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1.
Proc Natl Acad Sci U S A ; 115(12): 3072-3077, 2018 03 20.
Artigo em Inglês | MEDLINE | ID: mdl-29483242

RESUMO

The extent of increasing anthropogenic impacts on large marine vertebrates partly depends on the animals' movement patterns. Effective conservation requires identification of the key drivers of movement including intrinsic properties and extrinsic constraints associated with the dynamic nature of the environments the animals inhabit. However, the relative importance of intrinsic versus extrinsic factors remains elusive. We analyze a global dataset of ∼2.8 million locations from >2,600 tracked individuals across 50 marine vertebrates evolutionarily separated by millions of years and using different locomotion modes (fly, swim, walk/paddle). Strikingly, movement patterns show a remarkable convergence, being strongly conserved across species and independent of body length and mass, despite these traits ranging over 10 orders of magnitude among the species studied. This represents a fundamental difference between marine and terrestrial vertebrates not previously identified, likely linked to the reduced costs of locomotion in water. Movement patterns were primarily explained by the interaction between species-specific traits and the habitat(s) they move through, resulting in complex movement patterns when moving close to coasts compared with more predictable patterns when moving in open oceans. This distinct difference may be associated with greater complexity within coastal microhabitats, highlighting a critical role of preferred habitat in shaping marine vertebrate global movements. Efforts to develop understanding of the characteristics of vertebrate movement should consider the habitat(s) through which they move to identify how movement patterns will alter with forecasted severe ocean changes, such as reduced Arctic sea ice cover, sea level rise, and declining oxygen content.


Assuntos
Migração Animal , Bases de Dados Factuais , Oceanos e Mares , Vertebrados , Animais , Ecossistema
2.
Lett Appl Microbiol ; 59(4): 412-21, 2014 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-24888993

RESUMO

The antimicrobial activities of 44 methanolic extracts from different parts of Iranian indigenous plant species used in traditional medicines of Iran were tested against a panel of 35 pathogenic and multiresistant bacteria and 1 yeast. The antimicrobial efficacy was determined using Müller-Hinton agar in Petri dishes seeded by a multiple inoculator and minimal inhibition concentration (MIC) method. The 21 most active extracts (MIC < 0·3 mg ml(-1) for one or several micro-organisms) were submitted to a more refined measurement. The best antibacterial activity was obtained by 10 plants. Microdilution assays allowed to determinate the MIC and MBC of the 21 most active extracts. The lowest achieved MIC value was 78 µg ml(-1), with 4 extracts. This work confirms the antimicrobial activity of assayed plants and suggests further examination to identify the chemical structure of their antimicrobial compounds. Significance and impact of the study: This study describes the antimicrobial screening of Iranian plant extracts chosen according to traditional practice against 36 microbial strains, from reference culture collections or recent clinical isolates, and enables to select 4 candidates for further chemical characterization and biological assessment: Dorema ammoniacum, Ferula assa-foetida, Ferulago contracta (seeds) and Perovskia abrotanoides (aerial parts). This may be useful in the development of potential antimicrobial agents, from easily harvested and highly sustainable plant parts. Moreover, the weak extent of cross-resistance between plant extracts and antibiotics warrants further research and may promote a strategy based on less potent but time-trained products.


Assuntos
Anti-Infecciosos/farmacologia , Bactérias/efeitos dos fármacos , Farmacorresistência Bacteriana Múltipla , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Anti-Infecciosos/química , Irã (Geográfico) , Testes de Sensibilidade Microbiana , Extratos Vegetais/química
3.
Ann Rheum Dis ; 69(1): 113-9, 2010 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-19304567

RESUMO

OBJECTIVES: The primary objective was to compare a single, 6 ml, intra-articular injection of hylan G-F 20 with placebo in patients with symptomatic knee osteoarthritis. The safety of a repeat injection of hylan G-F 20 was also assessed. METHODS: Patients with primary osteoarthritis knee pain were randomly assigned to arthrocentesis plus a 6 ml intra-articular injection of either hylan G-F 20 or placebo in a prospective, double-blind (one injector/one blinded observer) study. RESULTS: were evaluated at 4, 8, 12, 18 and 26 weeks post-injection. The primary outcome criterion was change from baseline over 26 weeks in Western Ontario and McMaster Universities (WOMAC) Osteoarthritis Index A pain. Secondary outcome measures included WOMAC A1 and C, patient global assessment (PGA) and clinical observer global assessment (COGA) and Outcome Measures in Rheumatology, Osteoarthritis Research Society International responder rates. A 4-week, open, repeat treatment phase evaluated safety only. Results: A total of 253 patients (Kellgren-Lawrence grade II or III) was randomly assigned. Patients receiving hylan G-F 20 experienced statistically significantly greater improvements in WOMAC A pain scores (-0.15, SE 0.076, p = 0.047), and several of the secondary outcome measures (WOMAC A1, PGA and COGA), than patients receiving placebo. There was no difference between the safety results of the two groups. No increased risk of local adverse events was observed in the open, repeat treatment phase. CONCLUSIONS: This placebo-controlled study demonstrated that, in patients with knee osteoarthritis, a single 6 ml intra-articular injection of hylan G-F 20 is safe and effective in providing statistically significant, clinically relevant pain relief over 26 weeks, with a modest difference versus placebo.


Assuntos
Ácido Hialurônico/análogos & derivados , Osteoartrite do Joelho/tratamento farmacológico , Viscossuplementação/métodos , Viscossuplementos/administração & dosagem , Idoso , Materiais Biocompatíveis/administração & dosagem , Materiais Biocompatíveis/efeitos adversos , Método Duplo-Cego , Esquema de Medicação , Feminino , Humanos , Ácido Hialurônico/administração & dosagem , Ácido Hialurônico/efeitos adversos , Injeções Intra-Articulares , Masculino , Pessoa de Meia-Idade , Osteoartrite do Joelho/fisiopatologia , Índice de Gravidade de Doença , Resultado do Tratamento , Viscossuplementação/efeitos adversos , Viscossuplementos/efeitos adversos
4.
Arch Orthop Trauma Surg ; 129(3): 417-23, 2009 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-18365224

RESUMO

INTRODUCTION: Viscosupplementation by repeated intra-articular injections of hyaluronic acid (HA) is used widely in the treatment of symptomatic knee osteoarthritis (OA). The number of injections required can limit the availability of treatment and affect patient compliance. The aim of this study was to assess different dosing regimens of hylan G-F 20, a high molecular-weight cross-linked derivative of HA, in the treatment of pain due to knee OA. MATERIALS AND METHODS: Pilot, prospective, multi-centre, open-label, randomised trial in 100 patients with unilateral, symptomatic, tibio-femoral OA (Kellgren-Lawrence grade II or III), aged > or =40 years. Patients were randomised to receive varying dosing regimens of hylan G-F 20 (1 x 6 mL, 1 x 4 mL, 2 x 4 mL 2 weeks apart, 3 x 4 mL 1 week apart, or 3 x 2 mL 1 week apart). Adverse events (AE's) were monitored throughout the study. The primary efficacy endpoint was the change from baseline in the patient-rated knee OA pain assessment (100 mm visual analogue scale (VAS)) at 24 weeks. The secondary efficacy criteria included the WOMAC index, patient and physician global assessments using a 100 mm VAS, and knee OA pain assessment at all other visits. Concomitant use of permitted rescue medications (paracetamol) was also assessed. RESULTS: The treatment was well tolerated overall. Patients in the 3 x 4 mL group reported the highest percentage of device-related local AE's (30%) while patients in the 1 x 6 mL and 3 x 2 mL groups reported only 10%. There were no serious device-related AEs. There was a statistically significant improvement from baseline at week 24 in all efficacy endpoints for all treatment regimens. The 1 x 6 and 3 x 4 and 3 x 2 mL treatment groups showed the greatest mean improvements (-34.9, -32.6 and -36.7 mm respectively) in the patient-rated knee OA pain assessment VAS. CONCLUSION: This study suggests that a single 6 mL injection of hylan G-F 20 may be as efficacious, and as well tolerated, as 3 x 2 mL one week apart. A double-blind, controlled trial is needed to confirm these data.


Assuntos
Materiais Biocompatíveis/administração & dosagem , Ácido Hialurônico/análogos & derivados , Osteoartrite do Joelho/tratamento farmacológico , Viscossuplementação , Adulto , Idoso , Idoso de 80 Anos ou mais , Artralgia/tratamento farmacológico , Artralgia/etiologia , Relação Dose-Resposta a Droga , Feminino , Humanos , Ácido Hialurônico/administração & dosagem , Injeções Intra-Articulares , Masculino , Pessoa de Meia-Idade , Osteoartrite do Joelho/complicações , Projetos Piloto , Estudos Prospectivos , Resultado do Tratamento
5.
Proc Natl Acad Sci U S A ; 105(33): 11634-9, 2008 Aug 19.
Artigo em Inglês | MEDLINE | ID: mdl-18695241

RESUMO

Polar regions are particularly sensitive to climate change, with the potential for significant feedbacks between ocean circulation, sea ice, and the ocean carbon cycle. However, the difficulty in obtaining in situ data means that our ability to detect and interpret change is very limited, especially in the Southern Ocean, where the ocean beneath the sea ice remains almost entirely unobserved and the rate of sea-ice formation is poorly known. Here, we show that southern elephant seals (Mirounga leonina) equipped with oceanographic sensors can measure ocean structure and water mass changes in regions and seasons rarely observed with traditional oceanographic platforms. In particular, seals provided a 30-fold increase in hydrographic profiles from the sea-ice zone, allowing the major fronts to be mapped south of 60 degrees S and sea-ice formation rates to be inferred from changes in upper ocean salinity. Sea-ice production rates peaked in early winter (April-May) during the rapid northward expansion of the pack ice and declined by a factor of 2 to 3 between May and August, in agreement with a three-dimensional coupled ocean-sea-ice model. By measuring the high-latitude ocean during winter, elephant seals fill a "blind spot" in our sampling coverage, enabling the establishment of a truly global ocean-observing system.


Assuntos
Gelo , Focas Verdadeiras , Água do Mar , Animais , Temperatura
6.
Phytomedicine ; 15(8): 625-9, 2008 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-18061417

RESUMO

In the present study, the aphrodisiac properties of Microdesmis keayana J. Léonard root extract and major isolated alkaloids were evaluated by observing the sexual behavior of male rats. Aqueous extract (150mg/kg body weight) and pure alkaloids (3mg/kg body weight) were administered orally by gavage to male rats. Latent times of observation, intromission and ejaculation, mounting behavior, number of intromissions and mating performances were evaluated and compared to those obtained with untreated rats in the presence of receptive and non-receptive females. The results have shown that aqueous extract and alkaloids of M. keayana stimulate sexual parameters in rats' sexual behavior. A short-term toxicity study undertaken to establish the therapeutic index of aqueous extract, showed that a high dose of the extract (2g/kg body weight) caused no mortality or changes in rats' behavior.


Assuntos
Afrodisíacos/farmacologia , Magnoliopsida/química , Comportamento Sexual Animal/efeitos dos fármacos , Animais , Afrodisíacos/química , Ácidos Cumáricos/química , Ácidos Cumáricos/farmacologia , Feminino , Masculino , Estrutura Molecular , Extratos Vegetais , Ratos , Ratos Wistar , Espermidina/análogos & derivados , Espermidina/química , Espermidina/farmacologia , Espermina/análogos & derivados , Espermina/química , Espermina/farmacologia
7.
Proc Natl Acad Sci U S A ; 104(34): 13705-10, 2007 Aug 21.
Artigo em Inglês | MEDLINE | ID: mdl-17693555

RESUMO

Responses by marine top predators to environmental variability have previously been almost impossible to observe directly. By using animal-mounted instruments simultaneously recording movements, diving behavior, and in situ oceanographic properties, we studied the behavioral and physiological responses of southern elephant seals to spatial environmental variability throughout their circumpolar range. Improved body condition of seals in the Atlantic sector was associated with Circumpolar Deep Water upwelling regions within the Antarctic Circumpolar Current, whereas High-Salinity Shelf Waters or temperature/salinity gradients under winter pack ice were important in the Indian and Pacific sectors. Energetic consequences of these variations could help explain recently observed population trends, showing the usefulness of this approach in examining the sensitivity of top predators to global and regional-scale climate variability.


Assuntos
Comportamento Predatório/fisiologia , Migração Animal , Animais , Caniformia/fisiologia , Ecologia , Oceanografia , Dinâmica Populacional , Estações do Ano
8.
Clin Exp Rheumatol ; 21(5): 605-10, 2003.
Artigo em Inglês | MEDLINE | ID: mdl-14611109

RESUMO

OBJECTIVE: To obtain prospective data on feasibility and safety of intra-articular injections of hylan G-F20 in patients with symptomatic hip osteoarthritis (OA). METHODS: Fifty-seven patients with primary hip OA, Kellgren-Lawrence grade II-III, aged > or = 40 and walking pain 50-90 mm on a visual analogue scale (VAS) were enrolled in an open-label, multicentre pilot trial. Hylan G-F20 (2 ml) was injected intra-articularly (IA) in the hip under fluoroscopy at D0, and follow-up visits were performed at D7-30-60-90. The possibility of a second injection at D30-60 or 90 was considered if the reported pain level was equivalent to baseline. Adverse events, walking pain (VAS), WOMAC index, patient and physician's global assessment were recorded at each visit. RESULTS: Twenty-five patients 1 injection and 32 received 2 injections. Transient hip pain was reported following 10.1% of injections, but no patient withdrew from the study because of this. Two mild synovial fluid aseptic effusions occurred after the first injection. No systemic device-related adverse event was reported. Walking pain decreased from 69.3 mm at entry to 39.5 mm at the end point (p < 0.0001). All other outcome measures decreased significantly. CONCLUSION: Viscosupplementation with hylan G-F20 is feasible, easy to perform and well-tolerated in hip OA. A double-blind, controlled study should be performed to confirm data on its efficacy.


Assuntos
Ácido Hialurônico/análogos & derivados , Ácido Hialurônico/administração & dosagem , Osteoartrite do Quadril/tratamento farmacológico , Adulto , Idoso , Feminino , Seguimentos , Humanos , Injeções Intra-Articulares , Masculino , Pessoa de Meia-Idade , Projetos Piloto , Estudos Prospectivos , Resultado do Tratamento
9.
Pharmazie ; 58(8): 577-81, 2003 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-12967038

RESUMO

Polyphenol-rich diet decreases cardiovascular risk. LDL oxidation is the primary event in atherosclerosis plaque formation and antioxidants such as polyphenols were shown to inhibit LDL oxidation and atherosclerosis development. Hawthorn (Crataegus) and derived pharmaceuticals are rich in polyphenols and already prescribed to treat moderate heart failure, nervousness and sleep disorders. Extracts either from fresh plant parts (flower buds, flowers, young leaves or green fruits) or from dried pharmaceutical parts (flowers and flowering tops) were previously shown to be effective inhibitors of lipoperoxidation and scavengers of oxygen species. In this study, the capacity of total and ethyl-acetate extracts from dried pharmaceutical flowers, tops and fruits to inhibit Cu(2+)-induced LDL oxidation was tested. This capacity was positively linked to their content in total polyphenols, proanthocyanidins (global and oligomeric forms), as well as to their content in two individual phenolics: a flavanol, the dimeric procyanidin B2 and a flavonol glycoside, hyperoside. Flavanol-type phenolics showed to be higher active than the majority of the flavonoids tested in inhibiting Cu(2+)-induced LDL peroxidation. This study suggests that hawthorn could be a source of polyphenols able to inhibit LDL oxidation.


Assuntos
Biflavonoides , Crataegus/química , Lipoproteínas LDL/metabolismo , Proantocianidinas , Acetatos , Antioxidantes/química , Antioxidantes/farmacologia , Catequina/química , Catequina/farmacologia , Cromatografia Líquida de Alta Pressão , Colorimetria , Cobre/química , Flavonoides/química , Flavonoides/farmacologia , Humanos , Lipoproteínas LDL/sangue , Lipoproteínas LDL/química , Oxirredução , Fenóis/química , Fenóis/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Solventes
10.
Phytother Res ; 16(2): 157-61, 2002 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-11933119

RESUMO

Respiratory burst leads polymorphonuclear neutrophils (PMN) to produce reactive oxygen species (ROS) such as superoxide anions (O(2)(o-)), hypochlorous acid (HOCl) and hydrogen peroxide (H(2)O(2)) which may possess deleterious effects for the organism. Rosa canina fruits are well known to contain a large amount of vitamin C which is antioxidant. This study was focused on the polyphenolics contained in rose hips to evaluate their antioxidative properties. We prepared a rose hip extract deprived of vitamin C. The extract contained mainly phenolics such as proanthocyanidins and flavonoids. We investigated its effects directly against (O(2)(o-)), HOCl and H(2)O(2) and investigated its effects on isolated PMN. For that, in vitro inflammatory conditions were reproduced by stimulating PMN with stimuli having different transductional pathways, in order to determine a possible mechanism of action. The results showed that the extract can inhibit ROS tested in acellular and cellular systems. The IC(50) obtained were 5.73 mg/L, 1.33 mg/L and 2.34 mg/L respectively for (O(2)(o-)), HOCl and H(2)O(2) in acellular experiments. For cellular experiments, the IC(50) were quite similar. Thus, the extract did not present an effect on PMN metabolism. Therefore, the antioxidative effects of Rosa canina are due not only to vitamin C but also to polyphenolics.


Assuntos
Frutas/química , Neutrófilos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Proantocianidinas , Explosão Respiratória/efeitos dos fármacos , Rosa , Antocianinas/metabolismo , Ácido Ascórbico/metabolismo , Relação Dose-Resposta a Droga , Feminino , Flavonoides/metabolismo , Humanos , Peróxido de Hidrogênio/antagonistas & inibidores , Peróxido de Hidrogênio/metabolismo , Ácido Hipocloroso/antagonistas & inibidores , Ácido Hipocloroso/metabolismo , L-Lactato Desidrogenase/metabolismo , Masculino , Fenóis/química , Fenóis/isolamento & purificação , Fenóis/metabolismo , Polímeros/química , Polímeros/isolamento & purificação , Polímeros/metabolismo , Espécies Reativas de Oxigênio/antagonistas & inibidores , Espécies Reativas de Oxigênio/metabolismo , Superóxidos/antagonistas & inibidores , Superóxidos/metabolismo
11.
Biochem Syst Ecol ; 28(10): 1031-1033, 2000 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-10996268

RESUMO

Two lactoylate flavonoids, luteolin-7-lactate and luteolin-7-glucosyl-lactate were isolated from Ballota nigra. They should be used for the chemical standardization of this drug of medicinal interest.

12.
J Ethnopharmacol ; 72(1-2): 35-42, 2000 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-10967451

RESUMO

The interest of polyphenolics as therapeutic agents against diseases involving radical damage is growing. The phenolic contents of the hulls and flour from the seeds of Fagopyrum esculentum (French variety 'La Harpe') (total phenols, flavonoids, total flavanols, oligomeric proanthocyanidins) are compared with the antioxidative effects of the extracts against reactive oxygen species: hydrogen peroxide, hypochlorous acid, superoxide anion. The higher efficiency of the flour extract can be related to its higher flavanolic content rather than to flavonoids which are predominant in the hull extract.


Assuntos
Antioxidantes/farmacologia , Fagopyrum/química , Fenóis/farmacologia , Proantocianidinas , Antocianinas/análise , Antioxidantes/química , Cromatografia Líquida de Alta Pressão , Cromatografia em Camada Fina , Flavonoides/análise , Flavonoides/isolamento & purificação , Farinha/análise , Sequestradores de Radicais Livres/farmacologia , Peróxido de Hidrogênio/química , Ácido Hipocloroso/química , Fenóis/química , Sementes/química , Superóxidos/química
13.
Phytother Res ; 14(2): 93-8, 2000 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-10685104

RESUMO

From the European plant Ballota nigra L. various polyphenols including phenylpropanoid derivatives were isolated. There is increasing evidence that oxidized low-density lipoproteins (Ox-LDL) might be involved in the pathogenesis of atherosclerosis and it has been reported that polyphenols inhibit LDL peroxidation and atherogenesis. The goal of this study was to test whether the major polyphenolic compounds extracted from Ballota nigra, four phenylpropanoid glycosides, verbascoside, forsythoside B, arenarioside, and ballotetroside and one non-glycosidic phenylpropanoid, caffeoyl-L-malic acid, inhibit Cu(2+)-induced LDL peroxidation. The effectiveness of these compounds was compared to the activity of quercetin, a well-known polyphenol inhibitor of Cu(2+)-induced LDL oxidation. Antioxidant efficacious doses (ED 50) of arenarioside and ballotetroside were 1.8 microM and 7.5 microM respectively, while in the same conditions, the ED 50 of forsythoside B and verbascoside were similar (1 microM) and those of quercetin and of caffeoyl-L-malic acid were 2.3 microM and 9.5 microM respectively. Spectrophotometric studies show that quercetin is a Cu(2+) chelator while phenylpropanoid glycosides and caffeoyl-L-malic acid are not Cu(2+) chelators. Therefore, phenylpropanoid glycosides are strong inhibitors of Cu(2+)-induced LDL oxidation, independent of any capacity to act as Cu(2+) chelators.


Assuntos
Flavonoides , Glicosídeos/farmacologia , Lamiaceae , Peroxidação de Lipídeos/efeitos dos fármacos , Lipoproteínas LDL/efeitos dos fármacos , Fenóis/farmacologia , Polímeros/farmacologia , Ácidos Cafeicos/isolamento & purificação , Ácidos Cafeicos/farmacologia , Cobre/farmacologia , Glucosídeos/isolamento & purificação , Glucosídeos/farmacologia , Glicosídeos/isolamento & purificação , Humanos , Cinética , Lipoproteínas LDL/metabolismo , Malatos/isolamento & purificação , Malatos/farmacologia , Espectrometria de Massas , Fenóis/isolamento & purificação , Plantas Medicinais , Polímeros/isolamento & purificação , Polifenóis
14.
Arzneimittelforschung ; 50(1): 16-23, 2000 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-10683711

RESUMO

Ballota nigra is a European plant known for its neurosedative properties. In this study, the ability of five phenylpropanoids (verbascoside, forsythoside B, arenarioside, ballotetroside, and caffeoyl malic acid) isolated from a hydroalcoholic extract, to bind to benzodiazepine, dopaminergic, and morphinic receptors was investigated. To carry out these studies, affinity tests with rat striata, entire brains and receptor rich preparations were employed. In addition, the phenolic aspect of these five phenylpropanoid esters led to investigate antioxidant activities using cell-free experiments and cellular experiments including isolated polymorphonuclear neutrophils (PMN). Effects of phenylpropanoid esters against reactive oxygen species as superoxide anion, peroxide hydrogen, hypochlorous acid and hydroxyl radical were tested. These molecules are liberated by PMN during inflammatory disorders, so that reproduction of this process in vitro stimulating PMN by chemical stimulants was undertaken. Results show that four of the five compounds are able to bind to the studied receptors. Inhibitory concentrations at 50% were determined and vary from 0.4 to 4.7 mg/ml. This may be in relation with the Ballota nigra known neurosedative activities. Results concerning antioxidant investigations evidence an ability to scavenge reactive oxygen species. Inhibitory concentrations at 50% obtained are comparable to those of known antioxidant drugs (mesna or N-acetyl cysteine). Moreover, the use of different stimuli having various pathways of action on PMN oxidative metabolism permits to establish that each phenylpropanoid ester has its own particular way of action by using proteine kinase C or phospholipase C pathways.


Assuntos
Antioxidantes/farmacologia , Catecóis/farmacologia , Hipnóticos e Sedativos/farmacologia , Plantas Medicinais/química , Animais , Catecóis/isolamento & purificação , Ativação Enzimática/efeitos dos fármacos , Feminino , Humanos , Técnicas In Vitro , Inositol 1,4,5-Trifosfato/farmacologia , L-Lactato Desidrogenase/metabolismo , Masculino , N-Formilmetionina Leucil-Fenilalanina/farmacologia , Neutrófilos/efeitos dos fármacos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Proteína Quinase C/metabolismo , Ratos , Receptores Dopaminérgicos/efeitos dos fármacos , Receptores de GABA-A/efeitos dos fármacos , Receptores Opioides/efeitos dos fármacos , Espectrofotometria Ultravioleta , Superóxidos/metabolismo , Acetato de Tetradecanoilforbol/farmacologia
15.
J Nat Prod ; 63(1): 6-11, 2000 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-10650069

RESUMO

A reinvestigation of the stem bark of Cleistopholis glauca yielded 14 compounds, of which seven were either novel or had not been previously reported from this species. These were identified as the farnesane sesquiterpene methyl-(2E,6E)-10-oxo-3,7, 11-trimethyl-dodeca-2,6-dienoate (1); the azaanthracene alkaloid cleistopholine (4); two partially acetylated oligorhamnoside derivatives, 1-O-dodecanyl-2,3, 4-tri-O-acetyl-alpha-rhamnopyranosyl-(1-->3)-2, 4-di-O-acetyl-alpha-rhamnopyranosyl-(1-->3)-4-O-acetyl-alpha-rhamnopy ranosyl-(1-->4)-alpha-rhamnopyranoside (6) and 1-O-dodecanyl-2, 4-di-O-acetyl-alpha-rhamnopyranosyl-(1-->3)-2, 4-di-O-acetyl-alpha-rhamnopyranosyl-(1-->3)-4-O-acetyl-alpha-rhamnopy ranosyl-(1-->4)-alpha-rhamnopyranoside (8), for which the trivial names cleistetroside-7 and cleistetroside-6 were assigned, respectively; the dihydrobenzofuran neolignan rel-(2alpha, 3beta)-7-O-methylcedrusin (12); and the flavonoids dihydroquercetin (13) and quercetin (14). Structure assignments of all compounds were established by spectroscopic methods and comparison with published data. The chemosystematic significance of the occurrence of the isolated components is mentioned. Compounds 1, 6, and 8 are novel natural products.


Assuntos
Glicosídeos/isolamento & purificação , Plantas Medicinais/química , Sequência de Carboidratos , Glicosídeos/química , Dados de Sequência Molecular , Caules de Planta/química , Análise Espectral
16.
Phytochemistry ; 55(5): 439-46, 2000 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-11140605

RESUMO

The aerial parts of Goniothalamus gardneri (Annonaceae) has yielded the known flavonoids 2'-hydroxy-4,4',6'-trimethoxychalcone (flavokawain A), 2',4'-dihydroxy-4,6'-dimethoxydihydrochalcone, 4,2',4'-trihydroxy-6'-methoxydihydrochalcone, 5,7,4'-trimethoxyflavanone (naringenin trimethyl ether) and 7-hydroxy-5,4'-dimethoxyflavanone (tsugafolin) together with three novel compounds, the dimer characterised as (rel)-1beta,2alpha-di-(2,4-dihydroxy-6-methoxybenzoyl)-3beta,4alpha-di-(4-methoxyphenyl)-cyclobutane, 2',4'-dihydroxy-4,6'-dimethoxychalcone and 2'-hydroxy-4,4',6'-trimethoxydihydrochalcone. The last two have previously been synthesised but appear to be new natural products. A similar study of the aerial parts of G. thwaitesii led only to the isolation of the known flavonoids myricetin 4'-O-methyl ether-3-O-alpha-L-rhamnopyranoside (mearnsitrin) and myricetin-3-O-methyl ether (annulatin), together with the triterpenes friedelinol, friedelin and betulinic acid. All compounds were identified by spectroscopic analysis and, for known compounds, by comparison with published data.


Assuntos
Flavonoides/isolamento & purificação , Magnoliopsida/química , Flavonoides/química , Estrutura Molecular , Especificidade da Espécie , Análise Espectral
17.
Phytochemistry ; 52(3): 465-72, 1999 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-10501028

RESUMO

Three new partially acetylated derivatives of 1-O-dodecanyl-alpha-L- rhamnopyranosyl-(1-->3)-alpha-L-rhamnopyranosyl-(1-->3)-alpha-L- rhamnopyranoside and three partially acetylated derivatives of 1-O-dodecanyl-alpha-L-rhamnopyranosyl-(1-->3)- alpha-L-rhamnopyranosyl-(1-->3)-alpha-L-rhamnopyranosyl-(1-->4)- alpha-L-rhamnopyranoside, one of them new, have been isolated from the mature leaves of Cleistopholis patens (Annonaceae). Their structures, elucidated by using COSY, COSY-LR, TOCSY and FAB mass spectrometry, have been characterised as cleistrioside-2, -3, -4 and cleistetroside-1, -2 and -6. From the same source, shikimic acid was also isolated.


Assuntos
Glicosídeos/isolamento & purificação , Plantas/química , Acetilação , Configuração de Carboidratos , Sequência de Carboidratos , Éteres , Glicosídeos/química , Espectroscopia de Ressonância Magnética , Dados de Sequência Molecular , Ramnose/química , Espectrometria de Massas de Bombardeamento Rápido de Átomos
18.
J Ethnopharmacol ; 67(2): 197-202, 1999 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-10619384

RESUMO

In addition to the previously isolated phenylpropanoid glycosides verbascoside 1, forsythoside B 2, arenarioside 3 and ballotetroside 4, another four compounds were isolated from generative aerial parts of Ballota nigra: three phenylpropanoid glycosides, alyssonoside 5, lavandulifolioside 6 and angoroside A 7 and a non-glycosidic derivative (+)-(E)-caffeoyl-L-malic acid 8. The antibacterial activity of the five major compounds (1-4 and 8) was tested against gram-positive and gram-negative bacteria. Three of them (1-3) exhibited a moderate antimicrobial activity against Proteus mirabilis and Staphylococcus aureus including one methicillin-resistant strain.


Assuntos
Antibacterianos/farmacologia , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Proteus mirabilis/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Relação Dose-Resposta a Droga , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Fenóis/isolamento & purificação , Proteus mirabilis/isolamento & purificação , Staphylococcus aureus/isolamento & purificação , Relação Estrutura-Atividade
19.
Ann Pharm Fr ; 56(1): 31-5, 1998.
Artigo em Francês | MEDLINE | ID: mdl-9770033

RESUMO

A preliminary survey of the botanical characters of the species Ballota nigra and of its subspecies is reported. Phytochemical investigation of the flowered aerial parts led us to isolation and structural elucidation of one diterpene (13-hydroxyballonigrinolide) and four phenylpropanoid glycosides reported for the first time from the genus Ballota: verbascoside, forsythoside B, arenarioside and ballotetroside. These compounds appear to be characteristic of this species and could be used for the standardization of the drug. Moreover, the four phenylpropanoid glycosides isolated could justify the use of Ballota nigra as a neurosedative drug.


Assuntos
Diterpenos/análise , Fenilpropionatos/análise , Plantas Medicinais/química , Sequência de Carboidratos , Dados de Sequência Molecular
20.
Eur J Obstet Gynecol Reprod Biol ; 79(2): 145-8, 1998 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-9720832

RESUMO

OBJECTIVES: To determine the effectiveness of a 6-month course of nafarelin in the treatment of stage III-IV endometriosis and to determine if pre-operative use of nafarelin facilitates surgery. DESIGN: Prospective, multicenter, clinical trial. SETTING: Eight university hospitals and two private practice institutions in France. PATIENTS: Fifty-five patients with stage III and IV endometriosis. Two were excluded. INTERVENTIONS: The severity of endometriosis was assessed at the time of laparoscopy and patients were randomized to have either laparosopic surgery at that time following 6 months of nafarelin therapy (n=28), or laparoscopic surgery following 6 months of nafarelin therapy (n=25). All had 200 microg intranasal nafarelin twice a day for 6 months and a second look laparoscopy. MAIN OUTCOME MEASURE: Clinical efficacy, tolerance to the treatment. RESULTS: Efficacy and tolerance to the treatment were the same in both groups. AFS scores compared on both laparoscopies were significantly better if nafarelin was given prior to surgery (P=0.007). CONCLUSIONS: This preliminary study shows that in cases of combined medico-surgical treatment for stage III-IV endometriosis, preoperative medical treatment with GnRH-a gives a better AFS score improvement, but no conclusion was possible whether preoperative treatment facilitates surgery.


Assuntos
Endometriose/tratamento farmacológico , Hormônios/uso terapêutico , Nafarelina/uso terapêutico , Adulto , Método Duplo-Cego , Feminino , Humanos , Laparoscopia , Nafarelina/efeitos adversos , Estudos Prospectivos
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