158,201 results match your criteria mechanism action

Placental Angiogenesis in Mammals: A Review of the Regulatory Effects of Signaling Pathways and Functional Nutrients.

Adv Nutr 2021 Jun 24. Epub 2021 Jun 24.

Guangdong Laboratory of Lingnan Modern Agriculture, Guangdong Provincial Key Laboratory of Animal Nutrition Control, and National Engineering Research Center for Breeding Swine Industry, College of Animal Science, South China Agricultural University, Guangzhou, China.

Normal placental development and proper angiogenesis are essential for fetal growth during pregnancy. Angiogenesis involves the regulatory action of many angiogenic factors and a series of signal transduction processes inside and outside the cell. The obstruction of placental angiogenesis causes fetal growth restriction and serious pregnancy complications, even leading to fetal loss and pregnancy cessation. Read More

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Ameliorating effect on glycolipid metabolism and chemical profile of Millettia speciosa champ. extract.

J Ethnopharmacol 2021 Jun 21:114360. Epub 2021 Jun 21.

Center for Drug Research and Development, Guangdong Pharmaceutical University, Guangzhou, 510006, China. Electronic address:

Ethnopharmacological Relevance: Millettia speciosa Champ., also called Niu dali, is a fabaceous medicinal plant mainly distributed in southeast China, where it is a functional food for developing physical strength, and often used traditionally in medicinal treatment of numbness of the wrists, diabetes, hepatitis, and so on.

Aim Of The Study: To investigate the chemical profile, ameliorating effects of MSC on glycolipid metabolism in diabetic mice and to identify the possible mechanism of action. Read More

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Cedrus deodara (Roxb. ex D.Don) G.Don: A review of traditional use, phytochemical composition and pharmacology.

J Ethnopharmacol 2021 Jun 21:114361. Epub 2021 Jun 21.

Department of Pharmacy, Banasthali Vidyapith, Banasthali, Rajasthan, India. Electronic address:

Ethnopharmacological Relevance: Cedrus deodara (Roxb. ex D.Don) G. Read More

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A comprehensive review of herbacetin: From chemistry to pharmacological activities.

J Ethnopharmacol 2021 Jun 21:114356. Epub 2021 Jun 21.

School of Traditional Chinese Medicine, Southern Medical University, Guangzhou, 510515, China; Guangzhou Provincial Key Laboratory of Chinese Medicine Pharmaceutics, Guangzhou, 510515, China; Guangdong Provincial Engineering Laboratory of Chinese Medicine Preparation, Technology, Guangzhou, 510515, China. Electronic address:

Ethnopharmacological Relevance: Herbacetin is an active constituent of traditional Chinese medicines such as Ephedra sinica Stapf (MaHuang) and Sedum roseum (L.). Scop. Read More

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Antagonistic fungal enterotoxins intersect at multiple levels with host innate immune defences.

PLoS Genet 2021 Jun 24;17(6):e1009600. Epub 2021 Jun 24.

Aix Marseille Univ, CNRS, INSERM, CIML, Turing Centre for Living Systems, Marseille, France.

Animals and plants need to defend themselves from pathogen attack. Their defences drive innovation in virulence mechanisms, leading to never-ending cycles of co-evolution in both hosts and pathogens. A full understanding of host immunity therefore requires examination of pathogen virulence strategies. Read More

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[Efficacy of combination of needle extract, hesperidin and vitamin C in treatment of chronic venous diseases].

Angiol Sosud Khir 2021 ;27(2):82-91

Laboratory of Physiology of Visceral Systems named after K.M. Bykov, Institute of Experimental Medicine, Saint Petersburg, Russia.

Background: In Russia, physicians are virtually unaware of drugs based on needle extract. However, abroad, saponins and, in particular, a combined preparation containing needle extract, hesperidin and vitamin C is one of drugs of choice, if not the leading medication in treatment of venous oedemas and other venous symptoms.

Aim: The authors conducted a systematic review of the Russian-and English-language literature using the following search terms: saponins, hesperidin, needle, ruscus, ruscogenin (and their Russian equivalents), each of which was entered in a combination with the word 'venous' or its Russian equivalent, respectively. Read More

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January 2021

Mechanistic Insights into the Allosteric Inhibition of Androgen Receptors by Binding Function 3 Antagonists from an Integrated Molecular Modeling Study.

J Chem Inf Model 2021 Jun 24. Epub 2021 Jun 24.

Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States.

An androgen receptor (AR) is an intensively studied treatment target for castration-resistant prostate cancer that is irresponsive to conventional antiandrogen therapeutics. Binding function 3 (BF3) inhibitors with alternative modes of action have emerged as a promising approach to overcoming antiandrogen resistance. However, how these BF3 inhibitors modulate AR function remains elusive, hindering the development of BF3-targeting agents. Read More

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[Empagliflozin in the elderly].

Geriatr Psychol Neuropsychiatr Vieil 2021 Jun;19(2):137-147

Service de gériatrie, Hôpitaux Universitaires Paris Centre, Hôpital Broca, APHP, Paris, France, EA 4468, Université de Paris, France.

Glucose and sodium tubular reabsorption inhibitors, or gliflozins, are a new therapeutic class. Their novel mechanism of action involves inhibition of a glucose and Na+ reabsorption co-transporter in the renal proximal tubule. They reduce blood glucose levels by reducing renal glucose reabsorption. Read More

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Antiproliferative properties of 7,8-Ethylene Diamine Chelator-Lipophilic Fluoroquinolone Derivatives Against colorectal cancer Cell Lines.

Anticancer Agents Med Chem 2021 Jun 23. Epub 2021 Jun 23.

School of Pharmacy, University of Jordan, Queen Rania Street, Amman 11942, Jordan.

Background: Cancer is one of the most overwhelming diseases nowadays. It is considered the second cause of death after cardiovascular diseases. Due to the diversity of its types, stages, and genetic origin, there is no available drug to treat all cancers. Read More

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Nodakenin represses obesity and its complications via the inhibition of the VLDLR signalling pathway in vivo and in vitro.

Cell Prolif 2021 Jun 24:e13083. Epub 2021 Jun 24.

Department of Pharmacology, College of Korean Medicine, Sangji University, Wonju, Korea.

Objectives: Nodakenin (NK) is a coumarin glucoside that is found in the roots of Angelicae gigas. A limited number of studies have been conducted on the pharmacological activities of NK. Although NK is an important natural resource having anti-inflammatory and antioxidant effects, no investigation has been conducted to examine the effects of NK on obesity and obesity-induced inflammation. Read More

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Inhibition of lncRNA plays a protective role in hypoxia-ischemia-reoxygenation-induced myocardial injury by regulating miR-335 and RASA1 expression.

Mol Med Rep 2021 Aug 24;24(2). Epub 2021 Jun 24.

Department of Cardiology, Jiangxi Provincial People's Hospital Affiliated to Nanchang University, Nanchang, Jiangxi 330006, P.R. China.

Long non‑coding (lnc)RNAs serve a role in a number of diseases, including different types of cancer and acute myocardial infarction. The aim of the present study was to investigate the protective role of lncRNA small nucleolar RNA host gene 8 in hypoxia‑ischemia‑reoxygenation (HI/R)‑induced myocardial injury and its potential mechanism of action. Cell viability, proliferation, creatine kinase myocardial band, cell apoptosis and protein expression levels were determined by Cell Counting Kit‑8 assay, EdU assay, ELISA, flow cytometry and western blotting, respectively. Read More

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Phase 1 study of safety, pharmacokinetics, and pharmacodynamics of tivantinib in combination with bevacizumab in adult patients with advanced solid tumors.

Cancer Chemother Pharmacol 2021 Jun 23. Epub 2021 Jun 23.

Division of Hematology/Oncology, Department of Medicine, University of Pittsburgh School of Medicine, Pittsburgh, PA, USA.

Purpose: We investigated the combination of tivantinib, a c-MET tyrosine kinase inhibitor (TKI), and bevacizumab, an anti-VEGF-A antibody.

Methods: Patients with advanced solid tumors received bevacizumab (10 mg/kg intravenously every 2 weeks) and escalating doses of tivantinib (120-360 mg orally twice daily). In addition to safety and preliminary efficacy, we evaluated pharmacokinetics of tivantinib and its metabolites, as well as pharmacodynamic biomarkers in peripheral blood and skin. Read More

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Study of the Active Components and Molecular Mechanism of in the Treatment of Diabetic Nephropathy.

Front Mol Biosci 2021 7;8:664416. Epub 2021 Jun 7.

Graduate School, First Affiliated Hospital of Tianjin University of Traditional Chinese Medicine, Tianjin, China.

We aimed to explore the active ingredients and molecular mechanism of (TW) in the treatment of diabetic nephropathy (DN) through network pharmacology and molecular biology. First, the active ingredients and potential targets of TW were obtained through the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP) and related literature materials, and Cytoscape 3.7. Read More

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Click activated protodrugs against cancer increase the therapeutic potential of chemotherapy through local capture and activation.

Chem Sci 2021 Jan 5;12(4):1259-1271. Epub 2021 Jan 5.

University at Albany, SUNY 1400 Washington Ave., LS-1136 Albany NY 12222 USA

A desired goal of targeted cancer treatments is to achieve high tumor specificity with minimal side effects. Despite recent advances, this remains difficult to achieve in practice as most approaches rely on biomarkers or physiological differences between malignant and healthy tissue, and thus benefit only a subset of patients in need of treatment. To address this unmet need, we introduced a Click Activated Protodrugs Against Cancer (CAPAC) platform that enables targeted activation of drugs at a specific site in the body, , a tumor. Read More

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January 2021

Anticancer gold(iii)-bisphosphine complex alters the mitochondrial electron transport chain to induce tumor inhibition.

Chem Sci 2021 Apr 29;12(21):7467-7479. Epub 2021 Apr 29.

Department of Chemistry, University of Kentucky Lexington KY 40506 USA

Expanding the chemical diversity of metal complexes provides a robust platform to generate functional bioactive reagents. To access an excellent repository of metal-based compounds for probe/drug discovery, we capitalized on the rich chemistry of gold to create organometallic gold(iii) compounds by ligand tuning. We obtained novel organogold(iii) compounds bearing a 1,2-bis(diphenylphosphino)benzene ligand, providing structural diversity with optimal physiological stability. Read More

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Design, scope and mechanism of highly active and selective chiral NHC-iridium catalysts for the intramolecular hydroamination of a variety of unactivated aminoalkenes.

Chem Sci 2021 Feb 1;12(10):3751-3767. Epub 2021 Feb 1.

Department of Chemistry, School of Molecular Sciences, University of Western Australia M310, 35 Stirling Highway 6009 Perth WA Australia

Chiral, cationic NHC-iridium complexes are introduced as catalysts for the intramolecular hydroamination reaction of unactivated aminoalkenes. The catalysts show high activity in the construction of a range of 5- and 6-membered N-heterocycles, which are accessed in excellent optical purity, with various functional groups being tolerated with this system. A major deactivation pathway is presented and eliminated by using alternative reaction conditions. Read More

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February 2021

Traditional Medicinal Plants Conferring Protection Against Ovalbumin-Induced Asthma in Experimental Animals: A Review.

J Asthma Allergy 2021 14;14:641-662. Epub 2021 Jun 14.

D.S.T.S. Mandal's College of Pharmacy, Solapur, India.

Asthma is a chronic inflammatory disease of the respiratory tract in which the numerous immune cells, including eosinophils, neutrophils, macrophages, T-lymphocytes, mast cells and epithelial lining play key roles. The numerous anti-asthmatic drugs are available in modern medicine to treat asthma, but they have several disadvantages, including side effects and the cost variations, which compromise treatment compliance. The literature review reveals that traditional herbal medicines have good potential as alternative treatment and management for asthma. Read More

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A catalysis-driven artificial molecular pump.

Nature 2021 Jun 23;594(7864):529-534. Epub 2021 Jun 23.

Department of Chemistry, University of Manchester, Manchester, UK.

All biological pumps are autonomous catalysts; they maintain the out-of-equilibrium conditions of the cell by harnessing the energy released from their catalytic decomposition of a chemical fuel. A number of artificial molecular pumps have been reported to date, but they are all either fuelled by light or require repetitive sequential additions of reagents or varying of an electric potential during each cycle to operate. Here we describe an autonomous chemically fuelled information ratchet that in the presence of fuel continuously pumps crown ether macrocycles from bulk solution onto a molecular axle without the need for further intervention. Read More

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Cellular and metabolic mechanisms of nutrient actions in immune function.

Philip Newsholme

Eur J Clin Nutr 2021 Jun 23. Epub 2021 Jun 23.

Curtin Medical School Faculty of Health Sciences and Curtin Health Innovation Research Institute, Curtin University, Perth, WA, 6845, Australia.

Various nutrients can change cell structure, cellular metabolism, and cell function which is particularly important for cells of the immune system as nutrient availability is associated with the activation and function of diverse immune subsets. The most important nutrients for immune cell function and fate appear to be glucose, amino acids, fatty acids, and vitamin D. This perspective will describe recently published information describing the mechanism of action of prominent nutritional intervention agents where evidence exists as to their action and potency. Read More

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Inactivation of the infralimbic cortex decreases discriminative stimulus-controlled relapse to cocaine seeking in rats.

Neuropsychopharmacology 2021 Jun 23. Epub 2021 Jun 23.

Intramural Research Program, National Institute on Drug Abuse, Baltimore, MD, USA.

Persistent susceptibility to cue-induced relapse is a cardinal feature of addiction. Discriminative stimuli (DSs) are one type of drug-associated cue that signal drug availability (DS+) or unavailability (DS-) and control drug seeking prior to relapse. We previously established a trial-based procedure in rats to isolate DSs from context, conditioned stimuli, and other drug-associated cues during cocaine self-administration and demonstrated DS-controlled cocaine seeking up to 300 abstinence days. Read More

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Antipathogenic properties and applications of low-dimensional materials.

Nat Commun 2021 Jun 23;12(1):3897. Epub 2021 Jun 23.

School of Engineering, RMIT University, Melbourne, Australia.

A major health concern of the 21 century is the rise of multi-drug resistant pathogenic microbial species. Recent technological advancements have led to considerable opportunities for low-dimensional materials (LDMs) as potential next-generation antimicrobials. LDMs have demonstrated antimicrobial behaviour towards a variety of pathogenic bacterial and fungal cells, due to their unique physicochemical properties. Read More

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Postoperative complications in glaucoma surgery: literature review-based recommendations to improve reporting consistency.

Br J Ophthalmol 2021 Jun 23. Epub 2021 Jun 23.

Ophthalmology, Nottingham University Hospitals NHS Trust, Nottingham, UK

Aims: To recommend a list of complications of glaucoma surgery to be used in future glaucoma surgery research and reporting by exploring the spectrum of complications' names, the variety of definitions and time frames used for reporting them in glaucoma surgical trials.

Methods: Complications' names, definitions and time frames identified from a previously conducted systematic review of glaucoma surgery trials (registration number: CRD42019121226) were reviewed. Only postoperative complications were considered. Read More

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Phthalide derivative CD21 attenuates tissue plasminogen activator-induced hemorrhagic transformation in ischemic stroke by enhancing macrophage scavenger receptor 1-mediated DAMP (peroxiredoxin 1) clearance.

J Neuroinflammation 2021 Jun 24;18(1):143. Epub 2021 Jun 24.

Department of Pharmacology, West China School of Pharmacy, Sichuan University, Chengdu, 610041, PR China.

Background: Hemorrhagic transformation (HT) is a critical issue in thrombolytic therapy in acute ischemic stroke. Damage-associated molecular pattern (DAMP)-stimulated sterile neuroinflammation plays a crucial role in the development of thrombolysis-associated HT. Our previous study showed that the phthalide derivative CD21 attenuated neuroinflammation and brain injury in rodent models of ischemic stroke. Read More

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Piceatannol protects against sepsis-induced myocardial dysfunction via direct inhibition of JAK2.

Int Immunopharmacol 2021 Jul 24;96:107639. Epub 2021 May 24.

School of Traditional Chinese Medicine, Department of Traditional Chinese Medicine, Nanfang Hospital (ZengCheng Branch), Southern Medical University, Guangzhou 510515, China. Electronic address:

Sepsis-induced myocardial dysfunction (SIMD) represents one of the serious complications secondary to sepsis, which is a leading cause of the high mortality rate among septic cases. Subsequent cardiomyocyte apoptosis, together with the uncontrolled inflammatory response, has been suggested to be closely related to SIMD. Piceatannol (PIC) is verified with potent anti-apoptotic and anti-inflammatory effects, but its function and molecular mechanism in SIMD remain unknown so far. Read More

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Study on the treatment of Cu-organic compound wastewater by electro-Fenton coupled pulsed AC coagulation.

Chemosphere 2021 Oct 6;280:130679. Epub 2021 May 6.

College of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, China. Electronic address:

Electro-Fenton (EF) coupled with Pulsed alternating current coagulation (PACC) is an effective technology for the treatment of Cu-organic wastewater. In this study, the removal efficiency (R), electrical energy consumption (EEC) and removal mechanism of Cu-organic were analyzed and the optimal operation parameters were determined. SEM, EDS, XRD and FTIR were used to characterize the morphology, elemental composition, crystal structure, function groups of sludge produced in the EF-PACC. Read More

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October 2021

Thiazolidinediones (TZDs) enhance insulin secretory response via GPR40 and adenylate cyclase (AC).

J Cell Physiol 2021 Jun 16. Epub 2021 Jun 16.

Division of Endocrinology and Metabolism, Department of Internal Medicine, Eulji University Hospital, Uijeongbu Medical Center, Eulji University, Uijeongbu, Korea.

Thiazolidinediones are synthetic PPARγ ligands that enhance insulin sensitivity, and that could increase insulin secretion from β-cells. However, the functional role and mechanism(s) of action in pancreatic β-cells have not been investigated in detail. Read More

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Does pre-treatment functioning influence response to intravenous ketamine in adults with treatment-resistant depression?

J Affect Disord 2021 Jun 20;292:714-719. Epub 2021 Jun 20.

Mood Disorder Psychopharmacology Unit, University Health Network, Toronto, ON, Canada; Canadian Rapid Treatment Center of Excellence, Mississauga, ON, Canada; Department of Psychiatry, University of Toronto, Toronto, ON, Canada.

Background: The efficacy of monoamine-based antidepressants in adults with major depressive disorder (MDD) is attenuated in persons with greater pre-treatment functional impairment. Herein, we investigated whether pre-treatment functioning in outpatients with treatment-resistant depression (TRD) moderates response to intravenous (IV) ketamine.

Methods: Adults (N= 326; M = 45) with DSM-5-defined MDD or bipolar disorder and TRD received repeat-dose IV ketamine at a community-based clinic. Read More

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Structure-guided design of a perampanel-derived pharmacophore targeting the SARS-CoV-2 main protease.

Structure 2021 Jun 21. Epub 2021 Jun 21.

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520-8066, USA; Department of Molecular Biophysics and Biochemistry, Yale University School of Medicine, New Haven, CT 06520-8066, USA. Electronic address:

There is a clinical need for direct-acting antivirals targeting SARS-CoV-2, the coronavirus responsible for the COVID-19 pandemic, to complement current therapeutic strategies. The main protease (M) is an attractive target for antiviral therapy. However, the vast majority of protease inhibitors described thus far are peptidomimetic and bind to the active-site cysteine via a covalent adduct, which is generally pharmacokinetically unfavorable. Read More

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The Fc-mediated effector functions of a potent SARS-CoV-2 neutralizing antibody, SC31, isolated from an early convalescent COVID-19 patient, are essential for the optimal therapeutic efficacy of the antibody.

PLoS One 2021 23;16(6):e0253487. Epub 2021 Jun 23.

Biological Defence Programme, DSO National Laboratories, Singapore, Singapore.

Although SARS-CoV-2-neutralizing antibodies are promising therapeutics against COVID-19, little is known about their mechanism(s) of action or effective dosing windows. We report the generation and development of SC31, a potent SARS-CoV-2 neutralizing antibody, isolated from a convalescent patient. Antibody-mediated neutralization occurs via an epitope within the receptor-binding domain of the SARS-CoV-2 Spike protein. Read More

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Application of machine learning methods for the development of antidiabetic drugs.

Curr Pharm Des 2021 Jun 21. Epub 2021 Jun 21.

School of Life Sciences, Shanghai University, 200444, China.

Diabetes is a chronic non-communicable disease caused by several different routes, which has attracted increasing attention. In order to speed up the development of new selective drugs, machine learning (ML) technology has been applied in the process of diabetes drug development, which opens up a new blueprint for drug design. This review provides a comprehensive portrayal of the application of ML in antidiabetic drug use. Read More

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