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1.
Artigo em Inglês | MEDLINE | ID: mdl-36078523

RESUMO

The COVID-19 pandemic has changed the fitness-related field. More people started working out at home, and the use of fitness mobile apps that can measure the amount of exercise through a scientific method has increased compared to before the COVID-19 pandemic. This phenomenon is likely to continue even after the COVID-19 pandemic, and therefore this study aimed to investigate the importance of and satisfaction with a fitness app's functions according to consumers while using the fitness mobile app. Through this study, we intended to provide data for creating an environment where users can use fitness mobile apps consistently. A total of 420 questionnaires were distributed through Google Survey for about 3 months, from 13 September to 20 November 2020, and a total of 399 complete questionnaires were analyzed in this study. Regarding the data processing methods, frequency analysis, exploratory factor analysis, reliability analysis, descriptive statistical analysis, and IPA were used. The results are as follows. First, the first quadrant of the IPA matrix indicated the high importance of and satisfaction with the fitness mobile app, and included five attributes: cost-effectiveness, easy-to-understand information, ease of use and application, privacy protection, and compatibility with other devices. Second, the second quadrant of the matrix indicated relatively low satisfaction in association to high importance and included five attributes: accurate exercise information provision, design efficiency, daily exercise amount setting, convenient icons and interface, and provision of images and videos in appropriate proportions. Third, the third quadrant of the matrix, indicating low importance and low satisfaction, included five attributes: not sharing personal information, overall design composition and color, customer service, reliable security level, and providing information on goal achievement after exercising. Fourth, in the quadrant of the matrix, indicating low importance and high satisfaction, five attributes were included: exercise notification function, continuous service provision, step count and heart rate information, individual exercise recommendation, and individual body type analysis information.


Assuntos
COVID-19 , Aplicativos Móveis , COVID-19/epidemiologia , Exercício Físico , Humanos , Pandemias , Reprodutibilidade dos Testes
2.
Asia Pac J Public Health ; 33(5): 508-515, 2021 07.
Artigo em Inglês | MEDLINE | ID: mdl-34165349

RESUMO

The aim of this study was to examine the most cost-effective strategy of screening and vaccinating measles- and varicella-susceptible health care workers (HCWs). A retrospective cost-effectiveness analysis was conducted at a tertiary hospital in Korea with 300 HCWs who were at high risk of infection. Self-reported histories of vaccinations, infectious diseases, and contact with such cases were collected. Serological tests for immunoglobulin G titers of measles and varicella were performed. Data were analyzed using analysis of variance, Kruskal-Wallis test, χ2 test, and Fisher exact test. Seropositivity rates were 96.3% for measles and 95.7% for varicella. Four different strategies (cases) for vaccination were investigated. Considering the progressive decline in antibody concentrations and the false-positive responses in self-reported histories, case 3, which involved administering 2-dose vaccinations to susceptible HCWs demonstrated by antibody screening tests for both measles and varicella, was the most cost-effective strategy. Health care facilities should establish mandatory immunization policies that reduce the risk of transmission of vaccine-preventable diseases.


Assuntos
Varicela , Pessoal de Saúde , Programas de Rastreamento , Sarampo , Vacinação , Varicela/prevenção & controle , Análise Custo-Benefício , Pessoal de Saúde/estatística & dados numéricos , Humanos , Programas de Rastreamento/estatística & dados numéricos , Sarampo/prevenção & controle , Estudos Retrospectivos , Vacinação/estatística & dados numéricos
3.
J Korean Med Sci ; 35(37): e332, 2020 Sep 21.
Artigo em Inglês | MEDLINE | ID: mdl-32959546

RESUMO

BACKGROUND: The purpose of this study was to determine the extent of air and surface contamination of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) in four health care facilities with hospitalized coronavirus disease 2019 (COVID-19) patients. METHODS: We investigated air and environmental contamination in the rooms of eight COVID-19 patients in four hospitals. Some patients were in negative-pressure rooms, and others were not. None had undergone aerosol-generating procedures. On days 0, 3, 5, and 7 of hospitalization, the surfaces in the rooms and anterooms were swabbed, and air samples were collected 2 m from the patient and from the anterooms. RESULTS: All 52 air samples were negative for SARS-CoV-2 RNA. Widespread surface contamination of SARS-CoV-2 RNA was observed. In total, 89 of 320 (27%) environmental surface samples were positive for SARS-CoV-2 RNA. Surface contamination of SARS-CoV-2 RNA was common in rooms without surface disinfection and in rooms sprayed with disinfectant twice a day. However, SARS-CoV-2 RNA was not detected in a room cleaned with disinfectant wipes on a regular basis. CONCLUSION: Our data suggest that remote (> 2 m) airborne transmission of SARS-CoV-2 from hospitalized COVID-19 patients is uncommon when aerosol-generating procedures have not been performed. Surface contamination was widespread, except in a room routinely cleaned with disinfectant wipes.


Assuntos
Microbiologia do Ar , Infecções por Coronavirus/transmissão , Exposição Ambiental , Contaminação de Equipamentos , Pneumonia Viral/transmissão , Adulto , Aerossóis , Idoso , Idoso de 80 Anos ou mais , Ar , Betacoronavirus , COVID-19 , China , Desinfecção , Feminino , Hospitais , Humanos , Masculino , Pessoa de Meia-Idade , Pandemias , Quartos de Pacientes , SARS-CoV-2 , Fatores de Tempo , Adulto Jovem
4.
Diabetes Metab J ; 40(5): 396-405, 2016 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-27766247

RESUMO

BACKGROUND: Cognitive impairment and brain damage in diabetes is suggested to be associated with hypoglycemia. The mechanisms of hypoglycemia-induced neural death and apoptosis are not clear and reperfusion injury may be involved. Recent studies show that glucose deprivation/reperfusion induced more neuronal cell death than glucose deprivation itself. The forkhead box O (FOXO) transcription factors are implicated in the regulation of cell apoptosis and survival, but their role in neuronal cells remains unclear. We examined the role of FOXO transcription factors and the involvement of the phosphatidylinositol 3-kinase (PI3K)/Akt and apoptosis-related signaling pathways in PC-12 cells exposed to repeated glucose deprivation/reperfusion. METHODS: PC-12 cells were exposed to control (Dulbecco's Modified Eagle Medium [DMEM] containing 25 mM glucose) or glucose deprivation/reperfusion (DMEM with 0 mM glucose for 6 hours and then DMEM with 25 mM glucose for 18 hours) for 5 days. MTT assay and Western blot analysis were performed for cell viability, apoptosis, and the expression of survival signaling pathways. FOXO3/4',6-diamidino-2-phenylindole staining was done to ascertain the involvement of FOXO transcription factors in glucose deprivation/reperfusion conditions. RESULTS: Compared to PC-12 cells not exposed to hypoglycemia, cells exposed to glucose deprivation/reperfusion showed a reduction of cell viability, decreased expression of phosphorylated Akt and Bcl-2, and an increase of cleaved caspase-3 expression. Of note, FOXO3 protein was localized in the nuclei of glucose deprivation/reperfusion cells but not in the control cells. CONCLUSION: Repeated glucose deprivation/reperfusion caused the neuronal cell death. Activated FOXO3 via the PI3K/Akt pathway in repeated glucose deprivation/reperfusion was involved in genes related to apoptosis.

5.
Planta Med ; 74(12): 1481-7, 2008 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-18816430

RESUMO

A systematic structure-activity relationship of 3beta-hydroxy-27- P- E-coumaroyloxyurs-12-en-28-oic acid ( 7), a triterpene ester isolated from UNCARIA RHYNCHOPHYLLA as a phospholipase Cgamma1 inhibitor, was undertaken with a view toward elucidating its chemical mode of action on PLCgamma1. Related derivatives and analogues of 7 were synthesized and their inhibitory activities against PLCgamma1 were evaluated IN VITRO. The results indicate that 3-OH and 27-esterification may be essential, and that 28-COOH and the 2' double bond appear to be important for activity. Furthermore, the compound possessing a P-coumaroyloxy at position 27 rather than at the 3 and 28 positions shows the greatest inhibitory activity against PLCgamma1. Therefore, this inhibitor will be providing a chemical lead for the further development of cancer chemopreventive or cancer chemotherapeutic agents that have lower toxicity against normal tissues.


Assuntos
Inibidores Enzimáticos/farmacologia , Triterpenos Pentacíclicos/farmacologia , Fosfolipase C gama/antagonistas & inibidores , Uncaria/química , Animais , Bovinos , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Ésteres , Triterpenos Pentacíclicos/síntese química , Triterpenos Pentacíclicos/química , Triterpenos Pentacíclicos/isolamento & purificação , Relação Estrutura-Atividade
6.
Planta Med ; 74(5): 532-4, 2008 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-18543149

RESUMO

Nine long-chain phenols: four cardanols (1-4), two bilobols (5, 6) and three alkylsalicylic acids (7-9) [corrected] were isolated from the CH(2)Cl(2) extracts of the sarcotestas of Ginkgo biloba as HIV-1 protease (PR) inhibitors. From these phenols, the bilobols (IC (50), 2.6 - 5.8 microM) and alkylsalicylic acids (IC (50), 10.2 - 24.9 microM) exhibited dose-dependent potent inhibitory activities on HIV-1 PR, while the cardanols did not. On the other hand, only the alkylsalicylic acids (IC (50), 33.7 - 170.3 microM) inhibited the activities of RNase H of HIV-1 reverse transcriptase (RT), while all of the compounds failed to affect the RNA dependent DNA polymerase (RDDP) of HIV-1 RT. Therefore, we regard bilobols as a new class and selective inhibitors of HIV-1 PR; in addition, alkylsalicylic acids are elucidated as a new class of inhibitors against HIV-1 PR and RNase H of HIV-1 RT.


Assuntos
Ginkgo biloba/química , Inibidores da Protease de HIV/farmacologia , Fenóis/farmacologia , Inibidores da Transcriptase Reversa/farmacologia , Protease de HIV/metabolismo , Inibidores da Protease de HIV/isolamento & purificação , Transcriptase Reversa do HIV/antagonistas & inibidores , Fenóis/isolamento & purificação , Inibidores da Transcriptase Reversa/isolamento & purificação , Ribonuclease H do Vírus da Imunodeficiência Humana/antagonistas & inibidores
7.
Phytother Res ; 22(6): 772-7, 2008 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-18446841

RESUMO

An herbal mixture prepared with Cinnamomi Ramulus, Anemarrhenae Rhizoma and Alpiniae Officinari Rhizoma (CAA) is used in oriental medicine for treating several ailments. The purpose of this study was to determine the mechanisms by which CAA elicits an antiinflammatory effect on nitric oxide (NO) production in the mouse macrophage cell line RAW 264.7 cells. The results indicated that lipopolysaccharide (LPS)-induced NO production was inhibited by CAA in a dose-dependent manner. Western blotting and RT-PCR analysis demonstrated that CAA decreased LPS-induced inducible nitric oxide synthase (iNOS) protein and gene expression in RAW 264.7 cells. Furthermore, CAA inhibited the LPS-induced DNA binding activity of nuclear factor-kappa B (NF-kappaB) and this effect was mediated through inhibiting the degradation of inhibitory factor-kappaBalpha (IkappaBalpha). Therefore, the results demonstrate that CAA inhibits LPS-induced production of NO and expression of iNOS by blocking NF-kappaB activation. CAA might be a potential therapeutic candidate for treating inflammatory diseases such as arthritis.


Assuntos
Macrófagos/efeitos dos fármacos , NF-kappa B/metabolismo , Óxido Nítrico/metabolismo , Extratos Vegetais/farmacologia , Animais , Asparagaceae/química , Western Blotting , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Lauraceae/química , Lipopolissacarídeos/farmacologia , Macrófagos/citologia , Macrófagos/metabolismo , Camundongos , Óxido Nítrico Sintase Tipo II/genética , Óxido Nítrico Sintase Tipo II/metabolismo , Extratos Vegetais/química , Ligação Proteica/efeitos dos fármacos , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Zingiberaceae/química
8.
Chem Pharm Bull (Tokyo) ; 56(5): 711-4, 2008 May.
Artigo em Inglês | MEDLINE | ID: mdl-18451564

RESUMO

Two new hopane type triterpenes, named dryopteric acids A (1) and B (2), were isolated from the Rhizome of Dryopteris crassirhizoma (Aspiadaceae) together with sixteen known compounds (3-18). Of isolated compounds, ursolic acid (15), and dryopteric acid A (1) and B (2) showed potent inhibitory activities against HIV-1 protease with IC50 values of 8.9-44.5 microM. In addition, acetylated compounds 1 and 2 appreciably increased inhibitory activities with their IC50 values of 1.7 and 10.8 microM, respectively.


Assuntos
Dryopteris/química , Inibidores da Protease de HIV/farmacologia , HIV-1/enzimologia , Triterpenos/química , HIV-1/efeitos dos fármacos , Indicadores e Reagentes , Espectrometria de Massas , Raízes de Plantas/química , Espectrofotometria Infravermelho , Espectrofotometria Ultravioleta , Triterpenos/isolamento & purificação
9.
Phytother Res ; 19(6): 511-3, 2005 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-16114085

RESUMO

This study aimed to determine the antinociceptive effect of Aralia continentalis extract (AC) on Freund's adjuvant-induced arthritis in rats. Adult Sprague-Dawley rats received an injection of complete Freund's adjuvant (CFA) into the articular cavity of the ankle joint, and then antinociceptive behaviors and spinal Fos expression were examined. AC was found to suppress significantly nociceptive behaviors caused by CFA injection. In addition, it also decreased adjuvant-induced Fos expression in the lumbar spinal cord induced by CFA. In conclusion, this study showed that AC produced significant antinociceptive effects on CFA-induced arthritis in rats, and it is suggested that AC is recommended to alleviate the arthritis-related symptoms in humans.


Assuntos
Analgésicos/farmacologia , Aralia , Osteoartrite/prevenção & controle , Fitoterapia , Extratos Vegetais/farmacologia , Administração Oral , Analgésicos/administração & dosagem , Analgésicos/uso terapêutico , Animais , Articulação do Tornozelo , Adjuvante de Freund , Masculino , Osteoartrite/induzido quimicamente , Extratos Vegetais/administração & dosagem , Extratos Vegetais/uso terapêutico , Ratos , Ratos Sprague-Dawley , Coluna Vertebral
10.
Arch Pharm Res ; 27(10): 1043-7, 2004 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-15554262

RESUMO

Thirteen compounds were isolated from the CH2Cl2 fraction of Machilus thunbergii as phospholipase Cgamma1 (PLCgamma1) inhibitors. These compounds were identified as nine lignans, two neolignans, and two flavans by spectroscopic analysis. Of these, 5,7-di-O-methyl-3',4'-methylenated (-)-epicatechin (12) and 5,7,3'-tri-O-methyl (-)-epicatechin (13) have not been reported previously in this plant. In addition, seven compounds, machilin A (1), (-)-sesamin (3), machilin G (5), (+)-galbacin (9), licarin A (10), (-)-acuminatin (11) and compound 12 showed dose-dependent potent inhibitory activities against PLCgamma1 in vitro with IC50 values ranging from 8.8 to 26.0 microM. These lignans, neolignans, and flavans are presented as a new class of PLCgamma1 inhibitors. The brief study of the structure activity relationship of these compounds suggested that the benzene ring with the methylene dioxy group is responsible for the expression of inhibitory activities against PLCgamma1. Moreover, it is suggested that inhibition of PLCgamma1 may be an important mechanism for an antiproliferative effect on the human cancer cells. Therefore, these inhibitors may be utilized as cancer chemotherapeutic and chemopreventive agents.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Inibidores Enzimáticos/farmacologia , Flavinas/farmacologia , Lignanas/farmacologia , Plantas Medicinais/química , Fosfolipases Tipo C/antagonistas & inibidores , Animais , Antineoplásicos Fitogênicos/isolamento & purificação , Bovinos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Inibidores Enzimáticos/isolamento & purificação , Flavinas/isolamento & purificação , Humanos , Coreia (Geográfico) , Lignanas/isolamento & purificação , Cloreto de Metileno/química , Fosfolipase C gama , Casca de Planta/química , Extratos Vegetais/química , Solventes , Espectrometria de Massas por Ionização por Electrospray , Espectrofotometria Infravermelho , Relação Estrutura-Atividade
11.
Arch Pharm Res ; 27(5): 544-6, 2004 May.
Artigo em Inglês | MEDLINE | ID: mdl-15202561

RESUMO

Phytochemical investigation of the whole plants of Crotalaria sessiliflora L. led to the isolation of four flavonoids. The structures of these compounds were identified as 2',4',5,7-tetrahydroxyisoflavone (1), 2',4',7-trihydroxyisoflavone (2), 4',7-dihydroxyflavone (3), and isovitexin (4) using spectroscopic analysis. Among these, compounds 2, and 3 have not been reported from Crotalaria species, whereas compounds 1, and 4 were reported from this plant for the first time.


Assuntos
Crotalaria , Flavonoides/química , Flavonoides/isolamento & purificação , Componentes Aéreos da Planta , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação
12.
Biol Pharm Bull ; 27(4): 544-7, 2004 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-15056863

RESUMO

The bioassay-directed isolation of a marine brown alga, Ecklonia cava, afforded four phlorotannin derivatives, eckol (1), 8,8'-bieckol (2), 8,4"'-dieckol (3), and phlorofucofuroeckol A (4). Among these compounds, 2 and 3 exhibited an inhibitory effect on human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) and protease. Specifically, they inhibited the RT more potently than the protease. The inhibitory activity of compound 2 (IC(50), 0.51 microM) against HIV-1 RT was comparable to that of nevirapine (IC(50), 0.28 microM), a reference compound. An enzyme kinetic assay showed that this compound inhibited the RNA-dependent DNA synthesis activity of HIV-1 RT noncompetitively against dUTP/dTTP with a K(i) value of 0.78 microM. With respect to the homopolymeric template/primer, (rA)n(dT)15, 8,8'-bieckol (2) displayed an uncompetitive type of inhibition (K(i), 0.23 microM).


Assuntos
Protease de HIV/química , Transcriptase Reversa do HIV/antagonistas & inibidores , Phaeophyceae/química , Inibidores de Proteases/química , Inibidores da Transcriptase Reversa/química , Taninos/química , Transcriptase Reversa do HIV/química , DNA Polimerase Dirigida por RNA/isolamento & purificação , Taninos/isolamento & purificação
13.
Life Sci ; 74(22): 2769-79, 2004 Apr 16.
Artigo em Inglês | MEDLINE | ID: mdl-15043991

RESUMO

Oleanolic acid (OA) and ursolic acid (UA), triterpene acids having numerous pharmacological activities including anti-inflammatory, anti-cancer, and hepato-protective effects, were tested for their ability to modulate the activities of several cytochrome P450 (CYP) enzymes using human liver microsomes. OA competitively inhibited CYP1A2-catalyzed phenacetin O-deethylation and CYP3A4-catalyzed midazolam 1-hydroxylation, the major human drug metabolizing CYPs, with IC50 (Ki) values of 143.5 (74.2) microM and 78.9 (41.0) microM, respectively. UA competitively inhibited CYP2C19-catalyzed S-mephenytoin 4'-hydroxylation with an IC50 (Ki) value of 119.7 (80.3) microM. However, other CYPs tested showed no or weak inhibition by both OA and UA. The present study demonstrates that OA and UA have inhibitory effects on CYP isoforms using human liver microsomes. It is thus likely that consumption of herbal medicines containing OA or UA, or administration of OA or UA, can cause drug interactions in humans when used concomitantly with drugs that are metabolized primarily by CYP isoforms. In addition, it appears that the inhibitory effect of OA on CYP1A2 is, in part, related to its anti-inflammatory and anticancer activities.


Assuntos
Inibidores das Enzimas do Citocromo P-450 , Inibidores Enzimáticos/farmacologia , Microssomos Hepáticos/efeitos dos fármacos , Preparações de Plantas , Triterpenos/farmacologia , Cromatografia Líquida de Alta Pressão , Sistema Enzimático do Citocromo P-450/metabolismo , Relação Dose-Resposta a Droga , Humanos , Concentração Inibidora 50 , Isoenzimas/antagonistas & inibidores , Isoenzimas/metabolismo , Microssomos Hepáticos/enzimologia , Preparações de Plantas/química , Preparações de Plantas/metabolismo , Triterpenos/análise , Ácido Ursólico
14.
J Pharmacol Sci ; 93(3): 367-71, 2003 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-14646256

RESUMO

Harpagophytum procumbens (Pedaliaceae) has been used for the treatment of pain and arthritis. The effect of Harpagophytum procumbens against lipopolysaccharide-induced inflammation was investigated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, reverse transcription-polymerase chain reaction, prostaglandin E(2) (PGE(2)) immunoassay, and nitric oxide detection on mouse fibroblast cell line L929. The aqueous extract of Harpagophytum procumbens was shown to suppress PGE(2) synthesis and nitric oxide production by inhibiting lipopolysaccharide-stimulated enhancement of the cyclooxygenase-2 and inducible nitric oxide synthase (iNOS) mRNAs expressions in L929 cells. These results suggest that Harpagophytum procumbens exerts anti-inflammatory and analgesic effects probably by suppressing cyclooxygenase-2 and iNOS expressions.


Assuntos
Fibroblastos/efeitos dos fármacos , Harpagophytum , Isoenzimas/antagonistas & inibidores , Óxido Nítrico Sintase/antagonistas & inibidores , Animais , Linhagem Celular , Ciclo-Oxigenase 2 , Relação Dose-Resposta a Droga , Fibroblastos/enzimologia , Regulação Enzimológica da Expressão Gênica/efeitos dos fármacos , Regulação Enzimológica da Expressão Gênica/fisiologia , Isoenzimas/biossíntese , Lipopolissacarídeos/farmacologia , Camundongos , Óxido Nítrico Sintase/biossíntese , Óxido Nítrico Sintase Tipo II , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Prostaglandina-Endoperóxido Sintases/biossíntese
15.
Clin Chim Acta ; 337(1-2): 93-101, 2003 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-14568185

RESUMO

BACKGROUND: Chelidonii herba is classified as Papaver somniferum L. Aqueous extract from C. herba is traditionally used for disorders with symptoms like pain, bloating, abdominal cramp after meals. METHODS: Modulation of C. herba on glycine-activated and glutamate-activated ion currents in the acutely dissociated periaqueductal gray (PAG) neurons was investigated by the nystatin-perforated patch-clamp technique. RESULTS: C. herba inhibited glycine-activated ion current and increased glutamate-activated ion current. C. herba-induced inhibition on glycine-activated ion current is implicated in opioid receptors and GTP-binding proteins (G-proteins). Increased glutamate-activated ion current induced by C. herba is linked neither by opioid receptors nor GTP-binding proteins. CONCLUSIONS: Suppressed glycine-induced response and elevated glutamate-induced response by C. herba may increase neuronal excitability in PAG, results in activation of descending pain control system, and this mechanism can be suggested as one of the analgesic actions of C. herba.


Assuntos
Chelidonium/química , Neurônios/efeitos dos fármacos , Substância Cinzenta Periaquedutal/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Relação Dose-Resposta a Droga , Etilmaleimida/farmacologia , Feminino , Ácido Glutâmico/farmacologia , Glicina/farmacologia , Ativação do Canal Iônico/fisiologia , Masculino , Potenciais da Membrana/efeitos dos fármacos , Naltrexona/farmacologia , Neurônios/fisiologia , Nistatina/farmacologia , Técnicas de Patch-Clamp , Substância Cinzenta Periaquedutal/citologia , Substância Cinzenta Periaquedutal/fisiologia , Ratos , Ratos Sprague-Dawley
16.
Phytother Res ; 17(8): 983-5, 2003 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-13680842

RESUMO

Four phenolic compounds were isolated from Beta vulgaris L. var. cicla L. (Chenopodiaceae). These isolated compounds were identified as N-cis-feruloyl 3-O-methyldopamine (1), N-cis-feruloyl tyramine (2), N-trans-feruloyl 3-O-methyldopamine (3), N-trans-feruloyl tyramine (4), respectively, by spectroscopic analysis. The phenolic amides 1-4 exhibited modest inhibitory activity on LPS-activated nitric oxide production dose-dependently in RAW 264.7 cells.


Assuntos
Amidas/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Beta vulgaris , Óxido Nítrico/biossíntese , Fenóis/farmacologia , Fitoterapia , Extratos Vegetais/farmacologia , Amidas/administração & dosagem , Amidas/uso terapêutico , Animais , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/uso terapêutico , Linhagem Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Lipopolissacarídeos , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Fenóis/administração & dosagem , Fenóis/uso terapêutico , Extratos Vegetais/administração & dosagem , Extratos Vegetais/uso terapêutico , Sementes
17.
Arch Pharm Res ; 26(8): 631-7, 2003 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-12967198

RESUMO

Chloroquine has been used for many decades in the prophylaxis and treatment of malaria. It is metabolized in humans through the N-dealkylation pathway, to desethylchloroquine (DCQ) and bisdesethylchloroquine (BDCQ), by cytochrome P450 (CYP). However, until recently, no data are available on the metabolic pathway of chloroquine. Therefore, the metabolic pathway of chloroquine was evaluated using human liver microsomes and cDNA-expressed CYPs. Chloroquine is mainly metabolized to DCQ, and its Eadie-Hofstee plots were biphasic, indicating the involvement of multiple enzymes, with apparent Km and Vmax values of 0.21 mM and 1.02 nmol/min/mg protein 3.43 mM and 10.47 nmol/min/mg protein for high and low affinity components, respectively. Of the cDNA-expressing CYPs examined, CYP1A2, 2C8, 2C19, 2D6 and 3A4/5 exhibited significant DCQ formation. A study using chemical inhibitors showed only quercetin (a CYP2C8 inhibitor) and ketoconazole (a CYP3A4/5 inhibitor) inhibited the DCQ formation. In addition, the DCQ formation significantly correlated with the CYP3A4/5-catalyzed midazolam 1-hydroxylation (r = 0.868) and CYP2C8-catalyzed paclitaxel 6alpha-hydroxylation (r = 0.900). In conclusion, the results of the present study demonstrated that CYP2C8 and CYP3A4/5 are the major enzymes responsible for the chloroquine N-deethylation to DCQ in human liver microsomes.


Assuntos
Hidrocarboneto de Aril Hidroxilases/biossíntese , Cloroquina/metabolismo , Sistema Enzimático do Citocromo P-450/biossíntese , Microssomos Hepáticos/metabolismo , Hidrocarboneto de Aril Hidroxilases/antagonistas & inibidores , Biotransformação , Citocromo P-450 CYP2C8 , Citocromo P-450 CYP3A , Inibidores das Enzimas do Citocromo P-450 , DNA Complementar/análise , Inibidores Enzimáticos/farmacologia , Humanos , Microssomos Hepáticos/enzimologia
18.
J Pharmacol Sci ; 91(2): 95-104, 2003 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-12686753

RESUMO

To investigate whether bee venom (BV) induces apoptosis, the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, terminal deoxynucleotidyl transferase- mediated dUTP nick end-labeling assay, 4,6-diamidino-2-phenylindole staining, flow cytometric analysis, and DNA fragmentation assay were performed on NCI-H1299 lung cancer cells treated with BV. Through morphological and biochemical analyses, it was demonstrated that NCI-H1299 cells treated with BV exhibit several features of apoptosis. In addition, reverse transcription-polymerase chain reaction and prostaglandin E(2) (PGE(2)) immunoassay were performed to verify whether BV possesses an inhibitory effect on the expression of cyclooxygenase (COX) and PGE(2 )synthesis. Expression of COX-2 mRNA and synthesis of PGE(2) were inhibited by BV. These results suggest the possibility that BV may exert an anti-tumor effect on human lung cancer.


Assuntos
Apoptose/efeitos dos fármacos , Venenos de Abelha/farmacologia , Inibidores de Ciclo-Oxigenase , Regulação Enzimológica da Expressão Gênica/efeitos dos fármacos , Isoenzimas/biossíntese , Neoplasias Pulmonares/enzimologia , Prostaglandina-Endoperóxido Sintases/biossíntese , Proteínas Proto-Oncogênicas c-bcl-2 , RNA Mensageiro/biossíntese , Caspases/metabolismo , Ciclo Celular/efeitos dos fármacos , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Ciclo-Oxigenase 1 , Ciclo-Oxigenase 2 , Inibidores de Ciclo-Oxigenase 2 , Fragmentação do DNA/efeitos dos fármacos , Dinoprostona/metabolismo , Citometria de Fluxo , Corantes Fluorescentes , Genes bcl-2/efeitos dos fármacos , Humanos , Marcação In Situ das Extremidades Cortadas , Indicadores e Reagentes , Indóis , Isoenzimas/genética , Proteínas de Membrana , Prostaglandina-Endoperóxido Sintases/genética , Proteínas Proto-Oncogênicas/biossíntese , RNA Mensageiro/genética , RNA Mensageiro/isolamento & purificação , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Sais de Tetrazólio , Tiazóis , Proteína X Associada a bcl-2
19.
Planta Med ; 68(5): 457-9, 2002 May.
Artigo em Inglês | MEDLINE | ID: mdl-12058327

RESUMO

The bioassay-directed isolation of Terminalia chebula fruits afforded four human immunodeficiency virus type 1 (HIV-1) integrase inhibitors, gallic acid ( 1) and three galloyl glucoses ( 2 - 4). In addition, four flavonol glycoside gallates ( 5 - 8) from Euphorbia pekinensis containing the galloyl moiety also showed the inhibitory activity at a level comparable to those of 2 - 4. By comparison with the activities of the compounds not bearing this moiety, it is proposed that the galloyl moiety plays a major role for inhibition against the 3'-processing of HIV-1 integrase of these compounds.


Assuntos
Euphorbia , Ácido Gálico/farmacologia , Inibidores de Integrase de HIV/farmacologia , Integrase de HIV/efeitos dos fármacos , Taninos Hidrolisáveis , Taninos/farmacologia , Terminalia , Benzopiranos/farmacologia , Sequência de Carboidratos , Flavonoides/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Frutas/química , Ácido Gálico/análogos & derivados , Glucosídeos/farmacologia , Glicosídeos/farmacologia , Dados de Sequência Molecular , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , DNA Polimerase Dirigida por RNA/efeitos dos fármacos , Rutina/farmacologia
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