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21.
Quinuclidinyl Benzilate Binding in House Fly Heads and Rat Brain 总被引:4,自引:3,他引:1
Abstract: House fly heads contain a binding site for 3-quinuclidinyl benzilate (QNB) that is quite similar in pharmacology to the muscarinic acetylcholine receptor of vertebrate tissues. The house fly site binds [3 H]QNB reversibly with a K d of 260 PM and Bmax of 1 pmol/g of heads from direct binding measurements. The Kd calculated from the ratio of the dissociation rate constant (2 × 10−4 sec−1 ) to the association rate constant (2.5 × 106 M−1 Sec−1 ) was 80 pM. The house fly site binds (-)quinuclidinyl benzilate preferentially, as do classic muscarinic receptors. The binding is also sensitive to other muscarinic antagonists and agonists. Nicotinic and other drugs are no more effective on the house fly site than they are on the rat brain muscarinic receptor itself. These binding studies suggest that the house fly QNB binding site is a muscarinic receptor. 相似文献
22.
Most tethered adult crickets (Gryllus bimaculatus) assumed flight postures with or without flapping their wings in a windstream. Nymphal crickets (sixth and seventh, i.e. final, instars) also displayed the flight posture in spite of the incompleteness of wing development. These adult nymphal crickets rolled their heads towards the light source in response to unequal illumination of the compound eyes only while maintaining the flight posture. The amphtude of the head rolling movements was proportional to the change of light position up to 120°C, and independent of the light intensity if the duration was longer than 1 sec. The unequal illumination could also induce a transient increase in discharge frequency of the wing muscles on both sides, a decrease in wing beat amplitude of the ipsilateral wing on the illuminated side, and bending movements of the legs and abdomen towards the light. Cutting either of the nerve connectives at any level between the subosophageal and metathoracic ganglia did not affect the response of either the head or the abdomen to illumination. These results are discussed in relation to the steering mechanism associated with the dorsal light reaction. 相似文献
23.
The dielectric dispersion in the MHz range of the zwitterionic dipolar phosphocholine head groups has been measured from 0–70°C for various mixtures of (DPPC) and cholesterol. The abrupt change in the derived relaxation frequency observed for pure DPPC at the gel-to-liquid crystalline phase transition at 42°C reduces to a more gradual increase of frequency with temperature as the cholesterol content is increased. In general the presence of cholesterol increases the DPPC head group mobility due to its spacing effect. Below 42°C no sudden changes in are found at 20 or 33 mol% cholesterol, where phase boundaries have been suggested from other methods. Above 42°C, however, a decrease in at cholesterol contents up to 20–30 mol% is found. This is thought to be partly due to an additional restricting effect of the cholesterol on the number of hydrocarbon chain conformations and consequently on the area occupied by the DPPC molecules. 相似文献
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Wei Huang Shengyang Jin Wenbo Yang Shuo Tian Chunqing Meng Huan Deng Hong Wang 《Journal of cellular and molecular medicine》2020,24(3):2169-2177
A water‐soluble polysaccharide (APP‐AW) was isolated from Agrimonia pilosa and prepared to three sulphated derivatives (S1, S2 and S3). The results showed that pre‐treatment with APP‐AW, S1, S2 and S3 each at the concentration of 50 μg/mL for 48 hours was able to prevent cytotoxicity induced by 1 μmol/L dexamethasone (Dex) in MC3T3‐E1 cells via inhibition of apoptosis, which is in line with the findings in flow cytometry analysis. Meanwhile, the decreased ALP activity, collagen content, mineralization, BMP2, Runx2, OSX and OCN protein expression in DEX‐treated MC3T3‐E1 cells were reversed by the addition of APP‐AW, S1, S2 and S3. Moreover, APP‐AW, S1, S2 and S3 rescued DEX‐induced increase of Bax, cytochrome c and caspase‐3 and decrease of Bcl‐2, Wnt3, β‐catenin and c‐Myc protein expression in MC3T3‐E1 cells. Our findings suggest that pre‐treatment with APP‐AW, S1, S2 and S3 could significantly protect MC3T3‐E1 cells against Dex‐induced cell injury via inhibiting apoptosis and activating Wnt/β‐Catenin signalling pathway, thus application of these polysaccharides may be a promising alternative strategy for steroid‐induced avascular necrosis of the femoral head (SANFH) therapy. 相似文献
26.
Hongping Yu Daoyu Zhu Pei Liu Qianhao Yang Junjie Gao Yigang Huang Yixuan Chen Youshui Gao Changqing Zhang 《Journal of cellular and molecular medicine》2020,24(8):4439-4451
Characteristic pathological changes in osteonecrosis of the femoral head (ONFH) include reduced osteogenic differentiation of bone mesenchymal stem cells (BMSCs), impaired osseous circulation and increased intramedullary adipocytes deposition. Osthole is a bioactive derivative from coumarin with a wide range of pharmacotherapeutic effects. The aim of this study was to unveil the potential protective role of osthole in alcohol‐induced ONFH. In vitro, ethanol (50 mmol/L) remarkably decreased the proliferation and osteogenic differentiation of BMSCs and impaired the proliferation and tube formation capacity of human umbilical vein endothelial cell (HUVECs), whereas it substantially promoted the adipogenic differentiation of BMSCs. However, osthole could reverse the effects of ethanol on osteogenesis via modulating Wnt/β‐catenin pathway, stimulate vasculogenesis and counteract adipogenesis. In vivo, the protective role of osthole was confirmed in the well‐constructed rat model of ethanol‐induced ONFH, demonstrated by a cascade of radiographical and pathological investigations including micro‐CT scanning, haematoxylin‐eosin staining, TdT‐mediated dUTP nick end labelling, immunohistochemical staining and fluorochrome labelling. Taken together, for the first time, osthole was demonstrated to rescue the ethanol‐induced ONFH via promoting bone formation, driving vascularization and retarding adipogenesis. 相似文献
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28.
Mark Richard McNeill Chikako van Koten Stephen Latham Goldson 《Journal of Applied Entomology》2021,145(6):587-600
Listronotus bonariensis (Kuschel) is a pest of agriculturally important graminaceous species, with mining larvae that kill the stems of the host plants. In this study, larval populations were measured in spring and summer in irrigated dairy grassland comprising Lolium perenne L. (cv. Nui) with and without the endophyte Epichloë festucae var. lolii Latch, M.J. Chr. and Samuels and Poa annua L.. Larvae were extracted from tillers taken from the swards of these two grass species and extracted from turves, and L. bonariensis population densities were estimated from tiller and turf larval counts on a m−2 basis. Over the study period, the total number of larvae and larval densities extracted from turves was on average 2× greater than indicated from tillers. In most seasons, larval densities from turves were significantly higher than those from the tillers, though there was no correlation between tiller and turf larval densities. Mean head capsule widths of larvae emerging from turf samples showed significant seasonal effects compared with tillers, while mean head capsule widths of all four instars were significantly greater when extracted from tillers compared with turves. There was a significant endophyte effect on head capsule widths of larvae collected in summer, but the effect was not consistent across instars or source. Conversely, no significant endophyte effect on head capsule width was found in spring populations from either tillers or turves. This study shows that in irrigated dairy pasture, a high proportion of L. bonariensis larvae can live externally of tillers, presumably among the organic matter around the base of grasses in irrigated dairy pasture, and that density estimates based only on tiller populations will have significantly underestimated actual numbers. Having a precise indication of larval population densities is essential when developing life tables or determining economic damage threshold levels. 相似文献
29.
BackgroundWe investigated the relationship between genetic alterations and 18F-FDG PET/CT findings in head and neck squamous cell carcinoma (HNSC).MethodsUsing mRNA-sequences of HNSC samples (480 patients) from the Cancer Genome Atlas (TCGA) portal, gene coexpression networks were constructed via a weighted correlation network analysis (WGCNA) algorithm, and their association with the tumor-to-blood signal ratio on 18F-FDG PET/CT data (21 patients) was explored. An elastic-net regression model was developed to estimate the PET tumor-to-blood ratio from the gene networks and to derive an FDG signature score (FDGSS). The FDGSS was evaluated with regard to clinical variables and general mutational profiles, as well as alterations to oncogenic signaling pathways.FindingsThe FDGSS values differed across clinical stages (p = 0.027), HPV-status (p< 0.001), and molecular subtypes of HNSC (p< 0.001). Multivariate Cox regression demonstrated that FDGSS was an independent predictor for overall (p = 0.019) and progression-free survival (p = 0.024). FDGSS positively correlated with total mutation rate (p = 0.016), aneuploidy (p < 0.001), and somatic copy number alteration scores (p < 0.001). CDKN2A in the cell cycle pathway (q = 0.014) and the TP53 gene in the TP53 pathway (q = 0.005) showed significant differences between high and low FDGSS patients.ConclusionFDGSS based on the gene coexpression network was associated with the mutational landscape of HNSC. 18F-FDG PET/CT is therefore a valuable tool for the in vivo imaging of these cancers, being able to visualize the glucose metabolism of the tumor and allow inferences to be made on the underlying genetic alterations in the tumor. 相似文献
30.
Michael Sandberg Long Bin Tan Heow Pueh Lee 《Computer methods in biomechanics and biomedical engineering》2013,16(12):684-692
AbstractIn the present study, the free fall impact test in accordance with the EN1078 standard for certification of bicycle helmets is replicated using numerical simulations. The impact scenario is simulated using an experimentally validated, patient-specific head model equipped with and without a bicycle helmet. Head accelerations and intracranial biomechanical injury metrics during the impacts are recorded. It is demonstrated that wearing the bicycle helmet during the impact reduces biomechanical injury metrics, with the biggest reduction seen in the metric for skull fracture. 相似文献