naphthoquinones

Summary

Summary: Naphthalene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.

Top Publications

  1. ncbi Shikonin circumvents cancer drug resistance by induction of a necroptotic death
    Weidong Han
    Cancer Institute, The Second Affiliated Hospital, Zhejiang University School of Medicine, 88 Jiefang Road, Hangzhou, Zhejiang, China
    Mol Cancer Ther 6:1641-9. 2007
  2. pmc Shikonin extracted from medicinal Chinese herbs exerts anti-inflammatory effect via proteasome inhibition
    Li Lu
    Protein Modification and Degradation Lab, Department of Pathophysiology, Guangzhou Medical College, Guangzhou, Guangdong, PR China
    Eur J Pharmacol 658:242-7. 2011
  3. ncbi Plumbagin induces G2-M arrest and autophagy by inhibiting the AKT/mammalian target of rapamycin pathway in breast cancer cells
    Po Lin Kuo
    Cell Biology Laboratory, Department of Biotechnology, Chia Nan University of Pharmacy and Science, Tainan 717, Taiwan
    Mol Cancer Ther 5:3209-21. 2006
  4. ncbi Novel multiple apoptotic mechanism of shikonin in human glioma cells
    Ching Hsein Chen
    Department of Microbiology, Immunology and Biopharmaceuticals, College of Life Sciences, National Chiayi University, Chiayi, Taiwan, ROC
    Ann Surg Oncol 19:3097-106. 2012
  5. pmc Is nitric oxide decrease observed with naphthoquinones in LPS stimulated RAW 264.7 macrophages a beneficial property?
    Brígida R Pinho
    REQUIMTE Laboratório de Farmacognosia, Departamento de Quimica, Faculdade de Farmacia, Universidade do Porto, Porto, Portugal
    PLoS ONE 6:e24098. 2011
  6. ncbi Selective inactivation of parvulin-like peptidyl-prolyl cis/trans isomerases by juglone
    L Hennig
    Max Planck Research Unit, Enzymology of Protein Folding, Halle Saale, Germany
    Biochemistry 37:5953-60. 1998
  7. ncbi A multi-center phase II evaluation of the small molecule survivin suppressor YM155 in patients with unresectable stage III or IV melanoma
    Karl D Lewis
    University of Colorado Health Sciences Center, Aurora, CO, USA
    Invest New Drugs 29:161-6. 2011
  8. ncbi Plumbagin (5-hydroxy-2-methyl-1,4-naphthoquinone) induces apoptosis and cell cycle arrest in A549 cells through p53 accumulation via c-Jun NH2-terminal kinase-mediated phosphorylation at serine 15 in vitro and in vivo
    Ya Ling Hsu
    Department of Biotechnology, Chia Nan University of Pharmacy and Science, Tainan, Taiwan
    J Pharmacol Exp Ther 318:484-94. 2006
  9. ncbi The effects on Trypanosoma cruzi of novel synthetic naphthoquinones are mediated by mitochondrial dysfunction
    Rubem F S Menna-Barreto
    Laboratorio de Biologia Celular, Instituto Oswaldo Cruz, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ 21040 900, Brazil
    Free Radic Biol Med 47:644-53. 2009
  10. pmc Pharmacological stimulation of NADH oxidation ameliorates obesity and related phenotypes in mice
    Jung Hwan Hwang
    Department of Internal Medicine, Chungnam National University School of Medicine, Daejeon, Korea
    Diabetes 58:965-74. 2009

Research Grants

  1. Novel Mechanisms of Quinone Toxicity
    David Ross; Fiscal Year: 2013
  2. The Mechanism of Plumbagin-induced Stress Resistance and Lifespan Extension
    SUZANNE ELIZABETH BEREZOVSKY; Fiscal Year: 2013
  3. PLANT TUMOR INHIBITORS
    David Kingston; Fiscal Year: 1980
  4. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2005
  5. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2002
  6. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2008
  7. SYNTHESIS OF ANTICANCER AGENTS
    K C Nicolaou; Fiscal Year: 2010
  8. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2004
  9. Sterol Metabolism in Pneumocystis
    EDNA KANESHIRO; Fiscal Year: 2009
  10. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2009

Detail Information

Publications292 found, 100 shown here

  1. ncbi Shikonin circumvents cancer drug resistance by induction of a necroptotic death
    Weidong Han
    Cancer Institute, The Second Affiliated Hospital, Zhejiang University School of Medicine, 88 Jiefang Road, Hangzhou, Zhejiang, China
    Mol Cancer Ther 6:1641-9. 2007
    ..To our best knowledge, this is the first report to document the induction of necroptosis by a small molecular compound to circumvent cancer drug resistance...
  2. pmc Shikonin extracted from medicinal Chinese herbs exerts anti-inflammatory effect via proteasome inhibition
    Li Lu
    Protein Modification and Degradation Lab, Department of Pathophysiology, Guangzhou Medical College, Guangzhou, Guangdong, PR China
    Eur J Pharmacol 658:242-7. 2011
    ..The novel finding about macrophage proteasome as a target of shikonin suggests that this medicinal compound has great potential to be developed into an anti-inflammatory agent...
  3. ncbi Plumbagin induces G2-M arrest and autophagy by inhibiting the AKT/mammalian target of rapamycin pathway in breast cancer cells
    Po Lin Kuo
    Cell Biology Laboratory, Department of Biotechnology, Chia Nan University of Pharmacy and Science, Tainan 717, Taiwan
    Mol Cancer Ther 5:3209-21. 2006
    ..Taken together, these results imply a critical role for AKT inhibition in plumbagin-induced G2-M arrest and autophagy of human breast cancer cells...
  4. ncbi Novel multiple apoptotic mechanism of shikonin in human glioma cells
    Ching Hsein Chen
    Department of Microbiology, Immunology and Biopharmaceuticals, College of Life Sciences, National Chiayi University, Chiayi, Taiwan, ROC
    Ann Surg Oncol 19:3097-106. 2012
    ..However, the anticancer mechanism of shikonin in human glioma cells is unclear at present. In the present study, we demonstrated that shikonin induces apoptosis in three human glioma cell lines: U87MG, Hs683, and M059K cells...
  5. pmc Is nitric oxide decrease observed with naphthoquinones in LPS stimulated RAW 264.7 macrophages a beneficial property?
    Brígida R Pinho
    REQUIMTE Laboratório de Farmacognosia, Departamento de Quimica, Faculdade de Farmacia, Universidade do Porto, Porto, Portugal
    PLoS ONE 6:e24098. 2011
    ..Several naphthoquinones (plumbagin, naphthazarin, juglone, menadione, diosquinone and 1,4-naphthoquinone), plus p-hydroquinone and p-..
  6. ncbi Selective inactivation of parvulin-like peptidyl-prolyl cis/trans isomerases by juglone
    L Hennig
    Max Planck Research Unit, Enzymology of Protein Folding, Halle Saale, Germany
    Biochemistry 37:5953-60. 1998
    ..Thus, partial unfolding of the active site of the parvulins was thought to be the cause of the deterioration of PPIase activity...
  7. ncbi A multi-center phase II evaluation of the small molecule survivin suppressor YM155 in patients with unresectable stage III or IV melanoma
    Karl D Lewis
    University of Colorado Health Sciences Center, Aurora, CO, USA
    Invest New Drugs 29:161-6. 2011
    ..YM155 is a small molecule suppressant of survivin that has been shown in preclinical cell lines, xenograft models and phase I studies to have anti-tumor activity...
  8. ncbi Plumbagin (5-hydroxy-2-methyl-1,4-naphthoquinone) induces apoptosis and cell cycle arrest in A549 cells through p53 accumulation via c-Jun NH2-terminal kinase-mediated phosphorylation at serine 15 in vitro and in vivo
    Ya Ling Hsu
    Department of Biotechnology, Chia Nan University of Pharmacy and Science, Tainan, Taiwan
    J Pharmacol Exp Ther 318:484-94. 2006
    ..Taken together, these results suggest a critical role for JNK and p53 in plumbagin-induced G2/M arrest and apoptosis of human nonsmall cell lung cancer cells...
  9. ncbi The effects on Trypanosoma cruzi of novel synthetic naphthoquinones are mediated by mitochondrial dysfunction
    Rubem F S Menna-Barreto
    Laboratorio de Biologia Celular, Instituto Oswaldo Cruz, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ 21040 900, Brazil
    Free Radic Biol Med 47:644-53. 2009
    ..Our results indicate that the trypanocidal action of the naphthofuranquinones is associated with mitochondrial dysfunction, leading to increased reactive oxygen species generation and parasite death...
  10. pmc Pharmacological stimulation of NADH oxidation ameliorates obesity and related phenotypes in mice
    Jung Hwan Hwang
    Department of Internal Medicine, Chungnam National University School of Medicine, Daejeon, Korea
    Diabetes 58:965-74. 2009
    ..We tried to determine whether pharmacological stimulation of NADH oxidation provides therapeutic effects in rodent models of metabolic syndrome...
  11. ncbi Natural products as antiparasitic drugs
    O Kayser
    Freie Universitat Berlin, Institut fur Pharmazie, Pharmazeutische Biotechnologie, Kelchstrasse 31, 12169 Berlin, Germany
    Parasitol Res 90:S55-62. 2003
    ..Many novel lead structures, however, have severe chemico-physical drawbacks such as poor solubility. Here, innovative drug formulations and carrier systems might help, as discussed by the authors in another article of this series...
  12. ncbi YM155, a novel small-molecule survivin suppressant, induces regression of established human hormone-refractory prostate tumor xenografts
    Takahito Nakahara
    Institute for Drug Discovery Research, Astellas Pharma Inc, Tsukuba shi, Ibaraki, Japan
    Cancer Res 67:8014-21. 2007
    ..Further extensive investigation of YM155 in many types of cancer, including HRPC, seems to be worthwhile to develop this novel therapeutic approach...
  13. ncbi Shikonin, a Chinese plant-derived naphthoquinone, induces apoptosis in hepatocellular carcinoma cells through reactive oxygen species: A potential new treatment for hepatocellular carcinoma
    Ke Gong
    College of Life Sciences, Wuhan University, Wuhan 430072, People s Republic of China
    Free Radic Biol Med 51:2259-71. 2011
    ..Taken together, our data show that shikonin, which may be a promising agent in the treatment of liver cancer, induced apoptosis in HCC cells through the ROS/Akt and RIP1/NF-κB pathways...
  14. pmc Plumbagin inhibits invasion and migration of breast and gastric cancer cells by downregulating the expression of chemokine receptor CXCR4
    Kanjoormana Aryan Manu
    Department of Pharmacology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore 117597
    Mol Cancer 10:107. 2011
    ..Thus, novel agents that can downregulate the CXCR4/CXCL12 axis have therapeutic potential in inhibiting cancer metastasis...
  15. ncbi Plumbagin induces cell death through a copper-redox cycle mechanism in human cancer cells
    S Nazeem
    Department of Biochemistry, Faculty of Life Sciences, Aligarh Muslim University, Aligarh 202002, Uttar Pradesh, India
    Mutagenesis 24:413-8. 2009
    ....
  16. ncbi Cellular pharmacology studies of shikonin derivatives
    Xin Chen
    Laboratory of Molecular Immunoregulation, Division of Basic Sciences, National Cancer Institute Frederick, MD 21702 1201, USA
    Phytother Res 16:199-209. 2002
    ..This general inhibitory effect can account for the broad spectrum of shikonin biological and pharmacological activities...
  17. ncbi Phase I study of YM155, a novel survivin suppressant, in patients with advanced solid tumors
    Taroh Satoh
    Department of Medical Oncology, Kinki University School of Medicine, Osaka, Japan
    Clin Cancer Res 15:3872-80. 2009
    ..The aim of this study was to determine the maximum tolerated dose (MTD) and to assess the safety, pharmacokinetics, and antitumor activity of YM155 in patients with advanced refractory solid tumors...
  18. ncbi Antitumor effects of YM155, a novel survivin suppressant, against human aggressive non-Hodgkin lymphoma
    Aya Kita
    Drug Discovery Research, Astellas Pharma Inc, Tsukuba shi, Ibaraki, Japan
    Leuk Res 35:787-92. 2011
    ..YM155 increased survival significantly versus rituximab in disseminated Ramos models. This study suggests that YM155 may represent an effective treatment for aggressive lymphomas...
  19. ncbi YM155, a novel survivin suppressant, enhances taxane-induced apoptosis and tumor regression in a human Calu 6 lung cancer xenograft model
    Takahito Nakahara
    Institute for Drug Discovery Research, Astellas Pharma Inc, Tsukuba shi, Ibaraki, Japan
    Anticancer Drugs 22:454-62. 2011
    ....
  20. ncbi Broad spectrum and potent antitumor activities of YM155, a novel small-molecule survivin suppressant, in a wide variety of human cancer cell lines and xenograft models
    Takahito Nakahara
    Institute for Drug Discovery Research, Astellas Pharma, Inc, Tsukuba, Ibaraki, Japan
    Cancer Sci 102:614-21. 2011
    ..The broad and potent antitumor activity presented in the present study is indicative of the therapeutic potential of YM155 in the clinical setting...
  21. ncbi Anti-inflammatory effects of plumbagin are mediated by inhibition of NF-kappaB activation in lymphocytes
    Rahul Checker
    Radiation Biology and Health Sciences Division, Bhabha Atomic Research Centre, Mumbai 400085, India
    Int Immunopharmacol 9:949-58. 2009
    ..Further, plumbagin prevented Graft Versus Host Disease-induced mortality in mice. To our knowledge this is the first report showing the immunomodulatory effects of plumbagin in lymphocytes via modulation of NF-kappaB activation...
  22. ncbi Multicenter phase II trial of YM155, a small-molecule suppressor of survivin, in patients with advanced, refractory, non-small-cell lung cancer
    Giuseppe Giaccone
    Vrije Universiteit Medical Center, Amsterdam, The Netherlands
    J Clin Oncol 27:4481-6. 2009
    ..To evaluate the antitumor activity and safety of YM155, a novel, small-molecule suppressor of survivin, as single-agent therapy in patients with previously treated, advanced non-small-cell lung cancer (NSCLC)...
  23. ncbi Phase I and pharmacokinetic study of YM155, a small-molecule inhibitor of survivin
    Anthony W Tolcher
    Institute for Drug Development, Cancer Therapy and Research Center, San Antonio, TX, USA
    J Clin Oncol 26:5198-203. 2008
    ..To determine the maximum-tolerated dose (MTD) and assess the safety, pharmacokinetics, and preliminary evidence of antitumor activity of YM155, a small-molecule inhibitor of survivin...
  24. ncbi Plumbagin (5-hydroxy-2-methyl-1,4-naphthoquinone) suppresses NF-kappaB activation and NF-kappaB-regulated gene products through modulation of p65 and IkappaBalpha kinase activation, leading to potentiation of apoptosis induced by cytokine and chemotherape
    Santosh K Sandur
    Cytokine Research Laboratory, Department of Experimental Therapeutics, Unit 143, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    J Biol Chem 281:17023-33. 2006
    ..This may explain its cell growth modulatory, anticarcinogenic, and radiosensitizing effects previously described...
  25. pmc An NQO1- and PARP-1-mediated cell death pathway induced in non-small-cell lung cancer cells by beta-lapachone
    Erik A Bey
    Department of Pharmacology, Laboratory of Molecular Stress Responses, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA
    Proc Natl Acad Sci U S A 104:11832-7. 2007
    ..beta-Lapachone killed cells in a tumorselective manner and is indicated for use against NQO1+ NSCLC cancers...
  26. ncbi Cytotoxic action of juglone and plumbagin: a mechanistic study using HaCaT keratinocytes
    J Johnson Inbaraj
    Laboratory of Pharmacology and Chemistry, National Institute of Environmental Health Sciences, National Institutes of Health, Research Triangle Park, North Carolina 27709, USA
    Chem Res Toxicol 17:55-62. 2004
    ..However, it is probable that the antifungal, antiviral, and antibacterial properties of these quinones are the result of redox cycling...
  27. ncbi Necrostatin-1 reverts shikonin-induced necroptosis to apoptosis
    Weidong Han
    Cancer Institute, The Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, Zhejiang, 310009, China
    Apoptosis 14:674-86. 2009
    ..To the best of our knowledge, this is the first study to document a conversion from necroptosis to apoptosis...
  28. pmc Shikonin exerts antitumor activity via proteasome inhibition and cell death induction in vitro and in vivo
    Huanjie Yang
    Department of Pathophysiology, Guangzhou Medical College, Guangzhou, Guangdong, People s Republic of China
    Int J Cancer 124:2450-9. 2009
    ..Our results indicate that the tumor proteasome is one of the cellular targets of shikonin and inhibition of the proteasome activity by shikonin contributes to its antitumor property...
  29. pmc Beta-lapachone, a modulator of NAD metabolism, prevents health declines in aged mice
    Jeong Sook Lee
    Department of Biological Sciences, KAIST Korea Advanced Institute of Science and Technology, Daejeon, Korea
    PLoS ONE 7:e47122. 2012
    ..These results support the potentiation of NQO1 activity by a βL diet and could be an option for preventing age-related decline of muscle and brain functions...
  30. ncbi Beta-hydroxyisovalerylshikonin induces apoptosis in human leukemia cells by inhibiting the activity of a polo-like kinase 1 (PLK1)
    Yutaka Masuda
    Laboratory of Biological Chemistry, School of Pharmaceutical Sciences, Showa University, Tokyo 142 8555, Japan
    Oncogene 22:1012-23. 2003
    ..These results suggest that suppression of the activity of PLK1 via inhibition of tyrosine kinase activity by beta-HIVS might play a critical role in the induction of apoptosis...
  31. ncbi Activation of NAD(P)H:quinone oxidoreductase 1 prevents arterial restenosis by suppressing vascular smooth muscle cell proliferation
    Sun Yee Kim
    Department of Internal Medicine, Kyungpook National University School of Medicine, Daegu, South Korea
    Circ Res 104:842-50. 2009
    ..These observations provide the molecular basis that pharmacological stimulation of NQO1 activity is a new therapy for the treatment of vascular restenosis and/or atherosclerosis which are caused by proliferation of VSMCs...
  32. pmc Shikonin kills glioma cells through necroptosis mediated by RIP-1
    Chuanjiang Huang
    Department of Neurosurgery, First Bethune Hospital of Jilin University, Changchun, China
    PLoS ONE 8:e66326. 2013
    ..Shikonin was reported to induce necroptosis in leukemia cells, but apoptosis in glioma cell lines. Thus, it is needed to clarify whether shikonin could cause necroptosis in glioma cells and investigate its underlying mechanisms...
  33. ncbi Natural and synthetic naphthoquinones active against Trypanosoma cruzi: an initial step towards new drugs for Chagas disease
    Cristian O Salas
    Facultad de Quimica, Pontificia Universidad Catolica de Chile, Casilla 306, Santiago 6094411, Chile
    Curr Med Chem 18:144-61. 2011
    ..An overview of a number of natural naphthoquinones tested against T. cruzi parasites is provided...
  34. ncbi Synthesis of a small library of 2-phenoxy-1,4-naphthoquinone and 2-phenoxy-1,4-anthraquinone derivatives bearing anti-trypanosomal and anti-leishmanial activity
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, Bologna University, Via Belmeloro 6, I 40126 Bologna, Italy
    Bioorg Med Chem Lett 18:2272-6. 2008
    ..28microM, and IC(50)=1.26microM, respectively)...
  35. pmc Increased age reduces DAF-16 and SKN-1 signaling and the hormetic response of Caenorhabditis elegans to the xenobiotic juglone
    Aaron J Przybysz
    Department of Pharmacology, Vanderbilt University, 1161 21st Avenue South, Nashville, TN 37232, USA
    Mech Ageing Dev 130:357-69. 2009
    ..Our studies provide a foundation for developing a molecular understanding of how age affects cytoprotective transcriptional pathways...
  36. ncbi A novel triazolic naphthofuranquinone induces autophagy in reservosomes and impairment of mitosis in Trypanosoma cruzi
    M C Fernandes
    Laboratorio de Biologia Celular, Instituto Oswaldo Cruz, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ 21040 360, Brazil
    Parasitology 139:26-36. 2012
    ..In folk medicine, natural products including naphthoquinones have been employed for the treatment of different parasitic diseases...
  37. pmc Plumbagin inhibits tumour angiogenesis and tumour growth through the Ras signalling pathway following activation of the VEGF receptor-2
    Li Lai
    Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, 500 Dongchuan Road, Shanghai 200241, China
    Br J Pharmacol 165:1084-96. 2012
    ..Here, we sought to determine the biological effects of plumbagin on signalling mechanisms during tumour angiogenesis...
  38. pmc Endoplasmic reticulum stress-induced JNK activation is a critical event leading to mitochondria-mediated cell death caused by β-lapachone treatment
    Hyemi Lee
    Department of Microbiology, College of Medicine, Center for Advanced Medical Education by BK21 Project, Inha University, Incheon, Republic of Korea
    PLoS ONE 6:e21533. 2011
    ..Although β-lap has been reported to induce apoptosis in various cancer types in an NQO1-dependent manner, the signaling pathways by which β-lap causes apoptosis are poorly understood...
  39. ncbi Plumbagin induces apoptosis via the p53 pathway and generation of reactive oxygen species in human osteosarcoma cells
    Linqiang Tian
    Department of Orthopedics, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, PR China
    Mol Med Rep 5:126-32. 2012
    ..To conclude, PL exerted anticancer activity on osteosarcoma cells by inducing pro-apoptotic signaling and modulating the intracellular ROS that causes induction of apoptosis. These effects may relate to the p53 status...
  40. pmc A novel color change mechanism for breast cancer biomarker detection: naphthoquinones as specific ligands of human arylamine N-acetyltransferase 1
    Nicola Laurieri
    Department of Pharmacology, University of Oxford, Oxford, United Kingdom
    PLoS ONE 8:e70600. 2013
    ..This represents a new mechanism for selective biomarker sensing and may be exploited as a general approach to the specific detection of biomarkers in disease. ..
  41. ncbi Involvement of reactive oxygen species, but not mitochondrial permeability transition in the apoptotic induction of human SK-Hep-1 hepatoma cells by shikonin
    Ching Hsein Chen
    Department of Medical Technology, Fooyin University, Ta Liao, Kaohsiung, Taiwan, ROC
    Planta Med 69:1119-24. 2003
    ..Taken together, we suggest that shikonin-induced apoptosis of SK-Hep-1 cells proceeds by an oxidative stress-mediated pathway...
  42. ncbi A shikonin derivative, beta-hydroxyisovalerylshikonin, is an ATP-non-competitive inhibitor of protein tyrosine kinases
    Kazuyasu Nakaya
    School of Pharmaceutical Sciences, Showa University, Tokyo, Japan
    Anticancer Drugs 14:683-93. 2003
    ....
  43. pmc Artemisinin-naphthoquine combination (ARCO) therapy for uncomplicated falciparum malaria in adults of Papua New Guinea: a preliminary report on safety and efficacy
    Francis W Hombhanje
    Faculty of Health Sciences, Divine Word University, Madang Province, Papua New Guinea
    Malar J 8:196. 2009
    ..A study was undertaken to assess the safety, efficacy and tolerability of ANQ combination in areas of multi-drug resistance to generate preliminary baseline data in adult population of Papua New Guinea...
  44. ncbi Multiple stressors in Caenorhabditis elegans induce stress hormesis and extended longevity
    James R Cypser
    Institute for Behavioral Genetics, University of Colorado, Boulder 80303, USA
    J Gerontol A Biol Sci Med Sci 57:B109-14. 2002
    ..In dose-response studies, induced thermotolerance paralleled the induced increase in life expectancy, which is consistent with a common origin...
  45. ncbi Selective induction of necrotic cell death in cancer cells by beta-lapachone through activation of DNA damage response pathway
    Xiangao Sun
    Department of Therapeutic Biology, ArQule Biomedical Institute, Norwood, Massachusetts 02062, USA
    Cell Cycle 5:2029-35. 2006
    ..Our data suggest that selective necrotic cell death can be induced through activation of DNA damage response pathways, supporting the idea of selective necrotic cell death as a therapeutic strategy to eliminate cancer cells...
  46. ncbi Plumbagin-induced apoptosis of human breast cancer cells is mediated by inactivation of NF-kappaB and Bcl-2
    Aamir Ahmad
    Department of Pathology, Barbara Ann Karmanos Cancer Center and Wayne State University School of Medicine, Detroit, Michigan 48201, USA
    J Cell Biochem 105:1461-71. 2008
    ....
  47. pmc Prostate cancer radiosensitization through poly(ADP-Ribose) polymerase-1 hyperactivation
    Ying Dong
    Departments of Pharmacology, Radiation Oncology, Pathology, Biostatistics and Clinical Sciences, and Urology, Simmons Comprehensive Cancer Center, University of Texas Southwestern Medical Center, Dallas, TX 75390 8807, USA
    Cancer Res 70:8088-96. 2010
    ..Our findings offer a rationale for the clinical utilization of β-lap (Arq 501) as a radiosensitizer in prostate cancers that overexpress NQO1, offering a potentially synergistic targeting strategy to exploit PARP-1 hyperactivation...
  48. ncbi Calcium is a key signaling molecule in beta-lapachone-mediated cell death
    C Tagliarino
    Departments of Radiation Oncology and Pharmacology, Department of Anatomy, Case Western Reserve University, Cleveland, Ohio 44106-4942, USA
    J Biol Chem 276:19150-9. 2001
    ..Use of beta-Lap to trigger an apparently novel, calpain-like-mediated apoptotic cell death could be useful for breast and prostate cancer therapy...
  49. pmc Alteration of the repressor activity of MarR, the negative regulator of the Escherichia coli marRAB locus, by multiple chemicals in vitro
    M N Alekshun
    Center for Adaptation Genetics and Drug Resistance, Tufts University School of Medicine, Boston, Massachusetts 02111, USA
    J Bacteriol 181:4669-72. 1999
    ..It is proposed that these compounds can interact directly with MarR to affect its repressor activity...
  50. ncbi Induction of apoptosis by shikonin through a ROS/JNK-mediated process in Bcr/Abl-positive chronic myelogenous leukemia (CML) cells
    Xin Mao
    1State Key Laboratory of Virology, College of Life Sciences, Wuhan University, Wuhan 430072, China
    Cell Res 18:879-88. 2008
    ..Our data also suggest that shikonin may be a promising agent for the treatment of CML, as a generator of ROS...
  51. ncbi Inhibition of Nox-4 activity by plumbagin, a plant-derived bioactive naphthoquinone
    Yaxian Ding
    Department of Medicine, Case Western Reserve University and University Hospital of Cleveland, Cleveland, Ohio 44106, USA
    J Pharm Pharmacol 57:111-6. 2005
    ..Furthermore, plumbagin inhibited the superoxide production in Nox-4 transfected COS-7 cells. These results indicated that plumbagin directly interacted with Nox-4 and inhibited its activity...
  52. pmc Plumbagin, a medicinal plant-derived naphthoquinone, is a novel inhibitor of the growth and invasion of hormone-refractory prostate cancer
    Moammir H Aziz
    Department of Human Oncology, School of Medicine and Public Health, University of Wisconsin, Madison, Wisconsin 53792, USA
    Cancer Res 68:9024-32. 2008
    ..PL inhibits multiple molecular targets including PKCepsilon, a predictive biomarker of PCa aggressiveness. PL may be a novel agent for therapy of hormone-refractory PCa...
  53. ncbi The trypanocidal activity of naphthoquinones: a review
    Antonio Ventura Pinto
    Núcleo de Pesquisas em Produtos Naturais, Centro de Ciencias da Saude, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil
    Molecules 14:4570-90. 2009
    b>Naphthoquinones are compounds present in several families of higher plants. Their molecular structures confer redox properties, and they are involved in multiple biological oxidative processes...
  54. ncbi p53-mediated cell cycle arrest and apoptosis induced by shikonin via a caspase-9-dependent mechanism in human malignant melanoma A375-S2 cells
    Zhen Wu
    Department of Phytochemistry, Shenyang Pharmaceutical University, P R China
    J Pharmacol Sci 94:166-76. 2004
    ..Apoptosis-inducing factor, another apoptotic protein of mitochondria, partially contributed to shikonin-induced release of cytochrome c. Taken together, shikonin-induced DNA damage activates p53 and caspase-9 pathways...
  55. ncbi Naturally-occurring shikonin analogues--a class of necroptotic inducers that circumvent cancer drug resistance
    Yanyan Xuan
    Cancer Institute, The Key Laboratory of Cancer Prevention and Intervention, China National Ministry of Education, The Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, Zhejiang 310009, China
    Cancer Lett 274:233-42. 2009
    ..The results strengthen the previous findings that necroptotic induction could circumvent a broad spectrum of cancer drug resistance...
  56. ncbi Shikonin induces apoptosis through reactive oxygen species/extracellular signal-regulated kinase pathway in osteosarcoma cells
    I Chang Chang
    Institute of Medicine, Chung Shan Medical University, Taichung 40201, Taiwan
    Biol Pharm Bull 33:816-24. 2010
    ..Therefore, shikonin may be a promising chemotherapeutic agent for osteosarcoma treatment...
  57. ncbi Plumbagin induces reactive oxygen species, which mediate apoptosis in human cervical cancer cells
    Priya Srinivas
    Division of Cancer Biology, Rajiv Gandhi Centre for Biotechnology, Thiruvananthapuram, Kerala, India
    Mol Carcinog 40:201-11. 2004
    ....
  58. ncbi Cytochrome b mutations that modify the ubiquinol-binding pocket of the cytochrome bc1 complex and confer anti-malarial drug resistance in Saccharomyces cerevisiae
    Jacques J Kessl
    Department of Biochemistry, Dartmouth Medical School, Hanover, New Hampshire 03755
    J Biol Chem 280:17142-8. 2005
    ..By modeling the variations in cytochrome b structure and atovaquone binding with the mutated bc1 complexes, we obtained the first quantitative explanation for the molecular basis of atovaquone resistance in malaria parasites...
  59. ncbi Caenorhabditis elegans lifespan extension caused by treatment with an orally active ROS-generator is dependent on DAF-16 and SIR-2.1
    Tanja Heidler
    Department of Food and Nutrition, Molecular Nutrition Unit, Technical University of Munich, Am Forum 5, Freising, Germany
    Biogerontology 11:183-95. 2010
    ..1-dependent alterations in gene expression after a ROS challenge lead to a lifespan extension in C. elegans as long as the stressor concentration does not exceed the saturable protective capacity...
  60. pmc Putative polyketide synthase and laccase genes for biosynthesis of aurofusarin in Gibberella zeae
    Jung Eun Kim
    School of Agricultural Biotechnology and Center for Agricultural Biomaterials, Seoul National University, Seoul, Korea
    Appl Environ Microbiol 71:1701-8. 2005
    ..zeae. This information is the first information concerning the biosynthesis of these pigments by G. zeae and could help in studies of their toxicity in domesticated animals...
  61. ncbi Naphthoimidazoles promote different death phenotypes in Trypanosoma cruzi
    R F S Menna-Barreto
    Laboratorio de Biologia Celular, Instituto Oswaldo Cruz, Fundacao Oswaldo Cruz, Rio de Janeiro, Brazil
    Parasitology 136:499-510. 2009
    ..However, there are other pathways occurring concomitantly with variable intensities, justifying the need to detail the molecular features involved...
  62. ncbi Shikonin, an ingredient of Lithospermum erythrorhizon induced apoptosis in HL60 human premyelocytic leukemia cell line
    Y Yoon
    Laboratory of Cancer Research, Korea Institute of Oriental Medicine, Seoul
    Planta Med 65:532-5. 1999
    ..The DNA fragmentation induced by shikonin was completely inhibited by the pretreatment of z-VAD-fmk, a specific inhibitor of caspase, clearly showing that the mode of cell death is apoptotic...
  63. pmc Selective killing of cancer cells by beta -lapachone: direct checkpoint activation as a strategy against cancer
    Youzhi Li
    Division of Gastroenterology, Beth Israel Deaconess Medical Center, Harvard Medical School, 330 Brookline Avenue, Boston, MA 02215, USA
    Proc Natl Acad Sci U S A 100:2674-8. 2003
    ..This study suggests direct checkpoint activation as a strategy against cancer...
  64. ncbi Calcium-dependent modulation of poly(ADP-ribose) polymerase-1 alters cellular metabolism and DNA repair
    Melissa S Bentle
    Department of Pharmacology, Case Western Reserve University, Cleveland, Ohio 44106, USA
    J Biol Chem 281:33684-96. 2006
    ..Thus, Ca(2+) appears to be an important co-factor in PARP-1 hyperactivation after ROS-induced DNA damage, which alters cellular metabolism and DNA repair...
  65. ncbi Plumbagin induces cell cycle arrest and apoptosis through reactive oxygen species/c-Jun N-terminal kinase pathways in human melanoma A375.S2 cells
    Clay C C Wang
    Department of Chemistry, University of Southern California, College of Letters, Arts, and Sciences, University Park Campus, Los Angeles, CA 90089, USA
    Cancer Lett 259:82-98. 2008
    ..Moreover, blocking ERK and JNK by specific inhibitors suppressed plumbagin-triggered mitochondrial apoptotic pathway. Taken together, these results imply a critical role for ROS and JNK in the plumbagin's anticancer activity...
  66. ncbi Suppression of human prostate cancer cell growth by beta-lapachone via down-regulation of pRB phosphorylation and induction of Cdk inhibitor p21(WAF1/CIP1)
    Yung Hyun Choi
    Department of Biochemistry, College of Oriental Medicine, Dong Eui University and Research Center for Oriental Medicine, Pusan 614 052, Korea
    J Biochem Mol Biol 36:223-9. 2003
    ..Overall, our results demonstrate a combined mechanism that involves the inhibition of pRB phosphorylation and induction of p21 as targets for beta-lapachone. This may explain some of its anticancer effects...
  67. ncbi Alkannins and shikonins: a new class of wound healing agents
    V P Papageorgiou
    Laboratory of Organic Chemistry, Department of Chemical Engineering, Aristotle University of Thessaloniki, Greece
    Curr Med Chem 15:3248-67. 2008
    ..In this paper we review the findings and advances on the molecular and biological properties of A/S that promote wound healing...
  68. ncbi Shikonin induces programmed necrosis-like cell death through the formation of receptor interacting protein 1 and 3 complex
    Seungyeon Park
    Department of Pharmacy, Keimyung University, 1095 Sindang dong, Dalseo Gu, Daegu 704 701, South Korea
    Food Chem Toxicol 55:36-41. 2013
    ..Here, it is highlighted that SKN as well as TNFα can directly mediate cell death via a pronecrotic complex, but ROS were generated via different routes depending on cell death-inducing agents...
  69. ncbi Plumbagin induces apoptosis in Her2-overexpressing breast cancer cells through the mitochondrial-mediated pathway
    Anna Kawiak
    Department of Biotechnology, Intercollegiate Faculty of Biotechnology, University of Gdansk and Medical University of Gdansk, Kladki 24, 80 822 Gdansk, Poland
    J Nat Prod 75:747-51. 2012
    ....
  70. pmc Plumbagin, a plant derived natural agent inhibits the growth of pancreatic cancer cells in in vitro and in vivo via targeting EGFR, Stat3 and NF-κB signaling pathways
    Bilal Bin Hafeez
    Department of Human Oncology, Wisconsin Institute of Medical Research, Paul Carbone Comprehensive Cancer Center, School of Medicine and Public Health, University of Wisconsin, Madison, WI 53792, USA
    Int J Cancer 131:2175-86. 2012
    ..These results suggest that PL may be used as a novel therapeutic agent against human PC. Published 2012 Wiley-Liss, Inc. This article is a US Government work, and, as such, is in the public domain in the United States of America...
  71. ncbi Perspectives on medicinal properties of plumbagin and its analogs
    Subhash Padhye
    Department of Pathology, Barbara Ann Karmanos Cancer Institute, Wayne State University School of Medicine, Hudson Webber Cancer Research Center, Detroit, Michigan 48201, USA
    Med Res Rev 32:1131-58. 2012
    ..This comprehensive review is an attempt to understand the chemistry of plumbagin and catalog its biological activities reported to date...
  72. pmc Plumbagin inhibits osteoclastogenesis and reduces human breast cancer-induced osteolytic bone metastasis in mice through suppression of RANKL signaling
    Bokyung Sung
    Cytokine Research Laboratory, Department of Experimental Therapeutics, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA
    Mol Cancer Ther 11:350-9. 2012
    ..Overall, our results indicate that plumbagin, a vitamin K analogue, is a potent inhibitor of osteoclastogenesis induced by tumor cells and of breast cancer-induced osteolytic metastasis through suppression of RANKL signaling...
  73. ncbi In vitro antimicrobial activity of a new series of 1,4-naphthoquinones
    A Riffel
    Departamento de Ciências dos Alimentos, Instituto de Ciências e Tecnologia de Alimentos, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brasil
    Braz J Med Biol Res 35:811-8. 2002
    The antibacterial activity of a series of 1,4-naphthoquinones was demonstrated. Disk diffusion tests were carried out against several Gram-positive and Gram-negative bacteria...
  74. ncbi Novel o-naphthoquinones induce apoptosis of EL-4 T lymphoma cells through the increase of reactive oxygen species
    María Emilia Di Rosso
    Centro de Estudios Farmacologicos y Botanicos CEFYBO, Facultad de Medicina, Universidad de Buenos Aires CONICET, Paraguay 2155, piso 16, C1121ABG Buenos Aires, Argentina
    Toxicol In Vitro 27:2094-104. 2013
    ....
  75. ncbi Inhibition of mycobacterial growth by plumbagin derivatives
    Ritta Mathew
    Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500 046, India
    Chem Biol Drug Des 76:34-42. 2010
    ..smegmatis. Structural modifications of these molecules can further be improved upon to generate new molecules against mycobacteria...
  76. ncbi Plumbagin inhibits TPA-induced MMP-2 and u-PA expressions by reducing binding activities of NF-kappaB and AP-1 via ERK signaling pathway in A549 human lung cancer cells
    Jiunn Min Shieh
    Department of Pulmonary Medicine, Chi Mei Medical Center, Tainan 710, Taiwan
    Mol Cell Biochem 335:181-93. 2010
    ..Presented data reveals that plumbagin is a novel, effective, anti-metastatic agent that functions by down-regulating MMP-2 and u-PA gene expressions...
  77. ncbi Strategies for the synthesis of bioactive pyran naphthoquinones
    Vitor Francisco Ferreira
    Universidade Federal Fluminense, Instituto de Quimica, Departamento de Quimica Organica, CEG, Campus do Valonguinho, 24020 141 Niterói, Rio de Janeiro, Brazil
    Org Biomol Chem 8:4793-802. 2010
    Taking into account the numerous reports in the literature related to pyran naphthoquinones in searching for new pharmacologically promising molecules against different therapeutic targets, this review intends to explore the synthetic ..
  78. pmc A chemical genetic screen for modulators of asymmetrical 2,2'-dimeric naphthoquinones cytotoxicity in yeast
    Ashkan Emadi
    Department of Internal Medicine and Oncology, Johns Hopkins School of Medicine, Baltimore, Maryland, USA
    PLoS ONE 5:e10846. 2010
    Dimeric naphthoquinones (BiQ) were originally synthesized as a new class of HIV integrase inhibitors but have shown integrase-independent cytotoxicity in acute lymphoblastic leukemia cell lines suggesting their use as potential anti-..
  79. ncbi The biosynthetic pathway for aurofusarin in Fusarium graminearum reveals a close link between the naphthoquinones and naphthopyrones
    Rasmus J N Frandsen
    Department of Ecology, The Royal Veterinary and Agricultural University, DK 1871 Frederiksberg C, Copenhagen, Denmark
    Mol Microbiol 61:1069-80. 2006
    ..This links the biosynthesis of naphthopyrones and naphthoquinones together...
  80. ncbi Design, synthesis and biological evaluation of novel nitrogen and sulfur containing hetero-1,4-naphthoquinones as potent antifungal and antibacterial agents
    Vishnu K Tandon
    Department of Chemistry, University of Lucknow, Lucknow, India
    Eur J Med Chem 44:3130-7. 2009
    A series of 2-Arylamino-3-chloro-1,4-naphthoquinones (3), 2-Amino-3-arylsulfanyl-1,4-naphthoquinones (5), 2-Arylamino-3-arylsulfanyl-1,4-naphthoquinones (6), Dihydrobenzo[f]naphtho[2,3-b][1,4]thiazepine-6,11-diones (9) (via Pictet-..
  81. pmc Differential functional genomic effects of anti-inflammatory phytocompounds on immune signaling
    Shao Chih Chiu
    Graduate Institute of Immunology, China Medical University, 91 Hsueh Shih Rd, Taichung 40402, Taiwan
    BMC Genomics 11:513. 2010
    ....
  82. ncbi Antimicrobial activities of naphthazarins from Arnebia euchroma
    Chien Chang Shen
    National Research Institute of Chinese Medicine, Taipei 112, Taiwan
    J Nat Prod 65:1857-62. 2002
    ..6-5.4 microg/mL (CD(50)). Our results indicate that the ester derivatives of alkannin are potential candidates of anti-MRSA and anti-VRE agents with antitumor activity...
  83. ncbi Efficacy of oral single dose therapy with artemisinin-naphthoquine phosphate in uncomplicated falciparum malaria
    Thein Tun
    Department of Medical Research Upper Myanmar, Anisakhan, Pyin Oo Lwin 05062, Mandalay Division, Myanmar
    Acta Trop 111:275-8. 2009
    ..The drug was well tolerated and no adverse reactions were detected in the patients. Since it is a single dose therapy, health workers can administer the drug as directly observed treatment...
  84. ncbi Atovaquone-proguanil versus mefloquine for malaria prophylaxis in nonimmune travelers: results from a randomized, double-blind study
    D Overbosch
    Harbor Hospital and Institute of Tropical Medicine, Rotterdam, The Netherlands
    Clin Infect Dis 33:1015-21. 2001
    ..No confirmed diagnoses of malaria occurred in either group. Atovaquone-proguanil was better tolerated than was mefloquine, and it was similarly effective for malaria prophylaxis in nonimmune travelers...
  85. ncbi Initial response and cellular protection through the Keap1/Nrf2 system during the exposure of primary mouse hepatocytes to 1,2-naphthoquinone
    Takashi Miura
    Doctoral Programs in Medical Sciences, Graduate School of Comprehensive Human Sciences, Graduate School of Life and Environmental Sciences, University of Tsukuba, 1 1 1 Tennodai, Tsukuba, Ibaraki, Japan
    Chem Res Toxicol 24:559-67. 2011
    ..These findings suggest that the Keap1/Nrf2 system is essential for the prevention of cell damage resulting from exposure to 1,2-NQ...
  86. ncbi Causal prophylactic efficacy of atovaquone-proguanil (Malarone) in a human challenge model
    J D Berman
    Walter Reed Army Institute of Research, Silver Spring, MD 20910, USA
    Trans R Soc Trop Med Hyg 95:429-32. 2001
    ..No atovaquone-proguanil volunteer acquired malaria. Atovaquone-proguanil is the first licensed antimalarial agent that kills P. falciparum in the liver and that may be discontinued 7 days after the last exposure...
  87. ncbi In vitro antifungal activity of naphthoquinone derivatives
    Kenroh Sasaki
    Tohoku Pharmaceutical University, Sendai, Japan
    Biol Pharm Bull 25:669-70. 2002
    ..krusei compared with the standard. Against the filamentous fungus, Trichosporon cutaneum, all naphthoquinones were found to have a range of activity with lower potency than standard...
  88. ncbi Shikonin derivatives inhibited LPS-induced NOS in RAW 264.7 cells via downregulation of MAPK/NF-kappaB signaling
    Yu Wen Cheng
    School of Pharmacy, Taipei Medical University, Taipei, Taiwan, Republic of China
    J Ethnopharmacol 120:264-71. 2008
    ..In the present study, the effect and the underline molecular mechanism of shikonin derivatives isolated from root extracts of Lithospermum euchroma on lipopolysaccharide (LPS)-induced inflammatory response were investigated...
  89. ncbi Design of anti-parasitic and anti-fungal hydroxy-naphthoquinones that are less susceptible to drug resistance
    Louise M Hughes
    Department of Biochemistry, Dartmouth Medical School, 7200 Vail, Hanover, NH 03755, USA
    Mol Biochem Parasitol 177:12-9. 2011
    ..fungi and overcome drug resistance, we have synthesized and tested the inhibitory activity of novel hydroxy-naphthoquinones against blood stage P. falciparum and liver stage P...
  90. ncbi Chemical inducers of heat shock proteins derived from medicinal plants and cytoprotective genes response
    Kanwal Ahmed
    Division of Gastrointestinal Pathophysiology, Institute of Natural Medicine, University of Toyama, Toyama, Japan
    Int J Hyperthermia 28:1-8. 2012
    ..In short, the detailed mechanisms of Hsp70 induction by shikonin is not fully understood, Nrf2 and its target genes might be involved in the Hsp70 up-regulation in U937 cells...
  91. ncbi Targeted BIRC5 silencing using YM155 causes cell death in neuroblastoma cells with low ABCB1 expression
    Fieke Lamers
    Department of Oncogenomics, Academic Medical Center, University of Amsterdam, Meibergdreef 15, PO Box 22700, 1105 AZ Amsterdam, The Netherlands
    Eur J Cancer 48:763-71. 2012
    ..Therefore YM155 is a promising novel compound for treatment of neuroblastoma with low ABCB1 expression...
  92. pmc Plumbagin inhibits proliferative and inflammatory responses of T cells independent of ROS generation but by modulating intracellular thiols
    Rahul Checker
    Radiation Biology and Health Sciences Division, Bio Medical Group, Bhabha Atomic Research Centre, Mumbai 400085, Maharashtra, India
    J Cell Biochem 110:1082-93. 2010
    ..Our results for the first time show that antiproliferative effects of plumbagin are mediated by modulation of cellular redox. These results provide a rationale for application of thiol-depleting agents as anti-inflammatory drugs...
  93. pmc Tabebuia avellanedae naphthoquinones: activity against methicillin-resistant staphylococcal strains, cytotoxic activity and in vivo dermal irritability analysis
    Eliezer Menezes Pereira
    Instituto de Microbiologia Prof, Paulo de Góes, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil
    Ann Clin Microbiol Antimicrob 5:5. 2006
    ..In addition, its mechanism of action was also analyzed...
  94. pmc Marked anti-tumour activity of the combination of YM155, a novel survivin suppressant, and platinum-based drugs
    T Iwasa
    Department of Medical Oncology, Kinki University School of Medicine, 377 2 Ohno Higashi, Osaka Sayama, Osaka 589 8511, Japan
    Br J Cancer 103:36-42. 2010
    ..We have now investigated the effects of the combination of YM155, a novel small-molecule inhibitor of survivin expression, and platinum compounds (cisplatin and carboplatin) on human non-small cell lung cancer (NSCLC) cell lines...
  95. ncbi Activity of 7-methyljuglone derivatives against Mycobacterium tuberculosis and as subversive substrates for mycothiol disulfide reductase
    Anita Mahapatra
    Department of Botany, Faculty of Natural and Agricultural Sciences, University of Pretoria, Pretoria 0002, South Africa
    Bioorg Med Chem 15:7638-46. 2007
    ..g. other disulfide reductases)...
  96. ncbi Inhibition of tumor necrosis factor-alpha through selective blockade of Pre-mRNA splicing by shikonin
    Shao Chih Chiu
    Graduate Institute of Life Sciences, National Defense Medical Center and Agricultural Biotechnology Research Center, Academia Sinica, Taipei, Taiwan, ROC
    Mol Pharmacol 71:1640-5. 2007
    ....
  97. ncbi Studies on terpenoids produced by actinomycetes. 5-dimethylallylindole-3-carboxylic Acid and A80915G-8"-acid produced by marine-derived Streptomyces sp. MS239
    Keiichiro Motohashi
    Faculty of Applied Biosciences, Tokyo University of Agriculture, Sakuragaoka, Setagaya Ku, Tokyo, Japan
    J Antibiot (Tokyo) 61:75-80. 2008
    ..MS239, two new terpenoids named 5-dimethylallylindole-3-carboxylic acid and A80915G-8''-acid were isolated and their structures were determined mainly by NMR analyses...
  98. ncbi Growth inhibition and induction of apoptosis in human oral squamous cell carcinoma Tca-8113 cell lines by Shikonin was partly through the inactivation of NF-kappaB pathway
    Ruan Min
    Department of Oral and Maxillofacial Surgery, Affiliated No 9 People s Hospital, College of Medicine, Shanghai Jiao Tong University, Shanghai 200011, PRC
    Phytother Res 22:407-15. 2008
    ..Pharmacological inhibition of the NF-kappaB activity by Shikonin might be a powerful treatment option for OSCC in which activation of NF-kappaB plays a critical role in tumor growth and progression...
  99. ncbi Topoisomerase inhibitors as anti-arthritic agents
    J K Jackson
    Faculty of Pharmaceutical Sciences, University of British Columbia, Vancouver, B C, V6T 1Z3, Canada
    Inflamm Res 57:126-34. 2008
    ..The objective of this study was to investigate a variety of structurally unrelated anticancer topoisomerase inhibiting agents as inhibitors of aspects of these disease processes involved in RA...
  100. ncbi Genotoxicity of plumbagin and its effects on catechol and NQNO-induced DNA damage in mouse lymphoma cells
    Jemal Demma
    Department of Pharmaceutical Biosciences, Uppsala University, Division of Toxicology, Box 594, BMC, SE 751 24 Uppsala, Sweden
    Toxicol In Vitro 23:266-71. 2009
    ..The fact that non-DNA damaging concentrations of plumbagin diminished the DNA damage induced by catechol, provides further support for the idea that plumbagin may act as an antioxidative agent at low concentrations...
  101. ncbi Efficacy of beta-lapachone in pancreatic cancer treatment: exploiting the novel, therapeutic target NQO1
    Matthew Ough
    Department of Surgery, University of Iowa College of Medicine, Iowa City, Iowa 52242, USA
    Cancer Biol Ther 4:95-102. 2005
    ....

Research Grants51

  1. Novel Mechanisms of Quinone Toxicity
    David Ross; Fiscal Year: 2013
    DESCRIPTION (provided by applicant): Both benzoquinones and naphthoquinones have been found to perturb protein handling and degradation in a variety of cellular systems...
  2. The Mechanism of Plumbagin-induced Stress Resistance and Lifespan Extension
    SUZANNE ELIZABETH BEREZOVSKY; Fiscal Year: 2013
    ..Plumbagin induces stress resistance at micromolar concentrations, about 0.1% the level required for other naphthoquinones to produce the same effect...
  3. PLANT TUMOR INHIBITORS
    David Kingston; Fiscal Year: 1980
    ..The synthesis of some modified naphthoquinones as potential anticancer agents will also be carried out as a small portion of this project.
  4. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2005
    ..abstract_text> ..
  5. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2002
    ..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
  6. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2008
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  7. SYNTHESIS OF ANTICANCER AGENTS
    K C Nicolaou; Fiscal Year: 2010
    ..abstract_text> ..
  8. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2004
    ..The proposed work is expected to have significant impact in the area of cancer chemotherapy and should provide enabling technologies and tools for biology and medicine. ..
  9. Sterol Metabolism in Pneumocystis
    EDNA KANESHIRO; Fiscal Year: 2009
    ....
  10. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2009
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
  11. NINTH INTERNATIONAL WORKSHOPS ON OPPORTUNISTIC PEOTISTS (IWOP-9)
    EDNA KANESHIRO; Fiscal Year: 2006
    ..As in several IWOP meetings in the past, the 2006 Workshops will be held jointly with the annual meetings of the International Society of Protistologists ( formerly Society of Protozoologists). ..
  12. Pneumocystis Biochemistry: Ubiquinones
    EDNA KANESHIRO; Fiscal Year: 2002
    ..carinii CoQ biosynthesis and growth in axenic cultures, and (4) develop atovaquone-resistant P. carinii populations to evaluate CoQ synthesis in sensitive and resistant organisms. ..
  13. A Molecular Motor
    T Kelly; Fiscal Year: 2004
    ..The project should expand the understanding of chemically directed and controlled movement, which is a topic central to the understanding of biological systems. ..
  14. THE SYNTHESIS OF LACTONAMYCIN AND ANALOGS
    T Kelly; Fiscal Year: 2003
    ..To test, in collaboration with Pfizer Inc., analogs and synthetic intermediates for antibiotic, anticancer and other biological activities. ..
  15. Reduction of Alkylating Quinones and Nitroarenes
    ANTONIO ALEGRIA; Fiscal Year: 2003
    ..Undergraduate students will participate in this project, thus improving their qualifications to pursue biomedical research careers. ..
  16. A Therapeutic Target for Microsporidiosis
    Louis Weiss; Fiscal Year: 2007
    ..In addition, the approaches and methods developed in this R21 should also prove useful for studies on methionine aminopeptidases as therapeutic targets in other pathogenic protists. [unreadable] [unreadable] [unreadable]..
  17. CHEMICAL DIVERSITY LIBRARIES FROM MEDICINAL PLANTS (RMI)
    Kuo Hsiung Lee; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  18. Second International Workshop on Microsporidia from Vertebrate and Invertebrate H
    Louis Weiss; Fiscal Year: 2007
    ..Overall, the goal of this[unreadable] congress is to foster the exchange of information between these diverse groups of[unreadable] scientists leading to advances in research on these emergent pathogens. ..
  19. Peroxiredoxin 1 in radiotherapy of lung cancer
    Young Mee Park; Fiscal Year: 2007
    ..abstract_text> ..
  20. BIOCHEMICAL REGULATORS OF BLEOMYCIN INDUCED TUMORS
    JOHN LAZO; Fiscal Year: 2001
    ..The Specific Aims are to: 1) develop cells and mice deficient in BH, 2) develop cells and mice that overexpress BH, 3) isolate and characterize potential proteins that interact with BH and, 4) analyze the regulation of BH expression. ..
  21. LUNG INJURY BY NAPHTHALENES
    Alan Buckpitt; Fiscal Year: 2009
    ..These studies are expected to identify appropriate biomarker targets and metabolic proteins where polymorphisms could be important in altering individual susceptibility. ..
  22. TOXOPLASMA ENCEPHALITIS IN AIDS: BRADYZOITE REGULATION
    Louis Weiss; Fiscal Year: 2009
    ....
  23. SYNTHESIS OF CHLOROPEPTINS, GP120 CD4 BINDING INHIBITORS
    AMOS SMITH; Fiscal Year: 2001
    ..abstract_text> ..
  24. PLANT ANTITUMOR AGENTS
    Kuo Hsiung Lee; Fiscal Year: 2009
    ....
  25. TRANSMISSION OF PNEUMOCYSTIS INFECTION
    Melanie Cushion; Fiscal Year: 2001
    ..These studies will result in a clearer understanding of the biology leading to infection with Pc and will provide a rational basis for clinical management and therapeutic intervention. ..
  26. In Vitro High Throughput Screening Assay for MKP-3(RMI)
    JOHN LAZO; Fiscal Year: 2005
    ..Nonetheless, no potent or selective small molecule inhibitors of this protein phosphatase have been identified. This proposal will provide sufficient reagents to permit a high throughput screening of 100,000 compounds ..
  27. Pittsburgh Molecular Libraries Screening Center(RMI)
    JOHN LAZO; Fiscal Year: 2008
    ..unreadable] [unreadable]..
  28. CDNA MICROARRAY TO DETECT CELLULAR RESPONSES TO MIXTURES
    Alan Buckpitt; Fiscal Year: 2001
    ..By examining library clones, these studies may identify new genes whose regulation is altered by chemical exposure. ..
  29. Alkynyliodonium Salts and Derived Diyls in Synthesis
    Ken Feldman; Fiscal Year: 2009
    ..abstract_text> ..
  30. New Methodology for Indole Alkaloid Syntheses
    Ken S Feldman; Fiscal Year: 2010
    ..The use of a new variant of the Pummerer reaction to control both oxidation level and reaction site within the indole nucleus forms the basis of this chemistry. ..
  31. ACQUISITION OF MIRCOARRAY SPOTTER, READER, SOFTWARE
    Alan Buckpitt; Fiscal Year: 2001
    ..abstract_text> ..
  32. NMR systems : 2 Bruker Avance 500 Consoles
    AMOS SMITH; Fiscal Year: 2006
    ..The areas of public health research include, among others, cancer, infectious diseases, neurodegenerative diseases such as Alzheimer's disease, and heart and cardiovascular disease. [unreadable] [unreadable] [unreadable]..
  33. Natural Product Leads for Drug Development
    KATHLYN PARKER; Fiscal Year: 2009
    ..Molecular modeling will allow the design of candidates for more active drugs. Candidates will be evaluated in the squalene synthase assay. Collaborations for the medicinal chemistry components of the project have been arranged. ..
  34. PNEUMOCYSTIS GENOME PROJECT
    Melanie Cushion; Fiscal Year: 2004
    ..Thus, there is but a single aim to this proposal: 1. To finish sequencing the genome of pneumocystis carinii and provide a completed assembly. ..
  35. International Congress on Microsporidiosis
    Louis Weiss; Fiscal Year: 2004
    ..Overall, the goal of this congress is to foster the exchange of information between these diverse groups of scientists leading to advances in research on these emergent pathogens. ..
  36. STRATEGIES AND METHODS IN SYNTHESIS OF NATURAL PRODUCTS
    KATHLYN PARKER; Fiscal Year: 2003
    ..During the period which corresponds to this proposal, we plan to apply our new methodology to the synthesis of deacetylravidomycin and kidamycin, representatives of the remaining two major classes. ..
  37. MECHANISM, SPECIFICITY & REGULATION: CDC25 PHOSPHATASES
    Johannes Rudolph; Fiscal Year: 2004
    ..Thus, this research will greatly expand the knowledge of cell cycle transitions, their control on a molecular basis, and their role in oncogenesis. ..
  38. Design and Synthesis of HIV-1 Protease Inhibitors
    AMOS SMITH; Fiscal Year: 2004
    ....
  39. Chemical Complementation Assay for MKP-3 (RMI)
    JOHN LAZO; Fiscal Year: 2005
    ..This proposal will provide sufficient reagents, including cells and DMA transfection vectors, to permit the high throughput screening of 100,000 compounds. ..
  40. Microsporidiosis:A Therapeutic Target
    Louis Weiss; Fiscal Year: 2003
    ....
  41. In Vitro High Throughput Screening Assay for MKP-1(RMI)
    JOHN LAZO; Fiscal Year: 2005
    ..No potent or selective small molecule inhibitors of this protein phosphatase are known. This proposal will provide sufficient reagents to permit a high throughput screening of 100,000 compounds. ..
  42. Chemical Complementation Assay for MKP-1 (RMI)
    JOHN LAZO; Fiscal Year: 2005
    ..This proposal will provide sufficient reagents, including cells and DMA transfection vectors, to permit the high throughput screening of 100,000 compounds. ..
  43. New Approaches for Development of PcP Therapy
    Melanie Cushion; Fiscal Year: 2006
    ..Finally, they will select the most efficacious combinations of agents and evaluate their effects on gene expression again using the macroarray approach. ..
  44. P450 MEDIATED LUNG TOXICITY
    Alan Buckpitt; Fiscal Year: 2002
    ....
  45. SYNTHESIS OF SPONGISTATIN ANTITUMOR AGENTS
    AMOS SMITH; Fiscal Year: 2007
    ..abstract_text> ..
  46. Eighth International Workshops on Opportunistic Protists
    Melanie Cushion; Fiscal Year: 2003
    ..Mead's and Cushion's ancestors include native Americans; Marciano-Cabral is Hispanic; Kaneshiro has Pacific-Asian ancestry; Lindsay, Weiss are white. Lindsay is a physically handicapped individual. ..
  47. Bleomycin Hydrolase and Alzheimer's Disease
    JOHN LAZO; Fiscal Year: 2004
    ..These studies should provide new mechanistic information concerning the pathogenesis of AD as well as reagents for future therapeutic studies. ..
  48. Cyanohydrin based fluorescent substrates of sEH (RMI)
    Christophe Morisseau; Fiscal Year: 2004
    ..This will be done by screening the combinatorial libraries from the "NIH Roadmap", libraries contracted from commercial vendors, and more defined libraries generated in house. ..
  49. PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTS
    Douglass Taber; Fiscal Year: 2007
    ..In the course of these investigations, new molecular reactivity will be developed that will substantially shorten current routes to polycyclic natural products and drug candidates. ..
  50. Tissue Transglutaminase in Neurologic Injury
    THUNG SHEN LAI; Fiscal Year: 2007
    ..The inhibitors will be used to investigate the role of TTG in the pathogenesis of expanded polyQ diseases. Current proposal will lead to new therapy for HD and other neurologic disorders. [unreadable] [unreadable] [unreadable]..
  51. Chemical and Biological Studies on Biaryl Phenolics
    Ken Feldman; Fiscal Year: 2005
    ..The search for selective 20S proteosome inhibitors among the Ntn-type proteases will be advanced by these investigations. ..