Hydrophobic binding of phenoxyacetic and phenylacetic acids to horseradish peroxidase and human serum albumin: structure-activity relationships

Studies of protein binding in homologous series of drugs are of great interest for drug research. Apparent binding constants of phenoxyacetic and phenylacetic acids to horseradish peroxidase and to human serum albumin are evaluated by NMR studies and an optical method. These constants are good parameters to describe hydrophobic interactions, and the results are in a good agreement with our protein binding model described previously.     

Insects as a model system for aging studies

As the human lifespan has increased dramatically in recent decades, the amount of aging research has correspondingly increased. To investigate mechanisms of aging, an efficient model system is required. Although mammalian animal models are essential for aging studies, they are sometimes inappropriate due to their long lifespans and high maintenance costs. In this regard, insects can be effective alternative model systems for aging studies, as insects have a relatively short lifespan and cost less to maintain. Many species of insects have been used as model systems for aging studies, especially fruit flies, silkworm moths and several social insects. Fruit flies are most commonly used for aging studies due to the wide availability of abundant resources such as mutant stocks, databases and genetic tools. Silkworm moths are also good tools for studying aging at the tissue level due to their relatively large size. Last, social insects such as ants and bees are good for investigating lifespan determinants, as their lifespans significantly differ according to caste despite a constant genotype among the population. In this review, we discuss the current status and future prospects of aging research using insect model systems.     

Dendroclimatology in Kazakhstan

We have reviewed 43 studies related to dendroclimatology in Kazakhstan, and additionally 13 studies related to other subfields of dendrochronology, which have been published during the past 40 years. This review also includes studies published in Russian, Kazakh, German and Chinese languages, which are not easily accessible to international researchers.Dendroclimatic studies in Kazakhstan began back in the days of the Soviet Union and were actively conducted in the southern and northern parts of the country. With the collapse of the Soviet Union dendroclimatic studies stopped and resumed only 15-20 years later. Within the last 5 years, the intensity and quality of dendroclimatic studies increased significantly. Several research groups have investigated climate-growth relationships of Scots pine, Silver birch, Siberian larch, Siever’s apple and Schrenk spruce. Schrenk spruce was the most widely studied of these species, and several climatic reconstructions have been published based off their climate-growth relationships. Results of most studies on Schrenk spruce demonstrated good consistency, allowing the general patterns of climate-growth relationships to be accurately traced. Unfortunately, studies on other tree species have either lower level or represented just by one or two studies. It would therefore be premature to make any generalizations on these species at the current stage.We conclude that there is a good potential and good base for continuing dendroclimatic studies in Kazakhstan. There is a need to close several research gaps which limit our knowledge, such as chronologies’ length, application of new methods, species composition and spatial coverage. Closing these gaps let us significantly improve the dendrochronological network of Kazakhstan and provide important data for further hydrological and climate studies in Kazakhstan.     

Novel fluorescent membrane probe 2,3;5,6-bis(cyclohexyl)-BODIPY-labeled phosphatidylcholine

The novel fluorescent membrane probe, bis(cyclohexyl)-BODIPY (BCHB)-labeled phosphatidylcholine, is structurally similar to 1,3,5,7-tetramethyl-BODIPY (TMB)-labeled phosphatidylcholine. Formally, BCHB and TMB have similar systems of conjugated bonds; however, spectral properties of the probes are notably different. BCHB and TMB have a perfect spectral overlap. The fact makes BCHB a good FRET acceptor for TMB. Thus, the pair of phosphatidylcholines labeled with BCHB and TMB is a good tool for FRET-based membrane studies, e.g. lipid transfer studies.     

Preface: Ostracoda and the four pillars of evolutionary wisdom

Morphology, palaeontology, genetics and ecology are the main scientific domains contributing theories, concepts and new data to evolutionary biology. Ostracods are potentially very good model organisms for evolutionary studies because they combine an excellent fossil record with a wide extant distribution and, therefore, allow studies on both patterns and processes leading to extant diversity. This preface provides an overview of the 15 contributions to the present volume and concludes that this set of papers supports the claim that ostracod studies are situated in all main evolutionary domains.     

Screening of Indian plants for biological activity: Part XVI

Alcoholic extracts of 288 of plant materials from 199 plant species have been tested for various biological activities including chemotherapeutic and pharmacological screening. Biological activities, ranging from moderate to good degree, have been observed in 61 plants extracts. Follow up studies have been carried out in these extracts and some of them have shown moderate degree of activities at this Institute. However, none of the extracts was found to be good enough for further development. Results of the present studies, along with chemical investigations on different species of similar genera which were screened earlier, are also discussed.     

Valuing nature in context: the contribution of common-good approaches

We draw on a number of empirical studies undertaken in the UK to show how residents and farmers come to contest scientific approaches to valuing nature as the basis for adjudicating conflicts over protected natural areas. The findings of these studies suggest that a widening of the knowledge base on which the goals and practices of nature conservation are founded, and a more deliberative process of decision making about what nature is important locally, is required if effective conservation partnerships are to be sustained. We offer a common good approach to valuing nature as a means of addressing this problem. A common good approach is based on ethical and moral concerns about nature and expresses these values through a social and political process of consensus building. We illustrate how this common good approach can be used to prioritise issues in a Local Environment Agency Plan. When linked with a method of Stakeholder Decision Analysis this common good approach is capable of building coalitions and a measure of consensus between different interests. It achieves this through a transparent and deliberate process of debate and systematic analysis of values that makes explicit the foundation of different knowledge claims about nature.     

Benzimidazole- and benzoxazole-based inhibitors of Rho kinase

Inhibitors of Rho kinase have been developed based on two distinct scaffolds, benzimidazoles, and benzoxazoles. SAR studies and efforts to optimize the initial lead compounds are described. Novel selective inhibitors of ROCK-II with excellent potency in both enzyme and cell-based assays were obtained. These inhibitors possess good microsomal stability, low cytochrome P-450 inhibitions and good oral bioavailability.     

Molecular diversity in the context of leadlikeness: compound properties that enable effective biochemical screening

Molecular diversity is of vital importance in drug screening in general and for the discovery and development of new pharmacophores in particular. Biochemical screening is a powerful tool for pharmacophore development given understanding of the properties of a good lead compound operating in the biochemical environment. The properties of leadlikeness have evolved to accommodate the artificial conditions of a biochemical assay. Accordingly, the properties of leadlikeness that are suited for screening at protein targets biochemically are different and complementary to the properties of druglikeness used to guide the selection of good compounds studied biologically in cellular studies and animal models. The benefits of leadlikeness in the biochemical screening arena (including fragment-based screening and co-crystallization studies) are described here and recommendations are forwarded for the generation of leadlike molecular diversity. Chemically stable low molecular weight 'minimalist' compounds (or fragments) with dense heteroatom substitution and variable conformational constraint are promoted as conceptually superior compounds for biochemical screening.     

Selection, acclimation, training, and preparation of dogs for the research setting

Dogs have made and will continue to make valuable contributions as animal models in biomedical research. A comprehensive approach from time of breeding through completion of in-life usage is necessary to ensure that high-quality dog models are used in studies. This approach ensures good care and minimizes the impact of interanimal variability on experimental results. Guidance related to choosing and developing high-quality laboratory dogs and managing canine research colonies is provided in this article. Ensuring that dogs are healthy, well adapted, and cooperative involves good communication between vendors, veterinarians, care staff, and researchers to develop appropriate dog husbandry programs. These programs are designed to minimize animal stress and distress from the postweaning period through the transfer and acclimation period within the research facility. Canine socialization and training programs provided by skilled personnel, together with comprehensive veterinary health programs, can further enhance animal welfare and minimize interanimal and group variability in studies.     

Mycorrhizal symbioses: how to be seen as a good fungus

Plants continually encounter many microorganisms. Some are good, but many are bad. Two studies show how beneficial fungi tell the plant to let them in and how the fungus avoids setting off the plant's defense reaction.     

Towards a functional understanding of "good genes"

The Hamilton & Zuk hypothesis (1982) underpins our understanding of the relationship between secondary sexual characters, parasites, and immunological function. However, despite the wealth of empirical studies that attempt to address issues raised by the Hamilton & Zuk hypothesis, there have been no overt attempts to identify the "good genes" that females select or how those good genes influence the host's immune system. Behavioural ecologists have generally viewed this aspect of immunity as a black box. In this review we propose candidate good genes in vertebrates, discuss their role in immune function and parasite resistance, and discuss several aspects of the assumptions that pervade studies of parasite mediated sexual selection in vertebrates. We also examine invertebrates (specifically insects) where our current knowledge of these systems suggests the patterns apparent in vertebrates are not underpinned by the same genetic mechanisms.     

Display and Communications in Reptiles: An Historical Perspective

While the analysis of displays and communication in reptileshas accelerated during the past decade, much of the informationhas been anecdotal and gathered without focus. There are exceptions.In a few studies releasers and releasing mechanisms were analyzed.However, to date our understanding of the communication repertoireof even the best studied reptile, the lizard Anohs carolinensisis fragmentary. In a few other studies the quantitative natureof variation of particular display movements or acts has beenelucidated but there are many more acts for all species whosequantitative and qualitative variations are unknown. Only avery few investigators have postulated adaptive reasons forobserved patterns of variation between populations or species.There are no good tests of these hypotheses. Both broad comparativestudies that rigorously measure environmental variables andin-depth studies on single populations are badly needed to relievethis deficiency. Despite the lack of good data, recent techniques, some fromstudies with objectives entirely different from that of studyingbehavior, are likely to further our knowledge significantly.The projection image technique will enable the rigorous dissectionof the signal value of various visually oriented acts. For thestudy of adaptive significance of display variation within alizard population is presented an in-depth empirical approachthat utilizes demographic analysis, behavioral observation andfield experimentation.     

Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists

Structure-activity relationship studies leading to the discovery of novel mGlu5 receptor antagonists are described. These compounds show high in vitro potency, have good in vivo receptor occupancy, and a reasonable intravenous pharmacokinetic profile.     

From disease to development to cell biology and back

Nowadays, the focus of developmental studies is shifting away from formal models of developmental pathways that are characterised by flow charts of controlling factors connected by arrows, to mechanistic models that explain developmental processes at the cellular level. Surprisingly, this shift towards a cellular view of developmental biology is occurring simultaneously across a range of model organisms. One consequence of taking such a cell biological view of development is that many model organisms are now becoming good models for studies of human disease and therapy.     

Gene delivery into primary cerebral cortical neurons by lentiviral vector

Several studies have shown the ability of human immunodeficiency virus type 1 (HIV-1)-based lentiviral vectors to infect nondividing brain neurons. We are the first to show that primary embryonic cerebral cortical neurons can be efficiently transduced by an HIV-1-based lentiviral vector encoding enhanced green fluorescent protein (EGFP). We also describe the optimal conditions for the transduction of cerebral cortical neurons with lentiviral vectors, and the kinetic process of infection. The percentage of cells expressing EGFP is a function of the time in culture and virus dose. The highest percentage of EGFP-expression achieved was 46.77% at 4 days in vitro (DIV) with a multiplicity of infection (m.o.i.) of 20. The results show that lentiviral vectors are not only good prospects for in vivo gene delivery, but are also good candidates for in vitro studies of the function of gene products in primary cerebral cortical neurons.     

Long-term follow-up studies after homograft replacement of the mitral valve

Follow-up studies on 132 patients who have received fresh aortic homograft replacement of the mitral valve since May 1967 indicate good long-term function of the valve. Clinically the majority of patients are greatly improved and are free from the risks of long-term anticoagulant therapy. Hemodynamic studies performed on 13 patients at 25 to 41 months postoperatively showed a significant decrease in left atrial and pulmonary artery pressures with a small increase in cardiac output. Late deterioration of the homograft produced severe insufficiency in four cases and organic stenosis in two cases. Reasons for isolated deterioration are suggested.     

A technique to obtain fibroblast cells from skin biopsies of living bats (Chiroptera) for cytogenetic studies

We developed a procedure to obtain fibroblasts from bat skin. A small fragment of the ear is removed under ether anesthesia. This material is then cut up into small pieces and cultured in standard cell culture media. Very good quality chromosome preparations for cytogenetic studies are obtained in about three weeks. Secondary cultures can be used for other biological studies. This procedure does not require sacrificing the animals.     

Preparation and characterization of novel chitosan/gelatin membranes using chitosan hydrogel

Chitin and chitosan are novel biomaterials. The novel chitosan/gelatin membranes were prepared using the suspension of chitosan hydrogel mixed with gelatin. The prepared chitosan/gelatin membranes were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), mechanical, swelling, and thermal studies. The morphology of these chitosan/gelatin membranes was found to be very smooth and homogeneous. The XRD studies showed that the chitosan/gelatin membranes have good compatibility and interaction between the chitosan and gelatin. The stress and elongation of chitosan/gelatin membranes on wet condition showed excellent when the mixture ratio of gelatin was 0.50. The prepared chitosan/gelatin membranes showed good swelling, mechanical and thermal properties. Cell adhesion studies were also carried out using human MG-63 osteoblast-like cells. The cells incubated with chitosan/gelatin membranes for 24 h were capable of forming cell adhesion. Thus the prepared chitosan/gelatin membranes are bioactive and are suitable for cell adhesion suggesting that these membranes can be used for tissue-engineering applications. Therefore, these novel chitosan/gelatin membranes are useful for biomedical applications.