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1.
J Ethnopharmacol ; 281: 114521, 2021 Dec 05.
Artigo em Inglês | MEDLINE | ID: mdl-34390794

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Zhuanggu Guanjie Pill (ZGGJP), a modern Chinese medicine formula, is composed of 12 herbs and has been used to treat osteoporosis in China for almost 30 years. However, no in vivo study of the influences of ZGGJP on the cytochrome P450 (CYP) activities have been reported. AIM OF THE STUDY: The aim of this study was to evaluate the effects of ZGGJP on the activities and the mRNA expression of CYP enzymes (CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A) and their corresponding nuclear receptor levels in rats. MATERIALS AND METHODS: After 7 days oral treatment of ZGGJP at low- and high-dose, cocktail solution was given to rats. Blood samples were collected at series of time points. The plasma concentrations of probe drugs and their corresponding metabolites were determined by UPLC-MS/MS. The influence of ZGGJP on the activities of seven CYPs were evaluated the metabolic ratios (Cmax and AUC0-t) for metabolites/probe drugs. In addition, the effects of ZGGJP on the mRNA expression of CYPs and their corresponding nuclear receptors in rat liver were evaluated by real-time PCR. RESULTS: ZGGJP showed significant inductive effects on CYP1A2 and CYP2B6 of both male and female rats. The influence of ZGGJP on CYP2C9 and CYP3A showed gender difference. ZGGJP could induce the activities of CYP2C9 and CYP3A in female rats, but have no influence on the activities in male rats. ZGGJP had no effects on CYP2D6, CYP2C19 and CYP2E1. The mRNA expression results of CYPs were in accordance with the pharmacokinetic results. The mRNA expression levels of constitutive androstane receptor (CAR) and vitamin D receptor (VDR) were increased significantly in female rats at high dosage, but no significant changes were observed in male rats. CONCLUSION: ZGGJP had inductive effects on CYP1A2 and CYP2B6 in both male and female rats. The results showed that ZGGJP could induce the activities of CYP2C9 and CYP3A in female rats, but had no effect in male rats. This may suggest that the influence of ZGGJP on CYP2C9 and CYP3A exhibit gender difference. The inductive effects of ZGGJP on the activities of CYPs, exhibiting gender difference, may be regulated by CAR and VDR. Therefore, co-administration of ZGGJP with other drugs, especially using CYP2C9 and CYP3A substrates in females, may need dose adjustment to avoid herb-drug interaction.

2.
Int J Biol Macromol ; 188: 137-146, 2021 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-34364941

RESUMO

COVID-19 is a disease caused by SARS-CoV-2, which has led to more than 4 million deaths worldwide. As a result, there is a worldwide effort to develop specific drugs for targeting COVID-19. Papain-like protease (PLpro) is an attractive drug target because it has multiple essential functions involved in processing viral proteins, including viral genome replication and removal of post-translational ubiquitination modifications. Here, we established two assays for screening PLpro inhibitors according to protease and anti-ISGylation activities, respectively. Application of the two screening techniques to the library of clinically approved drugs led to the discovery of tanshinone IIA sulfonate sodium and chloroxine with their IC50 values of lower than 10 µM. These two compounds were found to directly interact with PLpro and their molecular mechanisms of binding were illustrated by docking and molecular dynamics simulations. The results highlight the usefulness of the two developed screening techniques for locating PLpro inhibitors.


Assuntos
Antivirais/farmacologia , COVID-19/tratamento farmacológico , Proteases Semelhantes à Papaína de Coronavírus/antagonistas & inibidores , Inibidores de Protease de Coronavírus/farmacologia , Reposicionamento de Medicamentos , SARS-CoV-2/enzimologia , Antivirais/química , Sítios de Ligação , Cloroquinolinóis/química , Cloroquinolinóis/farmacologia , Proteases Semelhantes à Papaína de Coronavírus/genética , Proteases Semelhantes à Papaína de Coronavírus/isolamento & purificação , Inibidores de Protease de Coronavírus/química , Ensaios de Triagem em Larga Escala/métodos , Humanos , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Fenantrenos/química , Fenantrenos/farmacologia , SARS-CoV-2/efeitos dos fármacos
3.
Adv Ther (Weinh) ; : 2000224, 2021 Feb 22.
Artigo em Inglês | MEDLINE | ID: mdl-33786369

RESUMO

SARS-CoV-2 caused the emerging epidemic of coronavirus disease in 2019 (COVID-19). To date, there are more than 82.9 million confirmed cases worldwide, there is no clinically effective drug against SARS-CoV-2 infection. The conserved properties of the membrane fusion domain of the spike (S) protein across SARS-CoV-2 make it a promising target to develop pan-CoV therapeutics. Herein, two clinically approved drugs, Itraconazole (ITZ) and Estradiol benzoate (EB), are found to inhibit viral entry by targeting the six-helix (6-HB) fusion core of SARS-CoV-2 S protein. Further studies shed light on the mechanism that ITZ and EB can interact with the heptad repeat 1 (HR1) region of the spike protein, to present anti-SARS-CoV-2 infections in vitro, indicating they are novel potential therapeutic remedies for COVID-19 treatment. Furthermore, ITZ shows broad-spectrum activity targeting 6-HB in the S2 subunit of SARS-CoV and MERS-CoV S protein, inspiring that ITZ have the potential for development as a pan-coronavirus fusion inhibitor.

4.
Analyst ; 145(6): 2331-2338, 2020 Mar 21.
Artigo em Inglês | MEDLINE | ID: mdl-32030384

RESUMO

Ultrasensitive detection of monomeric ß-amyloid peptides is of fundamental significance for studying the pathological progression of Alzheimer's disease (AD). In this article, by facilely engineering a gold microelectrode interface, we developed a novel electrochemical biosensor for sensitive and selective monitoring of ß-amyloid peptide (Aß) monomers in cerebrospinal fluid (CSF). Through specific Cu2+-Aß-hemin coordination, Aß directed the assembly of Cu2+-PEI/AuNPs-hemin nanoprobes into network aggregates on a microelectrode interface, which promoted the enrichment of Aß monomers on the microelectrode. Furthermore, the AuNP aggregate promotes the deposition of silver nanoparticles, which were utilized for the electrochemical stripping analysis of the Aß monomer. The proposed method displayed ultra-sensitivity for Aß monomers with the detection limit down to 0.2 pM. Besides, high selectivity toward Aß monomers was observed. These remarkable analytical performances render the electrochemical biosensor useful for evaluating the dynamic change of Aß monomer level in CSF of live mice with AD, promoting the investigation of the role that Aß monomers play in brain events.


Assuntos
Doença de Alzheimer/líquido cefalorraquidiano , Peptídeos beta-Amiloides/líquido cefalorraquidiano , Técnicas Eletroquímicas/métodos , Ouro/química , Nanopartículas Metálicas/química , Animais , Cátions Bivalentes/química , Cobre/química , Hemina/química , Humanos , Masculino , Nanopartículas Metálicas/ultraestrutura , Camundongos , Camundongos Endogâmicos C57BL , Microeletrodos
5.
J Biomater Sci Polym Ed ; 31(6): 804-815, 2020 04.
Artigo em Inglês | MEDLINE | ID: mdl-32028835

RESUMO

The aim of this study was to develop a new chitosan derivative and investigate its effects on fresh tissue healing in rats. A chitosan-fructose Schiff based quaternary ammonium salt (CS = Fru-DEAE) was synthesized for the first time and characterized using FT-IR and 1HNMR, and the modification rate and the solution properties were studied. A rat wound model was established, and the experimental group was treated using 0.1 g of the chitosan derivative hydrogel. The wound healing rate, and the concentration of collagen III and proline in the wounds were assessed in the experimental group and compared with those of the control group at 7, 10, and 15 d. The CS = Fru-DEAE hydrogel demonstrated good performance and promoted the healing of infected wounds in rats. The hydrogel could accelerate the infiltration of inflammatory cells and increase the amount of type III collagen in the wound area, which likely contributed to its efficacy.


Assuntos
Materiais Biocompatíveis/química , Materiais Biocompatíveis/farmacologia , Quitosana/química , Frutose/química , Compostos de Amônio Quaternário/química , Animais , Materiais Biocompatíveis/síntese química , Colágeno Tipo III/metabolismo , Hidrogéis/química , Prolina/metabolismo , Ratos , Bases de Schiff/química , Cicatrização/efeitos dos fármacos
6.
Parasitol Res ; 119(1): 203-214, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31845020

RESUMO

Infection with helminth parasites or the administration of their antigens can prevent or attenuate autoimmune diseases. To date, the specific molecules that prime the amelioration are only limited. In this study, recombinant Schistosoma japonicum cystatin (rSjcystatin) and fructose-1,6-bisphosphate aldolase (rSjFBPA) were administered to female NOD mice via intraperitoneal (i.p.) injection to characterize the immunological response by the recombinant proteins. We have shown that the administration of rSjcystatin or rSjFBPA significantly reduced the diabetes incidence and ameliorated the severity of type 1 diabetes mellitus (T1DM). Disease attenuation was associated with suppressed interferon-gamma (IFN-γ) production in autoreactive T cells and with a switch to the production of Th2 cytokines. Following rSjcystatin or rSjFBPA injection, regulatory T cells (Tregs) were remarkably increased, which was accompanied by increased expression of interleukin-10 (IL-10) and transforming growth factor beta (TGF-ß). Our study suggests that helminth-derived proteins may be useful in strategies to limit pathology by promoting the Th2 response and upregulating Tregs during the inflammatory tissue-damage process in T1DM.


Assuntos
Cistatinas/administração & dosagem , Diabetes Mellitus Tipo 1/tratamento farmacológico , Frutose-Bifosfato Aldolase/administração & dosagem , Proteínas de Helminto/administração & dosagem , Fatores Imunológicos/administração & dosagem , Schistosoma japonicum/enzimologia , Animais , Cistatinas/genética , Cistatinas/metabolismo , Citocinas/metabolismo , Diabetes Mellitus Tipo 1/imunologia , Modelos Animais de Doenças , Feminino , Frutose-Bifosfato Aldolase/genética , Frutose-Bifosfato Aldolase/metabolismo , Proteínas de Helminto/genética , Proteínas de Helminto/metabolismo , Fatores Imunológicos/genética , Fatores Imunológicos/metabolismo , Camundongos , Camundongos Endogâmicos NOD , Proteínas Recombinantes/administração & dosagem , Proteínas Recombinantes/genética , Proteínas Recombinantes/metabolismo , Linfócitos T Reguladores/imunologia
8.
Anal Chem ; 91(4): 3015-3020, 2019 02 19.
Artigo em Inglês | MEDLINE | ID: mdl-30644729

RESUMO

Although separation of single-walled carbon nanotubes (SWCNTs) according to their helicity and handedness has been attracting tremendous interest recently, exploration of the left- and right-handed SWCNT enantiomers (defined as "M" and "P") to chiral sensing still remains in the early stage. Here we presented a new electrochemical sensor for chiral discrimination, which for the first time amplified the chiral selection on the electrode surface based on the left- or right-handed semiconducting SWCNT enantiomers with (6,5)-enriched chirality. The enantioselectivity was demonstrated by different peak current response to analyte enantiomers, observed in differential pulse voltammogram (DPV). Chiral distinguishing might be a result of the formation of an efficient chiral nanospace originating from the high purity of single enantiomer of (6,5) SWCNT. The obtained chiral electrodes were also applied to determine the enantiomeric excess (ee) of DOPA. There was a good linear relationship between DPV peak currents and % ee of l-DOPA. This study is the first example showing how the structure of chiral SWCNTs influences electrochemical chiral recognition.

9.
Artigo em Chinês | MEDLINE | ID: mdl-26510360

RESUMO

OBJECTIVE: To clone, express and purify Schistosoma japonicum fructose-1, 6-bisphosphate aldolase (SjFBPA) in E. coli and observe its expression in different developmental stages of S. japonicum. METHODS: FBPA gene was amplified from S. japonicum adult worm cDNA by using PCR. The amplified product was recombined into pET28a plasmid, and inducibly expressed with IPTG in E. coli BL21. SDS-PAGE and Western blotting were employed to analyze and identify the recombinant protein SjFBPA (rSjFBPA). Then, rSjFBPA was purified by chromatographic purification and its purity was analyzed by SDS- PAGE. The protein concentration of rSjFBPA purified was measured by the BCA method. Furthermore, SjFBPA mRNA was ana- lyzed in different developmental stages of S. japonicum by RT-PCR. RESULTS: SjFBPA was successfully amplified by using PCR and identified by restriction enzyme digestion and sequencing. The Western blotting analysis confirmed that the recombinant pro- tein could specifically reactive to the anti-His-tag monoclonal antibody. The concentration of the purified recombinant protein was about 4 mg/ml. The result of RT-PCR showed that SjFBPA mRNA was expressed in cercaria, schistosomulum, adult worm and egg of S. japonicum. CONCLUSION: SjFBPA is successfully recombined and expressed in a prokaryotic system, and SjFBPA mRNA is expressed in cercaria, schistosomulum, adult worm and egg of S. japonicum.


Assuntos
Frutose-Bifosfato Aldolase/genética , Proteínas Recombinantes/biossíntese , Schistosoma japonicum/enzimologia , Animais , Escherichia coli/genética , Frutose-Bifosfato Aldolase/biossíntese , Frutose-Bifosfato Aldolase/isolamento & purificação , Reação em Cadeia da Polimerase em Tempo Real , Proteínas Recombinantes/isolamento & purificação , Schistosoma japonicum/crescimento & desenvolvimento
10.
Zhonghua Yu Fang Yi Xue Za Zhi ; 47(2): 124-8, 2013 Feb.
Artigo em Chinês | MEDLINE | ID: mdl-23719102

RESUMO

OBJECTIVE: To investigate the combined effects between the two polymorphisms murine double minute 2 (MDM2) rs2279744 T→G and P53 rs1042522 G→C on the genetic susceptibility of breast cancer. METHODS: A total of 600 female patients with diagnosed breast cancer were consecutively recruited from the Yuhang district, Hangzhou city during March 2001 to May 2009. In the same period as the cases were collected, 600 healthy women living in Yuhang district, Hangzhou city were selected from a nutritional survey conducted. Peripheral blood lymphocytes were obtained from the study subjects and the demographic information were collected through questionnaires. PCR-restriction fragment length polymorphism (PCR-RFLP) was used for genotyping MDM2 rs2279744 T→G and P53 rs1042522 G→C. Logistic regression analysis was used to analyze the combined effects of the two polymorphisms on breast cancer risk. RESULTS: The frequency of MDM2 rs2279744 GG, TG and TT genotypes were 31.5% (189/600), 45.5% (273/600), 23.0% (138/600) in case group and 19.0% (114/600), 49.2% (295/600), 31.8% (191/600) in control group. The frequency of P53 rs1042522 GG, GC and CC genotypes were 23.1% (139/600), 50.2% (301/600), 26.7% (160/600) in case group and 30.5% (183/600), 51.3% (308/600), 18.2% (109/600) in control group. Logistic regression analysis showed that carriers with rs2279744 TG, GG genotypes had a significant increased risk for developing breast cancer compared with rs2279744 TT carriers (OR = 1.31, 95%CI: 0.97 - 1.73 for TG; OR = 2.24, 95%CI: 1.61 - 3.09 for GG). When comparing with rs1042522 GG carriers, carriers with rs1042522 GC, CC genotypes had a significant increased risk for developing breast cancer (OR = 1.34, 95%CI: 0.94 - 1.68 for GC; OR = 1.89, 95%CI: 1.35 - 2.68 for CC). The united analysis of this two polymorphisms showed that compared with individuals carrying rs2279744 TT and rs1042522 GG (the frequency were 4.8% (29/600) in case group and 11.5% (69/600) in control group), carries with rs2279744 TG/GG and rs1042522 GC/GG genotypes (the frequency were 95.2% (571/600) in case group and 88.5% (531/600) in control group) showed significant higher risk in the susceptibility to breast cancer (OR = 2.30, 95%CI: 1.39 - 3.82 for TG/GC + GG; OR = 2.14, 95%CI: 1.29 - 3.55 for TT + GC/CC; OR = 2.86, 95%CI: 1.80 - 4.53 for TG/GG + GC/CC). The combination of MDM2 rs2279744 T→G and P53 rs1042522 G→C contributed to a significantly higher risk of breast cancer than did any one of the variant (P = 0.046). The risk of susceptibility to breast cancer was much higher when this two polymorphisms both variant. CONCLUSIONS: The MDM2 rs2279744 T→G and P53 rs1042522 G→C may be risk factor for breast cancer. Significant combined effects between the two polymorphisms may contribute to the genetic susceptibility to breast cancer.


Assuntos
Neoplasias da Mama/genética , Predisposição Genética para Doença , Polimorfismo de Nucleotídeo Único , Proteínas Proto-Oncogênicas c-mdm2/genética , Proteína Supressora de Tumor p53/genética , Adulto , Estudos de Casos e Controles , Feminino , Genótipo , Humanos , Pessoa de Meia-Idade , Fatores de Risco
11.
Zhongguo Zhong Yao Za Zhi ; 37(11): 1642-5, 2012 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-22993999

RESUMO

OBJECTIVE: To seek effective drugs inhibiting herpes simplex virus (HSV-2) with the signal pathway required by virus replication as the target spot. METHOD: HSV-2-induced Vero cytopathic effect was observed, and MTT method was adopted to detect call activity, in order to assess the antiviral capacity of freeze dried powder of aqueous extracts of Saururus chinensis (AESC). Western blot was used to check the effect of AESC on signal pathway induced by HSV-2 virus in HeLa cells. RESULT: AESC obviously inhibits the pathway activation of CPE induced by HSV-2 infection and NF-kappaB required for virus replication. The inhibition ratio of AESC freeze dried powder at 0.10, 0.03, 0.01 and 0.003 g x L(-1) were (70.68 +/- 3.39)%, (61.74 +/- 2.13)%, (39.31 +/- 1.10)% and (18.54 +/- 3.44)%, respectively. The IC50 was determined at (0.023 +/- 0.004) g x L(-1). The inhibition concentration of the positive control acyclovir was 0.001 g x L(-1) (5.0 x 10(-6) mol x L(-1)). The best administration time was from 2 h before infection to 6 h after infection. Western blot also showed that AESC can notably inhibit HSV-2-induced NF-kappaB nuclear transfer. CONCLUSION: AESC can inhibit HSV-2 virus replication, which is related to the pathway activation of NF-kappaB required for virus replication.


Assuntos
Antivirais/farmacologia , Medicamentos de Ervas Chinesas/farmacologia , Herpesvirus Humano 2/efeitos dos fármacos , Saururaceae/química , Animais , Antivirais/toxicidade , Chlorocebus aethiops , Medicamentos de Ervas Chinesas/toxicidade , Células HeLa , Herpesvirus Humano 2/fisiologia , Humanos , NF-kappa B/metabolismo , Transdução de Sinais/efeitos dos fármacos , Células Vero , Replicação Viral/efeitos dos fármacos
12.
J Mol Cell Cardiol ; 53(2): 250-8, 2012 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-22561100

RESUMO

Syndecan-4 (synd4) is a heparan sulfate proteoglycan, involved in repair following tissue damage, through modulating neovascularization and inflammation. In acute myocardial infarction its myocardial expression is up-regulated in a time-dependent manner, and in synd4-deficient mice severe cardiac dysfunction and abnormal remodeling are observed following induction of myocardial infarction. Here we explored the therapeutic potential of sustained synd4 over-expression in the context of myocardial infarction. Adenovirus containing the synd4 gene (Ad-synd4), or corresponding control adenovirus (Ad-null), was administered intramyocardially in rats immediately after induction of myocardial infarction. Cardiac function was ascertained by echocardiography, hemodynamic assessment and brain natriuretic peptide level 28 days post-intervention. Hearts were excised for molecular and histological analyses at predetermined time points. We observed reduced mortality and improved cardiac function post-myocardial infarction in the Ad-synd4 as compared to the Ad-null group, with associated attenuation of cardiac remodeling, less myocyte loss and reduced fibrosis. Additionally, the Ad-synd4 group exhibited endothelial cell activation and increased angiogenesis and arteriogenesis in the myocardium. The Ad-synd4 group also showed evidence of reduced myocardial inflammation as compared with the Ad-null group, with reduced inflammatory cell (CD45+) and myofibroblast (α-SMA+) infiltration as well as suppressed collagen III deposition and iNOS expression. Our results suggest that sustained synd4 over-expression in the myocardium is of therapeutic benefit following experimental myocardial infarction, through inducing neovascularization, suppressing tissue inflammation and fibrosis, with resultant improvements in cardiac function and remodeling.


Assuntos
Infarto do Miocárdio/metabolismo , Infarto do Miocárdio/terapia , Sindecana-4/metabolismo , Animais , Células Cultivadas , Modelos Animais de Doenças , Humanos , Masculino , Infarto do Miocárdio/genética , Miócitos Cardíacos/citologia , Miócitos Cardíacos/metabolismo , Ratos , Ratos Sprague-Dawley , Sindecana-4/genética
13.
Antiviral Res ; 95(1): 30-6, 2012 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-22584350

RESUMO

Stilbenoids including resveratrol contain the basic structural unit of 1,2-diphenylethylene. Naturally occurring stilbenoids have broad structural features due to oligomerization and modifications and some have demonstrated potent biological activities. In an effort to identify bioactive stilbenoids, we screened a group of dimeric and oligomeric stilbenoids against HSV-1 and HSV-2 infection. Several trimeric and tetrameric derivatives showed anti-herpetic activity at single digit micromolar concentrations. HSV-1 and HSV-2 replication requires for NF-κB and MAPK activation. The compounds showed no inhibitory activity against NF-κB and Erk/MAPK activation, instead those compounds promoted rapid and transient release of reactive oxygen species (ROS). Addition of N-acetylcysteine (NAC), a scavenger of ROS, reversed the inhibitory effect of those compounds against HSV replication. In addition to the identification of resveratrol derivatives with potent anti-HSV activity, our results uncover a mechanism of polyphenol-mediated anti-HSV response, linking anti-herpetic activity of oligomeric stilbenoids to innate immunity.


Assuntos
Antivirais/farmacologia , Herpesvirus Humano 1/efeitos dos fármacos , Herpesvirus Humano 2/efeitos dos fármacos , Espécies Reativas de Oxigênio/metabolismo , Estilbenos/farmacologia , Acetilcisteína/metabolismo , Animais , Linhagem Celular , Sequestradores de Radicais Livres/metabolismo , Humanos
14.
Int J Biochem Cell Biol ; 44(7): 1133-8, 2012 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-22531715

RESUMO

The 2',5'-oligoadenylate synthetases (OASs) are IFN-induced antiviral proteins and are upregulated by infection of viral and some bacterial pathogens. There are at least 2 transcripts of approximately 1.8 and 2.0 kb in interferon-beta treated samples that are recognized by a probe for human OASL in Northern blot assay. By RT-PCR amplification we have isolated a previously undescribed splice variant of human OASL, named OASL d. The new variant was derived from deletion of exons 4 and 5 and encodes a protein of 384 aa residues that shares the N-terminal 219 aa residues with OASL a. Sequence analysis indicates that OASL d also contains the entire ubiquitin-like domain identified in human OASL a. OASL d was strongly induced by IFNγ in THP-1 monocytic cells and in A549 epithelial cells by interferon-beta as detected by immunoblotting assay. Ectopic expression of OASL a or OASL d, but not OASL b that shares the N-terminus with OASL a and d, partially inhibited EV71 and VSV infection. No effect against HSV-2 infection was observed. Therefore, OASL d is a novel isoform of human OASL that possesses antiviral activity against RNA viruses.


Assuntos
2',5'-Oligoadenilato Sintetase/genética , 2',5'-Oligoadenilato Sintetase/biossíntese , 2',5'-Oligoadenilato Sintetase/imunologia , 2',5'-Oligoadenilato Sintetase/metabolismo , Animais , Linhagem Celular Tumoral , Chlorocebus aethiops , Éxons , Deleção de Genes , Regulação da Expressão Gênica , Células HEK293 , Células HeLa , Células Hep G2 , Humanos , Interferon beta/farmacologia , Isoformas de Proteínas , Transfecção , Células Vero
15.
Antiviral Res ; 92(2): 341-5, 2011 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-21951655

RESUMO

Houttuynia cordata Thunb. is a medicinal plant widely used in folk medicine in several Asian countries. It has been reported that a water extract of H. cordata exhibits activity against herpes simplex virus (HSV) and the virus of severe acute respiratory syndrome (SARS), although the mechanisms are not fully understood yet. Previous studies have demonstrated absolute requirement of NF-κB activation for efficient replication of HSV-1 and HSV-2 and inhibition of NF-κB activation has been shown to suppress HSV infection. Here we show that a hot water extract of H. cordata (HCWE) inhibits HSV-2 infection through inhibition of NF-κB activation. The IC(50) was estimated at 50 µg/ml of lyophilized HCWE powder. At 150 and 450 µg/ml, HCWE blocked infectious HSV-2 production by more than 3 and 4 logs, respectively. The inhibitory activity was concomitant with an inhibition of NF-κB activation by HSV-2 infection. Although activation of NF-κB and Erk MAPK has been implicated for HSV replication and growth, HCWE showed no effect on HSV-2-induced Erk activation. Furthermore, we show that treatment with quercetin, quercitrin or isoquercitrin, major water extractable flavonoids from H. cordata, significantly blocked HSV-2 infection. These results together demonstrated that H. cordata blocks HSV-2 infection through inhibition of NF-κB activation.


Assuntos
Antivirais/farmacologia , Herpesvirus Humano 2/crescimento & desenvolvimento , Houttuynia/química , NF-kappa B/antagonistas & inibidores , Extratos Vegetais/farmacologia , Animais , Antivirais/isolamento & purificação , Chlorocebus aethiops , Células HeLa , Humanos , Concentração Inibidora 50 , Extratos Vegetais/isolamento & purificação , Células Vero , Carga Viral , Ensaio de Placa Viral , Replicação Viral/efeitos dos fármacos
16.
Chem Commun (Camb) ; 47(36): 10094-6, 2011 Sep 28.
Artigo em Inglês | MEDLINE | ID: mdl-21829848

RESUMO

Based on stepwise deposition of MOF films on a colloid crystal substrate, a strategy for fabricating photonic MOF films was developed. We found that the integration of a photonic structure endows MOF materials with unique optical properties, which can be used as a general and effective transduction scheme for a convenient study of the host-guest chemistry of MOFs.

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