Search results for "010404 medicinal & biomolecular chemistry"
showing 10 items of 373 documents
The essential oil composition of Centaurea immanuelis-loewii Degen growing wild in Bulgaria and chemotaxonomy of section Acrocentron
2021
In the present study, the chemical composition of the essential oil from aerial parts of the Balkan endemic, Centaurea immanuelis-loewii Degen (sect. Acrocentron, Asteraceae), collected in Bulgaria was evaluated by GC-MS. The main components of the oil were β-caryophyllene (23.2%), germacrene D (13.7%) and caryophyllene oxide (12.4%). Furthermore, a complete literature review on the composition of the essential oils of all the other taxa of Centaurea, belonging to section Acrocentron, studied so far, was performed and the chemotaxonomical variations in the composition of the essential oils is discussed.
Oxidative Stress and the Epigenetics of Cell Senescence: Insights from Progeroid Syndromes.
2019
Background: Cell senescence constitutes a critical process to respond to a variety of insults and adverse circumstances. Senescence involves the detention of DNA replication and cell proliferation, and hence, genetic programs associated with DNA damage response, chromosome stability, chromatin rearrangement, epigenetic reprogramming, and cell cycle are tightly linked to the senescent phenotype. Although senescence increases with age, the real implication of senescence regulation in the progress of aging in humans is largely discussed. In this context, reactive oxygen species (ROS) accumulation has also been postulated to play a critical role in cell homeostasis, aging processes, and contro…
Chemical composition of the essential oils of Centaurea tomentella Hand.-Mazz. and C. haussknechtii Boiss. (Asteraceae) collected wild in Turkey and …
2018
In the present study the chemical composition of the essential oils from aerial parts of Centaurea tomentella Hand.-Mazz. and C. haussknechtii Boiss. collected in Turkey was evaluated by GC and GC-MS. The main components of C. tomentella L. were hexadecanoic acid (19.7%), caryophyllene oxide (6.6%) and spathulenol (4.8%) whereas C. haussknechtii was rich in hexadecanoic acid (26.2%), (Z,Z)-9,12-octadecadienoic acid (19.3%), heptacosane (5.3%) and nonacosane (5.1%). Antibacterial and antifungal activities against some microorganisms infesting historical art craft, were also determined.
Chemical composition of volatile and fixed oils from of Salvia argentea L. (Lamiaceae) growing wild in Sicily.
2015
The chemical compositions of the essential oil and of the non-polar extracts (petroleum ether, dichloromethane) of the aerial parts (flowers, leaves and stems) of Salvia argentea L. were determined by GC-FID and gas chromatographyâmass spectrometry analysis. 14-Hydroxy-α-humulene (40.1%) was recognised as the main constituents of the essential oil of S. argentea, together with 1,3,8-p-menthatriene (12.1%), globulol (7.4%) and β-sesquiphellandrene (5.8%). Tritriacontane (9.9% and 14.1%), heptacosane (8.4% and 10.5%), hentriacontane (8.3% and 10.9%), tetradecanal (8.4% and 10.2%) and methyldotriacontane (7.9% and 7.6%) were recognised as the main constituents of the extracts in petroleum …
The role played by doctors, the Government and the who in the implementation of poliomyelitis, measles and rubella serological surveys in Spain (1958…
2020
Serological surveys, which acquired considerable importance in the mid twentieth century, are still a key tool to address infectious diseases. This article, using archival and printed sources from the WHO and the medical and general press, analyses the role of doctors and scientists, government, and the WHO in the implementation of serological surveys to evaluate the situation of poliomyelitis, measles and rubella in Spain and to set up a plan of action against them. The paper shows the role of Florencio Pérez Gallardo and his group at the National School of Health, favoured by the Franco regime to receive the support of WHO collaborative programmes after Spain joined in 1951, and the impac…
Identification of Three-Way DNA Junction Ligands through Screening of Chemical Libraries and Validation by Complementary in Vitro Assays
2019
International audience; The human genome is replete with repetitive DNA sequences that can fold into thermodynamically stable secondary structures such as hairpins and quadruplexes. Cellular enzymes exist to cope with these structures whose stable accumulation would result in DNA damage through interference with DNA transactions such as transcription and replication. Therefore, the chemical stabilization of secondary DNA structures offers an attractive way to foster DNA transaction-associated damages to trigger cell death in proliferating cancer cells. While much emphasis has been recently given to DNA quadruplexes, we focused here on three-way DNA junctions (TWJ) and report on a strategy t…
Metabolomics analysis and biological investigation of three Malvaceae plants
2019
Introduction: Metabolomics is a fast growing technology that has effectively contributed to many plant-related sciences and drug discovery. Objective: To use the non-targeted metabolomics approach to investigate the chemical profiles of three Malvaceae plants, namely Hibiscus mutabilis L. (Changing rose), H. schizopetalus (Dyer) Hook.f. (Coral Hibiscus), and Malvaviscus arboreus Cav. (Sleeping Hibiscus), along with evaluating their antioxidant and anti-infective potential. Methodology: Metabolic profiling was carried out using liquid chromatography coupled with high-resolution electrospray ionisation mass spectrometry (LC-HR-ESI-MS) for dereplication purposes. The chemical composition of th…
LC–ESI–FT–MSn Metabolite Profiling of Symphytum officinale L. Roots Leads to Isolation of Comfreyn A, an Unusual Arylnaphthalene Lignan
2020
Preparations of comfrey (Symphytum officinale L.) roots are used topically to reduce inflammation. Comfrey anti-inflammatory and analgesic properties have been proven in clinical studies. However, the bioactive compounds associated with these therapeutic activities are yet to be identified. An LC&ndash
Pyrrolomycins as antimicrobial agents. Microwave-assisted organic synthesis and insights into their antimicrobial mechanism of action
2019
Abstract New compounds able to counteract staphylococcal biofilm formation are needed. In this study we investigate the mechanism of action of pyrrolomycins, whose potential as antimicrobial agents has been demonstrated. We performed a new efficient and easy method to use microwave organic synthesis suitable for obtaining pyrrolomycins in good yields and in suitable amount for their in vitro in-depth investigation. We evaluate the inhibitory activity towards Sortase A (SrtA), a transpeptidase responsible for covalent anchoring in Gram-positive peptidoglycan of many surface proteins involved in adhesion and in biofilm formation. All compounds show a good inhibitory activity toward SrtA, havi…
Asymmetric Disulfanylbenzamides as Irreversible and Selective Inhibitors of Staphylococcus aureus Sortase A
2020
Abstract Staphylococcus aureus is one of the most frequent causes of nosocomial and community‐acquired infections, with drug‐resistant strains being responsible for tens of thousands of deaths per year. S. aureus sortase A inhibitors are designed to interfere with virulence determinants. We have identified disulfanylbenzamides as a new class of potent inhibitors against sortase A that act by covalent modification of the active‐site cysteine. A broad series of derivatives were synthesized to derive structure‐activity relationships (SAR). In vitro and in silico methods allowed the experimentally observed binding affinities and selectivities to be rationalized. The most active compounds were f…