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[PMID]:29376212
[Au] Autor:Bustos-Segura C; Foley WJ
[Ad] Endereço:Division of Ecology and Evolution, Research School of Biology, The Australian National University, Canberra, ACT 2601, Australia. bustossc@gmail.com.
[Ti] Título:Foliar Terpene Chemotypes and Herbivory Determine Variation in Plant Volatile Emissions.
[So] Source:J Chem Ecol;44(1):51-61, 2018 Jan.
[Is] ISSN:1573-1561
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Plants that synthesize and store terpenes in specialized cells accumulate large concentrations of these compounds while avoiding autotoxicity. Stored terpenes may influence the quantity and profile of volatile compounds that are emitted into the environment and the subsequent role of those volatiles in mediating the activity of herbivores. The Australian medicinal tea tree, Melaleuca alternifolia, occurs as several distinct terpene chemotypes. We studied the profile of its terpene emissions to understand how variations in stored foliar terpenes influenced emissions, both constitutive and when damaged either by herbivores or mechanically. We found that foliar chemistry influenced differences in the composition of terpene emissions, but those emissions were minimal in intact plants. When plants were damaged by herbivores or mechanically, the emissions were greatly increased and the composition corresponded to the constitutive terpenes and the volatility of each compound, suggesting the main origin of emissions is the stored terpenes and not de novo biosynthesized volatiles. However, herbivores modified the composition of the volatile emissions in only one chemotype, probably due to the oxidative metabolism of 1,8-cineole by the beetles. We also tested whether the foliar terpene blend acted as an attractant for the specialized leaf beetles Paropsisterna tigrina and Faex sp. and a parasitoid fly, Anagonia zentae. None of these species responded to extracts of young leaves in an olfactometer, so we found no evidence that these species use plant odor cues for host location in laboratory conditions.
[Mh] Termos MeSH primário: Coleópteros/fisiologia
Plantas/química
Terpenos/análise
Compostos Orgânicos Voláteis/química
[Mh] Termos MeSH secundário: Animais
Coleópteros/efeitos dos fármacos
Cicloexanóis/análise
Cicloexanóis/farmacologia
Cromatografia Gasosa-Espectrometria de Massas
Herbivoria/efeitos dos fármacos
Interações Hospedeiro-Parasita/efeitos dos fármacos
Monoterpenos/análise
Monoterpenos/farmacologia
Folhas de Planta/química
Folhas de Planta/metabolismo
Folhas de Planta/parasitologia
Plantas/metabolismo
Plantas/parasitologia
Análise de Componente Principal
Terpenos/metabolismo
Terpenos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cyclohexanols); 0 (Monoterpenes); 0 (Terpenes); 0 (Volatile Organic Compounds); RV6J6604TK (eucalyptol)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180221
[Lr] Data última revisão:
180221
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180130
[St] Status:MEDLINE
[do] DOI:10.1007/s10886-017-0919-8


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[PMID]:29016623
[Au] Autor:Schriever VA; Han P; Weise S; Hösel F; Pellegrino R; Hummel T
[Ad] Endereço:Smell & Taste Clinic, Department of Otorhinolaryngology, Technical University of Dresden, Dresden, Germany.
[Ti] Título:Time frequency analysis of olfactory induced EEG-power change.
[So] Source:PLoS One;12(10):e0185596, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:OBJECTIVES: The objective of the present study was to investigate the usefulness of time-frequency analysis (TFA) of olfactory-induced EEG change with a low-cost, portable olfactometer in the clinical investigation of smell function. MATERIALS & METHODS: A total of 78 volunteers participated. The study was composed of three parts where olfactory stimuli were presented using a custom-built olfactometer. Part I was designed to optimize the stimulus as well as the recording conditions. In part II EEG-power changes after olfactory/trigeminal stimulation were compared between healthy participants and patients with olfactory impairment. In Part III the test-retest reliability of the method was evaluated in healthy subjects. RESULTS: Part I indicated that the most effective paradigm for stimulus presentation was cued stimulus, with an interstimulus interval of 18-20s at a stimulus duration of 1000ms with each stimulus quality presented 60 times in blocks of 20 stimuli each. In Part II we found that central processing of olfactory stimuli analyzed by TFA differed significantly between healthy controls and patients even when controlling for age. It was possible to reliably distinguish patients with olfactory impairment from healthy individuals at a high degree of accuracy (healthy controls vs anosmic patients: sensitivity 75%; specificity 89%). In addition we could show a good test-retest reliability of TFA of chemosensory induced EEG-power changes in Part III. CONCLUSIONS: Central processing of olfactory stimuli analyzed by TFA reliably distinguishes patients with olfactory impairment from healthy individuals at a high degree of accuracy. Importantly this can be achieved with a simple olfactometer.
[Mh] Termos MeSH primário: Eletroencefalografia/métodos
Transtornos do Olfato/diagnóstico
Olfatometria/métodos
Percepção Olfatória/fisiologia
[Mh] Termos MeSH secundário: Adolescente
Adulto
Idoso
Estudos de Casos e Controles
Sinais (Psicologia)
Cicloexanóis/análise
Eletroencefalografia/instrumentação
Feminino
Voluntários Saudáveis
Seres Humanos
Masculino
Meia-Idade
Monoterpenos/análise
Transtornos do Olfato/fisiopatologia
Olfatometria/instrumentação
Álcool Feniletílico/análise
Sensibilidade e Especificidade
Olfato/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cyclohexanols); 0 (Monoterpenes); ML9LGA7468 (Phenylethyl Alcohol); RV6J6604TK (eucalyptol)
[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:171011
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0185596


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[PMID]:28795803
[Au] Autor:Schubert M; Stichel J; Du Y; Tough IR; Sliwoski G; Meiler J; Cox HM; Weaver CD; Beck-Sickinger AG
[Ad] Endereço:Faculty of Biosciences, Pharmacy and Psychology, Institute of Biochemistry, Leipzig University , Leipzig 04103, Germany.
[Ti] Título:Identification and Characterization of the First Selective Y Receptor Positive Allosteric Modulator.
[So] Source:J Med Chem;60(17):7605-7612, 2017 Sep 14.
[Is] ISSN:1520-4804
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The human Y receptor (Y R) and its cognate ligand, pancreatic polypeptide (PP), are involved in the regulation of energy expenditure, satiety, and food intake. This system represents a potential target for the treatment of metabolic diseases and has been extensively investigated and validated in vivo. Here, we present the compound tBPC (tert-butylphenoxycyclohexanol), a novel and selective Y R positive allosteric modulator that potentiates Y R activation in G-protein signaling and arrestin3 recruitment experiments. The compound has no effect on the binding of the orthosteric ligands, implying its allosteric mode of action at the Y R and evidence for a purely efficacy-driven positive allosteric modulation. Finally, the ability of tBPC to selectively potentiate Y R agonism initiated by PP was confirmed in mouse descending colon mucosa preparations expressing native Y R, demonstrating Y R positive allosteric modulation in vitro.
[Mh] Termos MeSH primário: Regulação Alostérica/efeitos dos fármacos
Cicloexanóis/química
Cicloexanóis/farmacologia
Proteínas de Ligação ao GTP/metabolismo
Receptores de Neuropeptídeo Y/agonistas
Receptores de Neuropeptídeo Y/metabolismo
Transdução de Sinais/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Arrestinas/metabolismo
Células COS
Cercopithecus aethiops
Células HEK293
Seres Humanos
Modelos Moleculares
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Arrestins); 0 (Cyclohexanols); 0 (Receptors, Neuropeptide Y); 0 (arrestin3); 0 (neuropeptide Y4 receptor); EC 3.6.1.- (GTP-Binding Proteins)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170926
[Lr] Data última revisão:
170926
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170811
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jmedchem.7b00976


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[PMID]:28754363
[Au] Autor:Anan K; Masui M; Hara S; Ohara M; Kume M; Yamamoto S; Shinohara S; Tsuji H; Shimada S; Yagi S; Hasebe N; Kai H
[Ad] Endereço:Medicinal Chemistry Research Laboratory, Shionogi & Co Ltd, 1-1 Futabacho, 3-chome, Toyonaka 561-0825, Japan. Electronic address: kousuke.anan@shionogi.co.jp.
[Ti] Título:Discovery of orally bioavailable cyclohexanol-based NR2B-selective NMDA receptor antagonists with analgesic activity utilizing a scaffold hopping approach.
[So] Source:Bioorg Med Chem Lett;27(17):4194-4198, 2017 09 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:NR2B subunit containing N-methyl-d-aspartate (NMDA) receptor is an attractive target for chronic pain due to its involvement in disease states and its limited distribution in the central nervous system. Cyclohexanol-based leads 6a and 6c were identified as potent NR2B-selective NMDA antagonists utilizing a scaffold hopping approach. Further optimization of this series through replacement of the amide in the leads with an isoxazole and efforts to optimize the pharmacokinetic profiles led to the discovery of orally available brain penetrants 7k and 7l, which demonstrated analgesic activity in the mouse formalin test at early and late phases.
[Mh] Termos MeSH primário: Analgésicos/farmacologia
Cicloexanóis/farmacologia
Descoberta de Drogas
Dor/tratamento farmacológico
Receptores de N-Metil-D-Aspartato/antagonistas & inibidores
[Mh] Termos MeSH secundário: Administração Oral
Analgésicos/administração & dosagem
Analgésicos/química
Animais
Encéfalo/metabolismo
Cicloexanóis/administração & dosagem
Cicloexanóis/química
Relação Dose-Resposta a Droga
Formaldeído
Células HEK293
Seres Humanos
Camundongos
Estrutura Molecular
Dor/induzido quimicamente
Ratos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Analgesics); 0 (Cyclohexanols); 0 (NR2B NMDA receptor); 0 (Receptors, N-Methyl-D-Aspartate); 1HG84L3525 (Formaldehyde)
[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:170730
[St] Status:MEDLINE


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[PMID]:28701653
[Au] Autor:Asakawa Y; Ludwiczuk A; Sakurai K; Tomiyama K; Kawakami Y; Yaguchi Y
[Ad] Endereço:Faculty of Pharmaceutical Sciences, Tokushima Bunri University.
[Ti] Título:Comparative Study on Volatile Compounds of Alpinia japonica and Elettaria cardamomum.
[So] Source:J Oleo Sci;66(8):871-876, 2017 Aug 01.
[Is] ISSN:1347-3352
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:The volatile compounds obtained from the ether extracts, headspace gases and steam distillates of Alpinia japonica and Elettaria cardamomum were analyzed by GC/MS. Both species were rich sources of naturally rare fenchane-type monoterpenoids, fenchene, fenchone, fenchyl alcohol and its acetate, together with 1,8-cineole. The distributions of volatile sesquiterpenoids were very poor in both species. Chiralities of fenchone in A. japonica and E. cardamomum were 99% of (1S,4R)-(+)-form. Camphor in A. japonica is composed of a mixture of (1R,4R)-(+)-form (94.3%) and (1S,4S)-(-)-form (5.7%). On the other hand, E. cardamomum produced only (1R,4R)-(+)-camphor (99%).
[Mh] Termos MeSH primário: Alpinia/química
Elettaria/química
Monoterpenos/análise
Extratos Vegetais/química
Sesquiterpenos/análise
Compostos Orgânicos Voláteis/análise
[Mh] Termos MeSH secundário: Cânfora/análise
Cicloexanóis/análise
Éter
Cromatografia Gasosa-Espectrometria de Massas
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cyclohexanols); 0 (Monoterpenes); 0 (Plant Extracts); 0 (Sesquiterpenes); 0 (Volatile Organic Compounds); 0F5N573A2Y (Ether); 76-22-2 (Camphor); RV6J6604TK (eucalyptol)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171010
[Lr] Data última revisão:
171010
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170714
[St] Status:MEDLINE
[do] DOI:10.5650/jos.ess17048


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[PMID]:28533288
[Au] Autor:Hruba L; McMahon LR
[Ad] Endereço:Department of Pharmacology, University of Texas Health Science Center at San Antonio, San Antonio, Texas.
[Ti] Título:Apparent Affinity Estimates and Reversal of the Effects of Synthetic Cannabinoids AM-2201, CP-47,497, JWH-122, and JWH-250 by Rimonabant in Rhesus Monkeys.
[So] Source:J Pharmacol Exp Ther;362(2):278-286, 2017 Aug.
[Is] ISSN:1521-0103
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Synthetic cannabinoids have been prohibited due to abuse liability and toxicity. Four such synthetic cannabinoids, AM-2201 ([1-(5-fluoropentyl)indol-3-yl]-naphthalen-1-ylmethanone), CP-47,497 (2-[(1R,3S)-3-hydroxycyclohexyl]-5-(2-methyloctan-2-yl)phenol), JWH-122 [(4-methylnaphthalen-1-yl)-(1-pentylindol-3-yl)methanone], and JWH-250 [2-(2-methoxyphenyl)-1-(1-pentylindol-3-yl)ethanone], were tested for their capacity to produce CB receptor-mediated discriminative stimulus effects in two groups of rhesus monkeys. One group ( = 4) discriminated Δ -tetrahydrocannabinol (∆ -THC; 0.1 mg/kg i.v.), and a second group ( = 4) discriminated the cannabinoid antagonist rimonabant (1 mg/kg i.v.) while receiving 1 mg/kg/12 hours of ∆ -THC. AM-2201, JWH-122, CP-47,497, JWH-250, and ∆ -THC increased ∆ -THC lever responding. Duration of action was 1-2 hours for AM-2201, JWH-122, and JWH-250 and 4-5 hours for CP-47,497 and ∆ -THC. Rimonabant (1 mg/kg) surmountably antagonized the discriminative stimulus effects of all cannabinoid agonists; the magnitude of rightward shift was 10.6-fold for AM-2201, 10.7-fold for JWH-122, 11.0-fold for CP-47,497, and 15.7-fold for JWH-250. The respective pK values were not significantly different: 6.61, 6.65, 6.66, and 6.83. In ∆ -THC-treated monkeys discriminating rimonabant, AM-2201 (0.1 and 0.32 mg/kg), JWH-122 (0.32 and 1 mg/kg), JWH-250 (1 and 3.2 mg/kg), and CP-47,497 (0.32, 1, and 3.2 mg/kg) produced not only rate-decreasing effects that were reversed by rimonabant, but also dose-dependent, rightward shifts in the rimonabant discrimination dose-effect function. These results show striking similarity in the CB receptor mechanism mediating the subjective effects of AM-2201, JWH-122, JWH-250, and CP-47,497. For products containing AM-2201 and JWH-122, a short duration of action could lead to more frequent use; moreover, inattention to differences in potency among synthetic cannabinoids could underlie unexpected toxicity. Rapid reversal of effects by intravenous rimonabant has potential value in emergency situations.
[Mh] Termos MeSH primário: Antagonistas de Receptores de Canabinoides/metabolismo
Canabinoides/metabolismo
Cicloexanóis/metabolismo
Indóis/metabolismo
Naftalenos/metabolismo
Piperidinas/metabolismo
Pirazóis/metabolismo
[Mh] Termos MeSH secundário: Animais
Antagonistas de Receptores de Canabinoides/farmacologia
Canabinoides/farmacologia
Cicloexanóis/farmacologia
Aprendizagem por Discriminação/efeitos dos fármacos
Aprendizagem por Discriminação/fisiologia
Relação Dose-Resposta a Droga
Feminino
Indóis/farmacologia
Macaca mulatta
Masculino
Naftalenos/farmacologia
Piperidinas/farmacologia
Pirazóis/farmacologia
Receptor CB1 de Canabinoide/agonistas
Receptor CB1 de Canabinoide/antagonistas & inibidores
Receptor CB1 de Canabinoide/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 ((4-methyl-1-naphthyl)-(1-pentylindol-3-yl)methanone); 0 (1-((5-fluoropentyl)-1H-indol-3-yl)-(naphthalen-1-yl)methanone); 0 (Cannabinoid Receptor Antagonists); 0 (Cannabinoids); 0 (Cyclohexanols); 0 (Indoles); 0 (Naphthalenes); 0 (Piperidines); 0 (Pyrazoles); 0 (Receptor, Cannabinoid, CB1); 70434-82-1 (CP 47497); RML78EN3XE (rimonabant)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170802
[Lr] Data última revisão:
170802
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170524
[St] Status:MEDLINE
[do] DOI:10.1124/jpet.117.240572


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[PMID]:28514947
[Au] Autor:Casey AL; Karpanen TJ; Conway BR; Worthington T; Nightingale P; Waters R; Elliott TSJ
[Ad] Endereço:Department of Clinical Microbiology, University Hospitals Birmingham NHS Foundation Trust, Edgbaston, B15 2WB, Birmingham, UK.
[Ti] Título:Enhanced chlorhexidine skin penetration with 1,8-cineole.
[So] Source:BMC Infect Dis;17(1):350, 2017 May 17.
[Is] ISSN:1471-2334
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Chlorhexidine (CHG) penetrates poorly into skin. The purpose of this study was to compare the depth of CHG skin permeation from solutions containing either 2% (w/v) CHG and 70% (v/v) isopropyl alcohol (IPA) or 2% (w/v) CHG, 70% (v/v) IPA and 2% (v/v) 1,8-cineole. METHODS: An ex-vivo study using Franz diffusion cells was carried out. Full thickness human skin was mounted onto the cells and a CHG solution, with or without 2% (v/v) 1,8-cineole was applied to the skin surface. After twenty-four hours the skin was sectioned horizontally in 100 µm slices to a depth of 2000 µm and the concentration of CHG in each section quantified using high performance liquid chromatography (HPLC). The data were analysed with repeated measures analysis of variance. RESULTS: The concentration of CHG in the skin on average was significantly higher (33.3% [95%, CI 1.5% - 74.9%]) when a CHG solution which contained 1,8-cineole was applied to the skin compared to a CHG solution which did not contain this terpene (P = 0.042). CONCLUSIONS: Enhanced delivery of CHG can be achieved in the presence of 1,8-cineole, which is the major component of eucalyptus oil. This may reduce the numbers of microorganisms located in the deeper layers of the skin which potentially could decrease the risk of surgical site infection.
[Mh] Termos MeSH primário: Clorexidina/farmacocinética
Cicloexanóis/farmacocinética
Monoterpenos/farmacocinética
Absorção Cutânea/efeitos dos fármacos
[Mh] Termos MeSH secundário: 2-Propanol/administração & dosagem
2-Propanol/química
Anti-Infecciosos Locais/administração & dosagem
Anti-Infecciosos Locais/farmacocinética
Clorexidina/administração & dosagem
Clorexidina/química
Cicloexanóis/administração & dosagem
Cicloexanóis/química
Feminino
Seres Humanos
Meia-Idade
Monoterpenos/administração & dosagem
Monoterpenos/química
Soluções/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Infective Agents, Local); 0 (Cyclohexanols); 0 (Monoterpenes); 0 (Solutions); ND2M416302 (2-Propanol); R4KO0DY52L (Chlorhexidine); RV6J6604TK (eucalyptol)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170818
[Lr] Data última revisão:
170818
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170519
[St] Status:MEDLINE
[do] DOI:10.1186/s12879-017-2451-4


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[PMID]:28477412
[Au] Autor:Cutillas AB; Carrasco A; Martinez-Gutierrez R; Tomas V; Tudela J
[Ad] Endereço:GENZ-Group of Research on Enzymology (www.um.es/genz), Department of Biochemistry and Molecular Biology-A, Regional Campus of International Excellence 'Campus Mare Nostrum', University of Murcia, 30100, Murcia, Spain.
[Ti] Título:Salvia officinalis L. Essential Oils from Spain: Determination of Composition, Antioxidant Capacity, Antienzymatic, and Antimicrobial Bioactivities.
[So] Source:Chem Biodivers;14(8), 2017 Aug.
[Is] ISSN:1612-1880
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Four essential oils (EOs) from Salvia officinalis L. cultivated in Spain (Murcia Province) were analyzed by gas chromatography coupled with mass spectrometry (GC/MS) to determine their relative and absolute compositions. The main components were α-thujone (22.8 - 41.7%), camphor (10.7 - 19.8%), 1,8-cineole (4.7 - 15.6%), and ß-thujone (6.1 - 15.6%). Enantioselective gas chromatography identified (-)-α-thujone and (+)-camphor as the main enantiomers in all the analyzed EOs. Furthermore, when the EOs were tested to determine their antioxidant activity against free radicals and as ferric reducing and ferrous chelating agents, all were seen to have moderate activity due to the compounds they contained, such as linalool or terpinene. Because of their known relation with inflammatory illnesses and Alzheimer's disease, respectively, the inhibition of lipoxygenase and acetylcholinesterase was studied using the EOs. Some individual compounds also inhibited these enzymes. In addition, the studied EOs were able to inhibit the growth of Escherichia coli, Staphylococcus aureus, and Candida albicans. The characterization carried out increases our awareness of the possible uses of S. officinalis EO as natural additives in food, cosmetics, and pharmaceuticals.
[Mh] Termos MeSH primário: Óleos Voláteis/química
Salvia officinalis/química
[Mh] Termos MeSH secundário: Acetilcolinesterase/química
Acetilcolinesterase/metabolismo
Anti-Infecciosos/química
Anti-Infecciosos/isolamento & purificação
Anti-Infecciosos/farmacologia
Antioxidantes/química
Candida albicans/efeitos dos fármacos
Análise por Conglomerados
Cicloexanóis/análise
Escherichia coli/efeitos dos fármacos
Cromatografia Gasosa-Espectrometria de Massas
Concentração Inibidora 50
Lipoxigenase/química
Lipoxigenase/metabolismo
Monoterpenos/análise
Óleos Voláteis/análise
Óleos Voláteis/metabolismo
Análise de Componente Principal
Ligação Proteica
Salvia officinalis/metabolismo
Espanha
Staphylococcus aureus/efeitos dos fármacos
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Infective Agents); 0 (Antioxidants); 0 (Cyclohexanols); 0 (Monoterpenes); 0 (Oils, Volatile); 8ZI5R3T54Q (beta-thujone); D81QY6I88E (linalool); EC 1.13.11.12 (Lipoxygenase); EC 3.1.1.7 (Acetylcholinesterase); RV6J6604TK (eucalyptol)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170507
[St] Status:MEDLINE
[do] DOI:10.1002/cbdv.201700102


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[PMID]:28411115
[Au] Autor:Andersen RJ
[Ad] Endereço:Departments of Chemistry and Earth, Ocean & Atmospheric Sciences, University of British Columbia, 2036 Main Mall, Vancouver, British Columbia V6T 1Z1, Canada. Electronic address: raymond.andersen@ubc.ca.
[Ti] Título:Sponging off nature for new drug leads.
[So] Source:Biochem Pharmacol;139:3-14, 2017 Sep 01.
[Is] ISSN:1873-2968
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Marine sponges have consistently been the richest source of new marine natural products with unprecedented chemical scaffolds and potent biological activities that have been reported in the chemical literature since the early 1970s. During the last 40years, chemists in the Andersen laboratory at UBC, in collaboration with biologists, have discovered many novel bioactive sponge natural products. Four experimental drug candidates for treatment of inflammation and cancer, that were inspired by members of this sponge natural product collection, have progressed to phase I/II/III clinical trials. This review recounts the scientific stories behind the discovery and development of these four drug candidates; IPL576,092, HTI-286 (Taltobulin), EPI-506 (Ralaniten acetate), and AQX-1125.
[Mh] Termos MeSH primário: Organismos Aquáticos/química
Produtos Biológicos/química
Desenho de Drogas
Descoberta de Drogas
Drogas em Investigação/química
Poríferos/química
[Mh] Termos MeSH secundário: Animais
Antiasmáticos/efeitos adversos
Antiasmáticos/química
Antiasmáticos/farmacologia
Antiasmáticos/uso terapêutico
Anti-Inflamatórios não Esteroides/efeitos adversos
Anti-Inflamatórios não Esteroides/química
Anti-Inflamatórios não Esteroides/uso terapêutico
Antimitóticos/efeitos adversos
Antimitóticos/química
Antimitóticos/farmacologia
Antimitóticos/uso terapêutico
Antineoplásicos/efeitos adversos
Antineoplásicos/química
Antineoplásicos/farmacologia
Antineoplásicos/uso terapêutico
Compostos Benzidrílicos/efeitos adversos
Compostos Benzidrílicos/química
Compostos Benzidrílicos/farmacologia
Compostos Benzidrílicos/uso terapêutico
Produtos Biológicos/isolamento & purificação
Cicloexanóis/efeitos adversos
Cicloexanóis/química
Cicloexanóis/uso terapêutico
Drogas em Investigação/efeitos adversos
Drogas em Investigação/farmacologia
Drogas em Investigação/uso terapêutico
Glicerol/análogos & derivados
Glicerol/farmacologia
Glicerol/uso terapêutico
Seres Humanos
Indanos/efeitos adversos
Indanos/química
Indanos/uso terapêutico
Antiandrógenos não Esteroides/efeitos adversos
Antiandrógenos não Esteroides/química
Antiandrógenos não Esteroides/farmacologia
Antiandrógenos não Esteroides/uso terapêutico
Oligopeptídeos/efeitos adversos
Oligopeptídeos/química
Oligopeptídeos/farmacologia
Oligopeptídeos/uso terapêutico
Pró-Fármacos/efeitos adversos
Pró-Fármacos/química
Pró-Fármacos/farmacologia
Pró-Fármacos/uso terapêutico
Pirrolidinonas/efeitos adversos
Pirrolidinonas/química
Pirrolidinonas/isolamento & purificação
Pirrolidinonas/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (4-(4-(aminomethyl)-7a-methyl-1-methylideneoctahydro-1H-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexan-1-ol); 0 (Anti-Asthmatic Agents); 0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Antimitotic Agents); 0 (Antineoplastic Agents); 0 (Benzhydryl Compounds); 0 (Biological Products); 0 (Cyclohexanols); 0 (Drugs, Investigational); 0 (HTI-286); 0 (IPL576,092); 0 (Indans); 0 (Nonsteroidal Anti-Androgens); 0 (Oligopeptides); 0 (Prodrugs); 0 (Pyrrolidinones); 0 (Sterols); PDC6A3C0OX (Glycerol)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170818
[Lr] Data última revisão:
170818
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170416
[St] Status:MEDLINE


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[PMID]:28381767
[Au] Autor:Kunihiro K; Myoda T; Tajima N; Gotoh K; Kaneshima T; Someya T; Toeda K; Fujimori T; Nishizawa M
[Ad] Endereço:Department of Food and Cosmetic Science, Tokyo University of Agriculture.
[Ti] Título:Volatile Components of the Essential Oil of Artemisia montana and Their Sedative Effects.
[So] Source:J Oleo Sci;66(8):843-849, 2017 Aug 01.
[Is] ISSN:1347-3352
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:The sedative effects of volatile components in the essential oil of Artemisia montana ("Yomogi") were investigated and measured using gas chromatography-mass spectrometry (GC-MS). Major components identified included 1,8-cineol, camphor, borneol, α-piperitone, and caryophyllene oxide. Among them, 1,8-cineol exhibited the highest flavor dilution (FD) value in an aroma extract dilution analysis (AEDA), followed by borneol, o-cymene, ß-thujone, and bornyl acetate. The sedative effects of yomogi oil aroma were evaluated by sensory testing, analysis of salivary α-amylase activity, and measurement of relative fluctuation of oxygenated hemoglobin concentration in the brain using near-infrared spectroscopy (NIRS). All results indicated the stress-reducing effects of the essential oil following nasal exposure, and according to the NIRS analysis, 1,8-cineol is likely responsible for the sedative effects of yomogi oil.
[Mh] Termos MeSH primário: Aromaterapia
Artemia/química
Cicloexanóis/farmacologia
Hipnóticos e Sedativos/farmacologia
Monoterpenos/farmacologia
Óleos Voláteis/química
Fitoterapia
Óleos Vegetais/química
Estresse Psicológico/prevenção & controle
[Mh] Termos MeSH secundário: Administração Intranasal
Adulto
Animais
Encéfalo/metabolismo
Cicloexanóis/administração & dosagem
Cicloexanóis/isolamento & purificação
Feminino
Cromatografia Gasosa-Espectrometria de Massas
Hemoglobinas/metabolismo
Seres Humanos
Hipnóticos e Sedativos/isolamento & purificação
Masculino
Monoterpenos/administração & dosagem
Monoterpenos/isolamento & purificação
Saliva/enzimologia
Espectroscopia de Luz Próxima ao Infravermelho
Volatilização
Adulto Jovem
alfa-Amilases/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cyclohexanols); 0 (Hemoglobins); 0 (Hypnotics and Sedatives); 0 (Monoterpenes); 0 (Oils, Volatile); 0 (Plant Oils); EC 3.2.1.1 (alpha-Amylases); RV6J6604TK (eucalyptol)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171010
[Lr] Data última revisão:
171010
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170407
[St] Status:MEDLINE
[do] DOI:10.5650/jos.ess16006



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