32,545 results match your criteria strong inhibition

In vitro and in vivo anti-Helicobacter pylori activity of selected medicinal plants employed for the management of gastrointestinal disorders.

Pak J Pharm Sci 2020 Nov;33(6(Supplementary)):2809-2814

Department of Basic Medical Sciences, College of Medicine, King Saud bin Abdulaziz University of Health Sciences, Jeddah, KSA.

Five medicinal plants Mentha piperita L., Trachyspermum ammi L., Viola odorata Linn. Read More

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November 2020

The bone microenvironment increases phenotypic plasticity of ER breast cancer cells.

Dev Cell 2021 Apr;56(8):1100-1117.e9

Lester and Sue Smith Breast Center, Baylor College of Medicine, One Baylor Plaza, Houston, TX 77030, USA; Dan L. Duncan Cancer Center, Baylor College of Medicine, One Baylor Plaza, Houston, TX 77030, USA; Department of Molecular and Cellular Biology, Baylor College of Medicine, One Baylor Plaza, Houston, TX 77030, USA; McNair Medical Institute, Baylor College of Medicine, BCM600, One Baylor Plaza, Houston, TX 77030, USA. Electronic address:

Estrogen receptor-positive (ER) breast cancer exhibits a strong bone tropism in metastasis. How the bone microenvironment (BME) impacts ER signaling and endocrine therapy remains poorly understood. Here, we discover that the osteogenic niche transiently and reversibly reduces ER expression and activities specifically in bone micrometastases (BMMs), leading to endocrine resistance. Read More

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A crystallography-based investigation of weak interactions for drug design against COVID-19.

Phys Chem Chem Phys 2021 Mar 22;23(12):7261-7270. Epub 2021 Mar 22.

Department of Chemistry, Lady Brabourne College, Kolkata - 700017, India.

Interactions between proteins and small molecules play important roles in the inhibition of protein function. However, a lack of proper knowledge about non-covalent interactions can act as a barrier towards gaining a complete understanding of the factors that control these associations. To find effective molecules for COVID-19 inhibition, we have quantitatively investigated 143 X-ray crystal structures of the SARS-CoV-2 M protein of coronavirus with covalently or non-covalently bound small molecules (SMs). Read More

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Acclimation of photosystem II in a cyanobacterium and a eukaryotic green alga to high and fluctuating photosynthetic photon flux densities, simulating light regimes induced by mixing in lakes.

New Phytol 1994 Nov;128(3):407-424

Laboratory for Microbiology, University of Amsterdam, Nieuwe Achtergracht 127 1018 WS Amsterdam, The Netherlands.

Photoacclimation of Scenedesmus protuberans Fritsch and Microcystis aeruginosa Kützing emend. Elenkin to high and fluctuating PPFD was studied in continuous cultures with computer-controlled variable light regimes. The aim of the work was to provide a better understanding of species-specific acclimation to high PPFD (as encountered by cyanobacteria in surface waterblooms), and of suppression of the growth of colony-forming cyanobacteria during periods of prolonged mixing in lakes. Read More

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November 1994

Design, synthesis, and biological evaluation of new pyrimidine-5-carbonitrile derivatives bearing 1,3-thiazole moiety as novel anti-inflammatory EGFR inhibitors with cardiac safety profile.

Bioorg Chem 2021 Apr 8;111:104890. Epub 2021 Apr 8.

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt. Electronic address:

A new series of pyrimidine-5-carbonitrile derivatives 8a-p carrying the 1,3-thiazole moiety has been designed and synthesized as novel anti-inflammatory EGFR inhibitors with cardiac and gastric safety profiles. 8a-p have been assessed for their inhibitory activity against COX-1/COX-2 activity. Compounds 8h, 8n, and 8p were found to be potent and selective COX-2 inhibitors (IC = 1. Read More

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Noncovalent Functionalized Graphene Nanocarriers from Graphite for Treating Thyroid Cancer Cells.

ACS Biomater Sci Eng 2021 Apr 19. Epub 2021 Apr 19.

Department of Applied Chemistry, School of Engineering, Kyungpook National University, Buk-gu, Daehak-ro 80, Daegu 41566, Republic of Korea.

Here, biocompatible graphene (G) nanocarriers decorated with iron oxide nanoparticles (IONPs) were prepared using 2-(methacryloyloxy)ethyl phosphorylcholine (MPC) and poly(ethylene glycol) monomethacrylate (PEGMA). For this, we report the use of graphite directly instead of graphene oxide or reduced graphene oxide. Graphene nanocarrier ( GIOPMPC) was prepared in one-pot by copolymerization of MPC and PEGMA monomers in the presence of IONPs and G. Read More

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Competitive binding of STATs to receptor phospho-Tyr motifs accounts for altered cytokine responses.

Elife 2021 Apr 19;10. Epub 2021 Apr 19.

Division of Cell Signaling and Immunology, School of Life Sciences, University of Dundee, Dundee, United Kingdom.

Cytokines elicit pleiotropic and non-redundant activities despite strong overlap in their usage of receptors, JAKs and STATs molecules. We use IL-6 and IL-27 to ask how two cytokines activating the same signaling pathway have different biological roles. We found that IL-27 induces more sustained STAT1 phosphorylation than IL-6, with the two cytokines inducing comparable levels of STAT3 phosphorylation. Read More

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Aflatoxin B1 inhibited autophagy flux by inducing lysosomal alkalinization in HepG2 cells.

Toxicol Mech Methods 2021 Apr 18:1-7. Epub 2021 Apr 18.

College of Food Science and Engneering, Jilin University, Changchun, People's Republic of China.

Aflatoxin B1 (AFB1) is a hazard food pollutant and the most toxic one of all the aflatoxins. It is mainly metabolized in the liver and exerts strong hepatotoxicity and carcinogenesis. Autophagy is an important biological process to maintain the homeostasis of intracellular environment. Read More

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A Highly Specific Multiple Enhancement Theranostic Nanoprobe for PET/MRI/PAI Image-Guided Radioisotope Combined Photothermal Therapy in Prostate Cancer.

Small 2021 Apr 18:e2100378. Epub 2021 Apr 18.

Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), Department of Nuclear Medicine, Peking University Cancer Hospital and Institute, Beijing, 100142, China.

An integrated molecular probe for combined tumor-targeted multimodal imaging and therapy in the era of precision medicine requires a multiplexed platform that simultaneously has high targeting specificity, versatile conjugation capability, and biocompatibility. Here, a novel biocompatible melanin nanoprobe (PMNs-II-813) coupled with a highly specific prostate-specific membrane antigen small molecule inhibitor is developed for the targeted multimodal diagnosis and treatment of prostate cancer. The melanin nanoparticles demonstrate photoacoustic imaging and photothermal therapy (PTT) functionalities via strong near-infrared absorption. Read More

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A Bisphosphonate With a Low Hydroxyapatite Binding Affinity Prevents Bone Loss in Mice After Ovariectomy and Reverses Rapidly With Treatment Cessation.

JBMR Plus 2021 Apr 3;5(4):e10476. Epub 2021 Mar 3.

Department of Biomedical Engineering The City College of New York New York NY USA.

Bisphosphonates (BPs) are a mainstay of osteoporosis treatment; however, concerns about bone health based on oversuppression of remodeling remain. Long-term bone remodeling suppression adversely affects bone material properties with microdamage accumulation and reduced fracture toughness in animals and increases in matrix mineralization and atypical femur fractures in patients. Although a "drug holiday" from BPs to restore remodeling and improve bone quality seems reasonable, clinical BPs have long functional half-lives because of their high hydroxyapatite (HAP) binding affinities. Read More

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Inhibition of Chikungunya Virus Infection by 4-Hydroxy-1-Methyl-3-(3-morpholinopropanoyl)quinoline-2(1)-one (QVIR) Targeting nsP2 and E2 Proteins.

ACS Omega 2021 Apr 31;6(14):9791-9803. Epub 2021 Mar 31.

Molecular Virology Laboratory, Centre for Interdisciplinary Research in Basic Sciences, Jamia Millia Islamia, New Delhi 110025, India.

The re-emergence of Chikungunya virus (CHIKV) infection in humans with no approved antiviral therapies or vaccines is one of the major problems with global significance. In the present investigation, we screened 80 in-house quinoline derivatives for their anti-CHIKV activity by computational techniques and found 4-hydroxy-1-methyl-3-(3-morpholinopropanoyl)quinoline-2(1)-one (QVIR) to have potential binding affinities with CHIKV nsP2 and E2 glycoproteins. QVIR was evaluated for its anti-CHIKV potential. Read More

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β-asarone suppresses HCT116 colon cancer cell proliferation and liver metastasis in part by activating the innate immune system.

Oncol Lett 2021 Jun 31;21(6):435. Epub 2021 Mar 31.

Central Laboratory, Jiangsu Province Hospital of Chinese Medicine, Affiliated Hospital of Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210029, P.R. China.

Studies have revealed that β-asarone exerts a powerful inhibitory effect on the proliferation of human cancer cells. The authors' previous study demonstrated that β-asarone could induce LoVo colon cancer cell apoptosis and , indicating its anticancer properties. The present study aimed to determine the antineoplastic effect of β-asarone in HCT116 colon cancer cells. Read More

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Polyene-Producing spp. From the Fungus-Growing Termite Exhibit High Inhibitory Activity Against the Antagonistic Fungus .

Front Microbiol 2021 1;12:649962. Epub 2021 Apr 1.

State Key Laboratory of Microbial Technology, Microbial Technology Institute, Shandong University, Qingdao, China.

Fungus-growing termites are engaged in a tripartite mutualism with intestinal microbes and a monocultivar ( sp.) in the fungus garden. The termites are often plagued by entomopathogen () and fungus garden is always threatened by competitors ( spp. Read More

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Theaflavin protects against oxalate calcium-induced kidney oxidative stress injury via upregulation of SIRT1.

Int J Biol Sci 2021 2;17(4):1050-1060. Epub 2021 Mar 2.

Department of Urology, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.

Renal tubular cell injury induced by calcium oxalate (CaOx) is a critical initial stage of kidney stone formation. Theaflavin (TF) has been known for its strong antioxidative capacity; however, the effect and molecular mechanism of TF against oxidative stress and injury caused by CaOx crystal exposure in kidneys remains unknown. To explore the potential function of TF on renal crystal deposition and its underlying mechanisms, experiments were conducted using a CaOx nephrocalcinosis mouse model established by glyoxylate intraperitoneal injection, and HK-2 cells were subjected to calcium oxalate monohydrate (COM) crystals, with or without the treatment of TF. Read More

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In-silico pharmacophoric and molecular docking-based drug discovery against the Main Protease (Mpro) of SARS-CoV-2, a causative agent COVID-19.

Pak J Pharm Sci 2020 Nov;33(6):2697-2705

Centre for Agricultural Biochemistry and Biotechnology (CABB), University of Agriculture Faisalabad (UAF), Faisalabad, Pakistan.

COVID-19 (Coronavirus Disease 2019) caused by a novel 'SARS-CoV-2' virus resulted in public health emergencies across the world. An effective vaccine to cure this virus is not yet available, thus requires concerted efforts at various scales. In this study, we employed Computer-Aided Drug Design (CADD) based approach to identify the drug-like compounds - inhibiting the replication of the main protease (M) of SARS-CoV-2. Read More

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November 2020

Myricetin protects natural killer cells from arsenite induced DNA damage by attenuating oxidative stress and retaining poly(ADP-Ribose) polymerase 1 activity.

Mutat Res 2021 May 19;865:503337. Epub 2021 Feb 19.

East China University of Science and Technology, State Key Laboratory of Bioreactor Engineering, Shanghai, 200237, China; East China University of Science and Technology, School of Pharmacy, Department of Pharmaceutical Sciences, Shanghai, 200237, China; Department of Pharmacology and Toxicology and BIO5 Institute, University of Arizona, Tucson, AZ, 85721-0207, USA. Electronic address:

Environmental exposure to arsenite (As) is known to induce immunotoxicity. Natural killer (NK) cells are innate lymphoid cells act as professional killers of tumor cells. Our previous report indicated that 500 ppb As drinking water exposure induced significant DNA damage in the NK cells of C57BL/6 mice. Read More

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Synthesis and evaluation of N-(4-(substituted)-3-(trifluoromethyl) phenyl) isobutyramides and their N-ethyl analogous as anticancer, anti-angiogenic & antioxidant agents: In vitro and in silico analysis.

Comput Biol Chem 2021 Apr 8;92:107484. Epub 2021 Apr 8.

Department of Biotechnology, Savitribai Phule Pune University, Pune, 411007, MS, India. Electronic address:

N-(4-(substituted)-3-(trifluoromethyl) phenyl) isobutyramides and their N-ethyl analogues (flutamides) are versatile scaffolds with a wide spectrum of biological activities. A series of new N-(4-(substituted)-3-(trifluoromethyl) phenyl) isobutyramides (8a-t) and their N-ethyl analogous (9a-t) were synthesized and characterized. The inhibitory potential of the synthesized compounds on the viability of three human cancer cell lines HEP3BPN 11 (liver), MDA-MB 453 (breast), and HL 60 (leukemia) were assessed. Read More

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Metabolome and lipidome derangements during a severe mast cell activation event in a patient with indolent systemic mastocytosis.

J Allergy Clin Immunol 2021 Apr 14. Epub 2021 Apr 14.

Department of Clinical Pharmacology, Medical University of Vienna, Waehringer Guertel 18-20, 1090 Vienna, Austria.

Background: The number of mast cells in various organs is manifold elevated in individuals with systemic mastocytosis. Degranulation can lead to life-threatening symptomatology. No data have been published about the alterations of the metabolome and lipidome during an attack. Read More

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A new prenylated benzoquinone from Cyathocalyx pruniferus abrogates LPS-induced inflammatory responses associated with PGE, COX-2 and cytokines biosynthesis in human plasma.

Inflammopharmacology 2021 Apr 17. Epub 2021 Apr 17.

Faculty of Pharmacy, MAHSA University, Bandar Saujana Putra, 42610, Jenjarom, Selangor, Malaysia.

In our previous laboratory findings, Cyathocalyx pruniferus extracts exhibited platelet-activating factor inhibition, suggesting their anti-inflammatory potential. Hence, this study was designed with the aim to isolate phyto-constituents from C. pruniferus with potent anti-inflammatory activities. Read More

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Design, synthesis and biological evaluation of N-substituted indole-thiazolidinedione hybrid analogues as potential pancreatic lipase inhibitors.

Chem Biol Drug Des 2021 Apr 16. Epub 2021 Apr 16.

Laboratory of Natural Product Chemistry, Department of Pharmacy, Birla Institute of Technology and Science, Pilani (BITS Pilani), Pilani Campus, Pilani - 333 031, Rajasthan, India.

Pancreatic Lipase (PL) is a key enzyme responsible for 50-70% of dietary triglycerides, hence its inhibition is considered as a viable approach for the management of obesity. A series of indole-TZD hybrid analogues were synthesised, characterised, and evaluated for their PL inhibitory activity. Knoevenagel condensation of various substituted indole-3-carboxaldehyde with substituted thiazolidinediones resulted in the formation of titled analogues. Read More

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Strigolactone mimic 2-nitrodebranone is highly active in Arabidopsis growth and development.

Plant J 2021 Apr 15. Epub 2021 Apr 15.

Shenzhen Branch, Guangdong Laboratory for Lingnan Modern Agriculture, Genome Analysis Laboratory of the Ministry of Agriculture, Agricultural Genomics Institute at Shenzhen, Chinese Academy of Agricultural Sciences, Shenzhen, 518124, China.

Strigolactones play crucial roles in regulating plant architecture and development as endogenous hormones and orchestrating symbiotic interactions with fungi and parasitic plants as components of root exudates. rac-GR24 is currently the most widely used strigolactone analog and serves as a reference compound in investigating the action of strigolactones. In this study, we evaluated a suite of debranones and found that 2-nitrodebranone (2NOD) exhibited higher biological activity than rac-GR24 in various aspects of plant growth and development in Arabidopsis, including hypocotyl elongation inhibition, root hair promotion, and senescence acceleration. Read More

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Compensatory Transition of Bile Acid Metabolism from Fecal Disposition of Secondary Bile Acids to Urinary Excretion of Primary Bile Acids Underlies Rifampicin-Induced Cholestasis in Beagle Dogs.

ACS Pharmacol Transl Sci 2021 Apr 22;4(2):1001-1013. Epub 2021 Mar 22.

Key Laboratory of Drug Targeting and Drug Delivery System, Ministry of Education, West China School of Pharmacy, Sichuan University, No. 17 People's South Road, Chengdu 610041, China.

Drug induced cholestasis (DIC) is complexly associated with dysbiosis of the host-gut microbial cometabolism of bile acids (BAs). Murine animals are not suitable for transitional studies because the murine BA metabolism is quite different from human metabolism. In this work, the rifampicin (RFP) induced cholestasis was established in beagle dogs that have a humanlike BA profile to disclose how RFP affects the host-gut microbial cometabolism of BAs. Read More

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Highly Efficient Water-Soluble Photosensitizer Based on Chlorin: Synthesis, Characterization, and Evaluation for Photodynamic Therapy.

ACS Pharmacol Transl Sci 2021 Apr 4;4(2):802-812. Epub 2021 Feb 4.

National Engineering Laboratory for Resource Development of Endangered Crude Drugs in Northwest China, The Key Laboratory of Medicinal Resources and Natural Pharmaceutical Chemistry, The Ministry of Education, College of Life Sciences, Shaanxi Normal University, Xi'an, Shaanxi 710119, The People's Republic of China.

The clinical applications of many photosensitizers (PSs) are limited because of their poor water solubility, weak tissue penetration, low chemical purity, and severe toxicity in the absence of light. We designed a novel chlorin-based PS (designated as HPS) to achieve fluorescence image-guided photodynamic therapy (PDT) with efficient ROS generation. In addition to its simple fabrication process, HPS has other advantages such as excellent water solubility, strong NIR absorption, and high biocompatibility upon chemical functionalization for enhanced phototherapy. Read More

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Kinomic profile in patient-derived glioma cells during hypoxia reveals c-MET-PI3K dependency for adaptation.

Theranostics 2021 5;11(11):5127-5142. Epub 2021 Mar 5.

School of Biological Sciences, Nanyang Technological University Singapore, Singapore 637551, Singapore.

Hypoxic microenvironment is a hallmark of solid tumors, especially glioblastoma. The strong reliance of glioma-propagating cells (GPCs) on hypoxia-induced survival advantages is potentially exploitable for drug development. To identify key signaling pathways for hypoxia adaptation by patient-derived GPCs, we performed a kinase inhibitor profiling by screening 188 small molecule inhibitors against 130 different kinases in normoxia and hypoxia. Read More

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One-pot synthesis of zinc oxide nanoparticles via chemical precipitation for bromophenol blue adsorption and the antifungal activity against filamentous fungi.

Sci Rep 2021 Apr 15;11(1):8305. Epub 2021 Apr 15.

Department of Chemistry, University of the Free State, Bloemfontein, South Africa.

In this research, zinc oxide nanoparticles (ZnONPs) were prepared via a facile one-pot chemical precipitation approach and applied in the adsorption of bromophenol blue (BRB) and as antifungal agents against the filamentous fungi and plant pathogens; Alternaria alternata CGJM3078, Alternaria alternata CGJM3006 and Fusarium verticilliodes CGJM3823. The ZnONPs were characterized by the UV-Vis, FTIR, XRD, TGA, BET, SEM, TEM, and EDX techniques, which showed efficient synthesis. The characteristics ZnO UV-Vis absorption band was observed at 375 nm, while the XRD showed an average ZnONPs crystalline size of 47. Read More

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Interleukin-37 regulates innate immune signaling in human and mouse colonic organoids.

Sci Rep 2021 Apr 15;11(1):8206. Epub 2021 Apr 15.

Department of Pediatrics, BC Children's Hospital, University of British Columbia, Vancouver, BC, Canada.

Intestinal epithelial cells (IEC) reside in close proximity to the gut microbiota and are hypo-responsive to bacterial products, likely to prevent maladaptive inflammatory responses. This is in part due to their strong expression of Single Ig IL-1 related receptor (SIGIRR), a negative regulator of interleukin (IL)-1 and toll-like receptor signaling. IL-37 is an anti-inflammatory cytokine that inhibits innate signaling in diverse cells by signaling through SIGIRR. Read More

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A purified acidic polysaccharide from Sarcandra glabra as vaccine adjuvant to enhance anti-tumor effect of cancer vaccine.

Carbohydr Polym 2021 Jul 19;263:117967. Epub 2021 Mar 19.

Jiangsu Key Laboratory of Druggability of Biopharmaceuticals and State Key Laboratory of Natural Medicines, School of Life Science and Technology, China Pharmaceutical University, Nanjing, 210009, China. Electronic address:

Immunological adjuvants are an important part of tumor vaccines and are critical for stimulating anti-tumor immune responses. However, the clinical needs of strong adjuvants have not been met. In this work, we found that the purified acidic polysaccharide from Sarcandra glabra, named p-SGP, is an ideal adjuvant for tumor vaccines. Read More

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Assessing the aquatic toxicity and environmental safety of tracer compounds Rhodamine B and Rhodamine WT.

Water Res 2021 Apr 5;197:117109. Epub 2021 Apr 5.

Department of Environmental Engineering, Technical University of Denmark, Bygningstorvet, Building 115, DK-2800 Kgs. Lyngby, Denmark.

Tracer tests represent a well-established method for delineating key environmental processes in various media and engineered systems. Tracers like Rhodamine B and WT are frequently applied due to their strong fluorescence even at low concentrations.. Read More

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Design, synthesis and biological evaluation of novel pleuromutilin derivatives as potent anti-MRSA agents targeting the 50S ribosome.

Bioorg Med Chem 2021 Apr 2;38:116138. Epub 2021 Apr 2.

Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou 510642, China; Guangdong Laboratory for Lingnan Modern Agriculture, Guangzhou 510642, China. Electronic address:

A series of novel pleuromutilin derivatives were designed and synthesized with 1,2,4-triazole as the linker connected to benzoyl chloride analogues under mild conditions. The in vitro antibacterial activities of the synthesized derivatives against four strains of Staphylococcus aureus (MRSA ATCC 43300, ATCC 29213, AD3 and 144) were tested by the broth dilution method. Most of the synthesized derivatives displayed potent activities, and 22-(3-amino-2-(4-methyl-benzoyl)-1,2,4-triazole-5-yl)-thioacetyl)-22-deoxypleuromutilin (compound 12) was found to be the most active antibacterial derivative against MRSA (MIC = 0. Read More

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Luteolin and apigenin derived glycosides from Alphonsea elliptica abrogate LPS-induced inflammatory responses in human plasma.

J Ethnopharmacol 2021 Apr 12:114120. Epub 2021 Apr 12.

College of Pharmacy, University of Punjab, Allama Iqbal Campus, Mall Road Lahore, Pakistan. Electronic address:

Ethnopharmacological Relevance: Numerous Alphonsea species including Alphonsea elliptica (mempisang) leaves and fruits are indigenously used in inflammatory conditions such as postpartum swelling and rheumatism in southeast Asian countries. In our previous in-vitro findings, A. elliptica methanol extract exhibited platelet-activating factor inhibition, suggesting the presence of phyto-constituents with anti-inflammatory potential. Read More

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