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[PMID]:28460485
[Au] Autor:Lv LX; Zhou ZX; Zhou Z; Zhang LJ; Yan R; Zhao Z; Yang LY; Bian XY; Jiang HY; Li YD; Sun YS; Xu QQ; Hu GL; Guan WJ; Li YQ
[Ad] Endereço:Institute of Pharmaceutical Biotechnology and College of Pharmaceutical Sciences, Zhejiang University, 310058 Hangzhou, China.
[Ti] Título:Hispidin induces autophagic and necrotic death in SGC-7901 gastric cancer cells through lysosomal membrane permeabilization by inhibiting tubulin polymerization.
[So] Source:Oncotarget;8(16):26992-27006, 2017 Apr 18.
[Is] ISSN:1949-2553
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Hispidin and its derivatives are widely distributed in edible mushrooms. Hispidin is more cytotoxic to A549, SCL-1, Bel7402 and Capan-1 cancer cells than to MRC5 normal cells; by contrast, hispidin protects H9c2 cardiomyoblast cells from hydrogen peroxide-induced or doxorubicin-induced apoptosis. Consequently, further research on how hispidin affects normal and cancer cells may help treat cancer and reduce chemotherapy-induced side effects. This study showed that hispidin caused caspase-independent death in SGC-7901 cancer cells but not in GES-1 normal cells. Hispidin-induced increases in LC3-II occurred in SGC-7901 cells in a time independent manner. Cell death can be partially inhibited by treatment with ATG5 siRNA but not by autophagy or necroptosis inhibitors. Ultrastructural evidence indicated that hispidin-induced necrotic cell death involved autophagy. Hispidin-induced lysosomal membrane permeabilization (LMP) related to complex cell death occurred more drastically in SGC-7901 cells than in GES-1 cells. Ca2+ rather than cathepsins from LMP contributed more to cell death. Hispidin induced microtubule depolymerization, which can cause LMP, more drastically in SGC-7901 cells than in GES-1 cells. At 4.1 µM, hispidin promoted cell-free tubulin polymerization but at concentrations higher than 41 µM, hispidin inhibited polymerization. Hispidin did not bind to tubulin. Alterations in microtubule regulatory proteins, such as stathmin phosphorylation at Ser16, contributed to hispidin-induced SGC-7901 cell death. In conclusion, hispidin at concentrations higher than 41 µM may inhibit tubulin polymerization by modulating microtubule regulatory proteins, such as stathmin, causing LMP and complex SGC-7901 cell death. This mechanism suggests a promising novel treatment for human cancer.
[Mh] Termos MeSH primário: Autofagia/efeitos dos fármacos
Membranas Intracelulares/efeitos dos fármacos
Lisossomos/metabolismo
Multimerização Proteica/efeitos dos fármacos
Pironas/farmacologia
Tubulina (Proteína)/metabolismo
[Mh] Termos MeSH secundário: Apoptose/efeitos dos fármacos
Caspases/metabolismo
Morte Celular/efeitos dos fármacos
Linhagem Celular Tumoral
Seres Humanos
Microtúbulos/química
Microtúbulos/metabolismo
Óxido Nítrico/biossíntese
Permeabilidade
Fosforilação
Estatmina/metabolismo
Tubulina (Proteína)/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Pyrones); 0 (STMN1 protein, human); 0 (Stathmin); 0 (Tubulin); 31C4KY9ESH (Nitric Oxide); EC 3.4.22.- (Caspases); SSJ18CG55E (hispidin)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170503
[St] Status:MEDLINE
[do] DOI:10.18632/oncotarget.15935


  2 / 3656 MEDLINE  
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[PMID]:29371602
[Au] Autor:Gélinas R; Mailleux F; Dontaine J; Bultot L; Demeulder B; Ginion A; Daskalopoulos EP; Esfahani H; Dubois-Deruy E; Lauzier B; Gauthier C; Olson AK; Bouchard B; Des Rosiers C; Viollet B; Sakamoto K; Balligand JL; Vanoverschelde JL; Beauloye C; Horman S; Bertrand L
[Ad] Endereço:Pole of Cardiovascular Research, Institut de Recherche Expérimentale et Clinique, Université catholique de Louvain, Brussels, 1200, Belgium.
[Ti] Título:AMPK activation counteracts cardiac hypertrophy by reducing O-GlcNAcylation.
[So] Source:Nat Commun;9(1):374, 2018 01 25.
[Is] ISSN:2041-1723
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:AMP-activated protein kinase (AMPK) has been shown to inhibit cardiac hypertrophy. Here, we show that submaximal AMPK activation blocks cardiomyocyte hypertrophy without affecting downstream targets previously suggested to be involved, such as p70 ribosomal S6 protein kinase, calcineurin/nuclear factor of activated T cells (NFAT) and extracellular signal-regulated kinases. Instead, cardiomyocyte hypertrophy is accompanied by increased protein O-GlcNAcylation, which is reversed by AMPK activation. Decreasing O-GlcNAcylation by inhibitors of the glutamine:fructose-6-phosphate aminotransferase (GFAT), blocks cardiomyocyte hypertrophy, mimicking AMPK activation. Conversely, O-GlcNAcylation-inducing agents counteract the anti-hypertrophic effect of AMPK. In vivo, AMPK activation prevents myocardial hypertrophy and the concomitant rise of O-GlcNAcylation in wild-type but not in AMPKα2-deficient mice. Treatment of wild-type mice with O-GlcNAcylation-inducing agents reverses AMPK action. Finally, we demonstrate that AMPK inhibits O-GlcNAcylation by mainly controlling GFAT phosphorylation, thereby reducing O-GlcNAcylation of proteins such as troponin T. We conclude that AMPK activation prevents cardiac hypertrophy predominantly by inhibiting O-GlcNAcylation.
[Mh] Termos MeSH primário: Proteínas Quinases Ativadas por AMP/genética
Acetilglucosamina/metabolismo
Cardiomegalia/genética
Miocárdio/metabolismo
Miócitos Cardíacos/metabolismo
Transferases de Grupos Nitrogenados/genética
[Mh] Termos MeSH secundário: Proteínas Quinases Ativadas por AMP/deficiência
Acetilglucosamina/farmacologia
Acilação/efeitos dos fármacos
Animais
Animais Recém-Nascidos
Azasserina/farmacologia
Compostos Azo/farmacologia
Cardiomegalia/metabolismo
Cardiomegalia/patologia
Ativação Enzimática/efeitos dos fármacos
Ativadores de Enzimas/farmacologia
Regulação da Expressão Gênica
Glicosilação/efeitos dos fármacos
Ventrículos do Coração/efeitos dos fármacos
Ventrículos do Coração/metabolismo
Ventrículos do Coração/patologia
Masculino
Camundongos
Camundongos Knockout
Miocárdio/patologia
Miócitos Cardíacos/efeitos dos fármacos
Miócitos Cardíacos/patologia
Transferases de Grupos Nitrogenados/antagonistas & inibidores
Transferases de Grupos Nitrogenados/metabolismo
Norleucina/análogos & derivados
Norleucina/farmacologia
Fosforilação/efeitos dos fármacos
Cultura Primária de Células
Pironas/farmacologia
Ratos
Ratos Wistar
Transdução de Sinais
Tiofenos/farmacologia
Troponina T/genética
Troponina T/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (6-diazo-5-oxonorleucine); 0 (A 769662); 0 (Azo Compounds); 0 (Enzyme Activators); 0 (Pyrones); 0 (Thiophenes); 0 (Troponin T); 832C8OV84S (Norleucine); 87299V3Q9W (Azaserine); EC 2.6.- (Nitrogenous Group Transferases); EC 2.6.1.16 (Gfpt1 protein, mouse); EC 2.7.11.1 (AMPK alpha2 subunit, mouse); EC 2.7.11.31 (AMP-Activated Protein Kinases); V956696549 (Acetylglucosamine)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180215
[Lr] Data última revisão:
180215
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180127
[St] Status:MEDLINE
[do] DOI:10.1038/s41467-017-02795-4


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[PMID]:28901768
[Au] Autor:Mazzeo G; Cimmino A; Masi M; Longhi G; Maddau L; Memo M; Evidente A; Abbate S
[Ad] Endereço:Dipartimento di Medicina Molecolare e Traslazionale, Università degli Studi di Brescia , Viale Europa 11, 25123 Brescia, Italy.
[Ti] Título:Importance and Difficulties in the Use of Chiroptical Methods to Assign the Absolute Configuration of Natural Products: The Case of Phytotoxic Pyrones and Furanones Produced by Diplodia corticola.
[So] Source:J Nat Prod;80(9):2406-2415, 2017 Sep 22.
[Is] ISSN:1520-6025
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:α-Pyrones and furanones are metabolites produced by Diplodia corticola, a pathogen of cork oak. Previously, the absolute configuration (AC) of diplopyrone was defined by chiroptical methods and Mosher's method. Using X-ray and chiroptical methods, the AC of sapinofuranone C was assigned, while that of the (4S,5S)-enantiomer of sapinofuranone B was established by enantioselective total synthesis. Diplofuranone A and diplobifuranylones A-C ACs are still unassigned. Here electronic and vibrational circular dichroism (ECD and VCD) and optical rotatory dispersion (ORD) spectra are reported and compared with density functional theory computations. The AC of the (4S,5S)-enantiomer of sapinofuranone B and sapinofuranone C is checked for completeness. The AC of diplobifuranylones A-C is assigned as (2S,2'S,5'S,6'S), (2S,2'R,5'S,6'R), and (2S,2'S,5'R,6'R), respectively, with the Mosher's method applied to define the absolute configuration of the carbinol stereogenic carbon. The AC assignment of sapinofuranones is problematic: while diplofuranone A is (4S,9R), sapinofuranones B and C are (4S,5S) according to ORD and VCD, but not to ECD. To eliminate these ambiguities, ECD and VCD spectra of a di-p-bromobenzoate derivative of sapinofuranone C are measured and calculated. For phytotoxicity studies, it is relevant that all six compounds share the S configuration for the stereogenic carbon atom of the lactone moiety.
[Mh] Termos MeSH primário: Alcenos/química
Produtos Biológicos/química
Furanos/química
Lactonas/química
Pironas/química
Quercus/química
[Mh] Termos MeSH secundário: Alcenos/toxicidade
Ascomicetos
Dicroísmo Circular
Furanos/toxicidade
Lactonas/toxicidade
Estrutura Molecular
Dispersão Óptica Rotatória
Pironas/toxicidade
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkenes); 0 (Biological Products); 0 (Furans); 0 (Lactones); 0 (Pyrones); 0 (diplobifuranylone A); 0 (diplobifuranylone B); 0 (diplopyrone); 0 (sapinofuranone B)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170914
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jnatprod.7b00119


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[PMID]:28884584
[Au] Autor:Hussain H; Al-Sadi AM; Schulz B; Steinert M; Khan A; Green IR; Ahmed I
[Ad] Endereço:UoN Chair of Oman's Medicinal Plants & Marine Natural Products, University of Nizwa, PO Box 33, Birkat Al Mauz, Nizwa 616, Sultanate of Oman.
[Ti] Título:A fruitful decade for fungal polyketides from 2007 to 2016: antimicrobial activity, chemotaxonomy and chemodiversity.
[So] Source:Future Med Chem;9(14):1631-1648, 2017 Sep.
[Is] ISSN:1756-8927
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The last three decades have shown that the fungi can be 'biofactories' of novel, bioactive secondary metabolites that produce numerous natural products with novel skeletons and biological activities. Particularly in the last 10 years, large numbers of antimicrobial fungal secondary metabolites have been discovered. This review provides an overview of key, defining developments of the last 10 years regarding the discovery of antimicrobial activity, chemotaxonomy and chemodiversity of fungal polyketides.
[Mh] Termos MeSH primário: Anti-Infecciosos/química
Fungos/química
Policetídeos/química
[Mh] Termos MeSH secundário: Antraquinonas/química
Antraquinonas/isolamento & purificação
Antraquinonas/farmacologia
Anti-Infecciosos/isolamento & purificação
Anti-Infecciosos/farmacologia
Benzofenonas/química
Benzofenonas/isolamento & purificação
Benzofenonas/farmacologia
Cumarínicos/química
Cumarínicos/isolamento & purificação
Cumarínicos/farmacologia
Depsídeos/química
Depsídeos/isolamento & purificação
Depsídeos/farmacologia
Fungos/metabolismo
Bactérias Gram-Negativas/efeitos dos fármacos
Bactérias Gram-Positivas/efeitos dos fármacos
Lactonas/química
Lactonas/isolamento & purificação
Lactonas/farmacologia
Policetídeos/isolamento & purificação
Policetídeos/farmacologia
Pironas/química
Pironas/isolamento & purificação
Pironas/farmacologia
Xantonas/química
Xantonas/isolamento & purificação
Xantonas/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anthraquinones); 0 (Anti-Infective Agents); 0 (Benzophenones); 0 (Coumarins); 0 (Depsides); 0 (Lactones); 0 (Polyketides); 0 (Pyrones); 0 (Xanthones); 3580-77-6 (depsidone); 701M4TTV9O (benzophenone)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171025
[Lr] Data última revisão:
171025
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170909
[St] Status:MEDLINE
[do] DOI:10.4155/fmc-2017-0028


  5 / 3656 MEDLINE  
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[PMID]:28881289
[Au] Autor:Tempone AG; Ferreira DD; Lima ML; Costa Silva TA; Borborema SET; Reimão JQ; Galuppo MK; Guerra JM; Russell AJ; Wynne GM; Lai RYL; Cadelis MM; Copp BR
[Ad] Endereço:Centre for Parasitology and Mycology, Instituto Adolfo Lutz, Avenida Dr. Arnaldo, 351, 8° Andar. Cerqueira César, CEP 01246-902 São Paulo, SP, Brazil. Electronic address: atempone@usp.br.
[Ti] Título:Efficacy of a series of alpha-pyrone derivatives against Leishmania (L.) infantum and Trypanosoma cruzi.
[So] Source:Eur J Med Chem;139:947-960, 2017 Oct 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:The neglected tropical diseases Chagas disease and leishmaniasis affect together more than 20 million people living mainly in developing countries. The mainstay of treatment is chemotherapy, however the drugs of choice, which include benznidazole and miltefosine, are toxic and have numerous side effects. Safe and effective therapies are urgently needed. Marine alpha-pyrones have been previously identified as scaffolds with potential antiprotozoan activities. In this work, using a phenotypic screen, twenty-seven examples of 3-substituted 4-hydroxy-6-methyl alpha-pyrones were synthesized and their antiparasitic efficacy evaluated against Leishmania (L.) infantum and Trypanosoma cruzi in order to evaluate structure-activity relationships within the series. The mechanism of action and the in vivo efficacy of the most selective compound against T. cruzi were evaluated using different techniques. In vitro data indicated that compounds 8, 15, 25, 26 and 28 presented IC values in the range between 13 and 54 µM against L. infantum intracellular amastigotes. Among them, hexanoyl substituted pyrone 8 was the most selective and potent, with a Selectivity Index (SI) > 14. Fifteen of the alpha-pyrones were effective against T. cruzi trypomastigotes, with 3-undecanoyl (11) and 3-tetradecanoyl (12) substituted pyrones being the most potent against trypomastigotes, with IC values of 1 and 2 µM, respectively, and SI higher than 70. Using flow cytometry and fluorescent-based assays, pyrone 12 was found to induce hyperpolarization of the mitochondrial membrane potential of T. cruzi, without affecting plasma membrane permeability. An experimental acute phase-murine model, demonstrated that in vivo dosing of 12 (30 mg/kg/day; 5 days), had no efficacy at the first parasitemia onset of T. cruzi, but reduced the second onset by 55% (p < 0.05), suggesting a delayed action in BALB/c mice. Additionally, a histopathology study demonstrated no toxic effects to the treated mice. The finding that several 3-substituted alpha-pyrones have in vitro efficacy against both L. infantum and T. cruzi, and that one analogue exhibited moderate and non-toxic in vivo efficacy against T. cruzi is encouraging, and suggests that this compound class should be explored as long-term treatments in experimental Chagas disease.
[Mh] Termos MeSH primário: Antiprotozoários/farmacologia
Leishmania infantum/efeitos dos fármacos
Pironas/farmacologia
Trypanosoma cruzi/efeitos dos fármacos
[Mh] Termos MeSH secundário: Antiprotozoários/síntese química
Antiprotozoários/química
Relação Dose-Resposta a Droga
Estrutura Molecular
Testes de Sensibilidade Parasitária
Pironas/síntese química
Pironas/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antiprotozoal Agents); 0 (Pyrones)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171016
[Lr] Data última revisão:
171016
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170908
[St] Status:MEDLINE


  6 / 3656 MEDLINE  
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[PMID]:28854735
[Au] Autor:Wang S; Pike AM; Lee SS; Strong MA; Connelly CJ; Greider CW
[Ad] Endereço:Department of Molecular Biology and Genetics, Johns Hopkins University School of Medicine, Baltimore, MD 21205, USA.
[Ti] Título:BRD4 inhibitors block telomere elongation.
[So] Source:Nucleic Acids Res;45(14):8403-8410, 2017 Aug 21.
[Is] ISSN:1362-4962
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Cancer cells maintain telomere length equilibrium to avoid senescence and apoptosis induced by short telomeres, which trigger the DNA damage response. Limiting the potential for telomere maintenance in cancer cells has been long been proposed as a therapeutic target. Using an unbiased shRNA screen targeting known kinases, we identified bromodomain-containing protein 4 (BRD4) as a telomere length regulator. Four independent BRD4 inhibitors blocked telomere elongation, in a dose-dependent manner, in mouse cells overexpressing telomerase. Long-term treatment with BRD4 inhibitors caused telomere shortening in both mouse and human cells, suggesting BRD4 plays a role in telomere maintenance in vivo. Telomerase enzymatic activity was not directly affected by BRD4 inhibition. BRD4 is in clinical trials for a number of cancers, but its effects on telomere maintenance have not been previously investigated.
[Mh] Termos MeSH primário: Proteínas Nucleares/genética
Homeostase do Telômero/genética
Encurtamento do Telômero/genética
Fatores de Transcrição/genética
[Mh] Termos MeSH secundário: Acetanilidas/farmacologia
Animais
Azepinas/farmacologia
Southern Blotting
Linhagem Celular
Relação Dose-Resposta a Droga
Fibroblastos/citologia
Fibroblastos/efeitos dos fármacos
Fibroblastos/metabolismo
Expressão Gênica/efeitos dos fármacos
Células HeLa
Compostos Heterocíclicos com 3 Anéis/farmacologia
Compostos Heterocíclicos de 4 ou mais Anéis/farmacologia
Seres Humanos
Hibridização in Situ Fluorescente
Camundongos
Morfolinas/farmacologia
Proteínas Nucleares/antagonistas & inibidores
Proteínas Nucleares/metabolismo
Pironas/farmacologia
Interferência de RNA
Telomerase/genética
Telomerase/metabolismo
Telômero/efeitos dos fármacos
Telômero/enzimologia
Telômero/genética
Homeostase do Telômero/efeitos dos fármacos
Encurtamento do Telômero/efeitos dos fármacos
Fatores de Transcrição/antagonistas & inibidores
Fatores de Transcrição/metabolismo
Triazóis/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 ((+)-JQ1 compound); 0 (2-morpholin-4-yl-6-thianthren-1-yl-pyran-4-one); 0 (Acetanilides); 0 (Azepines); 0 (BRD4 protein, human); 0 (Brd4 protein, mouse); 0 (GSK1210151A); 0 (Heterocyclic Compounds, 3-Ring); 0 (Heterocyclic Compounds, 4 or More Rings); 0 (Morpholines); 0 (Nuclear Proteins); 0 (OTX015); 0 (Pyrones); 0 (Transcription Factors); 0 (Triazoles); EC 2.7.7.49 (Telomerase)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170901
[St] Status:MEDLINE
[do] DOI:10.1093/nar/gkx561


  7 / 3656 MEDLINE  
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[PMID]:28834433
[Au] Autor:Wang J; Mu FR; Jiao WH; Huang J; Hong LL; Yang F; Xu Y; Wang SP; Sun F; Lin HW
[Ad] Endereço:School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University , Shenyang 110016, People's Republic of China.
[Ti] Título:Meroterpenoids with Protein Tyrosine Phosphatase 1B Inhibitory Activity from a Hyrtios sp. Marine Sponge.
[So] Source:J Nat Prod;80(9):2509-2514, 2017 Sep 22.
[Is] ISSN:1520-6025
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Three new meroterpenoids, hyrtiolacton A (1), nakijinol F (2), and nakijinol G (3), along with three known ones, nakijinol B (4), nakijinol E (5), and dactyloquinone A (6), were isolated and characterized from a Hyrtios sp. marine sponge collected from the South China Sea. The new structures were determined based on extensive analysis of HRESIMS and NMR data, and their absolute configurations were assigned by a combination of single-crystal X-ray diffraction and electronic circular dichroism analyses. Hyrtiolacton A (1) represents an unprecedented meroterpenoid featuring an unusual 2-pyrone attached to the sesquiterpene core, which is the first example of a pyrone-containing 4,9-friedodrimane-type sesquiterpene. These compounds were evaluated for their protein tyrosine phosphatase (PTP1B) inhibitory and cytotoxic activities. Nakijinol G (3) showed PTP1B inhibitory activity with an IC value of 4.8 µM but no cytotoxicity against four human cancer cell lines.
[Mh] Termos MeSH primário: Benzoxazóis/isolamento & purificação
Benzoxazóis/farmacologia
Dysidea/química
Poríferos/química
Proteína Tirosina Fosfatase não Receptora Tipo 1/antagonistas & inibidores
Pironas/química
Sesquiterpenos/isolamento & purificação
Sesquiterpenos/farmacologia
[Mh] Termos MeSH secundário: Animais
Benzoxazóis/química
Linhagem Celular Tumoral
China
Seres Humanos
Estrutura Molecular
Proteína Tirosina Fosfatase não Receptora Tipo 1/química
Proteína Tirosina Fosfatase não Receptora Tipo 1/metabolismo
Sesquiterpenos/química
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2-pyrone); 0 (Benzoxazoles); 0 (Pyrones); 0 (Sesquiterpenes); 0 (hyrtiolacton A); 0 (nakijinol B); 0 (nakijinol F); 0 (nakijinol G); EC 3.1.3.48 (PTPN1 protein, human); EC 3.1.3.48 (Protein Tyrosine Phosphatase, Non-Receptor Type 1)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170824
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jnatprod.7b00435


  8 / 3656 MEDLINE  
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[PMID]:28806079
[Au] Autor:Puppala M; Narayanapillai SC; Leitzman P; Sun H; Upadhyaya P; O'Sullivan MG; Hecht SS; Xing C
[Ad] Endereço:Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota , Minneapolis, Minnesota 55455, United States.
[Ti] Título:Pilot in Vivo Structure-Activity Relationship of Dihydromethysticin in Blocking 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone-Induced O -Methylguanine and Lung Tumor in A/J Mice.
[So] Source:J Med Chem;60(18):7935-7940, 2017 Sep 28.
[Is] ISSN:1520-4804
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:(+)-Dihydromethysticin was recently identified as a promising lung cancer chemopreventive agent, while (+)-dihydrokavain was completely ineffective. A pilot in vivo structure-activity relationship (SAR) was explored, evaluating the efficacy of its analogs in blocking 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone-induced short-term O -methylguanine and long-term adenoma formation in the lung tissues in A/J mice. Both results revealed cohesive SARs, demonstrating that the methylenedioxy functional group in DHM is essential while the lactone functional group tolerates modifications.
[Mh] Termos MeSH primário: Adenoma/prevenção & controle
Anticarcinógenos/uso terapêutico
Guanina/análogos & derivados
Neoplasias Pulmonares/prevenção & controle
Pulmão/efeitos dos fármacos
Pironas/uso terapêutico
[Mh] Termos MeSH secundário: Adenoma/metabolismo
Adenoma/patologia
Animais
Anticarcinógenos/química
Carcinógenos
Feminino
Guanina/antagonistas & inibidores
Guanina/metabolismo
Pulmão/metabolismo
Pulmão/patologia
Neoplasias Pulmonares/induzido quimicamente
Neoplasias Pulmonares/metabolismo
Neoplasias Pulmonares/patologia
Camundongos
Nitrosaminas
Pironas/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (7,8-dihydromethysticin); 0 (Anticarcinogenic Agents); 0 (Carcinogens); 0 (Nitrosamines); 0 (Pyrones); 5Z93L87A1R (Guanine); 7S395EDO61 (4-(N-methyl-N-nitrosamino)-1-(3-pyridyl)-1-butanone); 9B710FV2AE (O-(6)-methylguanine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171123
[Lr] Data última revisão:
171123
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170815
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jmedchem.7b00921


  9 / 3656 MEDLINE  
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[PMID]:28803995
[Au] Autor:Saetang P; Rukachaisirikul V; Phongpaichit S; Preedanon S; Sakayaroj J; Borwornpinyo S; Seemakhan S; Muanprasat C
[Ad] Endereço:Department of Chemistry and Center of Excellence for Innovation in Chemistry, Faculty of Science, Prince of Songkla University, Hat Yai, Songkhla 90112, Thailand.
[Ti] Título:Depsidones and an α-pyrone derivative from Simpilcillium sp. PSU-H41, an endophytic fungus from Hevea brasiliensis leaf.
[So] Source:Phytochemistry;143:115-123, 2017 Nov.
[Is] ISSN:1873-3700
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Nine previously undescribed depsidones (simplicildones A-I) and one previously undescribed α-pyrone (simplicilopyrone) were isolated from the endophytic fungus Simplicillium sp. PSU-H41 along with 11 known compounds. Their structures were established by extensive spectroscopic analysis. Simplicildone A and known botryorhodine C displayed weak antibacterial against Staphylococcus aureus with equal MIC values of 32 µg/mL. Additionally, botryorhodine C was active against methicillin-resistant S. aureus with the same MIC value. Simplicildone C exhibited weak antifungal activity against Cryptococcus neoformans with an MIC value of 32 µg/mL. In addition, simplicildones A and C and botryorhodine C were noncytotoxic against noncancerous Vero cells.
[Mh] Termos MeSH primário: Antibacterianos/isolamento & purificação
Antifúngicos/isolamento & purificação
Depsídeos/isolamento & purificação
Euphorbiaceae/química
Hevea/química
Lactonas/isolamento & purificação
Pironas/isolamento & purificação
[Mh] Termos MeSH secundário: Animais
Antibacterianos/química
Antibacterianos/farmacologia
Antifúngicos/química
Antifúngicos/farmacologia
Cercopithecus aethiops
Cryptococcus neoformans/efeitos dos fármacos
Depsídeos/química
Depsídeos/farmacologia
Lactonas/química
Lactonas/farmacologia
Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos
Testes de Sensibilidade Microbiana
Estrutura Molecular
Folhas de Planta/química
Pironas/química
Pironas/farmacologia
Staphylococcus aureus/efeitos dos fármacos
Células Vero
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Antifungal Agents); 0 (Depsides); 0 (Lactones); 0 (Pyrones); 3580-77-6 (depsidone)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171002
[Lr] Data última revisão:
171002
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170815
[St] Status:MEDLINE


  10 / 3656 MEDLINE  
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[PMID]:28797798
[Au] Autor:Tian LW; Feng Y; Tran TD; Shimizu Y; Pfeifer T; Vu HT; Quinn RJ
[Ad] Endereço:Griffith Institute for Drug Discovery, Griffith University, Brisbane QLD 4111, Australia.
[Ti] Título:Achyrodimer F, a tyrosyl-DNA phosphodiesterase I inhibitor from an Australian fungus of the family Cortinariaceae.
[So] Source:Bioorg Med Chem Lett;27(17):4007-4010, 2017 09 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Mass-guided isolation of the dichloromethane/methanol extracts from a specimen of teleomorphic fungus of the family Cortinariaceae resulted in the identification of a new dimeric cyclobutane metabolite, achyrodimer F (1), along with the monomers hispidin (2) and bisnoryangonin (3). Their structures were determined by NMR and MS data analyses. Density Function Theory (DFT) NMR calculations was employed to confirm the chemical structure of achyrodimer F. Compound 1 inhibited tyrosyl-DNA phosphodiesterase I with an IC value of 1µM.
[Mh] Termos MeSH primário: Agaricales/química
Ciclobutanos/farmacologia
Inibidores de Fosfodiesterase/farmacologia
Diester Fosfórico Hidrolases/metabolismo
Pironas/farmacologia
[Mh] Termos MeSH secundário: Austrália
Ciclobutanos/química
Ciclobutanos/isolamento & purificação
Relação Dose-Resposta a Droga
Seres Humanos
Estrutura Molecular
Inibidores de Fosfodiesterase/química
Inibidores de Fosfodiesterase/isolamento & purificação
Pironas/química
Pironas/isolamento & purificação
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Cyclobutanes); 0 (Phosphodiesterase Inhibitors); 0 (Pyrones); 0 (achyrodimer F); EC 3.1.4.- (Phosphoric Diester Hydrolases); EC 3.1.4.- (TDP1 protein, human)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170812
[St] Status:MEDLINE



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