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1.
《Bioorganic & medicinal chemistry》2016,24(18):4444-4451
Nowadays, AT1 receptor (AT1R) antagonists (ARBs) constitute the one of the most prevalent classes of antihypertensive drugs that modulate the renin-angiotensin system (RAS). Their main uses include also treatment of diabetic nephropathy (kidney damage due to diabetes) and congestive heart failure. Towards this direction, our study has been focused on the discovery of novel agents bearing different scaffolds which may evolve as a new class of AT1 receptor antagonists. To fulfill this aim, a combination of computational approaches and biological assays were implemented. Particularly, a pharmacophore model was established and served as a 3D search query to screen the ChEMBL15 database. The reliability and accuracy of virtual screening results were improved by using molecular docking studies. In total, 4 compounds with completely diverse chemical scaffolds from potential ARBs, were picked and tested for their binding affinity to AT1 receptor. Results revealed high nanomolar to micromolar affinity (IC50) for all the compounds. Especially, compound 4 exhibited a binding affinity of 199 nM. Molecular dynamics simulations were utilized in an effort to provide a molecular basis of their binding to AT1R in accordance to their biological activities. 相似文献
2.
T. Tomiyama 《Journal of fish biology》2013,83(5):1334-1343
Variation of scales on the blind side of Pseudopleuronectes yokohamae in relation to sex, maturity and body size was examined. Immature males often have cycloid scales, while mature males have mostly ctenoid scales. Large females also often have ctenoid scales (but with fewer spines compared with males), and small females have mostly cycloid scales. The number of spines (ctenii) on the blind‐side scale increases with body size in both sexes, indicating an ontogenetic change in scale morphology. As P. yokohamae spawn demersal eggs with males positioning themselves above the females on the ocular side, it is hypothesized that ctenoid scales on the blind side in mature males function for maintaining contact with females during spawning. 相似文献
3.
Leonard F. Liebes Howard Fleit Dorothea Zucker-Franklin Robert Silber 《Biochimica et Biophysica Acta (BBA)/General Subjects》1980,633(2):245-257
Tubulin has been purified from human blood and tonsil lymphocytes. Using gel filtration, the molecular weight of human lymphocyte tubulin was estimated to be 119 000. The proteins was shown to consist of two subunits, with molecular weights of 61 000 and 58 000 comparable to the α and β polypeptides of human brain tubulin. A partial identity reaction was observed between lymphocyte tubulin and human tubulin when tested by double immunodiffusion against a rabbit anti-human brain tubulin antibody. In the presence of GTP, the purified protein polymerized to form microtubules. Tubulin was localized to the cell's juxtacentriolar region by immunofluorescence and electron microscopy. When assayed by a colchicine-binding assay corrected for time decay, the binding affinity was 1.50 ± 0.86 · 106M?1 and a level in normal lymphocytes of 1.21 · 10?2 ± 0.79 g/g of soluble protein was determined. Since chronic lymphocytic leukemia lymphocytes have an anomalous capping behavior as well as an unusual susceptibility to colchicine toxicity, the properties and levels of tubulin were determined in these cells. Similar values were obtained for the level, decay rate, molecular weight, and Ka for colchicine as for normal lymphocytes. Chronic lymphocytic leukemia lymphocyte tubulin polymerized in a normal fashion. It thus appears that a decrease in the quantity or function of tubulin does not account for these anomalies in the chronic lymphocytic leukemia lymphocyte. 相似文献
4.
Paula C. Rodríguez-Flores David Buckley Enrique Macpherson Laure Corbari Annie Machordom 《Zoologica scripta》2020,49(3):340-356
The ecology, abundance and diversity of galatheoid squat lobsters make them an ideal group to study deep-sea diversification processes. Here, we reconstructed the evolutionary and biogeographic history of Leiogalathea, a genus of circum-tropical deep-sea squat lobsters, in order to compare patterns and processes that have affected shallow-water and deep-sea squat lobster species. We first built a multilocus phylogeny and a calibrated species tree with a relaxed clock using StarBEAST2 to reconstruct evolutionary relationships and divergence times among Leiogalathea species. We used BioGeoBEARS and a DEC model, implemented in RevBayes, to reconstruct ancestral distribution ranges and the biogeographic history of the genus. Our results showed that Leiogalathea is monophyletic and comprises four main lineages; morphological homogeneity is common within and between clades, except in one; the reconstructed ancestral range of the genus is in the Atlantic and Indian oceans (Tethys). They also revealed the divergence of the Atlantic species around 25 million years ago (Ma), intense cladogenesis 15–25 Ma and low levels of speciation over the last 5 million years (Myr). The four Leiogalathea lineages showed similar patterns of speciation: allopatric speciation followed by range expansion and subsequent stasis. Leiogalathea started diversifying during the Oligocene, likely in the Tethyan. The Atlantic lineage then split from its Indo-Pacific sister group due to vicariance driven by closure of the Tethys Seaway. The Atlantic lineage is less speciose compared with the Indo-Pacific lineages, with the Tropical Southwestern Pacific being the current centre of diversity. Leiogalathea diversification coincided with cladogenetic peaks in shallow-water genera, indicating that historical biogeographic events similarly shaped the diversification and distribution of both deep-sea and shallow-water squat lobsters. 相似文献
5.
We conducted an experiment to assess the change in foraging efficiency resulting from diet-induced morphological and behavioural plasticity in a species of freshwater, threespine stickleback (Gasterosteus sp.). Different degrees of morphological and behavioural change were induced using two prey items commonly found in the diet of this species, allowing us to estimate the relative importance of each type of plasticity. The purpose of the experiment was twofold. First, earlier work had suggested that diet variability might be an important factor in the evolution of trophic morphological plasticity in sticklebacks. The present results extend this work by revealing the adaptive significance of morphological plasticity. The current experiment also qualitatively assessed the compatibility of the time scale of morphological change with that of the natural resource variability experienced by this species. The results indicate that diet-induced plasticity improves foraging efficiency continuously for up to 72 days of prey exposure. This is probably due in part to plasticity of the external trophic morphology but our results also suggest a complex interplay between morphology and behaviour. The time scale appears to be matched to that of natural diet variability although it is possible that some traits exhibit non-labile plasticity. Our discussion highlights the important distinction between conditions favouring the evolution of labile versus non-labile plasticity. The second objective of the experiment was to determine the relative importance of morphological and behavioural plasticity. Few studies have attempted to quantify the adaptive significance of morphological plasticity and no study to our knowledge has separated the effects of morphological and behavioural plasticity. Our experiment reveals that both behavioural and morphological plasticity are important and it also suggests a dichotomy between the two: behavioural plasticity predominately affects searching efficiency whereas morphological plasticity predominately affects handling efficiency. 相似文献
6.
《Saudi Journal of Biological Sciences》2017,24(1):1-10
Uranium has been defined in material research engineering field as one of the most energetic radioactive elements in the entire Mendeleev periodic table. The manipulation of uranium needs higher theories and sophisticated apparatus even in nuclear energy extraction or in many other chemical applications. Above the nuclear exploitation level, the chemical conventional approaches used, require a higher temperature and pressure to control the destination of ionic form. However, it has been discovered later that at biological scale, the manipulation of this actinide is possible under friendly conditions. The review summarizes the relevant properties of uranium element and a brief characterization of nanoparticles, based on some structural techniques. These techniques reveal the common link between chemical approaches and biological assistance in nanoparticles. Also, those biological entities have been able to get it after reduction. Uranium is known for its ability to destroy ductile materials. So, if biological cell can really reduce uranium, then how does it work? 相似文献
7.
《Journal of morphology》2017,278(1):4-28
The laterosensory system is a mechanosensory modality involved in many aspects of fish biology and behavior. Laterosensory perception may be crucial for individual survival, especially in habitats where other sensory modalities are generally useless, such as the permanently aphotic subterranean environment. In the present study, we describe the laterosensory canal system of epigean and subterranean species of the genus Ituglanis (Siluriformes: Trichomycteridae). With seven independent colonizations of the subterranean environment in a limited geographical range coupled with a high diversity of epigean forms, the genus is an excellent model for the study of morphological specialization to hypogean life. The comparison between epigean and subterranean species reveals a trend toward reduction of the laterosensory canal system in the subterranean species, coupled with higher intraspecific variability and asymmetry. This trend is mirrored in other subterranean fishes and in species living in different confined spaces, like the interstitial environment. Therefore, we propose that the reduction of the laterosensory canal system should be regarded as a troglomorphic (= cave‐related) character for subterranean fishes. We also comment about the patterns of the laterosensory canal system in trichomycterids and use the diversity of this system among species of Ituglanis to infer phylogenetic relationships within the genus. J. Morphol. 278:4–28, 2017. ©© 2016 Wiley Periodicals,Inc. 相似文献
8.
David A. Smith John L. Glover Laurace E. Townsend Diane E. Maupin 《In vitro cellular & developmental biology. Animal》1991,27(12):914-920
Summary Myocardial cell culture methods are now well established for animal and fetal human tissue. We present here a method for harvesting
and culturing adult human atrial myocardiocytes. Cells are obtained from fresh atrial tissue normally discarded after being
removed to cannulate the right atrium during open heart surgery. The atrial tissue is minced and then digested using collagenase.
The single cell suspension is initially cultured in serum-containing growth medium, then transferred to defined medium, selective
for myocardial cell growth. The cells are characterized by immunoperoxidase stains and transmission electron microscopy. The
cultured cells stain positive for myoglobin, whereas control cultured fibroblasts and endothelial cells do not. Electron microscopy
shows the presence of numerous myofibrils, Z-bodies, pleomorphic mitochondria, and secretory granules. The chronological age
of the donor was an important factor in culturing the adult tissue, the younger tissue correlated with a higher success rate.
This method provides a means for in vitro study of human adult myocardial cells and provides guidelines for appropriate atrial
tissue to use. 相似文献
9.
Rosalina Pomés Concepción Gil M.D. Cabetas César Nombela 《FEMS microbiology letters》1987,48(1-2):255-259
Abstract Colonies of Candida albicans wild-type strain 1001 were white and glossy, and this character was rather stably maintained. In contrast, 2 benomyl (methyl benzimidazole-2-yl-carbamate)-induced mutant strains, B17 and B14, that grew as long filamentous forms and displayed a rough-wrinkled colonial phenotype, switched to other colonial morphologies at significant frequencies. Clonal populations of B17 segregated smooth or sectored (rough/smooth) colonies at a frequency of 1.85%, when plated in nutrient-agar. Strains derived from these rough or smooth segregants switched back to one or the other phenotype at similar frequencies. Colonial variability in C. albicans B14 was not restricted to spontaneous switching from rough to smooth or vice versa, but eventually other types of variants, characterized as 'wavy' and 'fuzzy' were obtained, and shown to have their own capacity to switch. Smooth variants, derived from B14, were essentiallt unicellular, whereas fuzzy strains consisted only of long thin filaments, wavy and rough clones apparently being intermediate in their degree of filamentation. It is concluded that the capacity for colonial variation shown to exist in natural isolates could be activated by benomyl in others, such as 1001, which are quite stable and do not switch colonial morphology spontaneously. 相似文献
10.
F. J. NEIRA J. S. BRADLEY I. C. POTTER F.L.S. R. W. HILLIARD 《Zoological Journal of the Linnean Society》1988,92(4):383-408
Larvae of all three southern hemisphere anadromous parasitic lampreys were collected from rivers in Australia, New Zealand and South America. Body intervals were measured, trunk myomeres counted and the frequency of pigmentation in different body regions recorded. Morphometric data were subjected to multiple group principal components analysis (MGPCA) which took into account changes during growth. The components (together with myomere counts) and the pigmentation data were both subjected to discriminant analysis. Ordination and rank correlation tests revealed no evidence for either latitudinal clines or a continuum of circumpolar change amongst larval lamprey populations. Clustering of population centroids clearly distinguished between Mordacia lapicida (Gray) from Chile and M. mordax (Richardson) from south-eastern Australia. Populations of Geotria australis Gray divided into groups representing three geographical regions, namely Argentina, Chile and Australasia (Western Australia, Tasmania and New Zealand). Ammocoetes from Argentina were the most divergent, possessing a more posterior cloaca, taller dorsal fins, a greater gap between dorsal fins, and distinctive pigmentation on the head and caudal fin. Within the Australasian group, Western Australian and New Zealand populations clustered closer than either did with those from Tasmania. The cluster analyses for larval populations of G. australis suggest that, during their marine trophic phase, the adults of this species originating from Argentinian and Chilean rivers follow different migratory routes, whereas those from Western Australia, New Zealand and, to a lesser extent, Tasmania intermix. 相似文献