Antiviral and Cytotoxic Activities of Ilex aquifolium Silver Queen in the Context of Chemical Profiling of Two Ilex Species
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SUBMITTER: Pachura N
PROVIDER: S-EPMC11243556 | biostudies-literature | 2024 Jul
REPOSITORIES: biostudies-literature
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Project description:Through its natural or cultivated insular population distribution, Ilex aquifolium L. is a paramount species which is exceptionally suitable for studying phenotypic variability and plasticity through the assessment of morphological, physiological, biochemical and genomic features with respect to acclimation and/or adaptation efficiency. The current study is focused on four insular populations of Ilex aquifolium from Eastern Europe (i.e., in Romania, Hungary, Serbia and Bulgaria), and presents an initial evaluation of phenotypic variability in order to conclude our research on phylogenetic relationships and phytochemical profiles, including several descriptive and quantitative morphological traits. Taken together, the data from different methods in this paper indicate that the Bulgarian and Romanian populations can be distinguished from each other and from Serbian and Hungarian populations, while the latter show a higher level of resemblance with regards to their quantitative morphological traits. It is likely that these morphological traits are determined through some quantitative trait loci implicated in stress responses generated by light, temperature, soil water, soil fertility and salinity conditions that will need to be analysed in terms of their physiological, genomic and metabolomics traits in future studies.
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Project description:Propolis is a valuable natural substance obtained by honey bees after being collected from the bark, resin of trees, plant leaves and mixed with their saliva, and has been widely used for various biological activities. The properties of propolis can vary widely by botanical origin, location of the hives and colony population. It is thought that the color of propolis is one of the main factors determining its acceptability and originates from the flower markers, pollen and nectar of some plants and is directly related to its chemical content. It is important to compare and standardize the colors, chemical content and biological activities of propolis in our country, which has a rich endemic plant diversity. Thus, in this study, the color indexes of 39 propolis samples from different locations in Turkiye were determined by Lovibond Tintometer, for the first time. The color index, total phenolic content, cytotoxic and antioxidant activities relationship of propolis and two commercial propolis samples were also investigated by HCA and PCA. Turkish propolis, which is defined by its color indices, chemical contents and many different activity potentials, such as antioxidant, antiviral and cytotoxic activity, will find use in many fields from medicine to cosmetics with this study.
| S-EPMC9598055 | biostudies-literature
Project description:The capsid protein (CA) of HIV-1 plays essential roles in multiple steps of the viral replication cycle by assembling into functional capsid core, controlling the kinetics of uncoating and nuclear entry, and interacting with various host factors. Targeting CA represents an attractive yet underexplored antiviral approach. Of all known CA-targeting small molecule chemotypes, the peptidomimetic PF74 is particularly interesting because it binds to the same pocket used by a few important host factors, resulting in highly desirable antiviral phenotypes. However, further development of PF74 entails understanding its pharmacophore and mitigating its poor metabolic stability. We report herein the design, synthesis, and evaluation of a large number of PF74 analogs aiming to provide a comprehensive chemical profiling of PF74 and advance the understanding on its detailed binding mechanism and pharmacophore. The analogs, containing structural variations mainly in the aniline domain and/or the indole domain, were assayed for their effect on stability of CA hexamers, antiviral activity, and cytotoxicity. Selected analogs were also tested for metabolic stability in liver microsomes, alone or in the presence of a CYP3A inhibitor. Collectively, our studies identified important pharmacophore elements and revealed additional binding features of PF74, which could aid in future design of improved ligands to better probe the molecular basis of CA-host factor interactions, design strategies to disrupt them, and ultimately identify viable CA-targeting antiviral leads.
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Project description:Background and aimsDioecious plant species, i.e. those in which male and female functions are housed in different individuals, are particularly vulnerable to global environmental changes. For long-lived plant species, such as trees, long-term studies are imperative to understand how growth patterns and their sensitivity to climate variability affect the sexes differentially.MethodsHere, we explore long-term intersexual differences in wood traits, namely radial growth rates and water-use efficiency quantified as stable carbon isotope abundance of wood cellulose, and their climate sensitivity in Ilex aquifolium trees growing in a natural population in north-western Spain.Key resultsWe found that sex differences in secondary growth rates were variable over time, with males outperforming females in both radial growth rates and water-use efficiency in recent decades. Summer water stress significantly reduced the growth of female trees in the following growing season, whereas the growth of male trees was favoured primarily by cloudy and rainy conditions in the previous autumn and winter combined with low cloud cover and warm conditions in summer. Sex-dependent lagged correlations between radial growth and water availability were found, with a strong association between tree growth and cumulative water availability in females at 30 months and in males at 10 months.ConclusionsOverall, our results point to greater vulnerability of female trees to increasing drought, which could lead to sex-ratio biases threatening population viability in the future.
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