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[PMID]: 28465233 [Au] Autor: Zhao XL; Chen LF; Wang Z [Ad] Endereço: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. [Ti] Título: Aesculin modulates bone metabolism by suppressing receptor activator of NF-κB ligand (RANKL)-induced osteoclastogenesis and transduction signals. [So] Source: Biochem Biophys Res Commun;488(1):15-21, 2017 06 17. [Is] ISSN: 1090-2104 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Aesculin (AES), a coumarin compound derived from Aesculus hippocasanum L, is reported to exert protective role against inflammatory diseases, gastric disease and cancer. However, direct effect of AES in bone metabolism is deficient. In this study, we examined the effects of AES on osteoclast (OC) differentiation in receptor activator of NF-κB ligand (RANKL)-induced RAW264.7 cells. AES inhibits the OC differentiation in both dose- and time-dependent manner within non-toxic concentrations, as analyzed by Tartrate Resistant Acid Phosphatase (TRAP) staining. The actin ring formation manifesting OC function is also decreased by AES. Moreover, expressions of osteoclastogenesis related genes Trap, Atp6v0d2, Cathepsin K and Mmp-9 are decreased upon AES treatment. Mechanistically, AES attenuates the activation of MAPKs and NF-κB activity upon RANKL induction, thus leading to the reduction of Nfatc1 mRNA expression. Moreover, AES inhibits Rank expression, and RANK overexpression markedly decreases AES's effect on OC differentiation and NF-κB activity. Consistently, AES protects against bone mass loss in the ovariectomized and dexamethasone treated rat osteoporosis model. Taken together, our data demonstrate that AES can modulate bone metabolism by suppressing osteoclastogenesis and related transduction signals. AES therefore could be a promising agent for the treatment of osteoporosis. [Mh] Termos MeSH primário: Osso e Ossos/efeitos dos fármacos Osso e Ossos/metabolismo Esculina/farmacologia Osteogênese/efeitos dos fármacos Ligante RANK/antagonistas & inibidores Transdução de Sinais/efeitos dos fármacos [Mh] Termos MeSH secundário: Animais Células Cultivadas Relação Dose-Resposta a Droga Esculina/administração & dosagem Esculina/química Camundongos Conformação Molecular Ligante RANK/metabolismo Células RAW 264.7 Relação Estrutura-Atividade [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (RANK Ligand); 0 (Tnfsf11 protein, mouse); 1Y1L18LQAF (Esculin) [Em] Mês de entrada: 1709 [Cu] Atualização por classe: 171128 [Lr] Data última revisão: 171128 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170504 [St] Status: MEDLINE

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[PMID]: 28805379 [Au] Autor: Zhang M; Xin X; Lai F; Zhang X; Li X; Wu H [Ad] Endereço: College of Food Science and Engineering, ‡Research Institude of Shaoguan Huagong High-tech Industry, and §State Key Laboratory of Pulp and Paper Engineering, South China University of Technology , Guangzhou, Guangdong 510640, China. [Ti] Título: Cellular Transport of Esculin and Its Acylated Derivatives in Caco-2 Cell Monolayers and Their Antioxidant Properties in Vitro. [So] Source: J Agric Food Chem;65(34):7424-7432, 2017 Aug 30. [Is] ISSN: 1520-5118 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Esculin has many pharmacological effects, but these are difficult to observe after oral administration owing to poor lipid solubility. In our previous study, five acylated derivatives with different acyl chain lengths (EA, EP, EO, EL, and EM) were synthesized to improve the lipophilicity of esculin. In this study, the bioavailability and antioxidant activity of the five derivatives were investigated. The logP of esculin, EA, EP, EO, EL, and EM were -1.1 ± 0.1, -0.3 ± 0.14, 0.1 ± 0.17, 1.6 ± 0.09, 2.4 ± 0.11, and 2.8 ± 0.18, and their P were 0.71 ± 0.02, 1.24 ± 0.18, 1.74 ± 0.11, 11.6 ± 3.6, 4.11 ± 1.03, and 2.64 ± 0.97 × 10 cm/s, respectively. Besides, the bioavailability of EO, EL, and EM were seriously affected by carboxylesterase. The results of ABTS, ORAC, and DPPH assays indicated that the antiradical ability of the five derivatives did not exceed that of esculin. However, EA, EP, and EO showed more effective inhibition of AAPH-induced oxidative hemolysis than esculin did (p < 0.05), and EL and EM were less effective than esculin (p < 0.05). The mechanism was related to the distribution and localization of the derivatives in "oil-water interface" between the cytomembrane and the aqueous phase. [Mh] Termos MeSH primário: Antioxidantes/metabolismo Esculina/metabolismo [Mh] Termos MeSH secundário: Acilação Transporte Biológico Células CACO-2 Seres Humanos [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antioxidants); 1Y1L18LQAF (Esculin) [Em] Mês de entrada: 1709 [Cu] Atualização por classe: 170915 [Lr] Data última revisão: 170915 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170815 [St] Status: MEDLINE [do] DOI: 10.1021/acs.jafc.7b02525

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[PMID]: 28096449 [Au] Autor: Nieves-Morión M; Lechno-Yossef S; López-Igual R; Frías JE; Mariscal V; Nürnberg DJ; Mullineaux CW; Wolk CP; Flores E [Ad] Endereço: Instituto de Bioquímica Vegetal y Fotosíntesis, CSIC and Universidad de Sevilla, Seville, Spain. [Ti] Título: Specific Glucoside Transporters Influence Septal Structure and Function in the Filamentous, Heterocyst-Forming Cyanobacterium Anabaena sp. Strain PCC 7120. [So] Source: J Bacteriol;199(7), 2017 Apr 01. [Is] ISSN: 1098-5530 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: When deprived of combined nitrogen, some filamentous cyanobacteria contain two cell types: vegetative cells that fix CO through oxygenic photosynthesis and heterocysts that are specialized in N fixation. In the diazotrophic filament, the vegetative cells provide the heterocysts with reduced carbon (mainly in the form of sucrose) and heterocysts provide the vegetative cells with combined nitrogen. Septal junctions traverse peptidoglycan through structures known as nanopores and appear to mediate intercellular molecular transfer that can be traced with fluorescent markers, including the sucrose analog esculin (a coumarin glucoside) that is incorporated into the cells. Uptake of esculin by the model heterocyst-forming cyanobacterium sp. strain PCC 7120 was inhibited by the α-glucosides sucrose and maltose. Analysis of mutants identified components of three glucoside transporters that move esculin into the cells: GlsC (Alr4781) and GlsP (All0261) are an ATP-binding subunit and a permease subunit of two different ABC transporters, respectively, and HepP (All1711) is a major facilitator superfamily (MFS) protein that was shown previously to be involved in formation of the heterocyst envelope. Transfer of fluorescent markers (especially calcein) between vegetative cells of was impaired by mutation of glucoside transporter genes. GlsP and HepP interact in bacterial two-hybrid assays with the septal junction-related protein SepJ, and GlsC was found to be necessary for the formation of a normal number of septal peptidoglycan nanopores and for normal subcellular localization of SepJ. Therefore, beyond their possible role in nutrient uptake in , glucoside transporters influence the structure and function of septal junctions. Heterocyst-forming cyanobacteria have the ability to perform oxygenic photosynthesis and to assimilate atmospheric CO and N These organisms grow as filaments that fix these gases specifically in vegetative cells and heterocysts, respectively. For the filaments to grow, these types of cells exchange nutrients, including sucrose, which serves as a source of reducing power and of carbon skeletons for the heterocysts. Movement of sucrose between cells in the filament takes place through septal junctions and has been traced with a fluorescent sucrose analog, esculin, that can be taken up by the cells. Here, we identified α-glucoside transporters of that mediate uptake of esculin and, notably, influence septal structure and the function of septal junctions. [Mh] Termos MeSH primário: Transportadores de Cassetes de Ligação de ATP/metabolismo Anabaena/metabolismo Regulação Bacteriana da Expressão Gênica/fisiologia Glucosídeos/metabolismo [Mh] Termos MeSH secundário: Transportadores de Cassetes de Ligação de ATP/genética Anabaena/genética Proteínas de Bactérias/metabolismo Transporte Biológico Esculina/metabolismo Mutação Ligação Proteica [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Bacterial Proteins); 0 (Glucosides); 1Y1L18LQAF (Esculin) [Em] Mês de entrada: 1706 [Cu] Atualização por classe: 170914 [Lr] Data última revisão: 170914 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170119 [St] Status: MEDLINE

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[PMID]: 27875787 [Au] Autor: Yang L; Meng X; Yu X; Kuang H [Ad] Endereço: School of Pharmacy, Heilongjiang University of Traditional Chinese Medicine, Harbin 150040, Heilongjiang, China. Electronic address: lianrong_790717@sina.com. [Ti] Título: Simultaneous determination of anemoside B4, phellodendrine, berberine, palmatine, obakunone, esculin, esculetin in rat plasma by UPLC-ESI-MS/MS and its application to a comparative pharmacokinetic study in normal and ulcerative colitis rats. [So] Source: J Pharm Biomed Anal;134:43-52, 2017 Feb 05. [Is] ISSN: 1873-264X [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: A sensitive and rapid ultra-performance liquid chromatography-electrospray ionization-mass spectrometry (UPLC-ESI-MS/MS) method was developed for the simultaneous analysis of anemoside B4, phellodendrine, berberine, palmatine, obakunone, esculin, esculetin, toosendanin (IS of anemoside B4), tetrahydropalmatine (IS of phellodendrine, berberine, palmatine and obakunone) and scopoletin (IS of esculin and esculetin) and to compare the pharmacokinetics of these active ingredients in normal and ulcerative colitis rats. After methanol deproteinization, solvents were evaporated at 40°C under a gentle stream of nitrogen. Chromatography was performed using a C18 column with a gradient elution of 0.1% aqueous formic acid and acetonitrile at 0.4ml/min. Detection and measurement were performed on a 4000 QTRAP UPLC-MS/MS system from AB Sciex in the multiple reaction monitoring (MRM) mode. Phellodendrine, berberine, palmatine, obakunone, esculin, esculetin, tetrahydropalmatine (IS ) and scopoletin (IS ) were monitored under positive ionization conditions. Anemoside B4, and toosendanin (IS ) were monitored under negative ionization conditions. The optimized mass transition ion-pairs (m/z) were 1221.1/750.7 for anemoside B4, 343.2/193.2 for phellodendrine, 337.1/321.0 for berberine, 353.0/336.9 for palmatine, 455.1/161.1 for obakunone, 341.2/179.2 for esculin, 179.1/123.0 for esculetin, 573.4/531.4 for toosendanin (IS ), 356.2/192.2 for tetrahydropalmatine (IS ) and 193.0/133.1 for scopoletin (IS ). [Mh] Termos MeSH primário: Colite Ulcerativa/sangue Medicamentos de Ervas Chinesas/análise Medicamentos de Ervas Chinesas/metabolismo Espectrometria de Massas por Ionização por Electrospray/métodos [Mh] Termos MeSH secundário: Animais Berberina/análise Berberina/sangue Alcaloides de Berberina/análise Alcaloides de Berberina/sangue Cromatografia Líquida de Alta Pressão/métodos Esculina/análise Esculina/sangue Masculino Quinolizinas/análise Quinolizinas/sangue Ratos Ratos Sprague-Dawley Espectrometria de Massas em Tandem/métodos Umbeliferonas/análise Umbeliferonas/sangue [Pt] Tipo de publicação: COMPARATIVE STUDY; JOURNAL ARTICLE [Nm] Nome de substância: 0 (Berberine Alkaloids); 0 (Drugs, Chinese Herbal); 0 (Quinolizines); 0 (Umbelliferones); 0I8Y3P32UF (Berberine); 1Y1L18LQAF (Esculin); 6873-13-8 (phellodendrine); G50C034217 (palmatine); SM2XD6V944 (esculetin) [Em] Mês de entrada: 1705 [Cu] Atualização por classe: 170523 [Lr] Data última revisão: 170523 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161123 [St] Status: MEDLINE

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[PMID]: 27873354 [Au] Autor: Li W; Wang Y; Wang X; Zhang H; He Z; Zhi W; Liu F; Niu X [Ad] Endereço: School of Pharmacy, Xi'an Jiaotong University, Xi'an, 710061, China. [Ti] Título: Gastroprotective effect of esculin on ethanol-induced gastric lesion in mice. [So] Source: Fundam Clin Pharmacol;31(2):174-184, 2017 Apr. [Is] ISSN: 1472-8206 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: The gastroprotective effect of esculin was investigated in a mouse model of ethanol-induced gastric lesion. Administration of esculin at doses of 5, 10, and 20 mg/kg body weight prior to ethanol ingestion led to significant gastroprotection compared with untreated mice. Gastric mucosal lesions were evaluated by macroscopic and histopathological alterations, lesion index, and myeloperoxidase (MPO) activity. Pretreatment with esculin significantly reduced macroscopic and histopathological damage, gastric lesion index, and MPO activity in a dose-dependent manner. Moreover, esculin significantly reduced nitric oxide (NO) production, inducible NO synthase (iNOS) levels, and nuclear factor-kappa B (NF-κB) p65 protein expression in gastric tissues after ethanol challenge. Analysis of inflammatory cytokines indicated that esculin pretreatment markedly suppressed the increased expression of tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6) in ethanol-treated mice. The results demonstrate a protective effect of esculin against gastric injury and suggest that the underlying mechanism might be associated with inhibition of NF-κB activation, which subsequently reduces expression of iNOS, TNF-α, and IL-6. [Mh] Termos MeSH primário: Esculina/farmacologia Etanol/toxicidade Mucosa Gástrica/efeitos dos fármacos Úlcera Gástrica/prevenção & controle [Mh] Termos MeSH secundário: Animais Citocinas/metabolismo Modelos Animais de Doenças Relação Dose-Resposta a Droga Esculina/administração & dosagem Mucosa Gástrica/patologia Interleucina-6/metabolismo Masculino Camundongos Óxido Nítrico/metabolismo Peroxidase/metabolismo Úlcera Gástrica/induzido quimicamente Fator de Necrose Tumoral alfa/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Cytokines); 0 (Interleukin-6); 0 (Tumor Necrosis Factor-alpha); 1Y1L18LQAF (Esculin); 31C4KY9ESH (Nitric Oxide); 3K9958V90M (Ethanol); EC 1.11.1.7 (Peroxidase) [Em] Mês de entrada: 1706 [Cu] Atualização por classe: 170620 [Lr] Data última revisão: 170620 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161123 [St] Status: MEDLINE [do] DOI: 10.1111/fcp.12255

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[PMID]: 27825835 [Au] Autor: Mokdad Bzeouich I; Mustapha N; Maatouk M; Ghedira K; Ghoul M; Chekir-Ghedira L [Ad] Endereço: Laboratory of Cellular and Molecular Biology, Faculty of Dental Medicine, University of Monastir, Avicenna Street, 5000, Monastir, Tunisia; Unit of Bioactive and Natural Substances and Biotechnology UR12ES12, Faculty of Pharmacy, University of Monastir, Avicenna Street, 5000, Monastir, Tunisia. [Ti] Título: Genotoxic and anti-genotoxic effects of esculin and its oligomer fractions against mitomycin C-induced DNA damages in mice. [So] Source: Regul Toxicol Pharmacol;82:48-52, 2016 Dec. [Is] ISSN: 1096-0295 [Cp] País de publicação: Netherlands [La] Idioma: eng [Ab] Resumo: Mitomycin C is one of the most effective chemotherapeutic drugs against various solid tumors. However, despite its wide spectrum of clinical benefits, this agent is capable of inducing various types of genotoxicity. In this study, we investigated the effect of esculin and its oligomer fractions (E1, E2 and E3) against mitomycin C induced genotoxicity in liver and kidney cells isolated from Balb/C mice using the comet assay. Esculin and its oligomer fractions were not genotoxic at the tested doses (20 mg/kg and 40 mg/kg b.w). A significant decrease in DNA damages was observed, suggesting a protective role of esculin and its oligomer fractions against the genotoxicity induced by mitomycin C on liver and kidney cells. Moreover, esculin and its oligomer fractions did not induce an increase of malondialdehyde levels. [Mh] Termos MeSH primário: Antibióticos Antineoplásicos/toxicidade Antimutagênicos/farmacologia Dano ao DNA/efeitos dos fármacos Esculina/farmacologia Rim/efeitos dos fármacos Fígado/efeitos dos fármacos Micronúcleos com Defeito Cromossômico/efeitos dos fármacos Mitomicina/toxicidade [Mh] Termos MeSH secundário: Animais Antimutagênicos/toxicidade Relação Dose-Resposta a Droga Esculina/toxicidade Rim/metabolismo Rim/patologia Peroxidação de Lipídeos/efeitos dos fármacos Fígado/metabolismo Fígado/patologia Malondialdeído/metabolismo Camundongos Endogâmicos BALB C Micronúcleos com Defeito Cromossômico/induzido quimicamente Testes para Micronúcleos [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antibiotics, Antineoplastic); 0 (Antimutagenic Agents); 1Y1L18LQAF (Esculin); 4Y8F71G49Q (Malondialdehyde); 50SG953SK6 (Mitomycin) [Em] Mês de entrada: 1703 [Cu] Atualização por classe: 170316 [Lr] Data última revisão: 170316 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161110 [St] Status: MEDLINE

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[PMID]: 27746168 [Au] Autor: Li W; Wang Y; Wang X; He Z; Liu F; Zhi W; Zhang H; Niu X [Ad] Endereço: School of Pharmacy, Xi'an Jiaotong University, Xi'an 710061, PR China. Electronic address: liwf@mail.xjtu.edu.cn. [Ti] Título: Esculin attenuates endotoxin shock induced by lipopolysaccharide in mouse and NO production in vitro through inhibition of NF-κB activation. [So] Source: Eur J Pharmacol;791:726-734, 2016 Nov 15. [Is] ISSN: 1879-0712 [Cp] País de publicação: Netherlands [La] Idioma: eng [Ab] Resumo: Esculin, a coumarin compound derived from the traditional Chinese herbs such as Cortex Fraxini, has long been used for treating inflammatory and vascular diseases. In present study, we analyzed the role of esculin against macrophages and endotoxin shock induced by lipopolysaccharide (LPS) in mice. Here, we demonstrated that esculin suppressed inflammatory reactions in macrophages and protected mice from LPS-induced endotoxin shock. We found that esculin significantly inhibited the production of nitric oxide (NO) production via the inhibition of nuclear factor-κB (NF-κB) activation in macrophages. In animal model, esculin pretreatment significantly improved the survival rate of mice. LPS-induced increase of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in serum, lung, liver and kidney were markedly inhibited by esculin. IL-10, an anti-inflammatory cytokine, was up-regulated by esculin. Moreover, the histopathological analyses showed that esculin significantly attenuated the tissues injury of lung, liver, kidney in endotoxic mice. In addition, esculin significantly diminished the protein expression of NF-κB p65 in lung, liver, kidney, which resulted in lower levels of inflammatory mediators. These results suggest that esculin may be a potential drug for treatment of various inflammatory diseases. [Mh] Termos MeSH primário: Anti-Inflamatórios/farmacologia Esculina/farmacologia Lipopolissacarídeos/toxicidade Óxido Nítrico/biossíntese Choque Séptico/induzido quimicamente Choque Séptico/tratamento farmacológico Fator de Transcrição RelA/metabolismo [Mh] Termos MeSH secundário: Animais Anti-Inflamatórios/uso terapêutico Esculina/uso terapêutico Feminino Regulação da Expressão Gênica/efeitos dos fármacos Interleucina-10/sangue Interleucina-6/biossíntese Interleucina-6/sangue Macrófagos/efeitos dos fármacos Macrófagos/metabolismo Masculino Camundongos Óxido Nítrico/sangue Especificidade de Órgãos Choque Séptico/metabolismo Fator de Necrose Tumoral alfa/biossíntese Fator de Necrose Tumoral alfa/sangue [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Anti-Inflammatory Agents); 0 (Interleukin-6); 0 (Lipopolysaccharides); 0 (Transcription Factor RelA); 0 (Tumor Necrosis Factor-alpha); 130068-27-8 (Interleukin-10); 1Y1L18LQAF (Esculin); 31C4KY9ESH (Nitric Oxide) [Em] Mês de entrada: 1704 [Cu] Atualização por classe: 170821 [Lr] Data última revisão: 170821 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161018 [St] Status: MEDLINE

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[PMID]: 27060277 [Au] Autor: Tierney D; Copsey SD; Morris T; Perry JD [Ad] Endereço: Microbiology Department, Freeman Hospital, Newcastle upon Tyne, UK; Department of Applied Sciences, Northumbria University, Newcastle upon Tyne, UK. [Ti] Título: A new chromogenic medium for isolation of Bacteroides fragilis suitable for screening for strains with antimicrobial resistance. [So] Source: Anaerobe;39:168-72, 2016 Jun. [Is] ISSN: 1095-8274 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: There have been an increasing number of reports describing the acquisition of antimicrobial resistance by Bacteroides fragilis including the occurrence of strains with resistance to multiple antimicrobials that are relied upon for treatment of infections. The aim of this study was to design a chromogenic selective medium for isolation of B. fragilis that could be adapted for specific isolation of antimicrobial-resistant strains. Bacteroides chromogenic agar (BCA) was the result of this endeavour and allowed growth of Bacteroides spp. as black colonies and the efficient inhibition of almost all other genera tested. The medium also allowed some differentiation of B. fragilis from other members of the B. fragilis group. When compared with an adaptation of Bacteroides bile-esculin agar (BBE) for the isolation of B. fragilis from 100 stool samples, 30 isolates of B. fragilis were recovered on BCA compared with 19 isolates recovered on BBE (P = 0.022). When supplemented with meropenem (4 µg/ml) or metronidazole (2 µg/ml), BCA could be used to select for the growth of B. fragilis isolates with resistance to these agents. We conclude that BCA is a useful research tool for surveillance studies to assess the prevalence of B. fragilis and, in particular, the occurrence of antimicrobial-resistant strains. [Mh] Termos MeSH primário: Bacteroides fragilis/isolamento & purificação Compostos Cromogênicos/química Farmacorresistência Bacteriana Múltipla Esculina/análogos & derivados Testes de Sensibilidade Microbiana/métodos [Mh] Termos MeSH secundário: Ágar Antibacterianos/farmacologia Infecções por Bacteroides/microbiologia Bacteroides fragilis/efeitos dos fármacos Bacteroides fragilis/metabolismo Esculina/química Fezes/microbiologia Seres Humanos [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (3,4-cyclohexenoesculetin-glucoside); 0 (Anti-Bacterial Agents); 0 (Chromogenic Compounds); 1Y1L18LQAF (Esculin); 9002-18-0 (Agar) [Em] Mês de entrada: 1701 [Cu] Atualização por classe: 170116 [Lr] Data última revisão: 170116 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160410 [St] Status: MEDLINE

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[PMID]: 27038404 [Au] Autor: Wang Y; Zhao M; Ou Y; Zeng B; Lou X; Wang M; Zhao C [Ad] Endereço: School of Pharmacy, Shenyang Pharmaceutical University, Wenhua Road 103, Shenyang, Liaoning Province, China. [Ti] Título: Metabolic profile of esculin in rats by ultra high performance liquid chromatography combined with Fourier transform ion cyclotron resonance mass spectrometry. [So] Source: J Chromatogr B Analyt Technol Biomed Life Sci;1020:120-8, 2016 May 01. [Is] ISSN: 1873-376X [Cp] País de publicação: Netherlands [La] Idioma: eng [Ab] Resumo: Esculin, a coumarin derivative found in Fraxinus rhynchophylla, has been reported to possess multiple biological activities. This present study is designed to investigate the metabolic profile of esculin in vivo based on ultra high performance liquid chromatography coupled to Fourier transform ion cyclotron resonance mass spectrometry (UHPLC-FT-ICR-MS) for the first time. After oral administration of esculin (100 mg/kg) for rats, plasma, urine, feces and bile samples were collected to screen metabolites. As a result, a total of 19 metabolites (10 phase I metabolites and 9 phase II metabolites) were found and identified. Results showed that metabolic pathways of esculin included hydrolysis, dehydrogenation, hydroxylation, methylation, dehydrogenation, glucuronidation, sulfation, and glycine conjugation. It was also found that after oral administration of esculin, the esculin could be metabolized to esculetin in vivo via deglycosylation, and esculetin was found in all biological samples. This study also laid solid basis for in-depth development of esculin and provided important information for clarifying the biotransformation process of esculin in vivo. [Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/métodos Esculina/análise Esculina/metabolismo Espectrometria de Massas/métodos Metabolômica/métodos [Mh] Termos MeSH secundário: Animais Masculino Ratos Ratos Sprague-Dawley [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 1Y1L18LQAF (Esculin) [Em] Mês de entrada: 1612 [Cu] Atualização por classe: 161230 [Lr] Data última revisão: 161230 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160403 [St] Status: MEDLINE

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[PMID]: 26960691 [Au] Autor: Mokdad Bzeouich I; Mustapha N; Sassi A; Ghedira K; Ghoul M; Chebil L; Luis J; Chekir-Ghedira L [Ad] Endereço: Laboratory of Cellular and Molecular Biology. Faculty of Dental Medicine, University of Monastir, Avicenne Street 5000, Monastir, Tunisia. [Ti] Título: Oligoesculin fraction induces anti-tumor effects and promotes immune responses on B16-F10 mice melanoma. [So] Source: Tumour Biol;37(8):11349-58, 2016 Aug. [Is] ISSN: 1423-0380 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Laccase was used to enzymatically polymerize esculin. Oligoesculin fraction was obtained after ultrafiltration through a 5-kDa membrane. Several studies have been carried out to prove the effectiveness of natural substances such as immunomodulators to promote the anti-cancer activity in situ. The purpose of our report was to explore whether the anti-tumor potential of the oligoesculin fraction in vitro and in vivo is linked to its immunological mechanisms in melanoma-bearing mice. We revealed that oligoesculin fraction reduced B16-F10 proliferation and migration in vitro in a dose-related manner. Moreover, melanin synthesis and tyrosinase activity were inhibited in these melanoma cells in a concentration-dependent way. The anti-tumor potential of oligoesculin fraction was also assessed in vivo. Our results showed that intraperitoneal administration of oligoesculin fraction, at 50 mg/kg body weight (b.w.) for 21 days, reduced tumor size and weight with percentages of inhibition of 94 and 87 %, respectively. Oligoesculin fraction was effective in promoting lysosomal activity and nitric oxide (NO) production by peritoneal macrophages in tumor-implanted mice. In addition, the activities of natural killer (NK), cytotoxic T lymphocytes, and macrophages were significantly enhanced by oligoesculin fraction. These findings suggested that this polymer with its anti-tumor and immunomodulatory properties could be used for the treatment of melanoma. [Mh] Termos MeSH primário: Antineoplásicos/farmacologia Citotoxicidade Imunológica/efeitos dos fármacos Esculina/farmacologia Melanoma Experimental/imunologia Neoplasias Cutâneas/imunologia [Mh] Termos MeSH secundário: Animais Citotoxicidade Imunológica/imunologia Fatores Imunológicos/farmacologia Células Matadoras Naturais/efeitos dos fármacos Células Matadoras Naturais/imunologia Macrófagos/efeitos dos fármacos Macrófagos/imunologia Melanoma Experimental/patologia Camundongos Camundongos Endogâmicos BALB C Neoplasias Cutâneas/patologia Linfócitos T Citotóxicos/efeitos dos fármacos Linfócitos T Citotóxicos/imunologia [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antineoplastic Agents); 0 (Immunologic Factors); 1Y1L18LQAF (Esculin) [Em] Mês de entrada: 1702 [Cu] Atualização por classe: 171111 [Lr] Data última revisão: 171111 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160311 [St] Status: MEDLINE [do] DOI: 10.1007/s13277-016-5011-4

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