968 resultados para diterpene esters
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"Date Declassified:October 27, 1955."
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Mode of access: Internet.
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Mode of access: Internet.
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The biosynthetic origins of the dichloroimine group in the stylotellanes A and B 1,2 have been investigated by incorporation of [C-14]-labeled farnesyl isocyanide 7 and farnesyl isothiocyanate 3 into the sponge Stylotella aurantium. (C) 2002 Elsevier Science Ltd. All rights reserled.
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A total of 160 samples of 20 Australian-sourced feed ingredients of plant origin for pigs and poultry was analysed for total phosphorus and phytate-phosphorus contents and endogenous phytase activity. The majority of total P was present as phytate-phosphorus, and these concentrations were significantly correlated in 9 feed ingredients. The endogenous phytase activity in tested feed ingredients was negligible other than for wheat, its by-products and barley. Phytate-phosphorus was determined by a standard 'ferric chloride precipitation' method, which was satisfactory for individual feed ingredients, with the exception of lupins and faba beans. It appears that phytate is more difficult to extract from these two feedstuffs, possibly because of the affinity of phytate for protein. Ferric chloride precipitation methods are not suitable for phytate-phosphorus determinations of complete feed samples containing other sources of phosphorus, which is a distinct limitation. A lesser limitation is that these methods cannot distinguish between the various esters of myo-inositol phosphate present. Given the variation of phytate contents within ingredients, particularly wheat, the desirability of determining dietary substrate levels is emphasised to take full advantage of including exogenous phytases in pig and poultry diets to reduce phosphorus excretion and abate phosphorus pollution.
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Options for skin cancer treatment currently include surgery, radiotherapy, topical chemotherapy, cryosurgery, curettage, and electrodes-sication. Although effective, surgery is costly and unsuitable for certain patients. Radiotherapy can leave a poor cosmetic effect, and current chemotherapy is limited by low cure rates and extended treatment schedules. Here, we describe the preclinical activity of a novel topical chemotherapeutic agent for the treatment of skin cancer, 3-ingenyl angelate (PEP005), a hydrophobic diterpene ester isolated from the plant Euphorbia peplus. Three daily topical applications of 42 nmol (18 mug) of PEP005 cured a series of s.c. mouse tumors (B16 melanoma, LK2 UV-induced squamous cell carcinoma, and Lewis lung carcinoma; it = >14 tumors/group) and human tumors (DO4 melanoma, HeLa cervical carcinoma, and PC3 and DU145 prostate carcinoma; it = >4 tumors/group) previously established (5-10 mm(3)) on C57BL/6 or Fox1(nu) mice. The treatment produced a mild, short-term erythema and eschar formation but, ultimately, resulted in excellent skin cosmesis. The LD90 for PEP005 for a panel of tumor cell lines was 180-220 muM. Electron microscopy showed that treatment with PEP005 both ill vitro (230 tot) and ill vivo (42 nmol) rapidly caused swelling of mitochondria and cell death by primary necrosis. Cr-51 release, uptake of propidium iodide, and staining with the mitochondria dye JC1, revealed that PEP005 (230 muM) treatment of tumor cells ill vitro resulted in a rapid plasma membrane perturbation and loss of mitochondrial membrane potential. PEP005 thus emerges as a new topical anti-skin cancer agent that has a novel mode of action involving plasma membrane and mitochondrial disruption and primary necrosis, ultimately resulting in an excellent cosmetic outcome.
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Elevated extracellular concentrations of the neurotransmitter glutamate are neurotoxic and directly contribute to CNS damage as a result of ischemic pathologies. However, the main contributors to this uncontrolled rise in glutamate are still unconfirmed. It has been reported that the reversal of high-affinity glutamate transporters is a significant contributing factor. Conversely, it has also Peen observed that these transporters continue to take up glutamate, albeit at a reduced saturation concentration, under ischemic conditions. We sought to determine whether glutamate transporters continue to remove glutamate from the extracellular space under ischemic conditions by pharmacologically modulating the activity of high-affinity retinal glutamate transporters during simulated ischemia in vitro. Retinal glutamate transporter activity was significantly reduced under these ischemic conditions. The suppression of retinal glutamate transporter activity, with the protein kinase C inhibitor chelerythrine, significantly reduced ischemic glutamate uptake and enhanced retinal neurodegeneration. These findings imply a limited but protective role for retinal glutamate transporters under certain ischemic conditions, suggesting that pharmacological enhancement of high-affinity glutamate transporter activity may reduce tissue damage and loss of function resulting from toxic extracellular glutamate concentrations. (C) 2004 Wiley-Liss, Inc.
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As part of a 4-year project to study phenolic compounds in tea shoots over the growing seasons and during black tea processing in Australia, an HPLC method was developed and optimised for the identification and quantification of phenolic compounds, mainly flavanols and phenolic acids, in fresh tea shoots. Methanol proved to be the most suitable solvent for extracting the phenolic compounds, compared with chloroform, ethyl acetate and water. Immediate analysis, by HPLC, of the methanol extract showed higher separation efficiency than analyses after being dried and redissolved. This method exhibited good repeatability (CV 3-9%) and recovery rate (88-116%). Epigallocatechin gallate alone constituted up to 115 mg/g, on a dry basis, in the single sample of Australian fresh tea shoots examined. Four catechins (catechin, gallocatechin, epicatechin and epigallocatechin) and six catechin gallates (epigallocatechin gallate, catechin gallate, epicatechin gallate, gallocatechin gallate, epicatechin digallate and epigallocatechin digallate) have been identified and quantified by this HPLC method. In addition, two major tea alkaloids, caffeine and theobromine, have been quantified, while five flavonol glycosides and six phenolic acids, including quinic acids and esters, were identified and quantified. (C) 2003 Elsevier Ltd. All rights reserved.