RESUMO
A review of the leaf oils of the 13 species now recognised in the genus Backhousia is presented. This review carries on from, and incorporates data from, an earlier (1995) review of the then recognised eight species. The leaf oils of two new species of Backhousia, B. gundarara and B. tetraptera are reported for the first time. B. gundarara contains a mixture of mono- and sesquiterpenes, with α-pinene (14%) and spathulenol (11%) being the main members. In B. tetraptera, the principal component of the mainly terpenoid leaf oil is myrtenyl acetate (20-40%). The review also incorporates the two species of the genus Choricarpia, which have been subsumed into Backhousia, viz. B. leptopetala and B. subargentea. Due to its history in Backhousia, Syzygium anisatum, which has been transferred out of Backhousia, is included in the review for historical reasons.
RESUMO
The transition of clinical trial data to changes in routine clinical practice is often a slow process. We describe a rapid transition of patients from one form of antiviral therapy to a modified and potentially safer version that can occur quickly when there are no financial or organisational restrictions on the prescribers.
Assuntos
Adenina/análogos & derivados , Antivirais/uso terapêutico , Infecções por HIV/tratamento farmacológico , HIV-1/efeitos dos fármacos , Tenofovir/uso terapêutico , Adenina/uso terapêutico , Alanina , Instituições de Assistência Ambulatorial , Fármacos Anti-HIV/uso terapêutico , Austrália , Humanos , Auditoria Médica , Resultado do TratamentoRESUMO
Tocopherols (commonly referred to as "vitamin E") are frequently studied antioxidants in exercise research. However, the studies are highly heterogeneous, which has resulted in contradicting opinions. The aim of this review is to identify similar studies investigating the effects of tocopherol supplementation on exercise performance and oxidative stress and to perform minimally biased qualitative comparisons and meta-analysis. The literature search and study selection were performed according to Cochrane guidelines. A 2-dimensional study execution process was developed to enable selection of similar and comparable studies. Twenty relevant studies were identified. The high variability of study designs resulted in final selection of 6 maximally relevant studies. Markers of lipid peroxidation (malondialdehyde) and muscle damage (creatine kinase) were the 2 most frequently and similarly measured variables. Meta comparison showed that tocopherol supplementation did not result in significant protection against either exercise-induced lipid peroxidation or muscle damage. The complex antioxidant nature of tocopherols and low accumulation rates in muscle tissues could underlie an absence of protective effects.
Assuntos
Antioxidantes/farmacologia , Suplementos Nutricionais , Exercício Físico/fisiologia , Estresse Oxidativo/efeitos dos fármacos , Tocoferóis/farmacologia , Vitaminas/farmacologia , HumanosRESUMO
A comprehensive profile on Butyl methoxy dibenzoylmethane, one of the most commonly used ultraviolet (UV) filters in topical sunscreen products, is prepared. This UV filter, often referred to as Avobenzone, has its main absorbance in the UVA I region of the spectrum and is susceptible to photodegradation. The profile contains the following sections: general information, use and mechanism of action, method of preparation, physical characteristics, methods of analysis, stability, and toxicity. The physical characteristics section includes the melting range, differential scanning calorimetry, partition coefficient, ionization constant, solubility, and UV, infrared, nuclear magnetic resonance ((1)H NMR and (13)C NMR) and mass spectrometry and X-ray powder diffractometry. The method of analysis section in addition to compendial identification and purity and assay methods includes thin-layer gas and high-performance liquid chromatography. The photostability and photostabilization of Butyl methoxy dibenzoylmethane, in addition to its toxicity, are also documented.
Assuntos
Alcanos/química , Chalconas/química , Protetores Solares/química , Alcanos/análise , Alcanos/farmacologia , Alcanos/toxicidade , Animais , Chalconas/análise , Chalconas/farmacologia , Chalconas/toxicidade , Estabilidade de Medicamentos , Humanos , Propiofenonas , Análise EspectralRESUMO
Ianthellamide A (1), a novel octopamine derivative, was isolated from the Australian marine sponge Ianthella quadrangulata. Compound 1 selectively inhibited the activity of kynurenine 3-hydroxylase with an IC(50) value of 1.5 µM. It also significantly increased the level of endogenous kynurenic acid in rat brain and hence has the potential as a neuroprotective agent in the treatment of neurodegenerative disorders.
Assuntos
Benzenossulfonatos/farmacologia , Inibidores Enzimáticos/farmacologia , Quinurenina 3-Mono-Oxigenase/antagonistas & inibidores , Octopamina/análogos & derivados , Poríferos/química , Animais , Concentração Inibidora 50 , Espectroscopia de Ressonância Magnética , Biologia Marinha , Octopamina/farmacologiaRESUMO
Eusynstyelamides A-C (1-3) were isolated from the Great Barrier Reef ascidian Eusynstyela latericius, together with the known metabolites homarine and trigonelline. The structures of 1-3, with relative configurations, were elucidated by interpretation of their spectroscopic data (NMR, MS, UV, IR, and CD). The NMR data of 1 were found to be virtually identical to that reported for eusynstyelamide (4), isolated from E. misakiensis, indicating that a revision of the structure of 4 is needed. Eusynstyelamides A-C exhibited inhibitory activity against neuronal nitric oxide synthase (nNOS), with IC(50) values of 41.7, 4.3, and 5.8 microM, respectively, whereas they were found to be nontoxic toward the three human tumor cell lines MCF-7 (breast), SF-268 (CNS), and H-460 (lung). Compounds 1 and 2 displayed mild inhibitory activity toward Staphylococcus aureus (IC(50) 5.6 and 6.5 mM, respectively) and mild inhibitory activity toward the C(4) plant regulatory enzyme pyruvate phosphate dikinase (PPDK) (IC(50) values of 19 and 20 mM, respectively).
Assuntos
Indóis/isolamento & purificação , Indóis/farmacologia , Óxido Nítrico Sintase Tipo I/antagonistas & inibidores , Urocordados/química , Animais , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Humanos , Indóis/química , Concentração Inibidora 50 , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Piruvato Ortofosfato Diquinase/antagonistas & inibidores , Staphylococcus aureus/efeitos dos fármacosRESUMO
A new dolabellane type diterpene 1 has been isolated through its acetate 1a. The structure of 1a was elucidated by extensive 1D and 2D NMR spectroscopy and confirmed by mass spectrometry. The structure of 1 was deduced by comparison of its NMR spectral data with those of 1a, while its relative stereochemistry was deduced by NOESY. The absolute stereochemistry of C-7 was determined by analyses of 1 separately esterified with R and S O-mandelic acids.
Assuntos
Antozoários/química , Diterpenos/isolamento & purificação , Animais , Diterpenos/química , Conformação MolecularRESUMO
The dichloromethane extract of Cespitularia erecta afforded a new verticillane diterpenoid (1) and sarcophytol A (2) by silica gel chromatography. The structure of 1 was elucidated by extensive 1D and 2D NMR spectroscopy.
Assuntos
Antozoários/química , Diterpenos/química , Animais , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Estrutura MolecularRESUMO
A new hexacyclic pyridoacridine alkaloid, nordehydrocyclodercitin (1), from an ascidian, Aplidium sp., cf. Aplidium cratiferum collected at Arab Reef, Great Barrier Reef, Australia is reported. Nordehydrocyclodercitin is structurally related to stellettamine (2) and cyclodercitin (3), which are sponge metabolites, and cycloshermilamine D (4) which was isolated from the marine tunicate Cystodytes violatinctus. The structure of nordehydrocyclodercitin was determined by interpretation of spectroscopic data, particularly those obtained from HMBC correlations, and by comparison with reported data for known related pyridoacridine alkaloids.
Assuntos
Alcaloides/isolamento & purificação , Compostos Heterocíclicos de 4 ou mais Anéis/isolamento & purificação , Urocordados/química , Alcaloides/química , Animais , Compostos Heterocíclicos de 4 ou mais Anéis/química , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Espectrometria de Massas por Ionização por ElectrosprayRESUMO
The dichloromethane extract of Xenia viridis afforded two new xenicane diterpenoids (3 and 4) by silica gel chromatography. The oxirane ring of 3 was found to be susceptible to a slow ring opening under acidic conditions to afford 5. Their structures were elucidated by extensive 1D and 2D NMR spectroscopy.
Assuntos
Antozoários/química , Diterpenos/química , Animais , Biologia MolecularRESUMO
Branched chain amino acids (BCAA), particularly leucine, have been suggested to be ergogenic for both endurance and strength/power performance. This study investigated the effects of dietary leucine supplementation on the exercise performance of outrigger canoeists. Thirteen (ten female, three male) competitive outrigger canoeists [aged 31.6 (2.2) year, VO(2max) 47.1 (2.0) ml kg(-1) min(-1)] underwent testing before and after 6-week supplementation with either capsulated L: -leucine (45 mg kg(-1) d(-1); n = 6) or placebo (cornflour; n = 7). Testing included anthropometry, 10 s upper body power and work and a row to exhaustion at 70-75% maximal aerobic power where perceived exertion (RPE), heart rate (HR) and plasma BCAA and tryptophan concentrations were assessed. Leucine supplementation resulted in significant increases in plasma leucine and total BCAA concentrations. Upper body power and work significantly increased in both groups after supplementation but power was significantly greater after leucine supplementation compared to the placebo [6.7 (0.7) v. 6.0 (0.7) W kg(-1)]. Rowing time significantly increased [77.6 (6.3)-88.3 (7.3) min] and average RPE significantly decreased [14.5 (1.5)-12.9 (1.4)] with leucine supplementation while these variables were unchanged with the placebo. Leucine supplementation had no effect on the plasma tryptophan to BCAA ratio, HR or anthropometric variables. Six weeks' dietary leucine supplementation significantly improved endurance performance and upper body power in outrigger canoeists without significant change in the plasma ratio of tryptophan to BCAA.
Assuntos
Suplementos Nutricionais , Exercício Físico/fisiologia , Leucina/farmacologia , Adulto , Aminoácidos/sangue , Aminoácidos de Cadeia Ramificada/sangue , Composição Corporal/efeitos dos fármacos , Peso Corporal/efeitos dos fármacos , Proteínas Alimentares/análise , Método Duplo-Cego , Teste de Esforço , Feminino , Frequência Cardíaca/efeitos dos fármacos , Humanos , Leucina/administração & dosagem , Leucina/sangue , Masculino , Consumo de Oxigênio/efeitos dos fármacos , Resistência Física/efeitos dos fármacos , Esforço Físico/efeitos dos fármacos , Triptofano/sangueRESUMO
Using standard WHO methodology, this study investigated the susceptibility of 4(th) instar Aedes aegypti (L) and Culex annulirostris (Skuse) larvae to three extracts from Callitris glaucophylla (J. Thompson & L. Johnson) (1: steam distillation extract, 2: liquefied refrigerant gas extract, and 3: methanol reflux extract), lambda-cyhalothrin (a synthetic pyrethroid insecticide) and fenitrothion (an organophosphorous insecticide). Cx. annulirostris was significantly more susceptible than Ae. aegypti to all tested chemicals except lambda-cyhalothrin. Responses to the three C. glaucophylla extracts were exceptional for a botanical compound: Cx. annulirostris (LC(50) = 0.23, 9.53 and 38.95 mg/L) and Ae. aegypti (LC(50) = 0.69, 5.21 and 306.43 mg/L). Both Cx. annulirostris and Ae. aegypti larvae were significantly more susceptible to lambda-cyhalothrin (LC(50) = 0.00013 and 0.00016 mg/L) than fenitrothion (LC(50) = 0.0009 and 0.004 mg/L). As expected, the pyrethroid and organophosphorous insecticides were far more potent than the crude C. glaucophylla extracts. The steam distilled extract was fractionated and the major components guaiol and citronellic acid were identified and tested. Activities for these major components were lower than observed for the distillate. Minor components include lactones such as eldanolide, and future testing of minor components may indicate the active component.
Assuntos
Aedes , InseticidasRESUMO
An investigation of a new species of sponge from the genus Suberea collected at Lihou Reef in the Coral Sea afforded lihouidine, an unprecedented cytotoxic spiro nonacyclic polyaromatic alkaloid. The structure of the alkaloid, which was racemic, was determined by a combination of 1D and 2D NMR techniques and single-crystal X-ray structural analysis.
Assuntos
Alcaloides/isolamento & purificação , Antineoplásicos/isolamento & purificação , Poríferos/química , Compostos de Espiro/isolamento & purificação , Alcaloides/química , Alcaloides/farmacologia , Animais , Antineoplásicos/química , Antineoplásicos/farmacologia , Cristalografia por Raios X , Conformação Molecular , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Oceanos e Mares , Compostos de Espiro/química , Compostos de Espiro/farmacologiaRESUMO
Melioidosis is caused by the Gram-negative bacillus Burkholderia pseudomallei. Most clinical reports of disease are from south-east Asia and northern Australia. The organism is intrinsically resistant to most commonly available antibiotics. Standard therapy includes ceftazidime either alone or in combination with co-trimoxazole. The clinical advantage in adding co-trimoxazole has never been determined; nor has the activity of newer, fourth-generation cephalosporins, such as cefepime, been studied in the treatment of this condition. BALB/c mice have been shown to represent an animal model of melioidosis. This animal model was used in this study to compare the efficacy of ceftazidime and cefepime alone or with co-trimoxazole, in the therapy of melioidosis. Antibiotic levels in the mice were determined by HPLC, and dosing was modified to keep plasma antibiotic levels at or above the MIC for the organism-antibiotic combination for a significant part of a 12 h period. Bacterial load, as determined by splenic counts, showed that ceftazidime in combination with co-trimoxazole was the most effective therapeutic option. The animal model described in this study can be used as a preliminary evaluation of therapeutic options for melioidosis.
Assuntos
Antibacterianos/uso terapêutico , Modelos Animais de Doenças , Melioidose/tratamento farmacológico , Doença Aguda , Animais , Antibacterianos/sangue , Anti-Infecciosos/sangue , Anti-Infecciosos/uso terapêutico , Cefepima , Ceftazidima/sangue , Ceftazidima/uso terapêutico , Cefalosporinas/sangue , Cefalosporinas/uso terapêutico , Quimioterapia Combinada , Injeções Intraperitoneais , Melioidose/sangue , Camundongos , Camundongos Endogâmicos BALB C , Combinação Trimetoprima e Sulfametoxazol/sangue , Combinação Trimetoprima e Sulfametoxazol/uso terapêuticoRESUMO
Three new linear cytotoxic tripeptides, virenamides A-C have been isolated from extracts of the Didemnid ascidian Diplosoma virens collected on the Great Barrier Reef, Australia. Their structures were deduced from 1D and 2D NMR spectral data and confirmed by HPLC analysis of the constituent amino acids after hydrolysis of the peptides and derivatization with 1-fluoro-2,4-dinitrophen-5-yl-L-alanine amide using Marfey's procedure.