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1.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-970570

RESUMO

The present study investigated the chemical constituents in the aerial part of Cannabis sativa. The chemical constituents were isolated and purified by silica gel column chromatography and HPLC and identified according to their spectral data and physicochemical properties. Thirteen compounds were isolated from the acetic ether extract of C. sativa and identified as 3',5',4″,2-tetrahydroxy-4'-methoxy-3-methyl-3″-butenyl p-disubstituted benzene ethane(1), 16R-hydroxyoctadeca-9Z,12Z,14E-trienoic acid methyl ester(2),(1'R,2'R)-2'-(2-hydroxypropan-2-yl)-5'-methyl-4-pentyl-1',2',3',4'-tetrahydro-(1,1'-biphenyl)-2,6-diol(3), β-sitosteryl-3-O-β-D-glucopyranosyl-6'-O-palmitate(4), 9S,12S,13S-trihydroxy-10-octadecenoate methyl ester(5), benzyloxy-1-O-β-D-glucopyranoside(6), phenylethyl-O-β-D-glucopyranoside(7), 3Z-enol glucoside(8), α-cannabispiranol-4'-O-β-D-glucopyranose(9), 9S,12S,13S-trihydroxyoctadeca-10E,15Z-dienoic acid(10), uracil(11), o-hydroxybenzoic acid(12), and 2'-O-methyladenosine(13). Compound 1 is a new compound, compound 3 is a new natural product, and compounds 2, 4-8, 10, and 13 were isolated from Cannabis plant for the first time.


Assuntos
Cannabis , Produtos Biológicos , Ésteres , Di-Hidroestilbenoides , Componentes Aéreos da Planta
2.
Mol Divers ; 26(1): 27-38, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33200293

RESUMO

Here, two series of novel ursolic acid-based 1,2,4-triazolo[1,5-a]pyrimidines derivatives were synthesized and screened for their anti-inflammatory activity by evaluating their inhibition effect of using LPS-induced inflammatory response in RAW 264.7 macrophages in vitro; the effects of different concentrations of the compounds on the secretion of nitric oxide (NO) and inflammatory cytokines including TNF-α and IL-6 were evaluated. Their toxicity was also assessed in vitro. Results showed that the most prominent compound 3 could significantly decrease production of the above inflammatory factors. Docking study was performed for the representative compounds 3, UA, and Celecoxib to explain their interaction with cyclooxygenase-2 (COX-2) receptor active site. In vitro enzyme study implied that compound 3 exerted its anti-inflammatory activity through COX-2 inhibition.


Assuntos
Anti-Inflamatórios , Pirimidinas , Anti-Inflamatórios/química , Ciclo-Oxigenase 2/metabolismo , Lipopolissacarídeos/toxicidade , Simulação de Acoplamento Molecular , Pirimidinas/farmacologia , Relação Estrutura-Atividade , Triterpenos , Ácido Ursólico
3.
Mol Divers ; 26(2): 1129-1139, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-34080112

RESUMO

In order to discover novel anti-inflammatory agents, three series of compounds obtained by appending 1,2,3-triazole moieties on ursolic acid were designed and synthesized. All compounds have been screened for their anti-inflammatory activity by using an ear edema model. The potent anti-inflammatory compound was subjected to in vitro cyclooxygenase COX-1/COX-2 inhibition assays. In general, the derivatives were found to be potent anti-inflammatory activity. Especially, the compound 11b exhibited the strongest activity of all of the compounds prepared, with 82.81% inhibition after intraperitoneal administration, which was better than celecoxib as a positive control. Molecular docking results unclose the rationale for the interaction of the compound 11b with COX-2 enzyme. Further studies revealed that compound 11b exhibited effective COX-2 inhibitory activity, with half-maximal inhibitor concentration (IC50) value of 1.16 µM and selectivity index (SI = 64.66) value close to that of celecoxib (IC50 = 0.93 µM, SI = 65.47). Taken together, these results could suggest a promising chemotype for development of new COX-2-targeting anti-inflammatory agent.


Assuntos
Inibidores de Ciclo-Oxigenase 2 , Triazóis , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Celecoxib/farmacologia , Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase 2/farmacologia , Relação Dose-Resposta a Droga , Desenho de Fármacos , Simulação de Acoplamento Molecular , Estrutura Molecular , Relação Estrutura-Atividade , Triazóis/farmacologia , Triterpenos , Ácido Ursólico
4.
Chinese Journal of School Health ; (12): 851-854, 2022.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-934819

RESUMO

Objective@#To analyze the influence of reproductive health education in middle school on self efficacy and intention of condom use among college freshmen, so as to provide evidence for fertility protection related intervention and policy making.@*Methods@#A questionnaire survey was conducted among college freshmen in Beijing by hierarchical cluster sampling method. A total of 3 001 students were surveyed. The difference was compared by using χ 2 test and ANOVA. Multivariate linear and Logistic regression model was used to analyze the influencing factors associated with condom use self efficacy and condom use intention.@* Results@#The overall rate that reproductive health education received before college among freshmen in Beijing was 65.11%. The college freshmen from urban areas reported more adequate reproductive health education (71.11%) than those from non urban areas before college (59.36%)( P <0.05). The total scores of UNGASS (4.22±0.90 vs 4.05±0.98), condom use self efficacy (24.64±5.34 vs 23.09±4.93) and the intention of condom use (82.44% vs 70.88%) of college freshmen received reproductive health education in middle school were higher than those of college students without pre college reproductive health education( P <0.01). Multiple linear regression analysis showed that the score of condom use self efficacy of college students received pre college reproductive health education was higher than those without pre college reproductive health education( β =1.21, 95% CI =0.79-1.63, P <0.01). Multivariate Logistic regression analysis showed that reproductive health, the intention of condom use of college freshmen who received pre college reproductive health education was higher than that of college freshmen without reproductive health education( OR =1.63, 95% CI =1.33-2.01, P <0.01).@*Conclusion@#Reproductive health education in middle school can improve college freshmen s self efficacy and intention of condom use, contribute to the implementation of safe sex, and is of great significance to the protection of college students fertility.

5.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-940371

RESUMO

Cardiovascular diseases, with high incidence and high mortality, belong to the category of "chest impediment and heart pain" in traditional Chinese medicine (TCM). Chinese medicines have unique effect on the prevention and treatment of cardiovascular diseases with little side effects. Huoxin pills, one of the National Essential Drugs, is formulated based on the basic pathogenesis of weak pulse at Yang and wiry pulse at Yin and the pathological basis of myocardial ischemia and hypoxia and used for treating angina pectoris of coronary heart disease (Qi deficiency and blood stasis syndrome). This medicine is derived from the classic famous prescription and is composed of ten precious Chinese medicinal herbs. It can replenish Qi, activate blood, and warm collaterals to diffuse impediment by enhancing myocardial contractility and cardiac output to improve micro-circulation and increase coronary blood flow, regulating immune functions, alleviating inflammation, detoxifying, and tranquilizing mind. Clinically, it is suitable for patients with angina pectoris caused by the lack of heart Yang, chest tightness, shortness of breath, palpitation, fear of cold for limbs and so on, especially for the elderly with Yang deficiency or the patients with a history of myocardial infarction. On the basis of the available research reports, this paper explains the formula meaning of Huoxin pills from the perspective of the basic pathogenesis of coronary heart disease and predicts its action targets, location and links. Furthermore, we expound the mechanism of action of Huoxin pills based on basic research and clinical evidence-based research, aiming to provide data support and evidence for the clinical application of this medicine.

6.
Artigo em Inglês | WPRIM (Pacífico Ocidental) | ID: wpr-928598

RESUMO

OBJECTIVES@#To study the molecular epidemiological characteristics of the virus in children with acute viral diarrhea in Changdu of Tibet, China.@*METHODS@#Fecal specimens were collected from 96 children with acute diarrhea who visited the People's Hospital of Changdu, Tibet, from November 2018 to November 2020 and were tested for adenovirus, norovirus, astrovirus, sapovirus, and rotavirus. Gene sequencing was performed for the genotypes of these viruses.@*RESULTS@#The overall positive rate of the five viruses was 39% (37/96), among which astrovirus had the highest positive rate of 17%, followed by norovirus (9%), rotavirus (8%), adenovirus (7%), and sapovirus (5%). There was no significant difference in the positive rate of the five viruses among different age groups (P>0.05). Only the positive rate of astrovirus was significantly different among the four seasons (P<0.05). For adenovirus, 6 children had F41 type and 1 had C2 type; for norovirus, 6 had GⅠ.3 type, 1 had GⅠ.7 type, 1 had GⅡ.3 type, and 2 had GⅡ.4 Sydney_2012 type; HAstrV-1 type was observed in all children with astrovirus infection; for sapovirus, 1 child each had sporadic GⅠ.2, GⅠ.6, and GⅡ.1 sapovirus and 2 children had unknown type; 6 children had rotavirus G9[P8].@*CONCLUSIONS@#Astrovirus and norovirus are important pathogens in children with acute diarrhea in Changdu, Tibet. The positive rate of adenovirus, norovirus, astrovirus, sapovirus, and rotavirus is not associated with age, and only the positive rate of astrovirus has obvious seasonality. F41 type is the dominant genotype of adenovirus; GⅠ.3 is the dominant genotype of norovirus; HAstrV-1 is the dominant genotype of astrovirus; sporadic GⅠ.2, GⅠ.6, and GⅡ.1 are the dominant genotypes of sapovirus; G9[P8] is the dominant genotype of rotavirus.


Assuntos
Criança , Humanos , China , Diarreia/epidemiologia , Fezes , Gastroenterite , Tibet/epidemiologia , Vírus/genética
7.
Mol Divers ; 25(2): 861-876, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-32172491

RESUMO

In the present investigation, a series of dihydrotriazine derivatives-bearing 5-aryloxypyrazole moieties were synthesized and their structures were confirmed by different spectral tools. The biological evaluation in vitro revealed that some of the target compounds exerted good antibacterial and antifungal activity in comparison with the reference drugs. Among these novel hybrids, compound 10d showed the most potent activity with minimum inhibitory concentration values (MIC) of 0.5 µg/mL against S. aureus 4220, MRSA 3506 and E. coli 1924 strain. The cytotoxic activity of the compounds 6d, 6m, 10d and 10g was assessed in MCF-7 and HeLa cells. Growth kinetics study showed significant inhibition of bacterial growth when treated with different conc. of 10d. In vitro enzyme study implied that compound 10d exerted its antibacterial activity through DHFR inhibition. Moreover, significant inhibition of biofilm formation was observed in bacterial cells treated with MIC conc. of 10d as visualized by SEM micrographs. Twenty-nine target compounds were designed, synthesized and evaluated in terms of their antibacterial and antifungal activities.


Assuntos
Antibacterianos , Triazinas , Antibacterianos/síntese química , Antibacterianos/química , Antibacterianos/farmacologia , Bactérias/efeitos dos fármacos , Bactérias/crescimento & desenvolvimento , Biofilmes/efeitos dos fármacos , Biofilmes/crescimento & desenvolvimento , Sobrevivência Celular/efeitos dos fármacos , Células HeLa , Humanos , Células MCF-7 , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Relação Estrutura-Atividade , Tetra-Hidrofolato Desidrogenase/química , Triazinas/síntese química , Triazinas/química , Triazinas/farmacologia
8.
International Eye Science ; (12): 1808-1811, 2021.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-886729

RESUMO

@#AIM:To evaluate the clinical effect of 25G pars plana vitrectomy(PPV)combined with intraocular lens(IOL)ciliary sulcus suture fixation and replacement of IOL capsular bag complex.<p>METHODS: A retrospective analysis of 21 patients(21 eyes)in our hospital who applied 25G PPV combined with IOL ciliary sulcus suture and fixation replacement in our hospital from January 2015 to January 2020 to treat the IOL capsular complex completely detached from the clinical data.<p>RESULTS: All the cases were successfully removed the dislocated IOL complex during the operation. There was no iatrogenic retinal damage. During the operation, 4 cases(4 eyes)were found to have the retina hole, 2 cases(2 eyes)were found to be retinal lattice degeneration area, which were treated with laser photocoagulation of the retina. Follow-up for 6-18mo, best corrected visual acuity(BCVA)(LogMAR)increased from 0.40±0.30 before operation to 0.33±0.25 after operation(<i>P</i>=0.040). The BCVA at the last follow-up of all cases reached the BCVA before surgery. The absolute value of the difference between the postoperative spherical equivalent power and the preoperative IOL refractive power prediction value is less than or equal to 0.75D. At the last follow-up, the position of the intraocular lenses in all cases was good, and there were no complications such as retinal detachment. <p>CONCLUSION: The technique of 25G PPV and the exchange of IOL ciliary sulcus fixation with intraocular IOL capsule complex is a safe and effective procedure for dislocation of IOL-capsular bag complex entirely into the vitreous cavity.

9.
International Eye Science ; (12): 1597-1600, 2021.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-886443

RESUMO

@#AIM: To explore the effect and safety of pars plana vitrectomy(PPV)assisted by intravitreal injection of conbercept in the treatment of proliferative diabetic retinopathy(PDR)combined with vitreous hemorrhage(VH).<p>METHODS: In the prospective randomized controlled study, patients with PDR and VH who were admitted to ophthalmology department of the hospital from February 2017 to September 2019 were enrolled as the research objects. They were randomly divided into observation group(39 cases, 39 eyes)and control group(38 cases, 38 eyes). Both groups underwent standard 27G PPV. The observation group underwent intravitreal injection of conbercept within 6-7d before surgery. The perioperative indexes were collected. The best corrected visual acuity(BCVA), intraocular pressure and central macular thickness(CMT)were followed up. The occurrence of surgical related complications was statistically analyzed.<p>RESULTS: Operation time(74.18±15.26 <i>vs </i>96.17±14.27min), number of bleeding eyes(8% <i>vs </i>37%), ratio of silicone oil filling(18% <i>vs </i>53%)and incidence of iatrogenic retinal breaks(15% <i>vs </i>47%)were lower in observation than control group(<i>P</i><0.05). BCVA at 1mo after surgery(0.33±0.10 <i>vs </i>0.60±0.21), 3mo after surgery(0.29±0.08 <i>vs </i>0.59±0.30)and 6mo after surgery(0.28±0.10 <i>vs </i>0.66±0.25)were significantly better in observation than control group(<i>P</i><0.05). CMT at 3mo after surgery(252.15±56.96 <i>vs </i>278.41±57.48μm)and 6mo after surgery(239.65±41.52 <i>vs </i>268.59±33.71μm)were significantly better in observation than control group(<i>P</i><0.05). During follow up, the incidence rates of VH in observation group and control group were 5% and 21%, respectively(<i>P</i><0.05). In control group, there were 3 eyes(8%)with tractional retinal detachment after surgery, while there was no tractional retinal detachment in observation group(<i>P</i>>0.05).<p>CONCLUSION: For patients with PDR and VH, intravitreal injection of conbercept before PPV can shorten operation time, reduce intraoperative blood loss and alleviate macular edema to obtain better visual acuity, with better curative effect and safety.

10.
Drug Des Devel Ther ; 14: 2959-2975, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32801637

RESUMO

BACKGROUND AND PURPOSE: The traditional Chinese medicine, diosgenin (Dio), has attracted increasing attention because it possesses various therapeutic effects, including anti-tumor, anti-infective and anti-allergic properties. However, the commercial application of Dio is limited by its extremely low aqueous solubility and inferior bioavailability in vivo. Soluplus, a novel excipient, has great solubilization and capacity of crystallization inhibition. The purpose of this study was to prepare Soluplus-mediated Dio amorphous solid dispersions (ASDs) to improve its solubility, bioavailability and stability. METHODS: The crystallization inhibition studies were firstly carried out to select excipients using a solvent shift method. According to solubility and dissolution results, the preparation methods and the ratios of drug to excipient were further optimized. The interaction between Dio and Soluplus was characterized by differential scanning calorimetry (DSC), fourier transform infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), powder X-ray diffraction (PXRD) and molecular docking. The pharmacokinetic study was conducted to explore the potential of Dio ASDs for oral administration. Furthermore, the long-term stability of Dio ASDs was also investigated. RESULTS: Soluplus was preliminarily selected from various excipients because of its potential to improve solubility and stability. The optimized ASDs significantly improved the aqueous solubility of Dio due to its amorphization and the molecular interactions between Dio and Soluplus, as evidenced by dissolution test in vitro, DSC, FT-IR spectroscopy, SEM, PXRD and molecular docking technique. Furthermore, pharmacokinetic studies in rats revealed that the bioavailability of Dio from ASDs was improved about 5 times. In addition, Dio ASDs were stable when stored at 40°C and 75% humidity for 6 months. CONCLUSION: These results indicated that Dio ASDs, with its high solubility, high bioavailability and high stability, would open a promising way in pharmaceutical applications.


Assuntos
Diosgenina/farmacocinética , Desenvolvimento de Medicamentos , Medicamentos de Ervas Chinesas/farmacocinética , Excipientes/farmacocinética , Polietilenoglicóis/farmacocinética , Polivinil/farmacocinética , Administração Oral , Animais , Disponibilidade Biológica , Cromatografia Líquida de Alta Pressão , Cristalografia por Raios X , Diosgenina/administração & dosagem , Composição de Medicamentos , Estabilidade de Medicamentos , Medicamentos de Ervas Chinesas/administração & dosagem , Excipientes/administração & dosagem , Masculino , Medicina Tradicional Chinesa , Conformação Molecular , Simulação de Acoplamento Molecular , Polietilenoglicóis/administração & dosagem , Polivinil/administração & dosagem , Ratos , Ratos Sprague-Dawley , Solubilidade , Espectrometria de Massas em Tandem
11.
Bioorg Med Chem Lett ; 30(13): 127237, 2020 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-32386981

RESUMO

Twenty benzothiazole derivatives bearing a 1,3,4-oxadiazole moiety were synthesized and evaluated for their anti-oxidant and anti-inflammatory activities. Among these compounds, 8h and 8l were appeared to have high radical scavenging efficacies as 0.05 ± 0.02 and 0.07 ± 0.03 mmol/L of IC50 values in ABTS+ bioassay, respectively. In anti-inflammatory tests, compound 8h displayed good activity with 57.35% inhibition after intraperitoneal administration, which was more potent than the reference drug (indomethacin). Molecular modeling studies were performed to investigate the binding mode of the representative compound 8h into COX-2 enzyme. In vitro enzyme study implied that compound 8h exerted its anti-inflammatory activity through COX-2 inhibition.


Assuntos
Anti-Inflamatórios/uso terapêutico , Benzotiazóis/uso terapêutico , Sequestradores de Radicais Livres/uso terapêutico , Inflamação/tratamento farmacológico , Oxidiazóis/uso terapêutico , Animais , Anti-Inflamatórios/síntese química , Anti-Inflamatórios/metabolismo , Benzotiazóis/síntese química , Benzotiazóis/metabolismo , Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase 2/síntese química , Inibidores de Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase 2/uso terapêutico , Sequestradores de Radicais Livres/síntese química , Sequestradores de Radicais Livres/metabolismo , Humanos , Camundongos , Simulação de Acoplamento Molecular , Estrutura Molecular , Oxidiazóis/síntese química , Oxidiazóis/metabolismo , Relação Estrutura-Atividade
12.
Mol Divers ; 24(4): 1165-1176, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31792660

RESUMO

The present work describes the in vitro antibacterial evaluation of some new pyrimidine derivatives. Twenty-two target compounds were designed, synthesized and preliminarily explored for their antimicrobial activities. The antimicrobial assay revealed that some target compounds exhibited significantly inhibitory efficiencies toward bacteria and fungal including drug-resistant pathogens. Compound 7c presented the most potent inhibitory activities against Gram-positive bacteria (e.g., Staphylococcus aureus 4220), Gram-negative bacteria (e.g., Escherichia coli 1924) and the fungus Candida albicans 7535, with an MIC of 2.4 µmol/L. Compound 7c was also the most potent, with MICs of 2.4 or 4.8 µmol/L against four multidrug-resistant, Gram-positive bacterial strains. The toxicity evaluation of the compounds 7c, 10a, 19d and 26b was assessed in human normal liver cells (L02 cells). Molecular docking simulation and analysis suggested that compound 7c has a good interaction with the active cavities of dihydrofolate reductase (DHFR). In vitro enzyme study implied that compound 7c also displayed DHFR inhibition.


Assuntos
Antibacterianos/química , Antibacterianos/síntese química , Pirimidinas/química , Antibacterianos/farmacologia , Linhagem Celular , Fungos/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana/métodos , Simulação de Acoplamento Molecular/métodos , Relação Estrutura-Atividade
13.
Artigo em Inglês | WPRIM (Pacífico Ocidental) | ID: wpr-827209

RESUMO

To ensure the safety of medications, it is vital to accurately authenticate species of the Apocynaceae family, which is rich in poisonous medicinal plants. We identified Apocynaceae species by using nuclear internal transcribed spacer 2 (ITS2) and psbA-trnH based on experimental data. The identification ability of ITS2 and psbA-trnH was assessed using specific genetic divergence, BLAST1, and neighbor-joining trees. For DNA barcoding, ITS2 and psbA-trnH regions of 122 plant samples of 31 species from 19 genera in the Apocynaceae family were amplified. The PCR amplification for ITS2 and psbA-trnH sequences was 100%. The sequencing success rates for ITS2 and psbA-trnH sequences were 81% and 61%, respectively. Additional data involved 53 sequences of the ITS2 region and 38 sequences of the psbA-trnH region were downloaded from GenBank. Moreover, the analysis showed that the inter-specific divergence of Apocynaceae species was greater than its intra-specific variations. The results indicated that, using the BLAST1 method, ITS2 showed a high identification efficiency of 97% and 100% of the samples at the species and genus levels, respectively, via BLAST1, and psbA-trnH successfully identified 95% and 100% of the samples at the species and genus levels, respectively. The barcode combination of ITS2/psbA-trnH successfully identified 98% and 100% of samples at the species and genus levels, respectively. Subsequently, the neighbor joining tree method also showed that barcode ITS2 and psbA-trnH could distinguish among the species within the Apocynaceae family. ITS2 is a core barcode and psbA-trnH is a supplementary barcode for identifying species in the Apocynaceae family. These results will help to improve DNA barcoding reference databases for herbal drugs and other herbal raw materials.

14.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-878673

RESUMO

Objective To explore the clinical characteristics and risk factors of systemic lupus erythematosus(SLE)complicated with cytomegalovirus infection(CMV). Methods The medical records of patients diagnosed with SLE at discharge in the Department of Immunology at Peking Union Medical College Hospital between July 1,2017 and April 1,2019 were retrospectively reviewed,and the clinical and laboratory data related to CMV infection were analyzed. Results Of the 231 patients with SLE,115(49.8%)had CMV infection.Among them,78(67.8%)were asymptomatic CMV infection and 37(32.2%)were diagnosed with CMV disease.Univariate analysis showed the number of organs involved(


Assuntos
Humanos , Ciclofosfamida/uso terapêutico , Infecções por Citomegalovirus/epidemiologia , Imunossupressores/uso terapêutico , Lúpus Eritematoso Sistêmico/tratamento farmacológico , Metilprednisolona/uso terapêutico , Prednisolona/uso terapêutico , Estudos Retrospectivos , Fatores de Risco , Albumina Sérica Humana/análise
15.
Chinese Medical Journal ; (24): 2437-2443, 2020.
Artigo em Inglês | WPRIM (Pacífico Ocidental) | ID: wpr-877835

RESUMO

BACKGROUND@#Epithelial to mesenchymal transition (EMT) is strongly linked with tumor invasion and metastasis, which performs a vital role in carcinogenesis and cancer progression. Emerging evidence suggests that microRNAs (miRNAs) expression are closely associated to EMT by regulating targeted genes. MiR542 has been found to be involved in the EMT program and bound up with various cancers. However, the functions of miR542 and its underlying mechanism in glioblastoma multiforme (GBM) remain largely unknown. In the current study, we investigated the effect of astrocyte elevated gene-1 (AEG-1) on U251 cells aggressiveness, proliferation, apoptosis, and cell cycle.@*METHODS@#The screening of targeted miRNAs was performed, as well as the functional roles and mechanisms of miR542 were explored.@*RESULTS@#MiR542 was selected as the target because of the most significantly differential expression and this high level of expression negatively correlated with cell migration and proliferation, which suggested that miR542 could be a novel tumor suppressor. Moreover, we confirmed that AEG-1 was a direct targeted gene of miR542 by luciferase activity assay, reverse transcription-polymerase chain reaction, and immunoblotting analysis. Furthermore, miR542 suppressed the expression of AEG-1, which upgraded the level of E-cadherin and degraded Vimentin expression contributing to retraining EMT.@*CONCLUSION@#The in vitro findings demonstrated that miR542 inhibited the migration and proliferation of U251 cells and suppressed EMT through targeting AEG-1, indicating that miR542 may be a potential anti-cancer target for GBM.


Assuntos
Humanos , Astrócitos , Linhagem Celular Tumoral , Movimento Celular/genética , Proliferação de Células/genética , Transição Epitelial-Mesenquimal/genética , Regulação Neoplásica da Expressão Gênica , Glioblastoma/genética , MicroRNAs/genética , Invasividade Neoplásica/genética
16.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-873235

RESUMO

Objective:To establish a molecular identification method for Bupleurum chinense seeds based on ribosomal DNA internal transcribed spacer (ITS) sequence, ensuring the species authenticity of the cultivated seeds of B. chinense. Method:A total of 59 seeds samples of B. chinense and its main cultivated species, marketed B. chinense were collected. The effect of different sampling amounts and different water bath conditions on DNA extraction quality of the seeds was investigated, a DNA extraction method for seeds of Bupleurum was established. Their ITS sequences were obtained by polymerase chain reaction (PCR) and bidirectional sequencing. In addition, 34 ITS sequences of main cultivated Bupleurum species, such as B. chinense, B. scorzonerifolium, B. falcatum and B. smithii, were downloaded from GenBank to enrich identification database of B. chinense seeds. The neighbor-joining (NJ) dendrogram were constructed by MEGA-X 10.0.5 software to investigate the the species identification ability of ITS sequences for B. chinense seeds. And DNA barcoding identification of marketed B. chinense seeds was conducted based on BLAST method and NJ dendrogram method. Result:In total, 59 ITS sequences were obtained. ITS sequences of B. chinense could be divided into six haplotypes, including seven variable sites. The NJ dendrogram indicated that all the haplotypes of B. chinense could form independent branches, which could be distinguished from other cultivated species of Bupleurum in the collected samples, and possessed the ability to identify species of B. chinense seeds. Based on ITS sequence barcoding identification, 3 of the 19 marketed B. chinense seeds were B. falcatum with a counterfeit rate of 15.8%. Conclusion:DNA barcoding technology based on ITS sequence can accurately and reliably identify B. chinense seeds and its adulterants, providing reference for the standardization construction of Chinese medicinal materials seeds.

17.
Am J Cardiol ; 123(1): 1-6, 2019 01 01.
Artigo em Inglês | MEDLINE | ID: mdl-30539743

RESUMO

Patients with acute coronary syndrome (ACS) face high postevent mortality. This study aims to evaluate the impact of living without spouse on 1-year mortality of ACS patients. This retrospective study enrolled a total of 600 consecutive patients (≥75 years of age) with ACS hospitalized in our hospital between January 2013 and December 2016. Patients' clinical characteristics, laboratory values, hospital course, demographic characteristics, and angiographic data were collected. Patients were divided into 2 groups according to living with (n = 396) or without (n = 204) spouse. Patients living without spouse were older (79 [77,82] vs 77 [76,80], p <0.001), more frequently female (54.9% vs 31.8%, p <0.001), less smokers (23.5% vs 38.9%, p <0.001), lower left ventricular ejection fraction value (52.1±10.7% vs 54.4±9.8%, p = 0.021) compared with patients living with spouse. In addition, compared to patients living with spouse, patients living without spouse were less likely to get percutaneous coronary intervention (41.2% vs 54.0%, p = 0.003) during hospitalization and had higher 1-year mortality post-ACS (22.1% vs 13.4%, p = 0.006). Multivariate logistic regression analysis showed that living without spouse remained an independent risk factor for 1-year mortality after ACS in patients ≥75 years (odds ratio 2.350, 95% confidence interval 1.245 to 4.434, p = 0.008), after adjusted with age, gender, heart rate, systolic blood pressure, left ventricular ejection fraction value at baseline, hemoglobin, white blood cell, alanine aminotransferase, albumin, creatinine, brain natriuretic peptide, type of ACS, severe heart failure at admission, percutaneous coronary intervention treatment, ß blocker, diuretics application during hospital. In conclusion, living without spouse is an independent risk factor for 1-year all-cause mortality in ACS patients ≥75 years.


Assuntos
Síndrome Coronariana Aguda/mortalidade , Síndrome Coronariana Aguda/psicologia , Cônjuges , Atividades Cotidianas/psicologia , Idoso , Idoso de 80 Anos ou mais , Feminino , Hospitalização/tendências , Humanos , Masculino , Estudos Retrospectivos , Taxa de Sobrevida
18.
Nat Prod Res ; 33(20): 3021-3024, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30580580

RESUMO

A new flavanone glycoside, (2S)-dihydrooroxylin A 7-O-[ß-D-apiosyl(1→2)]-ß-D-glucoside (1), and four known compounds (2-5) were isolated from Tournefortia sibirica L. The chemical structures of these compounds were determined by 1 D and 2 D NMR and HR-ESI-MS spectra, and results were compared with data from the literature. These five compounds (1-5) were isolated from the family Boraginaceae for the first time. Anti-inflammatory effects of compounds (1-5) were evaluated in terms of inhibition of production of NO, TNF-α, and IL-6 in LPS-induced RAW 264.7 cells.


Assuntos
Anti-Inflamatórios/isolamento & purificação , Boraginaceae/química , Flavanonas/isolamento & purificação , Glicosídeos/isolamento & purificação , Animais , Anti-Inflamatórios/farmacologia , Flavonoides/química , Flavonoides/isolamento & purificação , Glicosídeos/química , Interleucina-6/antagonistas & inibidores , Interleucina-6/biossíntese , Camundongos , Estrutura Molecular , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico/biossíntese , Extratos Vegetais/química , Células RAW 264.7 , Análise Espectral , Fator de Necrose Tumoral alfa/antagonistas & inibidores , Fator de Necrose Tumoral alfa/biossíntese
19.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-1008313

RESUMO

Lanosterol synthase( LS) is a key enzyme involving in the mevalonate pathway( MVA pathway) to produce lanosterol,which is a precursor of ganoderma triterpenoid. And the transcriptional regulation of LS gene directly affects the content of triterpenes in Ganoderma lucidum. In order to study the transcriptional regulation mechanism of LS gene,yeast one-hybrid technique was used to screen the transcription regulators which interact withthe promoter of LS. The bait vector was constructed by LS promoter,then the vector was transformed yeast cells to construct bait yeast strain. One-hybrid c DNA library was constructed via SMART technology. Then the c DNA and p GADT7-Rec vector were co-transformed into the bait yeast strain to screen the upstream regulatory factors of the promoter region of LS by homologous recombination. Total of 23 positive clones were screened. After sequencing,blast was performed against the whole-genome sequence of G. lucidum. As a result,8 regulatory factors were screened out including the transcription initiation TFIIB,the alpha/beta hydrolase super family,ALDH-SF superfamily,60 S ribosomal protein L21,ATP synthase β-subunit,microtubule associated protein Cript,prote asome subunit β-1,and transaldolase. Until now,the regulation effect of these 8 regulatory factors in G.lucidum has not been reported. This study provides candidate proteins for in-depth study on the expression regulation of LS.


Assuntos
Biblioteca Gênica , Transferases Intramoleculares/metabolismo , Reishi/genética , Saccharomyces cerevisiae , Fatores de Transcrição/metabolismo
20.
Artigo em Inglês | WPRIM (Pacífico Ocidental) | ID: wpr-1010414

RESUMO

The denitrifier method is widely used as a novel pretreatment method for the determination of nitrogen and oxygen isotope ratios as it can provide quantitative and high-sensitivity measurements. Nevertheless, the method is limited by relatively low measurement accuracy for δ18O. In this study, we analyzed the factors influencing the accuracy of δ18O determination, and then systematically investigated the effects of dissolved oxygen concentrations and nitrate sample sizes on estimates of the δ15N and δ18O of nitrate reference materials. The δ18O contraction ratio was used to represent the relationship between the measured difference and true difference between two reference materials. We obtained the following main results: (1) a gas-liquid ratio of 3:10 (v/v) in ordinary triangular flasks and a shaking speed of 120 r/min produced an optimal range (1.9 to 2.6 mg/L) in the concentration of dissolved oxygen for accurately determining δ18O, and (2) the δ18O contraction ratio decreased as nitrate sample size decreased within a certain range (1.0 to 0.1 μmol). Our results suggested that δ18O contraction is influenced mainly by dissolved oxygen concentrations in pure culture, and provided a model for improving the accuracy of oxygen isotope analysis.


Assuntos
Desnitrificação , Nitratos/análise , Isótopos de Oxigênio/análise
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