Chemical composition and antibacterial activity of Origanum saccatum P.H. Davis essential oil obtained by solvent-free microwave extraction: comparison with hydrodistillation

The components of the essential oils (EOs) obtained by solvent-free microwave extraction (SFME) and hydrodistillation (HD) from endemic Origanum saccatum P.H. Davis were identified by using GC/MS. The main constituents of both EOs obtained by SFME and HD, respectively, from O. saccatum were p-cymene (72.5 and 70.6%), thymol (9.32 and 8.11%), and carvacrol (7.18 and 6.36%). The EO obtained by SFME contained substantially higher amounts of oxygenated compounds and lower amounts of monoterpenes than did the EO obtained by HD. The antibacterial activities of the EOs obtained by SFME and HD were evaluated with the disc diffusion method by comparison with 10 different bacterial strains. The antibacterial activity of the EO extracted by SFME was found to be more effective than that of the EO extracted by HD against seven of the tested bacteria.     

Optimisation and validation of liquid chromatographic and partial least-squares-1 methods for simultaneous determination of enalapril maleate and nitrendipine in pharmaceutical preparations

Simultaneous determination of enalapril maleate (ENA) and nitrendipine (NIT) in pharmaceutical preparations was performed using liquid chromatography (LC) and the partial least-squares-1 (PLS-1) method. In LC, the separation was achieved on a C8 column and the optimum mobile phase for good separation in a gradient elution programme was found to be acetonitrile-water (φ _r = 81: 19) and optimum flow-rate, temperature, injection volume, and detection wavelength were set at 1.0 mL min⁻¹, 25°C, 10 μL, and 210 nm, respectively. Dienogest was selected as an internal standard. In the spectrophotometry, a PLS-1 chemometric method was used. The absorbance data matrix related to the concentration data matrix was established by measurement of absorbances in their zero order spectra with an increment of Δλ = 1 nm in the 220–290 nm range for ENA and with Δλ = 1 nm in the 230–290 nm range for NIT in the PLS-1 method. Following this step, calibration was established by using this data matrix to predict the unknown concentrations of ENA and NIT in their binary mixture. These optimised methods were validated and successfully applied to a pharmaceutical preparation in tablet form and the results were subjected to comparison.     

Donor-acceptor oligorotaxanes made to order

Five donor–acceptor oligorotaxanes made up of dumbbells composed of tetraethylene glycol chains, interspersed with three and five 1,5‐dioxynaphthalene units, and terminated by 2,6‐diisopropylphenoxy stoppers, have been prepared by the threading of discrete numbers of cyclobis(paraquat‐p‐phenylene) rings, followed by a kinetically controlled stoppering protocol that relies on click chemistry. The well‐known copper(I)‐catalyzed alkyne–azide cycloaddition between azide functions placed at the ends of the polyether chains and alkyne‐bearing stopper precursors was employed during the final kinetically controlled template‐directed synthesis of the five oligorotaxanes, which were characterized subsequently by ¹H NMR spectroscopy at low temperature (233 K) in deuterated acetonitrile. The secondary structures, as well as the conformations, of the five oligorotaxanes were unraveled by spectroscopic comparison with the dumbbell and ring components. By focusing attention on the changes in chemical shifts of some key probe protons, obtained from a wide range of low‐temperature spectra, a picture emerges of a high degree of folding within the thread protons of the dumbbells of four of the five oligorotaxanes—the fifth oligorotaxane represents a control compound in effect—brought about by a combination of C? H???O and π–π stacking interactions between the π‐electron‐deficient bipyridinium units in the rings and the π‐electron‐rich 1,5‐dioxynaphthalene units and polyether chains in the dumbbells. The secondary structures of a foldamer‐like nature have received further support from a solid‐state superstructure of a related [3]pseudorotaxane and density functional calculations performed thereon.     

Anti-Inflammatory and Neuromodulatory Effects Induced by Tanacetum parthenium Water Extract: Results from In Silico,In Vitro and Ex Vivo Studies

Tanacetum parthenium (feverfew) has traditionally been employed as a phytotherapeutic remedy in the treatment of migraine. In this study, a commercial T. parthenium water extract was investigated to explore its anti-inflammatory and neuromodulatory effects. Isolated mouse cortexes were exposed to a K⁺ 60 mM Krebs-Ringer buffer and treated with T. parthenium water extract. The prostaglandin E₂ (PGE₂) level, brain-derived neurotrophic factor (BDNF), interleukin-10 (IL-10), and IL-1β gene expression were evaluated in the cortex. The effects on dopamine (DA) release and dopamine transporter (DAT) gene expression were assayed in hypothalamic HypoE22 cells. A bioinformatics analysis was conducted to further investigate the mechanism of action. The extract was effective in reducing cortex PGE₂ release and IL-1β gene expression. In the same experimental system, IL-10 and BDNF gene expressions increased, and in HypoE22 cells, the extract decreased the extracellular dopamine level and increased the DAT gene expression due to the direct interaction of parthenolide with the DAT. Overall, the present findings highlight the efficacy of T. parthenium water extract in controlling the inflammatory pathways that occur during cortical-spreading depression. Additionally, the inhibition of the hypothalamic DA release observed in this study further supports the role of dopaminergic pathways as key targets for novel pharmacological approaches in the management of migraine attacks.     

Phenolic Profile,Antioxidant and Enzyme Inhibitory Activities of Leaves from Two Cassia and Two Senna Species

Several species within the genera Cassia or Senna have a treasure of traditional medicines worldwide and can be a promising source of bioactive molecules. The objective of the present study was to evaluate the phenolic content and antioxidant and enzyme inhibition activities of leaf methanolic extracts of C. fistula L., C. grandis L., S. alexandrina Mill., and S. italica Mill. The two Cassia spp. contained higher total polyphenolic content (42.23–49.75 mg GAE/g) than the two Senna spp., and C. fistula had significantly (p ˂ 0.05) the highest concentration. On the other hand, the Senna spp. showed higher total flavonoid content (41.47–59.24 mg rutin equivalent per g of extract) than that found in the two Cassia spp., and S. alexandrina significantly (p ˂ 0.05) accumulated the highest amount. HPLC–MS/MS analysis of 38 selected bioactive compounds showed that the majority of compounds were identified in the four species, but with sharp variations in their concentrations. C. fistula was dominated by epicatechin (8928.75 µg/g), C. grandis by kaempferol-3-glucoside (47,360.04 µg/g), while rutin was the major compound in S. italica (17,285.02 µg/g) and S. alexandrina (6381.85). The methanolic extracts of the two Cassia species exerted significantly (p ˂ 0.05) higher antiradical activity, metal reducing capacity, and total antioxidant activity than that recorded from the two Senna species’ methanolic extracts, and C. fistula displayed significantly (p ˂ 0.05) the highest values. C. grandis significantly (p ˂ 0.05) exhibited the highest metal chelating power. The results of the enzyme inhibition activity showed that the four species possessed anti-AChE activity, and the highest value, but not significantly (p ≥ 0.05) different from those obtained by the two Cassia spp., was exerted by S. alexandrina. The Cassia spp. exhibited significantly (p ˂ 0.05) higher anti-BChE and anti-Tyr properties than the Senna spp., and C. grandise revealed significantly (p ˂ 0.05) the highest values. C. grandise revealed significantly (p ˂ 0.05) the highest α- amylase inhibition, while the four species had more or less the same effect against the α-glucosidase enzyme. Multivariate analysis and in silico studies showed that many of the identified phenols may play key roles as antioxidant and enzyme inhibitory properties. Thus, these Cassia and Senna species could be a promising source of natural bioactive agents with beneficial effects for human health.     

“Smart Extraction Chain” with Green Solvents: Extraction of Bioactive Compounds from Picea abies Bark Waste for Pharmaceutical,Nutraceutical and Cosmetic Uses

Secondary metabolites from the sawmill waste Picea abies bark were extracted using an innovative two-step extraction that includes a first step with supercritical CO₂ (SCO₂) and a second step using green solvents, namely ethanol, water, and water ethanol mixture. Maceration (M), ultrasound assisted extraction (UAE) and microwave assisted extraction (MAE) techniques were applied in the second step. A total of nineteen extract were obtained and yield were compared. Bark extracts were characterized by LC-DAD-MSⁿ and classes of compounds were quantified as abietane derivatives, piceasides, flavonoids, and phenolics to compare different extractions. Obtained extracts were studied by in vitro assay to evaluate potential pharmaceutical, nutraceutical and cosmetic uses assessing the antioxidant activity as well as the inhibitory activity on target enzymes. Results show that the “smart extraction chain” is advantageous in term of yield of extraction and phytoconstituent concentration. SCO₂ extract, presenting a unique composition with a large amount of abietane derivatives, exerted the best activity for amylase inhibition compared to the other extracts.     

Single-Chain Folding Nanoparticles as Carbon Nanotube Catchers

This contribution describes a simple method for preparing polymeric nanoparticles using photodimerization of anthracene moieties on the side chain of terpolymers in dilute regime and transformation of obtained polymeric nanoparticles into pyrene functional nanoparticles via Menschutkin quaternization procedure. Subsequently, pyrene possessing polymeric nanoparticles are attached onto multiwalled carbon nanotube (MWCNT) surfaces by π–π stacking strategy. Gel permeation chromatography, thermal gravimetric analysis, ultraviolet–visible, and fluorescence spectroscopies are used to analyze modified nanoparticles and their precursors. Electron microscopy and dispersion studies show that pyrene-modified polymeric nanoparticles are able to interconnect various CNTs. © 2018 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2018 , 56, 2709–2714