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1.
ACS Appl Mater Interfaces ; 16(12): 15143-15155, 2024 Mar 27.
Artigo em Inglês | MEDLINE | ID: mdl-38481099

RESUMO

Realizing controllable input of botanical pesticides is conducive to improving pesticide utilization, reducing pesticide residues, and avoiding environmental pollution but is extremely challenging. Herein, we constructed a smart pesticide-controlled release platform (namely, SCRP) for enhanced treatment of tobacco black shank based on encapsulating honokiol (HON) with mesoporous hollow structured silica nanospheres covered with pectin and chitosan oligosaccharide (COS). The SCRP has a loading capacity of 12.64% for HON and could effectively protect HON from photolysis. Owing to the pH- and pectinase-sensitive property of the pectin, the SCRP could smartly release HON in response to a low pH or a rich pectinase environment in the black shank-affected area. Consequently, the SCRP effectively inhibits the infection of P. nicotianae on tobacco with a controlled rate for tobacco black shank of up to 87.50%, which is mainly due to the SCRP's capability in accumulating ROS, changing cell membrane permeability, and affecting energy metabolism. In addition, SCRP is biocompatible, and the COS layer enables SCRP to show a significant growth-promoting effect on tobacco. These results indicate that the development of a stimuli-responsive controlled pesticide release system for plant disease control is of great potential and value for practical agriculture production.


Assuntos
Praguicidas , Praguicidas/farmacologia , Preparações de Ação Retardada/farmacologia , Preparações de Ação Retardada/química , Poligalacturonase , Agricultura , Pectinas
2.
Meat Sci ; 210: 109436, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38266434

RESUMO

Plant extracts are commonly used as feed additives to improve pork quality. However, due to their high cost, shortening the duration of supplement use can help reduce production costs. In this study, we aimed to investigate the effects of grape seed proanthocyanidin extract (GSPE) on meat quality and muscle fiber characteristics of finishing pigs during the late stage of fattening, which was 30 days in our experimental design. The results indicated that short-term dietary supplementation of GSPE significantly reduced backfat thickness, but increased loin eye area and improved meat color and tenderness. Moreover, GSPE increased slow myosin heavy chain (MyHC) expression and malate dehydrogenase (MDH) activity, while decreasing fast MyHC expression and lactate dehydrogenase (LDH) activity in the Longissimus thoracis (LT) muscle. Additionally, GSPE increased the expression of Sirt1 and PGC-1α proteins in the LT muscle of finishing pigs and upregulated AMP-activated protein kinase α 1 (AMPKα1), AMPKα2, nuclear respiratory factor 1 (NRF1), and calcium/calmodulin-dependent protein kinase kinase ß (CaMKKß) mRNA expression levels. These findings suggest that even during the late stage of fattening, GSPE treatment can regulate skeletal muscle fiber type transformation through the AMPK signaling pathway, thereby affecting the muscle quality of finishing pigs. Therefore, by incorporating GSPE into the diet of pigs during the late stage of fattening, producers can enhance pork quality while reducing production costs.


Assuntos
Extrato de Sementes de Uva , Carne de Porco , Proantocianidinas , Carne Vermelha , Suínos , Animais , Fibras Musculares Esqueléticas/metabolismo , Extrato de Sementes de Uva/farmacologia , Suplementos Nutricionais , Músculo Esquelético/metabolismo
3.
Biomech Model Mechanobiol ; 23(1): 241-254, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-37861916

RESUMO

Pulsed electric fields are extensively utilized in clinical treatments, such as subthalamic deep brain stimulation, where electric field loading is in direct contact with brain tissue. However, the alterations in brain tissue's mechanical properties and microstructure due to changes in electric field parameters have not received adequate attention. In this study, the mechanical properties and microstructure of the brain tissue under pulsed electric fields were focused on. Herein, a custom indentation device was equipped with a module for electric field loading. Parameters such as pulse amplitude and frequency were adjusted. The results demonstrated that following an indentation process lasting 5 s and reaching a depth of 1000 µm, and a relaxation process of 175 s, the average shear modulus of brain tissue was reduced, and viscosity decreased. At the same amplitude, high-frequency pulsed electric fields had a smaller effect on brain tissue than low-frequency ones. Furthermore, pulsed electric fields induced cell polarization and reduced the proteoglycan concentration in brain tissue. As pulse frequency increased, cell polarization diminished, and proteoglycan concentration decreased significantly. High-frequency pulsed electric fields applied to brain tissue were found to reduce impedance fluctuation amplitude. This study revealed the effect of pulsed electric fields on the mechanical properties and microstructure of ex vivo brain tissue, providing essential information to promote the advancement of brain tissue electrotherapy in clinical settings.


Assuntos
Encéfalo , Eletricidade , Animais , Suínos , Viscosidade , Impedância Elétrica , Proteoglicanas
4.
Sci Total Environ ; 912: 168749, 2024 Feb 20.
Artigo em Inglês | MEDLINE | ID: mdl-38007120

RESUMO

Rehabilitation of degraded soil health using high-performance and sustainable measures are urgently required for restoring soil primary productivity and mitigating greenhouse gas (GHG) emission of coastal ecosystems. However, the effect of livestock manure derived hydrochar on GHG emission and plant productivity in the coastal salt-affected soils, one of blue carbon (C) ecosystems, was poorly understood. Therefore, a cattle manure hydrochar (CHC) produced at 220 °C was prepared to explore its effects and mechanisms on CH4 and N2O emissions and tomato growth and fruit quality in a coastal soil in comparison with corresponding hydrochars derived from plant straws, i.e., sesbania straw hydrochars (SHC) and reed straw hydrochars (RHC) using a 63-day soil column experiment. The results showed that CHC posed a greater efficiency in reducing the global warming potential (GWP, 54.6 % (36.7 g/m2) vs. 45.5-45.6 % (22.2-30.6 g/m2)) than those of RHC and SHC. For the plant growth, three hydrochars at 3 % (w/w) significantly increased dry biomass of tomato shoot and fruit by 12.4-49.5 % and 48.6-165 %, respectively. Moreover, CHC showed the highest promotion effect on shoot and fruit dry biomass of tomato, followed by SHC ≈ RHC. Application of SHC, CHC and RHC significantly elevated the tomato sweetness compared with CK, with the order of CHC (54.4 %) > RHC (35.6 %) > SHC (22.1 %). Structural equation models revealed that CHC-depressed denitrification and methanogen mainly contributed to decreased GHG emissions. Increased soil phosphorus availability due to labile phosphorus supply from CHC dominantly accounted for elevated tomato growth and fruit production. Comparably, SHC-altered soil properties (e.g., decreased pH and increased total carbon content) determined variations of GHG emission and tomato growth. The findings provide the high-performance strategies to enhance soil primary productivity and mitigate GHG emissions in the blue C ecosystems.


Assuntos
Gases de Efeito Estufa , Solanum lycopersicum , Bovinos , Animais , Solo , Gases de Efeito Estufa/análise , Esterco , Ecossistema , Dióxido de Carbono/análise , Óxido Nitroso/análise , Metano/análise , Fertilizantes/análise , Carbono , Fósforo , Agricultura/métodos
5.
Bioresour Technol ; 378: 129010, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-37011842

RESUMO

A combined chemical-bacterial process was developed to convert vegetable straw waste to high value antifungal iturins. Straws from three widely cultivated vegetable (cucumber, tomato and pepper) were evaluated as feedstocks for iturin production. Microwave assisted hydrolysis with very dilute acid (0.2% w/w H2SO4) achieved efficient reducing sugar recovery. The high glucose concentration in non-detoxified hydrolysate from pepper straw facilitated the optimal growth of Bacillus amyloliquefaciens strain Cas02 and stimulated the production of iturin. The fermentation parameters were optimised to enhance the iturin production efficiency. The obtained fermentation extract was further purified using macroporous adsorption resin, resulting in an iturin-rich extract that exhibited strong antifungal activity against Alternaria alternata with an IC50 of 176.44 µg/mL. Each iturin homologue was identified using NMR. Overall, 1.58 g iturin-rich extract containing 164.06 mg/g iturins was obtained from 100 g pepper straw, illustrating the great potential of valorising pepper straw via this process.


Assuntos
Antifúngicos , Bacillus amyloliquefaciens , Antifúngicos/farmacologia , Antifúngicos/química , Verduras/metabolismo , Bacillus amyloliquefaciens/metabolismo , Fermentação , Extratos Vegetais , Peptídeos Cíclicos/química , Peptídeos Cíclicos/metabolismo
6.
ACS Biomater Sci Eng ; 8(12): 5349-5360, 2022 Dec 12.
Artigo em Inglês | MEDLINE | ID: mdl-36346997

RESUMO

Electrotherapy plays a crucial role in regulating neuronal activity. Nevertheless, the relevant therapeutic mechanisms are still unclear; thus, the effects of electric fields on brain tissue's mechanical properties and microstructure need to be explored. In this study, focusing on the changes in mechanical properties and microstructure of ex vivo porcine brain tissues under different types of electric fields, directional and alternating electric fields (frequencies of 5, 20, 50, and 80 Hz, respectively) integrate with a custom-designed indentation device. The experimental results showed that for the ex vivo brain tissue, the directional electric field (DEF) can reduce the elastic properties of brain tissue. Simultaneously, the DEF can increase the cell spacing and reduce the proteoglycan content. The transmission electron microscope (TEM) analysis observed that the DEF can reduce the integrity of the plasma membrane, the endoplasmic reticulum's stress response, and the myelin lamella's separation. The alternating electric field (AEF) can accelerate the stress relaxation process of brain tissue and change the time-dependent mechanical properties of brain tissue. Meanwhile, with the increase in frequency, the cell spacing decreased, and the proteoglycan content gradually approached the control group without electric fields. TEM analysis observed that with the increase in frequency, the integrity of the plasma membrane increases, and the separation of the myelin lamella gradually disappears. Understanding the changes in the mechanical properties and microstructure of brain tissue under AEF and DEF enables a preliminary exploration of the therapeutic mechanism of electrotherapy. Simultaneously, the essential data was provided to support the development of embedded electrodes. In addition, the ex vivo experiments build a solid foundation for future in vivo experiments.


Assuntos
Encéfalo , Proteoglicanas , Animais , Suínos , Encéfalo/fisiologia
7.
Plant Physiol Biochem ; 167: 816-830, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34530326

RESUMO

Apocynum venetum is a traditional Chinese medicinal herb with tolerance to various abiotic stresses, especially, salinity. However, only a few studies have investigated the salt-tolerant mechanism of this non-halophyte under salt stress at phenotypic and physiological levels. To explore the molecular mechanism of salinity tolerance in A. venetum, the global transcriptome profiles of seedling leaves under different salt-stress durations, using 200 mM NaCl, were analyzed. De novo assembly of approximately 715 million high-quality reads and approximately 105.61 Gb sequence data was performed. In total, 2822 differentially expressed genes (DEGs) were identified. DEGs were significantly enriched in flavonoid metabolism-related pathways such as "flavonoid biosynthesis" and "phenylpropanoid biosynthesis". Most of these DEGs were downregulated under salt stress. However, genes encoding the non-selective cation channels and antioxidants were upregulated under salt stress, whereas most cell wall-related DEGs were downregulated. Consequently, the concentration of flavonoids decreased, whereas that of Na+ increased with exposure time. Thus, we hypothesized that the accumulation of Na+ in the leaves, which resulted in reduced flavonoid concentration under salt stress, directly led to a decrease in the salt tolerance of A. venetum. This was verified by overexpressing four flavonoid synthesis pathway genes in Arabidopsis. The transgenic plants showed higher salt tolerance than the wild-type plants due to the accumulation of total flavonoids. These physiological and transcriptome analyses of A. venetum revealed major molecular underpinnings contributing to the responses of A. venetum to salt stress, thereby improving our understanding of the molecular mechanisms underlying salt tolerance in A. venetum and plants in general. The findings serve as a basis for functional studies on and engineering strategies for plant salinity tolerance.


Assuntos
Apocynum , Tolerância ao Sal , Apocynum/genética , Perfilação da Expressão Gênica , Regulação da Expressão Gênica de Plantas , Estresse Salino , Tolerância ao Sal/genética , Transcriptoma
8.
Biomed Pharmacother ; 127: 110182, 2020 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-32361160

RESUMO

Diabetes is one of the most concerned metabolic diseases worldwide and threaten public health. In the present work, two polysaccharide-rich extracts from Apocynum venetum leaves were extracted using distilled water and alkaline solution (0.05 M NaOH), and fully characterized. Hypoglycemic and hypolipidemic effects of two polysaccharide-rich extracts on high-fat diet and streptozocin-induced type 2 diabetic mice were investigated. Treatment of alkaline extracted polysaccharide-rich products significantly decreased the levels of fasting blood glucose, serum insulin, glycated serum protein, as well as serum lipids profiles including total cholesterol, triacylglycerols, low-density lipoprotein cholesterol, and nonesterified fatty acid. Meanwhile, the reduced glycogen contents in liver were prominently improved, and the oxidative damage were markedly ameliorated by alkaline extracted polysaccharide products in diabetic mice. Furthermore, both polysaccharide-rich extracts could reverse the gut microbiota dysbiosis in diabetic mice by increasing the abundance of genera Odoribacter, Anaeroplasma, Parasutterella, and Muribaculum; while by decreasing the abundance of genera Enterococcus, Klebsiella, and Aerococcus. This study provides new sights for exploitation of Apocynum venetum extracts as a promising anti-diabetic nutraceutical for the treatment of type 2 diabetes and metabolic syndrome.


Assuntos
Apocynum/química , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Extratos Vegetais/farmacologia , Polissacarídeos/farmacologia , Animais , Glicemia/efeitos dos fármacos , Diabetes Mellitus Experimental/fisiopatologia , Diabetes Mellitus Tipo 2/fisiopatologia , Dieta Hiperlipídica , Microbioma Gastrointestinal/efeitos dos fármacos , Hipolipemiantes/isolamento & purificação , Hipolipemiantes/farmacologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Folhas de Planta , Polissacarídeos/isolamento & purificação , Estreptozocina
9.
J Agric Food Chem ; 67(45): 12472-12480, 2019 Nov 13.
Artigo em Inglês | MEDLINE | ID: mdl-31642672

RESUMO

Brown macroalgae are an important source of polyphenols with multiple health functions. In this work, polyphenol extracts from Lessonia trabeculate were purified and investigated for the antidiabetic activity in vitro and in vivo. The purified polyphenol extracts exhibited good antioxidant activities, α-glucosidase and lipase inhibition activities (IC50 < 0.25 mg/mL). The HPLC-DAD-ESI-MS/MS analysis indicated that the compounds in polyphenol extracts were mainly phlorotannin derivatives, phenolic acid derivatives, and gallocatechin derivatives. In vivo, C57BL/6J rats treated with polyphenol extracts for 4 weeks had lower fasting blood glucose levels, insulin levels, as well as better serum lipid profiles and antioxidant stress parameters, compared with the diabetic control (DC) group. Histopathology revealed that polyphenol extracts preserved the architecture and function of the liver. Short-chain fatty acid contents in rats' fecal samples with polyphenols administration were significantly recovered as compared with the DC group. Furthermore, the gut microflora of rats was investigated with high-throughput 16S rRNA gene sequencing and results indicated that polyphenol extracts had a positive effect on regulating the dysbiosis of the microbial ecology in diabetic rats. All of the results from the study provided a scientific reference of the potentially beneficial effects of L. trabeculate polyphenols on diabetes management.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Microbioma Gastrointestinal/efeitos dos fármacos , Hiperglicemia/tratamento farmacológico , Hipoglicemiantes/administração & dosagem , Phaeophyceae/química , Extratos Vegetais/administração & dosagem , Polifenóis/administração & dosagem , Alga Marinha/química , Animais , Glicemia/metabolismo , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Experimental/microbiologia , Dieta Hiperlipídica/efeitos adversos , Humanos , Hiperglicemia/metabolismo , Hiperglicemia/microbiologia , Masculino , Camundongos Endogâmicos C57BL , Ratos , Estreptozocina/efeitos adversos
10.
Biomolecules ; 9(10)2019 09 21.
Artigo em Inglês | MEDLINE | ID: mdl-31546663

RESUMO

Flos Chrysanthemi indici, an important medicinal and aromatic plant in China, is considered to have many different preservative and pharmacological properties. Considering the capability of essential oils (EOs), the present study is conducted to compare different extraction methods in order to improve yield and biological activities. Hydro-distillation (HD), steam-distillation (SD), solvent-free microwave extraction (SFME), and supercritical fluid extraction (SFE) are employed to prepare EOs from Flos Chrysanthemi indici. A total of 71 compounds are assigned by gas chromatography/mass spectrometry (GC-MS) in comparison with retention indices. These include 32 (HD), 16 (SD), 31 (SFME) and 38 (SFE) compounds. Major constituents of EOs differ according to the extraction methods were heptenol, tricosane, camphor, borneol, and eucalyptol. EOs extracted by SFME exhibit higher antioxidant activity. All EOs show varying degrees of antimicrobial activity, with minimum inhibitory concentration (MIC) ranging from 0.0625 to 0.125 mg/mL and SFME and SFE prove to be efficient extraction methods. EOs alter the hyphal morphology of Alternaria alternata, with visible bumps forming on the mycelium. Overall, these results indicate that the extraction method can significantly influence the composition and biological activity of EOs and SFME and SFE are outstanding methods to extract EOs with high yield and antimicrobial activity.


Assuntos
Fracionamento Químico/métodos , Chrysanthemum/química , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Flores/química , Cromatografia Gasosa-Espectrometria de Massas , Hifas/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Micro-Ondas , Óleos de Plantas/química
11.
Food Res Int ; 113: 288-297, 2018 11.
Artigo em Inglês | MEDLINE | ID: mdl-30195523

RESUMO

Four economically important brown algae species (Ascophyllum nodosum, Laminaria japonica, Lessonia trabeculate and Lessonia nigrecens) were investigated for phenolic compound extraction and evaluated for their antioxidant, anti-hyperglycemic, and pancreatic lipase and tyrosinase inhibition activities. Microwave assisted extraction (MAE) at 110 °C for 15 min resulted in both higher crude yield and higher total phenolic content (TPC) for all algae species compared with those obtained by conventional extraction at room temperature for 4 h, and Ascophyllum nodosum yielded the highest TPC. Antioxidant tests indicated that extracts acquired by MAE from four species all exhibited higher DPPH, ABTS free radical scavenging ability and reducing power than the conventional method. The extract of Lessonia trabeculate exhibited good α-amylase, α-glucosidase, pancreatic lipase, and tyrosinase inhibition activities, and the MAE extract showed even better α-glucosidase inhibitory activity than acarbose.


Assuntos
Fracionamento Químico/métodos , Inibidores Enzimáticos , Phaeophyceae/química , Extratos Vegetais , Alga Marinha/química , Antioxidantes/química , Antioxidantes/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Lipase/antagonistas & inibidores , Micro-Ondas , Monofenol Mono-Oxigenase/antagonistas & inibidores , Extratos Vegetais/química , Extratos Vegetais/farmacologia
12.
J Pediatr Orthop B ; 24(1): 35-9, 2015 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-25305044

RESUMO

This study evaluates improvement of the acetabular index (AI) in patients with developmental dysplasia of the hip at 4 years after closed reduction, and determines the association between the final AI and a set of factors. Sixty-two patients (74 hips) treated with closed reduction were categorized into three groups according to age: group A (0-12 months, 18 hips), group B (13-18 months, 24 hips), and group C (>18 months, 32 hips). There was no difference in AI among the three groups before reduction (P=0.293). In groups A and C, the AI decreased significantly over time until 3 years after reduction and no differences were observed between the time points of 3 and 4 years. At 4 years after reduction, the AI of group C was significantly higher than that of groups A (P<0.001) and B (P=0.012). The overall AI improvement rate was 28.63%. The AI improvement rate of group A was significantly higher than that of group C (P=0.005). Pearson correlation analysis indicated no correlation between center-head distance discrepancy and the final AI (P=0.811). Linear regression suggested that age and initial AI correlated significantly with the final AI (R=0.617, F=15.031, P<0.001). Other factors, such as sex, center-edge angle of Wiberg, bilaterally involved, and avascular necrosis of the femoral head, showed no correlations with the final AI (P>0.05). According to the coefficients, initial AI (ß1=0.432, P<0.001) had greater effect than age (ß2=0.197, P=0.023) on the final AI. In conclusion, the AI decreases in all patients after reduction and stabilizes at 3 years after reduction. The AI improvement rate is correlated negatively with age. Age and initial AI are early predictors of the progress of AI after closed reduction in developmental dysplasia of the hip patients.


Assuntos
Acetábulo/crescimento & desenvolvimento , Diagnóstico Tardio , Luxação Congênita de Quadril/diagnóstico , Luxação Congênita de Quadril/terapia , Manipulações Musculoesqueléticas/métodos , Análise de Variância , Feminino , Luxação Congênita de Quadril/fisiopatologia , Humanos , Lactente , Recém-Nascido , Masculino , Análise de Regressão , Estudos Retrospectivos
13.
Calcif Tissue Int ; 93(5): 481-6, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-23897224

RESUMO

This study compared the effects of alendronate (ALN) and strontium ranelate (SR) on bone mineral density (BMD), bone histomorphometry, and biomechanics in ovariectomized (OVX) rats. We randomly assigned 48 3-month-old female Sprague-Dawley rats to four groups: sham, OVX, ALN, and SR. Rats in the OVX, ALN, and SR groups received bilateral OVX. Rats in the ALN and SR groups were orally administrated ALN (7 mg/kg/week) and SR (500 mg/kg/day). Rats in the sham and OVX groups were treated with saline. All treatments continued for 12 weeks. Femoral BMD examination, distal femoral bone histomorphometry analysis, and biomechanical tests at the femoral diaphysis and metaphysis were performed to evaluate the effects of treatments in OVX rats. Results showed that both ALN and SR significantly increased femoral BMD (total femur, diaphyseal BMD, and distal metaphyseal BMD), distal femoral bone histomorphometric parameters (BV/TV, Tb.N, and Tb.Th), and femoral biomechanical parameters (maximum load, failure load, stiffness) compared with the OVX group (P < 0.05). No differences were found between ALN and SR in increasing femoral BMD, distal femoral bone histomorphometric parameters (BV/TV, Tb.N, and Tb.Th), and femoral diaphysis biomechanical parameters (maximum load, failure load, stiffness) (P > 0.05). The SR group was inferior to the ALN group in femoral metaphysis biomechanical parameters (P < 0.05). In conclusion, ALN (7 mg/kg/week) and SR (500 mg/kg/day) have similar effects by increasing BMD, distal femoral bone histomorphometric parameters, and femoral metaphysis biomechanical properties. Although ALN has greater effects than SR on distal femoral metaphysis biomechanical properties, in general, ALN and SR have comparable effects on the femur in OVX rats.


Assuntos
Alendronato/farmacologia , Conservadores da Densidade Óssea/farmacologia , Fêmur/efeitos dos fármacos , Tiofenos/farmacologia , Animais , Fenômenos Biomecânicos/efeitos dos fármacos , Densidade Óssea/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Feminino , Fêmur/anatomia & histologia , Fêmur/ultraestrutura , Ovariectomia , Ratos , Ratos Sprague-Dawley
14.
Zhongguo Gu Shang ; 22(4): 271-3, 2009 Apr.
Artigo em Chinês | MEDLINE | ID: mdl-19408755

RESUMO

OBJECTIVE: To investigate the molecular mechanism of TFE (total flavone of epimedium) in the treatment of osteoporosis, and then provide experimental evidence for modernization and further development of TFE as an traditional Chinese medicine. METHODS: Sixty healthy female SD rats with aged 4 months were randomly divided into three groups (including control group in which rats received sham surgery, OVX group in which ovariectomized rats didn't give any medicine after the removal of ovaries and TFE group in which ovariectomized rats administrated TFE), 20 rats in each group. Compared bone mineral density (BMD) between before operation and at 4th week after operation in order to verify the establishment of osteoporotic model (criteria: BMD decreased more than 20% at 4th week after operation). The rats in TEF group were administrated total flavone of epimedium(concentration 30 mg/ml, 10 ml/kg, qd) orally for 4 weeks. After this, killed rats to harvest the lower part of the femur and detected BMD again. Applying the reverse transcriptase-polymerase chain reaction technique (RT-PCR) to detect expression of OPG, OPGL mRNA in bone tissue. RESULTS: (1) At 4th week after ovariectomy, the mean BMD of lumbar vertebra in TFE group fell to (0.084 +/- 0.020) g/cm2. Administrated with TFE for 4 weeks,the BMD increased to (0.112 +/- 0.009) g/cm2. There was significant improvement compare with the OVX group (P < 0.05). (2) Compared between OVX group and TFE group, The OPG mRNA expression of TFE group obviously enhanced. There was significant difference in statistics (P < 0.05). However,the promotion for OPGL mRNA expression were detected between OVX group and TFE group,there was no significant difference in statistics (P > 0.05). CONCLUSION: This study showed that TFE could inhibit differentiation and maturation of osteoclast through enhancing OPG mRNA expression, accordingly,to treat osteoporosis.


Assuntos
Epimedium/química , Flavonoides/farmacologia , Regulação da Expressão Gênica/efeitos dos fármacos , Osteoprotegerina/genética , Ovariectomia , Ligante RANK/genética , Animais , Densidade Óssea/efeitos dos fármacos , Medicamentos de Ervas Chinesas/farmacologia , Feminino , Flavonas , Osteoblastos/efeitos dos fármacos , Osteoblastos/metabolismo , Osteoblastos/fisiologia , RNA Mensageiro/genética , RNA Mensageiro/metabolismo , Ratos
15.
Chem Biodivers ; 4(7): 1586-93, 2007 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-17638340

RESUMO

The clerodane diterpenoid salvinorin A (1), the main active component of the psychotropic herb Salvia divinorum, has been reported to be a potent agonist at the kappa-opioid receptor. Computer modeling suggested that splendidin (2) from S. splendens, as well as related compounds, might possess similar activities. In the present study, this hypothesis was tested by determination of the binding properties of a series of structural congeners, compounds 2-8, at the mu-, delta-, and kappa-opioid receptors. However, none of these compounds showed significant binding to any of the opioid-receptor subtypes, thus disproving the above hypothesis. The novel compounds 7 and 8 were obtained semi-synthetically by selective modification of salvifarin (5), isolated from Salvia farinacea, upon epoxide-ring opening with AcOH in the presence of indium(III) triflate. Also, the X-ray crystal structure of salvifaricin (6; Fig.), obtained from S. farinacea, was determined for the first time and used, in combination with in-depth NMR experiments, to elucidate the absolute configurations of the new products. Our experiments demonstrate that the relatively well-accessible diterpenoid 6 could be used as starting material for future studies into the structure-activity relationship at the kappa-opioid receptor.


Assuntos
Analgésicos Opioides/isolamento & purificação , Diterpenos Clerodânicos/isolamento & purificação , Diterpenos/isolamento & purificação , Receptores Opioides kappa/agonistas , Salvia , Analgésicos Opioides/química , Analgésicos Opioides/farmacologia , Animais , Células CHO , Linhagem Celular Tumoral , Cricetinae , Cricetulus , Diterpenos/química , Diterpenos/farmacologia , Diterpenos Clerodânicos/química , Diterpenos Clerodânicos/farmacologia , Humanos , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia
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