Conus regius is a marine venomous mollusk of the Conus genus that captures its prey by injecting a rich cocktail of bioactive disulfide bond rich peptides called conotoxins. These peptides selectively target a broad range of ion channels, membrane receptors, transporters, and enzymes, making them valuable pharmacological tools and potential drug leads. C. regius-derived conotoxins are particularly attractive due to their marked potency and selectivity against specific nicotinic acetylcholine receptor subtypes, whose signalling is involved in pain, cognitive disorders, drug addiction, and cancer. However, the species-specific differences in sensitivity and the low stability and bioavailability of these conotoxins limit their clinical development as novel therapeutic agents for these disorders. Here, we give an overview of the main pharmacological features of the C. regius-derived conotoxins described so far, focusing on the molecular mechanisms underlying their potential therapeutic effects. Additionally, we describe adoptable chemical engineering solutions to improve their pharmacological properties for future potential clinical translation. 相似文献
The antinociceptive and anti-inflammatory activity of caulerpin was investigated. This bisindole alkaloid was isolated from the lipoid extract of Caulerpa racemosa and its structure was identified by spectroscopic methods, including IR and NMR techniques. The pharmacological assays used were the writhing and the hot plate tests, the formalin-induced pain, the capsaicin-induced ear edema and the carrageenan-induced peritonitis. Caulerpin was given orally at a concentration of 100 μmol/kg. In the abdominal constriction test caulerpin showed reduction in the acetic acid-induced nociception at 0.0945 μmol (0.0103–1.0984) and for dypirone it was 0.0426 μmol (0.0092–0.1972). In the hot plate test in vivo the inhibition of nociception by caulerpin (100 μmol/kg, p.o.) was also favorable. This result suggests that this compound exhibits a central activity, without changing the motor activity (seen in the rotarod test). Caulerpin (100 μmol/kg, p.o.) reduced the formalin effects in both phases by 35.4% and 45.6%, respectively. The possible anti-inflammatory activity observed in the second phase in the formalin test of caulerpin (100 μmol/kg, p.o.) was confirmed on the capsaicin-induced ear edema model, where an inhibition of 55.8% was presented. Indeed, it was also observed in the carrageenan-induced peritonitis that caulerpin (100 μmol/kg, p.o.) exhibited anti-inflammatory activity, reducing significantly the number of recruit cells by 48.3%. Pharmacological studies are continuing in order to characterize the mechanism(s) responsible for the antinociceptive and anti-inflammatory actions and also to identify other active principles present in Caulerpa racemosa. 相似文献
Abstract 1. Carcass cuts, chemical composition, colour, textural parameters, fatty acid and amino acid profiles, macro- and micromineral content and sensory properties of breast and drumstick meat from 10 month old common pheasant produced in an extensive rearing system were analysed.
2. Breast muscle was characterised by a high concentration of protein (254 g/kg), low content of intramuscular fat (1.3 g/kg), considerable amount of Fe-haeme (4.9 mg/kg) low shear force (1.96 kg/cm2) and hardness (4.07 kg/cm2).
3. The main drumstick characteristics were 222 g of protein/kg, 4.0 g of intramuscular fat/g and a significant higher cholesterol concentration compared to that of breast (7.7 vs. 2.9 g/kg).
4. Saturated, monounsaturated and polyunsaturated fatty acid mean values for both muscle types were approximately 34.5%, 43.3% and 24.2% of total fatty acid methyl esters, respectively, and n-3 content in breast was significantly higher (3.21% vs. 1.65%). Significant differences were found between the three tissues (breast, drumstick and subcutaneous fat).
5. Large differences in the amino acid profile between breast and drumstick were detected, especially in the non-essential fraction. The main essential amino acids were lysine and leucine, whereas aspartic and glutamic acids were the most important non-essential amino acids.
6. There were significant differences between muscle types in the mineral content with regard to iron, magnesium, sodium and zinc. Pheasant meat is a good nutritional source of iron as 100 g of drumstick may provide 23.6% of the recommended daily amount. 相似文献
Long pentraxin 3 (PTX3) is a conserved pattern-recognition secreted protein and a host-defence-related component of the humoral innate immune system. The aim of the present study was to characterize swine PTX3 (SwPTX3) protein expression in influenza virus infected pigs. First, we performed in silico studies to evaluate the cross-reactivity of PTX3 human antibodies against SwPTX3. Secondly, we used in vitro analysis to detect SwPTX3 presence in swine bone marrow dendritic cells (SwBMDC) upon stimulation with different agents by Western blot and immunofluorescence. Finally, the levels of SwPTX3 were assessed in experimental infection of pigs with different strains of influenza virus. This is a novel study where the expression of SwPTX3 was evaluated in the context of a pathogen infection. The initial characterization of SwPTX3 in influenza virus infected pigs contributes to understand the role of PTX proteins in the immune response. 相似文献
Celiac disease is a food intolerance triggered by the ingestion of gluten-containing cereals; the only therapy is a strict gluten-free diet for life. In recent years, amaranth flour has received considerable attention as an interesting source for the formulation of gluten-free products due to its high nutritional value and low content of prolamins, the toxic proteins for celiacs. The aim of this study was to characterize 40 amaranth varieties using both SDS-PAGE/immunoblotting and ELISA to assess their possible tolerance by celiac subjects. All of the amaranth samples studied showed similar binding affinities for both specific anti-gliadin antibodies and human IgAs. In most amaranth grains, the content of gluten-like proteins measured by ELISA was <20 ppm. The molecular characterization of amaranth proteins suggests that amaranth is safe for celiacs to consume. It is recommended that the most suitable amaranth varieties are those having the lowest content of proteins cross-reacting with anti-gliadin antibodies. 相似文献
Different kinds of cereal flours submitted to various technological treatments were classified on the basis of their mid-infrared spectra by pattern recognition techniques. Classification in the wavelet domain was achieved by using the wavelet packet transform for efficient pattern recognition (WPTER) algorithm, which allowed singling out the most discriminant spectral regions. Principal component analysis (PCA) on the selected features showed an effective clustering of the analyzed flours. Satisfactory classification models were obtained both on training and test samples. Furthermore, mixtures of varying composition of the studied flours were distributed in the PCA space according to their composition. 相似文献
Sustainable forest management is essential to confront the detrimental impacts of diseases on forest eco-systems.This review highlights the potential of vegetation spectroscopy in improving the feasibility of assessing forest disturbances induced by diseases in a timely and cost-effec-tive manner.The basic concepts of vegetation spectroscopy and its application in phytopathology are first outlined then the literature on the topic is discussed.Using several opti-cal sensors from leaf to landscape-level,a number of for-est diseases characterized by variable pathogenic processes have been detected,identified and quantified in many coun-try sites worldwide.Overall,these reviewed studies have pointed out the green and red regions of the visible spec-trum,the red-edge and the early near-infrared as the spectral regions most sensitive to the disease development as they are mostly related to chlorophyll changes and symptom develop-ment.Late disease conditions particularly affect the short-wave-infrared region,mostly related to water content.This review also highlights some major issues to be addressed such as the need to explore other major forest diseases and geographic areas,to further develop hyperspectral sensors for early detection and discrimination of forest disturbances,to improve devices for remote sensing,to implement long-term monitoring,and to advance algorithms for exploitation of spectral data.Achieving of these goals will enhance the capability of vegetation spectroscopy in early detection of forest stress and in managing forest diseases. 相似文献