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Pesquisa : D12.644.456.270 [Categoria DeCS]
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[PMID]:26162028
[Au] Autor:Kim DW; Woo HS; Kim JY; Ryuk JA; Park KH; Ko BS
[Ad] Endereço:a Korea Institute of Oriental Medicine, KM Convergence Research Division , Daejeon , Republic of Korea and.
[Ti] Título:Phenols displaying tyrosinase inhibition from Humulus lupulus.
[So] Source:J Enzyme Inhib Med Chem;31(5):742-7, 2016 Oct.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Tyrosinase is the rate-limiting enzyme for the production of melanin and other pigments via the oxidation of l-tyrosine. The methanol extract from Humulus lupulus showed potent inhibition against mushroom tyrosinase. The bioactivity-guided fractionation of this methanol extract resulted in the isolation of seven flavonoids (1-7), identified as xanthohumol (1), 4'-O-methylxanthohumol (2), xanthohumol C (3), flavokawain C (4), xanthoumol B (5), 6-prenylnaringenin (6) and isoxanthohumol (7). All isolated flavonoids (1-7) effectively inhibited the monophenolase (IC50s = 15.4-58.4 µM) and diphenolase (IC50s = 27.1-117.4 µM) activities of tyrosinase. Kinetic studies using Lineweaver-Burk and Dixon-plots revealed that chalcones (1-5) were competitive inhibitors, whereas flavanones (6 and 7) exhibited both mixed and non-competitive inhibitory characteristics. In conclusion, this study is the first to demonstrate that the phenolic phytochemicals of H. lupulus display potent inhibitory activities against tyrosinase.
[Mh] Termos MeSH primário: Humulus/química
Monofenol Mono-Oxigenase/antagonistas & inibidores
Fenóis/farmacologia
[Mh] Termos MeSH secundário: Bioensaio
Calônios/química
Calônios/isolamento & purificação
Calônios/farmacologia
Ativação Enzimática/efeitos dos fármacos
Inibidores Enzimáticos/química
Inibidores Enzimáticos/isolamento & purificação
Inibidores Enzimáticos/farmacologia
Flavonoides/química
Flavonoides/isolamento & purificação
Flavonoides/farmacologia
Concentração Inibidora 50
Metanol/química
Estrutura Molecular
Monofenol Mono-Oxigenase/química
Monofenol Mono-Oxigenase/metabolismo
Fenóis/química
Fenóis/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Chalones); 0 (Enzyme Inhibitors); 0 (Flavonoids); 0 (Phenols); EC 1.14.18.1 (Monophenol Monooxygenase); Y4S76JWI15 (Methanol)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170324
[Lr] Data última revisão:
170324
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150711
[St] Status:MEDLINE
[do] DOI:10.3109/14756366.2015.1063621


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[PMID]:27028114
[Au] Autor:Keppel Hesselink JM
[Ad] Endereço:Research and development, Institute Neuropathic Pain, Spoorlaan 2a, Bosch en Duin, 3735 MV, Netherlands.
[Ti] Título:The terms 'autacoid', 'hormone' and 'chalone' and how they have shifted with time.
[So] Source:Auton Autacoid Pharmacol;35(4):51-8, 2015 Dec.
[Is] ISSN:1474-8673
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The increase of knowledge in a particular field (endocrinology) can be understood if one follows how certain key concepts were constructed and transformed over time. To explore such construction and transformation (shifts in meaning), we studied the use of the concepts 'autacoid' and 'chalone' in a period of one century (1916-2016), since the introduction of these concepts by the British professor of physiology Sir Sharpey-Schäfer. We could identify that the use of 'autacoid' shifted from a very broad category encompassing both stimulating and inhibiting hormones, in the period 1916-1960, to a much more specific use of the term for locally produced bioactive molecules, from the 1960s onwards. Histamine was the first compound seen as an 'autacoid', followed by prostaglandins, ATP, ADP and bradykinin, and from 1993 onwards, compounds such as 'palmitoylethanolamide' were also classified as 'autacoids'. For 'chalone', a comparable shift was noticed around the 1960s, when the concept suddenly changed from the category of inhibiting hormones into a substance that is produced within a tissue, inhibiting mitosis of the cells of that tissue. For both concept shifts, we could not find any argument. Around 1980, authors started to relate autacoids to various promising indications in the field of inflammation and immune modulation. The Nobel laureate Rita Levi-Montalcini gave an extra dimension to the concept autacoid in 1993, and introduced a new class of compounds modulating mast cells, the ALIAmides (from Autacoid Local Inflammation Antagonist), of which palmitoylethanolamide was the prototype. Our exploration demonstrates that biomedical concepts can be constructed and defined differently as time goes by, while concept transformations seem to emerge without arguments.
[Mh] Termos MeSH primário: Autacoides/metabolismo
Calônios/metabolismo
Hormônios/metabolismo
[Mh] Termos MeSH secundário: Bradicinina/metabolismo
Endocanabinoides/metabolismo
Histamina/metabolismo
Seres Humanos
Inflamação/metabolismo
Mastócitos/metabolismo
Prostaglandinas/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Autacoids); 0 (Chalones); 0 (Endocannabinoids); 0 (Hormones); 0 (Prostaglandins); 820484N8I3 (Histamine); S8TIM42R2W (Bradykinin)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170117
[Lr] Data última revisão:
170117
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160331
[St] Status:MEDLINE
[do] DOI:10.1111/aap.12037


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[PMID]:24397993
[Au] Autor:Yu L; Zhang F; Hu Z; Ding H; Tang H; Ma Z; Zhao X
[Ad] Endereço:Institute of Marine Biology & Natural Products, Ocean College, Zhejiang University, No. 866 Yuhangtang Rd., Hangzhou 310058, China.
[Ti] Título:Novel prenylated bichalcone and chalcone from Humulus lupulus and their quinone reductase induction activities.
[So] Source:Fitoterapia;93:115-20, 2014 Mar.
[Is] ISSN:1873-6971
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:A new prenylated chalcone xanthohumol M (1), a novel prenylated bichalcone humulusol (2) and six known chalcones (3-8) were found from Humulus lupulus. Their structures were determined by spectroscopic methods. All the chalcones' electrophilic abilities were assessed by GSH (glutathione) rapid screening, and their QR (quinone reductase) induction activities were evaluated using hepa 1c1c7 cells. The results of electrophilic assay and QR induction activity assay were quite well. New compounds 1 and 2, along with some known prenylated chalcones, displayed certain QR induction activity.
[Mh] Termos MeSH primário: Chalconas/isolamento & purificação
Calônios/isolamento & purificação
Humulus/química
NAD(P)H Desidrogenase (Quinona)/biossíntese
[Mh] Termos MeSH secundário: Animais
Linhagem Celular Tumoral
Chalconas/química
Calônios/química
Indução Enzimática
Camundongos
Estrutura Molecular
Prenilação
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Chalcones); 0 (Chalones); 0 (humulusol); 0 (xanthohumol M); EC 1.6.5.2 (NAD(P)H Dehydrogenase (Quinone))
[Em] Mês de entrada:1502
[Cu] Atualização por classe:140224
[Lr] Data última revisão:
140224
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140109
[St] Status:MEDLINE


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[PMID]:24390142
[Au] Autor:Bakthavatsalam D; White MJ; Herlihy SE; Phillips JE; Gomer RH
[Ad] Endereço:Department of Biology, Texas A&M University, College Station, Texas, USA.
[Ti] Título:A retinoblastoma orthologue is required for the sensing of a chalone in Dictyostelium discoideum.
[So] Source:Eukaryot Cell;13(3):376-82, 2014 Mar.
[Is] ISSN:1535-9786
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Retinoblastoma-like proteins regulate cell differentiation and inhibit cell proliferation. The Dictyostelium discoideum retinoblastoma orthologue RblA affects the differentiation of cells during multicellular development, but it is unclear whether RblA has a significant effect on Dictyostelium cell proliferation, which is inhibited by the secreted proteins AprA and CfaD. We found that rblA⁻ cells in shaking culture proliferate to a higher density, die faster after reaching stationary density, and, after starvation, have a lower spore viability than wild-type cells, possibly because in shaking culture, rblA⁻ cells have both increased cytokinesis and lower extracellular accumulation of CfaD. However, rblA⁻ cells have abnormally slow proliferation on bacterial lawns. Recombinant AprA inhibits the proliferation of wild-type cells but not that of rblA⁻ cells, whereas CfaD inhibits the proliferation of both wild-type cells and rblA⁻ cells. Similar to aprA⁻ cells, rblA⁻ cells have a normal mass and protein accumulation rate on a per-nucleus basis, indicating that RblA affects cell proliferation but not cell growth. AprA also functions as a chemorepellent, and RblA is required for proper AprA chemorepellent activity despite the fact that RblA does not affect cell speed. Together, our data indicate that an autocrine proliferation-inhibiting factor acts through RblA to regulate cell density in Dictyostelium, suggesting that such factors may signal through retinoblastoma-like proteins to control the sizes of structures such as developing organs or tumors.
[Mh] Termos MeSH primário: Proliferação Celular
Calônios/farmacologia
Dictyostelium/metabolismo
Proteínas de Protozoários/metabolismo
Proteína p107 Retinoblastoma-Like/metabolismo
[Mh] Termos MeSH secundário: Ciclo Celular
Dictyostelium/efeitos dos fármacos
Dictyostelium/genética
Proteínas de Protozoários/genética
Proteína p107 Retinoblastoma-Like/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL
[Nm] Nome de substância:
0 (Chalones); 0 (Protozoan Proteins); 0 (Retinoblastoma-Like Protein p107)
[Em] Mês de entrada:1411
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140107
[St] Status:MEDLINE
[do] DOI:10.1128/EC.00306-13


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[PMID]:23425970
[Au] Autor:Cao D; Han X; Wang G; Yang Z; Peng F; Ma L; Zhang R; Ye H; Tang M; Wu W; Lei K; Wen J; Chen J; Qiu J; Liang X; Ran Y; Sang Y; Xiang M; Peng A; Chen L
[Ad] Endereço:State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Keyuan Road 4, Gaopeng Street, Chengdu 610041, China.
[Ti] Título:Synthesis and biological evaluation of novel pyranochalcone derivatives as a new class of microtubule stabilizing agents.
[So] Source:Eur J Med Chem;62:579-89, 2013 Apr.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Twenty-five novel pyranochalcone derivatives were synthesized and evaluated for their in vitro and in vivo antiproliferative activities. Among them, compound 10i exhibited superior potent activity against 21 tumor cell lines including multidrug resistant phenotype with the IC50 values ranged from 0.09 to 1.30 µM. In addition, 10i significantly induced cell cycle arrest in G2/M phase, promoted tubulin polymerization into microtubules and caused microtubule stabilization. Further studies confirmed that 10i significantly suppressed the growth of tumor volume in HepG2 xenograft tumor model. Our study demonstrated that 10i could have beneficial antitumor activity as a novel microtubule stabilizing agent.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Benzopiranos/farmacologia
Calônios/farmacologia
Microtúbulos/efeitos dos fármacos
Neoplasias/tratamento farmacológico
Moduladores de Tubulina/farmacologia
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/síntese química
Antineoplásicos/química
Benzopiranos/síntese química
Benzopiranos/química
Linhagem Celular
Proliferação Celular/efeitos dos fármacos
Calônios/síntese química
Calônios/química
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Feminino
Células Hep G2
Seres Humanos
Camundongos
Camundongos Endogâmicos BALB C
Camundongos Nus
Estrutura Molecular
Neoplasias/patologia
Relação Estrutura-Atividade
Moduladores de Tubulina/síntese química
Moduladores de Tubulina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (2-methoxy-5-(3-(5-methoxy-2,2-dimethyl-2H-chromen-8-yl)-3-oxoprop-1-en-1-yl)phenyl propionate); 0 (Antineoplastic Agents); 0 (Benzopyrans); 0 (Chalones); 0 (Tubulin Modulators)
[Em] Mês de entrada:1310
[Cu] Atualização por classe:130409
[Lr] Data última revisão:
130409
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130222
[St] Status:MEDLINE


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[PMID]:22784822
[Au] Autor:Wang G; Wu W; Peng F; Cao D; Yang Z; Ma L; Qiu N; Ye H; Han X; Chen J; Qiu J; Sang Y; Liang X; Ran Y; Peng A; Wei Y; Chen L
[Ad] Endereço:State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Keyuan Road 4, Gaopeng Street, Chengdu 610041, China.
[Ti] Título:Design, synthesis, and structure-activity relationship studies of novel millepachine derivatives as potent antiproliferative agents.
[So] Source:Eur J Med Chem;54:793-803, 2012 Aug.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:In this paper, 38 millepachine derivatives have been designed, synthesized and evaluated for their in vitro and in vivo antiproliferative activity. Among these novel derivatives, 15 displayed more potent antiproliferative activity than millepachine against HepG2, K562, SK-OV-3, HCT116, HT29, and SW620 tumor cells (mean IC(50) = 0.64 vs. 2.86 µM, respectively). Furthermore, 15 could effectively inhibit tubulin polymerization in HepG2 cells, and induce the HepG2 cell cycle arrest at the G2/M phase in a concentration-dependant manner. Further studies confirmed that 15 significantly suppressed the growth of tumor volume and exerted more potent anticancer potency than millepachine and anticancer drug cisplatin in A549 lung xenograft tumor model.
[Mh] Termos MeSH primário: Antineoplásicos/síntese química
Antineoplásicos/farmacologia
Benzopiranos/síntese química
Benzopiranos/farmacologia
Produtos Biológicos/síntese química
Produtos Biológicos/farmacologia
Calônios/síntese química
Calônios/farmacologia
Desenho de Drogas
[Mh] Termos MeSH secundário: Antineoplásicos/química
Benzopiranos/química
Produtos Biológicos/química
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Calônios/química
Técnicas de Química Sintética
Seres Humanos
Concentração Inibidora 50
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Benzopyrans); 0 (Biological Products); 0 (Chalones)
[Em] Mês de entrada:1212
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120713
[St] Status:MEDLINE
[do] DOI:10.1016/j.ejmech.2012.06.034


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[PMID]:21278229
[Au] Autor:Bowman RL; Xiong Y; Kirsten JH; Singleton CK
[Ad] Endereço:Department of Biological Sciences, Vanderbilt University, Nashville, TN 37235-1634, USA.
[Ti] Título:eIF2α kinases control chalone production in Dictyostelium discoideum.
[So] Source:Eukaryot Cell;10(4):494-501, 2011 Apr.
[Is] ISSN:1535-9786
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Growing Dictyostelium cells secrete CfaD and AprA, two proteins that have been characterized as chalones. They exist within a high-molecular-weight complex that reversibly inhibits cell proliferation, but not growth, via cell surface receptors and a signaling pathway that includes G proteins. How the production of these two proteins is regulated is unknown. Dictyostelium cells possess three GCN2-type eukaryotic initiation factor 2 α subunit (eIF2α) kinases, proteins that phosphorylate the translational initiation factor eIF2α and possess a tRNA binding domain involved in their regulation. The Dictyostelium kinases have been shown to function during development in regulating several processes. We show here that expression of an unregulated, activated kinase domain greatly inhibits cell proliferation. The inhibitory effect on proliferation is not due to a general inhibition of translation. Instead, it is due to enhanced production of a secreted factor(s). Indeed, extracellular CfaD and AprA proteins, but not their mRNAs, are overproduced in cells expressing the activated kinase domain. The inhibition of proliferation is not seen when the activated kinase domain is expressed in cells lacking CfaD or AprA or in cells that contain a nonphosphorylatable eIF2α. We conclude that production of the chalones CfaD and AprA is translationally regulated by eIF2α phosphorylation. Both proteins are upregulated at the culmination of development, and this enhanced production is lacking in a strain that possesses a nonphosphorylatable eIF2α.
[Mh] Termos MeSH primário: Calônios/biossíntese
Dictyostelium/metabolismo
Fator de Iniciação 2 em Eucariotos/metabolismo
Proteínas de Protozoários/metabolismo
[Mh] Termos MeSH secundário: Animais
Linhagem Celular
Proliferação Celular
Meios de Cultivo Condicionados/metabolismo
Dictyostelium/genética
Dictyostelium/fisiologia
Fator de Iniciação 2 em Eucariotos/genética
Proteínas de Protozoários/genética
Transdução de Sinais/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 (Chalones); 0 (Culture Media, Conditioned); 0 (Eukaryotic Initiation Factor-2); 0 (Protozoan Proteins)
[Em] Mês de entrada:1107
[Cu] Atualização por classe:150205
[Lr] Data última revisão:
150205
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:110201
[St] Status:MEDLINE
[do] DOI:10.1128/EC.00270-10


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[PMID]:19635129
[Au] Autor:Bakthavatsalam D; Choe JM; Hanson NE; Gomer RH
[Ad] Endereço:Department of Biochemistry and Cell Biology, MS-140, Rice University, Houston, TX, USA. db3@rice.edu
[Ti] Título:A Dictyostelium chalone uses G proteins to regulate proliferation.
[So] Source:BMC Biol;7:44, 2009 Jul 27.
[Is] ISSN:1741-7007
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Several studies have shown that organ size, and the proliferation of tumor metastases, may be regulated by negative feedback loops in which autocrine secreted factors called chalones inhibit proliferation. However, very little is known about chalones, and how cells sense them. We previously identified two secreted proteins, AprA and CfaD, which act as chalones in Dictyostelium. Cells lacking AprA or CfaD proliferate faster than wild-type cells, and adding recombinant AprA or CfaD to cells slows their proliferation. RESULTS: We show here that cells lacking the G protein components Galpha8, Galpha9, and Gbeta proliferate faster than wild-type cells despite secreting normal or high levels of AprA and CfaD. Compared with wild-type cells, the proliferation of galpha8-, galpha9- and gbeta- cells are only weakly inhibited by recombinant AprA (rAprA). Like AprA and CfaD, Galpha8 and Gbeta inhibit cell proliferation but not cell growth (the rate of increase in mass and protein per nucleus), whereas Galpha9 inhibits both proliferation and growth. galpha8- cells show normal cell-surface binding of rAprA, whereas galpha9- and gbeta- cells have fewer cell-surface rAprA binding sites, suggesting that Galpha9 and Gbeta regulate the synthesis or processing of the AprA receptor. Like other ligands that activate G proteins, rAprA induces the binding of [3H]GTP to membranes, and GTPgammaS inhibits the binding of rAprA to membranes. Both AprA-induced [3H]GTP binding and the GTPgammaS inhibition of rAprA binding require Galpha8 and Gbeta but not Galpha9. Like aprA- cells, galpha8- cells have reduced spore viability. CONCLUSION: This study shows that Galpha8 and Gbeta are part of the signal transduction pathway used by AprA to inhibit proliferation but not growth in Dictyostelium, whereas Galpha9 is part of a differealnt pathway that regulates both proliferation and growth, and that a chalone signal transduction pathway uses G proteins.
[Mh] Termos MeSH primário: Proliferação Celular
Calônios/fisiologia
Dictyostelium/fisiologia
Proteínas de Ligação ao GTP/fisiologia
Proteínas de Protozoários/fisiologia
[Mh] Termos MeSH secundário: Animais
Crescimento Celular
Membrana Celular/metabolismo
Calônios/análise
Calônios/deficiência
Calônios/metabolismo
Contagem de Colônia Microbiana
Dictyostelium/citologia
Proteínas de Fímbrias/análise
Proteínas de Fímbrias/deficiência
Proteínas de Fímbrias/fisiologia
Subunidades alfa de Proteínas de Ligação ao GTP/deficiência
Subunidades alfa de Proteínas de Ligação ao GTP/fisiologia
Subunidades beta da Proteína de Ligação ao GTP/deficiência
Subunidades beta da Proteína de Ligação ao GTP/fisiologia
Guanosina 5'-O-(3-Tiotrifosfato)/metabolismo
Guanosina Trifosfato/metabolismo
Proteínas Recombinantes/metabolismo
Transdução de Sinais
Esporos de Protozoários
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL
[Nm] Nome de substância:
0 (Chalones); 0 (GTP-Binding Protein alpha Subunits); 0 (GTP-Binding Protein beta Subunits); 0 (Protozoan Proteins); 0 (Recombinant Proteins); 0 (colonization factor antigens); 147680-16-8 (Fimbriae Proteins); 37589-80-3 (Guanosine 5'-O-(3-Thiotriphosphate)); 86-01-1 (Guanosine Triphosphate); EC 3.6.1.- (GTP-Binding Proteins)
[Em] Mês de entrada:0909
[Cu] Atualização por classe:161025
[Lr] Data última revisão:
161025
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090729
[St] Status:MEDLINE
[do] DOI:10.1186/1741-7007-7-44


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[PMID]:19453073
[Au] Autor:Huan Y; He Y; Liu M; Jin X; Li X; Liu X; Zhang Q
[Ad] Endereço:Abdominal Surgery, The Tumor Hospital of Harbin Medical University, Harbin 150081, China. jinxm55@163.com
[Ti] Título:A comparative study of tumor-suppression effects of enterotoxin B and Chalone 19-peptide on experimental gastric carcinoma.
[So] Source:Hepatogastroenterology;56(89):270-5, 2009 Jan-Feb.
[Is] ISSN:0172-6390
[Cp] País de publicação:Greece
[La] Idioma:eng
[Ab] Resumo:BACKGROUND/AIMS: In this paper, the in vivo tumor suppression effects of Staphyococal enterotoxin B (SEB) and Chalone 19-peptide, a form of Tumstain with modified coding sequence, on poorly differentiated human gastric carcinoma cells were compared. METHODOLOGY: Animal model for studying human gastric carcinoma was established by injecting tumor cells (Human poorly differentiated gastric carcinoma cell line, SGC-7901) underneath the gastric serosa of BALB/c nude mice. RESULTS: Results demonstrated that SEB induced tumor cell death on a large scale and destroyed surrounding normal tissue at the same time, leading to tumor cluster breaking down and seeding. SEB had no effect on lymphovascular metastasis. The administration of 19-peptide on gastric carcinoma resulted in sheets-like tumor central necrosis, decreased angiogenesis and a moderate tumor infiltration into surrounding tissue without distant metastasis. Therefore, both SEB and 19-peptide could suppress the local growth, distant metastasis and invasion of poorly differentiated gastric carcinoma cells into surrounding tissues. CONCLUSIONS: Data suggested that this model could effectively simulate the microenvironment of human gastric carcinoma, hence providing a platform for study on this cancer.
[Mh] Termos MeSH primário: Calônios/farmacologia
Enterotoxinas/farmacologia
Neoplasias Gástricas/tratamento farmacológico
Neoplasias Gástricas/patologia
[Mh] Termos MeSH secundário: Animais
Linhagem Celular Tumoral
Seres Humanos
Camundongos
Camundongos Endogâmicos BALB C
Camundongos Nus
Invasividade Neoplásica
Transplante de Neoplasias
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Chalones); 0 (Enterotoxins)
[Em] Mês de entrada:0906
[Cu] Atualização por classe:090520
[Lr] Data última revisão:
090520
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090521
[St] Status:MEDLINE


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[PMID]:19178775
[Au] Autor:dos Santos DA; de C Braga PA; da Silva MF; Fernandes JB; Vieira PC; Magalhães AF; Magalhães EG; Marsaioli AJ; de S Moraes VR; Rattray L; Croft SL
[Ad] Endereço:Departamento de Química, Universidade Federal de São Carlos, São Carlos, Brazil.
[Ti] Título:Anti-African trypanocidal and antimalarial activity of natural flavonoids, dibenzoylmethanes and synthetic analogues.
[So] Source:J Pharm Pharmacol;61(2):257-66, 2009 Feb.
[Is] ISSN:0022-3573
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVES: The known anti-protozoal activity of flavonoids has stimulated the testing of other derivatives from natural and synthetic sources. METHODS: As part of our efforts to find potential lead compounds, a number of flavonoids isolated from Neoraputia paraensis, N. magnifica, Murraya paniculata, (Rutaceae), Lonchocarpus montanus, L. latifolius, L. subglaucescens, L. atropurpureus, L. campestris, Deguelia hatschbachii (Leguminosae), dibenzoylmethanes from L. subglaucescens and synthetic analogues were tested for in-vitro activity against chloroquine-sensitive Plasmodium falciparum and Trypanosoma brucei rhodesiense bloodstream form trypomastigotes. An assay with KB cells has been developed in order to compare in-vitro cytotoxicity of flavonoids with a selective action on the parasites. KEY FINDINGS: Thirteen of the compounds tested had IC50 values ranging from 4.6 to 9.9 microm against T. brucei rhodesiense. In contrast, a small number of compounds showed significant activity against P. falciparum; seven of those tested had IC50 values ranging from 2.7 to 9.5 microm. Among the flavones only one had IC50 < 10 microm (7.6 microm), whereas against T. brucei rhodesiense seven had IC50 < 10 microm. Synthetic dibenzoylmethanes were the most active in terms of number (five) of compounds and the IC50 values (2.7-9.5 microm) against P. falciparum. CONCLUSIONS: Dibenzoylmethanes represent a novel class of compounds tested for the first time as antimalarial and trypanocidal agents.
[Mh] Termos MeSH primário: Antimaláricos/uso terapêutico
Descoberta de Drogas
Flavonoides/química
Tripanossomicidas/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Antimaláricos/química
Antimaláricos/isolamento & purificação
Antimaláricos/toxicidade
Chalconas/química
Chalconas/uso terapêutico
Chalconas/toxicidade
Calônios/química
Calônios/uso terapêutico
Calônios/toxicidade
Química Farmacêutica/métodos
Química Farmacêutica/tendências
Fabaceae/química
Flavonoides/isolamento & purificação
Flavonoides/uso terapêutico
Seres Humanos
Concentração Inibidora 50
Células KB
Estrutura Molecular
Plasmodium falciparum/efeitos dos fármacos
Rutaceae/química
Tripanossomicidas/química
Tripanossomicidas/isolamento & purificação
Tripanossomicidas/toxicidade
Trypanosoma brucei rhodesiense/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 (Antimalarials); 0 (Chalcones); 0 (Chalones); 0 (Flavonoids); 0 (Trypanocidal Agents)
[Em] Mês de entrada:0904
[Cu] Atualização por classe:090130
[Lr] Data última revisão:
090130
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090131
[St] Status:MEDLINE
[do] DOI:10.1211/jpp/61.02.0017



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