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1.
Sci Rep ; 14(1): 14085, 2024 06 18.
Artigo em Inglês | MEDLINE | ID: mdl-38890467

RESUMO

This study evaluated Aloe vera extract as a green inhibitor to prevent corrosion in seawater environments. A. vera extract was produced by maceration with methanol-water at room temperature. Electrochemical techniques were used to evaluate the corrosion inhibitor effectiveness of the A. vera extract. The morphology of the corrosion products was analyzed by FE-SEM equipped with EDS and AFM. FT-IR and LCMS characterized the functional and structural groups in this extract. The electrochemical measurements show that A. vera extract could effectively reduce the corrosion of API 5L steel in seawater environments. Inhibition efficiency (IE) increases with increasing concentration. Optimal corrosion inhibition efficiency of around 83.75% (PDP) and 88.60% (EIS) was obtained by adding 300 mg L-1 of extract at 310 K. Furthermore, the higher the concentration of A. vera extract, the greater the activation energy (Ea), with the highest activation energy being 48.24 kJ mol-1 for the concentration of 300 mg L-1. Conversely, increasing the temperature and exposure duration reduces the corrosion inhibition efficiency (IE) values; the best exposure period was 30 min with 88.34% IE by a concentration of 300 mg L-1 at 300 K. This corrosion inhibition is achieved by the adsorption process of A. vera bioactive on metal surfaces with a mixed inhibitor through a physisorption-chemisorption mechanism. This finding was confirmed by the smoother surface morphology of the steel treated with A. vera extract than without. This unveiling investigation found that A. vera extract has the potential to be an environmentally friendly corrosion inhibitor in the seawater environment.


Assuntos
Aloe , Extratos Vegetais , Água do Mar , Aço , Corrosão , Água do Mar/química , Aço/química , Aloe/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier
2.
Physiother Res Int ; 29(2): e2091, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38642068

RESUMO

INTRODUCTION: Stroke has emerged as the leading cause of disability globally. The provision of long-term rehabilitation to stroke survivors poses a health care burden to many countries. Robotic devices have created a major turning point in stroke rehabilitation program. Currently, the anthropometric evidence to support the benefit of robotic rehabilitation (RR) among stroke patients is scarce. Therefore, the aim of this study was to evaluate the impact of RR on the mid-thigh circumferences of the paretic limbs in stroke patients. METHODS: Twenty stroke patients from conventional rehabilitation (CR) (n = 10) and RR (n = 10) groups were recruited through a purposive sampling method. Patients in the CR group received a two-hour session of a five-day-a-week home-based CR program for 4 weeks. Patients in the RR group received a five-day-a-week of an hour combined physiotherapy and occupational therapy session and a one-hour robotic therapy session using the HAL® Cyberdyne lower-limb, for 4 weeks. The mid-thigh circumferences of both limbs were measured on day 1 (baseline), week 2 and week 4 of rehabilitation program. RESULTS: The results revealed no statistically significant difference in the mid-thigh circumferences between the paretic (F1.05,9.44 = 1.96, p = 0.20), and the normal (F1.05,9.44 = 1.96, p = 0.20) sides in the CR group (n = 10). For the comparison between the paretic and normal sides in the RR group (n = 10), the paretic mid-thigh circumferences revealed significant time effect results (F2,18 = 11.91, p = 0.001), which were due to changes between baseline and week 2, and baseline and week 4 measurements. Interestingly, the normal mid-thigh circumferences also revealed a significant time effect (F2,18 = 6.56, p = 0.007), which is due to changes between baseline and week 4. One-way analysis of variance was employed to compare the mean average between groups due to the difference in the baseline measurements of the mid-thigh circumferences between the paretic side of the CR and the RR groups. With this adjustment, the average means mid-thigh circumferences after 4 weeks of therapy were shown to be significantly different between the CR and RR groups (F1,18 = 12.49, p = 0.02). CONCLUSION: Significant increments in the mid-thigh circumferences following RR were seen in the paretic limbs of stroke patients. Hence, this study may provide some insights into further potential research related to the benefits of RR in stroke patients.


Assuntos
Procedimentos Cirúrgicos Robóticos , Robótica , Reabilitação do Acidente Vascular Cerebral , Acidente Vascular Cerebral , Humanos , Coxa da Perna , Acidente Vascular Cerebral/complicações , Acidente Vascular Cerebral/terapia , Reabilitação do Acidente Vascular Cerebral/métodos , Robótica/métodos
3.
Biol Pharm Bull ; 46(8): 1079-1087, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37532559

RESUMO

Chronic hepatitis C virus (HCV) infection can lead to liver cirrhosis and hepatocellular carcinoma. Although current medications using direct-acting antivirals (DAAs) are highly effective and well-tolerated for treating patients with chronic HCV, high prices and the existence of DAA-resistant variants hamper treatment. There is thus a need for easily accessible antivirals with different mechanisms of action. During the screening of Indonesian medicinal plants for anti-HCV activity, we found that a crude extract of Dryobalanops aromatica leaves possessed strong antiviral activity against HCV. Bioassay-guided purification identified an oligostilbene, vaticanol B, as an active compound responsible for the anti-HCV activity. Vaticanol B inhibited HCV infection in a dose-dependent manner with 50% effective and cytotoxic concentrations of 3.6 and 559.5 µg/mL, respectively (Selectivity Index: 155.4). A time-of-addition study revealed that the infectivity of HCV virions was largely lost upon vaticanol B pretreatment. Also, the addition of vaticanol B following viral entry slightly but significantly suppressed HCV replication and HCV protein expression in HCV-infected and a subgenomic HCV replicon cells. Thus, the results clearly demonstrated that vaticanol B acted mainly on the viral entry step, while acting weakly on the post-entry step as well. Furthermore, co-treatment of the HCV NS5A inhibitor daclatasvir with vaticanol B increased the anti-HCV effect. Collectively, the present study has identified a plant-derived oligostilbene, vaticanol B, as a novel anti-HCV compound.


Assuntos
Dipterocarpaceae , Hepatite C Crônica , Hepatite C , Humanos , Antivirais/farmacologia , Antivirais/uso terapêutico , Hepacivirus , Hepatite C Crônica/tratamento farmacológico , Hepatite C/tratamento farmacológico , Replicação Viral
4.
Microbiol Immunol ; 67(6): 281-292, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-36929353

RESUMO

Hepatitis B virus (HBV) is a leading cause of chronic hepatitis, liver cirrhosis, and hepatocellular carcinoma. Current therapeutic drugs for chronic HBV infection use IFN and nucleos(t)ide analogs; however, their efficacy is limited. Thus, there is an urgent need to develop new antivirals for HBV therapy. In this study, we identified a plant-derived polyphenolic bioflavonoid, amentoflavone, as a new anti-HBV compound. Amentoflavone treatment dose-dependently inhibited HBV infection in HBV-susceptible cells with HepG2-hNTCP-C4 and primary human hepatocyte PXB-cells. A mode-of-action study showed that amentoflavone inhibits the viral entry step, but not the viral internalization and early replication processes. Attachment of HBV particles as well as HBV preS1 peptide to HepG2-hNTCP-C4 cells was inhibited by amentoflavone. The transporter assay revealed that amentoflavone partly inhibits uptake of sodium taurocholate cotransporting polypeptide (NTCP)-mediated bile acid. Furthermore, effect of various amentoflavone analogs on HBs and HBe production from HBV-infected HepG2-hNTCP-C4 cells was examined. Robustaflavone exhibited comparable anti-HBV activity to that of amentoflavone and an amentoflavone-7,4', 4‴-trimethyl ether derivative (sciadopitysin) with moderate anti-HBV activity. Cupressuflavone or the monomeric flavonoid apigenin did not exhibit the antiviral activity. Amentoflavone and its structurally related biflavonoids may provide a potential drug scaffold in the design of a new anti-HBV drug inhibitor targeting NTCP.


Assuntos
Biflavonoides , Hepatite B , Humanos , Vírus da Hepatite B , Biflavonoides/farmacologia , Biflavonoides/metabolismo , Biflavonoides/uso terapêutico , Hepatite B/tratamento farmacológico , Hepatócitos , Antivirais/uso terapêutico , Internalização do Vírus
5.
South Med J ; 115(9): 693-697, 2022 09.
Artigo em Inglês | MEDLINE | ID: mdl-36055657

RESUMO

OBJECTIVES: Adenomatous polyps are common, occurring in up to 25% of the population older than 50 years of age in the United States. Conflicting data are present in the literature about the impact of specific adenoma locations and the prediction on the number and advanced histology of adenomas elsewhere. With this study we aimed to review the association between cecal adenoma and the risk of discovering more and advanced adenomas in the remainder of the colon. METHODS: We performed a retrospective study of 1880 patients who received outpatient colonoscopies between June 2012 and December 2014 at the Veterans Affairs Medical Center in Oklahoma City. The data collected included patient demographics, indications for colonoscopy, smoking history, alcohol use, family history of colon cancer, quality of bowel preparation, number of adenomas, location, size of adenomas, and the histology of adenomas and colon cancer. RESULTS: The mean age of the study population was 61.6 ± 9.4 year, with 95% of the population being men. Cecal adenomas were found in 243 (12.9%) of patients. Patients with cecal adenoma tended to be older (65 ± 7 vs 61 ± 10, P < 0.0001), more likely to be men (97% vs 94%, P = 0.06) and less likely to have a colonoscopy done for screening indication (11% vs. 13%., P = 0.03). After adjusting for age, sex, indication, and quality of bowel preparation, patients with cecal adenoma were found to have a sixfold increase in finding ≥10 other adenomas elsewhere (4.5% vs 0.8% P = 0.0009) and a threefold increase in finding advanced adenomas (17.7% vs 9.9% P = 0.002) in the remainder of the colon. Stratifying by location, the increased risk was more pronounced in the right side (24.7% vs 8.9% P ≤ 0.0001) compared with the left side. CONCLUSIONS: Cecal adenoma is associated with an increased risk of finding more and advanced adenomas in the remainder of the colon, especially on the right side; therefore, the discovery of a cecal adenoma should prompt a more thorough evaluation of the entire colon, particularly the right colon.


Assuntos
Adenoma , Neoplasias do Colo , Pólipos do Colo , Neoplasias Colorretais , Adenoma/diagnóstico , Neoplasias do Colo/diagnóstico , Pólipos do Colo/diagnóstico , Colonoscopia , Neoplasias Colorretais/diagnóstico , Feminino , Humanos , Masculino , Estudos Retrospectivos
6.
Iran J Microbiol ; 12(2): 127-137, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32494347

RESUMO

BACKGROUND AND OBJECTIVES: Endophytic actinomycetes have been known as a promising source for new antibiotics discovery against susceptible and resistant forms of pathogenic microorganisms. This study was aimed at determining antibacterial compound from Streptomyces sp. strain B-92 isolated from a medicinal plant Neesia altissima. MATERIALS AND METHODS: Streptomyces sp. strain UICC B-92 was endophytic actinomycetes of N. altissima that obtained from Universitas Indonesia Culture Collection (UICC). Isolation and determination of bioactive compound were carried out using thin layer chromatography (TLC), nuclear magnetic resonance spectroscopy (NMR), and liquid chromatography mass spectrometry (LC-MS) analyses. An in vitro antibacterial assay of pure bioactive compound from the endophytic actinomycetes strain was performed against Bacillus cereus strain ATCC 10876, Escherichia coli strain ATCC 25922, Salmonella typhimurium strain ATCC 25241, Shigella flexneri strain ATCC 12022 and Staphylococcus aureus strain ATCC 25923. RESULTS: The bioactive compound was identified as 4-((3S,4R,5S)-3,4,5-trihydroxy-6-(hydroxymethyl) tetrahydro-2H-pyran-2-yloxy) phenazine-1-carboxylic acid. In vitro antimicrobial assay showed that bioactive compound of Streptomyces sp. strain UICC B-92 exhibited antagonistic activities against two Gram-positive bacteria, viz, B. cereus strain ATCC 10876 and S. aureus strain ATCC 25923. CONCLUSION: The findings of this research showed that, bioactive compound of Streptomyces sp. strain UICC B-92 is suggested a new compound based on glycoside structure and its position.

7.
Cureus ; 11(2): e3999, 2019 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-30989008

RESUMO

Kikuchi-Fujimoto disease (KFD), or necrotizing histiocytic lymphadenitis, is a rare cause of lymphadenopathy and fever. Although the clinical course is usually benign, KFD is often mistaken for malignancy or infection. Recognition of typical and atypical cases of KFD is necessary to avoid unnecessary interventions. Here we report an atypical presentation of KFD with diffuse lymphadenopathy and leukocytosis associated with high levels of circulating Epstein-Barr viral DNA.

8.
Kobe J Med Sci ; 65(2): E71-E79, 2019 Nov 12.
Artigo em Inglês | MEDLINE | ID: mdl-31956259

RESUMO

Chronic hepatitis B virus (HBV) infection can lead to liver cirrhosis and hepatocellular carcinoma. Current therapeutic drugs for chronic hepatitis B using pegylated interferons and nucleos(t)ide analogs have limited efficacy. Therefore, the development of novel and safe antivirals is required. Natural products including medicinal plants produce complex and structurally diverse compounds, some of which offer suitable targets for antiviral screening studies. In the present study, we screened various crude extracts from Indonesian plants for anti-HBV activity by determining their effects on the production of extracellular HBV DNA in Hep38.7-Tet cells and HBV entry onto a HBV-susceptible cell line, HepG2-NTCP, with the following results: (1) In Hep38.7-Tet cells, Cananga odorata exhibited the highest anti-HBV activity with a 50% inhibitory concentration (IC50) of 56.5 µg/ml and 50% cytotoxic concentration (CC50) of 540.2 µg/ml (Selectivity Index: 9.6). (2) The treatment of HepG2-NTCP cells with Cassia fistula, C. odorata, and Melastoma malabathricum at concentrations of 100 µg/ml lowered the levels of HBsAg production to 51.2%, 58.0%, and 40.1%, respectively, compared to untreated controls, and IC50 and CC50 values of C. odorata were 142.9 µg/ml and >400 µg/ml. In conclusion, the C. odorata extract could be a good candidate for the development of anti-HBV drugs.


Assuntos
Antivirais/análise , Cananga/química , Vírus da Hepatite B/efeitos dos fármacos , Hepatite B/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Células Hep G2 , Humanos , Indonésia , Testes de Sensibilidade Microbiana , Fitoterapia , Extratos Vegetais/farmacologia , Plantas Medicinais , Replicação Viral/efeitos dos fármacos
9.
Gastrointest Endosc ; 88(2): 378-387, 2018 08.
Artigo em Inglês | MEDLINE | ID: mdl-29679692

RESUMO

BACKGROUND AND AIMS: Previous studies have described variable effects of fellow involvement on the adenoma detection rate (ADR), but few have stratified this effect by level of training. We aimed to evaluate the "fellow effect" on multiple procedural metrics including a newly defined adenoma management efficiency index, which may have a role in documenting colonoscopy proficiency for trainees. We also describe the impact of level of training on moderate sedation use. METHODS: We performed a retrospective review of 2024 patients (mean age, 60.9 ± 10 years; 94% men) who underwent outpatient colonoscopy between June 2012 and December 2014 at our Veterans Affairs Medical Center. Colonoscopies were divided into 5 groups. The first 2 groups were first-year fellows in the first 6 months and last 6 months of the training year. Second- and third-year fellows and attending-only procedures accounted for 1 group each. We collected data on doses of sedatives used, frequency of adjunctive agent use, procedural times, and location, size, and histology of polyps. We defined the adenoma management efficiency index as average time required per adenoma resected during withdrawal. RESULTS: Of the colonoscopies performed, 1675 involved a fellow and 349 were performed by the attending alone. There was no difference in ADR between fellows according to level of training (P = .8) or between fellows compared with attending-only procedures (P = .67). Procedural times decreased consistently during training and declined further for attending-only procedures. This translated into improvement in the adenoma management efficiency index (fellow groups by ascending level of training: 23.5 minutes vs 18.3 minutes vs 13.7 minutes vs 13.4 minutes vs attending group 11.7 minutes; P < .001). There was no difference in the average doses of midazolam and fentanyl used among fellow groups (P = .16 and P = .1, respectively). Compared with attending-only procedures, fellow involvement was associated with higher doses of fentanyl and midazolam and more frequent use of diphenhydramine and glucagon (P < .0001, P = .0002, P < .0001, and P = .01, respectively). CONCLUSIONS: ADR was similar at different stages of fellowship training and comparable with the attending group. Efficiency of detecting and resecting polyps improved throughout training without reaching the attending level. Fellow involvement led to a greater use of moderate sedation, which may relate to a longer procedure duration and an evolving experience in endoscopic technique.


Assuntos
Adenoma/diagnóstico por imagem , Adenoma/cirurgia , Colonoscopia/normas , Neoplasias Colorretais/diagnóstico por imagem , Neoplasias Colorretais/cirurgia , Bolsas de Estudo , Gastroenterologia/educação , Adjuvantes Anestésicos/administração & dosagem , Idoso , Competência Clínica , Pólipos do Colo/diagnóstico por imagem , Pólipos do Colo/cirurgia , Difenidramina/administração & dosagem , Feminino , Fentanila/administração & dosagem , Fármacos Gastrointestinais/administração & dosagem , Glucagon/administração & dosagem , Humanos , Hipnóticos e Sedativos/administração & dosagem , Masculino , Corpo Clínico Hospitalar , Midazolam/administração & dosagem , Pessoa de Meia-Idade , Duração da Cirurgia , Estudos Retrospectivos
10.
Malays J Med Sci ; 24(4): 47-54, 2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-28951689

RESUMO

INTRODUCTION: Oral cancer is a life-threatening disease. Lack of public awareness is a potent barrier for the early detection of oral cancer, especially for high-risk populations. OBJECTIVE: This study aimed to determine the awareness and knowledge of the signs, symptoms and risk factors of oral cancer among a Siamese ethnic group in Tumpat, Kelantan. METHODS: A cross-sectional study was conducted, using a guided questionnaire on sociodemography, habits, awareness and knowledge of the signs, symptoms and risk factors of oral cancer. Individuals under 18 years old and who had been diagnosed with oral cancer were excluded from this study. RESULTS: A total of 195 respondents participated, 61.5% were female and the mean age was 46 (1.64). About 41% of the respondents had received secondary education and 35.4% were illiterate. Most respondents were self-employed (21.5%), followed by farmers (19.5%) and housewives (20%). The majority of them had a monthly income that fell below the poverty level of RM 830 (76.9%). Among the respondents, 22.6% had the habit of smoking, 25.6% consumed alcohol, 8.2% were betel quid chewers and 2.6% chewed tobacco. Out of 195 respondents, only 6.7% were aware of oral cancer. About 16.9% of the respondents correctly answered all of the questions regarding the signs and symptoms of oral cancer and only 4.1% knew the risk factors of oral cancer. CONCLUSION: The awareness and knowledge of oral cancer in this targeted population were unsatisfactory. Future effective health promotion programs and education should be emphasised.

11.
J Microbiol ; 55(4): 289-295, 2017 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-28124775

RESUMO

This study's aim was to determine the identity of antibacterial compounds produced by Pseudomonas aeruginosa strain UICC B-40 and describe the antibacterial compounds' mechanisms of action for damaging pathogenic bacteria cells. Isolation and identification of the compounds were carried out using thin layer chromatography (TLC), nuclear magnetic resonance (NMR) spectroscopy and liquid chromatography mass spectrometry (LC-MS) analyses. Antibacterial activity was assayed via minimum inhibitory concentration (MIC) and the antibacterial compound mechanism was observed morphologically through scanning electron microscopy (SEM). This study successfully identified the (2E,5E)-phenyltetradeca-2,5-dienoate antibacterial compound (molecular weight 300 g/mol), composed of a phenolic ester, fatty acid and long chain of aliphatic group structures. MIC values for this compound were determined at 62.5 µg/ml against Staphylococcus aureus strain ATCC 25923. The mechanism of the compound involved breaking down the bacterial cell walls through the lysis process. The (2E,5E)-phenyltetradeca-2,5-dienoate compound exhibited inhibitory activity on the growth of Gram-positive bacteria.


Assuntos
Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Produtos Biológicos/isolamento & purificação , Produtos Biológicos/farmacologia , Bactérias Gram-Positivas/efeitos dos fármacos , Malvaceae/microbiologia , Pseudomonas aeruginosa/química , Antibacterianos/química , Produtos Biológicos/química , Cromatografia Líquida , Cromatografia em Camada Fina , Endófitos/química , Bactérias Gram-Positivas/ultraestrutura , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Testes de Sensibilidade Microbiana , Microscopia Eletrônica de Varredura , Peso Molecular
12.
Jpn J Infect Dis ; 69(3): 213-20, 2016 May 20.
Artigo em Inglês | MEDLINE | ID: mdl-26255732

RESUMO

Infection with hepatitis C virus (HCV) results in hepatitis C, a disease characterized by chronic infection, cirrhosis, and hepatocellular carcinoma. Currently, the standard therapy is a combination of pegylated interferon-α plus ribavirin with NS3 protease inhibitors. Addition of NS3 protease inhibitors to the standard therapy improves response rates; however, use of NS3 protease inhibitors is also associated with significant adverse effects and an increase in the overall cost of treatment. Therefore, there is a need to develop safe and inexpensive drugs for the treatment of HCV infections. In this study, we examined the antiviral activity of a crude extract from Dimocarpus longan leaves against HCV (genotype 2a strain JFH1). The D. longan crude extract (DL-CE) exhibited anti-HCV activity with a 50% effective concentration (EC50) of 19.4 µg/ml without cytotoxicity. A time-of-addition study demonstrated that DL-CE has anti-HCV activity at both the entry and post-entry steps and markedly blocks the viral entry step through direct virucidal activity with marginal inhibition of virion assembly. Co-treatment of DL-CE with cyclosporine A, an immunosuppressant or telaprevir, an NS3 protease inhibitor, resulted in additive and synergistic antiviral effects, respectively. Our findings suggest that DL-CE may be useful as an add-on therapy candidate for treating HCV infections.


Assuntos
Antivirais/farmacologia , Hepacivirus/efeitos dos fármacos , Extratos Vegetais/farmacologia , Folhas de Planta/química , Sapindaceae/química , Linhagem Celular Tumoral , Ciclosporina/farmacologia , Sinergismo Farmacológico , Quimioterapia Combinada , Hepacivirus/fisiologia , Hepatócitos/efeitos dos fármacos , Hepatócitos/virologia , Humanos , Concentração Inibidora 50 , Oligopeptídeos/farmacologia , Extratos Vegetais/química , Inibidores de Proteases/farmacologia , Internalização do Vírus/efeitos dos fármacos
13.
Bioorg Med Chem ; 21(14): 4358-64, 2013 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-23735825

RESUMO

An evaluation of Indonesian plants to identify compounds with immune modulating activity revealed that the methanolic extract of an Alphonsea javanica Scheff specimen possessed selective anti-inflammatory activity in a nuclear factor-kappa B (NF-κB) luciferase and MTT assay using transfected macrophage immune (Raw264.7) cells. A high-throughput LC/MS-ELSD based library approach of the extract in combination with the NF-κB and MTT assays revealed the styryl lactone (+)-altholactone (2) was responsible for the activity. Compound 2, its acetylated derivate (+)-3-O-acetylaltholactone (3), and the major compound of this class, (+)-goniothalmin (1), were further evaluated to determine their anti-inflammatory potential in the NF-κB assay. Concentration-response studies of 1-3 indicated that only 2 possessed NF-κB based anti-inflammatory activity. Compound 2 reduced the LPS-induced NO production, phosphorylation of IκBα, and the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) using Western blot analysis. Further studies using qPCR indicated 2 reduced the expression of eight pro-inflammatory cytokines/enzymes (0.8-5.0µM) which included: COX-2, iNOS, IP-10, IL-1ß, MCP-1, GCS-F, IL-6 and IFN-ß. These results indicated that 2 displays broad spectrum immune modulating activity by functioning as an anti-inflammatory agent against LPS-induced NF-κB signaling. Conversely the selective cytotoxicity and in vivo anti-tumor and anti-inflammatory activity previously reported for 1 do not appear to arise from a mechanism that is linked to the NF-κB immune mediated pathway.


Assuntos
Anti-Inflamatórios/farmacologia , Furanos/antagonistas & inibidores , Inflamação/tratamento farmacológico , Pironas/antagonistas & inibidores , Animais , Western Blotting , Linhagem Celular , Citocinas/antagonistas & inibidores , Citocinas/genética , Humanos , Imunomodulação , Concentração Inibidora 50 , Camundongos , Modelos Moleculares , Estrutura Molecular , Reação em Cadeia da Polimerase , RNA Mensageiro/genética
14.
Bioinformation ; 8(19): 901-6, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-23144548

RESUMO

Eugenol is an essential oil mainly found in the buds and leaves of clove (Syzygium aromaticum (L.) Merrill and Perry), which has been reported to have activity on inhibition of cell proliferation and apoptosis induction in human MCF-7 breast cancer cells. This biological activity is correlated to its activity as an estrogen receptor antagonist. In this article, we present the construction and validation of structure-based virtual screening (SBVS) protocols to identify the potent estrogen receptor α (ER) antagonists. The selected protocol, which gave acceptable enrichment factors as a virtual screening protocol, subsequently used to virtually screen eugenol, its analogs and their dimers. Based on the virtual screening results, dimer eugenol of 4-[4-hydroxy-3-(prop-2-en-1- yl)phenyl]-2-(prop-2-en-1-yl)phenol is recommended to be developed further in order to discover novel and potent ER antagonists.

15.
Pharmaceuticals (Basel) ; 5(12): 1282-90, 2012 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-24281337

RESUMO

Some novel 3-phenyl-2-[(E)-2-phenylethenyl]-3,4-dihydroquinazolin-4-one derivatives possessing para-sulfonamides groups on the phenyl ring of the 2-phenylethenyl moiety have been synthesized and their COX-2 inhibitory activity evaluated. The stuctures of the synthesized compounds were confirmed  on the basis of  FT-IR, 1H-NMR, 13C-NMR and mass spectral data. The COX-2 inhibition screening assay revealed that 4-[(E)-2-{3-(4-methoxyphenyl)-4-oxo-3,4-dihydroquinazolin-2-yl}ethenyl]benzene-1-sulfonamide had a  maximum COX-2 inhibition (47.1%), at a concentration of 20 µM.

16.
Molecules ; 14(8): 2850-6, 2009 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-19701128

RESUMO

Onenewalkaloid; (+)-N-(2-hydroxypropyl)lindcarpine (1),together with four known aporphine alkaloids, (+)-boldine (2) (+)-norboldine (3), (+)-lindcarpine (4) and (+)-methyllindcarpine (5) were isolated from the stem bark of Actinodaphne pruinosa Nees (Lauraceae). (+)-N-(2-Hydroxypropyl)lindcarpine (1) exhibited cytotoxic activity against P-388 murine leukemia cells with an IC(50 )value of 3.9 microg/mL. Structural elucidation of all the compounds were performed by spectral methods such as 1D- and 2D- NMR, IR, UV, and HRESIMS.


Assuntos
Aporfinas/química , Citotoxinas/química , Lauraceae/química , Animais , Aporfinas/isolamento & purificação , Aporfinas/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Citotoxinas/isolamento & purificação , Citotoxinas/farmacologia , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Camundongos , Estrutura Molecular , Caules de Planta/química , Espectrofotometria Ultravioleta
17.
J Asian Nat Prod Res ; 11(11): 929-32, 2009 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-20183255

RESUMO

A new farnesylated flavonol derivative, macagigantin (1), together with two known flavonoids, glyasperin A (2) and apigenin (3), had been isolated from the acetone extract of the leaves of Macaranga gigantea. The structure of the new compound was elucidated as 6-farnesylkaempferol based on its spectroscopic data, including UV, IR, 1D and 2D NMR, and HR-EI-MS spectra. Compounds 1-3 were evaluated for their cytotoxic properties against P-388 cells, their IC(50) values being 11.3, 6.0, and 5.1 microM, respectively.


Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Euphorbiaceae/química , Flavonóis/isolamento & purificação , Animais , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Flavonóis/química , Flavonóis/farmacologia , Indonésia , Leucemia P388 , Camundongos , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Folhas de Planta/química , Relação Estrutura-Atividade
19.
Pak J Biol Sci ; 11(21): 2517-20, 2008 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-19205275

RESUMO

In the course of continuing research for finding bioactive compounds from Indonesian plants, the leaves of Artocarpus communis was extracted by ethanol. This extract partitioned with n-hexane-water (1:4) and then water extract was partitioned with dichloromethane. Dichloromethane extract was purified by column chromatography techniques on silica gel to afford yellow crystal (F-1). Based on LC-MS, 1H-NMR and 13C-NMR (1D and 2D) spectra and compared with previous spectral data, it was identified as prenylated flavonoid, 1-(2,4-dihydroxyphenyl)-3-[8-hydroxy-2-methyl-2-(4-methyl-3-pentenyl)-2H-1-benzopyran-5-yl] 1-propanone. This compound showed significant cytotoxicity against murine P-388 leukemia cells.


Assuntos
Artocarpus/metabolismo , Ensaios de Seleção de Medicamentos Antitumorais/métodos , Extratos Vegetais/farmacologia , Folhas de Planta/metabolismo , Animais , Linhagem Celular Tumoral , Cromatografia Líquida/métodos , Etanol/química , Flavonoides/química , Concentração Inibidora 50 , Espectroscopia de Ressonância Magnética , Espectrometria de Massas/métodos , Camundongos , Modelos Químicos , Conformação Molecular
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