RESUMO
Specific flavonoid-rich foods/beverages are reported to exert positive effects on vascular function; however, data relating to effects in the postprandial state are limited. The present study investigated the postprandial, time-dependent (0-7 h) impact of citrus flavanone intake on vascular function. An acute, randomised, controlled, double-masked, cross-over intervention study was conducted by including middle-aged healthy men (30-65 years, n 28) to assess the impact of flavanone intake (orange juice: 128·9 mg; flavanone-rich orange juice: 272·1 mg; homogenised whole orange: 452·8 mg; isoenergetic control: 0 mg flavanones) on postprandial (double meal delivering a total of 81 g of fat) endothelial function. Endothelial function was assessed by flow-mediated dilatation (FMD) of the brachial artery at 0, 2, 5 and 7 h. Plasma levels of naringenin/hesperetin metabolites (sulphates and glucuronides) and nitric oxide species were also measured. All flavanone interventions were effective at attenuating transient impairments in FMD induced by the double meal (7 h post intake; P<0·05), but no dose-response effects were observed. The effects on FMD coincided with the peak of naringenin/hesperetin metabolites in circulation (7 h) and sustained levels of plasma nitrite. In summary, citrus flavanones are effective at counteracting the negative impact of a sequential double meal on human vascular function, potentially through the actions of flavanone metabolites on nitric oxide.
Assuntos
Doenças Cardiovasculares/prevenção & controle , Citrus , Endotélio Vascular/fisiopatologia , Flavanonas/uso terapêutico , Sucos de Frutas e Vegetais , Óxido Nítrico/agonistas , Adulto , Biomarcadores/sangue , Artéria Braquial , Desjejum , Doenças Cardiovasculares/epidemiologia , Doenças Cardiovasculares/metabolismo , Doenças Cardiovasculares/fisiopatologia , Estudos Cross-Over , Dieta Hiperlipídica/efeitos adversos , Dilatação Patológica/diagnóstico por imagem , Dilatação Patológica/etiologia , Dilatação Patológica/prevenção & controle , Método Duplo-Cego , Endotélio Vascular/diagnóstico por imagem , Endotélio Vascular/metabolismo , Inglaterra/epidemiologia , Flavanonas/administração & dosagem , Flavanonas/sangue , Humanos , Almoço , Masculino , Pessoa de Meia-Idade , Óxido Nítrico/sangue , Pacientes Desistentes do Tratamento , Período Pós-Prandial , Risco , UltrassonografiaRESUMO
Bioassay-guided fractionation of the EtOH extracts obtained from a plant identified as Cyphostemma greveana Desc. (Vitaceae) led to the identification of one macrolide, lasiodiplodin (1), three sesquiterpenoids, 12-hydroxy-15-oxoselina-4,11-diene (2), 1ß,6α-dihydroxyeudesm-4(15)-ene (3), and (7R*)-opposit-4(15)-ene-1ß,7-diol (5), and a new diterpenoid, 16,18-dihydroxykolavenic acid lactone (4). All the isolates were tested against the A2780 human ovarian cancer cell line, and compound 4 and a fraction containing 5 as the major constituent showed antiproliferative activities with IC(50) values of 0.44â µM (0.14â µg/ml) and 0.045â µg/ml, respectively. A partial synthesis of compound 5 was carried out, but the pure synthetic compound was inactive, indicating that the activity of the fraction containing it must be due to a very minor and as yet unidentified substance.
Assuntos
Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Neoplasias Ovarianas/tratamento farmacológico , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Vitaceae/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Humanos , Madagáscar , Extratos Vegetais/isolamento & purificação , ÁrvoresRESUMO
Fractionation of an ethanol extract of a Madagascar collection of the leaves and fruit of Cassipourea lanceolata Tul. led to the isolation of three euphane triterpenoids 1-3. The (1)H and (13)C NMR spectra of all compounds were fully assigned using a combination of 2D NMR experiments, including COSY, TOCSY, HSQC (HMQC), HMBC and ROESY sequences. The three compounds showed weak antiproliferative activities against the A2780 human ovarian cancer cell line, with IC(50) values of 25, 25 and 32 microM, respectively.
Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Neoplasias Ovarianas/tratamento farmacológico , Extratos Vegetais/química , Rhizophoraceae/química , Triterpenos/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Feminino , Frutas , Humanos , Concentração Inibidora 50 , Madagáscar , Estrutura Molecular , Fitoterapia , Extratos Vegetais/farmacologia , Folhas de Planta , Triterpenos/química , Triterpenos/farmacologiaRESUMO
Bioassay-guided fractionation of an ethanol extract of a Madagascar collection of the bark of Scutia myrtina led to the isolation of three new anthrone-anthraquinones, scutianthraquinones A, B and C (1-3), one new bisanthrone-anthraquinone, scutianthraquinone D (4), and the known anthraquinone, aloesaponarin I (5). The structures of all compounds were determined using a combination of 1D and 2D NMR experiments, including COSY, TOCSY, HSQC, HMBC, and ROESY sequences, and mass spectrometry. All the isolated compounds were tested against the A2780 human ovarian cancer cell line for antiproliferative activities, and against the chloroquine-resistant Plasmodium falciparum strains Dd2 and FCM29 for antiplasmodial activities. Compounds 1, 2 and 4 showed weak antiproliferative activities against the A2780 ovarian cancer cell line, while compounds 1-4 exhibited moderate antiplasmodial activities against P. falciparum Dd2 and compounds 1, 2, and 4 exhibited moderate antiplasmodial activities against P. falciparum FCM29.
Assuntos
Antraquinonas/química , Antimaláricos/química , Antineoplásicos Fitogênicos/química , Rhamnaceae/química , Animais , Antraquinonas/isolamento & purificação , Antraquinonas/farmacologia , Antimaláricos/isolamento & purificação , Antimaláricos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Humanos , Madagáscar , Casca de Planta/química , Extratos Vegetais/química , Plasmodium falciparum/efeitos dos fármacosRESUMO
Bioassay-guided fractionation of an ethanol extract of a Madagascar collection of the fruits of Cordyla madagascariensis ssp. madagascariensis led to the isolation of the four new cassane diterpenoids 1-4. The 1H and 13C NMR spectra of all compounds were fully assigned using a combination of 2D NMR experiments, including COSY, HSQC, HMBC, and ROESY sequences. All of the isolates were tested against the A2780 human ovarian cancer cell line, and compounds 1 and 2 showed mild antiproliferative activity with IC50 values of 10 and 36 microM, respectively.