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1.
ACS Omega ; 4(23): 20381-20393, 2019 Dec 03.
Artigo em Inglês | MEDLINE | ID: mdl-31815242

RESUMO

A series of novel trimethoxyphenyl-derived chalcone-benzimidazolium salts were synthesized. The biological properties of the compounds were screened in vitro against five different human tumor cell lines. The results suggest that the 5,6-dimethyl-benzimidazole or 2-methyl-benzimidazole ring as well as the 2-naphthylmethyl, 4-methylbenzyl, or 2-naphthylacyl substituent at position-3 of the benzimidazole ring was important to the cytotoxic activity. Notably, (E)-5,6-dimethyl-3-(naphthalen-2-ylmethyl)-1-(3-(4-(3-(3,4,5-trimethoxyphenyl)acryloyl)phenoxy)propyl)-1H-benzo[d]imidazol-3-ium bromide (7f) was more selective to HL-60, MCF-7, and SW-480 cell lines with IC50 values 8.0-, 11.1-, and 5.8-fold lower than DDP. Studies of the antitumor mechanism of action showed that compound 7f could induce cell-cycle G1 phase arrest and apoptosis in SMMC-7721 cells.

2.
ACS Omega ; 4(18): 17903-17909, 2019 Oct 29.
Artigo em Inglês | MEDLINE | ID: mdl-31681900

RESUMO

A novel fluorescent probe, amino-pillar[5]arene (APA), was prepared via a green, effective, and convenient synthetic method, which was characterized by nuclear magnetic resonance (NMR), infrared (IR), and high-resolution mass spectrometry. The fluorescence sensing behavior of the APA probe toward 22 metal ions in aqueous solutions were studied by fluorescence spectroscopy. The results showed that APA could be used as a selective fluorescent probe for the specificity detection of Au3+ ions. Moreover, the detection characteristics were investigated by fluorescence spectral titration, pH effect, fluorescence competitive experiments, Job's plot analysis, 1H NMR, and IR. The results indicated that detection of Au3+ ions by the APA probe could be achieved in the range of pH 1-13.5 and that other coexisting metal ions did not cause any marked interference. The titration analysis results indicated that the fluorescence intensity decreased as the concentration of Au3+ ions increased, with an excellent correlation (R 2 = 0.9942). The detection limit was as low as 7.59 × 10-8 mol·L-1, and the binding ratio of the APA probe with Au3+ ions was 2:1. Therefore, the APA probe has potential applications for detecting Au3+ ions in the environment and in living organisms.

3.
J Asian Nat Prod Res ; : 1-6, 2019 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-31552756

RESUMO

Two new ent-atisane diterpenes, sebiferumnins K and L (1 and 2), were isolated from the branches of Sapium sebiferum, together with four known compounds, ent-3-oxoatis-16α, 17-acetonide (3), ent-l6α, 17-dihydroxyatisan-3-one (4), ent-atisane-3ß, 16α, 17-triol (5), ent-3α-hydroxyatis-16α,17-acetonide (6). The structures of these two ent-atisane diterpenes were elucidated by extensive analyses of the spectroscopic data.

4.
Inflammation ; 42(6): 2267-2277, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31494796

RESUMO

This study aimed to explore the expression and correlation of microRNA-7 (miR-7) and trefoil factor 3 (TFF3) genes and proteins in inflammatory bowel disease (IBD) mouse models and to elucidate the effect of miR-7 inhibition in the intestinal mucosa in IBD models. A TNBS-induced IBD mouse model was established. Changes in intestinal inflammation were observed by HE staining, and the expression levels of miR-7 and TFF3 were detected by RT-PCR. After miRNA-antagomir injection, the degree of colonic tissue damage and the expression levels of miR-7 and TFF3 in intestinal tissues were compared. TNBS-induced IBD mice showed significant weight loss, significantly decreased disease activity index (DAI), and a significantly increased pathological damage score. miR-7 was highly expressed in the colon tissue of IBD mice, and TFF3 was downregulated. Inhibition of the expression of miR-7 improved the stool characteristics and fecal occult blood (OB) of IBD mice, significantly increased the expression of TFF3 protein, and decreased the pathological damage scores. In the IBD mouse model, miR-7 posttranscriptionally regulates TFF3. The inhibition of miR-7 expression improves some clinical manifestations of IBD mice, reduces the pathological damage of the intestinal mucosa, and shows a protective effect in IBD.

5.
Zhen Ci Yan Jiu ; 44(7): 516-9, 2019 Jul 25.
Artigo em Chinês | MEDLINE | ID: mdl-31368284

RESUMO

OBJECTIVE: To observe the therapeutic effect of body acupuncture combined with auricular acupuncture in the treatment of woman menopause insomnia induced by disharmony between the heart and kidney. METHODS: A total of 111 outpatients with menopausal insomnia were randomly divided into treatment group (n=55, body acupoints plus auricular points) and control group (n=56, body acupoints). For control group, Shenmen (HT7), Sanyinjiao (SP6), Anmian, Zhaohai (KI6), Shenmai (BL62), Sishencong (EX-HN1), Xinshu (BL15) and Shenshu (BL21) were needled with filiform needles, and HT7, SP6, Anmian, BL15 and BL21 were also stimulated with electroacupuncture (EA) for 30 min, once every other day, 3 times a week for 3 weeks. For the treatment group, auricular points as Kidney, Shenmen, Sympathetic and Endocrine around the ear canal and the ear cavity were punctured with filiform needles in combination with the same intervention methods mentioned above in the control group. The quality and efficiency of sleep were assessed by using Pittsburgh Sleep Quality Index (PSQI) scale before and after the treatment. The symptom scores of traditional Chinese medicine (TCM) and the therapeutic effect were determined according to the "Guide Principles for Clinical Research of New Drugs of TCM" (formulated by Chinese Ministry of Health, 1997). RESULTS: After the treatment, the scores of sleep quantity and effective rate of PSQI scale, and those of insomnia and dreaminess, dysphoria with feverish sensation in chest, palms and soles, paplpitation and irritability, fatigue and forgetfulness of TCM were reduced significantly in both groups compared with their own pre-treatment (P<0.05). Of the 56 and 55 cases in the control and treatment groups, 18 (32.1%) and 30 (54.5%) experienced a marked improvement in their symptoms, 28 (50.0%) and 22 (40.0%) were effective, and 10 (17.9%) and 3 (5.5%) failed, with the effective rate being 82.1% and 94.5%, respectively. The therapeutic effect of stimulation of the body acupoints plus auricular acupoints was significantly superior to that of stimulation of simple body acupoints in lowering scores of PSQI scale, insomnia and dreaminess, dysphoria with feverish sensation in chest, palms and soles, dizziness and tinninus, paplpitation and irritability, and tital fever and night sweating of TCM, as well as the effective rate (P<0.05). CONCLUSION: Both body acupuncture and body acupuncture combined with auricular acupuncture are effective in the treatment of woman menopause insomnia due to disharmony between the heart and kidney, and the two combined treatment was evidently better.


Assuntos
Acupuntura Auricular , Distúrbios do Início e da Manutenção do Sono , Pontos de Acupuntura , Feminino , Coração , Humanos , Rim , Menopausa , Distúrbios do Início e da Manutenção do Sono/terapia , Resultado do Tratamento
6.
Zhongguo Zhong Yao Za Zhi ; 44(24): 5429-5432, 2019 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-32237390

RESUMO

This research was carried out to study the secondary metabolites of endophytic fungus Aspergillosis fumigatus from Euphorbia royleana. The endophytic fungus A. fumigatus was fermented by solid fermentation,and purified by various chromatographic methods after extraction. The structures of the compounds were identified by1 H-NMR,13 C-NMR and HSQC,HMBC spectra and physicchemical properties. Three compounds were isolated and their structures were identified as 3-( 3,4-dihydroxybenzoyl)-5-( 3,4-dihydroxyphenyl)-6-methyl-5,6-dihydro-2 H-pyran-2-one( 1),hydroxysydonic acid( 2) and 11-hydroxysydonic acid( 3). Compound 1 is a new compound.


Assuntos
Aspergillus fumigatus/química , Euphorbia/microbiologia , Fenóis/isolamento & purificação , Endófitos/química , Fermentação
7.
Arthritis Res Ther ; 20(1): 130, 2018 06 19.
Artigo em Inglês | MEDLINE | ID: mdl-29921328

RESUMO

BACKGROUND: Previous studies have revealed that hepatitis B virus (HBV) infection may be related to rheumatoid arthritis (RA), but there are no studies on the presence of HBV antigens or nucleic acid in synovium from patients with RA with HBV infection. In the present study, we investigated the presence of HBV in the synovium and its clinical significance in RA. METHODS: Fifty-seven consecutive patients with active RA (Disease Activity Score 28-joint assessment based on C-reactive protein ≥ 2.6) and available synovial tissue who had completed 1 year of follow-up were recruited from a prospective cohort. The patients were divided into chronic HBV infection (CHB, n = 11) and non-CHB groups according to baseline HBV infection status. Clinical data were collected at baseline and at 1-, 3-, 6-, and 12-month follow-up. Radiographic changes of hand/wrist at baseline and month 12 were assessed with the Sharp/van der Heijde-modified Sharp score (mTSS). HBV in synovium was determined by immunohistochemical staining for hepatitis B virus surface antigen and hepatitis B virus core antigen (HBcAg) and by nested PCR for the HBV S gene. RESULTS: HBcAg was found in the synovium of patients with RA with CHB (7 of 11, 64%), which was confirmed by PCR for the HBV S gene. Compared with the non-CHB group, more CD68-positive macrophages, CD20-positive B cells, and CD15-positive neutrophils infiltrated the synovium in the CHB group (all p <  0.05). There were smaller improvements from baseline in most disease activity indicators mainly at month 12, and a significantly higher percentage of CHB patients experienced 1-year radiographic progression (ΔmTSS ≥ 0.5 unit/yr, 64% vs. 26%, p = 0.024). Multivariate logistic regression analysis showed that CHB status (OR 14.230, 95% CI 2.213-95.388; p = 0.006) and the density of synovial CD68-positive macrophages (OR 1.002, 95% CI 1.001-1.003; p = 0.003) were independently associated with 1-year radiographic progression. CONCLUSIONS: The presence of HBV in RA synovium may be involved in the pathogenesis of local lesions and exacerbate disease progression in RA.


Assuntos
Artrite Reumatoide/imunologia , Vírus da Hepatite B/imunologia , Hepatite B Crônica/imunologia , Membrana Sinovial/imunologia , Adulto , Artrite Reumatoide/patologia , Artrite Reumatoide/virologia , Linfócitos B/imunologia , Linfócitos B/metabolismo , Linfócitos B/patologia , Progressão da Doença , Feminino , Antígenos da Hepatite B/genética , Antígenos da Hepatite B/imunologia , Vírus da Hepatite B/genética , Vírus da Hepatite B/fisiologia , Hepatite B Crônica/virologia , Humanos , Macrófagos/imunologia , Macrófagos/metabolismo , Macrófagos/patologia , Masculino , Pessoa de Meia-Idade , Neutrófilos/imunologia , Neutrófilos/metabolismo , Neutrófilos/patologia , Índice de Gravidade de Doença , Membrana Sinovial/virologia
8.
Microb Pathog ; 117: 49-54, 2018 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-29438717

RESUMO

Ankylosing spondylitis (AS) is a chronic inflammatory arthritis of unknown origin. Its autoimmune origin has been suggested but never proven. Several reports have implicated K. pneumoniae as a triggering or perpetuating factor in AS; and the HLA-B27 antigen has also been found in association with AS. But there is no satisfactory explanation of why the presence of HLA-B27 predisposes to AS and the precise role played by K. pneumoniae in the disease has not yet been clarified. However, various studies have shown that the results of molecular, immunological, and microbiological studies could establish the link between K. pneumoniae infections and HLA-B27 in the aetiopathogenesis of AS. In this review, we have examined the evidence linking the interaction between K. pneumoniae infections and HLA-B27 in AS, and tried to exploit the possible mechanisms by which K. pneumoniae infections might induce pathologic processes to develop novel diagnostic criteria. Finally, we have also summarized some dietary regimens that could be helpful in the therapeutic management of AS patients.


Assuntos
Antígeno HLA-B27/imunologia , Infecções por Klebsiella/complicações , Infecções por Klebsiella/imunologia , Klebsiella pneumoniae/imunologia , Klebsiella pneumoniae/patogenicidade , Espondilite Anquilosante/etiologia , Espondilite Anquilosante/imunologia , Animais , Anticorpos Antibacterianos/imunologia , Autoanticorpos , Causalidade , Reações Cruzadas , Bases de Dados Factuais , Dieta , Dietoterapia , Humanos , Infecções por Klebsiella/microbiologia , Klebsiella pneumoniae/metabolismo , Mimetismo Molecular , Espondilite Anquilosante/dietoterapia , Espondilite Anquilosante/microbiologia , Amido/metabolismo
9.
Medicine (Baltimore) ; 97(2): e9084, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29480822

RESUMO

Pituitary stalk interruption syndrome (PSIS) is associated with simultaneous or subsequent pituitary hormone deficiencies (PHDs). Although the clinical features of multiple PHDs are well known, the status of the thyrotrophic axis in PSIS has not been thoroughly investigated.The clinical data of 89 PSIS patients and 34 Sheehan syndrome (SS) patients were retrospectively analyzed.The prevalence of central hypothyroidism in the PSIS patients and the SS patients was 79.8% and 70.6%, respectively. The thyroid-stimulating hormone (TSH) levels in the PSIS patients were significantly higher in comparison with the SS patients (5.13 ±â€Š3.40 vs 1.67 ±â€Š1.20 mU/L, P < .05). TSH elevation (8.79 ±â€Š3.17 mU/L) was noticed in 29 of 71 (40.85%) hypothyroid PSIS patients but not in the 24 hypothyroid SS patients. The TSH levels in the hypothyroid PSIS patients were significantly higher in comparison with the euthyroid PSIS patients (5.42 ±â€Š3.67 vs 3.66 ±â€Š1.50 mU/L). Thyroid hormone replacement significantly reduced the TSH levels in the PSIS patients with elevated TSH levels from 7.24 ±â€Š0.98 to 1.67 ±â€Š1.51 mU/L (P < .05). The logistic regression analysis suggested that TSH level was not significantly associated with pituitary stalk status and height of the anterior pituitary gland.PSIS is a newly recognized cause of central hypothyroidism. The proportion and amplitude of TSH elevations are higher in PSIS than in other causes of central hypothyroidism.


Assuntos
Doenças da Hipófise/metabolismo , Tireotropina/metabolismo , Adulto , Feminino , Terapia de Reposição Hormonal , Humanos , Modelos Logísticos , Masculino , Pessoa de Meia-Idade , Doenças da Hipófise/diagnóstico por imagem , Doenças da Hipófise/tratamento farmacológico , Doenças da Hipófise/epidemiologia , Hipófise/diagnóstico por imagem , Hipófise/efeitos dos fármacos , Hipófise/metabolismo , Prevalência , Estudos Retrospectivos , Tireotropina/administração & dosagem , Adulto Jovem
10.
Chem Biol Drug Des ; 92(1): 1206-1213, 2018 07.
Artigo em Inglês | MEDLINE | ID: mdl-29430875

RESUMO

A series of novel 3-substituted N-methylcarbazole-imidazolium salt derivatives has been prepared and evaluated in vitro against a panel of tumor cell lines (Hep G-2, Hela and PC12). The results suggest that the presence of substituted 2-methyl-imidazole or imidazole ring and substitution of the imidazolyl-3-position with a naphthylacyl or 4-bromophenacyl group were important for improving cytotoxic activity. Compounds 17, 18, 27, and 28 with 4-bromophenacyl and naphthylacyl groups displayed good activities with IC50 values of 0.09-7.20 µm against three tumor cell lines investigated and more active than DDP. Compound 35 exhibited cytotoxic activity selectively against Hela cell.


Assuntos
Antineoplásicos/síntese química , Carbazóis/química , Imidazóis/química , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Cristalografia por Raios X , Células HeLa , Humanos , Imidazóis/síntese química , Imidazóis/farmacologia , Conformação Molecular , Relação Estrutura-Atividade
11.
Neurol Sci ; 39(2): 225-234, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-29110148

RESUMO

Vitamin D receptor (VDR) polymorphisms have been inconsistently investigated in multiple sclerosis (MS). However, published studies demonstrated differences concerning design and effect size. A meta-analysis is necessary to determine the magnitude of the association between VDR polymorphisms and MS risk. The aim of the current study was to quantify the magnitude of the association between BsmI, FokI, ApaI, and TaqI VDR polymorphisms and MS risk. Following the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) guidelines, we conducted a systematic search and meta-analysis of the VDR gene polymorphisms and the risk of MS. The pooled odds ratios (OR) and 95% confidence interval (CI) were calculated by using Stata Version 11.0 with dominant and recessive models and allele analyses. A total of 4013 cases and 4218 controls in 24 case-control studies were included in the meta-analyses. The results did not indicate an association between any of the VDR polymorphisms and the risk of MS among overall populations, Asians, and Caucasians. However, our subgroup analysis suggests that the A allele was associated with MS risk in Asian populations (P = 0.005, OR = 1.267, 95% CI 1.074-1.496). Interestingly, the sensitivity analysis excluding studies with controls not in HWE showed insignificant association between the A allele and MS risk (P = 0.211), which was different from those in the non-sensitivity analysis. Our preliminary results indicate the VDR gene ApaI, BsmI, FokI, and TaqI polymorphisms may not be associated with elevated MS risk among overall populations. But ApaI polymorphism may confer different susceptibility to MS among different populations, and more well-designed studies with a large sample size are still needed to validate our results.


Assuntos
Predisposição Genética para Doença , Esclerose Múltipla/genética , Polimorfismo Genético/genética , Receptores de Calcitriol/genética , Grupo com Ancestrais do Continente Asiático/genética , Estudos de Casos e Controles , Humanos
12.
Endocr J ; 65(3): 269-279, 2018 Mar 28.
Artigo em Inglês | MEDLINE | ID: mdl-29279458

RESUMO

Primary macronodular adrenal hyperplasia (PMAH), also known in the past as bilateral macronodular adrenalhyperplasia or adrenocorticotropin (ACTH)-independent macronodular adrenal hyperplasia, is a rare type of Cushing's syndrome (CS) and is associated with bilateralenlargement of the adrenal glands. It accounts for <1% of all endogenous cases of CS. In order toidentify the pathogenic mutations in the causative gene of (AIMAH pedigrees, Whole-genome sequencing of three patients in family I was used to retrieve candidate causative genes. Meanwhile, the causative gene was identified by Sanger sequencing from the two pedigrees. Sequencing of ARMC5 exons of three patients was carried out to identify somatic mutations. Moreover, haploid clone of one tumor DNA sample was conducted. ARMC5 was the causative gene of two pedigrees confirmed by whole-genome sequencing (WGA) and Sanger sequencing. The variant sites of the two families were c.C943T (p.R315W) and c.C1960T (p.R654X), respectively. Autosomal dominant inheritance of AIMAH was confirmed by genotypes of one family member. Several somatic mutations were discovered in tumor DNA samples. In addition, haploid clone of tumor DNA was confirmed by germline mutation and somaticmutation, which suggested the pathogenic mechanism of "two-hit-model." ARMC5 was the causative gene of AIMAH pedigrees. This AIMAH in this study presented autosomal dominant inheritance, fitting to Mendelian inheritance law. However, the pathogenic mode of this disease showed as compound heterozygote.


Assuntos
Glândulas Suprarrenais/diagnóstico por imagem , Síndrome de Cushing/genética , Proteínas Supressoras de Tumor/genética , Adulto , Idoso , Proteínas do Domínio Armadillo , Síndrome de Cushing/diagnóstico por imagem , Feminino , Predisposição Genética para Doença , Genótipo , Humanos , Masculino , Pessoa de Meia-Idade , Mutação , Linhagem , Tomografia Computadorizada por Raios X , Sequenciamento Completo do Genoma
13.
Mod Rheumatol ; 28(4): 681-689, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29043878

RESUMO

OBJECTIVES: The main objective of this study was to summarize the existing evidence and quantitatively evaluate whether serum/plasma levels of homocysteine (Hcy) were associated with sclerosis (SSc) diseases by performing a meta-analysis of previous studies. METHODS: PubMed, Elsevier ScienceDirect and Cochrane Library databases were used to obtain all relative published literatures. Stata version 11.0 (StataCorp, College Station, TX) was used for statistical analysis. The effect size of each study was calculated by the standardized mean difference (SMD) with 95% confidence interval (CI) or quartiles. RESULTS: A total of eight studies including 475 cases and 265 controls were finally included in this meta-analysis. We found significant between-study heterogeneity and conducted analyses using random-effects models. No significant association was found between the serum levels of Hcy and SSc (pooled SMD =1.382 µmol/L, 95%CI = -0.442 to 3.206, p = .137), but there are two outlier studies that deviate significantly from most other studies, which made it difficult to generalize these results. After excluding these two studies, six studies were included in the meta-analysis. The results showed that the serum levels of Hcy in SSc were significantly higher than that in healthy controls (pooled SMD = 1.182µmol/L, 95%CI = 0.230-2.134, p = .015). CONCLUSION: Serum/plasma levels of Hcy in SSc diseases were higher than that in healthy controls.


Assuntos
Homocisteína/sangue , Escleroderma Sistêmico/sangue , Biomarcadores/sangue , Humanos , Escleroderma Sistêmico/patologia
14.
Cell Immunol ; 318: 1-7, 2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-28651741

RESUMO

It has been established that smoking has a profound impact on susceptibility and severity in some rheumatic diseases (e.g., rheumatoid arthritis), a mild impact in others (e.g., systemic lupus erythematosus) through epidemiological studies. And smoking is known to affect many inflammatory and autoimmune diseases through various mechanisms, including immunomodulation and chemical exposure. Although similar studies investigating the role of cigarette exposure in susceptibility to SSc have been rarely reported and specific mechanisms have never been established, the relationship between smoking and some SSc-related symptoms have been demonstrated during the last decade. However, due to the diversity of study designs, control populations, patient populations and the methodology used to determine smoking history, these results are contradictory in some respects. This paper will review current evidence on the association between smoking and SSc and summarize potential mechanisms.


Assuntos
Poluentes Atmosféricos/efeitos adversos , Escleroderma Sistêmico/imunologia , Fumar/efeitos adversos , Animais , Autoimunidade , Medicina Baseada em Evidências , Humanos , Imunomodulação , Inflamação , Risco , Escleroderma Sistêmico/epidemiologia
15.
Sci Rep ; 7(1): 3788, 2017 06 19.
Artigo em Inglês | MEDLINE | ID: mdl-28630475

RESUMO

In crop plants, a high-density genetic linkage map is essential for both genetic and genomic researches. The complexity and the large size of wheat genome have hampered the acquisition of a high-resolution genetic map. In this study, we report a high-density genetic map based on an individual mapping population using the Affymetrix Wheat660K single-nucleotide polymorphism (SNP) array as a probe in hexaploid wheat. The resultant genetic map consisted of 119 566 loci spanning 4424.4 cM, and 119 001 of those loci were SNP markers. This genetic map showed good collinearity with the 90 K and 820 K consensus genetic maps and was also in accordance with the recently released wheat whole genome assembly. The high-density wheat genetic map will provide a major resource for future genetic and genomic research in wheat. Moreover, a comparative genomics analysis among gramineous plant genomes was conducted based on the high-density wheat genetic map, providing an overview of the structural relationships among theses gramineous plant genomes. A major stable quantitative trait locus (QTL) for kernel number per spike was characterized, providing a solid foundation for the future high-resolution mapping and map-based cloning of the targeted QTL.


Assuntos
Mapeamento Cromossômico , Loci Gênicos , Polimorfismo de Nucleotídeo Único , Sementes/genética , Triticum/genética
16.
Mater Sci Eng C Mater Biol Appl ; 76: 1136-1145, 2017 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-28482478

RESUMO

The inclusion complexation behavior, characterization, and inclusion mode of podophyllotoxin (POD) with hydroxypropyl-ß-cyclodextrin (HPßCD) were investigated in both solution and the solid state by means of XRD, DSC, SEM, 1H and 2D NMR and UV-vis spectroscopy. The results showed that the water solubility and thermal stability of POD were obviously increased in the inclusion complex with HPßCD. The cytotoxicity of POD/HPßCD inclusion complex against all the human tumor cell lines investigated still remains. This satisfactory water solubility and high thermal stability of the POD/HPßCD complex will be potentially useful for their application as herbal medicines or healthcare products.


Assuntos
2-Hidroxipropil-beta-Ciclodextrina/química , Podofilotoxina/química , Varredura Diferencial de Calorimetria , Linhagem Celular Tumoral , Humanos , Solubilidade
17.
Sci Rep ; 7(1): 509, 2017 03 30.
Artigo em Inglês | MEDLINE | ID: mdl-28360411

RESUMO

ß-elemene, a compound extracted from Curcuma wenyujin plant, exhibits anticancer activity in many cancer types. However, the detailed mechanism by which ß-elemene inhibits growth of nasopharyngeal carcinoma (NPC) cells remains unknown. We showed that ß-elemene reduced phosphorylation of signal transducer and activator of transcription 3 (Stat3), and protein expressions of DNA methyltransferase 1 (DNMT1) and enhancer of zeste homolog 2 (EZH2). Exogenously expressed Stat3 antagonized the effect of ß-elemene on DNMT1 and EZH2 expressions. Furthermore, overexpressions of DNMT1 and EZH2 reversed the effect of ß-elemene on phosphorylation of Stat3 and cell growth inhibition. Intriguingly, exogenously expressed DNMT1 overcame ß-elemene-inhibited EZH2 protein expression and promoter activity. On the contrary, silencing of EZH2 and DNMT1 genes feedback strengthened the effect of ß-elemene on phosphorylation of Stat3. Consistent with this, ß-elemene inhibited tumor growth, phosphorylation of Stat3, expressions of DNMT1 and EZH2 in a mouse xenograft model. Collectively, this study shows that ß-elemene inhibits NPC cell growth via inactivation of Stat3, and reduces DNMT1 and EZH2 expressions. The interplay of DNMT1 and EZH2, and the mutual regulations among Stat3, EZH2 and DNMT1 contribute to the overall responses of ß-elemene. This study uncovers a novel mechanism by which ß-elemene inhibits growth of NPC cells.


Assuntos
Carcinoma/metabolismo , Carcinoma/patologia , DNA (Citosina-5-)-Metiltransferase 1/metabolismo , Proteína Potenciadora do Homólogo 2 de Zeste/metabolismo , Neoplasias Nasofaríngeas/metabolismo , Neoplasias Nasofaríngeas/patologia , Fator de Transcrição STAT3/metabolismo , Sesquiterpenos/farmacologia , Animais , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Modelos Animais de Doenças , Retroalimentação Fisiológica , Feminino , Humanos , Camundongos Nus , Carcinoma Nasofaríngeo , Fosforilação/efeitos dos fármacos , Regiões Promotoras Genéticas/genética
18.
Sci Total Environ ; 581-582: 19-24, 2017 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-28073056

RESUMO

OBJECTIVE: To reveal the difference of meteorological effect on scarlet fever in Beijing and Hong Kong, China, during different periods among 2004-2014. METHODS: The data of monthly incidence of scarlet fever and meteorological variables from 2004 to 2014 in Beijing and Hong Kong were collected from Chinese science data center of public health, meteorological data website and Hong Kong observatory website. The whole study period was separated into two periods by the outbreak year 2011 (Jan 2004-Dec 2010 and Jan 2011-Dec 2014). A generalized additive Poisson model was conducted to estimate the effect of meteorological variables on monthly incidence of scarlet fever during two periods in Beijing and Hong Kong, China. RESULTS: Incidence of scarlet fever in two districts were compared and found the average incidence during period of 2004-2010 were significantly different (Z=203.973, P<0.001) while average incidence became generally equal during 2011-2014 (Z=2.125, P>0.05). There was also significant difference in meteorological variables between Beijing and Hong Kong during whole study period, except air pressure (Z=0.165, P=0.869). After fitting GAM model, it could be found monthly mean temperature showed a negative effect (RR=0.962, 95%CI: 0.933, 0.992) on scarlet fever in Hong Kong during the period of 2004-2010. By comparison, for data in Beijing during the period of 2011-2014, the RRs of monthly mean temperature range growing 1°C and monthly sunshine duration growing 1h was equal to 1.196(1.022, 1.399) and 1.006(1.001, 1.012), respectively. The changes of meteorological effect on scarlet fever over time were not significant both in Beijing and Hong Kong. CONCLUSION: This study suggests that meteorological variables were important factors for incidence of scarlet fever during different period in Beijing and Hong Kong. It also support that some meteorological effects were opposite in different period although these differences might not completely statistically significant.


Assuntos
Escarlatina/epidemiologia , Pressão do Ar , Pequim/epidemiologia , China/epidemiologia , Hong Kong/epidemiologia , Humanos , Incidência , Luz Solar , Temperatura , Tempo (Meteorologia)
19.
Org Biomol Chem ; 14(39): 9423-9430, 2016 Oct 04.
Artigo em Inglês | MEDLINE | ID: mdl-27714171

RESUMO

The synthesis of a series of novel N-substituted tetrahydro-ß-carboline-imidazolium salt derivatives is presented. The biological properties of the compounds were evaluated in vitro against a panel of human tumor cell lines. The results suggest that the benzimidazole ring and 1-(naphthalen-2-yl)ethan-1-one or 2-naphthylmethyl substituent at the imidazolyl-3-position were vital for modulating cytotoxic activity. Compound 41 was observed as a potent derivative with IC50 values of 3.24-8.78 µM and exhibited cytotoxic activity selectively against HL-60, A-549 and MCF-7 cell lines. Meanwhile, high inhibitory activities selectively against HL-60 and MCF-7 cell lines were observed for compound 51. Moreover, compound 51 was able to induce G1 phase cell cycle arrest and apoptosis in MCF-7 cells. The cytotoxicity of compound 51 against human normal lung epithelial cell line BEAS-2B was further evaluated.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Imidazóis/síntese química , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Benzimidazóis/química , Carbolinas/química , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais/métodos , Pontos de Checagem da Fase G1 do Ciclo Celular/efeitos dos fármacos , Células HL-60 , Humanos , Células MCF-7 , Relação Estrutura-Atividade
20.
Food Nutr Res ; 60: 31288, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27356910

RESUMO

BACKGROUND: Type I interferons (IFN-α/ß) have broad and potent immunoregulatory and antiproliferative activities. However, it is still known whether the dietary flavonoids exhibit their antiviral and anticancer properties by modulating the function of type I IFNs. OBJECTIVE: This study aimed at determining the role of apigenin, a dietary plant flavonoid abundant in common fruits and vegetables, on the type I IFN-mediated inhibition of cancer cell viability. DESIGN: Inhibitory effect of apigenin on human 26S proteasome, a known negative regulator of type I IFN signaling, was evaluated in vitro. Molecular docking was conducted to know the interaction between apigenin and subunits of 26S proteasome. Effects of apigenin on JAK/STAT pathway, 26S proteasome-mediated interferon receptor stability, and cancer cells viability were also investigated. RESULTS: Apigenin was identified to be a potent inhibitor of human 26S proteasome in a cell-based assay. Apigenin inhibited the chymotrypsin-like, caspase-like, and trypsin-like activities of the human 26S proteasome and increased the ubiquitination of endogenous proteins in cells. Results from computational modeling of the potential interactions of apigenin with the chymotrypsin site (ß5 subunit), caspase site (ß1 subunit), and trypsin site (ß2 subunit) of the proteasome were consistent with the observed proteasome inhibitory activity. Apigenin enhanced the phosphorylation of signal transducer and activator of transcription proteins (STAT1 and STAT2) and promoted the endogenous IFN-α-regulated gene expression. Apigenin inhibited the IFN-α-stimulated ubiquitination and degradation of type I interferon receptor 1 (IFNAR1). Apigenin also sensitized the inhibitory effect of IFN-α on viability of cervical carcinoma HeLa cells. CONCLUSION: These results suggest that apigenin potentiates the inhibitory effect of IFN-α on cancer cell viability by activating JAK/STAT signaling pathway through inhibition of 26S proteasome-mediated IFNAR1 degradation. This may provide a novel mechanism for increasing the efficacy of IFN-α/ß.

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