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[PMID]:28460464
[Au] Autor:Nazim UM; Moon JH; Lee YJ; Seol JW; Park SY
[Ad] Endereço:Biosafety Research Institute, College of Veterinary Medicine, Chonbuk National University, Iksan, Jeonbuk 54596, South Korea.
[Ti] Título:PPARγ activation by troglitazone enhances human lung cancer cells to TRAIL-induced apoptosis via autophagy flux.
[So] Source:Oncotarget;8(16):26819-26831, 2017 Apr 18.
[Is] ISSN:1949-2553
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Members of the tumor necrosis factor (TNF) transmembrane cytokine superfamily, such as TNFα and Fas ligand (FasL), play crucial roles in inflammation and immunity. TRAIL is a member of this superfamily with the ability to selectively trigger cancer cell death but does not motive cytotoxicity to most normal cells. Troglitazone are used in the cure of type II diabetes to reduce blood glucose levels and improve the sensitivity of an amount of tissues to insulin. In this study, we revealed that troglitazone could trigger TRAIL-mediated apoptotic cell death in human lung adenocarcinoma cells. Pretreatment of troglitazone induced activation of PPARγ in a dose-dependent manner. In addition conversion of LC3-I to LC3-II and PPARγ was suppressed in the presence of GW9662, a well-characterized PPARγ antagonist. Treatment with troglitazone resulted in a slight increase in conversion rate of LC3-I to LC3-II and significantly decreased p62 expression levels in a dose-dependent manner. This indicates that troglitazone induced autophagy flux activation in human lung cancer cells. Inhibition of autophagy flux applying a specific inhibitor and genetically modified ATG5 siRNA enclosed troglitazone-mediated enhancing effect of TRAIL. These data demonstrated that activation of PPARγ mediated by troglitazone enhances human lung cancer cells to TRAIL-induced apoptosis via autophagy flux and also suggest that troglitazone may be a combination therapeutic target with TRAIL protein in TRAIL-resistant cancer cells.
[Mh] Termos MeSH primário: Apoptose/efeitos dos fármacos
Autofagia/efeitos dos fármacos
Cromanos/farmacologia
Neoplasias Pulmonares/metabolismo
PPAR gama/agonistas
PPAR gama/metabolismo
Ligante Indutor de Apoptose Relacionado a TNF/farmacologia
Tiazolidinedionas/farmacologia
[Mh] Termos MeSH secundário: Linhagem Celular Tumoral
Seres Humanos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Chromans); 0 (PPAR gamma); 0 (TNF-Related Apoptosis-Inducing Ligand); 0 (Thiazolidinediones); I66ZZ0ZN0E (troglitazone)
[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.15819


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[PMID]:29192699
[Au] Autor:Kim J; Kim I
[Ad] Endereço:College of Pharmacy and Yonsei Institute of Pharmaceutical Sciences, Yonsei University, 85 Songdogwahak-ro, Yeonsu-gu, Incheon, 21983, Republic of Korea. ikyonkim@yonsei.ac.kr.
[Ti] Título:Design and synthesis of a hybrid framework of indanone and chromane: total synthesis of a homoisoflavanoid, brazilane.
[So] Source:Org Biomol Chem;16(1):89-100, 2017 Dec 19.
[Is] ISSN:1477-0539
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A chemical backbone of tetracyclic homoisoflavanoid natural products such as brazilin inspired us to design a new chemical scaffold, 6a,11b-dihydroindeno[2,1-c]chromen-7(6H)-one, which is a hybrid structure of indanone and chromane. Pd-catalyzed Suzuki-Miyaura cross-coupling of 4-chloro-2H-chromene-3-carbaldehydes with (hetero)aryl boronic acids was employed as a means to introduce a wide variety of (hetero)aryl groups as the D ring and intramolecular Friedel-Crafts acylation was utilized to construct the C ring of this skeleton. Total synthesis of the natural product, brazilane, was also demonstrated via this new chemical framework.
[Mh] Termos MeSH primário: Produtos Biológicos/síntese química
Cromanos/química
Desenho de Drogas
Flavonoides/síntese química
Indanos/química
Isoflavonas/síntese química
[Mh] Termos MeSH secundário: Produtos Biológicos/química
Flavonoides/química
Isoflavonas/química
Estrutura Molecular
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biological Products); 0 (Chromans); 0 (Flavonoids); 0 (Indans); 0 (Isoflavones); 0 (brazilane); B926Y9U4QN (indacrinone)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180223
[Lr] Data última revisão:
180223
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171202
[St] Status:MEDLINE
[do] DOI:10.1039/c7ob02758c


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[PMID]:29198904
[Au] Autor:Fatima N; Reddy BVS; Gowravaram S; Yadav JS; Kadari S; Putta CS
[Ad] Endereço:Center for Semiochemicals Natural Products Chemistry Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India. Electronic address: dr.narjisiict@yahoo.com.
[Ti] Título:Synthesis and biological evaluation of 1-amino isochromans from 2-bromoethyl benzaldehyde and amines in acid medium.
[So] Source:Bioorg Med Chem Lett;28(2):196-201, 2018 01 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:We have developed a facile and efficient synthetic route to substituted isochromans for the first time by reacting 2-(2-bromoethyl)benzaldehyde with a variety of aryl, heteroaryl amines in AcOH. The reaction is catalyst/additive free and takes place at reflux conditions with short reaction time to furnish products in good to excellent yields. All the compounds have been characterized by spectral techniques such as IR, H NMR and Mass etc. Synthesized compounds were evaluated for antimicrobial activity against specific bacterial like 1) Staphylococcus strains aureus 2) Bacillus subtilis 3) Escherichia coli 4) Pseudomonas aeruginosa. Compounds 3e, 3n, 3 m, 3 l, 3 k, 3j and 3b showed most potent in vitro activity against bacterial strains.
[Mh] Termos MeSH primário: Ácido Acético/química
Aminas/química
Antibacterianos/farmacologia
Benzaldeídos/química
Cromanos/farmacologia
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Antibacterianos/química
Bacillus subtilis/efeitos dos fármacos
Benzaldeídos/síntese química
Cromanos/síntese química
Cromanos/química
Relação Dose-Resposta a Droga
Escherichia coli/efeitos dos fármacos
Testes de Sensibilidade Microbiana
Estrutura Molecular
Pseudomonas aeruginosa/efeitos dos fármacos
Staphylococcus aureus/efeitos dos fármacos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Amines); 0 (Anti-Bacterial Agents); 0 (Benzaldehydes); 0 (Chromans); Q40Q9N063P (Acetic Acid)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180216
[Lr] Data última revisão:
180216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171205
[St] Status:MEDLINE


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[PMID]:27776485
[Au] Autor:Okamoto A; Tanaka M; Sumi C; Oku K; Kusunoki M; Nishi K; Matsuo Y; Takenaga K; Shingu K; Hirota K
[Ad] Endereço:Department of Anesthesiology, Kansai Medical University, Hirakata, Japan.
[Ti] Título:The antioxidant N-acetyl cysteine suppresses lidocaine-induced intracellular reactive oxygen species production and cell death in neuronal SH-SY5Y cells.
[So] Source:BMC Anesthesiol;16(1):104, 2016 10 24.
[Is] ISSN:1471-2253
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The local anesthetic lidocaine can affect intra- and extra-cellular signaling pathways in both neuronal and non-neuronal cells, resulting in long-term modulation of biological functions, including cell growth and death. Indeed, lidocaine was shown to induce necrosis and apoptosis in vitro. While several studies have suggested that lidocaine-induced apoptosis is mitochondrial pathway-dependent, it remains unclear whether reactive oxygen species (ROS) are involved in this process and whether the observed cell death can be prevented by antioxidant treatment. METHODS: The effects of lidocaine and antioxidants on cell viability and death were evaluated using SH-SY5Y cells, HeLa cells, and HeLa cell derivatives. Cell viability was examined via MTS/PES ([3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt]/phenazine ethosulfate) assay. Meanwhile, cell apoptosis and necrosis were evaluated using a cell death detection assay with Annexin V-FITC and PI staining, as well as by assaying for caspase-3/7 and caspase-9 activity, and by measuring the release of lactate dehydrogenase, respectively. Mitochondrial transmembrane potential (ΔΨm) was assessed using the fluorescent probe tetramethylrhodamine ethyl ester. RESULTS: Lidocaine treatment resulted in suppression of the mitochondrial electron transport chain and subsequent attenuation of mitochondrial membrane potential, as well as enhanced ROS production, activation of caspase-3/7 and caspase-9, and induction of apoptosis and necrosis in SH-SY5Y cells in a dose- and time-dependent manner. Likewise, the anesthetics mepivacaine and bupivacaine also induced apoptosis in SH-SY5Y cells. Notably, the antioxidants N-acetyl cysteine (NAC) and Trolox successfully scavenged the mitochondria-derived ROS and suppressed local lidocaine-induced cell death. CONCLUSIONS: Our findings demonstrate that the local anesthetics lidocaine, mepivacaine, and bupivacaine inhibited the activity of mitochondria and induced apoptosis and necrosis in a dose-dependent manner. Furthermore, they demonstrate that treatment with the antioxidants NAC, Trolox, and GGA resulted in preservation of mitochondrial voltage and inhibition of apoptosis via suppression of caspase activation.
[Mh] Termos MeSH primário: Acetilcisteína/farmacologia
Antioxidantes/farmacologia
Lidocaína/farmacologia
Espécies Reativas de Oxigênio/metabolismo
[Mh] Termos MeSH secundário: Acetilcisteína/administração & dosagem
Anestésicos Locais/farmacologia
Antioxidantes/administração & dosagem
Apoptose/efeitos dos fármacos
Bupivacaína/farmacologia
Morte Celular/efeitos dos fármacos
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Cromanos/farmacologia
Relação Dose-Resposta a Droga
Células HeLa
Seres Humanos
Potencial da Membrana Mitocondrial/efeitos dos fármacos
Mepivacaína/administração & dosagem
Mitocôndrias/efeitos dos fármacos
Neuroblastoma/metabolismo
Fatores de Tempo
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anesthetics, Local); 0 (Antioxidants); 0 (Chromans); 0 (Reactive Oxygen Species); 98PI200987 (Lidocaine); B6E06QE59J (Mepivacaine); S18UL9710X (6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid); WYQ7N0BPYC (Acetylcysteine); Y8335394RO (Bupivacaine)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171204
[Lr] Data última revisão:
171204
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161026
[St] Status:MEDLINE


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[PMID]:28966274
[Au] Autor:Zhong Y; Han X; Li S; Qi H; Song Y; Qiao X
[Ad] Endereço:Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University.
[Ti] Título:Design, Synthesis, Antifungal Activity and Molecular Docking of Thiochroman-4-one Derivatives.
[So] Source:Chem Pharm Bull (Tokyo);65(10):904-910, 2017.
[Is] ISSN:1347-5223
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:N-Myristoyltransferase (NMT) has been validated pre-clinically as a target for treatment of fungal infections. Various substituted thiochroman-4-one derivatives have been synthesized by an efficient method. The synthesized compounds 7a-y and 8a-t were evaluated for their in vitro antifungal activity against the Canidia albicans, Cryptococcus neoformans, Epidermophyton floccosum, Mucor racemosus, Microsporum gypseum and Aspergillus nigerstrain. A series of compounds exhibited significant activity (minimal inhibitory concentrotion (MIC)=0.5-16 µg/mL) against Canidia albicans and Cryptococcus neoformans. The antifungal activity of compound 7b was reached to that of fluconazole, which can serve as a good starting point for further studies of structural diversity of the NMT inhibitors. The molecular docking studies revealed an interesting binding profile with very high receptor affinity for NMT of Canidia albicans.
[Mh] Termos MeSH primário: Aciltransferases/metabolismo
Antifúngicos/síntese química
Cromanos/química
Desenho de Drogas
Inibidores Enzimáticos/síntese química
[Mh] Termos MeSH secundário: Aciltransferases/química
Antifúngicos/química
Antifúngicos/farmacologia
Sítios de Ligação
Candida albicans/efeitos dos fármacos
Domínio Catalítico
Cromanos/síntese química
Cromanos/farmacologia
Cryptococcus neoformans/efeitos dos fármacos
Inibidores Enzimáticos/química
Inibidores Enzimáticos/farmacologia
Fluconazol/farmacologia
Testes de Sensibilidade Microbiana
Simulação de Acoplamento Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antifungal Agents); 0 (Chromans); 0 (Enzyme Inhibitors); 8VZV102JFY (Fluconazole); EC 2.3.- (Acyltransferases); EC 2.3.1.97 (glycylpeptide N-tetradecanoyltransferase)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171003
[St] Status:MEDLINE
[do] DOI:10.1248/cpb.c17-00274


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[PMID]:28844711
[Au] Autor:Fallatah MM; Liu S; Sevigny MB; Zou H; Louie MC
[Ad] Endereço:Department of Natural Sciences and Mathematics, Dominican University of California, 50 Acacia Avenue, San Rafael, CA 94901, USA.
[Ti] Título:Novel flexible heteroarotinoid, SL-1-18, promotes ERα degradation to inhibit breast cancer cell growth.
[So] Source:Cancer Lett;408:82-91, 2017 Nov 01.
[Is] ISSN:1872-7980
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:SL-1-18 (1-(chrysen-6-yl)-3-(4-nitrophenyl)thiourea) is new flexible heteroarotinoid (Flex-Het) analog derived from the parent compound, SHetA2, and our previous study showed comparable activity to SHetA2 in terms of inhibiting ER+ breast cancer cell growth. This current study aims to determine the molecular mechanism underlying SL-1-18's effect on breast cancer cell growth. Our results indicate that SL-1-18 inhibits cell proliferation of ER+ breast cancer cells (MCF-7 and T-47D) by preventing cell cycle progression. SL-1-18 treatment correlated positively with decreased expression of key cell-cycle regulators, such as cyclin D1, as well as other ERα-target genes at both the transcript and protein levels. Interestingly, decreased expression of ERα was also observed, with a significant reduction at the protein level within 2 h of SL-1-18 treatment, while the decrease in mRNA occurred at a later time point. ERα degradation was shown to be mediated by the ubiquitination-proteasome pathway. In summary, this is the first study to show that a Flex-Het- SL-1-18- can promote the degradation of ERα via the ubiquitin-proteasome pathway and should be further developed as a therapeutic option for ER+ breast cancer.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Neoplasias da Mama/tratamento farmacológico
Cromanos/farmacologia
Crisenos/farmacologia
Receptor alfa de Estrogênio/metabolismo
Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos
Proteólise/efeitos dos fármacos
Tioureia/análogos & derivados
[Mh] Termos MeSH secundário: Apoptose/efeitos dos fármacos
Neoplasias da Mama/metabolismo
Neoplasias da Mama/patologia
Ciclo Celular/efeitos dos fármacos
Proliferação Celular/efeitos dos fármacos
Feminino
Seres Humanos
Complexo de Endopeptidases do Proteassoma
Tionas/farmacologia
Tioureia/farmacologia
Células Tumorais Cultivadas
Ubiquitinação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 ((((4-nitrophenyl)amino)(2,2,4,4-tetramethyl thiochroman-6-yl)amino) methane-1-thione); 0 (1-(chrysen-6-yl)-3-(4-nitrophenyl)thiourea); 0 (Antineoplastic Agents); 0 (Chromans); 0 (Chrysenes); 0 (Estrogen Receptor alpha); 0 (Thiones); 0 (estrogen receptor alpha, human); EC 3.4.25.1 (Proteasome Endopeptidase Complex); GYV9AM2QAG (Thiourea)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171101
[Lr] Data última revisão:
171101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170829
[St] Status:MEDLINE


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[PMID]:28764097
[Au] Autor:Çelik EE; Rubio JMA; Andersen ML; Gökmen V
[Ad] Endereço:Food Quality and Safety (FoQuS) Research Group, Food Engineering Department, Hacettepe University, 06800 Beytepe, Ankara, Turkey; Chemometrics and Analytical Technology, Department of Food Science, Faculty of Science, University of Copenhagen, Rolighedsvej 26, 1958 Frederiksberg C, Denmark; Ingredie
[Ti] Título:Interactions between macromolecule-bound antioxidants and Trolox during liposome autoxidation: A multivariate approach.
[So] Source:Food Chem;237:989-996, 2017 Dec 15.
[Is] ISSN:0308-8146
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The interactions between free and macromolecule-bound antioxidants were investigated in order to evaluate their combined effects on the antioxidant environment. Dietary fiber (DF), protein and lipid-bound antioxidants, obtained from whole wheat, soybean and olive oil products, respectively and Trolox were used for this purpose. Experimental studies were carried out in autoxidizing liposome medium by monitoring the development of fluorescent products formed by lipid oxidation. Chemometric methods were used both at experimental design and multivariate data analysis stages. Comparison of the simple addition effects of Trolox and bound antioxidants with measured values on lipid oxidation revealed synergetic interactions for DF and refined olive oil-bound antioxidants, and antagonistic interactions for protein and extra virgin olive oil-bound antioxidants with Trolox. A generalized version of logistic function was successfully used for modelling the oxidation curve of liposomes. Principal component analysis revealed two separate phases of liposome autoxidation.
[Mh] Termos MeSH primário: Antioxidantes/química
[Mh] Termos MeSH secundário: Cromanos
Lipossomos
Azeite de Oliva
Oxirredução
Óleos Vegetais
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Chromans); 0 (Liposomes); 0 (Olive Oil); 0 (Plant Oils); S18UL9710X (6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171101
[Lr] Data última revisão:
171101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170803
[St] Status:MEDLINE


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[PMID]:28651915
[Au] Autor:Yang HS; Venkateswararao E; Boggu PR; Sharma VK; Kim Y; Jung SH
[Ad] Endereço:College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 34134, Republic of Korea.
[Ti] Título:Novel analogs of N-acylhydroxyethylaminomethyl-4H-chromen-4-one scaffold as IL-5 inhibitors.
[So] Source:Bioorg Med Chem;25(16):4330-4338, 2017 Aug 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A number of N-acyl substituted hydroxyethylaminomethyl-4H-chromen-4-ones 6a-u were prepared and evaluated for their IL-5 inhibitory activity. Among them, the compound 6r (95.0% inhibition at 30µM, IC =10.0µM, ClogP=4.1549) showed most potent inhibitory activity. The structure activity relationship revealed that the bulkier or hydrophobic substituents at urea, carbamate or amide group resulted in good inhibitory activity against IL-5. Moreover, electron donating group at phenyl ring (6g and 6s) is much more active than electron withdrawing group (6f). Finally, replacement of cyclohexylmethoxy group at 5 position of ring A with bulky aliphatic substituents resulted in the loss of activity.
[Mh] Termos MeSH primário: Cromanos/farmacologia
Interleucina-5/antagonistas & inibidores
[Mh] Termos MeSH secundário: Animais
Linhagem Celular
Proliferação Celular/efeitos dos fármacos
Cromanos/síntese química
Cromanos/química
Relação Dose-Resposta a Droga
Camundongos
Estrutura Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Chromans); 0 (Interleukin-5); 0 (N-acylhydroxyethylaminomethyl-4H-chromen-4-one)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170814
[Lr] Data última revisão:
170814
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170628
[St] Status:MEDLINE


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[PMID]:28645914
[Au] Autor:Cheng Y; Chen S; Freeden C; Chen W; Zhang Y; Abraham P; Nelson DM; Humphreys WG; Gan J; Lai Y
[Ad] Endereço:Pharmaceutical Candidate Optimization, Bristol-Myers Squibb, Princeton, New Jersey yaofeng.cheng@BMS.com.
[Ti] Título:Bile Salt Homeostasis in Normal and Bsep Gene Knockout Rats with Single and Repeated Doses of Troglitazone.
[So] Source:J Pharmacol Exp Ther;362(3):385-394, 2017 Sep.
[Is] ISSN:1521-0103
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The interference of bile acid secretion through bile salt export pump (BSEP) inhibition is one of the mechanisms for troglitazone (TGZ)-induced hepatotoxicity. Here, we investigated the impact of single or repeated oral doses of TGZ (200 mg/kg/day, 7 days) on bile acid homoeostasis in wild-type (WT) and Bsep knockout (KO) rats. Following oral doses, plasma exposures of TGZ were not different between WT and KO rats, and were similar on day 1 and day 7. However, plasma exposures of the major metabolite, troglitazone sulfate (TS), in KO rats were 7.6- and 9.3-fold lower than in WT on day 1 and day 7, respectively, due to increased TS biliary excretion. With Bsep KO, the mRNA levels of multidrug resistance-associated protein 2 (Mrp2), Mrp3, Mrp4, Mdr1, breast cancer resistance protein (Bcrp), sodium taurocholate cotransporting polypeptide, small heterodimer partner, and Sult2A1 were significantly altered in KO rats. Following seven daily TGZ treatments, Cyp7A1 was significantly increased in both WT and KO rats. In the vehicle groups, plasma exposures of individual bile acids demonstrated variable changes in KO rats as compared with WT. WT rats dosed with TGZ showed an increase of many bile acid species in plasma on day 1, suggesting the inhibition of Bsep. Conversely, these changes returned to base levels on day 7. In KO rats, alterations of most bile acids were observed after seven doses of TGZ. Collectively, bile acid homeostasis in rats was regulated through bile acid synthesis and transport in response to Bsep deficiency and TGZ inhibition. Additionally, our study is the first to demonstrate that repeated TGZ doses can upregulate Cyp7A1 in rats.
[Mh] Termos MeSH primário: Transportadores de Cassetes de Ligação de ATP/genética
Ácidos e Sais Biliares/metabolismo
Cromanos/farmacologia
Homeostase/efeitos dos fármacos
Homeostase/genética
Hipoglicemiantes/farmacologia
Tiazolidinedionas/farmacologia
[Mh] Termos MeSH secundário: Membro 11 da Subfamília B de Transportadores de Cassetes de Ligação de ATP
Animais
Bile/metabolismo
Colesterol 7-alfa-Hidroxilase/biossíntese
Colesterol 7-alfa-Hidroxilase/genética
Técnicas de Inativação de Genes
Fígado/efeitos dos fármacos
Fígado/metabolismo
Masculino
RNA Mensageiro/biossíntese
RNA Mensageiro/genética
Ratos
Ratos Sprague-Dawley
Regulação para Cima/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ATP Binding Cassette Subfamily B Member 11); 0 (Abcb11 protein, rat); 0 (Bile Acids and Salts); 0 (Chromans); 0 (Hypoglycemic Agents); 0 (RNA, Messenger); 0 (Thiazolidinediones); EC 1.14.14.23 (CYP7A1 protein, rat); EC 1.14.14.23 (Cholesterol 7-alpha-Hydroxylase); I66ZZ0ZN0E (troglitazone)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170625
[St] Status:MEDLINE
[do] DOI:10.1124/jpet.117.242370


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[PMID]:28635646
[Au] Autor:Gu T; Zhong Y; Lu YT; Sun Y; Dong ZX; Wu WY; Shi ZH; Li NG; Xue X; Fang F; Li HM; Tang YP
[Ad] Endereço:National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China. guting1992@163.com.
[Ti] Título:Synthesis and Bioactivity Characterization of Scutellarein Sulfonated Derivative.
[So] Source:Molecules;22(6), 2017 Jun 21.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Scutellarin ( ) has been widely used to treat acute cerebral infarction in clinic, but poor aqueous solubility decreases its bioavailability. Interestingly, scutellarin ( ) could be metabolized into scutellarein ( ) in vivo. In this study, a sulfonic group was introduced at position C-8 of scutellarein ( ) to enhance the aqueous solubility of the obtained derivative ( ). DPPH (1,1-diphenyl-2-picrylhydrazyl)-radical scavenging ability and antithrombic activity were also conducted to determine its bioactivity. The result showed that scutellarein derivate ( ) could be a better agent for ischemic cerebrovascular disease treatment.
[Mh] Termos MeSH primário: Cromanos/síntese química
Fibrinolíticos/síntese química
[Mh] Termos MeSH secundário: Animais
Antioxidantes/síntese química
Antioxidantes/química
Antioxidantes/farmacologia
Apigenina/síntese química
Apigenina/química
Apigenina/farmacologia
Compostos de Bifenilo/metabolismo
Isquemia Encefálica/tratamento farmacológico
Transtornos Cerebrovasculares/tratamento farmacológico
Cromanos/química
Cromanos/farmacologia
Cromanos/uso terapêutico
Erigeron/química
Fibrinolíticos/farmacologia
Fibrinolíticos/uso terapêutico
Depuradores de Radicais Livres/síntese química
Depuradores de Radicais Livres/química
Depuradores de Radicais Livres/farmacologia
Glucuronatos/química
Glucuronatos/farmacologia
Seres Humanos
Masculino
Picratos/metabolismo
Coelhos
Solubilidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (5,6,7-trihydroxy-2-(4-hydroxyphenyl)-4-oxo-4H-chromene-8-sulfonic acid); 0 (Antioxidants); 0 (Biphenyl Compounds); 0 (Chromans); 0 (Fibrinolytic Agents); 0 (Free Radical Scavengers); 0 (Glucuronates); 0 (Picrates); 16IGP0ML9A (scutellarin); 7V515PI7F6 (Apigenin); DFD3H4VGDH (1,1-diphenyl-2-picrylhydrazyl); P460GTI853 (scutellarein)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170622
[St] Status:MEDLINE



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