epoxy compounds

Summary

Top Publications

  1. ncbi Triptolide and its expanding multiple pharmacological functions
    Qiuyan Liu
    National Key Laboratory of Medical Immunology and Institute of Immunology, Second Military Medical University, 800 Xiangyin Road, Shanghai 200433, China
    Int Immunopharmacol 11:377-83. 2011
  2. pmc Triptolide downregulates Rac1 and the JAK/STAT3 pathway and inhibits colitis-related colon cancer progression
    Zhipeng Wang
    Department of Pharmacology, School of Pharmacy, The Fourth Military Medical University, Shaanxi Province 710032, China
    Exp Mol Med 41:717-27. 2009
  3. ncbi Treatment of db/db diabetic mice with triptolide: a novel therapy for diabetic nephropathy
    Qing Gao
    Research Institute of Nephrology, Jinling Hospital, Nanjing University School of Medicine, Nanjing, China
    Nephrol Dial Transplant 25:3539-47. 2010
  4. pmc Molecular understanding and modern application of traditional medicines: triumphs and trials
    Timothy W Corson
    Department of Molecular, Cellular and Developmental Biology, Yale University, New Haven, CT 06511, USA
    Cell 130:769-74. 2007
  5. ncbi Triptolide: structural modifications, structure-activity relationships, bioactivities, clinical development and mechanisms
    Zhao Li Zhou
    Division of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Zhangjiang Hi Tech Park, Shanghai, 201203, P R China
    Nat Prod Rep 29:457-75. 2012
  6. pmc Medicinal chemistry and pharmacology of genus Tripterygium (Celastraceae)
    Anita M Brinker
    Biotechnology Center for Agriculture and the Environment, Foran Hall, Cook College, Rutgers, The State University of New Jersey, 59 Dudley Road, New Brunswick, NJ 08901 8520, USA
    Phytochemistry 68:732-66. 2007
  7. pmc Heat shock protein 70 inhibits apoptosis in cancer cells through simultaneous and independent mechanisms
    Vikas Dudeja
    Department of Surgery, University of Minnesota, Minneapolis, Minnesota 55455, USA
    Gastroenterology 136:1772-82. 2009
  8. ncbi Potentiation of chemotherapeutic drugs by energy metabolism inhibitors 2-deoxyglucose and etomoxir
    Emma Hernlund
    Department of Oncology Pathology, Karolinska Institute, S 171 76 Stockholm, Sweden
    Int J Cancer 123:476-83. 2008
  9. ncbi Triptolide inhibits Bcr-Abl transcription and induces apoptosis in STI571-resistant chronic myelogenous leukemia cells harboring T315I mutation
    Xianping Shi
    Department of Pathophysiology, Zhongshan School of Medicine, The First Affiliated Hospital, Sun Yat Sen University, Guangzhou, China
    Clin Cancer Res 15:1686-97. 2009
  10. ncbi Triptolide, an inhibitor of the human heat shock response that enhances stress-induced cell death
    Sandy D Westerheide
    Department of Biochemistry, Molecular Biology, and Cell Biology, Rice Institute for Biomedical Research, Northwestern University, Evanston, Illinois 60208, USA
    J Biol Chem 281:9616-22. 2006

Research Grants

  1. SYNTHESIS OF SPONGISTATIN ANTITUMOR AGENTS
    AMOS SMITH; Fiscal Year: 2007
  2. SYNTHESIS OF CHLOROPEPTINS, GP120 CD4 BINDING INHIBITORS
    AMOS SMITH; Fiscal Year: 2001
  3. Design and Synthesis of HIV-1 Protease Inhibitors
    AMOS SMITH; Fiscal Year: 2004
  4. NMR systems : 2 Bruker Avance 500 Consoles
    AMOS SMITH; Fiscal Year: 2006
  5. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2004
  6. SYNTHESIS OF THE TEDANOLIDES, CYTOTOXIC POLYPROPIONATES
    Michael Jung; Fiscal Year: 2003
  7. SYNTHESIS OF ANTICANCER AGENTS
    K C Nicolaou; Fiscal Year: 2010
  8. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2005
  9. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2008
  10. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2002

Detail Information

Publications292 found, 100 shown here

  1. ncbi Triptolide and its expanding multiple pharmacological functions
    Qiuyan Liu
    National Key Laboratory of Medical Immunology and Institute of Immunology, Second Military Medical University, 800 Xiangyin Road, Shanghai 200433, China
    Int Immunopharmacol 11:377-83. 2011
    ..Importantly, PG490-88 has been approved entry into Phase I clinical trial for treatment of prostate cancer in USA. This review will focus on these breakthrough findings of triptolide and its implications...
  2. pmc Triptolide downregulates Rac1 and the JAK/STAT3 pathway and inhibits colitis-related colon cancer progression
    Zhipeng Wang
    Department of Pharmacology, School of Pharmacy, The Fourth Military Medical University, Shaanxi Province 710032, China
    Exp Mol Med 41:717-27. 2009
    ..This suggests that triptolide might be a candidate for prevention of colitis induced colon cancer because it reduces inflammation and prevents tumor formation and development...
  3. ncbi Treatment of db/db diabetic mice with triptolide: a novel therapy for diabetic nephropathy
    Qing Gao
    Research Institute of Nephrology, Jinling Hospital, Nanjing University School of Medicine, Nanjing, China
    Nephrol Dial Transplant 25:3539-47. 2010
    ..Herein, we investigated the therapeutic effects of triptolide on DN in db/db diabetic mice and studied the potential mechanisms...
  4. pmc Molecular understanding and modern application of traditional medicines: triumphs and trials
    Timothy W Corson
    Department of Molecular, Cellular and Developmental Biology, Yale University, New Haven, CT 06511, USA
    Cell 130:769-74. 2007
    ..Here, we highlight the challenges along this route, focusing on the compounds artemisinin, triptolide, celastrol, capsaicin, and curcumin...
  5. ncbi Triptolide: structural modifications, structure-activity relationships, bioactivities, clinical development and mechanisms
    Zhao Li Zhou
    Division of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Zhangjiang Hi Tech Park, Shanghai, 201203, P R China
    Nat Prod Rep 29:457-75. 2012
    ..This review will focus on the structural modifications, structure-activity relationships, pharmacology, and clinical development of triptolide in the last forty years...
  6. pmc Medicinal chemistry and pharmacology of genus Tripterygium (Celastraceae)
    Anita M Brinker
    Biotechnology Center for Agriculture and the Environment, Foran Hall, Cook College, Rutgers, The State University of New Jersey, 59 Dudley Road, New Brunswick, NJ 08901 8520, USA
    Phytochemistry 68:732-66. 2007
    ..This review discusses the biochemical composition and biological and pharmacological activities of Tripterygium extracts, and their main bioactive components...
  7. pmc Heat shock protein 70 inhibits apoptosis in cancer cells through simultaneous and independent mechanisms
    Vikas Dudeja
    Department of Surgery, University of Minnesota, Minneapolis, Minnesota 55455, USA
    Gastroenterology 136:1772-82. 2009
    ..We aimed to elucidate the mechanism by which HSP70 inhibits apoptosis in cancer cells...
  8. ncbi Potentiation of chemotherapeutic drugs by energy metabolism inhibitors 2-deoxyglucose and etomoxir
    Emma Hernlund
    Department of Oncology Pathology, Karolinska Institute, S 171 76 Stockholm, Sweden
    Int J Cancer 123:476-83. 2008
    ..We also conclude that although the potentiated drugs as yet have no obvious mechanistic factor in common, the strategy holds promise with genotoxic as well non-genotoxic anticancer drugs...
  9. ncbi Triptolide inhibits Bcr-Abl transcription and induces apoptosis in STI571-resistant chronic myelogenous leukemia cells harboring T315I mutation
    Xianping Shi
    Department of Pathophysiology, Zhongshan School of Medicine, The First Affiliated Hospital, Sun Yat Sen University, Guangzhou, China
    Clin Cancer Res 15:1686-97. 2009
    ..In the present study, we investigated the effect of triptolide on cell survival or apoptosis in CML cells bearing Bcr-Abl-T315I or wild-type Bcr-Abl...
  10. ncbi Triptolide, an inhibitor of the human heat shock response that enhances stress-induced cell death
    Sandy D Westerheide
    Department of Biochemistry, Molecular Biology, and Cell Biology, Rice Institute for Biomedical Research, Northwestern University, Evanston, Illinois 60208, USA
    J Biol Chem 281:9616-22. 2006
    ..The ability of triptolide to inhibit the heat shock response renders these cells sensitive to stress-induced cell death, which may be of great relevance to cancer treatments...
  11. pmc Inhibition of fatty acid metabolism reduces human myeloma cells proliferation
    Jose Manuel Tirado-Vélez
    Unidad de Investigacion, Hospital Universitario Puerta del Mar, Cadiz, Spain
    PLoS ONE 7:e46484. 2012
    ..In conclusion, inhibition of fatty acid metabolism represents a potential therapeutic approach to treat human multiple myeloma...
  12. pmc Triptolide inhibits MDM2 and induces apoptosis in acute lymphoblastic leukemia cells through a p53-independent pathway
    Mei Huang
    Department of Pediatrics, AFLAC Cancer and Blood Disorders Center, Emory University School of Medicine, Atlanta, Georgia 30322, USA
    Mol Cancer Ther 12:184-94. 2013
    ..These results suggest that increased inhibition of XIAP due to downregulation of MDM2 may play a critical role in triptolide-induced apoptosis in MDM2-overexpressing cancers...
  13. ncbi Triptolide therapy for neuroblastoma decreases cell viability in vitro and inhibits tumor growth in vivo
    Mara B Antonoff
    Department of Surgery, University of Minnesota, Minneapolis, MN 55455, USA
    Surgery 146:282-90. 2009
    ..Our objectives were to assess the effectiveness of triptolide, an Hsp-70 inhibitor, in treating neuroblastoma in vitro and in vivo, and to measure the associated effects on Hsp-70 levels and apoptosis markers...
  14. ncbi Triptolide and chemotherapy cooperate in tumor cell apoptosis. A role for the p53 pathway
    W T Chang
    Division of Pulmonary and Critical Care Medicine, Stanford University Medical Center, Stanford, California 94305-5236, USA
    J Biol Chem 276:2221-7. 2001
    ..Our data suggest that triptolide, by blocking p21-mediated growth arrest, enhances apoptosis in tumor cells...
  15. pmc Triptolide induces caspase-dependent cell death mediated via the mitochondrial pathway in leukemic cells
    Bing Z Carter
    Section of Molecular Hematology and Therapy, Department of Blood and Marrow Transplantation, The University of Texas, MD Anderson Cancer Center, Houston, 77030, USA
    Blood 108:630-7. 2006
    ..The potent antileukemic activity of triptolide in vitro warrants further investigation of this compound for the treatment of leukemias and other malignancies...
  16. ncbi 5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside-induced AMP-activated protein kinase phosphorylation inhibits basal and insulin-stimulated glucose uptake, lipid synthesis, and fatty acid oxidation in isolated rat adipocytes
    Mandeep Pinky Gaidhu
    School of Kinesiology and Health Science, York University, Toronto, Ontario M3J 1P3, Canada
    J Biol Chem 281:25956-64. 2006
    ....
  17. ncbi Immunosuppressive and anti-inflammatory mechanisms of triptolide, the principal active diterpenoid from the Chinese medicinal herb Tripterygium wilfordii Hook. f
    Daoming Qiu
    Division of Pulmonary and Critical Care Medicine, Stanford University Medical Center, Stanford, California 94305, USA
    Drugs R D 4:1-18. 2003
    ..Further characterisation of the molecular mechanisms of triptolide action will serve to elucidate pathways of immune system regulation...
  18. ncbi Triptolide induces pancreatic cancer cell death via inhibition of heat shock protein 70
    Phoebe A Phillips
    Department of Surgery, University of Minnesota, Minneapolis, Minnesota 55488, USA
    Cancer Res 67:9407-16. 2007
    ..Triptolide is a potential therapeutic agent that can be used to prevent the progression and metastases of pancreatic cancer...
  19. ncbi Enantioselective total synthesis of (+)-scuteflorin A using organocatalytic asymmetric epoxidation
    Christopher J Bartlett
    School of Chemistry, University of East Anglia, Norwich Research Park, Norwich, Norfolk NR4 7TJ, UK
    J Org Chem 77:772-4. 2012
    ..We report the first enantioselective total synthesis of (+)-scuteflorin A in 14% overall yield, employing a chiral iminium salt to effect an organocatalytic asymmetric epoxidation of xanthyletin in >99% ee as the key step...
  20. pmc Role of Hsp-70 in triptolide-mediated cell death of neuroblastoma
    Mara B Antonoff
    Department of Surgery, University of Minnesota, Minneapolis, Minnesota 55455, USA
    J Surg Res 163:72-8. 2010
    ..The principal objective of this study was to investigate the role of Hsp-70 in triptolide-mediated cell death in neuroblastoma...
  21. pmc Triptolide, histone acetyltransferase inhibitor, suppresses growth and chemosensitizes leukemic cells through inhibition of gene expression regulated by TNF-TNFR1-TRADD-TRAF2-NIK-TAK1-IKK pathway
    Byoungduck Park
    Cytokine Research Laboratory, Department of Experimental Therapeutics, The University of Texas MD Anderson Cancer Center, Houston, TX, USA
    Biochem Pharmacol 82:1134-44. 2011
    ..Overall, our results demonstrate that triptolide can block the inflammatory pathway activated by TNF-TNFR1-TRADD-TRAF2-NIK-TAK1-IKK, sensitizes cells to apoptosis, and inhibits invasion of tumor cells...
  22. ncbi The research on the anti-inflammatory activity and hepatotoxicity of triptolide-loaded solid lipid nanoparticle
    Zhinan Mei
    Department of Chemistry and Life Science, South Central University of Nationalities, Wuhan 430074, PR China
    Pharmacol Res 51:345-51. 2005
    ..The toxicity of TP-SLN to other tissues is under investigation...
  23. ncbi Triptolide-induced cell cycle arrest and apoptosis in human renal cell carcinoma cells
    Jingjie Li
    Department of Pharmacology, Zhong Shan School of Medicine, Sun Yat Sen University, Guangzhou, PR China
    Oncol Rep 25:979-87. 2011
    ..Therefore, triptolide emerges as a stimulator of apoptosis by influencing coordinate regulation of proliferation and apoptosis, and may be applicable to the treatment of human renal cell carcinoma...
  24. pmc Triptolide induces cell death independent of cellular responses to imatinib in blast crisis chronic myelogenous leukemia cells including quiescent CD34+ primitive progenitor cells
    Duncan H Mak
    Section of Molecular Hematology and Therapy, Department of Stem Cell Transplantation and Cellular Therapy, The University of Texas M D Anderson Cancer Center, Houston, TX 77030, USA
    Mol Cancer Ther 8:2509-16. 2009
    ....
  25. ncbi Triptolide ameliorates Crohn's colitis is associated with inhibition of TLRs/NF-κB signaling pathway
    Chao Yu
    Department of General Surgery, Jinling Hospital, Medical School of Nanjing University, Nanjing, PR China
    Fitoterapia 82:709-15. 2011
    ..These findings also support the possibility that targeted inhibition of TLR signaling pathway is an approach deserving further investigation as a therapeutic strategy for CD...
  26. ncbi Triptolide inhibits COX-2 expression and PGE2 release by suppressing the activity of NF-kappaB and JNK in LPS-treated microglia
    Yuntao Gong
    Department of Neurobiology, School of Basic Medical Sciences, Peking University Health Science Center, Ministry of Education, Key Laboratory for Neuroscience, Beijing, China
    J Neurochem 107:779-88. 2008
    ..Taken together, these results suggest that triptolide may suppress neuroinflammation via a mechanism that involves inactivation of two parallel signaling pathways: p38-NF-kappaB-COX-2-PGE(2) and JNK-PGE(2)...
  27. ncbi Analysis of hemoglobin adducts from acrylamide, glycidamide, and ethylene oxide in paired mother/cord blood samples from Denmark
    Hans von Stedingk
    Department of Materials and Environmental Chemistry, Environmental Chemistry Unit, Arrhenius Laboratory, Stockholm University, SE 106 91 Stockholm, Sweden
    Chem Res Toxicol 24:1957-65. 2011
    ..The evaluation of the new analytical method showed that it is suitable for monitoring of background exposures of the investigated electrophilic compounds in large population studies...
  28. ncbi Effect of triptolide on focal adhesion kinase and survival in MCF-7 breast cancer cells
    Bee Jen Tan
    Department of Pharmacy, Faculty of Science, National University of Singapore, Singapore 117543, Singapore
    Oncol Rep 26:1315-21. 2011
    ..In conclusion, our data present the first evidence of triptolide-mediated induction of FAK cleavage that correlates with cell detachment and loss of adhesion potential to the extracellular matrix...
  29. ncbi Novel target genes responsive to the anti-growth activity of triptolide in endometrial and ovarian cancer cells
    Haili Li
    Department of Obstetrics and Gynecology, Oita University Faculty of Medicine, Oita, Japan
    Cancer Lett 297:198-206. 2010
    ..We found a strong anticancer activity of TPL and identified some potential target genes of this drug, raising hopes that TPL may become a useful therapy for endometrial and ovarian cancers...
  30. ncbi Triptolide attenuate the oxidative stress induced by LPS/D-GalN in mice
    Yan Lu
    State Key Laboratory of Pharmaceutical Biotechnology, and Model Animal Research Center MARC of Nanjing University, Nanjing University, Nanjing 210093, China
    J Cell Biochem 113:1022-33. 2012
    ..These results showed that triptolide can effectively reduce the oxidative stress and partially rescue the damage in the liver induced by LPS/D-GalN...
  31. ncbi Dietary acrylamide exposure and hemoglobin adducts--National Health and Nutrition Examination Survey (2003-04)
    N L Tran
    E x ponent, Inc, Washington, DC 20036, USA
    Food Chem Toxicol 48:3098-108. 2010
    ....
  32. ncbi Effects of cytochrome P4503A inducer dexamethasone on the metabolism and toxicity of triptolide in rat
    Xiaochuan Ye
    Institute of Materia Medica, College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan, China
    Toxicol Lett 192:212-20. 2010
    ..This suggested that TP might decrease nephrotoxicity induced by DXM. These studies indicated that DXM had significant impact on the metabolism and the toxicity of TP as a therapeutic agent...
  33. ncbi The telltale structures of epoxide hydrolases
    Michael Arand
    Institute of Pharmacology and Toxicology, University of Wuerzburg, Wuerzburg, Germany
    Drug Metab Rev 35:365-83. 2003
    ....
  34. ncbi Heat shock protein 72 protects kidney proximal tubule cells from injury induced by triptolide by means of activation of the MEK/ERK pathway
    Zhipeng Wang
    Department of Pharmacology, School of Pharmacy, Fourth Military Medical University, Xi an, Shaanxi, 710032, China
    Int J Toxicol 28:177-89. 2009
    ..Collectively, our results suggested that HSP72 plays a protective role by means of the MEK/ERK pathway, against triptolide-induced kidney injury...
  35. pmc Triptolide-induced suppression of phospholipase D expression inhibits proliferation of MDA-MB-231 breast cancer cells
    Dong Woo Kang
    Department of Molecular Biology, College of Natural Science, Pusan National University, Busan 609 735, Korea
    Exp Mol Med 41:678-85. 2009
    ..Taken together, we demonstrate that triptolide suppresses the expression of PLD via inhibition of NFkappaB activation and then decreases cell proliferation...
  36. pmc XPB, a subunit of TFIIH, is a target of the natural product triptolide
    Denis V Titov
    Department of Pharmacology and Molecular Sciences, The Johns Hopkins University School of Medicine, Baltimore, Maryland, USA
    Nat Chem Biol 7:182-8. 2011
    ..These findings also suggest that triptolide can serve as a new molecular probe for studying transcription and, potentially, as a new type of anticancer agent through inhibition of the ATPase activity of XPB...
  37. ncbi Triptolide inhibits rat vascular smooth muscle cell proliferation and cell cycle progression via attenuation of ERK1/2 and Rb phosphorylation
    Rong Tao
    Department of Cardiology, Ruijin Hospital, Jiao Tong University, Shanghai 200025, China
    Exp Mol Pathol 90:137-42. 2011
    ..In the present study, we investigated effects of triptolide on in-stent restenosis in vivo and in vitro, and study the biological mechanism of this drug...
  38. ncbi Role of triptolide as an adjunct chemotherapy for ovarian cancer
    Suzanne D Westfall
    Center for Reproductive Biology, School of Molecular Biosciences, Washington State University, Pullman, WA 99164 4231, USA
    Chemotherapy 54:67-76. 2008
    ....
  39. ncbi Triptolide sensitizes lung cancer cells to TNF-related apoptosis-inducing ligand (TRAIL)-induced apoptosis by inhibition of NF-kappaB activation
    Kye Young Lee
    Department of Internal Medicine, Dankook University College of Medicine, Cheonan, Korea
    Exp Mol Med 34:462-8. 2002
    ..These observations suggest that triptolide may be a potentially useful drug to enhance TRAIL-induced tumor killing in lung cancer...
  40. ncbi Triptolide overcomes dexamethasone resistance and enhanced PS-341-induced apoptosis via PI3k/Akt/NF-kappaB pathways in human multiple myeloma cells
    Min Yang
    Department of Hematology, Zhejiang University, Hangzhou 310003, People s Republic of China
    Int J Mol Med 22:489-96. 2008
    ....
  41. ncbi Functional p53 is required for triptolide-induced apoptosis and AP-1 and nuclear factor-kappaB activation in gastric cancer cells
    X H Jiang
    Department of Gastroenterology, Rui-Jin Hospital, Shanghai, Peoples Republic of China
    Oncogene 20:8009-18. 2001
    ..However, a functional p53 is required for these proapoptotic, anti-inflammatory and anti-tumor effects...
  42. pmc Triptolide and TRAIL combination enhances apoptosis in cholangiocarcinoma
    Kimberly A Clawson
    Department of Surgery, Division of Basic and Translational Research, University of Minnesota, Minneapolis, Minnesota 55455, USA
    J Surg Res 163:244-9. 2010
    ..The principal objective of this study was to determine the effects of combination therapy with TRAIL and triptolide in cholangiocarcinoma...
  43. ncbi Triptolide simultaneously induces reactive oxygen species, inhibits NF-kappaB activity and sensitizes 5-fluorouracil in colorectal cancer cell lines
    Bing Xu
    Research Institute in Healthcare Science, School of Applied Sciences, University of Wolverhampton, Wolverhampton WV1 1SB, UK
    Cancer Lett 291:200-8. 2010
    ..PG490 and 5-FU treatment induced activated caspase 3 and Bax expression and inhibited Bcl-2 expression. PG490 simultaneously induced generation of reactive oxygen species (ROS) and inhibited NF-kappaB transcriptional activity...
  44. ncbi RNA-mediated sequestration of the RNA helicase eIF4A by Pateamine A inhibits translation initiation
    Marie Eve Bordeleau
    Department of Biochemistry, McGill University, McIntyre Medical Sciences Building, 3655 Promenade Sir William Osler, Montreal, Quebec H3G 1Y6, Canada
    Chem Biol 13:1287-95. 2006
    ..We demonstrate that Pateamine A is a chemical inducer of dimerization that forces an engagement between eIF4A and RNA and prevents eIF4A from participating in the ribosome-recruitment step of translation initiation...
  45. ncbi Triptolide impairs dendritic cell migration by inhibiting CCR7 and COX-2 expression through PI3-K/Akt and NF-kappaB pathways
    Qiuyan Liu
    Institute of Immunology and National Key Laboratory of Medical Immunology, Second Military Medical University, 800 Xiangyin Road, Shanghai 200433, PR China
    Mol Immunol 44:2686-96. 2007
    ..Therefore, inhibition of DC migration through decreasing COX-2 and CCR7 expression via PI3-K/Akt and NF-kappaB signal pathways provides additional mechanistic explanation for triptolide's immunosuppressive effect...
  46. ncbi Oral administration of triptolide ameliorates the clinical signs of experimental autoimmune encephalomyelitis (EAE) by induction of HSP70 and stabilization of NF-kappaB/IkappaBalpha transcriptional complex
    Pablo Kizelsztein
    Biotech Center, SEBS, Rutgers University, 59 Dudley Road, New Brunswick, NJ 08901, USA
    J Neuroimmunol 217:28-37. 2009
    ..These effects might be explained by the increase in Hsp70 levels driven by triptolide and stabilization of the NF-kappaB/IkappaBalpha complex leading to an attenuated inflammatory response...
  47. ncbi Eukaryotic initiation factor 2alpha-independent pathway of stress granule induction by the natural product pateamine A
    Yongjun Dang
    Department of Pharmacology and Molecular Sciences, Solomon H Snyder Department of Neuroscience, and Department of Oncology, Johns Hopkins School of Medicine, Baltimore, MD 21205, USA
    J Biol Chem 281:32870-8. 2006
    ....
  48. ncbi Pharmacokinetic study of triptolide, a constituent of immunosuppressive chinese herb medicine, in rats
    Feng Shao
    Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, China
    Biol Pharm Bull 30:702-7. 2007
    ..It was indicated that triptolide was metabolized extensively, eliminated rapidly, and also showed that the toxicity produced by the triptolide was lag behind the exposure concentration...
  49. ncbi Triptolide inhibits amyloid-beta1-42-induced TNF-alpha and IL-1beta production in cultured rat microglia
    Jian Jiao
    Neuroscience Research Institute and Department of Neurobiology, Peking University, Key Laboratory for Neuroscience of the Ministry of Education, 38 Xueyuan Road, Beijing 100083, PR China
    J Neuroimmunol 205:32-6. 2008
    ..Our results showed that oligomeric Abeta played an important role in mediating neuroinflammation and triptolide was able to suppress the production of pro-inflammatory cytokines from microglia...
  50. pmc Synergistic effect of triptolide combined with 5-fluorouracil on colon carcinoma
    Xiao Yan Tang
    Department of Gastroenterology, Zhongnan Hospital of Wuhan University, Wuhan, Hubei Province, China
    Postgrad Med J 83:338-43. 2007
    ..To investigate the inhibitive effects of triptolide (TPL) combined with 5-fluorouracil (5-FU) on colon carcinoma HT-29 cells in vitro and in vivo and their side effects...
  51. pmc Identification of triptolide, a natural diterpenoid compound, as an inhibitor of lung inflammation
    Gary W Hoyle
    Department of Environmental and Occupational Health Sciences, School of Public Health and Information Sciences, University of Louisville, Louisville, KY 40202, USA
    Am J Physiol Lung Cell Mol Physiol 298:L830-6. 2010
    ..The results demonstrate that triptolide exhibits anti-inflammatory activity in cultured lung cells and in an in vivo model of acute lung injury...
  52. ncbi Sex differences in subacute toxicity and hepatic microsomal metabolism of triptolide in rats
    Li Liu
    Jiangsu Center of Drug Screening, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210038, China Department of Pharmacology, School of Medicine, Yangzhou University, Yangzhou 225001, China
    Toxicology 271:57-63. 2010
    ..Results suggested that CYP3A2 made an important contribution to the sex-related metabolism of triptolide, which may result in the sex differences in triptolide toxicity...
  53. ncbi Triptolide inactivates Akt and induces caspase-dependent death in cervical cancer cells via the mitochondrial pathway
    Min Jung Kim
    Shinsegae Women s Hospital, Busan, Korea
    Int J Oncol 37:1177-85. 2010
    ..These findings show that triptolide induces caspase-dependent, mitochondria-mediated apoptosis in cervical cancer cells, in part, by negatively regulating Akt and Mcl-1...
  54. ncbi Biologic activity of triptolide in t(8;21) acute myeloid leukemia cells
    Gui sheng Zhou
    Laboratory of Molecular Carcinogenesis and Targeted Therapy for Cancer, Guangzhou Institute of Biomedicine and Health and State Key Laboratory of Biomembrane and Membrane Biotechnology, Institute of Zoology, Chinese Academy of Sciences, China
    Leuk Res 35:214-8. 2011
    ..Triptolide downregulates p65 and inhibits the DNA-binding activity of NF-κB. Our data indicate that triptolide might be an effective agent for t(8;21) leukemia...
  55. ncbi Triptolide induces Bcl-2 cleavage and mitochondria dependent apoptosis in p53-deficient HL-60 cells
    Chi Keung Wan
    Department of Biology and Chemistry, Bioactive Products Research Group, City University of Hong Kong, Kowloon, Hong Kong SAR, China
    Cancer Lett 241:31-41. 2006
    ....
  56. ncbi Triptolide, a novel diterpenoid triepoxide from Tripterygium wilfordii Hook. f., suppresses the production and gene expression of pro-matrix metalloproteinases 1 and 3 and augments those of tissue inhibitors of metalloproteinases 1 and 2 in human synovial
    N Lin
    Institute of Chinese Materia Medica, China Academy of Traditional Chinese Medicine, Beijing
    Arthritis Rheum 44:2193-200. 2001
    ..Triptolide's interference with gene expression of proinflammatory cytokines and its known inhibitory effects on PGE2 production are also probably very effective...
  57. ncbi PG490-88, a derivative of triptolide, causes tumor regression and sensitizes tumors to chemotherapy
    John M Fidler
    Pharmagenesis, Inc, Palo Alto, CA, USA
    Mol Cancer Ther 2:855-62. 2003
    ..Our findings that PG490-88 causes tumor regression and that it acts in synergy with DNA-damaging chemotherapeutic agents suggest a role as an antineoplastic agent and chemosensitizer for the treatment of patients with solid tumors...
  58. ncbi Triptolide is an inhibitor of RNA polymerase I and II-dependent transcription leading predominantly to down-regulation of short-lived mRNA
    Stéphane Vispé
    Centre de Recherche en Oncologie Expérimentale, Institut de Recherche Pierre Fabre, 3 rue des Satellites, BP94244, Toulouse Cedex 4, 31432 France
    Mol Cancer Ther 8:2780-90. 2009
    ..Overall, the data shed light on the effect of triptolide on transcription, along with its novel potential applications in cancers, including acute myeloid leukemia, which is in part driven by the aforementioned oncogenic factors...
  59. ncbi Highly enantioselective epoxidation of alpha, beta-unsaturated esters by chiral dioxirane
    Xin Yan Wu
    Department of Chemistry, Colorado State University, Fort Collins, Colorado 80523, USA
    J Am Chem Soc 124:8792-3. 2002
    ..High ee's have been obtained for a number of trans and trisubstituted substrates (82-98% ee). The results described show that it is feasible for dioxiranes to effectively epoxidize electron-deficient olefins with high ee's...
  60. ncbi Methionine aminopeptidases type I and type II are essential to control cell proliferation
    Sylvie G Bernier
    Department of Preclinical Research, Praecis Pharmaceuticals Incorporated, Waltham, Massachusetts 02451, USA
    J Cell Biochem 95:1191-203. 2005
    ..These results suggest that MetAP-1 and MetAP-2 have essential functions in the control of mammalian cell proliferation and that MetAP-dependent growth control is evolutionarily highly conserved...
  61. pmc Triptolide (TPL) inhibits global transcription by inducing proteasome-dependent degradation of RNA polymerase II (Pol II)
    Ying Wang
    Department of Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, People s Republic of China
    PLoS ONE 6:e23993. 2011
    ....
  62. ncbi Pramanicin induces apoptosis in Jurkat leukemia cells: a role for JNK, p38 and caspase activation
    O Kutuk
    Biological Sciences and Bioengineering Program, Sabanci University, 34956 Tuzla, Istanbul, Turkey
    Apoptosis 10:597-609. 2005
    ..These results suggest pramanicin as a potential apoptosis-inducing small molecule, which acts through a well-defined JNK- and p38-dependent apoptosis signalling pathway in Jurkat T leukemia cells...
  63. ncbi Oxaziridinium salts as hydrophobic epoxidation reagents: remarkable hydrophobically-directed selectivity in olefin epoxidation
    Mark R Biscoe
    Department of Chemistry, Columbia University, New York, NY 10027, USA
    J Am Chem Soc 127:10812-3. 2005
    ..Furthermore, the oxaziridinium ions could be generated with oxone from catalytic amounts of the corresponding iminium salts. These substrate selectivities should also carry over to positional selectivities in polyenes...
  64. ncbi Dietary exposure to chemical migrants from food contact materials: a probabilistic approach
    M J Holmes
    Department for Environment, Food and Rural Affairs, Central Science Laboratory, Sand Hutton, York, UK
    Food Addit Contam 22:907-19. 2005
    ....
  65. ncbi On the enantioselective olefin epoxidation by doubly bridged biphenyl azepine derivatives--mixed tropos/atropos chiral biaryls
    Jérôme Vachon
    Department of Organic Chemistry, University of Geneva, Quai Ernest Ansermet 30, CH 1211 Geneva 4, Switzerland
    Org Biomol Chem 5:501-6. 2007
    ....
  66. ncbi Inhibition of vascular endothelial growth factor expression and production by triptolide
    Ke Bin Hu
    Planta Med 68:368-9. 2002
    ..This effect may be one of the mechanisms underlying the therapeutic effects of triptolide on rheumatoid arthritis...
  67. ncbi Clinical outcomes in children with Henoch-Schönlein purpura nephritis grade IIIa or IIIb
    Yonghui Xia
    Department of Nephrology, The Children s Hospital, Zhejiang University School of Medicine, Hangzhou 310006, Zhejiang Province, China
    Pediatr Nephrol 26:1083-8. 2011
    ..Our results may also suggest that treatment with steroid may not alter the clinical outcome of such grade IIIa or IIIb patients...
  68. ncbi Triptolide functions as a potent angiogenesis inhibitor
    Ming Fang He
    Department of Biology, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong, People s Republic of China
    Int J Cancer 126:266-78. 2010
    ..Our findings suggest that antitumor action of triptolide is partly via inhibition of tumor angiogenesis by blocking 2 endothelial receptor-mediated signaling pathways, and triptolide can be a promising antiangiogenic agent...
  69. ncbi Triptolide inhibits the growth and metastasis of solid tumors
    Shanmin Yang
    Department of Oncology, Georgetown University Medical Center, Washington, DC 20007, USA
    Mol Cancer Ther 2:65-72. 2003
    ..Taken together, these results suggest that TPL has several attractive features as a new antitumor agent...
  70. pmc Potent in vitro and in vivo anticancer activities of des-methyl, des-amino pateamine A, a synthetic analogue of marine natural product pateamine A
    Galina Kuznetsov
    Division of Biological Research, and 3Scientific Administration, Eisai Research Institute of Boston, Inc, Andover, Massachusetts 01810, USA
    Mol Cancer Ther 8:1250-60. 2009
    ..DMDA-PatA thus represents a promising natural product-based anticancer agent that warrants further investigation...
  71. pmc A methionine aminopeptidase-2 inhibitor, PPI-2458, for the treatment of rheumatoid arthritis
    Sylvie G Bernier
    Department of Preclinical Research, PRAECIS Pharmaceuticals, Incorporated, 830 Winter Street, Waltham, MA 02451, USA
    Proc Natl Acad Sci U S A 101:10768-73. 2004
    ....
  72. pmc Inhibition of nonsense-mediated mRNA decay by the natural product pateamine A through eukaryotic initiation factor 4AIII
    Yongjun Dang
    Department of Pharmacology, Howard Hughes Medical Institute, Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA
    J Biol Chem 284:23613-21. 2009
    ..Furthermore, we have characterized the mechanisms by which PatA and cycloheximide modulate NMD. Unlike CHX, PatA was found to inhibit NMD by a novel mechanism that is independent of the phosphorylation of Up-frameshift protein 1...
  73. ncbi [Research progress on immunosuppressive activity of monomers extracted from Chinese medicine]
    Shiqin Sun
    Harbin Medical University Daqing Campus, Department of Pharmacy, Daqing 163319, China
    Zhongguo Zhong Yao Za Zhi 35:393-6. 2010
    ....
  74. ncbi Triptolide, a Chinese herbal extract, enhances drug sensitivity of resistant myeloid leukemia cell lines through downregulation of HIF-1α and Nrf2
    Feili Chen
    Department of Hematology, Nanfang Hospital, Southern Medical University, Guangzhou 510515, PR China
    Pharmacogenomics 14:1305-17. 2013
    ..To explore whether triptolide (TPL) can enhance drug sensitivity of resistant myeloid leukemia cell lines through downregulation of HIF-1α and Nrf2...
  75. ncbi Synergistic effect of triptolide and tacrolimus on rat cardiac allotransplantation
    Ruzheng Li
    Department of Cardiovascular Surgery, Juntendo University School of Medicine, Tokyo, Japan
    Jpn Heart J 45:657-65. 2004
    ..These results suggest that triptolide is a moderately effective immunosuppressive agent. Triptolide combined with a subtherapeutic dose of tacrolimus produced a synergistic effect in prolonging rat cardiac allograft survival...
  76. ncbi The epoxy group of pramanicin is required for the optimal endothelium-dependent relaxation of rat aorta
    Chiu Yin Kwan
    Department of Medicine, Faculty of Health Sciences, McMaster University, Ontario, Canada
    J Pharmacol Sci 92:203-8. 2003
    ..The potent, selective, and irreversible inhibitory effect of PMC on the endothelial function points to its potential development into an anti-angiogenic drug...
  77. ncbi Effects of triptolide from Tripterygium wilfordii on ERalpha and p53 expression in two human breast cancer cell lines
    Jing Liu
    National Center of Drug Screening, China Pharmaceutical University, 1 Shennong Road, Nanjing 210038, China
    Phytomedicine 16:1006-13. 2009
    ..The results showed that triptolide is much more sensitive to ERalpha-positive MCF-7 cells than to ERalpha-negative MDA-MB-231 cells, and the sensitivity is significantly associated with the ERalpha and p53 status...
  78. pmc Triptolide reduces cystogenesis in a model of ADPKD
    Stephanie J Leuenroth
    Yale University, Department MCD Biology, P O Box 208103, New Haven, CT 06520 8103, USA
    J Am Soc Nephrol 19:1659-62. 2008
    ..Because the proliferative index of kidney epithelium in neonates versus adults is significantly different, future studies will need to address whether triptolide delays or reduces cyst progression in the Pkd1 adult model...
  79. ncbi Knockout of hepatic P450 reductase aggravates triptolide-induced toxicity
    Xiang Xue
    Center for Drug Safety Evaluation and Research, State Key Laboratory of New Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China
    Toxicol Lett 205:47-54. 2011
    ..It is suggested that P450 inhibition/inactivation might pose a significant health risk in the clinic use of triptolide...
  80. ncbi Triptolide promotes generation of FoxP3+ T regulatory cells in rats
    Gutian Zhang
    Department of Urology, Nanjing Drum Tower Hospital, Nanjing University Medical School, 321 Zhong Shan Road, Nanjing 210008, China
    J Ethnopharmacol 125:41-6. 2009
    ..Triptolide (TPT), a component of the Chinese herb Triptergium wilfordii, has potent immunosuppressive and anti-inflammatory activity and is used clinically in recipients of kidney transplantation...
  81. ncbi Pramanicin, an antifungal agent, raises cytosolic Ca2+ and causes cell death in vascular endothelial cells
    Chiu Yin Kwan
    Department of Medicine, HSC 4N40, Faculty of Health Sciences, McMaster University, 1200 Main Street West, Hamilton, Ontario, Canada L8N 3Z5
    Vascul Pharmacol 40:35-42. 2003
    ....
  82. ncbi Mechanism of triptolide-induced apoptosis: Effect on caspase activation and Bid cleavage and essentiality of the hydroxyl group of triptolide
    Xianxi Wang
    Department of Pediatrics, Center for Developmental Pharmacology and Toxicology, Children s Research Institute, The Ohio State University, Columbus, OH 43205, USA
    J Mol Med (Berl) 84:405-15. 2006
    ..Our results indicate that both the apoptosis-promoting and the antiinflammatory activities of triptolide depend on the 14-OH group...
  83. pmc Increased accumulation of hypoxia-inducible factor-1α with reduced transcriptional activity mediates the antitumor effect of triptolide
    Zhao Li Zhou
    Division of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
    Mol Cancer 9:268. 2010
    ..However, the anticancer action mechanisms of triptolide remains to be further investigated. Here we used human ovarian SKOV-3 cancer cells as a model to probe the effect of triptolide on HIF-1α...
  84. ncbi Antiproliferative and proapoptotic activities of triptolide (PG490), a natural product entering clinical trials, on primary cultures of human prostatic epithelial cells
    Taija M Kiviharju
    Department of Urology, Stanford University School of Medicine, Stanford, California 94305 5118, USA
    Clin Cancer Res 8:2666-74. 2002
    ..Our preclinical studies suggest that triptolide might be an effective preventive as well as therapeutic agent against prostate cancer and that triptolide may activate a functional p53 pathway in prostate cells...
  85. ncbi Structure of human epoxide hydrolase reveals mechanistic inferences on bifunctional catalysis in epoxide and phosphate ester hydrolysis
    German A Gomez
    Roy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104 6323, USA
    Biochemistry 43:4716-23. 2004
    ..Natl. Acad. Sci. U.S.A. 100, 1558-1563]. The binding of Mg(2+)-HPO4(2-) to the N-terminal domain of human sEH in its CIU complex reveals structural features relevant to those of the enzyme-substrate complex in the phosphatase reaction...
  86. ncbi [Progress in research on mechanisms of anti-rheumatoid arthritis of triptolide]
    Chun Fang Liu
    Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China
    Zhongguo Zhong Yao Za Zhi 31:1575-9. 2006
    ..Triptolide is a potent immunosuppressant...
  87. ncbi In vivo doses of acrylamide and glycidamide in humans after intake of acrylamide-rich food
    Anna C Vikström
    Department of Materials and Environmental Chemistry, Environmental Chemistry Unit, Arrhenius Laboratory, Stockholm University, SE 106 91 Stockholm, Sweden
    Toxicol Sci 119:41-9. 2011
    ..Furthermore, the values of AUC-AA and AUC-GA are five and two times higher, respectively, than the corresponding values for F344 rats exposed to AA at levels as in published cancer bioassays...
  88. ncbi Chlorohydrins of bisphenol A diglycidyl ether (BADGE) and of bisphenol F diglycidyl ether (BFDGE) in canned foods and ready-to-drink coffees from the Japanese market
    Y Uematsu
    Tokyo Metropolitan Research Laboratory of Public Health, Japan
    Food Addit Contam 18:177-85. 2001
    ..2HCl anti BFDGE.HCl.H2O at a level of 1.5 mg/kg. A Beilstein test confirmed that all cans containing foods contaminated with BADGE.2HCl or BFDGE.2HCl had at lest one part coated with a PVC organosol...
  89. ncbi Involvement of mitochondrial pathway in triptolide-induced cytotoxicity in human normal liver L-02 cells
    Jincheng Yao
    National Center of Drug Screening, China Pharmaceutical University, 1 Shennong Road, Nanjing 210038, China
    Biol Pharm Bull 31:592-7. 2008
    ..Triptolide-increased activity of caspase 9 and caspase 3 was also observed. These results indicate that triptolide induced cytotoxicity in L-02 cells by apoptosis, which is mediated through mitochondrial pathway...
  90. ncbi A strategy for position-selective epoxidation of polyprenols
    Vijay Gnanadesikan
    Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, USA
    J Am Chem Soc 130:8089-93. 2008
    ..5 mM. With polyprenol substrates having the hydroxyl function at one terminus, the internal epoxidation can be directed at the double bond of the polyprenol, which is either four or five away from the terminal hydroxyprenyl subunit...
  91. ncbi Experimental AA amyloidosis in mice is inhibited by treatment with triptolide, a purified traditional Chinese medicine
    Dan Cui
    First Department of Pathology, Yamaguchi University School of Medicine, 1 1 1 Minami kogushi, Ube, Yamaguchi 755 8505, Japan
    Int Immunopharmacol 7:1232-40. 2007
    ..These results suggest that through suppression of IL-6, triptolide can reduce production of SAA. Amyloid deposition is prevented when levels of the amyloid-forming precursor protein SAA are decreased significantly...
  92. ncbi [Effect of tripterygium polyglucoside on T-lymphocyte subsets and serum interleukin-5 level in asthma patients]
    X H Wang
    Medical Department of Respiratory Diseases, Affiliated Hospital of Nanjing Railway Medical College, Nanjing 210009
    Zhongguo Zhong Xi Yi Jie He Za Zhi 21:25-7. 2001
    ..61, P < 0.01). CONCLUSION: TII is highly effective in treating asthma through regulating T-lymphocyte subset disorder and inhibiting production of IL-5...
  93. ncbi Differential effects of triptolide and tetrandrine on activation of COX-2, NF-kappaB, and AP-1 and virus production in dengue virus-infected human lung cells
    Jun Ting Liou
    Division of Cardiology, Department of Medicine, Tri Service General Hospital, School of Medicine, National Defense Medical Center, Taipei, Taiwan, ROC
    Eur J Pharmacol 589:288-98. 2008
    ..Our findings imply that triptolide and tetrandrine may attenuate dengue virus infection in human lung cells, but through distinct pathways...
  94. ncbi The effect of etomoxir on insulin sensitivity in type 2 diabetic patients
    A Hubinger
    Diabetes Forschungsinstitut Düsseldorf, Universitat Dusseldorf, Germany
    Horm Metab Res 24:115-8. 1992
    ..We conclude that Etomoxir improves insulin sensitivity in type 2 diabetic patients...
  95. ncbi Levels of bisphenol A diglycidyl ether (BADGE) and bisphenol F diglycidyl ether (BFDGE) in canned liquid infant formula products in Canada and dietary intake estimates
    Xu Liang Cao
    Health Canada, Food Research Division, Bureau of Chemical Safety, Food Directorate, 251 Frederick Banting Driveway, AL 2203D, Ottawa, ON, Canada K1A 0K9
    J AOAC Int 92:1780-9. 2009
    ..The maximum PDI of BADGE was 22 microg/kg body weight/day for the 12-18 months old with the maximum formula intake. The maximum PDI of BFDGE was < 3.4 microg/kg body weight/day...
  96. pmc Aspartate-catalyzed asymmetric epoxidation reactions
    Gorka Peris
    Department of Chemistry, Yale University, P O Box 208107, New Haven, Connecticut 06520 8107, USA
    J Am Chem Soc 129:8710-1. 2007
  97. ncbi Triptolide inhibits cyclooxygenase-2 and inducible nitric oxide synthase expression in human colon cancer and leukemia cells
    Xiangmin Tong
    Institute of Hematologic Disease, Department of Hematology, First Affiliated Hospital, Medical School, Zhejiang University, Hangzhou 310003, China
    Acta Biochim Biophys Sin (Shanghai) 39:89-95. 2007
    ..These results indicated that the inhibition of the inflammatory factor COX-2 and iNOS activity could be involved in the antitumor mechanisms of TP...
  98. ncbi New structural and chemical insight into the catalytic mechanism of epoxide hydrolases
    R N Armstrong
    Department of Biochemistry, Center in Molecular Toxicology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 0146, USA
    Drug Metab Rev 32:327-38. 2000
    ..The data reveal that, in addition to the catalytic triad located in the core domain that carries out the hydrolytic reaction, there are two tyrosine residues, located in the cap domain, which assist in the initial alkylation event...
  99. ncbi Synthesis and biological evaluation of novel triptolide analogues for anticancer activity
    Bing Zhou
    Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Road Zu Chong Zhi, Zhangjiang Hi Tech Park, Shanghai 201203, PR China
    Bioorg Med Chem Lett 20:6217-21. 2010
    ..05nM for SKOV-3 cells, clearly challenging the traditional viewpoint on the necessity of 9,11-β-epoxide group of triptolide. In addition, structure-activity relationships for three classes of compounds were studied...
  100. ncbi Anti-tumour and immuno-modulation effects of triptolide-loaded polymeric micelles
    Lingyun Xu
    College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan, China
    Eur J Pharm Biopharm 70:741-8. 2008
    ..Therefore, TP encapsulated in polymeric micelles does not demonstrate immuno-suppressive activity but does not lose its anti-tumour effect. These results show that polymeric micelles are a promising carrier for cancer therapy using TP...
  101. pmc Triptolide inhibits IL-12/IL-23 expression in APCs via CCAAT/enhancer-binding protein alpha
    Yan Zhang
    Department of Microbiology and Immunology, Weill Medical College, eill Graduate School of Medical Sciences, Cornell University, New York, NY 10065, USA
    J Immunol 184:3866-77. 2010
    ..This study provides mechanistic insights into the immunomodulatory capacity of triptolide and has strong implications for its therapeutic applications in autoimmune diseases...

Research Grants68

  1. SYNTHESIS OF SPONGISTATIN ANTITUMOR AGENTS
    AMOS SMITH; Fiscal Year: 2007
    ..abstract_text> ..
  2. SYNTHESIS OF CHLOROPEPTINS, GP120 CD4 BINDING INHIBITORS
    AMOS SMITH; Fiscal Year: 2001
    ..abstract_text> ..
  3. Design and Synthesis of HIV-1 Protease Inhibitors
    AMOS SMITH; Fiscal Year: 2004
    ....
  4. 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]..
  5. 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. ..
  6. SYNTHESIS OF THE TEDANOLIDES, CYTOTOXIC POLYPROPIONATES
    Michael Jung; Fiscal Year: 2003
    ....
  7. SYNTHESIS OF ANTICANCER AGENTS
    K C Nicolaou; Fiscal Year: 2010
    ..abstract_text> ..
  8. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2005
    ..abstract_text> ..
  9. 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. ..
  10. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2002
    ..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
  11. 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. ..
  12. Asymmetric Synthesis of Cytotoxic Natural Products
    Robert Coleman; Fiscal Year: 2005
    ..abstract_text> ..
  13. 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. ..
  14. Azinomycins - Total Synthesis and Mechanism of Action
    Robert Coleman; Fiscal Year: 2007
    ..abstract_text> ..
  15. LC-MS/MS Methods for Analysis of Hemoglogbin Adducts
    Timothy Fennell; Fiscal Year: 2004
    ..abstract_text> ..
  16. Synthesis of Tumor Inhibitory Marine Natural Products
    James Marshall; Fiscal Year: 2004
    ..The main chemical issues to be addressed include the control of stereochemistry by means of chiral organometal chemistry and the design of new and efficient routes to structurally novel natural products. ..
  17. Hospital and Community Acquired Acute Renal Failure
    Glenn Chertow; Fiscal Year: 2006
    ..This study will efficiently inform the Nephrology community by providing a foundation of fundamental information (ARF definitions, incidence, consequences and costs) upon which a clinical trials network can be built. ..
  18. Asymmetric Aminocatalysis
    SUBHASH SINHA; Fiscal Year: 2003
    ..2) Designing novel aminocatalysts for aldol, Mannich, and Michael reactions. (3) High-throughput screening of aminocatalytic libraries. (4) Synthesizing biologically active natural products and drugs using aminocatalysis. ..
  19. Selective Antibody Conjugates
    Subhash C Sinha; Fiscal Year: 2010
    ..This strategy has the advantage that only a single antibody is required for a multiplicity of tasks and it taps into the unlimited chemical diversity and the specificity that can be engendered by organic synthesis. ..
  20. SYNTHESIS OF ANNONACEOUS ACETOGENINS AND ANALOGUES
    James Marshall; Fiscal Year: 2001
    ..The synthetic approach will employ chiral allylic and allenic organometal reagents to introduce stereogenic centers with concurrent formation of carbon-carbon bonds. ..
  21. Diepoxide Cross-Linking of DNA
    JULIE MILLARD; Fiscal Year: 2003
    ..Denaturing PAGE will also be used to characterize DNA reaction products of epichiorohydrin to elucidate the impact of a three-carbon chain length in cross-linking. ..
  22. ONTOGENY OF METABOLIC CONTROLS OF INGESTIVE BEHAVIOR
    SUSAN SWITHERS; Fiscal Year: 2002
    ..Finally, the neural mechanisms involved in translating physiological changes related to energy utilization into increases in ingestive behavior are tested. ..
  23. NEW STRATEGIES FOR GLYCOCONJUGATE SYNTHESIS
    Frank McDonald; Fiscal Year: 2005
    ....
  24. Microbial metabolism of aliphatic alkenes & epoxides
    SCOTT ENSIGN; Fiscal Year: 2008
    ..We intend to further our work on the central roles of carboxylation and novel cofactors/enzymes in bacterial hydrocarbon/epoxide/ketone metabolism by pursuing the biochemical, structural, and genetic characterization of these processes. ..
  25. Neural basis of learned food aversion and nausea
    CHARLES HORN; Fiscal Year: 2009
    ..Effective treatment of nausea may substantially improve the quality of life for patients with chronic disease. ..
  26. CONTROL OF FEEDING BEHAVIOR--HEPATIC AFFERENT SIGNALING
    CHARLES HORN; Fiscal Year: 2002
    ..Results from this project may contribute to a better understanding of metabolic stimuli that are sensed by the nervous system, and may elucidate neural controls that are involved in obesity, anorexia, and diabetes. ..
  27. UMKC School of Dentistry Oral and Craniofacial Biology
    J Eick; Fiscal Year: 2006
    ..unreadable] [unreadable] [unreadable]..
  28. 20-HETE IN NO-MEDIATED REGULATION OF RENAL FUNCTION
    Adebayo Oyekan; Fiscal Year: 2001
    ....
  29. ASYMMETRIC SYNTHESIS OF VANCOMYCIN ANTIBIOTICS
    David Evans; Fiscal Year: 2001
    ..During the course of this project we intend to confirm (correct) the absolute stereochemical assignments of the principal members of this family by total synthesis. ..
  30. ASYMMETRIC SYNTHESIS OF IONOPHORE/MACROLIDE ANTIBIOTICS
    David Evans; Fiscal Year: 2005
    ..Our goal has been to set in place all of the reactions necessary for the rapid assemblage of any polyketide target structure. ..
  31. Novel Amino Acid-Based Glass-Ionomer Biomaterials
    Dong Xie; Fiscal Year: 2005
    ..abstract_text> ..
  32. CONFORMATION ACTIVITY RELATIONSHIPS
    Richard Taylor; Fiscal Year: 2003
    ..This increased understanding of epothilone's mode of action at the molecular level will allow for the preparation of the next generation of microtubule-stabilizing anti-mitotic agents. ..
  33. Conformation-Activity Relationships
    Richard Taylor; Fiscal Year: 2009
    ..Moreover, where appropriate, we have incorporated the development of a number of new synthetic methods for the preparation of complex structural units common to polyketide natural products. ..
  34. MYRIAPORONES: SYNTHETIC AND BIOLOGICAL STUDIES
    Richard Taylor; Fiscal Year: 2003
    ..abstract_text> ..
  35. The Role of N1-Inosine Adducts in Butadiene Mutagenesis
    Gunnar Boysen; Fiscal Year: 2005
    ..Addressing this hypothesis is essential for determining the sources of BD mutations and will ultimately increase our ability to accurately assess the risk of BD to humans. ..
  36. SYNTHESIS OF NATURAL PRODUCTS WITH OXAZOLE MOIETIES
    Peter Wipf; Fiscal Year: 2005
    ..The proposed program represents a multi-dimensional effort to increase the basic knowledge of the function of marine natural products, establish new methods in heterocyclic chemistry, and identify novel pharmacophores. ..
  37. Novel Nanostructured Dental Glass-Ionomers for Advanced Dental Restoratives
    Dong Xie; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  38. Synthesis of Polyketides and Terpenes
    David A Evans; Fiscal Year: 2010
    ..As a consequence, organic synthesis is a critical discipline that continues to have an important impact on the fields of both medicine and biology. ..
  39. BIOCHEMICAL MODEL REACTIONS
    Ronald Breslow; Fiscal Year: 2007
    ..In addition, both parts of the project will help us understand natural enzymes. [unreadable] [unreadable]..
  40. New Methods for Simultaneous Arming and SAR Studies of Natural Products
    Daniel Romo; Fiscal Year: 2010
    ..Subsequent SAR studies (this proposal) will be pursued to identify potential new bioactivities and suitable sites for probe attachment enabling subsequent mode of action studies (not in this proposal) relevant to these diseases. ..
  41. Sequence Distribution of Tabacco Carcinogen-DNA Adducts
    Natalia Tretyakova; Fiscal Year: 2007
    ..The proposed research is significant because of the widespread human exposure to tobacco products and because of their central role in the initiation of lung cancer in humans. ..
  42. Integrated Wireless Tracking and Dosimetry for Radiation Oncology
    Babak Ziaie; Fiscal Year: 2008
    ..The paragraphs that we have added or changed in response to the review use a different font (Palatino Linotype). [unreadable] [unreadable] [unreadable]..
  43. Inhibition of Alzheimer's Beta-Amyloid Fibril Formation
    Duy Hua; Fiscal Year: 2009
    ..However, soluble oligomeric Abeta showed high neuronal toxicity. Inhibition of the formation of these toxic soluble Abeta oligomers would provide therapeutics for AD. ..
  44. CNS Fatty Acid Metabolism in Regulation of Food Intake
    Susan Aja; Fiscal Year: 2007
    ..We will measure changes in intracellular AMP/ATP ratio and activity of AMP-activated protein kinase, levels of mRNAs for feeding-related neuropeptides, and neuropeptide production and release. ..
  45. SYNTHETIC/MECHANISTIC STUDIES OF BIOACTIVE MARINE AGENTS
    Daniel Romo; Fiscal Year: 2008
    ..In this regard, several unique strategies are outlined for the synthesis of the natural product targets proposed. [unreadable] [unreadable]..
  46. Structural and Functional Studies on Proteins
    Jon Clardy; Fiscal Year: 2007
    ..This scan, if successful, would provide functional annotation for the endogenous function of previously characterized small molecules. Finally, some polypeptides with antibiotic activity will be investigated. ..
  47. PATHOPHYSIOLOGICAL ROLE OF 12-R-LIPOXYGENASE
    ALAN BRASH; Fiscal Year: 2002
    ..abstract_text> ..
  48. HEPATIC MECHANISM FOR CONTROL OF FOOD INTAKE
    Mark Friedman; Fiscal Year: 2003
    ..To address this, an experiment will be performed to determine whether a metabolic hunger signal originates from hepatocytes. ..
  49. 9th International Neurotoxicology Assoc (INA9) Meeting
    Michael Aschner; Fiscal Year: 2003
    ....
  50. DEVELOPMENT OF LIGAND ASSISTED ASYMMETRIC SYNTHESES
    Arun Ghosh; Fiscal Year: 2001
    ..Besides the broad range of scope and generality, this line of research will provide excellent opportunities to teach and train graduate and undergraduate students in the laboratory. ..
  51. Lovelace Respiratory Symposium 2003
    Rogene Henderson; Fiscal Year: 2003
    ..Future topics will be developed with the same sensitivity to meeting the information needs of our audience. Continuing medical education credits are available through the University of New Mexico School of Medicine. ..
  52. Acquisition of a 500 MHz NMR Spectrometer
    Scott Rychnovsky; Fiscal Year: 2004
    ..This new instrument will bring much needed new capabilities to the NMR facility and will greatly facilitate the research programs of the PI and co-PIs of this proposal. ..
  53. TRIOXANES FOR CHEMOTHERAPY OF MALARIA AND CANCER
    Gary Posner; Fiscal Year: 2005
    ....
  54. Enzyme Repair of Excoyclic Adducts
    Bo Hang; Fiscal Year: 2005
    ..abstract_text> ..
  55. Nutritional/Inflammatory Evaluation of Dialysis Patients
    Kamyar Kalantar Zadeh; Fiscal Year: 2005
    ....
  56. Alkyllithium Cyclizations in Organic Snythesis
    Scott Rychnovsky; Fiscal Year: 2005
    ..These compounds are of interest to synthetic and medicinal chemists, and have the types of rigid, polycyclic and polar structures found to show high bioactivity in many assays. ..
  57. SYNTHESIS OF COCARCINOGENIC DITERPENES
    JAMES RIGBY; Fiscal Year: 2005
    ..These projected investigations should generate substantial new knowledge about complex synthesis as well as providing additional insight into some of the bioactivity exhibited by the subject natural products. ..
  58. Pathophysiology of Arginine-induced Pancreatitis in Mice
    Ashok Saluja; Fiscal Year: 2006
    ..Successful completion of these studies will provide an excellent model of pancreatitis for future studies dealing with therapeutic interventions. ..
  59. SYNTHESIS OF CYTOTOXIC GUAIANOLIDES AND OTHER TERPENOIDS
    JAMES RIGBY; Fiscal Year: 2006
    ..unreadable] [unreadable]..
  60. Novel epoxide hydrolase inhibitor for stroke prevention
    JOHN IMIG; Fiscal Year: 2005
    ..In the Phase II work, Arete Therapeutics will use the collected information to progress toward clinical trials in the area of stroke and possible new therapeutic avenues. ..
  61. FANCONI ANEMIA--HETEROGENEITY AND CARRIER DETECTION
    ARLEEN AUERBACH; Fiscal Year: 2007
    ..This will be combined with functional complementation[unreadable] in an effort to accelerate the identification of these genes.[unreadable] [unreadable]..
  62. Mechanisms of Regulation of GLUT4 Expression
    ANN OLSON; Fiscal Year: 2005
    ..abstract_text> ..
  63. Insulin Regulation of Adipocyte Microtubules
    ANN OLSON; Fiscal Year: 2008
    ..unreadable] [unreadable]..
  64. Synthesis of (-)-cananodine, an alkaloid active against hepatocellular carcinoma
    JAMES VYVYAN; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  65. Regulation of Mammalian Oocyte Maturation
    Stephen Downs; Fiscal Year: 2007
    ..Furthermore, these studies will benefit the development of in vitro systems where either meiotic arrest or completion of meiotic maturation is the desired endpoint. ..
  66. Gene transfer to the kidney using lentiviral vectors
    Frank Park; Fiscal Year: 2004
    ..abstract_text> ..