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2.
Int J Mol Sci ; 21(7)2020 Apr 08.
Artigo em Inglês | MEDLINE | ID: mdl-32276406

RESUMO

Ramelteon is a Melatonin 1 (MT1)-and Melatonin 2 (MT2)-receptor agonist conferring cardioprotection by pharmacologic preconditioning. While activation of mitochondrial calcium-sensitive potassium (mKCa)-channels is involved in this protective mechanism, the specific upstream signaling pathway of Ramelteon-induced cardioprotection is unknown. In the present study, we (1) investigated whether Ramelteon-induced cardioprotection involves activation of protein kinase G (PKG) and/or protein kinase B (Akt) and (2) determined the precise sequence of PKG and Akt in the signal transduction pathway of Ramelteon-induced preconditioning. Hearts of male Wistar rats were randomized and placed on a Langendorff system, perfused with Krebs-Henseleit buffer at a constant pressure of 80 mmHg. All hearts were subjected to 33 min of global ischemia and 60 min of reperfusion. Before ischemia, hearts were perfused with Ramelteon (Ram) with or without the PKG or Akt inhibitor KT5823 and MK2206, respectively (KT5823 + Ram, KT5823, MK2206 + Ram, MK2206). To determine the precise signaling sequence, subsequent experiments were conducted with the guanylate cyclase activator BAY60-2770 and the mKCa-channel activator NS1619. Infarct size was determined by 2,3,5-triphenyltetrazolium chloride (TTC) staining. Ramelteon-induced infarct size reduction was completely blocked by KT5823 (p = 0.0012) and MK2206 (p = 0.0005). MK2206 with Ramelteon combined with BAY60-2770 reduced infarct size significantly (p = 0.0014) indicating that PKG activation takes place after Akt. Ramelteon and KT5823 (p = 0.0063) or MK2206 (p = 0.006) respectively combined with NS1619 also significantly reduced infarct size, indicating that PKG and Akt are located upstream of mKCa-channels. This study shows for the first time that Ramelteon-induced preconditioning (1) involves activation of PKG and Akt; (2) PKG is located downstream of Akt and (3) both enzymes are located upstream of mKCa-channels in the signal transduction pathway.


Assuntos
Proteínas Quinases Dependentes de GMP Cíclico/metabolismo , Coração/efeitos dos fármacos , Indenos/farmacologia , Precondicionamento Isquêmico Miocárdico , Proteínas Proto-Oncogênicas c-akt/metabolismo , Animais , Cardiotônicos/farmacologia , Masculino , Infarto do Miocárdio , Miocárdio/metabolismo , Ratos , Ratos Wistar , Transdução de Sinais
3.
Pest Manag Sci ; 76(6): 2049-2057, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31943704

RESUMO

BACKGROUND: Indaziflam is an alkylazine herbicide used to control annual bluegrass (Poa annua L.). Several locations in the southeastern USA reported poor annual bluegrass control following treatment with indaziflam during autumn 2015. A series of controlled environment experiments were conducted to confirm putative resistance to indaziflam in annual bluegrass collected from these field locations. RESULTS: Indaziflam (25 g ha-1 ) effectively controlled all putative-resistant annual bluegrass collections when applied preemergence (PRE), but was ineffective when applied early-postemergence (< 2.5 cm plant height; BBCH scale = 1; EPOST). In agarose-based plate assays, EPOST I50 values for putative-resistant collections ranged from 2424 to 4305 pm compared with 633 pm for the herbicide-susceptible control; therefore, resistance indexes (R/S) ranged from 3.8 to 6.8. Resistant collections were not controlled by foramsulfuron, flumioxazin, glyphosate, glufosinate, metribuzin, pronamide, or simazine applied EPOST. Indaziflam content in herbicide-susceptible annual bluegrass was greater than a resistant collection from 0 to 10 days after treatment (DAT). Susceptibility was not restored when resistant collections were treated with indaziflam plus 1-aminobenzotriazole (10 mg L-1 ), tebuconazole (1510 g ha-1 ), or malathion (400 g ha-1 ). CONCLUSIONS: This is a first report of resistance to indaziflam in any plant. Additionally, we confirm that these annual bluegrass collections are resistant to several other herbicidal modes-of-action. It is unclear if this multi-herbicide resistance is due to a single resistance gene, multiple resistance genes, non-target site mechanisms, or a combination thereof. Additional research to better understand resistance mechanisms in these annual bluegrass collections is warranted. © 2020 Society of Chemical Industry.


Assuntos
Poa , Herbicidas , Indenos , Triazinas
4.
FASEB J ; 34(1): 1576-1590, 2020 01.
Artigo em Inglês | MEDLINE | ID: mdl-31914614

RESUMO

Inflammatory bowel diseases (IBDs) are characterized by an inflammatory and oxidative stress condition in the intestinal tissue. In this study, we evaluated the effect of plumericin, one of the main bioactive components of Himatanthus sucuuba (Woodson) bark, on intestinal inflammation and oxidative stress, both in vitro and in vivo. The effect of plumericin (0.5-2 µM) in vitro was evaluated in rat intestinal epithelial cells (IEC-6) treated with lipopolysaccharides from E. coli (10 µg/mL) plus interferon-γ (10 U/mL). Moreover, a 2,4,6-dinitrobenzene sulfonic acid (DNBS)-induced colitis model was used to evaluate the anti-inflammatory and antioxidant activity of plumericin (3 mg/kg) in vivo. The results showed that plumericin significantly reduces intestinal inflammatory factors such as tumor necrosis factor-α, cyclooxygenase-2 and inducible nitric oxide synthase expression, and nitrotyrosine formation. Plumericin also inhibited nuclear factor-κB translocation, reactive oxygen species (ROS) release, and inflammasome activation. Moreover, plumericin activated the nuclear factor erythroid-derived 2 pathway in IEC-6. Using the DNBS-induced colitis model, a significant reduction in the weight loss and in the development of the macroscopic and histologic signs of colon injury, together with a reduced inflammatory and oxidative stress state, were observed in plumericin-treated mice. These results indicate that plumericin exerts a strong anti-inflammatory and antioxidant activity. Thus, it might be a candidate for the development of a new pharmacologic approach for IBDs treatment.


Assuntos
Anti-Inflamatórios/farmacologia , Colo/efeitos dos fármacos , Indenos/farmacologia , Inflamação/tratamento farmacológico , Iridoides/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Animais , Linhagem Celular , Colite/tratamento farmacológico , Colite/metabolismo , Colo/metabolismo , Ciclo-Oxigenase 2/metabolismo , Inflamação/metabolismo , Doenças Inflamatórias Intestinais/tratamento farmacológico , Doenças Inflamatórias Intestinais/metabolismo , Mucosa Intestinal/efeitos dos fármacos , Mucosa Intestinal/metabolismo , Masculino , Camundongos , NF-kappa B/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Ratos , Espécies Reativas de Oxigênio/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
5.
Planta ; 251(2): 43, 2020 Jan 06.
Artigo em Inglês | MEDLINE | ID: mdl-31907627

RESUMO

MAIN CONCLUSION: Co-expression and regulatory networks yield important insights into the growth-defense tradeoffs mechanism under jasmonic acid (JA) signals in Arabidopsis. Elevated defense is commonly associated with growth inhibition. However, a comprehensive atlas of the genes associated with the plant growth-defense tradeoffs under JA signaling is lacking. To gain an insight into the dynamic architecture of growth-defense tradeoffs, a coexpression network analysis was employed on publicly available high-resolution transcriptomes of Arabidopsis treated with coronatine (COR), a mimic of jasmonoyl-l-isoleucine. The genes involved in JA-mediated growth-defense tradeoffs were systematically revealed. Promoter enrichment analysis revealed the core regulatory module in which the genes underwent rapid activation, sustained upregulation after COR treatment, and mediated the growth-defense tradeoffs. Several transcription factors (TFs), including RAP2.6L, MYB44, WRKY40, and WRKY18, were identified as instantly activated components associated with pathogen and insect resistance. JA might rapidly activate RAV1 and KAN1 to repress brassinosteroid (BR) response genes, upregulate KAN1, the C2H2 TF families ZF2, ZF3, ZAT6, and STZ/ZAT10 to repress the biosynthesis, transport, and signaling of auxin to arrest growth. Independent datasets and preserved analyses validated the reproducibility of the results. Our study provided a comprehensive snapshot of genes that respond to JA signals and provided valuable resources for functional studies on the genetic modification of breeding population that exhibit robust growth and defense simultaneously.


Assuntos
Arabidopsis/metabolismo , Ciclopentanos/metabolismo , Oxilipinas/metabolismo , Aminoácidos/farmacologia , Arabidopsis/efeitos dos fármacos , Proteínas de Arabidopsis/genética , Proteínas de Arabidopsis/metabolismo , Regulação da Expressão Gênica de Plantas/efeitos dos fármacos , Regulação da Expressão Gênica de Plantas/genética , Indenos/farmacologia , Transdução de Sinais/efeitos dos fármacos , Transdução de Sinais/genética , Fatores de Transcrição/genética , Fatores de Transcrição/metabolismo
6.
J Pharmacol Sci ; 142(2): 79-82, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31864840

RESUMO

We investigated the effects of sleep-inducing agents with different mechanisms of action on the loss of the righting reflex induced by isoflurane or a mixture of medetomidine, midazolam, and butorphanol (MMB), followed by atipamezole reversal. Chlorpromazine and brotizolam delayed recovery from both types of anesthesia, whereas the melatonin receptor agonist ramelteon had no effect. The orexin receptor antagonist suvorexant delayed recovery from anesthesia only in the case of MMB, while the sleep-promoting supplement glycine only delayed recovery in the case of isoflurane. These results suggest that the simple comparison method is applicable for testing substances expected to exert sleep-inducing effects.


Assuntos
Anestésicos/farmacologia , Medicamentos Indutores do Sono/farmacologia , Anestesia/métodos , Animais , Azepinas/metabolismo , Butorfanol/farmacologia , Clorpromazina/metabolismo , Combinação de Medicamentos , Imidazóis/farmacologia , Indenos/metabolismo , Isoflurano/farmacologia , Masculino , Medetomidina/farmacologia , Camundongos , Camundongos Endogâmicos ICR , Midazolam/farmacologia , Antagonistas dos Receptores de Orexina/metabolismo , Triazóis/metabolismo
7.
J Clin Psychiatry ; 81(1)2019 12 17.
Artigo em Inglês | MEDLINE | ID: mdl-31851436

RESUMO

OBJECTIVE: The aim of this study was to examine the effectiveness of ramelteon and suvorexant for delirium prevention in real-world practice. It explored whether ramelteon and/or suvorexant would affect delirium prevention among both patients at risk for but without delirium (patients at risk) and those with delirium the night before a consultation. METHODS: This multicenter, prospective, observational study was conducted by trained psychiatrists at consultation-liaison psychiatric services from October 1, 2017, to October 7, 2018. Patients who were aged 65 years or older and hospitalized because of acute diseases or elective surgery, had risk factors for delirium, and had insomnia or delirium on the night before the consultation were prescribed ramelteon and/or suvorexant. The decision to take medication was left to the discretion of each patient. The primary outcome was incidence of delirium based on the Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition, during the first 7 days. RESULTS: Among 526 patients at risk, those taking ramelteon and/or suvorexant developed delirium significantly less frequently than those who did not, after control for the effects of risk factors on the estimate of an independent association between the effects of ramelteon and/or suvorexant and the outcome of developing delirium (15.7% vs 24.0%; odds ratio [OR] = 0.48;, 95% CI, 0.29-0.80; P = .005). Similar results were found among 422 patients with delirium (39.9% vs 66.3%; OR = 0.36; 95% CI, 0.22-0.59; P < .0001). CONCLUSIONS: Ramelteon and suvorexant appear to be effective for delirium prevention in real-world practice.


Assuntos
Azepinas/uso terapêutico , Delírio/prevenção & controle , Indenos/uso terapêutico , Medicamentos Indutores do Sono/uso terapêutico , Triazóis/uso terapêutico , Idoso , Delírio/etiologia , Feminino , Hospitalização , Humanos , Estimativa de Kaplan-Meier , Masculino , Estudos Prospectivos , Fatores de Risco , Resultado do Tratamento
8.
Tunis Med ; 97(3): 432-437, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31729717

RESUMO

BACKGROUND: Atrial fibrillation is the most common heart rhythm disorder in the general population. It is associated with increased cardiovascular morbidity and mortality. Given this risk, anticoagulant therapy is vital. AIM: To estimate the incidence of thromboembolic and hemorrhagic events in patients with Atrial fibrillation and treated by oral anticoagulant in a cardiology department. METHODS: We carried out an observational longitudinal study over a period of three years (January 2013 - December 2015) in the external consultation of cardiology of Farhat Hached hospital of Sousse. Pre-established individual records were used as a source and tool for data collection. RESULTS: Overall, 200 patients were eligible. Forty-nine percent had valvular atrial fibrillation. After an average follow-up of 2.6 years, 15 thromboembolic events were noted affecting 13 patients (6.5%), with an incidence of 2.8%. We found a significant association between TTR <50% and the occurrence of stroke and transient ischemic events. Half of the patients had minor bleeding and 9.5% had major bleeding, with an incidence of 3.6%. No significant correlation between these accidents and the TTR was found. In addition, 9.5% of patients were hospitalized for international normalized ratio equilibration. They were mainly patients with valvular atrial fibrillation (72%) (p = 0.002). CONCLUSION: Anticoagulant therapy with anti-vitamin-K remains the most adequate treatment. Thus, a well-conducted treatment ensures a reduction in thromboembolic risk and minimizes the occurrence of hemorrhages inherent to this therapy. Therefore, an assessment of the quality of anticoagulation is essential.


Assuntos
4-Hidroxicumarinas/uso terapêutico , Fibrilação Atrial/tratamento farmacológico , Fibrilação Atrial/epidemiologia , Hemorragia/epidemiologia , Indenos/uso terapêutico , Tromboembolia/epidemiologia , Vitamina K/antagonistas & inibidores , Adulto , Idoso , Idoso de 80 Anos ou mais , Anticoagulantes/uso terapêutico , Feminino , Hemorragia/induzido quimicamente , Humanos , Incidência , Estudos Longitudinais , Masculino , Pessoa de Meia-Idade , Fatores de Risco , Acidente Vascular Cerebral/epidemiologia , Tromboembolia/prevenção & controle , Tunísia/epidemiologia , Vitamina K/uso terapêutico
10.
Tunis Med ; 97(1): 113-121, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31535702

RESUMO

INTRODUCTION:   The quality of chronic anticoagulation and predictor factors of poor anticoagulant control in patients under acenocoumarol were unknown in North Africa. METHODS: It is an observational study, carried out between November 2015 and November 30, 2016. The international normalized ratio (INR) values were prospectively obtained, and TTR was calculated using the Rosendaal method. RESULTS: Overall, 215 patients were included in this study, with a mean age of 63±0,8 years. The prevalence of poor anticoagulation control was 78.1%; 95% CI [72.2-83.2] (168 patients with TTR less than 65%). The median TTR with the Rosendaal method was 44.4%. After multivariate adjustment, variables significantly associated with adequate anticoagulation level were: history of ischemic stroke (Adjusted OR equal to 4.3, 95% CI: 1.4-12.9), associated prescription of antiplatelet therapy (Adjusted OR equal to 3.5, 95% CI: 1.1-11.2), daily prescribed dose of coumarins less than 6 mg (Adjusted OR equal to 6.4, 95% CI: 1.1- 36) and lower risk of bleeding assessed as HAS-BLED score (Adjusted OR: 0.5, 95% CI: 0.3-0.8). CONCLUSION: The quality of anticoagulation management with VKA among outpatients who received acenocoumarol was suboptimal. Strategies should be undertaken by clinicians and patients to improve the quality of anticoagulation, to address challenges to adverse cardiovascular outcomes in individuals treated with chronic anticoagulation.


Assuntos
4-Hidroxicumarinas/administração & dosagem , 4-Hidroxicumarinas/farmacocinética , Indenos/administração & dosagem , Indenos/farmacocinética , Adesão à Medicação/estatística & dados numéricos , Vitamina K/antagonistas & inibidores , Administração Oral , Adulto , Idoso , Idoso de 80 Anos ou mais , Anticoagulantes/administração & dosagem , Anticoagulantes/farmacocinética , Fibrilação Atrial/tratamento farmacológico , Fibrilação Atrial/epidemiologia , Fibrilação Atrial/metabolismo , Doenças Cardiovasculares/tratamento farmacológico , Doenças Cardiovasculares/epidemiologia , Doenças Cardiovasculares/metabolismo , Monitoramento de Medicamentos/estatística & dados numéricos , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Pacientes Ambulatoriais/estatística & dados numéricos , Prevalência , Fatores Socioeconômicos , Tromboembolia/tratamento farmacológico , Tromboembolia/epidemiologia , Tromboembolia/metabolismo , Fatores de Tempo , Resultado do Tratamento , Tunísia/epidemiologia , Vitamina K/administração & dosagem , Vitamina K/farmacocinética
12.
J Agric Food Chem ; 67(37): 10498-10504, 2019 Sep 18.
Artigo em Inglês | MEDLINE | ID: mdl-31452369

RESUMO

Owing to the changing needs of agriculture, the exploration of new pest control agents remains as critical as ever. The analogues 3a-3v of the natural product cerbinal were synthesized from genipin by an efficient and practical method under additive-free conditions. The antiviral and insecticidal effects of cerbinal and these cyclopenta[c]pyridines (3a-3v) were evaluated systematically. Most of the synthesized compounds exhibited higher anti-TMV activities than the lead compound cerbinal. Compound 3s (2-(4-methoxyphenyl)) had the most promising inhibitory activities against TMV (inactivation effect 49.0 ± 0.8%, curative effect 41.2 ± 4.3%, and protection effect 51.5 ± 2.7% at 500 µg/mL). Among the synthesized compounds, only 3v (2-(2-chloro-4-(trifluoromethoxy)phenyl)) reached the activity level of cerbinal against Plutella xylostella. This suggested that the cyclopenta[c]pyridines obtained by modifications of cerbinal at position 2 are very significant for the anti-TMV activity, and yet were exceptionally less active for the insecticidal activities.


Assuntos
Antivirais/síntese química , Antivirais/farmacologia , Produtos Biológicos/síntese química , Produtos Biológicos/farmacologia , Indenos/química , Indenos/farmacologia , Inseticidas/química , Inseticidas/farmacologia , Animais , Antivirais/química , Produtos Biológicos/química , Descoberta de Drogas , Indenos/síntese química , Inseticidas/síntese química , Iridoides/química , Estrutura Molecular , Mariposas/efeitos dos fármacos , Mariposas/crescimento & desenvolvimento , Piridinas/síntese química , Piridinas/química , Piridinas/farmacologia , Relação Estrutura-Atividade , Vírus do Mosaico do Tabaco/efeitos dos fármacos , Vírus do Mosaico do Tabaco/crescimento & desenvolvimento
14.
J Sep Sci ; 42(19): 3141-3151, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31376226

RESUMO

A simple and efficient multiresidue method using dispersive solid phase extraction and liquid chromatography coupled with tandem mass spectrometry was developed for the targeted analysis of indaziflam and its five metabolites (indaziflam-diaminotriazine, indaziflam-carboxylic acid, indaziflam-triazine indanone, indaziflam-hydroxyethyl, and indaziflam-olefin) in pitaya samples (including roots, plants, flowers, peels, pulp, and whole fruit). The analytes were extracted with acetonitrile, and the extracts were purified using multiwalled carbon nanotubes. The method was validated using pitaya samples spiked at 0.5, 5, and 50 µg/kg, and the average recoveries varied from 61.1 to 103.7% with relative standard deviations lower than 12.7% (n = 5). This method exhibited sufficient linearity within the concentration range of 0.1-100 µg/L. The limits of detection and quantification were in the ranges of 0.001-0.1 and 0.003-0.3 µg/kg, respectively. The method was successfully applied to analyze pitaya samples in Nanning, and no indaziflam or its metabolites were detected in the samples analyzed.


Assuntos
Cactaceae/química , Indenos/análise , Extração em Fase Sólida , Triazinas/análise , Cromatografia Líquida de Alta Pressão , Frutas/química , Frutas/metabolismo , Indenos/metabolismo , Espectrometria de Massas em Tandem , Triazinas/metabolismo
15.
Chirality ; 31(11): 958-967, 2019 11.
Artigo em Inglês | MEDLINE | ID: mdl-31468608

RESUMO

In this study, a newly isolated strain screened from the indoxacarb-rich agricultural soils, Bacillus cereus WZZ006, has a high stereoselectivity to racemic substrate 5-chloro-1-oxo-2,3-dihydro-2-hydroxy-1H-indene-2-carboxylic acid methyl ester. (S)-5-chloro-1-oxo-2,3-dihydro-2-hydroxy-1H-indene-2-carboxylic acid methyl ester was obtained by bio-enzymatic resolution. After the 36-hour hydrolysis in 50-mM racemic substrate under the optimized reaction conditions, the e.e.s was up to 93.0% and the conversion was nearly 53.0% with the E being 35.0. Therefore, B cereus WZZ006 performed high-level ability to produce (S)-5-chloro-1-oxo-2,3-dihydro-2-hydroxy-1H-indene-2-carboxylic acid methyl ester. This study demonstrates a new biocatalytic process route for preparing the indoxacarb chiral intermediates and provides a theoretical basis for the application of new insecticides in agricultural production.


Assuntos
Bacillus cereus/citologia , Bacillus cereus/metabolismo , Biocatálise , Indenos/metabolismo , Oxazinas/metabolismo , Bacillus cereus/enzimologia , Hidrolases de Éster Carboxílico/metabolismo , Concentração de Íons de Hidrogênio , Hidrólise , Indenos/química , Cinética , Rotação , Microbiologia do Solo , Solventes/química , Estereoisomerismo , Temperatura
16.
Pain Res Manag ; 2019: 1260353, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31354896

RESUMO

The most common neurological complication in patients receiving successful combination antiretroviral therapy (cART) is peripheral neuropathic pain. Data show that distal symmetric polyneuropathy (DSP) also develops along with murine acquired immunodeficiency syndrome (MAIDS) after infection with the LP-BM5 murine retrovirus mixture. Links between cannabinoid receptor 2 (CB2R) and peripheral neuropathy have been established in animal models using nerve transection, chemotherapy-induced pain, and various other stimuli. Diverse types of neuropathic pain respond differently to standard drug intervention, and little is currently known regarding the effects of modulation through CB2Rs. In this study, we evaluated whether treatment with the exogenous synthetic CB2R agonists JWH015, JWH133, Gp1a, and HU308 controls neuropathic pain and neuroinflammation in animals with chronic retroviral infection. Hind-paw mechanical hypersensitivity in CB2R agonist-treated versus untreated animals was assessed using the MouseMet electronic von Frey system. Multicolor flow cytometry was used to determine the effects of CB2R agonists on macrophage activation and T-lymphocyte infiltration into dorsal root ganglia (DRG) and lumbar spinal cord (LSC). Results demonstrated that, following weekly intraperitoneal injections starting at 5 wk p.i., JWH015, JWH133, and Gp1a, but not HU308 (5 mg/kg), significantly ameliorated allodynia when assessed 2 h after ligand injection. However, these same agonists (2x/wk) did not display antiallodynic effects when mechanical sensitivity was assessed 24 h after ligand injection. Infection-induced macrophage activation and T-cell infiltration into the DRG and LSC were observed at 12 wk p.i., but this neuroinflammation was not affected by treatment with any CB2R agonist. Activation of JAK/STAT3 has been shown to contribute to development of neuropathic pain in the LSC and pretreatment of primary murine microglia (2 h) with JWH015-, JWH133-, or Gp1a-blocked IFN-gamma-induced phosphorylation of STAT1 and STAT3. Taken together, these data show that CB2R agonists demonstrate acute, but not long-term, antiallodynic effects on retrovirus infection-induced neuropathic pain.


Assuntos
Agonistas de Receptores de Canabinoides/farmacologia , Neuralgia/virologia , Infecções por Retroviridae/complicações , Animais , Canabinoides/farmacologia , Modelos Animais de Doenças , Humanos , Hiperalgesia/virologia , Indenos/farmacologia , Indóis/farmacologia , Masculino , Camundongos , Pirazóis/farmacologia , Retroviridae
17.
J Microencapsul ; 36(4): 410-419, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31269832

RESUMO

Poly(urea-formaldehyde) (PUF) microcapsules filled with dicyclopentadiene (DCPD) were prepared by in situ polymerisation and the effect of synthesis parameters, such as pH of the solution and agitation rate, on microcapsules size and shell thickness was evaluated. Scanning electron microscopy (SEM) and Fourier transform infra-red spectroscopy (FTIR) were performed. Adjusted pH conditions (pH = 3.5) and agitation rate (1350 RPM) were found using a design of experiments (DOE). SEM results indicated that microcapsule size was directly affected by agitation rate, whereas shell thickness was mostly affected by pH. After obtaining adjusted synthesis conditions, microcapsules presenting mean size of 60 µm and mean shell thickness of 4 µm were embedded in an epoxy matrix for evaluating the self-healing effect. FTIR and SEM analyses in damaged samples suggested that a healing agent was delivered to the crack location.


Assuntos
Cápsulas/síntese química , Formaldeído/síntese química , Polímeros/síntese química , Cápsulas/química , Técnicas de Química Sintética , Composição de Medicamentos , Formaldeído/química , Concentração de Íons de Hidrogênio , Indenos/administração & dosagem , Tamanho da Partícula , Polimerização , Polímeros/química
18.
Nature ; 571(7766): S19-S21, 2019 07.
Artigo em Inglês | MEDLINE | ID: mdl-31341310
19.
Eur J Med Chem ; 178: 1-12, 2019 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-31167153

RESUMO

Indenopyrazole is emerging as one of the most promising and privileged scaffold in medicinal chemistry. This scaffold have been investigated for the development of novel derivatives and hybrids with other moieties and substituents exhibiting a wide range of medicinal properties like antimycobacterial, antipsychotic, antihypertensive, cannabinoid receptor affinity, anti-tumor, antimicrobial, etc. Furthermore, indenopyrazoles function as inhibitors in various mechanistic pathways which has been well established based on its anticancer potential. This review illustrates various synthetic strategies adopted and reveals the extensive significant biological properties of indenopyrazoles. Furthermore, ample scope is available for this scaffold which needs to be explored by medicinal chemists for the development of new potential drug candidates.


Assuntos
Indenos/farmacologia , Pirazóis/farmacologia , Animais , Linhagem Celular Tumoral , Química Farmacêutica/métodos , Humanos , Indenos/síntese química , Pirazóis/síntese química
20.
Plant Physiol Biochem ; 141: 133-141, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31163340

RESUMO

Ruscus aculeatus is a threatened medicinal plant whose main bioactive components, the ruscogenins, have long been used in the treatment of hemorrhoids and varicose veins, but recently demonstrated activity against some types of cancer. Plant cell biofactories could constitute an alternative to the whole plant as a source of ruscogenins. In this pipeline, despite the in vitro recalcitrance of R. aculeatus, after many attempts we developed friable calli and derived plant cell suspensions, and their ruscogenin production was compared with that of organized in vitro plantlet and root-rhizome cultures. Root-rhizomes showed a higher capacity for biomass and ruscogenin production than the cell suspensions and the yields were greatly improved by elicitation with coronatine. Although ruscogenins accumulate in plants mainly in the root-rhizome, it was demonstrated that the aerial part could play an important role in their biosynthesis, as production was higher in the whole plant than in the root-rhizome cultures.


Assuntos
Biotecnologia/métodos , Ruscus/metabolismo , Espirostanos/metabolismo , Aminoácidos/farmacologia , Biomassa , Técnicas de Cultura de Células , Indenos/farmacologia , Irã (Geográfico) , Luz , Células Vegetais , Extratos Vegetais , Raízes de Plantas , Plantas Medicinais , Rizoma , Saponinas , Sementes/metabolismo , Técnicas de Cultura de Tecidos
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