Antibacterial and antioxidant activity of cinnamon essential oil-laden 45S5 bioactive glass/soy protein composite scaffolds for the treatment of bone infections and oxidative stress.

This study aimed to fabricate cinnamon essential oil (CO)-laden 45S5 bioactive glass (BG)/soy protein (SP) scaffolds exhibiting antioxidant and antibacterial activity. In this regard, 45S5 BG-based scaffolds were produced by the foam replica method, and subsequently the scaffolds were coated with various concentrations of CO (2.5, 5 and 7 (v/v) %) incorporated SP solution. Scanning electron microscopy images revealed that the CO-laden SP effectively attached to the 45S5 BG scaffold struts. The presence of 45S5 BG, SP and CO was confirmed using Fourier transform infrared spectroscopy. Compressive strength results indicated that SP based coatings improved the scaffolds' mechanical properties compared to uncoated BG scaffolds. The loading efficiency and releasing behaviour of the different CO concentrations were tested by gas chromatography-mass spectroscopy and UV-Vis spectroscopy. The results showed that CO incorporated scaffolds have controlled releasing behaviour over seven days. Furthermore, the coating on the scaffold surfaces slightly retarded, but it did not inhibit, the in vitro bioactivity of the scaffolds. Moreover, the antioxidant and antibacterial activity of CO was studied. The free radical scavenging activity measured by DPPH was 5 ± 1, 41 ± 3, 44 ± 1 and 43 ± 1 % for BGSP, CO2.5, CO5 and CO7, respectively. The antioxidant activity was thus enhanced by incorporating CO. Agar diffusion and colony counting results indicated that the incorporation of CO increased the antibacterial activity of scaffolds against S. aureus and E. coli. In addition, cytotoxicity of the scaffolds was investigated using MG-63 osteoblast-like cells. The results showed that the BG-SP scaffold was non-toxic under the investigated conditions, whereas dose-dependent toxicity was observed in CO-laden scaffolds. Considered together, the developed phytotherapeutic agent laden 45S5 BG-based scaffolds are promising for bone tissue engineering exhibiting capability to combat bone infections and to protect against oxidative stress damage.

Sesquiterpenes and sesquiterpenoids harbor modulatory allosteric potential and affect inhibitory GABAA receptor function in vitro.

Naturally occurring compounds such as sesquiterpenes and sesquiterpenoids (SQTs) have been shown to modulate GABAA receptors (GABAA Rs). In this study, the modulatory potential of 11 SQTs at GABAA Rs was analyzed to characterize their potential neurotropic activity. Transfected HEK293 cells and primary hippocampal neurons were functionally investigated using electrophysiological whole-cell recordings. Significantly different effects of ß-caryophyllene and α-humulene, as well as their respective derivatives ß-caryolanol and humulol, were observed in the HEK293 cell system. In neurons, the concomitant presence of phasic and tonic GABAA R configurations accounts for differences in receptor modulation by SQTs. The in vivo presence of the γ2 and δ subunits is important for SQT modulation. While phasic GABAA receptors in hippocampal neurons exhibited significantly altered GABA-evoked current amplitudes in the presence of humulol and guaiol, negative allosteric potential at recombinantly expressed α1 ß2 γ2 receptors was only verified for humolol. Modeling and docking studies provided support for the binding of SQTs to the neurosteroid-binding site of the GABAA R localized between transmembrane segments 1 and 3 at the (+ α)-(- α) interface. In sum, differences in the modulation of GABAA R isoforms between SQTs were identified. Another finding is that our results provide an indication that nutritional digestion affects the neurotropic potential of natural compounds.

Isolation of sesquiterpenoids from Matricaria chamomilla by means of solvent assisted flavor evaporation and centrifugal partition chromatography.

The (semi)volatile fraction of Matricaria chamomilla L., an annual herbal plant from the family of Asteraceae, contains high quantities of sesquiterpenes and sesquiterpenoids. A method was developed to achieve isolation and separation of these compounds, using a combination of solvent assisted flavor evaporation (SAFE) and solid support-free liquid-liquid chromatography. The biphasic liquid solvent system n-heptane/ethyl acetate/methanol/water, 5/2/5/2 v/v/v/v (Arizona S) was elaborated as a suitable solvent system for the simultaneous separation of the target compounds. The lab-scale liquid-liquid chromatography separation performed in a countercurrent chromatography (CCC) column was successfully transferred to a semi-preparative centrifugal partition chromatography (CPC) column, which enabled the isolation of artemisia ketone, artemisia alcohol, α-bisabolone oxide A, and (E)-en-yn-dicycloether. α-Bisabolol oxide A and (Z)-en-yn-dicycloether co-eluted, but were successfully separated by subsequent size-exclusion chromatography (SEC). Similarly, spathulenol and α-bisabolol oxide B were obtained as a mixture, and were separated by means of column chromatography using silica gel as stationary phase. The isolated compounds were characterized by means of nuclear magnetic resonance spectroscopy (NMR) and gas chromatography-mass spectrometry (GC-MS).