RESUMEN
Histone methylation is one of the key post-translational modifications that plays a critical role in various heart diseases, including diabetic cardiomyopathy. A great deal of evidence has shown that histone methylation is closely related to hyperglycemia, insulin resistance, lipid and advanced glycation end products deposition, inflammatory and oxidative stress, endoplasmic reticulum stress and cell apoptosis, and these pathological factors play an important role in the pathogenesis of diabetic cardiomyopathy. In order to provide a novel theoretical basis and potential targets for the treatment of diabetic cardiomyopathy from the perspective of epigenetics, this review discussed and elucidated the association between histone methylation and the pathogenesis of diabetic cardiomyopathy in details.
Asunto(s)
Humanos , Diabetes Mellitus , Cardiomiopatías Diabéticas/patología , Histonas , Metilación , Estrés Oxidativo , Procesamiento Proteico-PostraduccionalRESUMEN
Persistent infection with high-risk human papillomavirus (HR-HPV) is a well-defined etiology of cervical cancer, but not all HR-HPV infections lead to cervical cancer, indicating that many factors are involved in the regulation of HR-HPV pathogenicity. Toll-like receptors (TLRs) are a class of pattern recognition receptors that specifically recognize pathogen-associated molecular patterns (PAMPs) to provoke host innate and adaptive immunity against viruses. Relevant studies have shown that HR-HPV alters the local immune microenvironment by regulating the expression and signaling pathways of TLRs, leading to persistent infection with HR-HPV as well as cervical cancer. This review summarized and discussed the immune function and possible pathogenesis of TLRs in HPV infection-caused cervical cancer and the application of TLRs agonists in HPV vaccines.
RESUMEN
Ubiquitin-proteasome system (UPS) plays an important role in neurodegenerative diseases, such as Alzheimer's disease (AD), Parkinson's disease (PD), and Huntington's disease (HD). The discovery of UPS activators for anti-neurodegenerative diseases is becoming increasingly important. In this study, we aimed to identify potential UPS activators using the high-throughput screening method with the high-content fluorescence imaging system and validate the neuroprotective effect in the cell models of AD. At first, stable YFP-CL1 HT22 cells were successfully constructed by transfecting the YFP-CL1 plasmid into HT22 cells, together with G418 screening. The degradation activity of the test compounds via UPS was monitored by detecting the YFP fluorescence intensity reflected by the ubiquitin-proteasome degradation signal CL1. By employing the high-content fluorescence imaging system, together with stable YFP-CL1 HT22 cells, the UPS activators were successfully screened from our established TCM library. The representative images were captured and analyzed, and quantification of the YFP fluorescence intensity was performed by flow cytometry. Then, the neuroprotective effect of the UPS activators was investigated in pEGFP-N1-APP (APP), pRK5-EGFP-Tau P301L (Tau P301L), or pRK5-EGFP-Tau (Tau) transiently transfected HT22 cells using fluorescence imaging, flow cytometry, and Western blot. In conclusion, our study established a high-content fluorescence imaging system coupled with stable YFP-CL1 HT22 cells for the high-throughput screening of the UPS activators. Three compounds, namely salvianolic acid A (SAA), salvianolic acid B (SAB), and ellagic acid (EA), were identified to significantly decrease YFP fluorescence intensity, which suggested that these three compounds are UPS activators. The identified UPS activators were demonstrated to clear AD-related proteins, including APP, Tau, and Tau P301L. Therefore, these findings provide a novel insight into the discovery and development of anti-AD drugs.
Asunto(s)
Humanos , Enfermedad de Alzheimer/tratamiento farmacológico , Fármacos Neuroprotectores , Imagen Óptica , Complejo de la Endopetidasa Proteasomal , UbiquitinaRESUMEN
Objective:To observe the effects of Albiziae Flos (AF) and Polygalae Radix (PR) alone and their combination on the improvement of depression-like behavior in rats with chronic unpredictable stress (CUS) as well as on hippocampal ultrastructure and the expression of cyclic adenosine monophosphate response element binding protein (CREB) and nicotinamide adenine dinucleotide phosphate oxidase 2 (NOX2), to explore their action mechanisms. Method:Seventy-two Wistar rats were randomly divided into the normal group, model group, AF group, PR group, AF-PR group, and fluoxetine group. Rats in all groups except for the normal group were exposed to CUS and separated feeding to induce depression. Since the first day of modeling, rats in the AF group, PR group, AF-PR group were provided with the corresponding decoction containing 1.05 g·kg<sup>-1</sup> total crude drug by gavage, the ones in the fluoxetine group with 2.1 mg·kg<sup>-1</sup> fluoxetine hydrochloride aqueous solution, and those in the normal group and model group with the distilled water, for 28 successive days. The open field test and forced swimming test were performed 1 d before modeling and 7, 14, 21, 28 d after modeling, respectively. The morphological changes in hippocampus were observed under an electron microscope on the 28<sup>th</sup> day. The superoxide dismutase (SOD) and malondialdehyde (MDA) levels in hippocampus were detected by ultraviolet spectrophotometry, and the expression levels of CREB and NOX2 were detected by real-time polymerase chain reaction (Real-time PCR) and Western blot. Result:The behavioral experiment results showed that the number of horizontal activities and sugar water consumption in the model group declined as compared with those in the normal group, while the immobility time in the forced swimming test was prolonged (<italic>P</italic><0.05, <italic>P</italic><0.01). Compared with the model group, the AF group, PR group, and AF-PR group exhibited elevated number of horizontal activities, increased sugar water consumption but shortened immobility time in the forced swimming test (<italic>P</italic><0.05, <italic>P</italic><0.01). Compared with the AF group or PR group, the AF-PR group showed significantly different behavioral indexes (<italic>P</italic><0.05). Morphological results showed that the mitochondria of the model group were obviously swollen and the ultrastructure of the hippocampus was destroyed. By contrast, the hippocampal ultrastructure in each administration group was close to normal. The comparison with the normal group revealed that the activity of SOD in the hippocampus of the model group was significantly reduced, whereas the content of MDA was elevated (<italic>P</italic><0.01). Compared with the model group, the AF group, PR group, and AF-PR group displayed increased activity of SOD and decreased content of MDA in the hippocampal tissues (<italic>P</italic><0.05, <italic>P</italic><0.01). Compared with AF or PR alone, the herbal pair AF-PR resulted in significant differences in the above-mentioned indexes (<italic>P</italic><0.05, <italic>P</italic><0.01). The results of Real-time PCR and Western blot demonstrated that NOX2 expression in the hippocampus of the model group was up-regulated in comparison with that in the normal group, while the CREB expression was down-regulated (<italic>P</italic><0.05, <italic>P</italic><0.01). Compared with the model group, the AF group, PR group, and AF-PR group all showed diminished NOX2 expression but elevated CREB expression in the hippocampal tissues (<italic>P</italic><0.05, <italic>P</italic><0.01). The protein expression levels of NOX2 and CREB in the AF group or PR group were significantly different from those in the AF-PR group (<italic>P</italic><0.01). Conclusion:AF and PR alone and their combination improve the depression-like behavior of rats exposed to CUS, which may be related to the reduction of oxidative stress, the up-regulation of CREB expression, and the down-regulation of NOX2 expression in hippocampus.
RESUMEN
OBJECTIVE@#To explore the genetic basis for a female with a peripheral lymphocyte karyotype of trisomy 18 but normal intelligence.@*METHODS@#G-banding karyotype analysis, fluorescence in situ hybridization (FISH) and single nucleotide polymorphism microarray (SNP array) were employed to analyze the peripheral blood sample and buccal cells from the patient.@*RESULTS@#Chromosomal karyotyping, SNP array and FISH analysis of the patient's peripheral blood all suggested 47,XX,+18. Interphase FISH analysis of buccal cells, however, revealed presence of 45,X and low percentage of trisomy 18 and monosomy 18.@*CONCLUSION@#The clinical manifestation of germ layer chromosomal mosaicism is complex. The impact of the genetic disorder on the individual will depend on the structure and function derived from the affected germ layer.
Asunto(s)
Femenino , Humanos , Hibridación Fluorescente in Situ , Inteligencia , Cariotipo , Cariotipificación , Linfocitos , Mosaicismo , Mucosa Bucal , Polimorfismo de Nucleótido Simple , Síndrome de la Trisomía 18 , GenéticaRESUMEN
Acupuncture has been widely used for treating diseases since the ancient days in China, but the mechanism by which acupuncture exerts such powerful roles is unclear. Epigenetics, including DNA methylation, histone modification, and post-transcriptional regulation of miRNAs, is the study of heritable changes in gene expression that do not include DNA sequence alterations. Epigenetics has become a new strategy for the basic and clinical research of acupuncture in the last decade. Some investigators have been trying to illustrate the mechanism of acupuncture from an epigenetics perspective, which has shed new lights on the mechanisms and applications of acupuncture. Moreover, the introduction of epigenetics into the regulatory mechanism in acupuncture treatment has provided more objective and scientific support for acupuncture theories and brought new opportunities for the improvement of acupuncture studies. In this paper, we reviewed the literatures that has demonstrated that acupuncture could directly or indirectly affect epigenetics, in order to highlight the progress of acupuncture studies correlated to epigenetic regulations. We do have to disclose that the current evidence in this review is not enough to cover all the complex interactions between multiple epigenetic modifications and their regulations. However, the up-to-date results can help us to better understand acupuncture's clinical applications and laboratory research.
RESUMEN
To study the biopharmaceutics characteristics of paris saponin VII (PSVII). The solubility of PSVII was evaluated by measurement of the equilibrium solubility in different solvents and media. The permeability of PSVII was evaluated by measuring the oil/water partition coefficient (lgP) and determining the apparent permeability coefficient (PC) on a mono-layer Caco-2 cell model. The effects of p-glycoprotein and multidrug resistance related protein 2 on PSVII transport in mono-layer Caco-2 cell model were further investigated. Finally, the small intestinal absorption of PSVII was investigated in rat. In solvents of different pH, the equilibrium solubility of PSVII was quite low, and the dose number of PSVII was larger than 1. The lgP of PSVII was less than 0. The apparent permeability coefficient [PC] of PSVII in mono-layer Caco-2 cell model was less than 14.96 × 10 cm·s, and the efflux ratio of PSVII in mono-layer Caco-2 cell model was less than 1. The transport rate of PSVII in mono-layer Caco-2 cell model was not affected by the inhibitors of p-glycoprotein and multidrug resistance related protein 2. After oral administration, PSVII could be detected in rat intestinal contents, but could not be detected in the small intestinal mucosa. PSVII showed low solubility and permeability, which would result in low oral bioavailability in clinic. PSVII belonged to Class IV compound in biopharmaceutics classification system.
RESUMEN
Objective:To investigate the effect of Yisui Jiedu prescription on hippocampal neuron damage in vascular dementia (VD) rats and to regulate phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt)/recombinant Bcl-2 associated death promoter (Bad) mechanisms of signaling pathways of neuronal apoptosis. Method:The 40 SD rats were divided into sham operation group, model group, donepezil hydrochloride group and Yisui Jiedu prescription group, with 10 rats in each group.VD animal model was prepared by bilateral carotid artery permanent ligation (2-VO) method.The sham operation group and the model group were intragastrically administered with normal saline, the donepezil hydrochloride group was intragastrically administered with donepezil hydrochloride 0.52 mg·kg-1. The Yisui Jiedu prescription group was administered with Yisui Jiedu prescription (11.11 g·kg-1), 1 time/d . After 30 days, Morris water maze was used to test the learning and memory ability of rats, hematoxylin-eosin (HE) staining was used to observe the histomorphological structure of hippocampal CA1 region. Ultrasound of neuron in rat hippocampal CA1 region was observed by transmission electron microscopy (TEM).Real-time fluorescent quantitative(Real-time PCR) was used to detect the Akt, Bad mRNA expression.Western blot was used to detect the Akt, p-Akt and Bad protein expression in hippocampus. Result:Compared with sham operation group, the learning and memory ability of model group decreased significantly(P<0.05). The pathological structure and neuronal ultrastructure of the hippocampus were changed obviously. Hippocampal tissue Akt mRNA and the Akt,p-Akt protein expression level decreased significantly(P<0.05), and the levels of Bad mRNA and protein were significantly increased (P<0.05). Compared with model group, Yisui Jiedu prescription group can significantly improve the learning and memory ability of rats, improve the neuronal cells and ultrastructural changes in hippocampal CA1 area,and increase the expression of Akt mRNA and Akt,p-Akt protein in hippocampus. Decreased Bad mRNA and Bad protein expression levels (P<0.05). Conclusion:Yisui Jiedu prescription can significantly improve the learning and memory ability of VD rats, improve the ultrastructural pathological changes of hippocampus and neurons, and repair damaged neurons, which may promote Akt phosphorylation and activate PI3K/Akt/Bad. The signaling pathway plays a role in the defense of neurons against apoptosis.
RESUMEN
OBJECTIVE@#To observe the effects of electroacupuncture (EA) on sympathetic nerve-related substance in myocardial tissue in mice with myocardial ischemia (MI), and to explore its possible mechanism.@*METHODS@#Thirty adult male C57BL/6 mice were randomly divided into a sham operation group, a model group and an EA group, 10 mice in each one. The model of MI was established in the model group and EA group by ligating the left anterior descending branch of coronary artery. The mice in the sham operation group were not treated with ligating at left anterior descending branch of coronary artery, but the remaining procedure was similar with the model group. The mice in the EA group were treated with EA at "Neiguan" (PC 6) with 2 Hz/100 Hz of frequency and 2 mA of intensity, 20 min per treatment, once a day for totally 5 days. No EA was given for model group and sham operation group. The electrocardiogram was recorded and △ST value was calculated to evaluate the model. TTC staining was applied to evaluate the infarct size. Immunohistochemical (IHC) method was applied to evaluate the positive nerve fiber density in myocardial tissue. Western blot method was applied to test the protein expression levels of neuregulin-1 (NRG-1), tyrosine hydroxylase (TH), growth associated protein-43 (GAP-43).@*RESULTS@#The electrocardiogram (lead II) results indicated compared with the sham operation group, the S-T segments in the model group and EA group were increased obviously (both <0.01), indicating the MI model was established successfully. The TTC staining results indicated compared with sham operation group, the infarction size was significantly increased in the model group (<0.01); compared with the model group, the infarction size in the EA group was significantly reduced (<0.01). The IHC results indicated compared with the sham operation group, the positive nerve fiber density in myocardial was increased in the model group (<0.01); compared with the model group, the positive nerve fiber density in myocardial was reduced in the EA group (<0.05). The Western blot results indicated compared with the sham operation group, the expression levels of TH, NRG-1 and GAP-43 were significantly increased in the model group (<0.01); compared with the model group, the expression level of TH and GAP-43 were significantly reduced (<0.01) and that of NRG-1 was increased in the EA group (<0.05).@*CONCLUSION@#EA could increase the expression of NRG-1 and reduce the expression of TH and GAP-43 in myocardial tissues in MI mice, which could suppress sympathetic nerve hyperexcitability after infarction to achieve myocardial protection effect.
Asunto(s)
Animales , Masculino , Ratones , Enfermedad de la Arteria Coronaria , Electroacupuntura , Ratones Endogámicos C57BL , Isquemia Miocárdica , MiocardioRESUMEN
Mixed linked leukemia 4 (MLL4) is a specific methyltransferase of histone 3 position lysine 4 (H3K4). It is also one of the important members of COMPASS/Set1-like protein complex. Both MLL4 protein itself and its mediated H3K4 methylation modification can cause changes in chromatin structure and function, thus regulating gene transcription and expression. With the studies of MLL4 protein in recent years, the roles of MLL4 gene, MLL4 protein and protein complex in the development of tissues and organs, tumor diseases and other physiological and pathophysiological processes have been gradually revealed. In this paper, the research progress of MLL4 gene, MLL4 protein characteristics, biological function and its effect on disease were reviewed, in order to further understand the effect of histone methyltransferase on gene expression regulation, as well as its non-enzyme dependent function. This paper may provide new ideas for the prevention, diagnosis and treatment of related diseases.
Asunto(s)
Humanos , Proteínas de Unión al ADN , Fisiología , N-Metiltransferasa de Histona-Lisina , Fisiología , Histonas , Química , MetilaciónRESUMEN
Aim To explore the novel anti-fatigue a-gents targeting AMPA receptor. Methods Three ben-zoic acids of different methoxy substitutions were em-ployed, including piperonylic acid, 3,4,5-trimethoxy benzoic acid and 3,4-dimethoxy benzoic acid, which as mother nucleus and cyclic aliphatic amine or pheny-lpiperazine derivatives were introduced to modify the nitrogen atoms connecting to amino bonds. Forty-three compounds were synthesized and identified by 1 H-NMR. MTT assay, then pentobarbital induced hypno-sis experiment and mice burden swimming experiment were applied respectively to evaluate the new synthesized compounds’ cytotoxicity, CNS excitability and anti-fatigue activity. Results Compound 2j had low cytotoxicity,presenting certain central excitability and significant advantages on anti-fatigue. Conclusion The further development of compounds 2j with good anti-fatigue activities could be cultivated in further study.
RESUMEN
<p><b>OBJECTIVE</b>To investigate diagnostic value of MRI, X ray and CT for bone infarction in children with systemic lupus erythematosus.</p><p><b>METHODS</b>Eleven systemic lupus erythematosus children with bone infarction were retrospectively analyzed from January 2015 to January 2017 , and tested by MRI, X-ray and CT. Among them, including 1 male and 10 females aged from 6 to 16 years old with an average of 13 years old. All patients were detected by MRI, 9 patients were detected by X-ray and 3 patients were detected by CT, imaging findings were analyzed.</p><p><b>RESULTS</b>The location of bone infarction involved 60 sits, 30 sites located on metaphyseal-diaphyseal region, 8 located on patella, 21 located on epiphysis, and 1 located on talus. Focus of 11 patients were detected by MRI, the main manifestation showed geographic change, long T1 and T2 signal could seen around focus, and showed double ring sign and three ring sign; 5 of 9 patients by X-ray examination detected focus;2 of 3 patients by CT examination detected focus. No abnormity seen at early stage by X-ray and CT examination, and low density focus around harden edge at chronic stage.</p><p><b>CONCLUSIONS</b>MRI could display bone fracture at early stage, X-ray and CT could only display lesion at chronic stage, MRI is the most effective method in diagnosing bone infarction.</p>
Asunto(s)
Adolescente , Niño , Femenino , Humanos , Masculino , Huesos , Diagnóstico por Imagen , Patología , Infarto , Diagnóstico por Imagen , Lupus Eritematoso Sistémico , Imagen por Resonancia Magnética , Radiografía , Tomografía Computarizada por Rayos XRESUMEN
Objective: To assess the feasibility of HEAD-US scale in the clinical application of hemophilic arthropathy (HA) and propose an optimized ultrasound scoring system. Methods: From July 2015 to August 2017, 1 035 joints ultrasonographic examinations were performed in 91 patients. Melchiorre, HEAD-US (Hemophilic Early Arthropathy Detection with UltraSound) and HEAD-US-C (HEAD-US in China) scale scores were used respectively to analyze the results. The correlations between three ultrasound scales and Hemophilia Joint Health Scores (HJHS) were evaluated. The sensitivity differences of the above Ultrasonic scoring systems in evaluation of HA were compared. Results: All the 91 patients were male, with median age of 16 (4-55) years old, including 86 cases of hemophilia A and 5 cases hemophilia B. The median (P25, P75) of Melchiorre, HEAD-US and HEAD-US-C scores of 1 035 joints were 2(0,6), 1(0,5) and 2(0,6), respectively, and the correlation coefficients compared with HJHS was 0.747, 0.762 and 0.765 respectively, with statistical significance (P<0.001). The positive rates of Melchiorre, HEAD-US-C and HEAD-US scale score were 63.0% (95%CI 59.7%-65.9%), 59.5% (95%CI 56.5%-62.4%) and 56.6% (95%CI 53.6%-59.6%) respectively, and the difference was statistically significant (P<0.001). Even for 336 cases of asymptomatic joints, the positive rates of Melchiorre, HEAD-US-C and HEAD-US scale score were 25.0% (95%CI 20.6%-29.6%), 17.0% (95%CI 12.6%-21.1%) and 11.9% (95%CI 8.4%-15.7%) respectively, and the difference was statistically significant (P<0.001). There were significant changes (P<0.05) in the ultrasonographic score of HA before and after onset of hemorrhage in 107 joints of 40 patients. The difference in variation amplitude of HEAD-US-C scores and HEAD-US scores before and after joint bleeding was statistically significant (P<0.001). Conclusion: Compared with Melchiorre, there were similar good correlations between HEAD-US, HEAD-US-C and HJHS. HEAD-US ultrasound scoring system is quick, convenient and simple to use. The optimized HEAD-US-C scale score is more sensitive than HEAD-US, especially for patients with HA who have subclinical state, which make up for insufficiency of sensitivity in HEAD-US scoring system.
Asunto(s)
Adolescente , Adulto , Niño , Preescolar , Humanos , Masculino , Persona de Mediana Edad , Adulto Joven , China , Hemartrosis , Hemofilia A , Hemofilia B , UltrasonografíaRESUMEN
Objective: To explore the evaluation of joint injury by HEAD-US-C (Hemophilic Early Arthropathy Detection with UltraSound in China, HEAD-US-C) in patients with moderate or severe hemophilia A treated with prophylaxis vs on-demand. Methods: The patients from June 2015 to July 2017 with moderate or severe hemophilia A were examined by ultrasound imaging of the elbows, knees and ankles; Meanwhile the HEAD-US-C ultrasound assessment scale and hemophilia joint health score scale 2.1 (HJHS2.1) were used to score the joint status. The correlation between the HEAD-US-C and HJHS score was performed in prophylaxis group and on-demand group patients, respectively. Results: A total of 925 cases of joint ultrasonography were conducted in 70 patients with moderate or severe hemophilia A. Among patients with moderate hemophilia, the median (IQR) of HEAD-US-C score and HJHS score in on-demand group were significantly higher than those in the prophylaxis group[1 (0, 6) vs 0.5 (0, 3) , z=0.177, P=0.046],[2 (0, 4) vs 2 (0, 3) z=0.375, P=0.007], even though there was no significant difference of the median (IQR) number of annualized target joints bleeding episodes between on-demand and prophylaxis groups[1 (0, 7) vs 1 (0, 5) , z=1.271, P=0.137]. Unlike in moderate cases, on-demand treatment group had more annualized target joints bleeding episodes than prophylaxis group among patients with severe hemophilia[3 (0, 8) vs 2 (0, 8) , z=0.780 P=0.037]. The prophylaxis group compared favorably with on-demand therapy group in terms of HEAD-US-C score[1 (0, 6) vs 4 (0, 7) , z=2.189, P=0.008], and HJHS score[2 (0, 5) , 4 (1, 6) , z=3646, P<0.001]for the severe hemophilia patients. The positive correlation between HEAD-US-C score and HJHS score was identified (P<0.05) , whether on-demand treatment or prophylaxis groups. The correlation coefficient between HEAD-US-C score and HJHS score in on-demand treatment and prophylaxis groups were 0.739 (95% CI 0.708-0.708) , 0.865 (95% CI 0.848-0.848) respectively, and 95% CI didn't overlap (P<0.05) , indicating that the correlation coefficient in prophylaxis group had stronger correlation than that in on-demand group. Conclusions: Clinical effects of prophylaxis were significantly better than those of on-demand treatment in patients with moderate or se-vere haemophilia A. HEAD-US-C scoring system could effectively evaluate joints damage in hemophilia A patients treated with on-demand or prophylaxis, companied by significantly positive correlation with HJHS clinical evaluation system, and provided objective index for clinical effect assessment.
Asunto(s)
Humanos , China , Hemofilia A , Hemorragia , Artropatías , UltrasonografíaRESUMEN
Ten compounds were isolated from the barks of Jasminum giraldii by means of various of chromatographic techniques such as silica gel, Sephadex LH-20 and Rp-HPLC. Their structures were identified by spectroscopic data analysis as (+)-medioresinol (1), (+) -syringaresinol (2), syringaresinol-4'-O-beta-D-glucopyranoside (3), oleanic acid (4), 3-methoxy-4-hydroxy-trans-cinnamaldehyde (5), trans-sinapaldehyde (6), syringaldehyde (7), 1-(4-methoxy -phenyl) -ethanol (8), trans-cinnamic acid (9), and 4-(1-methoxyethyl) -phenol (10). Among them, compounds 1-3, 5-8 and 10 were isolated from the J. genus for the first time and compounds 4 and 9 were obtained from J. giraldii for the first time. In the DPPH free radical scavenging assay, compound 1 exhibited significant activity (IC50 55.1 micromol x L(-1)), compared with vitamin C(IC50 59.9 micromol x L(-1)); and compound 2 showed moderate activity (IC50 79.0 micromol x L(-1)), compared with 2, 6-di-tert-butyl4-methylphenol (IC50 236 micromol x L(-1)).
Asunto(s)
Antioxidantes , Química , Medicamentos Herbarios Chinos , Química , Jasminum , Química , Espectroscopía de Resonancia Magnética , Estructura Molecular , Espectrometría de Masa por Ionización de ElectrosprayRESUMEN
Ten compounds were isolated from the leaf of Eucommia ulmoides by means of recrystallization and chromatographic techniques such as D-101 macroporous resin, MCI resin, ODS gel, Sephadex LH-20 and Rp-HPLC. Their structures were identified by NMR spectral analyses as kaempferide 3-O-beta-D-glucoside (1), quercetin-3-O-beta-D-glucoside (2), quercetin (3), quercetin-3-O-beta-D-xylosyl-(1-->2)-beta-D-galactoside (4), kaempferol-3-O-alpha-L-rhamnosyl-(1-->6)-beta-D-glucoside (5), (2S,3S)-taxifolin 3-O-beta-D-glucoside (6) ,4-hydroxy cinnamic acid (7), (+)-cycloolivil (8), pinoresinol beta-D-glucoside (9), squalene (10). Among them compounds 1,5-7,10 were isolated from the Eucommia genus for the first time. In the DPPH free radical scavenging assay, compound 2 exhibited significant activity (IC50 13.7 micromol x L(-1)), compared with vitamin C (IC50 59.9 micromol x L(-1)); compounds 1, 3 and 9 showed moderate activity (IC50 161,137, 214 micromol x L(-1)), compared with 2,6-di-tert-butyl-4-methylphenol (IC50 236 micromol x L(-1)); compound 4 and 6 showed weak activity (IC50 264, 299 micromol x L(-1)).
Asunto(s)
Antioxidantes , Química , Cromatografía Líquida de Alta Presión , Medicamentos Herbarios Chinos , Química , Eucommiaceae , Química , Espectroscopía de Resonancia Magnética , Estructura Molecular , Hojas de la Planta , QuímicaRESUMEN
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)
Animales , Benzamidas , Química , Farmacología , Dioxoles , Química , Farmacología , Fatiga , Piperidinas , Química , Farmacología , Ensayo de Unión Radioligante , Receptores AMPA , Metabolismo , NataciónRESUMEN
<p><b>OBJECTIVE</b>To explore the feasibility of karyotype analysis using cells cultured from fetal bladder centesis samples.</p><p><b>METHODS</b>Samples were derived from fetal bladder centesis for 3 fetuses featuring giant bladder and oligohydramnios. Following in vitro culture, cells were routinely processed and stained for chromosome analysis.</p><p><b>RESULTS</b>For all 3 cases, cell culture has achieved success. Sufficient metaphase cells were obtained for chromosome counting and karyotype analysis. The karyotypes of the 3 fetuses were respectively 46, XY, 46, XX, t(1;5)(q22;q12)[7]/46, XX[4], and 46, XY.</p><p><b>CONCLUSION</b>Cells cultured from fetal bladder centesis may be used for karyotype analysis following in vitro culturing. This new approach can enable prenatal chromosome analysis for fetuses featuring smaller gestational weeks, giant bladder and oligohydramnios.</p>
Asunto(s)
Femenino , Humanos , Embarazo , Células Cultivadas , Cariotipificación , Diagnóstico Prenatal , Métodos , Vejiga Urinaria , Anomalías CongénitasRESUMEN
<p><b>OBJECTIVE</b>To evaluate anti-depressive effects of acupuncture on selective serotonin reuptake inhibitors (SSRIs).</p><p><b>METHODS</b>Totally 60 patients with depression were randomly assigned to the control group (30 cases) and the treatment group (30 cases). All patients took one kind of SSRIs. Those in the treatment group were additionally treated by acupuncture. All were treated for 6 weeks. Patients' efficacies were evaluated with Hamilton Depression Scale (HAMD), Self-rating Depression Scale (SDS), and Eisenberg antidepressant side effects scale (Asberg).</p><p><b>RESULTS</b>Compared with the control group after 6 weeks of treatment, the cured-markedly effective rate was improved by 33.4% in the treatment group (P < 0.05). The HAMD was lower in the treatment group. The tendency of interaction of sleep disorder factor and anxiety/somatization factor was different between at the end of 1-week treatment and at the end of 6-week treatment in the treatment group (P < 0.05). The SDS score decreased at the end of 6-week treatment in the treatment group. The reduction rate was elevated by 19.23% (P < 0.05). By the end of 6-week treatment, the average score of Asberg decreased by 3.77 score in average in the treatment group, while it decreased by 0.07 score in average in the control group (P < 0.05).</p><p><b>CONCLUSION</b>Acupuncture could effectively improve anti-depressive effects of SSRIs and reduce their adverse reactions.</p>
Asunto(s)
Adulto , Anciano , Femenino , Humanos , Masculino , Persona de Mediana Edad , Adulto Joven , Terapia por Acupuntura , Antidepresivos , Farmacología , Usos Terapéuticos , Depresión , Terapéutica , Inhibidores Selectivos de la Recaptación de Serotonina , Farmacología , Usos Terapéuticos , Resultado del TratamientoRESUMEN
<p><b>OBJECTIVE</b>To investigate the effects of naringin on the proliferation, differention and maturaion of rat calvarial osteoblasts (ROB).</p><p><b>METHOD</b>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.</p><p><b>RESULT</b>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.</p><p><b>CONCLUSION</b>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.</p>