RESUMO
Exercise and healthy diet consumption support healthy aging. Schisandra chinensis (Turcz.) also known as "Baill." has anti-inflammatory and antioxidant properties. However, the role of S. chinensis as an antiaging compound has yet to be demonstrated. This study elucidated the antiaging effect of S. chinensis ethanol-hexane extract (C1) and the effect of C1 treatment on muscle and bone following physical exercise in ovariectomized (OVX) rats. RAW 264.7, human diploid fibroblasts (HDFs), C2C12 myoblasts, bone marrow macrophages, and MC3T3-E1 cells were used for in vitro, and muscle and bone of OVX rats were used for in vivo study to demonstrate the effect of C1. The C1 significantly inhibited the expression of inflammatory molecules, ß-galactosidase activity, and improved antioxidant activity via down-regulation of reactive oxygen species in RAW 264.7 and aged HDF cells. The C1 with exercise improved muscle regeneration in skeletal muscle of OVX rats by promoting mitochondrial biogenesis and autophagy. C1 induced osteoblast differentiation, and C1 + exercise modulated the bone formation and bone resorption in OVX rats. C1 exhibited anti-inflammatory, antioxidant, myogenic, and osteogenic effects. C1 with exercise improved age-related muscle wasting and bone loss. Therefore, S. chinensis may be a potential prevent agent for age-related diseases such as sarcopenia and osteoporosis.
Assuntos
Osteoporose/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Sarcopenia/tratamento farmacológico , Schisandra , Animais , Linhagem Celular , Feminino , Frutas , Humanos , Camundongos , Ovariectomia , Ratos Sprague-DawleyRESUMO
Gomisin A from the fruit of Schisandra chinensis has many pharmacological properties, including hepato-protective, anti-diabetic, and anti-oxidative stress. However, the potential benefit of gomisin A is still not well understood, especially in aging progression. Therefore, the aim of this study was to clarify whether the promotion of mitochondrial biogenesis and autophagy of gomisin A affects anti-aging progression, and its mechanism. Intermediate (PD32) human diploid fibroblast (HDF) cells were brought to stress-induced premature senescence (SIPS) using hydrogen peroxide. Gomisin A inhibited reactive oxygen species production even in the SIPS-HDF cells. Gomisin A was also able to attenuate the activity of senescence-associated ß-galactosidase and the production of pro-inflammatory molecules in the SIPS as well as aged HDF cells. The antioxidant activity of gomisin A was determined by recovering the Cu/Zn, Mn-SOD, and HO-1 expression in the SIPS-HDF cells. In mechanistic aspect, gomisin A inhibited the mitogen-activated protein kinase pathway and the translocation of nuclear factor kappa B to the nucleus. In addition, gomisin A promoted the autophagy and mitochondrial biogenesis factors through the translocation of nuclear factor erythroid 2-related factor-2, and inhibited aging progression in the SIPS-HDF cells. In summary, the enhanced properties of mitochondrial biogenesis and autophagy of gomisin A has a benefit to control age-related molecules against SIPS-induced chronic oxidative stress, and gomisin A may be a potential therapeutic compound for the enhancement of intracellular homeostasis to aging progression.
Assuntos
Envelhecimento/efeitos dos fármacos , Ciclo-Octanos/farmacologia , Dioxóis/farmacologia , Diploide , Fibroblastos/citologia , Fibroblastos/efeitos dos fármacos , Lignanas/farmacologia , Biogênese de Organelas , Envelhecimento/metabolismo , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Autofagia/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Regulação para Baixo/efeitos dos fármacos , Fibroblastos/metabolismo , Humanos , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Fator 2 Relacionado a NF-E2/metabolismo , NF-kappa B/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Transporte Proteico/efeitos dos fármacos , Espécies Reativas de Oxigênio/metabolismoRESUMO
The purpose was to evaluate the effects of dienogest on Korean women with endometriosis. A cross-sectional questionnaire-based survey was conducted for 100 premenopausal women. They had taken or were taking 2 mg of dienogest daily. We assessed the pelvic pain score and quality-of-life (QOL) score before and after taking dienogest as well as the prevalence of short-term (≤12 weeks) and long-term adverse effects (>52 weeks). Patients were classified into three groups: dienogest treatment immediately following surgery (A), dienogest treatment for a recurrence of endometriosis after surgery (B), or dienogest treatment without any surgery (C). In groups A and C, the median pain score (from 5 to 0, p <.001; from 7 to 1.5, p <.001) and median QOL score (from 10 to 5, p = .002; from 7.5 to 6.5, p = .008) were significantly decreased. Irregular bleeding and decreased menstrual flow were more prevalent in patients with dienogest intake of fewer than 12 weeks, while amenorrhea, weight gain, hair loss, and dorsal pain were more prevalent in patients with dienogest treatment of over 52 weeks. Accordingly, proper counseling is necessary when prescribing dienogest.
Assuntos
Endometriose/tratamento farmacológico , Nandrolona/análogos & derivados , Adulto , Alopecia/induzido quimicamente , Estudos Transversais , Depressão/induzido quimicamente , Endometriose/cirurgia , Feminino , Humanos , Menstruação/efeitos dos fármacos , Distúrbios Menstruais/induzido quimicamente , Pessoa de Meia-Idade , Nandrolona/efeitos adversos , Nandrolona/uso terapêutico , Dor Pélvica , Pré-Menopausa , Qualidade de Vida , Recidiva , República da Coreia , Inquéritos e Questionários , Fatores de Tempo , Aumento de Peso/efeitos dos fármacosRESUMO
The methanol extract from the aerial parts of Dictamnus albus was active in inhibiting monoamine oxidase (MAO) from the mouse brain. Activity-guided fractionation led to the isolation of four known coumarins, 7-(6'R-hydroxy-3', 7'-dimethyl-2'E, 7'-octadienyloxy) coumarin (1), auraptene (2), umbelliferone (3), and xanthotoxin (4), as active compounds along with an inactive alkaloid, skimmianine (5). Compounds 1 and 2 inhibited MAO activity in a concentration-dependent manner with IC50 values of 0.7 and 1.7 microM, respectively. Compounds 1 and 2 showed a slight and potently selective inhibitory effect against MAO-B (IC50 0.5 and 0.6 microM, respectively) compared to MAO-A (IC50 1.3 and 34.6 microM, respectively). According to kinetic analyses derived by Lineweaver-Burk reciprocal plots, compounds 1 and 2 exhibited a competitive inhibition to MAO-B.
Assuntos
Cumarínicos/farmacologia , Dictamnus/química , Inibidores da Monoaminoxidase , Animais , Encéfalo/efeitos dos fármacos , Encéfalo/enzimologia , Clorgilina/farmacologia , Relação Dose-Resposta a Droga , Técnicas In Vitro , Cinética , Espectroscopia de Ressonância Magnética , Camundongos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/enzimologia , Monoaminoxidase/metabolismo , Selegilina/farmacologia , Espectrofotometria Infravermelho , Espectrofotometria UltravioletaRESUMO
The neutral cluster beam deposition (NCBD) method has been applied to produce and characterize organic thin-film transistors (OTFTs) based upon tetracene and pentacene molecules as active layers. Organic thin films were prepared by the NCBD method on hexamethyldisilazane (HMDS)-untreated and -pretreated silicon dioxide (SiO2) substrates at room temperature. The surface morphology and structures for the tetracene and pentacene thin films were examined by atomic force microscopy (AFM) and X-ray diffraction (XRD). The measurements demonstrate that the weakly bound and highly directional neutral cluster beams are efficient in producing high-quality single-crystalline thin films with uniform, smooth surfaces and that SiO2 surface treatment with HMDS enhances the crystallinity of the pentacene thin-film phase. Tetracene- and pentacene-based OTFTs with the top-contact structure showed typical source-drain current modulation behavior with different gate voltages. Device parameters such as hole carrier mobility, current on/off ratio, threshold voltage, and subthreshold slope have been derived from the current-voltage characteristics together with the effects of surface treatment with HMDS. In particular, the high field-effect room-temperature mobilities for the HMDS-untreated OTFTs are found to be comparable to the most widely reported values for the respective untreated tetracene and pentacene thin-film transistors. The device performance strongly correlates with the surface morphology, and the structural properties of the organic thin films are discussed.
RESUMO
A methylene chloride soluble fraction of the fruits of Cudrania tricuspidata significantly inhibited the mouse brain monoamine oxidase (MAO). Three known prenylated isoflavones were isolated and identified by activity-guided fractionation. Gancaonin A (1), 4'-O-methylalpinumisoflavone (2), and alpinumisoflavone (3) inhibited MAO activity in a concentration-dependent manner with IC50 values of 19.4, 23.9, and 25.8 microM, respectively. Of these, gancaonin A (1) showed a selective and potent inhibitory effect against MAO-B (IC50 0.8 microM) than MAO-A (IC50 >800 microM). The kinetic analysis using Lineweaver-Burk plots indicated that gancaonin A (1) competitively inhibited MAO-B.