Genomes and Genes
Summary: Derivatives of the simplest aromatic ketone acetophenone (of general formula C6H5C(O)CH3).
- Trumbull K, McAllister D, Gandelman M, Fung W, Lew T, Brennan L, et al. Diapocynin and apocynin administration fails to significantly extend survival in G93A SOD1 ALS mice. Neurobiol Dis. 2012;45:137-44 pubmed publisher..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. ..
- Olukman M, Orhan C, Celenk F, Ulker S. Apocynin restores endothelial dysfunction in streptozotocin diabetic rats through regulation of nitric oxide synthase and NADPH oxidase expressions. J Diabetes Complications. 2010;24:415-23 pubmed publisher..Apocynin effectively prevents the increased NADPH oxidase expression in diabetic aorta and restores the alterations in NOS expression, blocking the vicious cycle leading to diabetes-associated endothelial dysfunction. ..
- Leppänen T, Jalonen U, Korhonen R, Tuominen R, Moilanen E. Inhibition of protein kinase Cdelta reduces tristetraprolin expression by destabilizing its mRNA in activated macrophages. Eur J Pharmacol. 2010;628:220-5 pubmed publisher..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. ..
- Lee C, Lin C, Lee I, Lee H, Yang C. Activation and induction of cytosolic phospholipase A2 by TNF-? mediated through Nox2, MAPKs, NF-?B, and p300 in human tracheal smooth muscle cells. J Cell Physiol. 2011;226:2103-14 pubmed publisher..These results suggested that in HTSMCs, activation of p47(phox) , MAPKs, NF-?B, and p300 is essential for TNF-?-induced cPLA(2) expression and PGE(2) release. ..
- Tang C, Hsu C, Fong Y. The CCL5/CCR5 axis promotes interleukin-6 production in human synovial fibroblasts. Arthritis Rheum. 2010;62:3615-24 pubmed publisher..The present results suggest that the interaction between CCL5 and CCR5 increases IL-6 production in human synovial fibroblasts via the PKC?/c-Src/c-Jun and AP-1 signaling pathways. ..
- Heumüller S, Wind S, Barbosa Sicard E, Schmidt H, Busse R, Schröder K, et al. Apocynin is not an inhibitor of vascular NADPH oxidases but an antioxidant. Hypertension. 2008;51:211-7 pubmed..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. ..
- Ramnath R, Sun J, Adhikari S, Zhi L, Bhatia M. Role of PKC-delta on substance P-induced chemokine synthesis in pancreatic acinar cells. Am J Physiol Cell Physiol. 2008;294:C683-92 pubmed..These results show that PKC-delta is an important proinflammatory signal transducer for SP-NK1R-induced chemokine production in pancreatic acinar cells...
- Torricelli C, Fortino V, Capurro E, Valacchi G, Pacini A, Muscettola M, et al. Rottlerin inhibits the nuclear factor kappaB/cyclin-D1 cascade in MCF-7 breast cancer cells. Life Sci. 2008;82:638-43 pubmed publisher..Indeed the drug prevented calcium-induced CaMKII autophosphorylation which, in turn, led to decreased NFkappaB activation. ..
- Castor L, Locatelli K, Ximenes V. Pro-oxidant activity of apocynin radical. Free Radic Biol Med. 2010;48:1636-43 pubmed publisher..This characteristic may underlie some of the recent findings regarding beneficial or deleterious effects of the phytochemical. ..
- Bhatt K, Pandey R, Dahiya Y, Sodhi A. Protein kinase Cdelta and protein tyrosine kinase regulate peptidoglycan-induced nuclear factor-kappaB activation and inducible nitric oxide synthase expression in mouse peritoneal macrophages in vitro. Mol Immunol. 2010;47:861-70 pubmed publisher..These observations suggest that PGN induces enhanced expression of iNOS and NO production through activation of protein tyrosine kinases and PKCdelta, which in turn initiates NF-kappaB activation and translocation to nucleus...
- Behrens M, Ali S, Dao D, Lucero J, Shekhtman G, Quick K, et al. Ketamine-induced loss of phenotype of fast-spiking interneurons is mediated by NADPH-oxidase. Science. 2007;318:1645-7 pubmed..These results suggest that NADPH oxidase may represent a novel target for the treatment of ketamine-induced psychosis. ..
- Valacchi G, Pecorelli A, Mencarelli M, Carbotti P, Fortino V, Muscettola M, et al. Rottlerin: a multifaced regulator of keratinocyte cell cycle. Exp Dermatol. 2009;18:516-21 pubmed publisher..These results open the way to further investigation on the Rottlerin therapeutic potential against keratinocyte hyper-proliferative disorders. ..
- Chen H, Song Y, Chan P. Inhibition of NADPH oxidase is neuroprotective after ischemia-reperfusion. J Cereb Blood Flow Metab. 2009;29:1262-72 pubmed publisher..This study suggests that NOX plays a role in oxidative stress and inflammation, thus contributing to ischemic brain injury. ..
- Pandey A, Kour K, Bani S, Suri K, Satti N, Sharma P, et al. Amelioration of adjuvant induced arthritis by apocynin. Phytother Res. 2009;23:1462-8 pubmed publisher..These observations validate the immunoregulatory potential of apocynin. ..
- Yoshioka H, Niizuma K, Katsu M, Okami N, Sakata H, Kim G, et al. NADPH oxidase mediates striatal neuronal injury after transient global cerebral ischemia. J Cereb Blood Flow Metab. 2011;31:868-80 pubmed publisher..These findings suggest that NOX has pivotal roles in MSN injury after tGCI and could be a therapeutic target for brain ischemia. ..
- Gupte S, Labinskyy N, Gupte R, Csiszar A, Ungvari Z, Edwards J. Role of NAD(P)H oxidase in superoxide generation and endothelial dysfunction in Goto-Kakizaki (GK) rats as a model of nonobese NIDDM. PLoS ONE. 2010;5:e11800 pubmed publisher..Hyperglycemic induced increases in NAD(P)H oxidase activity that did not come from an increase in the expression of the NAD(P)H oxidase subunits, but more likely as a result of chronic activation via intracellular signaling pathways. ..
- Stefanska J, Sokolowska M, Sarniak A, Wlodarczyk A, Doniec Z, Nowak D, et al. Apocynin decreases hydrogen peroxide and nitrate concentrations in exhaled breath in healthy subjects. Pulm Pharmacol Ther. 2010;23:48-54 pubmed publisher..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. ..
- Feng B, Toyama B, Wille H, Colby D, Collins S, May B, et al. Small-molecule aggregates inhibit amyloid polymerization. Nat Chem Biol. 2008;4:197-9 pubmed publisher..They also blocked infection of yeast cells with Sup35 prions, which suggests that colloidal inhibition may be relevant in more biological milieus. ..
- Nizamutdinova I, Jin Y, Kim J, Yean M, Kang S, Kim Y, et al. Paeonol and paeoniflorin, the main active principles of Paeonia albiflora, protect the heart from myocardial ischemia/reperfusion injury in rats. Planta Med. 2008;74:14-8 pubmed publisher..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...
- Basu A, Adkins B, Basu C. Down-regulation of caspase-2 by rottlerin via protein kinase C-delta-independent pathway. Cancer Res. 2008;68:2795-802 pubmed publisher..Furthermore, down-regulation of caspase-2 by rottlerin can explain its antiapoptotic function during DNA damage-induced apoptosis. ..
- Wind S, Beuerlein K, Eucker T, Muller H, Scheurer P, Armitage M, et al. Comparative pharmacology of chemically distinct NADPH oxidase inhibitors. Br J Pharmacol. 2010;161:885-98 pubmed publisher..Based on the effects of VAS3947, NADPH oxidases appear to be a major source of ROS in aortas of SHRs. ..
- Edlund J, Fasching A, Liss P, Hansell P, Palm F. The roles of NADPH-oxidase and nNOS for the increased oxidative stress and the oxygen consumption in the diabetic kidney. Diabetes Metab Res Rev. 2010;26:349-56 pubmed publisher..Inhibition of either NADPH-oxidase or nNOS prevented the increased oxygen consumption. The effect of blocking both these enzymes was less than additive suggesting overlapping pathways which warrant further studies. ..
- Kojima K, Motoshima H, Tsutsumi A, Igata M, Matsumura T, Kondo T, et al. Rottlerin activates AMPK possibly through LKB1 in vascular cells and tissues. Biochem Biophys Res Commun. 2008;376:434-8 pubmed publisher..These data suggest for the first time that LKB1 mediates rottlerin-induced activation of AMPK in vascular cells and tissues. ..
- Lim J, Park J, Choi K, Park Y, Kwon T. Rottlerin induces apoptosis via death receptor 5 (DR5) upregulation through CHOP-dependent and PKC delta-independent mechanism in human malignant tumor cells. Carcinogenesis. 2009;30:729-36 pubmed publisher..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. ..
- Sun G, Wan X, Xu S, Wang H, Liu S, Wang Z. Antiproliferation and apoptosis induction of paeonol in human esophageal cancer cell lines. Dis Esophagus. 2008;21:723-9 pubmed publisher..The results show that Pae shows growth inhibitory and apoptosis induction property and may be a promising agent for the EC treatment. ..
- Schlüter T, Steinbach A, Steffen A, Rettig R, Grisk O. Apocynin-induced vasodilation involves Rho kinase inhibition but not NADPH oxidase inhibition. Cardiovasc Res. 2008;80:271-9 pubmed publisher..Its use as a pharmacological tool to investigate vascular NADPH oxidase should be discontinued. ..
- Zhong M, Gao J, Zhang F, Xu B, Fan Z, Wang W, et al. Reactive oxygen species in rostral ventrolateral medulla modulate cardiac sympathetic afferent reflex in rats. Acta Physiol (Oxf). 2009;197:297-304 pubmed publisher..These results suggest that the NAD(P)H oxidase-derived ROS in the RVLM modulate the CSAR. The ROS in the RVLM is necessary for the enhanced CSAR response caused by Ang II in the PVN. ..
- Schiavone S, Sorce S, Dubois Dauphin M, Jaquet V, Colaianna M, Zotti M, et al. Involvement of NOX2 in the development of behavioral and pathologic alterations in isolated rats. Biol Psychiatry. 2009;66:384-92 pubmed publisher..These results provide a molecular mechanism for the coupling between social stress and brain oxidative stress, as well as potential new therapeutic avenues. ..
- Scott Thomas A, Syhre M, Pattemore P, Epton M, Laing R, Pearson J, et al. 2-Aminoacetophenone as a potential breath biomarker for Pseudomonas aeruginosa in the cystic fibrosis lung. BMC Pulm Med. 2010;10:56 pubmed publisher..001) and CF subjects not colonised with Ps. aeruginosa (median 0, range 0-287; p < 0.003). Our results report 2-AA as a promising breath biomarker for the detection of Ps. aeruginosa infections in the cystic fibrosis lung. ..
- Song K, Kim J, Yun E, Kim Y, Seo K, Park J, et al. 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. Autophagy. 2008;4:650-8 pubmed
- Longpre J, Loo G. Protection of human colon epithelial cells against deoxycholate by rottlerin. Apoptosis. 2008;13:1162-71 pubmed publisher..In contrast, epigallocatechin gallate, curcumin, and genistein were ineffective. ..
- Lim J, Park J, Kim S, Choi Y, Choi K, Kwon T. Rottlerin induces pro-apoptotic endoplasmic reticulum stress through the protein kinase C-delta-independent pathway in human colon cancer cells. Apoptosis. 2008;13:1378-85 pubmed publisher..Taken together, the present study thus provides strong evidence to support an important role of ER stress response in mediating the rottlerin-induced apoptosis. ..
- Lima F, Niger C, Hebert C, Stains J. Connexin43 potentiates osteoblast responsiveness to fibroblast growth factor 2 via a protein kinase C-delta/Runx2-dependent mechanism. Mol Biol Cell. 2009;20:2697-708 pubmed publisher..Thus, Cx43 plays a critical role in regulating the ability of osteoblasts to respond to FGF2 by impacting PKCdelta and Runx2 function. ..
- Scott Thomas A, Pearson J, Chambers S. Potential sources of 2-aminoacetophenone to confound the Pseudomonas aeruginosa breath test, including analysis of a food challenge study. J Breath Res. 2011;5:046002 pubmed publisher..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. ..
- Dumont M, Stack C, Elipenhali C, Calingasan N, Wille E, Beal M. Apocynin administration does not improve behavioral and neuropathological deficits in a transgenic mouse model of Alzheimer's disease. Neurosci Lett. 2011;492:150-4 pubmed publisher..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. ..
- Bayorh M, Rollins Hairston A, Adiyiah J, Lyn D, Eatman D. Eplerenone suppresses aldosterone/ salt-induced expression of NOX-4. J Renin Angiotensin Aldosterone Syst. 2011;12:195-201 pubmed publisher..Aldosterone-induced expression of NOX-4 plays a pivotal role in the end-organ damage effect of aldosterone, as eplerenone tended to reduce kidney damage and inhibit NOX expression. ..
- Chunhu Z, Suiyu H, Meiqun C, Guilin X, Yunhui L. Antiproliferative and apoptotic effects of paeonol on human hepatocellular carcinoma cells. Anticancer Drugs. 2008;19:401-9 pubmed publisher..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. ..
- Soltani O, Ariger M, Vázquez Villa H, Carreira E. Transfer hydrogenation in water: enantioselective, catalytic reduction of alpha-cyano and alpha-nitro substituted acetophenones. Org Lett. 2010;12:2893-5 pubmed publisherCatalytic 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.
- Impellizzeri D, Mazzon E, Esposito E, Paterniti I, Bramanti P, Cuzzocrea S. Effect of Apocynin, an inhibitor of NADPH oxidase, in the inflammatory process induced by an experimental model of spinal cord injury. Free Radic Res. 2011;45:221-36 pubmed publisher..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. ..
- Brennan A, Suh S, Won S, Narasimhan P, Kauppinen T, Lee H, et al. NADPH oxidase is the primary source of superoxide induced by NMDA receptor activation. Nat Neurosci. 2009;12:857-63 pubmed publisher..These findings identify NADPH oxidase as the primary source of NMDA-induced superoxide production. ..
- Harraz M, Marden J, Zhou W, Zhang Y, Williams A, Sharov V, et al. SOD1 mutations disrupt redox-sensitive Rac regulation of NADPH oxidase in a familial ALS model. J Clin Invest. 2008;118:659-70 pubmed publisher..This redox sensor mechanism may explain the gain-of-function seen with certain SOD1 mutations associated with ALS and defines new therapeutic targets. ..
- Ye J, Deng T, Zhang J. Influence of paeonol on expression of COX-2 and p27 in HT-29 cells. World J Gastroenterol. 2009;15:4410-4 pubmed..One of the apoptotic mechanisms of paeonol is down-regulation of COX-2. p27 is up-regulated simultaneously and plays an important part in controlling cell proliferation and is a crucial factor in the Fas/FasL apoptosis pathway. ..
- Chen J, Cho J, Hwang T, Chen I. Benzoic acid derivatives, acetophenones, and anti-inflammatory constituents from Melicope semecarpifolia. J Nat Prod. 2008;71:71-5 pubmed publisher..acid (1) and (E)-3-acetyl-4-(3,7-dimethylocta-2,6-dienyloxy)-2,6-dihydroxybenzoic acid (2), and three new acetophenones, (E)-1-(5-(3,7-dimethylocta-2,6-dienyloxy)-7-hydroxy-2,2-dimethyl-2 H-chromen-8-yl)ethanone (3), (E)-1-(5-(3,7-..
- Luchtefeld R, Luo R, Stine K, Alt M, Chernovitz P, Smith R. Dose formulation and analysis of diapocynin. J Agric Food Chem. 2008;56:301-6 pubmed..The log of the octanol/water partition coefficient (log P) was 1.01 for apocynin and 1.82 for diapocynin. A solution of 5.5 mg/mL (16.7 mM) diapocynin in DMSO was found to be stable for at least 30 days when stored at room temperature. ..
- Lull M, Levesque S, Surace M, Block M. Chronic apocynin treatment attenuates beta amyloid plaque size and microglial number in hAPP(751)(SL) mice. PLoS ONE. 2011;6:e20153 pubmed publisher..Despite absence of clear neuroinflammation, apocynin was still able to reduce both plaque size and microglial number, suggesting that apocynin may have additional therapeutic effects independent of anti-inflammatory characteristics. ..
- Jackman K, Miller A, De Silva T, Crack P, Drummond G, Sobey C. Reduction of cerebral infarct volume by apocynin requires pretreatment and is absent in Nox2-deficient mice. Br J Pharmacol. 2009;156:680-8 pubmed publisher..Apocynin improves outcome following stroke when administered before ischaemia in wild-type but not Nox2(-/-) mice. ..
- Zilbeyaz K, Taskin M, Kurbanoglu E, Kurbanoglu N, Kilic H. Production of (R)-1-phenylethanols through bioreduction of acetophenones by a new fungus isolate Trichothecium roseum. Chirality. 2010;22:543-7 pubmed publisherA total of 120 fungal strains were isolated from soil samples and evaluated in the bioreduction of substituted acetophenones to the corresponding (R)-alcohols...