhibitors possess potent inhibitory activity against HIV-1, HIV-2, and simian immunodeficiency virus.

Emerg Microbes Infect 2021 Apr 13:1-31. Epub 2021 Apr 13.

NHC Key Laboratory of Systems Biology of Pathogens, Institute of Pathogen Biology and Center for AIDS Research, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China.

EK1 peptide is a membrane fusion inhibitor with broad-spectrum activity against human coronaviruses (CoVs). In the outbreak of COVID-19, we generated a lipopeptide EK1V1 by modifying EK1 with cholesterol, which exhibited significantly improved antiviral activity. In this study, we surprisingly found that EK1V1 also displayed potent cross-inhibitory activities against divergent HIV-1, HIV-2, and simian immunodeficiency virus (SIV) isolates. Read More

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The anti-depressant effects of a novel PDE4 inhibitor derived from resveratrol.

Pharm Biol 2021 Dec;59(1):418-423

School of Pharmacy & School of Medicine, Changzhou University, Changzhou, PR China.

Context: Resveratrol has shown anti-stress and anti-depressant-like abilities involved in inhibiting phosphodiesterase-4 (PDE4) enzyme. However, its application is limited due to its low efficacy, bioavailability and selectivity.

Objective: This study synthesized a new resveratrol derivative RES003 and evaluated its PDE4 inhibitory and anti-depressant-like activities and , respectively. Read More

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December 2021

Diphenhydramine and levofloxacin combination therapy against antimicrobial resistance in respiratory tract infections.

Future Microbiol 2021 Apr 13. Epub 2021 Apr 13.

Department of Microbiology, University of Veterinary & Animal Sciences, Lahore, Pakistan.

Antibiotics are in use since decades to treat various infections caused by Gram-positive and Gram-negative bacteria such as and . Diphenhydramine, an H1 receptor blocker possesses a weak antibiotic action but when combined with other antibiotics may potentiate their antibacterial activity. This study investigated antibacterial activity of diphenhydramine when used alone and in combination with levofloxacin against methicillin-resistant  and . Read More

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Anti-babesial potential and chemical composition of essential oil from yarrow Achillea millefolium.

Pol J Vet Sci 2021 Mar;24(1):79-84

Department of Epizootiology and Clinic of Infectious Diseases, Faculty of Veterinary Medicine, University of Life Sciences, Głęboka 30, 20-612 Lublin, Poland.

Essential oils from plants used in traditional medicine are known as a rich source of chemically diverse compounds with specific biological activities. Achillea millefolium essential oil (AEO) was screened for in vitro activity against Babesia canis. The AEO was obtained by hydrodistillation and analysed by gas chromatography coupled to mass spectrometry (GC-MS). Read More

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Effect of suberoylanilide hydroxamic acid on peripheral blood mononuclear cell cytotoxicity towards tumor cells in canines.

T Oyamada S Okano

Pol J Vet Sci 2021 Mar;24(1):35-41

Department of Small Animal Surgery 2, School of Veterinary Medicine, Kitasato University, Higashi 23-35-1, Towada, Aomori, 034-8628, Japan.

Suberoylanilide hydroxamic acid (SAHA) is a histone deacetylase inhibitor (HDACi) that suppresses the growth of tumor cells in humans and canines. SAHA reportedly enhances the antitumor activity of human peripheral blood mononuclear cell (PBMC). However, it is unclear whether a similar effect is exerted in canines. Read More

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Pathological coagulation parameters in as many as 54 patients with autoimmune acquired factor XIII deficiency due to anti-factor XIII autoantibodies.

Haemophilia 2021 Apr 12. Epub 2021 Apr 12.

Department of Molecular Patho-Biochemistry and Patho-Biology, Yamagata University School of Medicine, Yamagata, Japan.

Introduction: Autoimmune factor XIII (FXIII) deficiency (AiF13D) due to anti-FXIII autoantibodies is an extremely rare, life-threatening bleeding disorder that mostly occurs in the elderly. The number of patients diagnosed with AiF13D has been increasing in Japan, probably because of the nationwide survey on AiF13D supported by the Japanese Ministry of Health, Labour and Welfare.

Aim: To explore the pathologic characteristics of coagulation parameters in AiF13D. Read More

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Augmentation of the heat shock axis during exceptional longevity in Ames dwarf mice.

Geroscience 2021 Apr 13. Epub 2021 Apr 13.

Department of Geriatrics, School of Medicine and Health Sciences, University of North Dakota, Grand Forks, ND, 58202, USA.

How the heat shock axis, repair pathways, and proteostasis impact the rate of aging is not fully understood. Recent reports indicate that normal aging leads to a 50% change in several regulatory elements of the heat shock axis. Most notably is the age-dependent enhancement of inhibitory signals associated with accumulated heat shock proteins and hyper-acetylation associated with marked attenuation of heat shock factor 1 (HSF1)-DNA binding activity. Read More

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Characterization of an L-α,β-diaminopropionic acid polymer with comb-like structure isolated from a poly(ε-L-lysine)-producing Streptomyces sp.

Appl Microbiol Biotechnol 2021 Apr 12. Epub 2021 Apr 12.

Department of Life Science and Biotechnology, Graduate School of Science and Engineering, Kansai University, 3-3-35 Yamate-cho, Suita, Osaka, 564-8680, Japan.

Polymers of basic amino acids function as polycationic compounds under physiological conditions and exhibit intriguing biological properties, such as antimicrobial and antiviral activities, immunopotentiating ability, and DNA-binding activity. Poly(ε-L-lysine) (ε-PL) produced by some strains of Streptomyces spp. is a cationic homopolymer of L-lysine linking between ε-amino and α-carboxylic acid functional groups and has been used as a food preservative based on its biocompatibility and biodegradability. Read More

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Progesterone suppresses the progression of colonic carcinoma by increasing the activity of the GADD45α/JNK/c‑Jun signalling pathway.

Oncol Rep 2021 Jun 13;45(6). Epub 2021 Apr 13.

College of Medicine, Southwest Jiaotong University, Chengdu, Sichuan 610031, P.R. China.

Colorectal cancer (CRC) is the third most diagnosed cancer worldwide. Progesterone is associated with a decreased risk of CRC and leads to a favourable prognosis. However, the specific mechanism by which progesterone suppresses malignant progression remains to be elucidated. Read More

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Celastrol attenuates the inflammatory response by inhibiting IL‑1β expression in triple‑negative breast cancer cells.

Oncol Rep 2021 Jun 13;45(6). Epub 2021 Apr 13.

Department of Breast Cancer Center, Samsung Medical Center, Sungkyunkwan University School of Medicine, Seoul 06351, Republic of Korea.

IL‑1 promotes cancer cell proliferation and invasiveness in various malignancies, such as breast and colorectal cancer. In the present study, the functional roles of IL‑1β (IL1B) and the inhibitory effect of celastrol on IL1B expression were investigated in triple‑negative breast cancer (TNBC) cells. The data revealed that celastrol markedly decreased IL1B expression and suppressed TNBC cell proliferation in a dose‑dependent manner. Read More

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Berberine inhibits the proliferation, invasion and migration of endometrial stromal cells by downregulating miR‑429.

Mol Med Rep 2021 Jun 13;23(6). Epub 2021 Apr 13.

Institution of Traditional Chinese Medicine, Jiangxi University of Traditional Chinese Medicine, Nanchang, Jiangxi 330004, P.R. China.

Endometriosis (EM) is a common gynecological disease, and its pathological process is accompanied by the migration and proliferation of uterine cells. Berberine (BBR) has been shown to exhibit antitumor activity; however, the effects of BBR on EM have seldom been reported to date. The expression of microRNA (miR)‑429 is upregulated in EM and miR‑429 can be used as a target for drug regulation of cancer cells. Read More

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Nicotinamide riboside, an NAD precursor, attenuates inflammation and oxidative stress by activating sirtuin 1 in alcohol-stimulated macrophages.

Lab Invest 2021 Apr 12. Epub 2021 Apr 12.

Department of Nutritional Sciences, University of Connecticut, Storrs, CT, USA.

Macrophages play an essential role in alcohol-induced inflammation and oxidative stress. We investigated the effects of nicotinamide riboside (NR), a natural nicotinamide adenine dinucleotide (NAD) precursor, on alcohol-induced inflammation and oxidative stress in macrophages. NR significantly decreased ethanol-induced inflammatory gene expression, with a concomitant decrease in nuclear translocation of nuclear factor κB p65 in RAW 264. Read More

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Tick defensin γ-core reduces Fusarium graminearum growth and abrogates mycotoxins production with high efficiency.

Sci Rep 2021 Apr 12;11(1):7962. Epub 2021 Apr 12.

INRAE, Mycology and Food Safety (MycSA), 33882, Villenave d'Ornon, France.

Fusarium graminearum is a major fungal pathogen affecting crops of worldwide importance. F. graminearum produces type B trichothecene mycotoxins (TCTB), which are not fully eliminated during food and feed processing. Read More

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Multisubstituted pyrimidines effectively inhibit bacterial growth and biofilm formation of Staphylococcus aureus.

Sci Rep 2021 Apr 12;11(1):7931. Epub 2021 Apr 12.

Drug Research Program, Division of Pharmaceutical Chemistry and Technology, Faculty of Pharmacy, University of Helsinki, P.O. Box 56, (Viikinkaari 5 E), FI-00014, Helsinki, Finland.

Biofilms are multicellular communities of microorganisms that generally attach to surfaces in a self-produced matrix. Unlike planktonic cells, biofilms can withstand conventional antibiotics, causing significant challenges in the healthcare system. Currently, new chemical entities are urgently needed to develop novel anti-biofilm agents. Read More

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Design, synthesis and docking studies of novel thiazole derivatives incorporating pyridine moiety and assessment as antimicrobial agents.

Sci Rep 2021 Apr 12;11(1):7846. Epub 2021 Apr 12.

Chemistry Department, Faculty of Science, Jazan University, Jazan, Saudi Arabia.

A novel series of substituted 4,6-dimethyl-2-oxo-1-(thiazol-2-ylamino)-1,2-dihydropyridine-3-carbonitrile derivatives 6, 9, 13, 15, and 17 was synthesized in a good to excellent yield from the reaction of 1-(3-cyano-4,6-dimethyl-2-oxopyridin-1(2H)-yl)thiourea with 2-oxo-N'-arylpropanehydrazonoyl chloride, chloroacetone, α-bromoketones, ethyl chloroacetate, and 2,3-dichloroquinoxaline, respectively. The potential DNA gyrase inhibitory activity was examined using in silico molecular docking simulation. The novel thiazoles exhibit dock score values between - 6. Read More

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Prefrontal responses during proactive and reactive inhibition are differentially impacted by stress in anorexia and bulimia nervosa.

J Neurosci 2021 Apr 12. Epub 2021 Apr 12.

Department of Psychiatry, University of Cambridge, Herchel Smith Building, Addenbrooke's Hospital, Cambridge CB2 0SZ, UK.

Binge-eating is a distressing, transdiagnostic eating disorder symptom associated with impulsivity, particularly in negative mood states. Neuroimaging studies of bulimia nervosa (BN) report reduced activity in fronto-striatal regions implicated in self-regulatory control, and an influential theory posits that binge-eating results from self-regulation failures under stress. However, there is no direct evidence that psychological stress impairs self-regulation in binge-eating disorders, or that any such self-regulatory deficits generalize to binge-eating in underweight individuals (i. Read More

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New dammarane-type glycosides from Gynostemma pentaphyllum and their lipid-lowering activity.

Bioorg Chem 2021 Apr 1;111:104843. Epub 2021 Apr 1.

Department of Natural Medicinal Chemistry, School of TCM & State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 211198, PR China. Electronic address:

Gynostemma pentaphyllum (Thunb.) Makino has a long history as food and diary supplement in China. At present, there are some products for hyperlipidemia in the market, including G. Read More

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Design, synthesis, modelling studies and biological evaluation of 1,3,4-oxadiazole derivatives as potent anticancer agents targeting thymidine phosphorylase enzyme.

Bioorg Chem 2021 Mar 29;111:104873. Epub 2021 Mar 29.

Shobhaben Pratapbhai Patel School of Pharmacy Technology Management, SVKM's NMIMS, Mumbai, India. Electronic address:

A series of novel 1,3,4-oxadiazole derivatives with substituted phenyl ring were designed and synthesized with an objective of discovering newer anti-cancer agents targeting thymidine phosphorylase enzyme (TP). The 1,3,4-oxadiazole derivatives were synthesized by simple and convenient methods in the lab. Chemical structure of the all the synthesized compounds were characterized by IR, H NMR and mass spectral methods and evaluated for cytotoxicity by MTT method against two breast cancer cell lines (MCF-7 and MDA-MB-231). Read More

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Antifungal activity and potential mechanism of Asiatic acid alone and in combination with fluconazole against Candida albicans.

Biomed Pharmacother 2021 Apr 10;139:111568. Epub 2021 Apr 10.

Department of Clinical Pharmacy, The First Affiliated Hospital of Shandong First Medical University & Shandong Provincial Qianfoshan Hospital, Shandong Engineering and Technology Research Center for Pediatric Drug Development, Shandong Medicine and Health Key Laboratory of Clinical Pharmacy, Jinan, Shandong Province 250014, People's Republic of China. Electronic address:

Candida albicans (C. albicans) infection remains a challenge to clinicians due to the limited available antifungals. With the widespread use of antifungals in the clinic, the drug resistance has been emerging continuously, especially fluconazole. Read More

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On-cell saturation transfer difference NMR for the identification of FimH ligands and inhibitors.

Bioorg Chem 2021 Mar 29;112:104876. Epub 2021 Mar 29.

BioOrg NMR Lab, Department of Biotechnology and Biosciences, University of Milano-Bicocca, P.zza della Scienza, 2, 20126 Milan, Italy. Electronic address:

We describe the development of an on-cell NMR method for the rapid screening of FimH ligands and the structural identification of ligand binding epitopes. FimH is a mannose-binding bacterial adhesin expressed at the apical end of type 1 pili of uropathogenic bacterial strains and responsible for their d-mannose sensitive adhesion to host mammalian epithelial cells. Because of these properties, FimH is a key virulence factor and an attractive therapeutic target for urinary tract infection. Read More

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