- Apocynin is not an inhibitor of vascular NADPH oxidases but an antioxidant
Institut für Kardiovaskuläre Physiologie, Johann Wolfgang Goethe Universitat, Theodor Stern Kai 7, D 60596 Frankfurt am Main, Germany
Hypertension 51:211-7. 2008
..These observations indicate that apocynin predominantly acts as an antioxidant in endothelial cells and vascular smooth muscle cells and should not be used as an NADPH oxidase inhibitor in vascular systems...
- A quorum sensing regulated small volatile molecule reduces acute virulence and promotes chronic infection phenotypes
Department of Surgery, Harvard Medical School and Massachusetts General Hospital, Boston, Massachusetts, United States of America
PLoS Pathog 7:e1002192. 2011
..aeruginosa. We propose that 2-AA mediates changes in a subpopulation of cells that facilitate the exploitation of dynamic host environments and promote gene expression changes that favor chronic infections...
- Inhibition of NADPH oxidase is neuroprotective after ischemia-reperfusion
Department of Neurosurgery, Stanford University School of Medicine, Stanford, California 94305, USA
J Cereb Blood Flow Metab 29:1262-72. 2009
..This study suggests that NOX plays a role in oxidative stress and inflammation, thus contributing to ischemic brain injury...
- Inhibition of NADPH oxidase activation in endothelial cells by ortho-methoxy-substituted catechols
David K Johnson
Department of Chemistry, State University of New York College at Geneseo, USA
Endothelium 9:191-203. 2002
..These findings identify a metabolite of an ortho-methoxy-substituted catechol, which may be the active compound formed within stimulated ECs that prevents NADPH oxidase complex assembly and activation...
- Apocynin protects against global cerebral ischemia-reperfusion-induced oxidative stress and injury in the gerbil hippocampus
Department of Biochemistry, M743 Medical Sciences Building, University of Missouri Columbia, Columbia, MO 65212, USA
Brain Res 1090:182-9. 2006
- Adventitial application of the NADPH oxidase inhibitor apocynin in vivo reduces neointima formation and endothelial dysfunction in rabbits
Elsa C Chan
Bernard O Brien Institute of Microsurgery, University of Melbourne, 42 Fitzroy Street, Fitzroy, Victoria 3065, Australia
Cardiovasc Res 75:710-8. 2007
..We have now examined the action of the NADPH oxidase inhibitor apocynin, given via the adventitia, on the neointima formation and endothelial function in this model...
- Bioavailability of apocynin through its conversion to glycoconjugate but not to diapocynin
Department of Biochemistry, M743 Medical Sciences Building, University of Missouri, M743 Medical Sciences Building, Columbia, MO 65212, USA
Phytomedicine 15:496-503. 2008
..No diapocynin was detected in any samples. These results indicate rapid glycosylation of apocynin and its transport to blood and other organs but no apparent conversion to diapocynin in vivo...
- Effect of Apocynin, an inhibitor of NADPH oxidase, in the inflammatory process induced by an experimental model of spinal cord injury
Department of Clinical and Experimental Medicine and Pharmacology, School of Medicine, University of Messina, Italy
Free Radic Res 45:221-36. 2011
..Moreover, Apocynin significantly ameliorated the loss of limb function (evaluated by motor recovery score). Thus, it is proposed that Apocynin may be useful in the treatment of inflammation associated with spinal cord trauma...
- Apocynin improves outcome in experimental stroke with a narrow dose range
X N Tang
Department of Neurology, University of California, San Francisco and San Francisco Veterans Affairs Medical Center, San Francisco, CA 94121, USA
Neuroscience 154:556-62. 2008
..Apocynin at protective doses markedly prevented ischemia-induced increases in O.*. Our data suggested that apocynin can protect against experimental stroke, but with a narrow therapeutic window...
- Apocynin reduces reactive oxygen species concentrations in exhaled breath condensate in asthmatics
Department of Immunopathology, Medical University of Lodz, Lodz, Poland
Exp Lung Res 38:90-9. 2012
..No adverse events have been observed throughout the study. This research confirmed anti-inflammatory properties of nebulized apocynin, which might be an effective and safe drug in bronchial asthma...
- Role of NAD(P)H oxidase on vascular alterations in angiotensin II-infused mice
CIHR Multidisciplinary Research Group on Hypertension, Clinical Research Institute of Montreal, University of Montreal, Quebec, Canada
J Hypertens 22:535-42. 2004
..Angiotensin (Ang) II stimulates vascular reactive oxygen species generation via NAD(P)H oxidase activation. We investigated whether vascular NAD(P)H oxidase influences structure and function of resistance arteries from Ang II-infused mice...
- Diapocynin and apocynin administration fails to significantly extend survival in G93A SOD1 ALS mice
Kari A Trumbull
Linus Pauling Institute, Department of Biochemistry and Biophysics, Oregon State University, Corvallis, OR 97331, USA
Neurobiol Dis 45:137-44. 2012
..Diapocynin was also detected in the CNS of apocynin-treated mice. The failure to achieve significant protection with either apocynin or diapocynin raises questions about the utility for treating ALS patients...
- Anti-oxidative effect of apocynin on insulin resistance in high-fat diet mice
Department of Endocrinology, Nanjing Drum Tower Hospital, Nanjing University School of Medicine, 321 Zhongshan Road, Nanjing, 210008, China
Ann Clin Lab Sci 41:236-43. 2011
..These results suggest that apocynin may ameliorate insulin resistance by reducing systemic and hepatic oxidative stress in HFD fed mice...
- Down-regulation of caspase-2 by rottlerin via protein kinase C-delta-independent pathway
Department of Molecular Biology and Immunology, University of North Texas Health Science Center, Fort Worth, TX 76107, USA
Cancer Res 68:2795-802. 2008
..Furthermore, down-regulation of caspase-2 by rottlerin can explain its antiapoptotic function during DNA damage-induced apoptosis...
- Comparative pharmacology of chemically distinct NADPH oxidase inhibitors
Rudolf Buchheim Institute for Pharmacology, Justus Liebig University, Giessen, Germany
Br J Pharmacol 161:885-98. 2010
..One of these sources may be NADPH oxidases. However, due to increasing concerns about the specificity of the compounds commonly used as NADPH oxidase inhibitors, data obtained with these compounds may have to be re-interpreted...
- 2-Aminoacetophenone as a potential breath biomarker for Pseudomonas aeruginosa in the cystic fibrosis lung
Amy J Scott-Thomas
Christchurch School of Medicine and Health Sciences, Department of Pathology, University of Otago, Christchurch, 8140, New Zealand
BMC Pulm Med 10:56. 2010
..Growth of Ps. aeruginosa releases a "grape-like" odour that has been identified as the microbial volatile organic compound 2-aminoacetophenone (2-AA)...
- Rottlerin sensitizes colon carcinoma cells to tumor necrosis factor-related apoptosis-inducing ligand-induced apoptosis via uncoupling of the mitochondria independent of protein kinase C
David M Tillman
Division of Molecular Therapeutics, Department of Hematology Oncology, St Jude Children s Research Hospital, Memphis, Tennessee 38105, USA
Cancer Res 63:5118-25. 2003
..Data suggest that rottlerin affects mitochondrial function independent of PKC delta, thereby sensitizing cells to TRAIL, and that mitochondria constitute an important target in overcoming inherent resistance to TRAIL in colon carcinomas...
- Neuroprotective effect of protein kinase C delta inhibitor rottlerin in cell culture and animal models of Parkinson's disease
Parkinson s Disorder Research Laboratory, Department of Biomedical Sciences, Iowa Center for Advanced Neurotoxicology, Iowa State University, Ames, IA 50011 1250, USA
J Pharmacol Exp Ther 322:913-22. 2007
- Small-molecule aggregates inhibit amyloid polymerization
Brian Y Feng
Department of Pharmaceutical Chemistry and Graduate Group in Chemistry and Chemical Biology, University of California San Francisco, 1700 4th Street, San Francisco, California 94158 2330, USA
Nat Chem Biol 4:197-9. 2008
..They also blocked infection of yeast cells with Sup35 prions, which suggests that colloidal inhibition may be relevant in more biological milieus...
- NADH/NADPH oxidase and enhanced superoxide production in the mineralocorticoid hypertensive rat
R A Beswick
Department of Physiology, Medical College of Georgia, Augusta, USA
Hypertension 38:1107-11. 2001
..These findings suggest that NADPH oxidase is increased and is responsible for increased O(2-) production and possibly contributes to increased blood pressure in the DOCA-salt hypertensive rat...
- Stable compounds of cigarette smoke induce endothelial superoxide anion production via NADPH oxidase activation
Edgar A Jaimes
Nephrology and Hypertension Section, Veterans Affairs Medical Center, Miami, Fla 33125, USA
Arterioscler Thromb Vasc Biol 24:1031-6. 2004
..In these studies, we investigated whether stable compounds present in CS activate specific pathways responsible for the increased endothelial O2* production...
- Rottlerin induces autophagy and apoptotic cell death through a PKC-delta-independent pathway in HT1080 human fibrosarcoma cells: the protective role of autophagy in apoptosis
Kyoung Sub Song
Department of Biochemistry, Chungnam National University, Munhwa dong, Joong Gu, Daejeon, Korea
Autophagy 4:650-8. 2008
- Apocynin restores endothelial dysfunction in streptozotocin diabetic rats through regulation of nitric oxide synthase and NADPH oxidase expressions
Department of Pharmacology and Clinical Pharmacology, Faculty of Medicine, Ege University, Bornova, Izmir, Turkey
J Diabetes Complications 24:415-23. 2010
..This study aimed to investigate the effects of apocynin, an NADPH oxidase inhibitor, on endothelial dysfunction and on the expression of NO synthase (NOS) and NADPH oxidase in thoracic aorta of diabetic rats...
- Increased reactive oxygen species contributes to kidney injury in mineralocorticoid hypertensive rats
Department of Physiology, Medical College of Georgia, Augusta, GA, USA
J Physiol Pharmacol 57:343-57. 2006
..These data suggest that renal injury characteristic of mineralocorticoid hypertension is associated with oxidative stress and is partly independent of blood pressure...
- Apocynin suppresses the progression of atherosclerosis in apoE-deficient mice by inactivation of macrophages
Department of Metabolic Medicine, Faculty of Life Sciences, Kumamoto University, Kumamoto 860 8556, Japan
Biochem Biophys Res Commun 431:124-30. 2013
..Therefore, apocynin may be a potential therapeutic material to prevent the progression of atherosclerosis...
- Apocynin but not allopurinol prevents and reverses adrenocorticotropic hormone-induced hypertension in the rat
High Blood Pressure Research Unit, John Curtin School of Medical Research, Australian National University, Australian Capital Territory, Canberra, Australia
Am J Hypertens 18:910-6. 2005
..Adrenocorticotropic hormone (ACTH)-induced hypertension in the rat is accompanied by increased oxidative stress. This study examines the enzymatic source of reactive oxygen species in ACTH-hypertension...
- FGF-2 and TPA induce matrix metalloproteinase-9 secretion in MCF-7 cells through PKC activation of the Ras/ERK pathway
Jian Feng Liu
Laboratoire de Recherche sur la Croissance Cellulaire, la Réparation et la Régénération Tissulaires, CNRS UPRES A 7053, Universite Paris XII, avenue du General de Gaulle, 94000 Creteil, France
Biochem Biophys Res Commun 293:1174-82. 2002
..These results demonstrated that FGF-2 and TPA induce MMP-9 secretion in MCF-7 cells mainly through PKC-dependent activation of the Ras/ERK(1/2) signaling pathway...
- Tissue transglutaminase inhibits autophagy in pancreatic cancer cells
Department of Experimental Therapeutics, The University of Texas M D Anderson Cancer Center, Houston, TX 77030, USA
Mol Cancer Res 5:241-9. 2007
..In conclusion, these results suggest a novel mechanism of regulation of TG2 and TG2-mediated autophagy in pancreatic cancer cells...
- Potential sources of 2-aminoacetophenone to confound the Pseudomonas aeruginosa breath test, including analysis of a food challenge study
Department of Pathology, Christchurch School of Medicine and Health Sciences, University of Otago, PO Box 4345, Christchurch, 8140, New Zealand
J Breath Res 5:046002. 2011
..Analysis of mixed breath samples reported that the levels of 2-aminoacetophenone were immediately elevated after corn chip consumption, but after 2 h the level of 2-aminoacetophenone had reduced back to the 'baseline' for each subject...
- Pro-oxidant activity of apocynin radical
Lidyane Regina Gomes Castor
Departamento de Farmacologia, Instituto de Biociencias de Botucatu, Unesp Univ Estadual Paulista, Botucatu, SP, Brasil
Free Radic Biol Med 48:1636-43. 2010
..This characteristic may underlie some of the recent findings regarding beneficial or deleterious effects of the phytochemical...
- Effect of protein kinase C delta (PKC-δ) inhibition on the transcriptome of normal and systemic sclerosis human dermal fibroblasts in vitro
Peter J Wermuth
Jefferson Institute of Molecular Medicine, Thomas Jefferson University, Philadelphia, Pennsylvania, United States of America
PLoS ONE 6:e27110. 2011
..These results indicate that isoform-specific inhibition of PKC-δ profibrotic effects may represent a novel therapeutic approach for SSc and other fibrotic diseases...
- Rottlerin inhibits migration of follicular thyroid carcinoma cells by PKCdelta-independent destabilization of the focal adhesion complex
Chien Jung Lin
Department of Anatomy and Cell Biology, College of Medicine, National Taiwan University, Taipei 10051, Taiwan
J Cell Biochem 110:428-37. 2010
..In summary, we demonstrated that rottlerin inhibits the migration of CGTH W-2 cells by disassembly of focal adhesion complexes in a PKCdelta-independent manner, and might play as a mitochondrial uncoupler role in these events...
- Apocynin administration does not improve behavioral and neuropathological deficits in a transgenic mouse model of Alzheimer's disease
Weill Cornell Medical College, Department of Neurology and Neuroscience, 525 East 68th Street, New York, NY 10065, USA
Neurosci Lett 492:150-4. 2011
..Also, the reduction of NOX-mediated oxidative stress may not be sufficient to prevent AD, since other sources of reactive oxygen species such as mitochondria may be more important...
- Evidence against a role for NADPH oxidase modulating hepatic vascular tone in cirrhosis
Hepatic Hemodynamic Laboratory, Liver Unit, IMDiM, Hospital Clinic, Ciberehd and Institut d Investigacions Biomèdiques August Pi i Sunyer, University of Barcelona, Spain
Gastroenterology 133:959-66. 2007
..Thus, our aims were to study the molecular and biochemical state of NADPH-oxidase in cirrhotic livers and to investigate its possible role in modulating hepatic vascular tone in cirrhosis...
- Paeonol and paeoniflorin, the main active principles of Paeonia albiflora, protect the heart from myocardial ischemia/reperfusion injury in rats
Irina Tsoy Nizamutdinova
Department of Pharmacology, School of Medicine, Institute of Health Sciences, Gyeongsang National University, Jinju, Korea
Planta Med 74:14-8. 2008
..The results show that both PF and PN reduced myocardial damage in rat through protection from apoptosis, suggesting that Paeonia albiflora Pallas might be useful in treating myocardial infarction...
- Effect of sildenafil citrate and a nitric oxide donating sildenafil derivative, NCX 911, on cavernosal relaxation and superoxide formation in hypercholesterolaemic rabbits
Bristol Heart Institute, Department of Cardiac Surgery, Bristol Royal Infirmary, Bristol BS2 8HW, UK
Eur J Pharmacol 517:224-31. 2005
..It also indicates that NO donating sildenafil may be therapeutically more beneficial than conventional sildenafil in treating erectile dysfunction with an oxidative stress-related aetiology...
- Influence of co-administered danshensu on pharmacokinetic fate and tissue distribution of paeonol in rats
Institute of Materia Medica, School of Pharmacy, Fourth Military Medical University, Xi an, People s Republic of China
Planta Med 78:135-40. 2012
- Aggregation inhibitory activity of minor acetophenones from Paeonia species
H C Lin
School of Pharmacy, National Defense Medical Center, Taipei, Taiwan
Planta Med 65:595-9. 1999
Two minor acetophenones, 2,5-dihydroxy-4-methoxy-acetophenone (2) and 2,5-dihydroxy-4-methylacetophenone (7) from Paeonia species were found to selectively inhibit the aggregation of rabbit platelets induced by arachidonic acid...
- Caspase-3-dependent proteolytic cleavage of protein kinase Cdelta is essential for oxidative stress-mediated dopaminergic cell death after exposure to methylcyclopentadienyl manganese tricarbonyl
Parkinson Disorders Research Program, Department of Biomedical Sciences, Iowa Sate University, Ames, Iowa 50011, USA
J Neurosci 22:1738-51. 2002
..For the first time, these data demonstrate that caspase-3-dependent proteolytic activation of PKCdelta plays a key role in oxidative stress-mediated apoptosis in dopaminergic cells after exposure to an environmental neurotoxic agent...
- Effect of apocynin, a NADPH oxidase inhibitor, on acute lung inflammation
Department of Clinical and Experimental Medicine and Pharmacology, School of Medicine, University of Messina, Via C Valeria Gazzi, 98100 Messina, Italy
Biochem Pharmacol 81:636-48. 2011
..Thus, based on these findings we propose that NADPH oxidase inhibitor such as apocynin may be useful in the treatment of various inflammatory diseases...
- Protein kinase Ctheta is a specific target for inhibition of the HIV type 1 replication in CD4+ T lymphocytes
María Rosa López-Huertas
AIDS Immunopathology Unit, National Center of Microbiology, Instituto de Salud Carlos III, 28220 Majadahonda, Madrid, Spain
J Biol Chem 286:27363-77. 2011
- Inhibition of protein kinase Cdelta reduces tristetraprolin expression by destabilizing its mRNA in activated macrophages
The Immunopharmacology Research Group, University of Tampere Medical School and Research Unit, Tampere University Hospital, Tampere, Finland
Eur J Pharmacol 628:220-5. 2010
..The results suggest that PKCdelta up-regulates the expression of TTP by stabilizing its mRNA which may serve as a feed-back loop to regulate the inflammatory response...
- Chronic apocynin treatment attenuates beta amyloid plaque size and microglial number in hAPP(751)(SL) mice
Melinda E Lull
Department of Anatomy and Neurobiology, Virginia Commonwealth University Medical Campus, Richmond, Virginia, United States of America
PLoS ONE 6:e20153. 2011
- Apocynin attenuates tubular apoptosis and tubulointerstitial fibrosis in transgenic mice independent of hypertension
Department of Medicine, Universite de Montreal, Centre Hospitalier de l Universite de Montreal Hotel Dieu, Research Centre, Montreal, Quebec, Canada
Kidney Int 75:156-66. 2009
- Inhibition of NAD(P)H oxidase activity blocks vascular endothelial growth factor overexpression and neovascularization during ischemic retinopathy
Vascular Biology Center, Medical College of Georgia, 1120 15th St, Augusta, GA 30912 2500, USA
Am J Pathol 167:599-607. 2005
..In conclusion, NAD(P)H oxidase activity is required for hypoxia-stimulated increases in VEGF expression and retinal neovascularization. Inhibition of NAD(P)H oxidase offers a new therapeutic target for the treatment of retinopathy...
- Apocynin decreases hydrogen peroxide and nitrate concentrations in exhaled breath in healthy subjects
Department of Immunopathology, Medical University of Lodz, 251 Pomorska Street, Building C5, 92 213 Lodz, Poland
Pulm Pharmacol Ther 23:48-54. 2010
..Thus, as apocynin significantly influence ROS concentration, it might have also antiinflammatory properties. As it is safe, it may have a potential to become a drug in airway inflammatory diseases treatment...
- Apocynin-induced vasodilation involves Rho kinase inhibition but not NADPH oxidase inhibition
Department of Physiology, University of Greifswald, Greifswalder Street 11C, D17495 Greifswald, Karlsburg, Germany
Cardiovasc Res 80:271-9. 2008
..Further experiments were performed in normotensive rats and in NADPH oxidase subunit knock-out mice to test if apocynin-induced vasodilation depends on NADPH oxidase inhibition at all...
- Protein kinase C-delta is commonly expressed in multiple myeloma cells and its downregulation by rottlerin causes apoptosis
Department of Pathology, Loyola University Medical Center, EMS Building, 2160 S First Avenue, Maywood, IL 60153, USA
Br J Haematol 121:849-56. 2003
..Our results indicate that PKC-delta is commonly expressed in myeloma cells and plays an important role in plasma cell survival...
- Apocynin attenuate spatial learning deficits and oxidative responses to intermittent hypoxia
Department of Respiratory Medicine, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Key Laboratory of Respiratory Disease, Ministry of Health, Wuhan 430030, China
Sleep Med 11:205-12. 2010
- NADPH oxidase inhibition improves neurological outcomes in surgically-induced brain injury
Department of Physiology, Loma Linda University and Loma Linda University School of Medicine, Loma Linda, CA 92350, USA
Neurosci Lett 414:228-32. 2007
..These results suggest that chronic and acute inhibition of NADPH oxidase activity does not reduce brain edema after SBI. Long-term inhibition of NADPH oxidase, however improves neurological functions after SBI...
- NAD(P)H oxidase inhibition improves endothelial function in rat and human blood vessels
Carlene A Hamilton
BHF Blood Pressure Group, Department of Medicine and Therapeutics, Western Infirmary, Glasgow, Scotland
Hypertension 40:755-62. 2002
..The increases in NO bioavailability shown here suggest that the NAD(P)H oxidase pathway may be a novel target for drug intervention in cardiovascular disease...
- Inhibition of NAD(P)H oxidase reduces apoptosis and avascular retina in an animal model of retinopathy of prematurity
Department of Ophthalmology, University of North Carolina, Chapel Hill, NC 27599 7041, USA
Mol Vis 13:840-53. 2007
- Role of xanthine oxidoreductase in the reversal of diastolic heart failure by candesartan in the salt-sensitive hypertensive rat
Department of Pharmacology and Molecular Therapeutics, Kumamoto University Graduate School of Medical Sciences, 1 1 1 Honjyo, Kumamoto 860 8556, Japan
Hypertension 50:657-62. 2007
..In conclusion, candesartan slowed the exacerbation of hypertensive diastolic heart failure in DS rats by causing reverse cardiac remodeling. Cardiac xanthine oxidoreductase contributed to these beneficial effects of candesartan...
- Apocynin inhibits NADPH oxidase in phagocytes but stimulates ROS production in non-phagocytic cells
Institute of Medical Biochemistry, 1st Faculty of Medicine, Charles University, Katerinska 32, 121 08 Prague 2, Czech Republic
Biochim Biophys Acta 1722:143-7. 2005
..It acts as an inhibitor of phagocyte NADPH oxidase but also as a ROS production stimulator in non-phagocyte cells...
- The oxidation of apocynin catalyzed by myeloperoxidase: proposal for NADPH oxidase inhibition
Valdecir F Ximenes
Departamento de Quimica, Faculdade de Ciencias, Universidade Estadual Paulista, Bauru, SP, Brazil
Arch Biochem Biophys 457:134-41. 2007
..We suggest that the reactivity of apocynin radical with thiol compounds could be involved in the inhibitory effect of this methoxy-catechol on NADPH oxidase complex...
- Proteomic analysis of Agrobacterium tumefaciens response to the Vir gene inducer acetosyringone
Erh Min Lai
Institute of Plant and Microbial Biology, Academia Sinica, Taipei, Taiwan
Proteomics 6:4130-6. 2006
..This report presents the first proteomics study successfully identifying both known and new AS-induced proteins that are implicated in Agrobacterium virulence...
- Selective inhibition by rottlerin of macropinocytosis in monocyte-derived dendritic cells
Experimental Immunology Branch, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA
Immunology 116:513-24. 2005
..We conclude that rottlerin is a useful tool for investigating FPE and its functional importance...
- Altered protein kinase C (PKC) isoforms in non-small cell lung cancer cells: PKCdelta promotes cellular survival and chemotherapeutic resistance
Amy S Clark
Cancer Therapeutics Branch, Center for Cancer Research, National Cancer Institute, Bethesda, Maryland 20889, USA
Cancer Res 63:780-6. 2003
..Our studies provide a rationale for targeting PKC isoforms in NSCLC cells, especially PKCdelta...
- Rottlerin, a PKC isozyme-selective inhibitor, affects signaling events and cytokine production in human monocytes
Department of Pathophysiology and Immunology, Institute of Rheumatology, Warsaw, Poland
J Leukoc Biol 67:249-58. 2000
..Thus, we propose that cytosol-to-membrane translocation of PKCalpha and PKdelta isoenzymes may represent early steps in the signaling cascades that lead to TNF-alpha and IL-1beta production in human monocytes...
- Role of protein kinase C-delta in the regulation of collagen gene expression in scleroderma fibroblasts
S A Jimenez
Division of Rheumatology, Department of Medicine, Thomas Jefferson University, Philadelphia, Pennsylvania 19107 5541, USA
J Clin Invest 108:1395-403. 2001
..The results indicate that PKC-delta participates in the upregulation of collagen gene transcription in SSc and suggest that treatment with PKC-delta inhibitors could suppress fibrosis in this disease...
- NADPH oxidase mediates striatal neuronal injury after transient global cerebral ischemia
Department of Neurosurgery, Stanford University School of Medicine, Stanford, California 94305 5487, USA
J Cereb Blood Flow Metab 31:868-80. 2011
..These findings suggest that NOX has pivotal roles in MSN injury after tGCI and could be a therapeutic target for brain ischemia...
- Rottlerin synergistically enhances imatinib-induced apoptosis of BCR/ABL-expressing cells through its mitochondrial uncoupling effect independent of protein kinase C-delta
Department of Hematology, Graduate School of Medicine, Tokyo Medical and Dental University, Tokyo, Japan
Oncogene 26:2975-87. 2007
- Interpreting steep dose-response curves in early inhibitor discovery
Brian K Shoichet
Department of Pharmaceutical Chemistry, University of California San Francisco, 1700 4th Street, San Francisco, California 94158, USA
J Med Chem 49:7274-7. 2006
..Most steep dose-response curves in screening may be due to this effect...
- Activation and induction of cytosolic phospholipase A2 by TNF-α mediated through Nox2, MAPKs, NF-κB, and p300 in human tracheal smooth muscle cells
Chiang Wen Lee
Department of Nursing, Division of Basic Medical Sciences, Chronic Diseases and Health Promotion Research Center, Chang Gung Institute of Technology, Chia Yi, Taiwan
J Cell Physiol 226:2103-14. 2011
..These results suggested that in HTSMCs, activation of p47(phox) , MAPKs, NF-κB, and p300 is essential for TNF-α-induced cPLA(2) expression and PGE(2) release...
- Effect of apocynin on ozone-induced airway hyperresponsiveness to methacholine in asthmatics
E A Peters
Department of Pulmonology, Leiden University Medical Center, The, Leiden, Netherlands
Free Radic Biol Med 31:1442-7. 2001
..025). We conclude that apocynin markedly reduced O(3)-induced hyperreactivity for Mch as well as maximal airway narrowing. The results suggest that apocynin may have a role in preventing ozone-induced exacerbations of asthma...
- Hypercholesterolemia-induced erectile dysfunction: endothelial nitric oxide synthase (eNOS) uncoupling in the mouse penis by NAD(P)H oxidase
Department of Urology, Johns Hopkins University, Baltimore, MD 21287, USA
J Sex Med 7:3023-32. 2010
- Antiproliferative and apoptotic effects of paeonol on human hepatocellular carcinoma cells
Research Institute of Integrated Traditional Chinese and Western Medicine, Xiangya Hospital, Central South University, Changsha, Hunan, China
Anticancer Drugs 19:401-9. 2008
..In addition, paeonol induced DNA fragmentation in the HCC cell line BEL-7404. These observations suggest that paeonol has the potential to be explored for use as an effective antitumor agent for HCC...
- Role of NAD(P)H oxidase in superoxide generation and endothelial dysfunction in Goto-Kakizaki (GK) rats as a model of nonobese NIDDM
Department of Biochemistry and Molecular Biology, University of South Alabama, Mobile, Alabama, United States of America
PLoS ONE 5:e11800. 2010
..This impairment is likely the result of decreased bioavailability of nitric oxide (NO) within the vasculature. However, it is unclear whether hyperglycemia per se stimulates NADPH oxidase-derived superoxide generation in vascular tissue...
- Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenones
Anthony B Pinkerton
Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
Bioorg Med Chem Lett 14:5329-32. 2004
We have identified and synthesized a series of aryl-tetrazoyl acetophenones as positive allosteric potentiators of the metabotropic glutamate receptor 2...
- Rottlerin induces apoptosis via death receptor 5 (DR5) upregulation through CHOP-dependent and PKC delta-independent mechanism in human malignant tumor cells
Jun Hee Lim
Department of Immunology and Chronic Disease Research Center and Institute for Medical Science, School of Medicine, Keimyung University, 194 DongSan Dong Jung Gu, Taegu 700 712, South Korea
Carcinogenesis 30:729-36. 2009
..Thus, DR5-mediated apoptosis, which is induced by rottlerin alone or by the combined treatment with rottlerin and TRAIL, may offer a new therapeutic strategy against cancer...
- NADPH oxidase-mediated oxidative damage to proteins in the postsynaptic density after transient cerebral ischemia and reperfusion
Department of Molecular and Cellular Pharmacology, Tokyo University of Pharmacy and Life Sciences, 1432 1 Horinouchi, Hachioji, Tokyo 192 0392, Japan
Mol Cell Neurosci 46:681-8. 2011
- Ketamine-induced loss of phenotype of fast-spiking interneurons is mediated by NADPH-oxidase
M Margarita Behrens
Department of Medicine, Division of Geriatric Medicine, University of California San Diego, La Jolla, CA 92093 0746, USA
Science 318:1645-7. 2007
..These results suggest that NADPH oxidase may represent a novel target for the treatment of ketamine-induced psychosis...
- PKCdelta protects human breast tumor MCF-7 cells against tumor necrosis factor-related apoptosis-inducing ligand-mediated apoptosis
National Laboratory of Medical Molecular Biology, Institute of Basic Medical Sciences, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100005, China
J Cell Biochem 96:522-32. 2005
..These findings indicate that PKCdelta functions as a survival factor protecting MCF-7 cells from the apoptosis induced by rsTRAIL...
- Paeonol reduced cerebral infarction involving the superoxide anion and microglia activation in ischemia-reperfusion injured rats
Ching Liang Hsieh
Department of Chinese Medicine, China Medical University Hospital, Taichung City, Taiwan
J Ethnopharmacol 106:208-15. 2006
..Paeonol suppresses and scavenges superoxide anion, and inhibit microglia activation and IL-1beta in ischemia-reperfusion injured rats...
- Inhibition of NADPH oxidase prevents advanced glycation end product-mediated damage in diabetic nephropathy through a protein kinase C-alpha-dependent pathway
JDRF Albert Einstein Centre for Diabetes Complications, Diabetes and Metabolism Division, Baker Medical Research Institute, P O Box 6492, St Kilda Rd, Central, Melbourne, Victoria, Australia
Diabetes 57:460-9. 2008
..Since NADPH oxidase activation is closely linked to other putative pathways, its interaction with changes in protein kinase C (PKC) and increased advanced glycation was examined...
- Rottlerin: an inappropriate and ineffective inhibitor of PKCdelta
Stephen P Soltoff
Division of Signal Transduction, Department of Medicine, Beth Israel Deaconess Medical Center, Harvard Medical School, New Research Building, Room 1030 J, 77 Avenue Louis Pasteur, Boston, MA 02115, USA
Trends Pharmacol Sci 28:453-8. 2007
- Antiproliferation and apoptosis induction of paeonol in human esophageal cancer cell lines
G P Sun
Department of Oncology, The First Affiliated Hospital of Anhui Medical University, Hefei, China
Dis Esophagus 21:723-9. 2008
..The results show that Pae shows growth inhibitory and apoptosis induction property and may be a promising agent for the EC treatment...
- Fas activation opposes PMA-stimulated changes in the localization of PKCdelta: a mechanism for reducing neutrophil adhesion to endothelial cells
Department of Pharmacology, Rush University, 2242 W Harrison, Room 264, Chicago, IL 60612, USA
J Leukoc Biol 71:863-70. 2002
..There was no additive effect of Fas activation and rottlerin on reducing adhesion, suggesting that both agents were using a common pathway...
- Apocynin attenuates cerebral infarction after transient focal ischaemia in rats
L L Tang
Department of Infectious Disease, The First Affiliated Hospital, College of Medicine, Zhejiang University, Hangzhou, The People s Republic of China
J Int Med Res 35:517-22. 2007
..These results indicate that inhibition of NADPH oxidase attenuates cerebral infarction after transient focal ischaemia in rats, suggesting that inhibition of NADPH oxidase may provide a therapeutic strategy for ischaemic stroke...
- The NADPH oxidase inhibitor apocynin induces nitric oxide synthesis via oxidative stress
Dipartimento di Genetica, Biologia e Biochimica, Universita di Torino, Via Santena 5 bis, 10126 Torino, Italy
Toxicol Appl Pharmacol 228:277-85. 2008
- Protein kinase C delta regulates anti-apoptotic alphaB-crystallin in the retina of type 2 diabetes
Y H Kim
Department of Anatomy and Neurobiology, School of Medicine, Institute of Health Science, Gyeongsang National University, Jinju, Chilam dong 92, Jinju, Gyeongnam 660 751, South Korea
Neurobiol Dis 28:293-303. 2007
..These changes were abolished by rottlerin treatment, a highly specific PKC delta inhibitor. These results suggest that PKC delta is involved in regulation of anti-apoptotic function of alphaBC in the retina of type 2 diabetes...
- Functional role of NADPH oxidase in activation of platelets
Department of Experimental Pharmacology, Jagiellonian University Medical College, Krakow, Poland
Antioxid Redox Signal 6:691-8. 2004
- Reactive oxygen species in rostral ventrolateral medulla modulate cardiac sympathetic afferent reflex in rats
M K Zhong
Department of Physiology, Nanjing Medical University, China
Acta Physiol (Oxf) 197:297-304. 2009
- Production of (R)-1-phenylethanols through bioreduction of acetophenones by a new fungus isolate Trichothecium roseum
Faculty of Sciences, Department of Chemistry, Ataturk University, Erzurum 25240, Turkey
Chirality 22:543-7. 2010
A total of 120 fungal strains were isolated from soil samples and evaluated in the bioreduction of substituted acetophenones to the corresponding (R)-alcohols...
- PKC delta and tissue transglutaminase are novel inhibitors of autophagy in pancreatic cancer cells
Department of Experimental Therapeutics, The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, USA
Autophagy 3:480-3. 2007
..In conclusion, our data suggest a novel role of PKC delta/TG2 in regulation of autophagy, and that TG2 may serve as an excellent therapeutic target in pancreatic cancer cells...
- Kalopanaxsaponin A inhibits PMA-induced invasion by reducing matrix metalloproteinase-9 via PI3K/Akt- and PKCdelta-mediated signaling in MCF-7 human breast cancer cells
Sun Kyu Park
Department of Applied Life Science, The Graduate School, Yonsei University, Seoul, Korea
Carcinogenesis 30:1225-33. 2009
..Therefore, KPS-A may be a promising anti-invasive agent with the advantage of oral dosing...
- The effects of paeonol on the electrophysiological properties of cardiac ventricular myocytes
Yu ling Ma
Department of Pharmacology, United Medical and Dental Schools, St Thomas Hospital, Lambeth Palace Road, London SE1 7EH, UK
Eur J Pharmacol 545:87-92. 2006
..These findings suggest that paeonol, and therefore Mudanpi, may possess antiarrhythmic activity, which may confer its cardioprotective effects...
- NF-kappa B activation in tumor necrosis factor alpha-stimulated neutrophils is mediated by protein kinase Cdelta. Correlation to nuclear Ikappa Balpha
Division of Neonatal Perinatal Medicine, Schneider Children s Hospital, Long Island Jewish Medical Center The Long Island Campus for the Albert Einstein College of Medicine, New Hyde Park, New York 11040, USA
J Biol Chem 276:19746-52. 2001
- Effects of methoxylation of apocynin and analogs on the inhibition of reactive oxygen species production by stimulated human neutrophils
E van den Worm
Department of Medicinal Chemistry, Utrecht Institute for Pharmaceutical Sciences, Faculty of Pharmacy, Utrecht University, PO Box 80082, 3508 TB, Utrecht, The Netherlands
Eur J Pharmacol 433:225-30. 2001
..Our approach may lead to the development of more effective anti-inflammatory agents which are safe and which lack the side effects of steroids...
- Chromobacterium violaceum ω-transaminase variant Trp60Cys shows increased specificity for (S)-1-phenylethylamine and 4'-substituted acetophenones, and follows Swain-Lupton parameterisation
Karim Engelmark Cassimjee
KTH Royal Institute of Technology, Division of Biochemistry, School of Biotechnology, AlbaNova University Centre, SE 106 91 Stockholm, Sweden
Org Biomol Chem 10:5466-70. 2012
..The variant Trp60Cys gave increased specificity for (S)-1-phenylethylamine (29-fold) and 4'-substituted acetophenones (∼5-fold). To further study the effect of the mutation the reaction rates were Swain-Lupton parameterised...
- Protective effects of apocynin on "two-hit" injury induced by hemorrhagic shock and lipopolysaccharide
The Second Department of Research Institute of Surgery, Third Military Medical University, Chongqing 400042, China
Acta Pharmacol Sin 23:1023-8. 2002
..To evaluate the protective effects of apocynin on "two-hit" injury in rats...
- Acetophenones with selective antimycobacterial activity
Department of Biological Sciences and Border Biomedical Research Center, The University of Texas at El Paso, El Paso, TX 79968, USA
Lett Appl Microbiol 40:212-7. 2005
..In this study, the antimycobacterial activity of a small library of acetophenone (AP) compounds was analysed...
- Rottlerin, a specific inhibitor of protein kinase C-delta, impedes barrier repair response by increasing intracellular free calcium
Bong K Ahn
Department of Dermatology, Yonsei University College of Medicine, Seoul, Korea
J Invest Dermatol 126:1348-55. 2006
..Furthermore, PKCdelta is important in controlling a decrease in intracellular calcium concentration...
- Involvement of NOX2 in the development of behavioral and pathologic alterations in isolated rats
Department of Human Physiology and Pharmacology, Vittorio Erspamer, University of Rome, La Sapienza, Italy
Biol Psychiatry 66:384-92. 2009
..Loss of parvalbumin in interneurons is an important feature of these diseases. We studied the role of the superoxide-producing nicotinamide adenosine dinucleotide phosphate (NADPH) oxidase 2 (NOX2) in rats exposed to social isolation...
- Long-term effects of intrauterine malnutrition on vascular function in female offspring: implications of oxidative stress
Maria C P Franco
Laboratory of Hypertension, Diabetes and Inflammation, Department of Pharmacology, Institute of Biomedical Sciences Av Prof Lineu Prestes, University of Sao Paulo, Sao Paulo, SP, Brazil
Life Sci 80:709-15. 2007
..These effects may be mediated via modulation of enzyme systems that generate superoxide...
- Transfer hydrogenation in water: enantioselective, catalytic reduction of alpha-cyano and alpha-nitro substituted acetophenones
Laboratorium fur Organische Chemie, ETH Zurich, Honggerberg, Switzerland
Org Lett 12:2893-5. 2010
Catalytic reduction of alpha-substituted acetophenones under conditions involving asymmetric transfer hydrogenation in water is described. The reaction is conducted in water and open to air, and formic acid is used as reductant.
- Synergistic effect of combining paeonol and cisplatin on apoptotic induction of human hepatoma cell lines
Shu Ping Xu
Institute of Clinical Pharmacology, Anhui Medical University, Key Laboratory of Anti inflammatory and Immunological Pharmacology, Key Laboratory of Research and Development of Chinese Medicine, Hefei 230032, China
Acta Pharmacol Sin 28:869-78. 2007
..To investigate whether paeonol (Pae) has synergistic effects with cisplatin (CDDP) on the growth-inhibition and apoptosis-induction of human hepatoma cell lines HepG2 and SMMC-7721...
- Rottlerin induces pro-apoptotic endoplasmic reticulum stress through the protein kinase C-delta-independent pathway in human colon cancer cells
Jun Hee Lim
Department of Immunology, Chronic Disease Research Center, Institute for Medical Science, School of Medicine, Keimyung University, 194 DongSan Dong Jung Gu, Taegu 700 712, South Korea
Apoptosis 13:1378-85. 2008
..Taken together, the present study thus provides strong evidence to support an important role of ER stress response in mediating the rottlerin-induced apoptosis...
- Rottlerin inhibits stimulated enzymatic secretion and several intracellular signaling transduction pathways in pancreatic acinar cells by a non-PKC-delta-dependent mechanism
J A Tapia
Digestive Diseases Branch, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA
Biochim Biophys Acta 1763:25-38. 2006
..Our results give reasons for a more careful choice of rottlerin for PKC-delta investigation...
- Rottlerin is a mitochondrial uncoupler that decreases cellular ATP levels and indirectly blocks protein kinase Cdelta tyrosine phosphorylation
S P Soltoff
Division of Signal Transduction, Harvard Institutes of Medicine, Boston, Massachusetts 02215, USA
J Biol Chem 276:37986-92. 2001
..These results demonstrate that rottlerin directly uncouples mitochondrial respiration from oxidative phosphorylation. Previous studies using rottlerin should be evaluated cautiously...
- Rottlerin stimulates apoptosis in pancreatic cancer cells through interactions with proteins of the Bcl-2 family
Veterans Affairs Greater Los Angeles Healthcare System, Departments of Medicine, David Geffen School of Medicine, University of California, Los Angeles, California, USA
Am J Physiol Gastrointest Liver Physiol 298:G63-73. 2010
..Thus rottlerin represents a promising novel agent for pancreatic cancer treatment...