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1.
Anti-fungal activities of two essential oils (peppermint oil and eucalyptus oil) and their main components (menthol and eucalyptol, respectively) against molds (Aspergillus niger, Penicillium chrysogenum, and Penicillium sp.) and a white-rot decay fungus (Trametes versicolor) identified from rubberwood surfaces were investigated. The broth dilution method and the agar diffusion technique were employed to determine the minimal inhibitory concentration (MIC) and the minimal fungicidal concentration (MFC) using the concentration of substances between 100 and 800 μl ml?1. Inhibitory effects of essential oils and their main components at the MICs against mold growth, fungal decay, and termite attack on rubberwood were further examined by means of the dip treatment method. It was found that MFC values against molds for all treatments examined were about 50–100 μl ml?1 higher than MIC values. Peppermint oil and menthol exhibited high fungistatic and fungicidal activities, with MICs of 300 μl ml?1 and 350 μl ml?1, respectively, against the test molds and the decay fungus. Eucalyptus oil and eucalyptol were also effective against these microbes but at higher concentrations of 600 μl ml?1 and 500 μl ml?1, respectively. Only peppermint oil at the MIC was capable of providing a complete protection from mold growth on rubberwood for up to 12 weeks at storage conditions of 25 °C and 100% RH. Both peppermint oil and eucalyptus oil at the MICs showed moderate resistance to fungal decay and high resistance to termite attack.  相似文献   
2.
Fibroblast growth factor 21 (FGF21) is a promising drug candidate for the treatment of type 2 diabetes. However, the use of wild type native FGF21 is challenging due to several limitations. Among these are its short half-life, its susceptibility to in vivo proteolytic degradation and its propensity to in vitro aggregation. We here describe a rationale-based protein engineering approach to generate a potent long-acting FGF21 analog with improved resistance to proteolysis and aggregation. A recombinant Fc-FGF21 fusion protein was constructed by fusing the Fc domain of human IgG1 to the N-terminus of human mature FGF21 via a linker peptide. The Fc positioned at the N-terminus was determined to be superior to the C-terminus as the N-terminal Fc fusion retained the βKlotho binding affinity and the in vitro and in vivo potency similar to native FGF21. Two specific point mutations were introduced into FGF21. The leucine to arginine substitution at position 98 (L98R) suppressed FGF21 aggregation at high concentrations and elevated temperatures. The proline to glycine replacement at position 171 (P171G) eliminated a site-specific proteolytic cleavage of FGF21 identified in mice and cynomolgus monkeys. The derived Fc-FGF21(RG) molecule demonstrated a significantly improved circulating half-life while maintaining the in vitro activity similar to that of wild type protein. The half-life of Fc-FGF21(RG) was 11 h in mice and 30 h in monkeys as compared to 1-2 h for native FGF21 or Fc-FGF21 wild type. A single administration of Fc-FGF21(RG) in diabetic mice resulted in a sustained reduction in blood glucose levels and body weight gains up to 5-7 days, whereas the efficacy of FGF21 or Fc-FGF21 lasted only for 1 day. In summary, we engineered a potent and efficacious long-acting FGF21 analog with a favorable pharmaceutical property for potential clinical development.  相似文献   
3.
Few basidiomycetes are known to have a coelomycete anamorph. The partial SSU and LSU of nu-rDNA of three coelomycete genera (Chaetospermum, Giulia, Mycotribulus) were sequenced to determine their phylogenetic relationship. M. mirabilis was well placed in the Physalacriaceae, Agaricales, whereas G. tenuis clusters with the Corticiaceae, Corticiales. C. camelliae and C. artocarpi form a close relationship with the Sebacinaceae, Sebacinales. Although morphologically these coelomycetes are pycnidial and with appendaged conidia, they show no consistency in their phylogenetic relationship, belonging to disparate major taxonomic groups with putative teleomorphs in the Agaricales, Corticiales and Sebacinales. Further molecular studies of coelomycetes may be rewarding to evaluate their phylogenetic affinities.  相似文献   
4.
The antifungal activities of cinnamon oil, clove oil, anise oil, and peppermint oil, and their main components (cinnamaldehyde, eugenol, trans-anethole, and menthol, respectively) against molds identified from areca palm leaf sheath (Mucor dimorphosporus, Penicillium sp., Aspergillus niger, and Rhizopus sp.) were investigated. An agar dilution method was employed to determine the minimum inhibitory concentration (MIC) of essential oils and their main components. Zone inhibition tests and the inhibitory effect of the leaf sheath dip-treated with essential oils against those molds were examined. Major components of essential oils on the leaf sheath during storage were quantified by gas chromatography analysis. The MIC values of essential oils on agar and on the leaf sheath were identical. With an MIC of 50 ??g ml−1, cinnamon oil had the strongest inhibitory effect. At their MICs the oils were capable of providing protection against mold growth on the leaf sheath for at least 12 weeks during storage at 25 °C and 100% RH. Scanning electron microscope examination showed that essential oils prevented spore germination. Except for menthol in peppermint oil, the main components of the essential oils, which were fairly stable over the storage period, largely contributed to the antifungal activity.  相似文献   
5.
The insecticidal activity of Bacillus thuringiensis (Bt) Cry toxins involves toxin stabilization, oligomerization, passage across the peritrophic membrane (PM), binding to midgut receptors and pore-formation. The residues Arg-158 and Tyr-170 have been shown to be crucial for the toxicity of Bt Cry4Ba. We characterized the biological function of these residues. In mosquito larvae, the mutants R158A/E/Q (R158) could hardly penetrate the PM due to a significantly reduced ability to alter PM permeability; the mutant Y170A, however, could pass through the PM, but degraded in the space between the PM and the midgut epithelium. Further characterization by oligomerization demonstrated that Arg-158 mutants failed to form correctly sized high-molecular weight oligomers. This is the first report that Arg-158 plays a role in the formation of Cry4Ba oligomers, which are essential for toxin passage across the PM. Tyr-170, meanwhile, is involved in toxin stabilization in the toxic mechanism of Cry4Ba in mosquito larvae. [BMB Reports 2014; 47(10): 546-551]  相似文献   
6.
Yam (Dioscorea esculenta) starch was modified by carboxymethylation. The effect of reaction parameters, amount of sodium hydroxide (NaOH), amount of sodium monochloroacetate (SMCA), and reaction time on the degree of substitution (DS) of carboxymethyl yam starch (CMS), was studied using the Box–Behnken experimental design. Physicochemical and potency to be a tablet disintegrant of CMS were evaluated. CMS with DS in the range of 0.08–0.19 were obtained. The results from regression analysis indicated that the most important factor in controlling DS was the amount of NaOH followed by SMCA content and reaction time. However, high concentration of NaOH and SMCA lowered the DS. The optimal conditions to achieve the highest DS (0.19) were found to be at molar ratios of NaOH and SMCA to anhydroglucose unit of 1.80 and 2.35, respectively, and with the reaction time of 4.8 h. The swelling power and viscosity of CMS increased with an increase in the degree of modification. CMS showed satisfying tablet disintegrant properties. The tablets containing 1.0–4.0 % CMS disintegrated faster than 5 min. Hence carboxymethyl yam starch can be used as an excellent tablet disintegrant in low concentration.  相似文献   
7.
Thalassemic patients often exhibit high levels of oxidative stress and iron overload, which can lead to hazardous complications. Curcuminoids, extracted from the spice turmeric, are known to have antioxidant and iron-chelating properties and have been proposed as a potential upstream therapy of thalassemia. Here we have applied proteomic techniques to study the protein profile and oxidative damage in the plasma of β-thalassemia/Hb E patients before and after treatment with curcuminoids. In this study, 10 β-thalassemia/Hb E patients were treated with 500 mg curcuminoids daily for 12 months. The plasma protein profile and protein carbonyl content were determined at baseline, 6 and 12 months using two-dimensional fluorescence difference gel electrophoresis and carbonyl immunoblotting, respectively. Other hematological, clinical, and biochemical parameters were also analyzed. Twenty-six spots, identified as coagulation factors and proteins involved in iron homeostasis, showed significantly decreased intensity in thalassemic plasma, compared to those of normal subjects. Treatment with curcuminoids up-regulated the plasma levels of these proteins and reduced their oxidative damage. Serum non-transferrin bound iron, platelet factor-3 like activity, oxidative stress parameters and antioxidant enzymes were also improved after curcuminoids treatment. This study is the first proteomic study of plasma in the thalassemic state and also shows the ameliorating role of curcuminoids towards oxidative stress and iron overload in the plasma proteome.  相似文献   
8.
9.
The antifungal activities of anise oil, lime oil, and tangerine oil against molds identified from rubberwood surfaces (Aspergillus niger, Penicillium chrysogenum, and Penicillium sp.) were investigated. The broth dilution method was employed to determine the minimal inhibitory concentration (MIC) and minimal fungicidal concentration (MFC) using the concentration of essential oils between 20 and 200 μl ml−1. Inhibitory effects of the essential oils against those molds on rubberwood were also examined by means of the dip treatment and vacuum impregnation treatment. It was found that the MIC and MFC values for each treatment on agar were identical for all conditions examined. Anise oil was the strongest inhibitor with the MIC and MFC of 40 μl ml−1 against Penicillium sp. and A. niger, and 60 μl ml−1 against P. chrysogenum. Lime oil and tangerine oil were also effective against those molds at higher concentrations of 100–180 μl ml−1. All essential oils at the MIC and MFC provided a protection from mold growth on rubberwood for at least 12 weeks at storage conditions of 30 °C with 100% RH.  相似文献   
10.
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