Repurposing of monocyclic β-lactams as anti-inflammatory agents - The case of new ferrocene-azetidin-2-one hybrids.

There is growing interest in developing monotherapy drugs that treat inflammation caused by microbial infections, focusing on dual antimicrobial and anti-inflammatory agents with minimal side effects and high safety margins. This study synthesized and characterized a library of novel cis-4-ferrocenylazetidin-2-ones, evaluating their antimicrobial and anti-inflammatory activities. These organometallic monocyclic β-lactams showed moderate in vitro antimicrobial activity against various standard microbial strains, including yeasts and Gram-negative and Gram-positive bacteria.

Bioisosteric ferrocenyl 1,3-thiazolidine-4-carboxylic acid derivatives: In vitro antiproliferative and antimicrobial evaluations.

To improve the antiproliferative effect of ALC67 (diastereomeric mixture of ethyl 2-phenyl-3-propioloyl-1,3-thiazolidine-4-carboxylate), its structure was modified via (i) bioisosteric substitution of the phenyl ring by the ferrocene unit and (ii) replacing the propiolamide side-chain in ACL67 with other acyl groups having differing electrophilicities. In this way, a small library of methyl N-acyl-2-ferrocenyl-1,3-thiazolidine-4-carboxylates (13 compounds in total) was created and characterized by spectral and crystallographic means. The last N-acylation step was highly diastereoselective toward the cis-diastereomer.

New Iron Twist to Chloroquine─Upgrading Antimalarials with Immunomodulatory and Antimicrobial Features.

Herein, upgraded chloroquine (CQ) derivatives capable of overcoming resistance and, at the same time, suppressing excessive immune response and risk of concurrent bacteremia were developed. Twelve new ferrocene- hybrids tethered with a small azathia heterocycle (1,3-thiazolidin-4-one, 1,3-thiazinan-4-one, or 5-methyl-1,3-thiazolidin-4-one) were synthesized and fully characterized. All hybrids were evaluated for their in vitro antiplasmodial, antimicrobial, and immunomodulatory activities.

An HPLC-based assay for improved measurement of glutamate decarboxylase inhibition/activation.

L-Glutamic acid decarboxylase (GAD) is an enzyme that ensures the balance between the levels of two neurotransmitters, γ-aminobutyric acid (GABA) and L-glutamic acid (L-Glu), necessary for proper brain functioning. A reduction in the concentrations of GABA and/or GAD activity has been implicated in the symptoms associated with epilepsy, which could be plausibly alleviated by the application of GAD activators. As any unnecessary interference in GAD catalytic activity could be detrimental, it is important to study whether CNS (or other) drug candidates act on GAD or not.

Linking the antimicrobial and anti-inflammatory effects of immortelle essential oil with its chemical composition - The interplay between the major and minor constituents.

Immortelle (Helichrysum italicum, Asteraceae) essential oil has been widely used in alternative medicine to accelerate wound healing, as well as in cosmetic products to stimulate skin regeneration and to reduce the appearance of wrinkles. It is also considered a natural and safe culinary spice that could also be applied in the food industry as a preservative in the future. The therapeutic efficacy of this oil changes with the natural variability of the composition.

Very-Long-Chain Wax Constituents from Primula veris and P. acaulis: Does the Paradigm of Non-Branched vs. Branched Chain Dominance Universally Hold in all Plant Taxa?

Herein n-, iso- and anteiso-series of very-long-chained (VLC) alkanes (C -C ), fatty acid benzyl esters (FABEs; C -C ), and 2-alkanones (C -C ) were identified in the wax of Primula veris L. and P. acaulis (L.

New neryl esters from (Roth) G. Don (Asteraceae) essential oil.

(immortelle) is a dwarf aromatic shrub native to the Mediterranean region. The typical subspecies () produces an essential oil rich in neryl acetate and characteristic β-diketones, italidiones, highly valued in the perfume industry. As esters are an important group of aroma-active volatiles, herein the composition of the ester fraction of this immortelle chemotype essential oil was studied in detail.

Anti-virulence potential of basil and sage essential oils: Inhibition of biofilm formation, motility and pyocyanin production of Pseudomonas aeruginosa isolates.

The effects of basil (Ocimum basilicum) and sage (Salvia officinalis) essential oils on selected virulence factors (biofilm formation, mature biofilm resistance, motility, and pyocyanin production) of Pseudomonas aeruginosa clinical isolates were evaluated in the present study for the first time. The two essential oils were chemically characterized by GC and GC-MS analyses. Linalool and (E)-anethole were found to be the main components of the investigated basil oil, while α-thujone and camphor were the major constituents of the studied sage essential oil.

Maternal age has more pronounced effect on breast milk retinol and β-carotene content than maternal dietary pattern.

Objective: The effects on breast milk composition of advanced maternal age and maternal dietary habits during pregnancy and lactation have not, to our knowledge, been investigated in southeastern Europe and the Balkans. The aim of this study was to compare the content of retinol and β-carotene in colostrum and mature milk samples obtained from different maternal age (MA) groups and to assess the potential relationship with maternal and demographic characteristics, dietary patterns, and lifestyle habits during pregnancy and lactation.

Methods: Forty-three nursing mothers were divided in two groups according to MA: ≥35 y of age (n = 22) and <35 y of age (n = 21).

Genomics-Based Insights Into the Biosynthesis and Unusually High Accumulation of Free Fatty Acids by sp. NP10.

sp. NP10 was previously shown to synthesize large amounts of free fatty acids (FFAs). In this work, we report the first insights into the biosynthesis of these fatty acids (FAs) gained after genome sequencing and identification of the genes involved.

Prenylated β-diketones, two new additions to the family of biologically active Hypericum perforatum L. (Hypericaceae) secondary metabolites.

Two novel β-diketones, 2,6,9-trimethyl-8-decene-3,5-dione (A) and 3,7,10-trimethyl-9-undecene-4,6-dione (B), were identified from the renowned medicinal plant Hypericum perforatum L. The structures of β-diketones A and B were corroborated by syntheses (4 steps starting from methyl acetoacetate, overall yields 30% and 23%, respectively). In solution, these β-diketones predominantly exist as two rapidly interconverting β-keto-enol tautomers.

Toxic essential oils. Part V: Behaviour modulating and toxic properties of thujones and thujone-containing essential oils of Salvia officinalis L., Artemisia absinthium L., Thuja occidentalis L. and Tanacetum vulgare L.

Neurotoxic thujones (α- and β-diastereoisomers) are common constituents of plant essential oils. In this study, we employed a statistical approach to determine the contribution of thujones to the overall observed behaviour-modulating and toxic effects of essential oils (Salvia officinalis L., Artemisia absinthium L.

Essential-Oil Constituents and Alkanes of Cephalaria ambrosioides Roem. & Schult. (Family Caprifoliaceae, Subfamily Dipsacaceae) and (Chemo)taxonomic Discernment of the Subfamilies Dipsacaceae and Morinaceae.

Herein, the results of the first study of the volatile and alkane profiles of Cephalaria ambrosioides Roem. & Schult. (Caprifoliaceae, subfamily Dipsacaceae) were reported.

Structural diversity and possible functional roles of free fatty acids of the novel soil isolate Streptomyces sp. NP10.

Herein, a novel soil bacterium Streptomyces sp. NP10 able to grow outside usual streptomycetes optimum conditions (e.g.