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1.
Pharm Biol ; 62(1): 544-561, 2024 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-38946248

RESUMEN

CONTEXT: Diabetic peripheral neuropathy (DPN) results in an enormous burden and reduces the quality of life for patients. Considering there is no specific drug for the management of DPN, traditional Chinese medicine (TCM) has increasingly drawn attention of clinicians and researchers around the world due to its characteristics of multiple targets, active components, and exemplary safety. OBJECTIVE: To summarize the current status of TCM in the treatment of DPN and provide directions for novel drug development, the clinical effects and potential mechanisms of TCM used in treating DPN were comprehensively reviewed. METHODS: Existing evidence on TCM interventions for DPN was screened from databases such as PubMed, the Cochrane Neuromuscular Disease Group Specialized Register (CENTRAL), and the Chinese National Knowledge Infrastructure Database (CNKI). The focus was on summarizing and analyzing representative preclinical and clinical TCM studies published before 2023. RESULTS: This review identified the ameliorative effects of about 22 single herbal extracts, more than 30 herbal compound prescriptions, and four Chinese patent medicines on DPN in preclinical and clinical research. The latest advances in the mechanism highlight that TCM exerts its beneficial effects on DPN by inhibiting inflammation, oxidative stress and apoptosis, endoplasmic reticulum stress and improving mitochondrial function. CONCLUSIONS: TCM has shown the power latent capacity in treating DPN. It is proposed that more large-scale and multi-center randomized controlled clinical trials and fundamental experiments should be conducted to further verify these findings.


Asunto(s)
Neuropatías Diabéticas , Medicamentos Herbarios Chinos , Medicina Tradicional China , Humanos , Neuropatías Diabéticas/tratamiento farmacológico , Medicina Tradicional China/métodos , Medicamentos Herbarios Chinos/uso terapéutico , Medicamentos Herbarios Chinos/farmacología , Animales , Calidad de Vida , Estrés Oxidativo/efectos de los fármacos , Evaluación Preclínica de Medicamentos/métodos
2.
Pharm Biol ; 62(1): 592-606, 2024 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-39028269

RESUMEN

CONTEXT: The global prevalence of type 2 diabetes mellitus (T2DM) has increased significantly in recent decades. Despite numerous studies and systematic reviews, there is a gap in comprehensive and up-to-date evaluations in this rapidly evolving field. OBJECTIVE: This review provides a comprehensive and current overview of the efficacy of Traditional Chinese Medicine (TCM) in treating T2DM. METHODS: A systematic review was conducted using PubMed, Web of Science, Wanfang Data, CNKI, and Medline databases, with a search timeframe extending up to November 2023. The search strategy involved a combination of subject terms and free words in English, including 'Diabetes,' 'Traditional Chinese Medicine,' 'TCM,' 'Hypoglycemic Effect,' 'Clinical Trial,' and 'Randomized Controlled Trial.' The studies were rigorously screened by two investigators, with a third investigator reviewing and approving the final selection based on inclusion and exclusion criteria. RESULTS: A total of 108 relevant papers were systematically reviewed. The findings suggest that TCMs not only demonstrate clinical efficacy comparable to existing Western medications in managing hypoglycemia but also offer fewer adverse effects and a multitarget therapeutic approach. Five main biological mechanisms through which TCM treats diabetes were identified: improving glucose transport and utilization, improving glycogen metabolism, promoting GLP-1 release, protecting pancreatic islets from damage, and improving intestinal flora. CONCLUSIONS: TCM has demonstrated significant protective effects against diabetes and presents a viable option for the prevention and treatment of T2DM. These findings support the further exploration and integration of TCM into broader diabetes management strategies.


Asunto(s)
Diabetes Mellitus Tipo 2 , Medicamentos Herbarios Chinos , Hipoglucemiantes , Medicina Tradicional China , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Humanos , Medicina Tradicional China/métodos , Hipoglucemiantes/uso terapéutico , Hipoglucemiantes/farmacología , Medicamentos Herbarios Chinos/farmacología , Medicamentos Herbarios Chinos/uso terapéutico , Resultado del Tratamiento , Animales , Ensayos Clínicos Controlados Aleatorios como Asunto , Glucemia/efectos de los fármacos , Glucemia/metabolismo
3.
Int J Mol Sci ; 23(24)2022 Dec 13.
Artículo en Inglés | MEDLINE | ID: mdl-36555485

RESUMEN

Hypoxia is a major stressor and a prominent feature of pathological conditions, such as bacterial infections, inflammation, wounds, and cardiovascular defects. In this study, we investigated whether reoxygenation has a protective effect against hypoxia-induced acute injury and burn using the C57BL/6 mouse model. C57BL/6 mice were exposed to hypoxia and treated with both acute and burn injuries and were in hypoxia until wound healing. Next, C57BL/6 mice were exposed to hypoxia for three days and then transferred to normoxic conditions for reoxygenation until wound healing. Finally, skin wound tissue was collected to analyze healing-related markers, such as inflammation, vascularization, and collagen. Hypoxia significantly increased inflammatory cell infiltration and decreased vascular and collagen production, and reoxygenation notably attenuated hypoxia-induced infiltration of inflammatory cells, upregulation of pro-inflammatory cytokine levels (IL-6 and TNF-α) in the wound, and remission of inflammation in the wound. Immunofluorescence analysis showed that reoxygenation increased the expression of the angiogenic factor α-SMA and decreased ROS expression in burn tissues compared to hypoxia-treated animals. Moreover, further analysis by qPCR showed that reoxygenation could alleviate the expression of hypoxic-induced inflammatory markers (IL-6 and TNF), increase angiogenesis (SMA) and collagen synthesis (Col I), and thus promote wound healing. It is suggested that oxygen can be further evaluated in combination with oxygen-releasing materials as a supplementary therapy for patients with chronic hypoxic wounds.


Asunto(s)
Quemaduras , Interleucina-6 , Ratones , Animales , Ratones Endogámicos C57BL , Cicatrización de Heridas , Hipoxia/complicaciones , Colágeno , Oxígeno/farmacología , Quemaduras/patología , Inflamación/metabolismo
4.
Phys Chem Chem Phys ; 23(47): 26864-26873, 2021 Dec 08.
Artículo en Inglés | MEDLINE | ID: mdl-34821236

RESUMEN

A four-band terahertz tunable narrow-band perfect absorber based on a bulk Dirac semi-metallic (BDS) metamaterial with a microstructure is designed. The three-layer structure of this absorber from top to bottom is the Dirac semi-metallic layer, the dielectric layer and the metal reflector layer. Based on the Finite Element Method (FEM), we use the simulation software CST STUDIO SUITE to simulate the absorption characteristics of the designed absorber. The simulation results show that the absorption rate of the absorber is over 93% at frequencies of 1.22, 1.822, 2.148 and 2.476 THz, and three of them have achieved a perfect absorption rate of more than 95%. We use the localized surface plasmon resonance (LSPR), impedance matching and other theories to analyze its physical mechanism in detail. The influence of the geometric structure parameters of the absorber and the incident angle of electromagnetic waves on the absorption performance has also been studied in detail. Due to the rotational symmetry of the structure, the designed absorber has excellent polarization insensitivity. In addition, the maximum adjustable range of absorption frequency is 0.051 THz, which can be achieved by changing the Fermi energy of BDS. We also define the refractive index sensitivity (S), which is 39.1, 75.4, 119.1 and 122.0 GHz RIU-1 for the four absorption modes when the refractive index varies in the range of 1 to 1.9. This high-performance absorber has a very good development prospect in the frontier fields of bio-chemical sensing and special environmental detection.

5.
Acta Pharmacol Sin ; 41(11): 1476-1486, 2020 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-32934346

RESUMEN

Recent studies demonstrate that diet quercetin (Quer) has obvious bone protective effects on ovariectomized rodents but thus far there is no direct evidence to support the inhibitory effect of Quer on bone loss caused by long-term unloading. In the present study, we investigated whether Quer could prevent bone loss induced by unloading in mice. Mice were subjected to hindlimb suspension (HLS) and received Quer (25, 50, 100 mg· kg-1 ·day-1, ig) for 4 weeks. Before euthanasia blood sample was collected; the femurs were harvested and subjected to MicroCT analysis. We showed that Quer administration markedly improved bone microstructure evidenced by dose-dependently reversing the reduction in bone volume per tissue volume, trabecular number, and bone mineral density, and the increase of trabecular spacing in mice with HLS. Analysis of serum markers and bone histometric parameters confirmed that Quer at both middle and high doses significantly decreased bone resorption-related markers collagen type I and tartrate-resistant acid phosphatase 5b, and increased bone formation-related marker procollagen 1 N-terminal propeptide as compared with HLS group. Treatment with Quer (1, 2, 5 µM) dose-dependently inhibited RANKL-induced osteoclastogenesis through promoting the expression of antioxidant hormone stanniocalcin 1 (STC1) and decreasing ROS generation; knockdown of STC1 blocked the inhibitory effect of Quer on ROS generation. Knockdown of STC1 also significantly promoted osteoclastogenesis in primary osteoclasts. In conclusion, Quer protects bones and prevents unloading-caused bone loss in mice through STC1-mediated inhibition of osteoclastogenesis. The findings suggest that Quer has the potential to prevent and treat off-load bone loss as an alternative supplement.


Asunto(s)
Conservadores de la Densidad Ósea/uso terapéutico , Resorción Ósea/prevención & control , Glicoproteínas/metabolismo , Osteogénesis/efectos de los fármacos , Quercetina/uso terapéutico , Animales , Resorción Ósea/patología , Huesos/efectos de los fármacos , Huesos/patología , Suspensión Trasera , Masculino , Ratones Endogámicos C57BL , Osteoclastos/efectos de los fármacos , Ligando RANK/metabolismo , Especies Reactivas de Oxígeno/metabolismo
6.
Virol J ; 16(1): 144, 2019 11 26.
Artículo en Inglés | MEDLINE | ID: mdl-31771604

RESUMEN

BACKGROUND: MicroRNAs (miRNAs) is increasingly recognized as an important element in regulating virus-host interactions. Our previous results showed that cellular miR-30a-5p was significantly downregulated after duck enteritis virus (DEV) infection cell. However, whehter or not the miR-30a-5p is involved in DEV infection has not been known. METHODS: Quantitative reverse-transcription PCR (qRT-PCR) was used to measure the expression levels of miRNAs(miR-30a-5p) and Beclin-1 mRNA. The miR-30a-5p - Beclin-1 target interactions were determined by Dual luciferase reporter assay (DLRA). Western blotting was utilized to analyze Beclin-1-mediated duck embryo fibroblast (DEF) cells autophagy activity. DEV titers were estimated by the median tissue culture infective dose (TCID50). RESULTS: The miR-30a-5p was significantly downregulated and the Beclin-1 mRNA was significantly upregulated in DEV-infected DEF cells. DLRA confirmed that miR-30a-5p directly targeted the 3'- UTR of the Beclin-1 gene. Overexpression of miR-30a-5p significantly reduced the expression level of Beclin-1protein (p < 0.05), leading to the decrease of Beclin-1-mediated autophagy activity, which ultimately suppressed DEV replication (P < 0.05). Whereas transfection of miR-30a-5p inhibitor increased Beclin-1-mediated autophagy and triggered DEV replication during the whole process of DEV infection (P < 0.01). CONCLUSIONS: This study shows that miR-30a-5p can inhibit DEV replication through reducing autophagy by targeting Beclin-1. These findings suggest a new insight into virus-host interaction during DEV infection and provide a potential new antiviral therapeutic strategy against DEV infection.


Asunto(s)
Autofagia , Beclina-1/metabolismo , Regulación hacia Abajo , Interacciones Huésped-Patógeno , Mardivirus/crecimiento & desarrollo , MicroARNs/metabolismo , Replicación Viral , Animales , Western Blotting , Células Cultivadas , Patos , Fibroblastos/virología , Perfilación de la Expresión Génica , Reacción en Cadena en Tiempo Real de la Polimerasa
7.
Mol Pharm ; 16(2): 689-700, 2019 02 04.
Artículo en Inglés | MEDLINE | ID: mdl-30601012

RESUMEN

The excessive increase of intracellular reactive oxygen species (ROS) makes tumor cells usually in the state of oxidative stress. Although tumor cells can adapt to this state to a certain extent by upregulating antioxidant systems, the further ROS insults disrupt the transient intracellular redox balance, eventually leading to apoptosis and necrosis. Therefore, increasing the intracellular ROS level can effectively amplify the oxidative stress and induce apoptosis, which can be employed as a strategy for tumor treatment. Herein, a unique pH-responsive ROS inducing micellar system was reported in this study to specifically amplify the ROS signal in tumor cells. This micellar system was constructed by a new amphiphilic polymer, PIAThydCA, composed of poly(itaconic acid) (PIA) as the hydrophilic backbone, d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) as the hydrophobic side chain, and cinnamaldehyde (CA) as the ROS-generating agent, which were linked to PIA by the pH-sensitive hydrazone bond. PIAThydCA micelles could be degraded in the intracellular acidic environment through the hydrolysis of hydrazone bond and release CA. CA and TPGS could amplify oxidative stress cooperatively to kill MCF-7 human breast cells preferentially through the mitochondrial apoptosis pathway. Therefore, we anticipate that the PIAThydCA micelles could exert great potential in anticancer therapy.


Asunto(s)
Estrés Oxidativo/efectos de los fármacos , Polímeros/química , Acroleína/análogos & derivados , Acroleína/química , Antineoplásicos/química , Antineoplásicos/farmacología , Antioxidantes/metabolismo , Apoptosis/efectos de los fármacos , Humanos , Concentración de Iones de Hidrógeno , Células MCF-7 , Micelas , Oxidación-Reducción/efectos de los fármacos , Polietilenglicoles/química , Polímeros/farmacología , Especies Reactivas de Oxígeno/metabolismo
8.
Neural Plast ; 2019: 5271573, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31007684

RESUMEN

Motor capability recovery after ischemic stroke involves dynamic remodeling processes of neural connectomes in the nervous system. Various neuromodulatory strategies combining direct stimulating interventions with behavioral trainings for motor recovery after ischemic stroke have been developed. However, the effectiveness of these interventions varies widely due to unspecific activation or inhibition of undefined neuronal subtypes. Optogenetics is a functional and structural connection-based approach that can selectively activate or inhibit specific subtype neurons with a higher precision, and it has been widely applied to build up neuronal plasticities of the nervous system, which shows a great potential in restoring motor functions in stroke animal models. Here, we reviewed neurobiological mechanisms of enhanced brain plasticities underlying motor recovery through the optogenetic stimulation after ischemic stroke. Several brain sites and neural circuits that have been previously proven effective for motor function rehabilitation were identified, which would be helpful for a more schematic understanding of effective neuronal connectomes in the motor function recovery after ischemic stroke.


Asunto(s)
Isquemia Encefálica/fisiopatología , Encéfalo/fisiopatología , Plasticidad Neuronal , Optogenética , Rehabilitación de Accidente Cerebrovascular/métodos , Accidente Cerebrovascular/fisiopatología , Animales , Isquemia Encefálica/complicaciones , Humanos , Neurogénesis , Recuperación de la Función , Accidente Cerebrovascular/complicaciones
9.
BMC Vet Res ; 14(1): 144, 2018 Apr 28.
Artículo en Inglés | MEDLINE | ID: mdl-29704894

RESUMEN

BACKGROUND: Duck enteritis virus (DEV) belongs to the family Herpesviridae and is an important epornitic agent that causes economic losses in the waterfowl industry. The Chinese virulent (CHv) and attenuate vaccines (VAC) are two different pathogenic DEV strains. MicroRNAs (miRNAs) are a class of non-coding RNAs that regulate gene expression in viral infection. Nonetheless, there is little information on virulent duck enteritis virus (DEV)-encoded miRNAs. RESULTS: Using high-throughput sequencing, we identified 39 mature viral miRNAs from CHv-infected duck embryo fibroblasts cells. Compared with the reported 33 VAC-encoded miRNAs, only 13 miRNA sequences and 22 "seed sequences" of miRNA were identical, and 8 novel viral miRNAs were detected and confirmed by stem-loop RT-qPCR in this study. Using RNAhybrid and PITA software, 38 CHv-encoded miRNAs were predicted to target 41 viral genes and formed a complex regulatory network. Dual luciferase reporter assay (DLRA) confirmed that viral dev-miR-D8-3p can directly target the 3'-UTR of CHv US1 gene (p < 0.05). Gene Ontology analysis on host target genes of viral miRNAs were mainly involved in biological regulation, cellular and metabolic processes. In addition, 598 novel duck-encoded miRNAs were detected in this study. Thirty-eight host miRNAs showed significant differential expression after CHv infection: 13 miRNAs were up-regulated, and 25 miRNAs were down-regulated, which may affect viral replication in the host cell. CONCLUSIONS: These data suggested that CHv encoded a different set of microRNAs and formed a unique regulatory network compared with VAC. This is the first report of DEF miRNAs expression profile and an analysis of these miRNAs regulatory mechanisms during DEV infection. These data provide a basis for further exploring miRNA regulatory roles in the pathogenesis of DEV infection and contribute to the understanding of the CHv-host interaction at the miRNA level.


Asunto(s)
Enteritis/veterinaria , Herpesviridae/genética , MicroARNs/genética , Enfermedades de las Aves de Corral/virología , Animales , Células Cultivadas , Patos/genética , Patos/virología , Enteritis/virología , Regulación Viral de la Expresión Génica , Secuenciación de Nucleótidos de Alto Rendimiento/veterinaria , ARN Viral/genética , Reacción en Cadena en Tiempo Real de la Polimerasa/veterinaria
10.
Phytother Res ; 32(1): 115-124, 2018 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-29044703

RESUMEN

Radix Astragalus has been shown to exert beneficial effects regarding the prevention postmenopausal osteoporosis. However, its mechanism of action remains to be investigated. Calycosin, formononetin, and calycosin-7-O-ß-d-glucoside are the main isoflavone constituents of Astragalus. In this study, the abilities of these 3 compounds to promote osteogenic function of osteoblasts were compared, and the structure-activity relationships of these osteotrophic isoflavones were determined. Calycosin exhibited a greater effect than formononetin and calycosin-7-O-ß-d-glucoside regarding improvements in osteogenic function of osteoblasts, as demonstrated by cell proliferation, alkaline phosphatase activity, collagen I and osteocalcin secretion, and the number and area of mineralized bone nodules. This suggests that calycosin may be better than formononetin and calycosin-7-O-ß-d-glucoside at preserving bone mass. In addition, calycosin, formononetin, and calycosin-7-O-ß-d-glucoside stimulate the expression of bone morphogenetic protein 2 and runt-related transcription factor 2 proteins, which indicates that all 3 agents may promote the osteogenesis of osteoblasts via regulation of bone morphogenetic protein 2 expression. In conclusion, calycosin may be the best candidate, with higher osteogenic activity than formononetin and calycosin-7-O-ß-d-glucoside. The higher osteogenic activity of calycosin could be attributable to the superiority of its chemical structure (a hydroxyl group at position C3 of Ring B and no glucosyl group).


Asunto(s)
Medicamentos Herbarios Chinos/química , Isoflavonas/uso terapéutico , Osteoblastos/metabolismo , Raíces de Plantas/química , Planta del Astrágalo/química , Humanos , Isoflavonas/farmacología
11.
J Fluoresc ; 27(6): 2111-2117, 2017 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-28785903

RESUMEN

A novel fluorescein-based dual probe was designed and synthesized. The probe exhibited highly sensitive and selective colormetric response to Fe3+ and turn-on fluorescence response towards OCl- with very low detection limits of 100 and 50 nM, respectively. It was successfully applied for quantitative detection of Fe3+ and OCl- in real water samples. Moreover, probe 1 was expected to be a potentially powerful tool for studying and providing further insights into OCl- and Fe3+ chemistry in the near future.

12.
Pharm Biol ; 53(1): 110-6, 2015 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-25243871

RESUMEN

CONTEXT: Radix Dipsaci is a kidney tonifying herbal medicine with a long history of safe use for treatment of bone fractures and joint diseases in China. Previous studies have shown that Radix Dipsaci extract (RDE) could prevent bone loss in ovariectomized rats. OBJECTIVE: This study investigates the effect of RDE against bone loss induced by simulated microgravity. MATERIALS AND METHODS: A hindlimb unloading rat model was established to determine the effect of RDE on bone mineral density and bone microarchitecture. Twenty-four male Sprague-Dawley rats were divided into four groups (n = 6 per group): control (CON), hindlimb unloading with vehicle (HLU), hindlimb unloading treated with alendronate (HLU-ALN, 2.0 mg/kg/d), and hindlimb unloading treated with RDE (HLU-RDE, 500 mg/kg/d). RDE or ALN was administrated orally for 4 weeks. RESULTS: Treatment with RDE had a positive effect on mechanical strength, BMD, BMC, bone turnover markers, and the changes in urinary calcium and phosphorus excretion. MicroCT analysis showed that RDE significantly prevented the reduction of the bone volume fraction, connectivity density, trabecular number, thickness, tissue mineral density, and tissue mineral content as well as improved the trabecular separation and structure model index. DISCUSSION AND CONCLUSION: RDE was demonstrated to prevent the loss of bone mass induced by HLU treatment, which suggests the potential application of RDE in the treatment of microgravity-induced bone loss.


Asunto(s)
Conservadores de la Densidad Ósea/uso terapéutico , Dipsacaceae/química , Medicamentos Herbarios Chinos/uso terapéutico , Osteoporosis/prevención & control , Ingravidez/efectos adversos , Animales , Densidad Ósea/efectos de los fármacos , Conservadores de la Densidad Ósea/administración & dosificación , Conservadores de la Densidad Ósea/aislamiento & purificación , Calcio/sangre , Calcio/orina , Creatinina/sangre , Creatinina/orina , Medicamentos Herbarios Chinos/administración & dosificación , Medicamentos Herbarios Chinos/aislamiento & purificación , Fémur/efectos de los fármacos , Fémur/metabolismo , Suspensión Trasera , Masculino , Osteoporosis/sangre , Osteoporosis/etiología , Osteoporosis/orina , Fósforo/sangre , Fósforo/orina , Raíces de Plantas/química , Ratas Sprague-Dawley
13.
J Fluoresc ; 24(3): 775-86, 2014 May.
Artículo en Inglés | MEDLINE | ID: mdl-24492956

RESUMEN

Eight novel chlorinated fluorescent proteins-labeling probes with a linker and reactive group were prepared in 7 steps by the reaction of chlorinated resorcinols with 3, 6-dichloro-4-carboxyphthalic anhydride in the presence of methanesulfonic acid. Structures of target compounds and intermediates were determined via IR, MS, (1)H NMR and element analysis. The spectral properties of the chlorinated fluoresceins were studied. These fluorescent probes showed absorbance peaks at 508-536 nm and fluorescence peaks at 524-550 nm. It was found that they have absorption and emission maxima at long wavelengths and high fluorescence quantum yields. Emission spectra of chlorinated fluoresceins shifted towards long wavelength with increase in chlorine. The probes were used for fluorescence imaging of cells in order to investigate whether they can conjugate to cells. The fluorescence imaging of living cells showed that they were localized in cell nucleus. However, they were localized in cytosol of chemically fixed cells. These probes will be useful reagents for the preparation of stable fluorescent conjugates.


Asunto(s)
Fluoresceínas/síntesis química , Colorantes Fluorescentes/síntesis química , Halogenación , Proteínas/química , Coloración y Etiquetado/métodos , Núcleo Celular/metabolismo , Células Cultivadas , Fluorescencia , Humanos , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Microscopía Fluorescente , Osteoblastos/citología , Osteoblastos/metabolismo , Espectrometría de Fluorescencia , Espectrofotometría Infrarroja
14.
Biol Pharm Bull ; 37(1): 13-7, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-24141261

RESUMEN

The current study was designed to investigate the effects of 1-(1,3-benzodioxol-5-yl-carbonyl) piperidine (1-BCP) on swimming endurance capacity which as one indicator of fatigue in the weight-loaded forced swimming mice. Mice were given either vehicle or 1-BCP (0.1, or 0.2 mmol/kg body weight daily) by intraperitoneal injection once daily for 2 weeks. The 1-BCP groups showed a significant increase in swimming time to exhaustion compared with the control group. 1-BCP increased the liver glycogen (LG) and muscle glycogen (MG) contents significantly, while decreased the lactic acid (LA) and blood urea nitrogen (BUN) levels notably compared with control group. Besides, 1-BCP treatment also significantly improved the endogenous cellular antioxidant enzymes in mice by increasing the activities of superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GSH-Px). Therefore, this study demonstrated for the first time that the supplementation of 1-BCP, as a positive allosteric modulator of α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor, could enhance the endurance capacity of mice and facilitated them recovery from fatigue. Thus, we provide a new effective therapeutic strategy for fatigue.


Asunto(s)
Dioxoles/uso terapéutico , Fatiga/tratamiento farmacológico , Resistencia Física , Piperidinas/uso terapéutico , Receptores AMPA/metabolismo , Natación , Ácido alfa-Amino-3-hidroxi-5-metil-4-isoxazol Propiónico/metabolismo , Animales , Antioxidantes/metabolismo , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Nitrógeno de la Urea Sanguínea , Catalasa/metabolismo , Suplementos Dietéticos , Dioxoles/farmacología , Fatiga/metabolismo , Glutatión Peroxidasa/metabolismo , Glucógeno/metabolismo , Ácido Láctico/sangre , Hígado/metabolismo , Masculino , Ratones , Ratones Endogámicos , Músculo Esquelético/metabolismo , Piperidinas/farmacología , Superóxido Dismutasa/metabolismo
15.
Molecules ; 19(1): 1034-46, 2014 Jan 16.
Artículo en Inglés | MEDLINE | ID: mdl-24441653

RESUMEN

A series of benzamide derivatives such as 1-(1,3-benzodioxol-5-ylcarbonyl) piperidine (1-BCP) were synthesized by the reaction of substituted benzoic acids with piperidine, morpholine or pyrrolidine using a novel method. The crystals of these benzamide derivatives were obtained by recrystallization. Structures of target and intermediate compounds were determined via FT-IR, 1H-NMR and elemental analysis and X-ray crystallography of select examples. The crystal structures of these compounds have potential applications to identify the binding site for allosteric modulators of the α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor. The anti-fatigue effects of the benzamide derivatives in weight-loaded forced swimming mice were investigated in a swimming endurance capacity test used as an indicator of fatigue. The swimming times to exhaustion were longer in the b3, d3, and e3 groups than in the caffeine group (p<0.05). In conclusion, b3, d3 and e3 enhanced the forced swimming capacity of mice. The mechanism of the anti-fatigue effects will be studied in the future.


Asunto(s)
Benzamidas/síntesis química , Estimulantes del Sistema Nervioso Central/síntesis química , Animales , Benzamidas/química , Benzamidas/farmacología , Estimulantes del Sistema Nervioso Central/química , Estimulantes del Sistema Nervioso Central/farmacología , Cristalografía por Rayos X , Evaluación Preclínica de Medicamentos , Tolerancia al Ejercicio/efectos de los fármacos , Masculino , Ratones , Estructura Molecular , Esfuerzo Físico/efectos de los fármacos , Piperidinas/química , Espectroscopía Infrarroja por Transformada de Fourier , Natación
16.
Yao Xue Xue Bao ; 49(10): 1442-5, 2014 Oct.
Artículo en Zh | MEDLINE | ID: mdl-25577876

RESUMEN

To explore novel antifatigue agents targeting with AMPA receptor, 10 compounds were synthesized and their structures were confirmed by 1H NMR, ESI-MS and elemental analysis. 1-BCP was treated as the leading compound. The antifatigue activities were evaluated by weight-loaded forced swimming test, and the AMPA receptor binding affinities were tested with radioligand receptor binding assays. The results unveiled that 5b appeared to possess potent antifatigue activities and high affinity with AMPA receptor, which deserved further studies.


Asunto(s)
Benzamidas/farmacología , Fatiga/prevención & control , Animales , Benzamidas/química , Dioxoles/química , Dioxoles/farmacología , Piperidinas/química , Piperidinas/farmacología , Ensayo de Unión Radioligante , Receptores AMPA/metabolismo , Natación
17.
Pharmazie ; 68(9): 713-22, 2013 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-24147339

RESUMEN

The purpose of this systematic review is to assess the efficacy and pharmacological profiles of Herba Epimedii in osteoporosis therapy. Four databases were extensively retrieved that include two Chinese electronic databases (VIP Information and CNKI) and two English electronic databases (CA and MEDLINE). Herba Epimedii has been an important traditional herbal medicine for centuries in China and other Asian countries. Recently, quite a few pharmacological effects of Herba Epimedii, its extracts and active components have been identified that include improving bone health and cardiovascular function, regulating hormone level, modulating immunological function, and inhibiting tumor growth. The anti-osteoporosis activity of Herba Epimedii and its extracts have attracted world-wide attention. The literature search has revealed that a lot of studies have recently been carried out related to the bone-strengthening activity of Herba Epimedii and some of its active compounds, such as total flavonoids and icariin. Pharmacokinetic and toxicity studies have confirmed the efficacy and safety of Herba Epimedii and its most abundant active component icariin, while only a few authors have reviewed the anti-osteoporosis properties of the plants. So we summarize the work of various investigators on the effects of Herba Epimedii, its extracts and active components against osteoporosis. The underlying mechanism of osteoprotective action, derivatives of icariin, animal models and cell lines used in the research were also reviewed in this paper.


Asunto(s)
Conservadores de la Densidad Ósea/uso terapéutico , Medicamentos Herbarios Chinos/uso terapéutico , Epimedium/química , Osteoporosis/tratamiento farmacológico , Animales , Línea Celular , Bases de Datos Factuales , Modelos Animales de Enfermedad , Etnofarmacología , Flavonoides/química , Flavonoides/uso terapéutico , Humanos , Extractos Vegetales/uso terapéutico
18.
Zhongguo Zhong Yao Za Zhi ; 38(1): 105-11, 2013 Jan.
Artículo en Zh | MEDLINE | ID: mdl-23596885

RESUMEN

OBJECTIVE: To investigate the effects of naringin on the proliferation, differention and maturaion of rat calvarial osteoblasts (ROB). METHOD: Segregated neonatal SD rat skull, enzyme digestion to obtain ROB. The culture medium was replaced every three days. Serial subcultivation proceeded when cells covered with 80% culture dish. Naringin supplemented into the culture at 1 x 10(-4), 1 x 10(-5), 1 x 10(-6), 1 x 10(-7) mol x L(-1) respectively. MTT method was adopted in proliferation analysis and the activity of ALP was examined after induced 9 days. Search the best concentration and supplemented into the medium, then the osteogenic differentiation markers including the secretion amount of osteocalcin, osteopontin and bone morphogenetic protein-2 were compared between the naringin-supplemented group and the control. Total RNA was isolated and the mRNA level of bFGF, IGF-1, Runx-2, Osterix, ERa and ERbeta was investigated by Real time RT-PCR. Total protein also was isolated and the expression ERa, ERbeta and collagen I was examined by Western blot. After the addition of ICI 182.780, an inhibitor of the estrogen signal pathway, these index also was examined and the changes were compared. RESULT: The ROB proliferation was motivated by naringin dose-dependently. And it evidently leads to osteogenic process and maturation. 1 x 10(-5) mol x L(-1) is the best concentration. Naringin improved the secretion of osteocalcin, osteopontin, bone morphogenetic protein-2 and collagen I significantly. Besides, it can also enhanced the mRNA level of bFGF, IGF-1, Runx-2, Osterix, ERalpha and ERbeta. While all these effects can be restrained by ICI 182.780. CONCLUSION: The naringin with final concentration of 1 x 10(-5) mol x L(-1) enhances the osteogenic differentiation and maturation of ROB significantly, while the promoting effects vanished after the addition of ICI 182.780. These results suggesting that naringin is one of the phytoestrogens and have the activity of bone formation may via estrogen signal pathway, it can be developed into a new drug for osteoporosis therapy.


Asunto(s)
Diferenciación Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Medicamentos Herbarios Chinos/farmacología , Flavanonas/farmacología , Osteoblastos/efectos de los fármacos , Cráneo/citología , Fosfatasa Alcalina/genética , Fosfatasa Alcalina/metabolismo , Animales , Células Cultivadas , Factor I del Crecimiento Similar a la Insulina/genética , Factor I del Crecimiento Similar a la Insulina/metabolismo , Osteoblastos/citología , Osteoblastos/metabolismo , Osteocalcina/genética , Osteocalcina/metabolismo , Ratas , Ratas Sprague-Dawley , Cráneo/efectos de los fármacos , Cráneo/metabolismo
19.
Int J Biol Macromol ; 232: 123271, 2023 Mar 31.
Artículo en Inglés | MEDLINE | ID: mdl-36646352

RESUMEN

The most important function of skin is to prevent biological dehydration and protect internal structures from the environment. When a wound becomes infected, the bacteria cause a sustained inflammatory response at the infected site, further delaying the healing process. Therefore, the search for better antibacterial strategies has become a topic of great concern. Therefore, the development of multifunctional hydrogels with antibacterial properties, ROS removal, and hemostasis is urgently required for promoting wound healing process. Chitosan is the only cationic natural polysaccharide with good biocompatibility, antibacterial and hemostatic ability. It is a candidate material to prepare hydrogel wound dressing. Hyaluronic acid (HA) is a natural biological macromolecule that belongs to a group of heteropolysaccharides known as non-sulfated glycosaminoglycans. It is a major component of the skin extracellular matrix (ECM) and is involved in inflammation, angiogenesis, and tissue regeneration. Here, the hydrogel was designed with the natural macromolecular of the gallic acid-grafted quaternized chitosan (GA-QCS) and oxidized hyaluronic acid (OHA) via Schiff base and/or Michael addition reaction. It was found that the GA-QCS/OHA hydrogel exhibited multifunctional capabilities with injectable, hemostasis, degradation, and release of medicines. In addiation, GA-QCS/OHA hydrogels exhibited remarkable antioxidant and migration promoting effects in vitro. And the mupirocin-loaded GA-QCS/OHA hydrogels had inhibitory effects on E. coli (Gram-negative bacterium) and S. aureus (Gram-positive bacterium) in vitro. A full-thickness skin of S. aureus infection mouse wound model was used to test the bioactive effect of the hydrogels and the accelerated wound healing was obtained due to the inhibiting the proinflammatory factor TNF-α and upregulating the vascularization factor CD31. This study proposed an effective strategy based on antioxidant, antibacterial, self-healing multifunctional hydrogel for wound healing under various infectious complications. This natural macromolecular hydrogel could act as an effective reactive oxygen species scavenger to promote the wound healing in the future.


Asunto(s)
Quitosano , Ratones , Animales , Quitosano/farmacología , Quitosano/química , Hidrogeles/farmacología , Hidrogeles/química , Antioxidantes/química , Ácido Hialurónico/farmacología , Ácido Hialurónico/química , Staphylococcus aureus , Escherichia coli , Cicatrización de Heridas , Antibacterianos/farmacología , Antibacterianos/química
20.
Front Psychiatry ; 14: 1291988, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-38130293

RESUMEN

Background: Sexual dysfunction is commonly observed in individuals with Major Depressive Disorder (MDD), along with various psychological symptoms such as anxiety, somatic complaints, interpersonal sensitivity, and obsessive-compulsive tendencies. However, there is a research gap in understanding the impact of these psychological symptoms on sexual functioning in MDD. Furthermore, there is limited data on the incidence of sexual dysfunction among drug-naive MDD patients in West China. This study aims to determine the prevalence of sexual dysfunction in this patient population and explore its association with other psychological indicators. Methods: We conducted a retrospective analysis of patient data from October 2020 to September 2022 using propensity score matching. A focused group of 165 males and 490 females was selected from a total of 1941 MDD patients. This allowed for a comparative analysis of demographic data, as well as scores from the Self-Rating Depression Scale (SDS), Self-Rating Anxiety Scale (SAS), and Symptom Checklist-90 (SCL-90), the Arizona Sexual Experience Scale (ASEX). Results: Our findings reveal that 46.2% of drug-naive MDD patients experienced sexual dysfunction. Notably, there was a higher prevalence of sexual dysfunction among female patients (50.3%) compared to males (37.5%). MDD patients without sexual dysfunction consistently exhibited higher SDS scores than those with sexual dysfunction (p < 0.01), There were no statistically significant differences between male and female MDD patients with or without concomitant sexual dysfunction in terms of Somatic complaints, Obsessive-compulsive, Interpersonal sensitivity, Anxiety, Phobic anxiety, Paranoid ideation, Psychoticism and Diet/sleep difficulties (p > 0.05). In addition, male MDD patients with sexual dysfunction showed a emerging trend towards elevated Hostility scores on the SCL-90 (p = 0.058), male MDD patients with sexual dysfunction showed an increasing trend in hostility scores on the SCL-90, whereas female MDD patients with sexual dysfunction did not show such a trend. Conclusion: The study highlights a significant gender difference in the prevalence of sexual dysfunction among MDD patients, with females being more susceptible than males. There is a positive correlation between the severity of depression and sexual dysfunction in both genders. Interestingly, male MDD patients demonstrated a potential protective effect of hostility against sexual dysfunction, which was not observed in female patients.

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