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BACKGROUND: This study focused on the integrated post-acute care (PAC) stage of stroke patients, and employed a retrospective study to examine the satisfaction with life quality in two groups, one that received home-based rehabilitation and one that received hospital-based rehabilitation. A secondary purpose was to analyze the correlations among the index and components concerning their quality of life (QOL) and compare the advantages and disadvantages of these two approaches to PAC. METHODS: This research was a retrospective study of 112 post-acute stroke patients. The home-based group received rehabilitation for one to two weeks, and two to four sessions per week. The hospital-based group received the rehabilitation for three to six weeks, and 15 sessions per week. The home-based group mainly received the training and guidance of daily activities at the patients' residence. The hospital-based group mainly received physical facilitation and functional training in the hospital setting. RESULTS: The mean scores of QOL assessment for both groups were found to be significantly improved after intervention. Between-group comparisons showed that the hospital-based group had better improvement than the home-based group in mobility, self-care, pain/discomfort and depression/anxiety. In the home-based group, the MRS score and the participant's age can explain 39.4% of the variance of QOL scores. CONCLUSION: The home-based rehabilitation was of lower intensity and duration than the hospital-based one, but it still achieved a significant improvement in QOL for the PAC stroke patients. The hospital-based rehabilitation offered more time and treatment sessions. Therefore hospital-based patients responded with better QOL outcomes than the home-based patients.
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Reabilitação do Acidente Vascular Cerebral , Acidente Vascular Cerebral , Humanos , Qualidade de Vida , Estudos Retrospectivos , Cuidados Semi-Intensivos , Acidente Vascular Cerebral/terapia , HospitaisRESUMO
Chloroplast movement is important for plants to avoid photodamage and to perform efficient photosynthesis. Phototropins are blue light receptors in plants that function in chloroplast movement, phototropism, stomatal opening, and they also affect plant growth and development. In this study, full-length cDNAs of two PHOTOTROPIN genes, PaPHOT1 and PaPHOT2, were cloned from a moth orchid Phalaenopsis aphrodite, and their functions in chloroplast movement were investigated. Phylogenetic analysis showed that PaPHOT1 and PaPHOT2 orthologs were highly similar to PHOT1 and PHOT2 of the close relative Phalaenopsis equestris, respectively, and clustered with monocots PHOT1 and PHOT2 orthologs, respectively. Phalaenopsis aphrodite expressed a moderate level of PaPHOT1 under low blue light of 5 µmol�m-2�s-1 (BL5) and a high levels of PaPHOT1 at >BL100. However, PaPHOT2 was expressed at low levels at
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Orchidaceae/fisiologia , Fototropinas/metabolismo , Fototropismo , Proteínas de Arabidopsis/genética , Proteínas de Arabidopsis/metabolismo , Cloroplastos/metabolismo , Cloroplastos/efeitos da radiação , DNA Complementar/genética , Expressão Gênica , Inativação Gênica , Hibridização In Situ , Luz , Mutação , Orchidaceae/genética , Orchidaceae/efeitos da radiação , Fotossíntese , Fototropinas/genética , Filogenia , Folhas de Planta/genética , Folhas de Planta/fisiologia , Folhas de Planta/efeitos da radiação , Proteínas de Plantas/genética , Proteínas de Plantas/metabolismo , Plantas Geneticamente Modificadas , Proteínas Serina-Treonina Quinases/genética , Proteínas Serina-Treonina Quinases/metabolismoRESUMO
The liquid-air interface of Cassie droplets on superhydrophobic/superlyophobic surfaces has been directly captured with a high-precision laser displacement meter. The measured profile of the interface shape and the critical voltage with which the Cassie-to-Wenzel transition occurs are compared against those from numerical simulations of the electric field coupled with the interface shape. Under the applied voltage, the collapsing behavior of water, glycerol, and hexadecane droplets on SU-8, CYTOP, and overhanging Si/SiO2 pillars has been uniquely identified depending on the liquid properties, the pillar geometry, and the pillar material. It is shown that, with increasing voltage, the contact angle at the three-phase contact line approaches the maximum advancing angle along the pillar sidewalls, above which the depinning from the pillar edge leads to a slide-down motion. The slide-down instability is dominant over the pull-in instability both on dielectric pillars and conductive overhanging pillars examined in the present study. It is indicated that the collapsing behavior on the present overhanging pillars is closely related to contact angle saturation in electrowetting and stick-slip motion of the contact line.
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BACKGROUND: The underlying mechanism of exercise on the development of diabetes-associated neuropathic pain is not well understood. We investigated in rats whether exercise regulates the functional recovery and heat shock protein 72 (Hsp72), tumor necrosis factor (TNF)-α, and interleukin (IL)-6 expression in streptozotocin (STZ)-induced diabetes. METHODS: Male Wistar rats were divided into 4 groups: normal sedentary rats, normal rats with exercise, sedentary STZ-diabetic (SS) rats, and STZ-diabetic rats with exercise. Diabetes was induced with STZ (65 mg/kg IV). The trained rats ran daily on a treadmill 30 to 60 min/d with an intensity of 20 to 25 m/min. We monitored thermal withdrawal latency and mechanical withdrawal threshold as well as Hsp72, TNF-α, and IL-6 expression in the spinal cord and peripheral nerves. RESULTS: Two weeks after STZ injection, sedentary rats exhibited a marked and sustained hypersensitivity to von Frey tactile and heat stimuli. In contrast, diabetic rats undergoing exercise demonstrated delayed progress of tactile and thermal hypersensitivity. Exercise significantly suppressed diabetes-induced blood glucose levels and body weight loss, although they were not restored to control levels. Compared with normal sedentary rats, SS rats displayed significantly higher TNF-α and IL-6 levels in the spinal cord and peripheral nerves. The STZ-diabetic rats with exercise group showed greater Hsp72 expression and similar TNF-α or IL-6 level compared with the SS group in the spinal cord and peripheral nerves on day 14 after STZ treatment. CONCLUSIONS: These results suggest that progressive exercise training markedly decreases diabetes-associated neuropathic pain, including thermal hyperalgesia and mechanical allodynia. In rats, this protective effect is related to the increase of Hsp72, but not TNF-α and IL-6, expression in the spinal cord and peripheral nerves of STZ-induced diabetes.
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Neuropatias Diabéticas/complicações , Proteínas de Choque Térmico HSP72/biossíntese , Hiperalgesia/complicações , Condicionamento Físico Animal/fisiologia , Animais , Glicemia/metabolismo , Citocinas/biossíntese , Diabetes Mellitus Experimental/complicações , Diabetes Mellitus Experimental/patologia , Diabetes Mellitus Tipo 1/complicações , Temperatura Alta , Interleucina-6/biossíntese , Masculino , Nervos Periféricos/metabolismo , Estimulação Física , Ratos , Ratos Wistar , Medula Espinal/metabolismo , Fator de Necrose Tumoral alfa/biossíntese , Redução de Peso/fisiologiaRESUMO
BACKGROUND: The underlying mechanism of exercise on neuropathic pain is not well understood. We investigated whether physical exercise regulates the functional recovery and heat shock protein 72 (Hsp72), tumor necrosis factor-α (TNF-α), and interlukin-1ß (IL-1ß) expression after chronic constriction injury (CCI) of the sciatic nerve. METHODS: Male Sprague-Dawley rats were divided into 7 groups: control, sham operated (SO), SO with swimming or treadmill exercise (SOSE or SOTE), CCI, CCI with swimming or treadmill exercise (CCISE or CCITE). We recorded body weight, thermal withdrawal latency, and mechanical withdrawal threshold as well as Hsp72, TNF-α, and IL-1ß expression in sciatic nerve. RESULTS: The body weights in the control and SO groups were heavier than those in the SOSE, SOTE, CCI, CCISE, and CCITE groups. CCI rats with swimming or treadmill exercise showed significant increase in thermal withdrawal latency and mechanical withdrawal threshold when compared with CCI rats without exercise on day 21 after CCI. Both CCISE and CCITE groups demonstrated greater Hsp72 expression and lower TNF-α or IL-1ß level than did the CCI group in sciatic nerve on day 21 after CCI. CONCLUSIONS: These results suggest that progressive exercise training decreases peripheral neuropathic pain as well as TNF-α and IL-1ß overproduction and increases HSP72 expression after CCI of the sciatic nerve.
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Citocinas/metabolismo , Limiar da Dor , Esforço Físico , Nervo Isquiático/fisiopatologia , Neuropatia Ciática/prevenção & controle , Animais , Peso Corporal , Constrição , Modelos Animais de Doenças , Proteínas de Choque Térmico HSP72/metabolismo , Hiperalgesia/imunologia , Hiperalgesia/fisiopatologia , Hiperalgesia/prevenção & controle , Interleucina-1beta/metabolismo , Masculino , Medição da Dor , Ratos , Ratos Sprague-Dawley , Tempo de Reação , Corrida , Nervo Isquiático/imunologia , Nervo Isquiático/lesões , Nervo Isquiático/patologia , Neuropatia Ciática/etiologia , Neuropatia Ciática/imunologia , Neuropatia Ciática/fisiopatologia , Natação , Fatores de Tempo , Fator de Necrose Tumoral alfa/metabolismoRESUMO
Spasticity is a common complication for patients with stroke, but only few studies investigate the relation between spasticity and voluntary movement. This study proposed a novel automatic system for assessing the severity of spasticity (SS) of four upper-limb joints, including the elbow, wrist, thumb, and fingers, through voluntary movements. A wearable system which combined 19 inertial measurement units and a pressure ball was proposed to collect the kinematic and force information when the participants perform four tasks, namely cone stacking (CS), fast flexion and extension (FFE), slow ball squeezing (SBS), and fast ball squeezing (FBS). Several time and frequency domain features were extracted from the collected data, and two feature selection approaches based on recursive feature elimination were adopted to select the most influential features. The selected features were input into five machine learning techniques for assessing the SS for each joint. The results indicated that using CS task to assess the SS of elbow and fingers and using FBS task to assess the SS of thumb and wrist can reach the highest weighted-average F1-score. Furthermore, the study also concluded that FBS is the optimal task for assessing all the four upper-limb joints. The overall result shown that the proposed automatic system can assess four upper-limb joints through voluntary movements accurately, which is a breakthrough of finding the relation between spasticity and voluntary movement.
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Vibrio vulnificus, a highly virulent marine bacterium, causes serious wound infections and fatal septicemia in many areas of the world. To identify V. vulnificus genes required for killing macrophages, we made an insertional mutant library of V. vulnificus and screened it for reduced macrophage cytotoxicity. One mutant defective in macrophage cytotoxicity had an insertion in ychF, a gene encoding a putative GTPase. In addition to reduced cytotoxicity, this mutant had attenuated growth in iron-limited medium and reduced virulence in iron-overloaded mice. The ychF mutation also down-regulated the transcription level of the rtxA1 gene. RtxA1 mutants significantly decreased cytotoxicity to macrophages compared to wild-type bacteria. Overall, these results show that YchF elicits macrophage cytotoxicity through an rtxA1 pathway and is important for mouse virulence.
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Proteínas de Bactérias/metabolismo , GTP Fosfo-Hidrolases/metabolismo , Ferro/metabolismo , Macrófagos/microbiologia , Vibrio vulnificus/patogenicidade , Animais , Proteínas de Bactérias/genética , Toxinas Bacterianas/genética , Toxinas Bacterianas/metabolismo , Linhagem Celular , Clonagem Molecular , Meios de Cultivo Condicionados , Elementos de DNA Transponíveis , Regulação para Baixo , Feminino , GTP Fosfo-Hidrolases/genética , Regulação Bacteriana da Expressão Gênica , Biblioteca Gênica , Genes Bacterianos , Interações Hospedeiro-Patógeno , Ferro/sangue , Sobrecarga de Ferro/metabolismo , Dose Letal Mediana , Macrófagos/metabolismo , Camundongos , Camundongos Endogâmicos BALB C , Mutagênese Insercional/métodos , Plasmídeos/genética , Plasmídeos/metabolismo , Transcrição Gênica , Vibrioses/metabolismo , Vibrioses/microbiologia , Vibrio vulnificus/enzimologia , Vibrio vulnificus/metabolismo , VirulênciaRESUMO
BACKGROUND: Memantine blocks N-methyl-D-aspartate receptors and the Na(+) current, one principal mechanism of local anesthesia. Until now, no study mentioned that memantine had a local anesthetic effect, and therefore we investigated the local anesthetic effect of memantine. METHODS: After blockade of cutaneous trunci muscle reflex with subcutaneous injections, we evaluated the cutaneous analgesic effect of memantine, lidocaine, and dizocilpine (MK-801) in rats. The dose-dependent response of memantine on cutaneous analgesia was compared with lidocaine and MK-801 in rats. The duration of action for each drug was evaluated and compared on an equipotent basis (20% effective dose [ED(20)], ED(50), and ED(80)). Lidocaine, a frequently used local anesthetic, was used as control. RESULTS: We demonstrated that memantine, lidocaine, and MK-801 produced dose-dependent local anesthetic effects as infiltrative cutaneous analgesia. The relative potency was MK-801 (10.4 [9.7-11.1]) > memantine (17.6 [15.2-20.4]) > lidocaine (25.9 [23.8-28.1 ]) (P < 0.01). On an equipotent basis, memantine showed longer duration than lidocaine (P = 0.012) and MK-801 (P = 0.008). Coadministration of memantine (13.3 µmol/kg) and MK-801 (1.3 µmol/kg) produced greater blockade and duration than memantine (13.3 µmol/kg) or MK-801 (1.3 µmol/kg) alone. Neither local injection of saline nor intraperitoneal administration of a large dose of memantine, lidocaine, or MK-801 produced cutaneous analgesia (data not shown). CONCLUSIONS: This study indicated that memantine is less potent than MK-801, and that memantine elicits longer analgesic duration than both lidocaine and MK-801. When combined with MK-801, memantine demonstrates a synergetic effect of cutaneous analgesia. We conclude that memantine produces better local analgesia than lidocaine and that N-methyl-D-aspartate receptors also contribute to the analgesic effect of memantine.
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Analgesia/métodos , Maleato de Dizocilpina/administração & dosagem , Lidocaína/administração & dosagem , Memantina/administração & dosagem , Anestésicos Locais , Animais , Maleato de Dizocilpina/farmacocinética , Relação Dose-Resposta a Droga , Injeções Subcutâneas , Lidocaína/farmacocinética , Masculino , Memantina/farmacocinética , Ratos , Ratos Sprague-DawleyRESUMO
PURPOSE: Dextrorphan, a major metabolite of dextromethorphan, produces the duration of spinal and cutaneous anesthesia similar to bupivacaine. The purpose of this study was to test the central nervous system and cardiovascular toxicity of bupivacaine, dextromethorphan, and dextrorphan. METHODS: First, dose-response curves for dextromethorphan, dextrorphan, and bupivacaine (n = 8 at each testing point) were determined for cutaneous analgesia on the rat back, and equipotent doses were calculated. Next, during continuous intravenous infusion of equipotent doses of bupivacaine, dextromethorphan, and dextrorphan (n = 8 in each group), we observed the time to seizure, apnea, and complete cardiac arrest. A saline group (n = 7) was used for comparison. Mean arterial blood pressure (MAP), heart rate (HR), stroke volume (SV), and cardiac output (CO) were also monitored. RESULTS: Bupivacaine, dextromethorphan, and dextrorphan produced dose-dependent cutaneous anesthesia. A longer duration of equipotent infusion doses was required to produce seizures in the dextromethorphan group (10.6 ± 1.3 min) than in the bupivacaine group (7.6 ± 2.1 min) (P = 0.005). Dextrorphan did not produce any seizures. Compared with bupivacaine, time to apnea and complete cardiac arrest was longer with dextrorphan (P < 0.001) and with dextromethorphan (P = 0.001). Cardiovascular collapse, defined as a decline in MAP, HR, CO, and SV, was slower in the dextromethorphan and dextrorphan groups than in the bupivacaine group (P < 0.001 for both comparisons). CONCLUSION: At equipotent doses for local anesthesia, dextromethorphan and dextrorphan were less likely than bupivacaine to induce central nervous system and cardiovascular toxicity.
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Anestésicos Locais/toxicidade , Bupivacaína/toxicidade , Dextrometorfano/toxicidade , Dextrorfano/toxicidade , Anestésicos Locais/administração & dosagem , Animais , Apneia/induzido quimicamente , Bupivacaína/administração & dosagem , Dextrometorfano/administração & dosagem , Dextrorfano/administração & dosagem , Relação Dose-Resposta a Droga , Antagonistas de Aminoácidos Excitatórios/administração & dosagem , Antagonistas de Aminoácidos Excitatórios/toxicidade , Parada Cardíaca/induzido quimicamente , Infusões Intravenosas , Masculino , Ratos , Ratos Sprague-Dawley , Convulsões/induzido quimicamente , Fatores de TempoRESUMO
Vascular embolization provides an effective approach for the treatment of hemorrhage, aneurysms, and other vascular abnormalities. However, current embolic materials, such as metallic coils and liquid embolic agents, are limited by their inability to provide safe, consistent, and controlled embolization. Here, we report an injectable hydrogel that can remain at the injection site and subsequently undergo in situ covalent crosslinking, leading to the formation of a dual-crosslinking network (DCN) hydrogel for endovascular embolization. The DCN hydrogel is simple to prepare, easy to deploy via needles and catheters, and mechanically stable at the target injection site, thereby avoiding embolization of nontarget vessels. It possesses efficient hemostatic activity and good biocompatibility. The DCN hydrogel is also clearly visible under X-ray imaging, thereby allowing for targeted embolization. In vivo tests in a rabbit artery model demonstrates that the DCN hydrogel is effective in achieving immediate embolization of the target artery with long-term occlusion by inducing luminal fibrosis. Collectively, the DCN hydrogel provides a viable, biocompatible, and cost-effective alternative to existing embolic materials with clinical translation potential for endovascular embolization.
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Artérias/efeitos dos fármacos , Materiais Biomiméticos/farmacologia , Reagentes de Ligações Cruzadas/farmacologia , Embolização Terapêutica , Fibrose/tratamento farmacológico , Hidrogéis/farmacologia , Animais , Materiais Biomiméticos/administração & dosagem , Materiais Biomiméticos/química , Células Cultivadas , Reagentes de Ligações Cruzadas/administração & dosagem , Reagentes de Ligações Cruzadas/química , Humanos , Hidrogéis/administração & dosagem , Hidrogéis/química , Teste de Materiais , Camundongos , Estrutura MolecularRESUMO
BACKGROUND: Although proxymetacaine and oxybuprocaine produce topical ocular and spinal anesthesia, they have never been tested as cutaneous anesthetics. We compared cutaneous analgesia of proxymetacaine and oxybuprocaine with bupivacaine and tested their central nervous system and cardiovascular toxicity. METHODS: After blockade of cutaneous trunci muscle reflex with subcutaneous injections, we evaluated the local anesthetic effect of proxymetacaine and oxybuprocaine on cutaneous analgesia in rats. After i.v. infusions of equipotent doses of oxybuprocaine, proxymetacaine, and bupivacaine, we observed the onset time of seizure, apnea, and impending death and monitored mean arterial blood pressure and heart rate. RESULTS: Proxymetacaine and oxybuprocaine acted like bupivacaine and produced dose-related cutaneous analgesia. On a 50% effective dose basis, the ranks of potencies were proxymetacaine > oxybuprocaine > bupivacaine (P < 0.01). Under equipotent doses, the infusion times of proxymetacaine or oxybuprocaine required to cause seizure, apnea, and impending death were longer than that of bupivacaine (P < 0.05). The decrease in mean arterial blood pressure and heart rate was slower with oxybuprocaine and proxymetacaine compared with bupivacaine (P < 0.05 for the differences) at equipotent doses. CONCLUSIONS: Oxybuprocaine and proxymetacaine were more potent at producing cutaneous anesthesia but were less potent than bupivacaine at producing central nervous system and cardiovascular toxicity.
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Anestésicos Locais/toxicidade , Bupivacaína/toxicidade , Procaína/análogos & derivados , Propoxicaína/toxicidade , Analgesia , Anestésicos Locais/administração & dosagem , Animais , Bupivacaína/administração & dosagem , Relação Dose-Resposta a Droga , Hemodinâmica/efeitos dos fármacos , Infusões Intravenosas , Masculino , Síndromes Neurotóxicas/fisiopatologia , Medição da Dor/efeitos dos fármacos , Procaína/administração & dosagem , Procaína/toxicidade , Propoxicaína/administração & dosagem , Ratos , Ratos Sprague-Dawley , Convulsões/induzido quimicamenteRESUMO
Many daily activities require people to complete a motor task while walking. The purpose of this study was to analyze subjects' ability to perform motor tasks while walking. Subjects were classified into three different groups. The first group included 15 full community ambulators post-stroke. The second group included 15 least limited community ambulators post-stroke. The final group included 15 age-matched healthy subjects. Gait performance was measured under three different conditions: (1) preferred walking (single task); (2) walking buttoning up (buttoning task); (3) walking while carrying a tray with glasses (tray-carrying task). Gait velocity, cadence, stride time, stride length, temporal and spatial symmetry indices were examined with the GAITRite system. Our results showed that there were no significant differences between full community ambulators and control subjects for all gait variables. However, there were significant differences in dual-task-related gait decrement between the full community ambulators and control subjects. There were also significant differences in dual-task-related gait decrement between least limited community ambulators and control subjects. The findings of this study suggest that subjects with stroke including the full community ambulators have difficulty performing two motor tasks concurrently.
Assuntos
Transtornos Neurológicos da Marcha/fisiopatologia , Destreza Motora/fisiologia , Acidente Vascular Cerebral/fisiopatologia , Adulto , Idoso , Estudos de Casos e Controles , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Paresia/fisiopatologia , Caminhada/fisiologiaRESUMO
Bacillus cereus QQ308 produced antifungal hydrolytic enzymes, comprising chitinase, chitosanase and protease, when grown in a medium containing shrimp and crab shell powder (SCSP) produced from marine waste. The growth of the plant-pathogenic fungi Fusarium oxysporum, Fusarium solani, and Pythium ultimum were considerably affected by the presence of the QQ308 culture supernatant. The supernatant inhibited spore germination and germ tube elongation of F. oxysporum, F. solani, and P. ultimum. The increase in the growth time of the fungal culture was associated with a gradual decrease in inhibition. Besides antifungal activity, QQ308 enhanced growth of Chinese cabbage. These characteristics were unique among known strains of B. cereus. To our knowledge, this is the first report on the antifungal and Chinese cabbage growth enhancing compounds produced by B. cereus.
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Antifúngicos/farmacologia , Bacillus cereus/enzimologia , Quitina/metabolismo , Quitinases/farmacologia , Glicosídeo Hidrolases/farmacologia , Peptídeo Hidrolases/farmacologia , Frutos do MarRESUMO
Dynamic wetting problems are fundamental to understanding the interaction between liquids and solids. Even in a superficially simple experimental situation, such as a droplet spreading over a dry surface, the result may depend not only on the liquid properties but also strongly on the substrate-surface properties; even for macroscopically smooth surfaces, the microscopic geometrical roughness can be important. In addition, because surfaces may often be naturally charged or electric fields are used to manipulate fluids, electric effects are crucial components that influence wetting phenomena. We investigate the interplay between electric forces and surface structures in dynamic wetting. Although surface microstructures can significantly hinder spreading, we find that electrostatics can "cloak" the microstructures, that is, deactivate the hindering. We identify the physics in terms of reduction in contact-line friction, which makes the dynamic wetting inertial force dominant and insensitive to the substrate properties.
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Shogaols are a group of the active constituents of ginger that have been identified to have various biological activities. The aim of the current study was to investigate the antitumor activity of 6-shogaol in hepatocellular carcinoma (HCC) and the possible involvement of reactive oxygen species as a putative mechanism of action. HCC cell lines, HepG2 and Huh-7, were used to study the in vitro anti-cancer activity of 6-shogaol via the application of various molecular biology techniques. Results showed that 6-shogaol effectively inhibited the cell viability, caused cell cycle arrest at G2/M phase and induced apoptosis in HCC cells as indicated by MTT assay, DAPI nuclear staining, annexin V assay, cell cycle analysis, and activation of caspase-3. Western blot analysis revealed the ability of 6-shogaol to target cancer survival signaling pathways mediated by mitogen-activated protein kinase (MAPK), 5' AMP-activated protein kinase (AMPK) and Akt. In addition, 6-Shogaol induced alteration of cyclin proteins expression and caused cleavage of protein kinase C delta. Furthermore, 6-Shogaol was able to induce the production of reactive oxygen species and endoplasmic reticulum (ER) stress-associated proteins and the consequent activation of autophagy in HepG2 cells. Taken together, the current study highlights evidences that 6-shogaol induces apoptosis, modulates cyclins expression and targets cancer survival signaling pathways in HCC cell lines, at least in part, via the production of reactive oxygen species. These findings support 6-shogaol's clinical promise as a potential candidate for HCC therapy.
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Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Carcinoma Hepatocelular/patologia , Catecóis/farmacologia , Pontos de Checagem da Fase G2 do Ciclo Celular/efeitos dos fármacos , Neoplasias Hepáticas/patologia , Pontos de Checagem da Fase M do Ciclo Celular/efeitos dos fármacos , Autofagia/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Estresse do Retículo Endoplasmático/efeitos dos fármacos , Células Hep G2 , Humanos , Fosforilação/efeitos dos fármacos , Espécies Reativas de Oxigênio/metabolismo , Transdução de Sinais/efeitos dos fármacosRESUMO
The purpose of this study was to estimate the local anesthetic effect of orphenadrine, an anti-muscarinic agent, in spinal anesthesia and its comparison with the local anesthetic lidocaine. After the rat was injected intrathecally, the spinal block of orphenadrine and lidocaine was constructed in a dosage-dependent fashion. The potency and duration of spinal anesthesia with orphenadrine were compared with that of lidocaine. Our data demonstrated that orphenadrine and lidocaine elicited dose-dependent spinal blockades on the motor function, sensory, and proprioception. On the 50% effective dose (ED50) basis, the ranks of potency in motor function, nociception, and proprioception were orphenadrine>lidocaine (P<0.01). At equipotent doses (ED25, ED50, ED75), the block duration elicited by orphenadrine was greater than that elicited by lidocaine (P<0.01). Orphenadrine, but not lidocaine, exhibited longer duration of nociceptive/sensory blockade than that of motor blockade at equipotent doses. Ineffective-dose orphenadrine as adjuvant did not enhance spinal anesthesia with lidocaine. The preclinical data revealed that orphenadrine with a more sensory-selective action over motor block exhibited more potent and longer spinal anesthesia when compared to lidocaine.
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Raquianestesia/métodos , Anestésicos Locais/administração & dosagem , Orfenadrina/administração & dosagem , Animais , Relação Dose-Resposta a Droga , Injeções Espinhais , Lidocaína/administração & dosagem , Masculino , Antagonistas Muscarínicos/administração & dosagem , Nociceptividade/efeitos dos fármacos , Propriocepção/efeitos dos fármacos , Desempenho Psicomotor/efeitos dos fármacos , Ratos , Ratos Sprague-DawleyRESUMO
The aim of this study was to investigate infiltrative cutaneous anesthesia of 2-adamantanamine and rimantadine. After subcutaneous injections of drugs in rats, the blockade of cutaneous trunci muscle reflex by 2-adamantanamine and rimantadine was evaluated. Lidocaine, a common local anesthetic, was used as control. We showed that rimantadine and 2-adamantanamine as well as the local anesthetic lidocaine produced infiltrative anesthesia of skin in a dose-dependent fashion. Saline (vehicle) group displayed no cutaneous anesthesia. The relative potency of these drugs was rimantadine [23.8 (21.1-26.8)] = lidocaine [26.4 (22.7-30.6)] > 2-adamantanamine [64.6 (55.0-75.9)] (P < 0.01). On an equianesthetic basis [25% effective dose (ED25 ), ED50 , and ED75 ], rimantadine and 2-adamantanamine had longer duration of action than lidocaine (P < 0.05). Neither local injection of saline nor intraperitoneal administration of a large dose of drugs elicited cutaneous anesthesia (data not shown). These data demonstrated for the first time that rimantadine had a similar potent and longer duration of skin infiltrative anesthesia than did lidocaine, whereas 2-adamantanamine had a less potency but longer duration of cutaneous anesthesia than did lidocaine.
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Amantadina/análogos & derivados , Anestesia Local/métodos , Anestésicos Locais/farmacologia , Rimantadina/farmacologia , Pele/efeitos dos fármacos , Amantadina/administração & dosagem , Amantadina/química , Amantadina/farmacologia , Anestésicos Locais/administração & dosagem , Anestésicos Locais/química , Animais , Comportamento Animal/efeitos dos fármacos , Relação Dose-Resposta a Droga , Injeções Subcutâneas , Masculino , Estrutura Molecular , Medição da Dor , Estimulação Física , Ratos , Ratos Sprague-Dawley , Reflexo/efeitos dos fármacos , Rimantadina/administração & dosagem , Rimantadina/química , Pele/inervaçãoRESUMO
Although diphenhydramine has been shown to produce longer duration of spinal block than lidocaine, few studies disclose its skin infiltrative anesthesia when compared with a long-lasting local anesthetic, bupivacaine. The purpose of this study was to investigate whether diphenhydramine elicited cutaneous analgesia in comparison with bupivacaine. After inhibition of cutaneous trunci muscle reflex via subcutaneous injection of drugs in rats, we examined the local anesthetic effect of diphenhydramine and bupivacaine as infiltrative cutaneous analgesia in a dose-dependent fashion. We showed that diphenhydramine, as well as bupivacaine displayed a dose-dependent cutaneous analgesia in response to dorsal cutaneous noxious stimuli. The relative potency (50% effective dose) was bupivacaine (0.023 [0.013-0.035]%) > diphenhydramine (0.078 [0.068-0.091]%; P < 0.001). On an equipotent basis, diphenhydramine had a similar duration of action to bupivacaine. Neither local injection of saline nor intraperitoneal administration of a large dose of diphenhydramine or bupivacaine produced cutaneous analgesia (data not shown). We conclude that diphenhydramine is less potent than bupivacaine at producing cutaneous analgesia. At equipotent doses for infiltrative cutaneous analgesia, the duration of action of diphenhydramine is equal to that of bupivacaine.
Assuntos
Anestésicos Locais/farmacologia , Bupivacaína/farmacologia , Difenidramina/farmacologia , Pele/efeitos dos fármacos , Analgesia/métodos , Analgésicos/administração & dosagem , Analgésicos/farmacologia , Anestésicos Locais/administração & dosagem , Animais , Bupivacaína/administração & dosagem , Preparações de Ação Retardada , Difenidramina/administração & dosagem , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Masculino , Dor/tratamento farmacológico , Ratos , Ratos Sprague-Dawley , Pele/patologia , Fatores de TempoRESUMO
The purpose of this study was to examine the effect of epinephrine as adjuvant for memantine or lidocaine as an infiltrative anesthetic. Using a rat model of cutaneous trunci muscle reflex (CTMR), we evaluated the effects of adding epinephrine to memantine or lidocaine on infiltrative cutaneous analgesia. Lidocaine, a known local anesthetic, was used as control. We found that epinephrine, memantine, and lidocaine produced a dose-dependent local anesthetic effect as infiltrative cutaneous analgesia. On a 50% effective dose (ED50) basis, the relative potencies were epinephrine [0.012 (0.006-0.020)µmol]>memantine [4.010 (3.311-4.988)µmol]>lidocaine [6.177 (5.333-7.218)µmol] (P<0.05 for each comparison). Mixtures of epinephrine (2.7nmol or 13.7nmol) with drugs (memantine or lidocaine) at ED50 or ED95, respectively, enhanced the potency and prolonged the duration of action on infiltrative cutaneous analgesia. Intraperitoneal injection of co-administration of drugs (memantine or lidocaine) at ED95 with epinephrine (13.7nmol) produced no cutaneous analgesia (data not shown). Epinephrine, memantine, and lidocaine were shown to have local anesthetic effects as infiltrative cutaneous analgesia. Epinephrine increased the duration and potency of memantine and lidocaine as an infiltrative anesthetic.
Assuntos
Analgésicos , Anestésicos Combinados , Anestésicos Locais , Epinefrina , Memantina , Dor/tratamento farmacológico , Analgésicos/uso terapêutico , Animais , Epinefrina/uso terapêutico , Lidocaína , Masculino , Memantina/uso terapêutico , Dor/fisiopatologia , Ratos Sprague-Dawley , Pele/fisiopatologiaRESUMO
The aim of this study was to evaluate the effect of epinephrine as additive for propranolol as an infiltrative anesthetic. Using a rat model of cutaneous trunci muscle reflex (CTMR), we tested the effect of co-administration of epinephrine with propranolol on infiltrative cutaneous analgesia. Bupivacaine, a long-lasting local anesthetic, was used as control. Subcutaneous propranolol and bupivacaine elicited a dose-dependent local anesthetic effect on infiltrative cutaneous analgesia. On the 50% effective dose (ED50) basis, the relative potency was bupivacaine [2.05 (1.95-2.21) µmol/kg]>propranolol [9.21 (9.08-9.42) µmol/kg] (P<0.01 for each comparison). Subcutaneous epinephrine (0.012 µmol/kg) did not produce cutaneous analgesia. Mixtures of epinephrine (0.012 µmol/kg) with drugs (propranolol or bupivacaine) at ED50 or ED95, respectively, intensified and prolonged drug action on infiltrative cutaneous analgesia. Intraperitoneal injection of combined drugs (propranolol or bupivacaine) at ED95 with epinephrine (0.012 µmol/kg) exhibited no cutaneous analgesia. We concluded that propranolol was less potent but produced a similar duration of action when compared to bupivacaine on infiltrative cutaneous analgesia. Epinephrine as adjuvant for propranolol or bupivacaine enhanced the potency and extended the duration of action on infiltrative cutaneous analgesia.