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1.
Gastroenterol Rep (Oxf) ; 11: goad054, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37705510

RESUMO

Background: Metabolic dysfunction-associated fatty liver disease (MAFLD) is a common liver disease, the risk of which can be increased by poor diet. The objective of this study was to evaluate the associations between food items and MAFLD, and to propose reasonable dietary recommendations for the prevention of MAFLD. Methods: Physical examination data were collected from April 2015 through August 2017 at Nanping First Hospital (n = 3,563). Dietary intakes were assessed using a semi-quantitative food frequency questionnaire. The association between food intake and the risk of MAFLD was assessed by using the inverse probability weighted propensity score. Results: Beverages (soft drinks and sugar-sweetened beverages) and instant noodles were positively associated with MAFLD risk, adjusting for smoking, drinking, tea intake, and weekly hours of physical activity [adjusted odds ratio (ORadjusted): 1.568; P = 0.044; ORadjusted: 4.363; P = 0.001]. Milk, tubers, and vegetables were negatively associated with MAFLD risk (ORadjusted: 0.912; P = 0.002; ORadjusted: 0.633; P = 0.007; ORadjusted: 0.962; P = 0.028). In subgroup analysis, the results showed that women [odds ratio (OR): 0.341, 95% confidence interval (CI): 0.172-0.676] had a significantly lower risk of MAFLD through consuming more tubers than men (OR: 0.732, 95% CI: 0.564-0.951). Conclusions: These findings suggest that reducing consumption of beverages (soft drinks and sugar-sweetened beverages) and instant noodles, and consuming more milk, vegetables, and tubers may reduce the risk of MAFLD.

2.
Eur J Med Chem ; 258: 115544, 2023 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-37300915

RESUMO

Heterocycles are common in the structure of drugs used clinically to deal with diseases. Such drugs usually contain nitrogen, oxygen and sulfur, which possess electron-accepting capacity and can form hydrogen bonds. These properties often bring enhanced target binding ability to these compounds when compared to alkanes. Pyrazine is a nitrogen-containing six-membered heterocyclic ring and many of its derivatives are identified as bioactive molecules. We review here the most active pyrazine compounds in terms of their structure, activity in vitro and in vivo (mainly antitumor activity) and the reported mechanisms of action. References have been downloaded through Web of Science, PubMed, Science Direct, Google Scholar and SciFinder Scholar. Publications reporting only the chemistry of pyrazine derivatives are beyond the scope of this review and have not been included. We found that compounds in which a pyrazine ring was fused into other heterocycles especially pyrrole or imidazole were the highly studied pyrazine derivatives, whose antineoplastic activity had been widely investigated. To the best of our knowledge, this is the first review of pyrazine derivatives and their bioactivity, especially their antitumor activity. This review should be useful for those engaged in development of medications based on heterocyclic compounds especially those based on pyrazine.


Assuntos
Antineoplásicos , Compostos Heterocíclicos , Pirazinas/farmacologia , Pirazinas/química , Compostos Heterocíclicos/farmacologia , Antineoplásicos/farmacologia , Antineoplásicos/química , Nitrogênio
3.
Bioorg Med Chem ; 82: 117234, 2023 03 15.
Artigo em Inglês | MEDLINE | ID: mdl-36906964

RESUMO

Cancer with low survival rates is the second main cause of death among all diseases in the world and consequently, effective antineoplastic agents are urgently needed. Allosecurinine is a plant-derived indolicidine securinega alkaloid shown bioactivity. The object of this study is to investigate synthetic allosecurinine derivatives with considerable anticancer capacity against nine human cancer cell lines as well as mechanism of action. We synthesized twenty-three novel allosecurinine derivatives and evaluated their antitumor activity against nine cancer cell lines for 72 h by MTT and CCK8 assays. FCM was applied to analyze the apoptosis, mitochondrial membrane potential, DNA content, ROS production, CD11b expression. Western blot was selected to analyze the protein expression. Structure-activity relationships were established and potential anticancer lead BA-3 which induced differentiation of leukemia cells towards granulocytosis at low concentration and apoptosis at high concentration was identified. Mechanism studies showed that mitochondrial pathway mediated apoptosis within cancer cells with cell cycle blocking was induced by BA-3. In addition, western blot assays revealed that BA-3 induced expression of the proapoptotic factor Bax, p21 and reduced the levels of antiapoptotic protein such as Bcl-2, XIAP, YAP1, PARP, STAT3, p-STAT3, and c-Myc. Collectively, BA-3 was a lead compound for oncotherapy at least in part, through the STAT3 pathway. These results were an important step in further studies on allosecurinine-based antitumor agent development.


Assuntos
Alcaloides , Antineoplásicos , Compostos Heterocíclicos de Anel em Ponte , Neoplasias , Humanos , Antineoplásicos/farmacologia , Azepinas/farmacologia , Compostos Heterocíclicos de Anel em Ponte/farmacologia , Lactonas/farmacologia , Apoptose , Alcaloides/farmacologia , Proliferação de Células , Ensaios de Seleção de Medicamentos Antitumorais , Linhagem Celular Tumoral
4.
Lipids Health Dis ; 22(1): 44, 2023 Mar 29.
Artigo em Inglês | MEDLINE | ID: mdl-36991386

RESUMO

BACKGROUND: Nonalcoholic fatty liver disease (NAFLD), a common liver disease worldwide, can be reversed early in life with lifestyle and medical interventions. This study aimed to develop a noninvasive tool to screen NAFLD accurately. METHODS: Risk factors for NAFLD were identified using multivariate logistic regression analysis, and an online NAFLD screening nomogram was developed. The nomogram was compared with reported models (fatty liver index (FLI), atherogenic index of plasma (AIP), and hepatic steatosis index (HSI)). Nomogram performance was evaluated through internal and external validation (National Health and Nutrition Examination Survey (NHANES) database). RESULTS: The nomogram was developed based on six variables. The diagnostic performance of the present nomogram for NAFLD (area under the receiver operator characteristic curve (AUROC): 0.863, 0.864, and 0.833, respectively) was superior to that of the HSI (AUROC: 0.835, 0.833, and 0.810, respectively) and AIP (AUROC: 0.782, 0.773, and 0.728, respectively) in the training, validation, and NHANES sets. Decision curve analysis and clinical impact curve analysis presented good clinical utility. CONCLUSION: This study establishes a new online dynamic nomogram with excellent diagnostic and clinical performance. It has the potential to be a noninvasive and convenient method for screening individuals at high risk for NAFLD.


Assuntos
Hepatopatia Gordurosa não Alcoólica , Humanos , Hepatopatia Gordurosa não Alcoólica/diagnóstico , Inquéritos Nutricionais , Nomogramas , Fatores de Risco , Testes de Função Hepática
5.
Hip Int ; 32(3): 334-344, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-32750257

RESUMO

OBJECTIVE: To evaluate the feasibility and accuracy of three-dimensional (3D)-printed individualised guiding templates in total hip arthroplasty (THA) for the treatment of developmental dysplasia of the hip (DDH). METHODS: 12 hips in 12 patients with Crowe type IV DDH were treated with THA. A 3D digital model of the pelvis and lower limbs was reconstructed using the computed tomography data of the patients. Preoperative surgical simulations were performed to determine the most suitable surgical planning, including femoral osteotomy and prosthesis placement. Based on the ideal surgical planning, individualised guiding templates were designed by software, manufactured using a 3D printer, and used in acetabulum reconstruction and femoral osteotomy during surgery. RESULTS: 12 patients were followed up for an average of 72.42 months (range 38-135 months). During surgery, the guiding template for each case was matched to the bony markers of the acetabulum and proximal femur. Preoperative and follow-up Harris Hip Scores were 34.2 ± 3.7 and 85.2 ± 4.2; leg-length discrepancy, 51.5 ± 6.5 mm and 10.2 ± 1.5 mm; and visual analogue scale scores, 6.2 ± 0.8 and 1.3 ± 0.3, respectively, with statistical difference. Shortened deformity and claudication of the affected limb were obviously improved after surgery. However, 1 patient had artificial hip dislocation 2 weeks after surgery, and another patient had sciatic nerve traction injury, both of whom recovered after physical treatment. CONCLUSIONS: Preoperative surgical simulation and 3D-printed individualised guiding templates can fulfil surgeon-specific requirements for the treatment of Crowe type IV DDH. Accurate THA can be achieved using 3D-printed individualised templates, which provide a new personalised surgical plan for the precise positioning and orientation of acetabular reconstruction and femoral osteotomy.


Assuntos
Artroplastia de Quadril , Displasia do Desenvolvimento do Quadril , Luxação Congênita de Quadril , Acetábulo/diagnóstico por imagem , Acetábulo/cirurgia , Artroplastia de Quadril/métodos , Fêmur/diagnóstico por imagem , Fêmur/cirurgia , Luxação Congênita de Quadril/diagnóstico por imagem , Luxação Congênita de Quadril/cirurgia , Humanos , Impressão Tridimensional , Estudos Retrospectivos
6.
Future Med Chem ; 13(23): 2083-2105, 2021 12.
Artigo em Inglês | MEDLINE | ID: mdl-34633220

RESUMO

Transthyretin (TTR) is associated with several human amyloid diseases. Various kinetic stabilizers have been developed to inhibit the dissociation of TTR tetramer and the formation of amyloid fibrils. Most of them are bisaryl derivatives, natural flavonoids, crown ethers and carborans. In this review article, we focus on TTR tetramer stabilizers, genetic therapeutic approaches and fibril remodelers. The binding modes of typical bisaryl derivatives, natural flavonoids, crown ethers and carborans are discussed. Based on knowledge of the binding of thyroxine to TTR tetramer, many stabilizers have been screened to dock into the thyroxine binding sites, leading to TTR tetramer stabilization. Particularly, those stabilizers with unique binding profiles have shown great potential in developing the therapeutic management of TTR amyloidogenesis.


Assuntos
Amiloide/antagonistas & inibidores , Compostos de Boro/farmacologia , Éteres de Coroa/farmacologia , Desenvolvimento de Medicamentos , Flavonoides/farmacologia , Pré-Albumina/antagonistas & inibidores , Amiloide/metabolismo , Compostos de Boro/química , Éteres de Coroa/química , Flavonoides/química , Humanos , Pré-Albumina/metabolismo
7.
Future Med Chem ; 13(24): 2153-2166, 2021 12.
Artigo em Inglês | MEDLINE | ID: mdl-34608806

RESUMO

Dyslipidemia has been associated with the development of osteoarthritis. Our previous study found that 5,7,3',4'-tetramethoxyflavone (TMF) exhibited protective activities against the pathological changes of osteoarthritis. Aim: To investigate the roles of TMF in regulating ABCA1-mediated cholesterol metabolism. Methods: Knockdown and overexpression were employed to study gene functions. Protein-protein interaction was investigated by co-immunoprecipitation, and the subcellular locations of proteins were studied by immunofluorescence. Results: IL-1ß decreased ABCA1 expression and induced apoptosis. Therapeutically, TMF ameliorated the effects of IL-1ß. FOXO3a knockdown expression abrogated the effects of TMF, and FOXO3a overexpression increased ABCA1 expression by interacting with LXRα. TMF promoted FOXO3a nuclear translocation by activating SIRT1 expression. Conclusions: TMF ameliorates cholesterol dysregulation by increasing the expression of FOXO3a/LXRα/ABCA1 signaling through SIRT1 in C28/I2 cells.


Assuntos
Transportador 1 de Cassete de Ligação de ATP/metabolismo , Condrócitos/efeitos dos fármacos , Proteína Forkhead Box O3/metabolismo , Luteolina/farmacologia , Osteoartrite/tratamento farmacológico , Sirtuína 1/metabolismo , Transportador 1 de Cassete de Ligação de ATP/genética , Células Cultivadas , Colesterol/metabolismo , Condrócitos/metabolismo , Condrócitos/patologia , Proteína Forkhead Box O3/genética , Humanos , Luteolina/química , Osteoartrite/metabolismo , Osteoartrite/patologia , Transdução de Sinais/efeitos dos fármacos , Sirtuína 1/genética
8.
BMC Musculoskelet Disord ; 22(1): 745, 2021 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-34461878

RESUMO

BACKGROUND: To introduce a novel transoral instrumentation in the treatment of unstable fractures of the atlas. METHODS: From January 2008 to May 2018, 22 patients with unstable C1 fractures who received Jefferson-fracture reduction plate (JeRP) via transoral approach were retrospectively analyzed. The case history and the radiographs before and after surgery were noted. The type of fracture, the reduction of the fracture, and position of the internal fixation were assessed through preoperative and postoperative CT scans. RESULTS: All 22 patients successfully underwent anterior C1-ring osteosynthesis using the JeRP system, with a follow-up of 26.84 ± 9.23 months. Among them, 9 patients had transverse atlantal ligament (TAL) injury, including 3 in Dickman type I and 6 in type II. The preoperative lateral mass displacement (LMD) decreased from 7.13 ± 1.46 mm to 1.02 ± 0.65 mm after the operation. Bone union was achieved in all patients without implant failure or loss of reduction. There were no surgery-related complications, such as wound infection, neurological deficit, or vertebral artery injury. However, atlantoaxial dislocation occurred in 3 patients with Dickman type I TAL injury 3 months postoperatively without any neurological symptoms or neck pain. CONCLUSIONS: Transoral C1-ring osteosynthesis with JeRP is an effective surgical strategy to treat unstable atlas fractures with a safe, direct, and satisfactory reduction. The primary indication for the JeRP system is an unstable fracture (Gehweiler type I/III) or/ and TAL injury (Dickman type II).


Assuntos
Atlas Cervical , Fraturas da Coluna Vertebral , Placas Ósseas , Atlas Cervical/diagnóstico por imagem , Atlas Cervical/lesões , Atlas Cervical/cirurgia , Fixação Interna de Fraturas , Humanos , Estudos Retrospectivos , Fraturas da Coluna Vertebral/diagnóstico por imagem , Fraturas da Coluna Vertebral/cirurgia
9.
World Neurosurg ; 149: e969-e981, 2021 05.
Artigo em Inglês | MEDLINE | ID: mdl-33508486

RESUMO

OBJECTIVE: This study aimed to explore the clinical application of three-dimensional (3D) printing technology in the surgical treatment of congenital scoliosis caused by hemivertebrae. METHODS: Twenty-four patients (11 in the 3D-printing group and 13 in the conventional group) with scoliosis secondary to a single hemivertebra were retrospectively reviewed. All patients underwent hemivertebrectomy and short-segment fixation. Virtual preoperative planning, operation simulation, and intraoperative application of 3D-printed patient-specific templates were performed in the 3D-printing group. Hemorrhage volume, operation time, transfusion, and complications were noted. Radiographic parameters were evaluated preoperatively, postoperatively, and at final follow-up. RESULTS: All patients had different degrees of successfully corrected scoliosis. There was a similar correction of the Cobb angle postoperatively between the 2 groups. The operation time, blood loss, transfusion, time for the insertion of each screw, accuracy of screw placement, and complication rate in the 3D-printing group were significantly superior to those in the control group. No patient experienced major complications. No significant correction loss or instrument dysfunction was observed during follow-up. CONCLUSIONS: As a viable and effective auxiliary technology, 3D printing makes it possible for surgery to meet both surgeon-specific and patient-specific requirements. 3D-printed individualized templates allow surgery for the correction of congenital scoliosis to enter a new stage of personalized precision surgery.


Assuntos
Procedimentos Neurocirúrgicos/métodos , Impressão Tridimensional , Escoliose/cirurgia , Coluna Vertebral/anormalidades , Coluna Vertebral/cirurgia , Adolescente , Transfusão de Sangue/estatística & dados numéricos , Criança , Feminino , Hemorragia/diagnóstico por imagem , Hemorragia/cirurgia , Humanos , Masculino , Duração da Cirurgia , Planejamento de Assistência ao Paciente , Parafusos Pediculares , Complicações Pós-Operatórias/epidemiologia , Estudos Retrospectivos , Escoliose/congênito , Escoliose/etiologia , Treinamento por Simulação , Fusão Vertebral , Resultado do Tratamento
10.
Fungal Biol ; 124(12): 1004-1012, 2020 12.
Artigo em Inglês | MEDLINE | ID: mdl-33213780

RESUMO

Sparassis latifolia is a valuable edible fungus cultivated in East Asia that is rich in ß-glucans. Understanding the mating system and sexual life cycle is important not only for breeding programs to improve strains but also for studies on speciation and population structures. In the present study, mating experiments using monokaryons derived from two different parental strains were performed. Chi-squared test indicated satisfied Mendel segregation, which supported a tetrapolar mating system. A search in the genome for homologs to the well-defined homeodomain and pheromone/receptors, as well as frequently found flanking genes, resulted in the identification of known mating-type loci previously identified in tetrapolar basidiomycetes, each represented by two idiomorphic alleles on separate contigs. Deficiency of the ß-flanking protein in S. latifolia and S. crispa around the MAT-A locus may be explained by the locus being rich in transposable elements adjacent to HD genes. Monokaryotic mycelia are characterized by a slower growth rate and a relative lack of aerial mycelia compared with the parental strain. Chlamydospores can be produced in both monokaryotic and dikaryotic mycelial stages. We provide genetic and molecular evidence for the mating system of S. latifolia, a finding that will be helpful for the cross-breeding of this mushroom.


Assuntos
Basidiomycota , Genes Fúngicos Tipo Acasalamento , Polyporales , Basidiomycota/genética , Polyporales/genética , Receptores de Feromônios/genética
11.
Orthop Surg ; 12(6): 1947-1953, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33080108

RESUMO

OBJECTIVE: Spinal fusion is one of the most common surgical interventions for spine reconstruction. Despite the efforts to promote osteogenesis after spinal fusion, osteogenesis after spinal fusion remains a clinical challenge and new methods are still needed. The bone morphogenetic protein-2 (BMP-2) is a widely reported factor that can facilitate the osteogenesis in spinal fusion. In previous research, we found that the delivery of chitosan nanospheres could promote the effects of BMP-2 on osteogenic activity. The coralline hydroxyapatite (CHA) is one of the most frequently used implants in bone fusion. However, up to now no study has focused on the osteogenic efficacy of the CHA composite with recombinant human BMP-2 (rhBMP-2)-loaded chitosan nanospheres. This study aimed to investigate the effects of the CHA implant with rhBMP-2-loaded chitosan nanospheres on osteogenesis in spinal fusion. METHODS: The rhBMP-2-loaded microspheres and CHA composite (rhBMP-2 microspheres/CHA) were prepared and were used for implantation of the rats. All SD rats were divided into four groups: the rhBMP-2 microspheres/CHA composite group (containing 0.5 mg rhBMP-2), the rhBMP-2-loaded CHA (rhBMP-2/CHA) composite group (containing 0.5 mg rhBMP-2), the blank CHA group, and the negative control group. The microsphere morphology was scanned and analyzed using a scanning electron microscope. Micro-computed tomography examination and three-dimensional reconstruction were performed 4 weeks after the surgery. Hematoxylin and eosin staining was conducted for histological analysis. Both alkaline phosphatase (ALP) and calcium content were measured. RESULTS: The rhBMP-2-loaded CHA (rhBMP-2/CHA) composite was successfully prepared. Spherical regularity and a smooth and unwrinkled surface of the spheres were observed in all chitosan (CS)/rhBMP-2 microspheres. No side effects, infections, or abnormal behaviors were found in the animals. After 4 weeks of surgery, obvious new bone formation and bone fusion could be observed around the implant in both the rhBMP-2 microspheres/CHA composite group and the rhBMP-2/CHA composite group. No ectopic osteogenesis was found in the vertebral canal or other muscle tissues. After 4 weeks of implantation, in both the rhBMP-2 microspheres/CHA composite group and the rhBMP-2/CHA composite group, osteoid tissues could be found, and bone cells, bone marrow, and trabecular bone turned into mature sclerotin, obvious bone tissue formation could be also seen. Both ALP activity and calcium content in the rhBMP-2 microspheres/CHA composite group (6.52 ± 0.50 kat/g and 17.54 ± 2.49 µg/mg) were significantly higher than in all other groups. CONCLUSION: The composite with rhBMP-2-loaded CS nanospheres could enhance osteogenic efficacy and increase the ALP activity and calcium content. These results might provide a novel method for osteogenesis in spinal fusion and offer new insight into the role of BMP-2 in osteogenesis.


Assuntos
Proteína Morfogenética Óssea 2/farmacologia , Cerâmica/farmacologia , Quitosana/farmacologia , Hidroxiapatitas/farmacologia , Osteogênese/fisiologia , Fusão Vertebral/métodos , Coluna Vertebral/cirurgia , Fator de Crescimento Transformador beta/farmacologia , Animais , Materiais Biocompatíveis , Implantes de Medicamento , Humanos , Masculino , Nanosferas , Ratos , Ratos Sprague-Dawley , Proteínas Recombinantes/farmacologia
12.
J Org Chem ; 85(12): 8185-8195, 2020 06 19.
Artigo em Inglês | MEDLINE | ID: mdl-32452681

RESUMO

The first facile and efficient acid-catalyzed direct coupling of a wide range of unprotected 2,3-allenols with arylphosphine oxides was developed, offering a general, one-step approach for the synthesis of structurally diverse γ-ketophosphine oxides accompanied by concurrent C-P/C═O bond formation with remarkable functional group tolerance and complete atom-economy under metal- and additive-free conditions. Mechanistic studies showed that this transformation involved a rearrangement and a phospha-Michael reaction.

13.
Drug Des Devel Ther ; 13: 2009-2019, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31354246

RESUMO

Background: miR-29a, a downstream factor of Wnt/ß-catenin signaling, promotes the activity of the Wnt/ß-catenin signaling in a positive feedback loop. Our previous work showed that 5,7,3',4'-tetramethoxyflavone (TMF), a major constituent from Murraya exotica L., exhibited chondroprotective activity by inhibiting the activity of Wnt/ß-catenin signaling. Purpose: To investigate whether TMF showed the inhibitory effects on miR-29a/ß-catenin signaling by up regulation of Foxo3a expression. Methods: Rat knee OA models were duplicated by using Hulth's method. TMF (5 µg/mL and 20 µg/mL) was used for administration to cultured cells, which were isolated from the rat cartilages. Analysis of chondrocytes apoptosis, gene expression, and protein expression were conducted. In addition, miR-29a mimics and pcDNA3.1(+)-Foxo3a vector were used for transfection, luciferase reporter assay for detecting the activity of Wnt/ß-catenin signaling, and co-immunoprecipitation for determining proteins interaction. Results: TMF down regulated miR-29a/ß-catenin signaling activity and cleaved caspase-3 expression and up regulated Foxo3a expression in OA rat cartilages. In vitro, miR-29a mimics down regulated the expression of Foxo3a and up regulated the activity of Wnt/ß-catenin signaling and cleaved caspase-3 expression. TMF ameliorated miR-29a/ß-catenin-induced chondrocytes apoptosis by up regulation of Foxo3a expression. Conclusion: TMF exhibited chondroprotective activity by up regulating Foxo3a expression and subsequently inhibiting miR-29a/Wnt/ß-catenin signaling activity.


Assuntos
Condrócitos/efeitos dos fármacos , Proteína Forkhead Box O3/metabolismo , Luteolina/farmacologia , MicroRNAs/antagonistas & inibidores , Osteoartrite/tratamento farmacológico , Via de Sinalização Wnt/efeitos dos fármacos , beta Catenina/antagonistas & inibidores , Administração Oral , Animais , Apoptose/efeitos dos fármacos , Células Cultivadas , Condrócitos/metabolismo , Condrócitos/patologia , Modelos Animais de Doenças , Regulação para Baixo/efeitos dos fármacos , Luteolina/administração & dosagem , MicroRNAs/metabolismo , Osteoartrite/metabolismo , Osteoartrite/patologia , Ratos , Regulação para Cima/efeitos dos fármacos , beta Catenina/metabolismo
14.
Biomed Res Int ; 2019: 1847130, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31240205

RESUMO

Over years, various biological constituents are isolated from Traditional Chinese Medicine and confirmed to show multifunctional activities. Magnolol, a hydroxylated biphenyl natural compound isolated from Magnolia officinalis, has been extensively documented and shows a range of biological activities. Many signaling pathways include, but are not limited to, NF-κB/MAPK, Nrf2/HO-1, and PI3K/Akt pathways, which are implicated in the biological functions mediated by magnolol. Thus, magnolol is considered as a promising therapeutic agent for clinic research. However, the low water solubility, the low bioavailability, and the rapid metabolism of magnolol dramatically limit its clinical application. In this review, we will comprehensively discuss the last five-year progress of the biological activities of magnolol, including anti-inflammatory, antimicroorganism, antioxidative, anticancer, neuroprotective, cardiovascular protection, metabolism regulation, and ion-mediating activity.


Assuntos
Compostos de Bifenilo/metabolismo , Compostos de Bifenilo/farmacologia , Lignanas/metabolismo , Lignanas/farmacologia , Medicina Tradicional Chinesa , Anti-Inflamatórios/análise , Antineoplásicos/análise , Antioxidantes/análise , Compostos de Bifenilo/química , Compostos de Bifenilo/uso terapêutico , Fármacos Cardiovasculares/análise , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/metabolismo , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Humanos , Lignanas/química , Lignanas/uso terapêutico , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Magnolia/química , Fator 2 Relacionado a NF-E2/efeitos dos fármacos , Fator 2 Relacionado a NF-E2/metabolismo , NF-kappa B/efeitos dos fármacos , NF-kappa B/metabolismo , Fármacos Neuroprotetores/análise , Fosfatidilinositol 3-Quinases/efeitos dos fármacos , Fosfatidilinositol 3-Quinases/metabolismo , Transdução de Sinais/efeitos dos fármacos
15.
Pharmazie ; 74(2): 67-72, 2019 02 01.
Artigo em Inglês | MEDLINE | ID: mdl-30782253

RESUMO

Psoralidin, a prenylated coumestrol isolated from the seed of a traditional Chinese medicine Psoralea corylifolia L., has been demonstrated to exhibit anti-inflammatory, anti-cancer, anti-oxidative, estrogenic, neuroprotective, anti-bacterial, and anti-parasite activities. Due to prenylation, psoralidin exhibits stronger estrogenic activity with no obvious adverse effects and shows a close association with management of osteoporosis and some cancers. However, the hydrophobicity and low bioavailability of psoralidin limit its clinical application, although recent investigation has gained valuable data. This review will discuss the biological activities of psoralidin in health.


Assuntos
Benzofuranos/farmacologia , Cumarínicos/farmacologia , Animais , Antibacterianos/química , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Antineoplásicos/química , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Antioxidantes/química , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Benzofuranos/química , Benzofuranos/uso terapêutico , Cumarínicos/química , Cumarínicos/uso terapêutico , Estrogênios/química , Estrogênios/farmacologia , Estrogênios/uso terapêutico , Humanos , Redes e Vias Metabólicas/efeitos dos fármacos , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/uso terapêutico , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico
16.
J Orthop Sci ; 22(4): 630-634, 2017 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-28336191

RESUMO

BACKGROUND: The purpose of this study was to evaluate the possibility of implanting the anterior atlantoaxial lateral mass intervertebral cage, a new type of fixation, by the transoral approach. METHOD: This study examined the possibility of implantation in vivo by the quantitative measurement on the dry atlantoaxial bone and implantation of the anterior atlantoaxial lateral mass intervertebral cage in specimens. Anterior atlantoaxial lateral mass intervertebral cages were implanted in 10 atlantoaxial joint specimens using the transoral approach. Eight anatomical parameters (width, the thickness, ordinates, abscissas, and declination angles of the mass) from each of the 30 dry atlas and axis bone specimens were measured. These parameters determined the size and the design of the cage and the way of implantation. RESULTS: The course of the vertebral artery forms the safe boundary for transoral surgery. The shape of the area of work exposure was an inverted trapezoid. In specimens, the anterior atlantoaxial lateral mass intervertebral cages could be successfully implanted using the transoral approach. The parameters of the human atlantoaxial lateral masses exposed anteriorly showed that there was enough space, for the safe anterior implantation of the cage. The surgery using the transoral atlantoaxial reduction and plate makes possible the implantation of the anterior cage. CONCLUSION: The implantation of anterior atlantoaxial lateral mass intervertebral cage through transoral approach is possible.


Assuntos
Articulação Atlantoaxial/cirurgia , Fixadores Internos , Luxações Articulares/cirurgia , Boca , Fusão Vertebral/métodos , Adulto , Cadáver , Humanos , Luxações Articulares/diagnóstico por imagem , Masculino , Pessoa de Meia-Idade , Fusão Vertebral/instrumentação
17.
Biomed Pharmacother ; 89: 1262-1268, 2017 May.
Artigo em Inglês | MEDLINE | ID: mdl-28320093

RESUMO

Endoplasmic reticulum (ER) stress-induced chondrocyte apoptosis plays a critical role in osteoarthritis cartilage degeneration. Previous studies showed that 5,7,3',4'-tetramethoxyflavone (TMF) exhibited chondroprotective activity through inhibiting PGE2-induced ER stress and down regulating the expression of GSK-3ß. To further investigate the role of GSK-3ß in ER stress-induced chondrocytes apoptosis and the protective role of TMF, GSK-3ß siRNA and pcDNA3.1-myc-GSK-3ß were employed to knock down and overexpress GSK-3ß, respectively, in chondrocytes. Results showed that TM-induced ER stress significantly promoted chondrocytes apoptosis. These could be effectively reversed by GSK-3ß deficiency, while GSK-3ß overexpression significantly up regulated ER stress and increased chondrocytes apoptosis. In addition, TMF down regulated the expression of GSK-3ß and inhibited ER stress-induced chondrocytes apoptosis. Collectively, TMF is a potential natural compound with chondroprotective property through inhibition of ER stress-induced apoptosis with down regulation of GSK-3ß.


Assuntos
Apoptose/efeitos dos fármacos , Condrócitos/efeitos dos fármacos , Regulação para Baixo/efeitos dos fármacos , Estresse do Retículo Endoplasmático/efeitos dos fármacos , Glicogênio Sintase Quinase 3 beta/metabolismo , Lactamas/farmacologia , Mupirocina/análogos & derivados , Substâncias Protetoras/farmacologia , Animais , Condrócitos/metabolismo , Mupirocina/farmacologia , Osteoartrite/metabolismo , RNA Interferente Pequeno/metabolismo , Ratos , Transdução de Sinais/efeitos dos fármacos
18.
Eur Spine J ; 26(3): 840-846, 2017 03.
Artigo em Inglês | MEDLINE | ID: mdl-26951169

RESUMO

PURPOSE: This study explored the performance characteristics of a cuff-leak test (CLT) combined with interventional fiberoptic bronchoscopy (FBS) for evaluating whether early nasoendotracheal extubation was possible for patients who had received transoral atlantoaxial reduction plate (TARP) internal fixation surgery. METHODS: 318 patients who underwent surgery were retrospectively analyzed (between January 2006 and December 2012). Extubation was performed by conventional approach (CA group, until December 2008) and improved approach (IA group, from January 2009) including CLT and an interventional FBS procedure. The extubation success within 1-3 days after surgery, incidence of postextubation stridor and tracheal reintubation were examined. RESULTS: More IA-treated patients experienced extubation during the first 2 days than those CA-treated, median extubation time was 3 (2, 3) days in the CA group and 2 (1, 2) days in the IA group (all P < 0.01). The incidence of stridor and reintubation was 5.69 and 0.57 % in IA and 11.98 and 4.93 % in CA, respectively (both P < 0.05). For the CLT-positive patients in the IA group that remained intubated until day 3-4, interventional FBS was applied for safe extubation and achieved 100 % success. CONCLUSION: Early extubation through IA is safe and interventional FBS assists successful extubation for CLT-positive patients who underwent TARP surgery.


Assuntos
Extubação/métodos , Articulação Atlantoaxial/cirurgia , Placas Ósseas , Broncoscopia/métodos , Fusão Vertebral/métodos , Adulto , Feminino , Humanos , Incidência , Intubação Intratraqueal , Masculino , Pessoa de Meia-Idade , Cirurgia Endoscópica por Orifício Natural , Cuidados Pós-Operatórios/métodos , Sons Respiratórios , Estudos Retrospectivos , Adulto Jovem
19.
Artigo em Chinês | MEDLINE | ID: mdl-27281871

RESUMO

UNLABELLED: OBJECTIVE To evaluate the ectopic osteogenesis of recombinant human bone morphogenetic protein 2 (rhBMP-2) loaded chitosan (CS)/dextran sulfate (DS) by micro-CT. METHODS: rhBMP-2/CS/DS microspheres were prepared by the ionic crosslinking and its shape was observed under the scanning electron microscope. The release of rhBMP-2 was determined from resultant microspheres by ELISA assay. Forty-eight Sprague Dawley male rats were randomly divided into 4 groups (n = 12), quadriceps muscle bag model was made, gelatin sponge (group A), CS/DS microspheres (group B), rhBMP-2 (group C), and CS/DS/rhBMP-2 microspheres (group D) were implanted into the bags respectively. The tissue samples with heterotopic ossification were harvested for micro-CT scanning at 4, 8, 12, and 16 weeks. The tissue mineral density (TMD), bone volume fraction (BVF), trabecular thickness (Tb.Th), trabecular number (Tb.N), bone mineral density (BMD), and tissue mineral content (TMC) were measured. RESULTS: The prepared rhBMP-2/CS/DS microspheres with smooth surfaces were spherical and evenly disperses without obvious agglomeration. At 2 hours, microsphere started a sudden release period in vitro; the release reached a peak at 2 days; and the release cycle lasted about 20 days. The rats survived to the end of the experiment. At each time point after operation, no radiation developed and no osteogenesis was observed by three dimensional reconstruction in groups A and B. However, radioactive strength and reconstructed bone tissue gradually increased in groups C and D, and group D had more radioautography and more bone tissues than group C. At each time point, TMD, BVF, Tb.Th, Tb.N, BMD, and TMC of groups A and B were zero. Ectopic bone formed with time, the other parameters showed an increasing trend except Tb.N in groups C and D, showing significant difference when compared with groups A and B at each time point (P < 0.05). There was no significant difference between groups C and D at 4 weeks (P > 0.05); the parameters of group D were significantly higher than those of group C at 8-16 weeks (P < 0.05). CONCLUSION: rhBMP-2/CS/DS microspheres have stronger ability of ectopic bone formation than single rhBMP-2.


Assuntos
Proteína Morfogenética Óssea 2 , Quitosana , Sulfato de Dextrana , Osteogênese , Fator de Crescimento Transformador beta , Animais , Densidade Óssea , Gelatina , Humanos , Masculino , Microesferas , Ossificação Heterotópica , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley , Proteínas Recombinantes , Microtomografia por Raio-X
20.
Zhongguo Zhong Xi Yi Jie He Za Zhi ; 35(12): 1459-62, 2015 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-26882608

RESUMO

OBJECTIVE: To evaluate the efficacy and safety of Jinying Capsule (JC) in treating pelvic inflammatory disease patients with accumulated damp-heat syndrome (ADHS). METHODS: Totally 328 patients were recruited in a prospective, positive drug parallel controlled, and multi-center clinical trial. Of them 213 patients in the treatment group took JC (0.5 g per capsule), 4 capsules each time, 3 times per day, while 115 patients in the control group took Kangfuyan Capsule (KC, 0.4 g per capsule), 3 capsules each time, twice per day. The course of treatment was 4 weeks for all. Scores of Chinese medical syndromes, visual analogue scale (VAS) of the lower abdominal pain, and European quality of life-five dimension scale (EQ-5D) were observed before treatment and after 4 weeks of treatment. RESULTS: There were 204 patients in the treatment group and 109 in the control group who completed this trial. The total effective rate of Chinese medical syndrome was 89.71% (183/204 cases) in the treatment group and 76.15% (83/109 cases) in the control group (P < 0.01). Compared with before treatment in the same group, EQ-5D scores increased, and VAS scores of the lower abdominal pain decreased in the two groups after treatment. EQ-5D scores was 0.857 ± 0.157 in the treatment group, obviously higher than that in the control group (0.753 ± 0.126, P < 0.05). VAS scores of the lower abdominal pain was 2.14 ± 1.23 in the treatment group, lower than that in the control group (2.33 ± 1.24), but with no statistical difference between the two groups (P > 0.05). No adverse reaction occurred in the two groups. CONCLUSION: JC was superior to KC in improving Chinese medical syndrome and quality of life of pelvic inflammatory disease patients with accumulated damp-heat syndrome.


Assuntos
Medicamentos de Ervas Chinesas/uso terapêutico , Medicina Tradicional Chinesa , Doença Inflamatória Pélvica/tratamento farmacológico , Cápsulas , Feminino , Temperatura Alta , Humanos , Fitoterapia , Estudos Prospectivos , Qualidade de Vida , Segurança , Síndrome
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