66,881 results match your criteria compound induced

Chlorogenic acid is a positive regulator of MDA5, TLR7 and NF-κB signaling pathways mediated antiviral responses against Gammacoronavirus infection.

Int Immunopharmacol 2021 May 7;96:107671. Epub 2021 May 7.

Natural Medicine Research Center, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, China. Electronic address:

Chlorogenic acid (CGA) is a phenolic compound that has been well studied for its antiviral, anti-inflammatory and immune stimulating properties. This research was aimed to focus on the antiviral properties of CGA on infectious bronchitis virus (IBV) in vivo and in vitro for the very first time. The outcome of in vitro experiments validated that, out of five previously reported antiviral components, CGA significantly reduced the relative mRNA expression of IBV-N in CEK cells. Read More

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Evaluation of heptelidic acid as a potential inhibitor for tau aggregation-induced Alzheimer's disease and associated neurotoxicity.

Int J Biol Macromol 2021 May 7. Epub 2021 May 7.

Department of Nanotechnology, Faculty of Advanced Sciences and Technology, Tehran Medical Sciences, Islamic Azad University, Tehran, Iran. Electronic address:

Tau is a major component of protein plaques in tauopathies, especially Alzheimer's disease (AD). The purpose of the present study is to explore the inhibitory effects of heptelidic acid as a bioactive compound from fungus T. koningii on tau fibrillization and associated neurotoxicity. Read More

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Usnic acid suppresses cervical cancer cell proliferation by inhibiting PD-L1 expression and enhancing T-lymphocyte tumor-killing activity.

Phytother Res 2021 May 10. Epub 2021 May 10.

Molecular Medicine Research Center, College of Pharmacy, Yanbian University, Yanji, China.

The programmed cell death 1 (PD-1)/programmed death ligand 1 (PD-L1) pathway is abnormally expressed in cervical cancer cells. Moreover, PD-1/PD-L1 blockade reduces the apoptosis and exhaustion of T cells and inhibits the development of malignant tumors. Usnic acid is a dibenzofuran compound originating from Usnea diffracta Vain and has anti-inflammatory, antifungal, and anticancer activities. Read More

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Design, synthesis, and molecular docking of novel 3,5-disubstituted-1,3,4-oxadiazole derivatives as iNOS inhibitors.

Arch Pharm (Weinheim) 2021 May 9:e2000469. Epub 2021 May 9.

Department of Pharmacology, Faculty of Pharmacy, Yeditepe University, Istanbul, Turkey.

To obtain new anti-inflammatory agents, recent studies have aimed to replace the carboxylate functionality of nonsteroidal anti-inflammatory drugs with less acidic heterocyclic bioisosteres like 1,3,4-oxadiazole to protect the gastric mucosa from free carboxylate moieties. In view of these observations, we designed and synthesized a series of 3,5-disubstituted-1,3,4-oxadiazole derivatives as inhibitors of prostaglandin E (PGE ) and NO production with an improved activity profile. As initial screening, and to examine the anti-inflammatory activities of the compounds, the inhibitions of the productions of lipopolysaccharide-induced NO and PGE in RAW 264. Read More

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Perillaldehyde Inhibition of cGAS Reduces dsDNA-Induced Interferon Response.

Front Immunol 2021 22;12:655637. Epub 2021 Apr 22.

State Key Laboratory of Natural Medicines, School of Life Science and Technology, China Pharmaceutical University, Nanjing, China.

Cyclic GMP-AMP synthase (cGAS), serving as a primary sensor of intracellular DNA, is essential to initiate anti-microbial innate immunity. Inappropriate activation of cGAS by self-DNA promotes severe autoinflammatory diseases such as Aicardi-Goutières syndrome (AGS); thus, inhibition of cGAS may provide therapeutic benefit in anti-autoimmunity. Here we report that perillaldehyde (PAH), a natural monoterpenoid compound derived from , suppresses cytosolic-DNA-induced innate immune responses by inhibiting cGAS activity. Read More

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An Improved 2-Aminoimidazole Based Anti-Biofilm Coating for Orthopedic Implants: Activity, Stability, and Biocompatibility.

Front Microbiol 2021 21;12:658521. Epub 2021 Apr 21.

Department of Trauma Surgery, University Hospitals Leuven, Leuven, Belgium.

Orthopedic device-related infections remain a serious challenge to treat. Central to these infections are bacterial biofilms that form on the orthopedic implant itself. These biofilms shield the bacteria from the host immune system and most common antibiotic drugs, which renders them essentially antibiotic-tolerant. Read More

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Hydroxytyrosol Acetate Inhibits Vascular Endothelial Cell Pyroptosis via the HDAC11 Signaling Pathway in Atherosclerosis.

Front Pharmacol 2021 23;12:656272. Epub 2021 Apr 23.

Department of Pharmacology, Xi'an Jiaotong University Health Science Center, Xi'an, China.

Hydroxytyrosol acetate (HT-AC), a natural polyphenolic compound in olive oil, exerts an anti-inflammatory effect in cardiovascular diseases (CVDs). Pyroptosis is a newly discovered form of programmed inflammatory cell death and is suggested to be involved in the atherosclerosis (AS) process. However, the effect of HT-AC on vascular endothelial cell pyroptosis remains unknown. Read More

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Evaluating the Therapeutic Mechanisms of Selected Active Compounds in Cornus Officinalis and Paeonia Lactiflora in Rheumatoid Arthritis via Network Pharmacology Analysis.

Front Pharmacol 2021 21;12:648037. Epub 2021 Apr 21.

College of Pharmaceutical Sciences, Zhejiang Chinese Medical University, Hangzhou, China.

Cornus officinalis Sieb et. Zucc and Paeonia lactiflora Pall. have exhibited favorable therapeutic effects against rheumatoid arthritis (RA), but the specific mechanisms of their active compounds remain unclear. Read More

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Cannabinoid Receptor Agonist Inhibits Atrial Electrical Remodeling in a Tachypaced Rat Model.

Front Pharmacol 2021 22;12:642398. Epub 2021 Apr 22.

College of Pharmacy, Rady Faculty of Health Sciences, University of Manitoba, Winnipeg, MB, Canada.

Atrial fibrillation (AF) leads to rate-dependent atrial changes collectively defined as atrial remodelling (AR). Shortening of the atrial effective refractory period (AERP) and decreased conduction velocity are among the hallmarks of AR. Pharmacological strategies to inhibit AR, thereby reducing the self-perpetual nature of AF, are of great clinical value. Read More

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Effects of Anacardic Acid Monoene on the Respiratory System of Mice Submitted to Acute Respiratory Distress Syndrome.

Rev Bras Farmacogn 2021 May 3:1-7. Epub 2021 May 3.

Centro de Ciências e Tecnologia, Universidade Estadual do Ceará, Fortaleza, Brasil.

The acute respiratory distress syndrome caused by viral pathogens is a worldwide public health emergency. It is suggested that patients with this condition should be screened using therapies that address the need to prevent mortality. Anacardic acids found in species have biological activities related to the antioxidant capacity of their double bonds in the lateral alkyl chain. Read More

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Small molecule QF84139 ameliorates cardiac hypertrophy via activating the AMPK signaling pathway.

Acta Pharmacol Sin 2021 May 9. Epub 2021 May 9.

CAS Key Laboratory of Tissue Microenvironment and Tumor, Laboratory of Molecular Cardiology, Shanghai Institute of Nutrition and Health, University of Chinese Academy of Sciences, CAS, Shanghai, 200031, China.

Cardiac hypertrophy is a common adaptive response to a variety of stimuli, but prolonged hypertrophy leads to heart failure. Hence, discovery of agents treating cardiac hypertrophy is urgently needed. In the present study, we investigated the effects of QF84139, a newly synthesized pyrazine derivative, on cardiac hypertrophy and the underlying mechanisms. Read More

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Alterations of Kiss 1 receptor, GnRH receptor and nuclear receptors of the hypothalamo-pituitary-ovarian axis following low dose bisphenol-A exposure in Wistar rats.

Anat Cell Biol 2021 May 10. Epub 2021 May 10.

Department of Anatomy, Faculty of Basic Medical Sciences, University of Ilorin, Ilorin, Nigeria.

Bisphenol A is a chemical used primarily as a monomer in the production of polycarbonate plastics and epoxy resins. It is a synthetic chemical compound that is produced in billions of pounds annually, and tagged as an endocrine disruptor. Bisphenol A is a high production synthetic chemical compound that is used in the production of many consumables and equipments of daily consumption and use by man. Read More

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Inhibition of the sonic hedgehog pathway activates TGF-β-activated kinase (TAK1) to induce autophagy and suppress apoptosis in thyroid tumor cells.

Cell Death Dis 2021 May 8;12(5):459. Epub 2021 May 8.

Institute of Comparative Medicine, College of Veterinary Medicine, Yangzhou University, 225009, Yangzhou, Jiangsu Province, P. R. China.

The sonic hedgehog (Shh) pathway is highly activated in a variety of malignancies and plays important roles in tumorigenesis, tumor growth, drug resistance, and metastasis. Our recent study showed that the inhibitors of the Shh pathway such as cyclopamine (CP), a Smothened (SMO) inhibitor, and GANT61, a Gli1 inhibitor, have modest inhibitory effects on thyroid tumor cell proliferation and tumor growth. The objective of this study was to determine whether autophagy was induced by inhibition of the Shh pathway and could negatively regulate GANT61-induced apoptosis. Read More

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Discovery of pyrazolones as novel carboxylesterase 2 inhibitors that potently inhibit the adipogenesis in cells.

Bioorg Med Chem 2021 Apr 30;40:116187. Epub 2021 Apr 30.

Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China. Electronic address:

Carboxylesterase 2 (CES2) is one of the most important Phase I drug metabolizing enzymes in the carboxylesterase family. It plays crucial roles in the bioavailability of oral ester prodrugs and the therapeutic effect of some anticancer drugs such as irinotecan (CPT11) and capecitabine. In addition to the well-known roles of CES2 in xenobiotic metabolism, the enzyme also participates in endogenous metabolism and the production of lipids. Read More

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Design, synthesis and lipid-lowering activities of penipyridone derivatives.

Bioorg Med Chem 2021 May 1;40:116192. Epub 2021 May 1.

Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, People's Republic of China; Laboratory for Marine Drugs and Bioproducts of Qingdao Pilot National Laboratory for Marine Science and Technology, Qingdao 266237, People's Republic of China; Open Studio for Druggability Research of Marine Natural Products, Pilot National Laboratory for Marine Science and Technology, Qingdao 266237, People's Republic of China. Electronic address:

On the basis of our earlier discovered natural product penipyridone G with potential lipid-lowering utility, 35 penipyridone derivatives were designed, synthesized and characterized. Based on the oleic acid-induced HepG2 cell lipid accumulation model, compounds 12c, 14, 15f, 15k, 15o, 15p and 16f showed potent lipid-lowering activities among the synthetic compounds at 10 μM. In particular, compounds 4, 15k, 15o showed significant activities on inhibiting lipid accumulation in insulin resistant HepG2 cells, and these three compounds were safe and non-toxic within the concentration range of 400 μM. Read More

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Asiatic acid attenuates diabetic retinopathy through TLR4/MyD88/NF-κB p65 mediated modulation of microglia polarization.

Life Sci 2021 May 6:119567. Epub 2021 May 6.

Department of Ophthalmology, The First Affiliated Hospital of Zhengzhou University, 450052 Zhengzhou, Henan, China. Electronic address:

Aim: This study aimed to evaluate the effects of Asiatic acid (AA), a naturally occurring compound of pentacyclic triterpenoid, on the pathological processes of diabetic retinopathy (DR).

Methods: SD rats were induced to develop early DR by intraperitoneal injection of STZ (60 mg/kg). Four weeks after injection, the diabetic rats were orally administrated with 37. Read More

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Glyoxalase I disruption and external carbonyl stress impair mitochondrial function in human induced pluripotent stem cells and derived neurons.

Transl Psychiatry 2021 May 8;11(1):275. Epub 2021 May 8.

Laboratory of Molecular Psychiatry, RIKEN Center for Brain Science, Wako, Saitama, 351-0198, Japan.

Carbonyl stress, a specific form of oxidative stress, is reported to be involved in the pathophysiology of schizophrenia; however, little is known regarding the underlying mechanism. Here, we found that disruption of GLO1, the gene encoding a major catabolic enzyme scavenging the carbonyl group, increases vulnerability to external carbonyl stress, leading to abnormal phenotypes in human induced pluripotent stem cells (hiPSCs). The viability of GLO1 knockout (KO)-hiPSCs decreased and activity of caspase-3 was increased upon addition of methylglyoxal (MGO), a reactive carbonyl compound. Read More

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Facile synthesis of an aggregation-induced emission (AIE) active imidazoles for sensitive detection of trifluralin.

Spectrochim Acta A Mol Biomol Spectrosc 2021 Apr 27;259:119880. Epub 2021 Apr 27.

Guangxi Key Laboratory of Electrochemical and Magneto-chemical Functional Materials, College of Chemistry and Bioengineering, Guilin University of Technology, Guangxi 541006, PR China; National Engineering and Technology Research Center for Colloidal Materials, Shandong University, Jinan, Shandong 250100, PR China. Electronic address:

A novel imidazoles fluorescent probe (2) was synthesized from vanillin, o-phenylenediamine, and N,N-diphenylcarbamyl chloride. Its structure was characterized by fluorescence spectra, UV-Vis spectra, H NMR, C NMR, and high-resolution mass spectrometry (HRMS). Moreover, its aggregation-induced emission (AIE) feature was investigated in THF/MeOH solution. Read More

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Suppression of palmitic acid-induced hepatic oxidative injury by neohesperidin-loaded pectin-chitosan decorated nanoliposomes.

Int J Biol Macromol 2021 May 6. Epub 2021 May 6.

Department of Traditional Chinese Medicine, Sir Run Run Shaw Hospital, School of Medicine, Zhejiang University, Hangzhou 310016, China; Department of Food Science and Nutrition, Zhejiang University, Hangzhou 310058, China; Ningbo Research Institute, Zhejiang University, Ningbo 315100, China. Electronic address:

The biological activity of neohesperidin (NH, a flavanone glycoside) is limited due to instability in the physiological environment. Thus, the current study aimed to explore the protective effect of NH-loaded pectin-chitosan decorated liposomes (P-CH-NH-NL) against palmitic acid (PA)-induced hepatic oxidative injury in L02 cells. The particles were characterized using DLS, TEM, HPLC, DSC, and cellular uptake study. Read More

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Homoseongomycin, a compound isolated from marine actinomycete bacteria K3-1, is a potent inhibitor of encephalitic alphaviruses.

Antiviral Res 2021 May 6:105087. Epub 2021 May 6.

National Center for Biodefense and Infectious Diseases, George Mason University, Manassas, VA, 20110 USA; Department of Biomedical Sciences and Pathobiology, Virginia Polytechnic Institute and State University, Blacksburg, VA, 24061, USA; Center for Zoonotic and Arthropod-borne Pathogens, Virginia Polytechnic Institute and State University, Blacksburg, VA, 24061, USA. Electronic address:

Marine microorganisms have been a resource for novel therapeutic drugs for decades. In addition to anticancer drugs, the drug acyclovir, derived from a marine sponge, is FDA-approved for the treatment of human herpes simplex virus-1 infections. Most alphaviruses that are infectious to terrestrial animals and humans, such as Venezuelan and eastern equine encephalitis viruses (VEEV and EEEV), lack efficient antiviral drugs and it is imperative to develop these remedies. Read More

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Plumbagin Inhibits Proliferation, Migration, and Invasion of Retinal Pigment Epithelial Cells Induced by FGF-2.

Tissue Cell 2021 Apr 28;72:101547. Epub 2021 Apr 28.

Department of Ophthalmology, The second Hospital of Hebei Medical University, Shijiazhuang, 05000, China. Electronic address:

Proliferative vitreoretinopathy (PVR) is a serious ophthalmic disease and characterized by the formation of proliferative membranes by retinal pigment epithelial (RPE) cells. In PVR, the contraction and traction of the fibrocellular membranes cause retinal detachment, which can cause reduction surgery for retinal detachment to fail. Fibroblast growth factor-2 (FGF-2) causes RPE cells to form extracellular matrix (ECM), promotes chemotaxis, mitosis, and positively promotes the disease process of PVR. Read More

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Tryptophan derivatives regulate the seed germination and radicle growth of a root parasitic plant, Orobanche minor.

Bioorg Med Chem Lett 2021 May 5:128085. Epub 2021 May 5.

Department of Agricultural Chemistry, School of Agriculture, Meiji University, 1-1-1 Higashi-mita, Tama-ku, Kawasaki-shi, Kanagawa, 214-8571, Japan. Electronic address:

Root parasitic plant germination is induced by the host-derived chemical, strigolactone (SL). We found that a major microbial culture broth component, tryptone, inhibits the SL-inducible germination of a root parasitic plant, Orobanche minor. l-tryptophan (1a, l-Trp) was isolated as the active compound from tryptone. Read More

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Design and Synthesis of Novel Diosgenin-triazole Hybrids Targeting Inflammation as Potential Neuroprotective Agents.

Bioorg Med Chem Lett 2021 May 5:128092. Epub 2021 May 5.

Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, China. Electronic address:

Alzheimer's disease is a progressive neurodegenerative disease, and its incidence is expected to increase as the global population ages. Recent studies provide increasing evidence that inflammation plays a key role in the pathogenesis and progression of AD. Diosgenin, an active ingredient in Dioscorea nipponica Makino, is a promising bioactive lead compound in the treatment of Alzheimer's disease, which exhibited anti-inflammatory activity. Read More

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Baicalin promotes hippocampal neurogenesis via the Wnt/β-catenin pathway in a chronic unpredictable mild stress-induced mouse model of depression.

Biochem Pharmacol 2021 May 5:114594. Epub 2021 May 5.

Hebei University of Chinese Medicine, Shijiazhuang 050200, China; Hebei Province Academy of Chinese Medicine Sciences, Shijiazhuang 050031, China. Electronic address:

Hippocampal neurogenesis is known to be related to depressive symptoms. Increasing evidence indicates that Wnt/β-catenin signaling regulates multiple aspects of adult hippocampal neurogenesis. Baicalin is a major flavonoid compound with multiple pharmacological effects such as anti-inflammatory, anti-apoptotic, and neuroprotective effects. Read More

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Antileishmanial activity evaluation of a natural amide and its synthetic analogs against Leishmania (V.) braziliensis: an integrated approach in vitro and in silico.

Parasitol Res 2021 May 8. Epub 2021 May 8.

Federal University of Rondônia - UNIR, Porto Velho, Rondônia, Brazil.

Leishmaniasis is considered a neglected disease, which makes it an unattractive market for the pharmaceutical industry; hence, efforts in the search for biologically active substances are hampered by this lack of financial motivation. Thus, in the present study, we report the leishmanicidal activity and the possible mechanisms of action of compounds with promising activity against the species Leishmania (V.) braziliensis, the causative agent of the skin disease leishmaniasis. Read More

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Synthesis and radioprotective effects of novel hybrid compounds containing edaravone analogue and 3-n-butylphthalide ring-opening derivatives.

J Cell Mol Med 2021 May 8. Epub 2021 May 8.

Tianjin Key Laboratory of Radiation Medicine and Molecular Nuclear Medicine, Institute of Radiation Medicine, Peking Union Medical College and Chinese Academy of Medical Science, Tianjin, China.

As the potential risk of radiation exposure is increasing, radioprotectors studies are gaining importance. In this study, novel hybrid compounds containing edaravone analogue and 3-n-butylphthalide ring-opening derivatives were synthesized, and their radioprotective effects were evaluated. Among these, compound 10a displayed the highest radioprotective activity in IEC-6 and HFL-1 cells. Read More

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Caspase-3, a primary target for natural and synthetic compounds for cancer therapy.

Chem Biol Drug Des 2021 May 8. Epub 2021 May 8.

Pharmacy College Saifai, Uttar Pradesh University of Medical Sciences Saifai, Etawah, U.P., 206130, India.

Caspases, a group of protease enzymes (cysteine proteases) exist as inactive zymogens in the cells and execute apoptosis (programmed cell death). Caspase-3, an executioner caspase plays an imperative role in apoptosis and becomes a primary target for cancer treatment. A number of analogues of quinazoline, quinazolinone, indoloquinazolines, quinone, naphthoquinones, pyrroloiminoquinones, styrylquinolines, tetheredtetrahydroquinoline, fluoroquinolone, thiosemicarbazones, benzotriazole, pyrimidines, chalcone and carbazoles have been reported till date, representing caspase-3 mediated apoptosis for cancer therapy. Read More

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Indigo enhances wound healing activity of Caco-2 cells via activation of the aryl hydrocarbon receptor.

J Nat Med 2021 May 7. Epub 2021 May 7.

Pharmacology Laboratory, Department of Biomedical Sciences, College of Life Sciences, Ritsumeikan University, 1-1-1 Noji Higashi, Kusatsu, Shiga, 525-8577, Japan.

Indigo Naturalis, also known as Qing Dai (QD) is a compound obtained from Indigofera tinctoria, Isatis tinctoria, and Polygonum tinctoria and is known to ameliorate refractory ulcerative colitis (UC) by an unknown mechanism. QD maintains both homeostasis and the integrity of colon epithelia in mice that have experimentally induced colitis. The primary component of QD, indigo, comprises 42. Read More

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Diterpenoids from the seeds of Euphorbia lathyris and their anti-inflammatory activity.

Bioorg Chem 2021 Apr 26;112:104944. Epub 2021 Apr 26.

Wuya College of Innovation, Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China. Electronic address:

Twelve previously undescribed diterpenoids, euplarisans A-L (1-12), including one premyrsinane and eleven lathyranes, along with ten known analogues 13-22 were isolated from the seeds of Euphorbia lathyris. Their chemical structures were delineated by spectroscopic analysis and single-crystal X-ray diffraction. Interestingly, both 5 and 6 possessed an unusual trans-gem-dimethylcyclopropane as structural features and compound 8 was elucidated as premyrsinane-type diterpenoid. Read More

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3-O-trans-caffeoyloleanolic acid improves acute lung injury via antiinflammation and antioxidative stress involved PI3K/AKT pathway.

Chem Biol Drug Des 2021 May 7. Epub 2021 May 7.

Department of Respiratory and Critical Care Medicine, Jiangxi Chest (Third people) Hospital, Nanchang, Jiangxi, 330006, PR China.

3-O-trans-caffeoyloleanolic acid (COA) is a pentacyclic triterpenoid compound, with significant anti-inflammatory effects. In this study, we report the protective effects of COA on LPS-induced acute lung injury (ALI) and explored its mechanism of action. LPS was used to construct in vivo mouse ALI models to observe the effects of COA pretreatment on lung pathology, inflammation and oxidative stress. Read More

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