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BACKGROUND: Stair-climbing (SC) is an essential daily life skill, and stair-climbing exercise (SCE) serves as a valuable method for promoting physical activity in older adults. This study aimed to compare the impact of SCEs with heel contact (HC) and heel off (HO) during SC on functional mobility and trunk muscle (TM) activation amplitudes in community-dwelling older adults. METHODS: In the pilot randomized controlled trial, participants were randomly allocated to either the HC group (n = 17; mean age 75.9 ± 6.3 years) or the HO group (n = 17; mean age 76.5 ± 4.6 years). The HC participants performed SCE with the heel of the ankle in contact with the ground, while the HO participants performed SCE with the heel of the ankle off the ground during SC. Both groups participated in progressive SCE for one hour per day, three days per week, over four consecutive weeks (totaling 12 sessions) at the community center. We measured timed stair-climbing (TSC), timed up and go (TUG), and electromyography (EMG) amplitudes of the TMs including rectus abdominis (RA), external oblique (EO), transverse abdominus and internal oblique abdominals (TrA-IO), and erector spinae (ES) during SC before and after the intervention. RESULTS: Both groups showed a significant improvement in TSC and TUG after the intervention (P < .01, respectively), with no significant difference between the groups. There was no significant difference in the EMG activity of the TMs between the groups after the intervention. The amplitude of TMs significantly decreased after the intervention in both groups (P < .01, respectively). CONCLUSION: Both SCE methods could improve balance and SC ability in older adults while reducing the recruitment of TMs during SC. Both SCE strategies are effective in improving functional mobility and promoting appropriate posture control during SC in older adults.
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Eletromiografia , Vida Independente , Subida de Escada , Humanos , Idoso , Masculino , Projetos Piloto , Feminino , Subida de Escada/fisiologia , Idoso de 80 Anos ou mais , Tronco/fisiologia , Músculo Esquelético/fisiologiaRESUMO
In this study, we investigated the efficacy of kaempferol (a flavonoid found in plants and plant-derived foods such as kale, beans, tea, spinach and broccoli) on vascular contractibility and aimed to clarify the detailed mechanism underlying the relaxation. Isometric contractions of divested muscles were stored and linked with western blot analysis which was carried out to estimate the phosphorylation of myosin phosphatase targeting subunit 1 (MYPT1) and phosphorylation-dependent inhibitory protein for myosin phosphatase (CPI-17) and to estimate the effect of kaempferol on the RhoA/ROCK/CPI-17 pathway. Kaempferol conspicuously impeded phorbol ester-, fluoride- and a thromboxane mimetic-derived contractions regardless of endothelial nitric oxide synthesis, indicating its direct effect on smooth muscles. It also conspicuously impeded the fluoride-derived elevation in phospho-MYPT1 rather than phospho-CPI-17 levels and phorbol 12,13-dibutyrate-derived increase in phospho-CPI-17 and phospho-ERK1/2 levels, suggesting the depression of PKC and MEK activities and subsequent phosphorylation of CPI-17 and ERK1/2. Taken together, these outcomes suggest that kaempferol-derived relaxation incorporates myosin phosphatase retrieval and calcium desensitization, which appear to be modulated by CPI-17 dephosphorylation mainly through PKC inactivation.
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In this investigation, we made a study of the efficacy of luteolin (a flavonoid found in plants such as vegetables, herbs and fruits) on vascular contractibility and to elucidate the mechanism underlying the relaxation. Isometric contractions of denuded muscles were stored and combined with western blot analysis which was conducted to assess the phosphorylation of myosin phosphatase targeting subunit 1 (MYPT1) and phosphorylation-dependent inhibitory protein for myosin phosphatase (CPI-17) and to examine the effect of luteolin on the RhoA/ROCK/CPI-17 pathway. Luteolin significantly alleviated phorbol ester-, fluoride- and thromboxane mimetic-elicited contractions regardless of endothelial nitric oxide synthesis, implying its direct effect on smooth muscle. It also significantly alleviated the fluoride-elicited elevation in pCPI-17 and pMYPT1 levels and phorbol 12,13-dibutyrate-elicited increase in pERK1/2 level, suggesting depression of ROCK and PKC/MEK activity and ensuing phosphorylation of MYPT1, CPI-17 and ERK1/2. Taken together, these results suggest that luteolin-elicited relaxation includes myosin phosphatase reactivation and calcium desensitization, which seems to be arbitrated by CPI-17 dephosphorylation via ROCK/PKC inhibition.
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In this study, we investigated the influence of galangin on vascular contractibility and to determine the mechanism underlying the relaxation. Isometric contractions of denuded aortic muscles were recorded and combined with western blot analysis which was performed to measure the phosphorylation of phosphorylation-dependent inhibitory protein of myosin phosphatase (CPI-17) and myosin phosphatase targeting subunit 1 (MYPT1) and to evaluate the effect of galangin on the RhoA/ROCK/CPI-17 pathway. Galangin significantly inhibited phorbol ester-, fluoride- and thromboxane mimetic-induced vasoconstrictions regardless of endothelial nitric oxide synthesis, suggesting its direct effect on vascular smooth muscle. Galangin significantly inhibited the fluoride-dependent increase in pMYPT1 and pCPI-17 levels and phorbol 12,13-dibutyrate-dependent increase in pERK1/2 level, suggesting repression of ROCK and MEK activity and subsequent phosphorylation of MYPT1, CPI-17 and ERK1/2. Taken together, these results suggest that galangin-induced relaxation involves myosin phosphatase reactivation and calcium desensitization, which appears to be mediated by CPI-17 dephosphorylation via not PKC but ROCK inactivation.
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BACKGROUND: Taekkyon, a Korean form of martial arts, has been trained for a long period. However, it is not yet known whether the Taekkyon exercise has better effects on functional mobility or balance in older adults than other types of well-investigated exercise programs such as Tai Chi (TC). OBJECTIVE: This study aimed to compare the effects of TC and Taekkyon exercise programs on the lower-extremity strength, balance, and gait ability of community-dwelling older women as a fall prevention method. METHODS: Community-dwelling older women were randomly allocated into the TC group (n1= 23) and the Taekkyon group (n2= 23). Both groups completed 1 h of either TC or Taekkyon exercises twice weekly for 12 consecutive weeks (24 sessions in total). We measured the Timed Up and Go test (TUG), Functional Reach test (FR), one-leg standing test (OLS), Five Times Sit-to-Stand test (5 × STS), 30 Second Sit-to-Stand test (30 s STS), and spatiotemporal gait parameters (gait velocity, step length, step width, stride time, and cadence) before and after the intervention. RESULTS: Both groups similarly showed statistically significant improvements in balance (TUG, FR, and OLS), lower-extremity strength (5 × STS and 30 s STS), and spatiotemporal gait parameters except for step width (P< 0.05). Moreover, the TC group showed greater improvement in the OLS test than the Taekkyon group (P< 0.05). CONCLUSIONS: The results from this study support the efficacy of the TC and Taekkyon exercise programs at improving mobility in this population of older women. However, this study did not clarify which exercise program is more effective as general balance and mobility training program for older women.
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Terapia por Exercício/métodos , Marcha/fisiologia , Artes Marciais , Equilíbrio Postural/fisiologia , Amplitude de Movimento Articular/fisiologia , Tai Chi Chuan , Acidentes por Quedas/prevenção & controle , Idoso , Idoso de 80 Anos ou mais , Exercício Físico/fisiologia , Feminino , Humanos , Vida Independente , Método Simples-Cego , Estudos de Tempo e MovimentoRESUMO
Phosphatidylcholine (PPC) formula has been therapeutically used to reduce areas of localized fat. However, no single research has been carried out on its effect on a variety of cells in adipose and muscle tissues. Herein, the current study aimed to explore the activity of PPC on different cells in adipose and muscle tissues and to investigate the molecular mechanisms contributing to the effects of PPC on lipolysis and apoptosis. mRNA expression levels of various genes were measured by quantitative real-time PCR. Protein expression levels were observed through Western blotting and cell viability was measured by MTT assay. Lipolysis and caspase 3 activity assay were performed using commercial kits. PPC induces lipolysis and apoptosis in adipocytes (3T3-L1), but not in the other tested cells, including skeletal muscle cells (C2C12 myocytes), endothelial cells (HUVEC), and fibroblasts (BJ). The possible role of TNFα and IL-1ß-mediated pathways on the effects of PPC was also revealed. We confirmed that treatment with PPC caused lipolysis and apoptosis in a dose-dependent manner (only in 3T3-L1 adipocytes). The effect of PPC observed in 3T3-L1 adipocytes was not evident in C2C12 myocytes, HUVEC, and fibroblasts. PPC also increased TNFα and IL-1ß expression and release in 3T3-L1 adipocytes in a dose-dependent fashion, but not in C2C12 myocytes, HUVEC, and BJ. Suppression of TNFα or IL-1ß reversed PPC-induced lipolysis and apoptosis in 3T3-L1 adipocytes, suggesting that PPC could promote adipocyte-specific lipolysis and apoptosis through TNFα and IL-1ß-mediated signaling. We conclude that the specific activity of PPC on adipocyte in adipose without other tissue damages can be an effective approach for melting lipid.
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Apoptose/efeitos dos fármacos , Lipólise/efeitos dos fármacos , Fosfatidilcolinas/farmacologia , Células 3T3-L1 , Adipócitos/citologia , Adipócitos/efeitos dos fármacos , Adipócitos/metabolismo , Animais , Linhagem Celular , Fibroblastos/citologia , Fibroblastos/efeitos dos fármacos , Fibroblastos/metabolismo , Células Endoteliais da Veia Umbilical Humana , Humanos , Interleucina-1beta/antagonistas & inibidores , Interleucina-1beta/genética , Interleucina-1beta/metabolismo , Camundongos , Músculo Esquelético/citologia , Músculo Esquelético/efeitos dos fármacos , Músculo Esquelético/metabolismo , NF-kappa B/antagonistas & inibidores , NF-kappa B/genética , NF-kappa B/metabolismo , Interferência de RNA , RNA Interferente Pequeno/metabolismo , Transdução de Sinais/efeitos dos fármacos , Fator de Necrose Tumoral alfa/antagonistas & inibidores , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/metabolismoRESUMO
[Purpose] The purpose of this study was to examine the effects of Taekkyon training on balance control during stair descent in community-dwelling older adults. [Participants and Methods] Participants were randomly assigned to either the Taekkyon group or wellness education group. The participants in the Taekkyon group received Taekkyon training 2 times a week for 12 weeks. The participants in the wellness education group participated in a health education program 1 hour weekly for 12 weeks. Subjects stood in a predetermined position on the top of the custom-built 3-step staircase and then descended the stairs at a self-paced speed. The changes in the translation of the center of pressure before and after Taekkyon training were measured. [Results] The Taekkyon group showed a greater increase in the displacement of the center of pressure in the anteroposterior and mediolateral directions as well as the average velocity of the center of pressure in posttesting than the wellness education group. The Taekkyon group also showed a significant increase in all measures after Taekkyon training. However, little change was found in all measures in the wellness education group. [Conclusion] These findings support the use of Taekkyon training as an effective fall-preventive rehabilitation program to reduce falling in older adults.
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In this study, we investigated the effects of pelargonidin, an anthocyanidin found in many fruits and vegetables, on endothelium-independent vascular contractility to determine the underlying mechanism of relaxation. Isometric contractions of denuded aortic muscles from male rats were recorded, and the data were combined with those obtained in western blot analysis. Pelargonidin significantly inhibited fluoride-, thromboxane A2-, and phorbol ester-induced vascular contractions, regardless of the presence or absence of endothelium, suggesting a direct effect of the compound on vascular smooth muscles via a different pathway. Pelargonidin significantly inhibited the fluoride-dependent increase in the level of myosin phosphatase target subunit 1 (MYPT1) phosphorylation at Thr-855 and the phorbol 12,13-dibutyrate-dependent increase in the level of extracellular signal-regulated kinase (ERK) 1/2 phosphorylation at Thr202/Tyr204, suggesting the inhibition of Rho-kinase and mitogen-activated protein kinase kinase (MEK) activities and subsequent phosphorylation of MYPT1 and ERK1/2. These results suggest that the relaxation effect of pelargonidin on agonist-dependent vascular contractions includes inhibition of Rho-kinase and MEK activities, independent of the endothelial function.
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The present study was undertaken to investigate the influence of hypothermia on endothelium-independent vascular smooth muscle contractility and to determine the mechanism underlying the relaxation. Denuded aortic rings from male rats were used and isometric contractions were recorded and combined with molecular experiments. Hypothermia significantly inhibited fluoride-, thromboxane A2-, phenylephrine-, and phorbol ester-induced vascular contractions regardless of endothelial nitric oxide synthesis, suggesting that another pathway had a direct effect on vascular smooth muscle. Hypothermia significantly inhibited the fluoride-induced increase in pMYPT1 level and phorbol ester-induced increase in pERK1/2 level, suggesting inhibition of Rho-kinase and MEK activity and subsequent phosphorylation of MYPT1 and ERK1/2. These results suggest that the relaxing effect of moderate hypothermia on agonist-induced vascular contraction regardless of endothelial function involves inhibition of Rho-kinase and MEK activities.
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[Purpose] To investigate the effects of a pelvic compression belt (PCB) and chair height on the kinematics and kinetics of the lower extremity during sit-to-stand (STS) maneuvers in healthy people. [Subjects and Methods] Twenty-two people participated in this study. They were required to perform STS maneuvers under four conditions. Hip joint moment and angular displacement of the hip, knee, and ankle were measured. A PCB was also applied below the anterior superior iliac spine. [Results] The angular displacement of the ankle joint increased while performing STS maneuvers from a normal chair with a PCB in phase 1, and decreased during phase 2 when performing STS maneuvers from a high chair. The overall angular displacement in phase 3 was decreased while rising from a chair with a PCB and rising from a high chair. When performed STS maneuvers from a high chair, the angular displacement of the hip, knee, and ankle joint decreased considerably in phase 3. This decreased lower extremity motion in phase 3 indicated that participants required less momentum to complete the maneuver. [Conclusion] The results of this study suggest that a PCB might be appropriate for patients with pelvic girdle pain and lower back pain related to pregnancy.
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Ribosomal S6 kinase is a family of serine/threonine protein kinases involved in the regulation of cell viability. There are two subfamilies of ribosomal s6 kinase, (p90rsk, p70rsk). Especially, p90rsk is known to be an important downstream kinase of p44/42 MAPK. We investigated the role of p90rsk on ethanol-induced cell proliferation of HepG2 cells. HepG2 cells were treated with 10~50 mM of ethanol with or without ERK and p90rsk inhibitors. Cell viability was measured by MTT assay. The expression of pERK1, NHE1 was measured by Western blots. The phosphorylation of p90rsk was measured by ELISA kits. The expression of Bcl-2 was measured by qRT-PCR. When the cells were treated with 10~30 mM of ethanol for 24 hour, it showed significant increase in cell viability versus control group. Besides, 10~30 mM of ethanol induced increased expression of pERK1, p-p90rsk, NHE1 and Bcl-2. Moreover treatment of p90rsk inhibitor attenuated the ethanol-induced increase in cell viability and NHE1 and Bcl-2 expression. In summary, these results suggest that p90rsk, a downstream kinase of ERK, plays a stimulatory role on ethanol-induced hepatocellular carcinoma progression by activating anti-apoptotic factor Bcl-2 and NHE1 known to regulate cell survival.
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Fisetin, a natural flavonoid found in a variety of vegetables and fruits, has been shown to possess many biological functions. The present study was undertaken to investigate the influence of fisetin on vascular smooth muscle contractility and to determine the mechanism involved. Denuded aortic rings from male rats were used and isometric contractions were recorded and combined with molecular experiments. Fisetin significantly relaxed fluoride-, thromboxane A2- or phorbol ester-induced vascular contraction suggesting as a possible anti-hypertensive on the agonist-induced vascular contraction regardless of endothelial nitric oxide synthesis. Furthermore, fisetin significantly inhibited fluoride-induced increases in pMYPT1 levels and phorbol ester-induced increases in pERK1/2 levels suggesting the mechanism involving the inhibition of Rho-kinase activity and the subsequent phosphorylation of MYPT1 and MEK activity and the subsequent phosphorylation of ERK1/2. This study provides evidence regarding the mechanism underlying the relaxation effect of fisetin on agonist-induced vascular contraction regardless of endothelial function.
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The present study was undertaken to investigate the influence of cardamonin on vascular smooth muscle contractility and to determine the mechanism(s) involved. Denuded aortic rings from male rats were used and isometric contractions were recorded and combined with molecular experiments. Cardamonin significantly relaxed fluoride-, phenylephrine-, and phorbol ester-induced vascular contractions, suggesting that it has an anti-hypertensive effect on agonist-induced vascular contraction regardless of endothelial nitric oxide synthesis. Furthermore, cardamonin significantly inhibited the fluoride-induced increase in pMYPT1 level and phenylephrine-induced increase in pERK1/2 level, suggesting inhibition of Rho-kinase and MEK activity and subsequent phosphorylation of MYPT1 and ERK1/2. This study provides evidence that the relaxing effect of cardamonin on agonist-induced vascular contraction regardless of endothelial function involves inhibition of Rho-kinase and MEK activity.
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[Purpose] This study investigated the effects of accuracy constraints (targets) placed on the stepping-limb heel-strike (HS) on the electromyogram (EMG) and ground reaction forces (GRFs) during gait initiation. [Subjects and Methods] Twenty healthy subjects (29.2 ± 2.9â years) were asked to begin walking or stepping over a 10-cm-high obstacle at a fast speed. A 3-cm-diameter target was placed on the ground to dictate the position and accuracy of the stepping-limb HS. [Results] The results showed that the initiation velocity increase in the no-target conditions was due to modulation of the stance- and stepping-limb GRFs and a corresponding increase in the tibialis anterior (TA) activities of both limbs before stepping-limb toe-off. This was achieved by significantly increasing the stepping- and stance-limb TAEMG1 (determined between the onset of movement and time to peak anteroposterior (A-P) GRF of the stepping- and stance- limb) for the no-target conditions. It seems, therefore, that TAEMG1 and the slope to stepping-limb peak A-P GRF contributed to the intended velocity of initiation. [Conclusion] These data indicate that gait initiation and/or stepping over an obstacle may prove to be tasks by which motor control can be measured. The present study provides insight into the working mechanisms of the stepping and stance limbs and shows a clear need to further investigate whether the intact or affected limb should be used to initiate gait during rehabilitation and prosthetic training.
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Shikonin, a natural flavonoid found in the roots of Lithospermum erythrorhizon, has been shown to possess many biological functions. The present study was undertaken to investigate the influence of shikonin on vascular smooth muscle contractility and to determine the mechanism involved. Denuded aortic rings from male rats were used and isometric contractions were recorded and combined with molecular experiments. Shikonin significantly relaxed fluoride-, thromboxane A2- or phorbol ester-induced vascular contraction suggesting as a possible anti-hypertensive on the agonist-induced vascular contraction regardless of endothelial nitric oxide synthesis. Furthermore, shikonin significantly inhibited fluoride-induced increases in pMYPT1 levels and phorbol ester-induced increases in pERK1/2 levels suggesting the mechanism involving the inhibition of Rho-kinase activity and the subsequent phosphorylation of MYPT1 and the inhibition of MEK activity and the subsequent phosphorylation of ERK1/2. This study provides evidence regarding the mechanism underlying the relaxation effect of shikonin on agonist-induced vascular contraction regardless of endothelial function.
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Apigenin, a natural flavonoid found in a variety of vegetables and fruits, has been shown to possess many biological functions. The present study was undertaken to investigate the influence of apigenin on vascular smooth muscle contractility and to determine the mechanism involved. Denuded aortic rings from male rats were used and isometric contractions were recorded and combined with molecular experiments. Apigenin significantly relaxed fluoride-, thromboxane A2 mimetic- or phorbol ester-induced vascular contraction, which suggests that apigenin could be an anti-hypertensive that reduces agonist-induced vascular contraction regardless of endothelial nitric oxide synthesis. Furthermore, apigenin significantly inhibited fluoride-induced increases in pMYPT1 levels and phorbol ester-induced increases in pERK1/2 levels, which suggests the mechanism involving the inhibition of Rho-kinase and MEK activity and the subsequent phosphorylation of MYPT1 and ERK1/2. This study provides evidence regarding the mechanism underlying the relaxation effect of apigenin on agonist-induced vascular contraction regardless of endothelial function.
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The present study was undertaken to investigate the influence of vitexin on vascular smooth muscle contractility and to determine the mechanism involved. Intact or denuded aortic rings from male rats were used and isometric contractions were recorded and combined with molecular experiments. Vitexin more significantly relaxed phorbol ester-induced vascular contraction than thromboxane A2 or fluoride-induced contraction suggesting as a possible anti-hypertensive on the agonist-induced vascular contraction regardless of endothelial nitric oxide synthesis. Furthermore, vitexin significantly inhibited phorbol ester-induced increases in pERK1/2 levels. On the other hand, it did not significantly inhibit thromboxane A2-induced increases in pMYPT1 levels suggesting the mechanism involving the primarily inhibition of MEK activity and the subsequent phosphorylation of ERK1/2. This study provides evidence regarding the mechanism underlying the relaxation effect of vitexin on agonist-induced vascular contraction regardless of endothelial function.
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Apigenina/farmacologia , Músculo Liso Vascular/efeitos dos fármacos , Animais , Aorta Torácica/efeitos dos fármacos , Western Blotting , Ativadores de Enzimas/farmacologia , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Masculino , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Contração Muscular/efeitos dos fármacos , Ésteres de Forbol/farmacologia , Proteína Fosfatase 1/metabolismo , Ratos , Ratos Sprague-Dawley , Fluoreto de Sódio/farmacologia , Tromboxano A2/farmacologia , Quinases Associadas a rho/metabolismoRESUMO
AIMS: Phragmites rhizoma was reported to have anti-oxidative and free radical scavenging activity. It also has been traditionally used to suppress inflammation. In the present study, we aimed to evaluate the topical effects of the polysaccharide-rich extract of P. rhizoma (PEP) on atopic dermatitis. MAIN METHODS: We induced AD-like skin lesions by an extract of the house-dust mite Dermatophagoides farinae (Dfb) in NC/Nga mice, and then performed macroscopic analysis, immunohistochemical staining and measurement of total serum IgE and cytokine production by ELISA. KEY FINDINGS: Topically applied PEP suppressed dermatitis with a decrease in dermatitis score and scratch number. The histological manifestations of atopic skin lesions including thickened epidermis and increased numbers of mast cells, polymorphonuclear leukocytes and nerve fibers were significantly attenuated. The activation of IgE and the levels of cytokines such as IFN-γ IL-4 and IL-10 were also decreased. SIGNIFICANCE: Our results indicated that PEP might have an inhibitory effect on atopic dermatitis-like lesion and be a promising natural resource in the treatment of atopic dermatitis.
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Dermatite Atópica/tratamento farmacológico , Imunoglobulina E/sangue , Extratos Vegetais/farmacologia , Poaceae/química , Polissacarídeos/farmacologia , Animais , Citocinas/metabolismo , Dermatite Atópica/imunologia , Dermatite Atópica/patologia , Dermatophagoides farinae/imunologia , Modelos Animais de Doenças , Ensaio de Imunoadsorção Enzimática , Feminino , Mastócitos/metabolismo , Camundongos , Fibras Nervosas/metabolismo , Neutrófilos/metabolismo , Polissacarídeos/isolamento & purificaçãoRESUMO
The aim of this study was to determine whether an 8-week period of backward walking (BW) training on the treadmill can improve the gross motor function measure (GMFM), weight-bearing symmetry, and temporospatial gait parameters in individuals with spastic cerebral palsy. Twelve participants aged 5-15 years with spastic cerebral palsy participated in this study. The BW training was conducted on a treadmill for up to 20 min, with three sessions per week for 8 consecutive weeks. Before each treadmill training session, lower limb stretching was included in the session. Interlimb differentials of vertical ground reaction force while standing, temporal-distance gait parameters, and scores of dimension D and dimension E of the GMFM were determined. Participants showed statistically significant improvements in a measure of GMFM (P<0.01) and weight-bearing symmetry value (P<0.05), forward walking velocity (P<0.05), and step/stride length (P<0.05 or P<0.01). This pilot study suggests that BW therapy on a treadmill may help to improve walking abilities and other gross motor skills in this sample of patients.
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Paralisia Cerebral/reabilitação , Terapia por Exercício/métodos , Transtornos Neurológicos da Marcha/reabilitação , Adolescente , Paralisia Cerebral/fisiopatologia , Criança , Pré-Escolar , Feminino , Transtornos Neurológicos da Marcha/fisiopatologia , Humanos , Masculino , Projetos Piloto , Caminhada/fisiologiaRESUMO
The present study was undertaken to investigate the influence of eupatilin on vascular smooth muscle contractility and to determine the mechanism involved. Denuded aortic rings from male rats were used and isometric contractions were recorded and combined with molecular experiments. Eupatilin more significantly relaxed fluoride-induced vascular contraction than thromboxane A(2) or phorbol ester-induced contraction suggesting as a possible anti-hypertensive on the agonist-induced vascular contraction regardless of endothelial nitric oxide synthesis. Furthermore, eupatilin significantly inhibited fluoride-induced increases in pMYPT1 levels. On the other hand, it didn't significantly inhibit phorbol ester-induced increases in pERK1/2 levels suggesting the mechanism involving the primarily inhibition of Rho-kinase activity and the subsequent phosphorylation of MYPT1. This study provides evidence regarding the mechanism underlying the relaxation effect of eupatilin on agonist-induced vascular contraction regardless of endothelial function.