Enhanced Bioactivity of Rosemary, Sage, Lavender, and Chamomile Essential Oils by Fractionation, Combination, and Emulsification.

This study aimed to increase the bioactivity of essential oils by fractionation, combination, and emulsification. In this regard, pharmaceutical quality Rosmarinus officinalis L. (rosemary), Salvia sclarea L. (clary sage), Lavandula latifolia Medik. (spike lavender), and Matricaria chamomilla L. (chamomile) essential oils were fractionated by vacuum-column chromatography. The main components of the essential oils were verified, and their fractions were characterized by thin layer chromatography, gas chromatography-flame ionization detector, and gas chromatography/mass spectrometry. Besides, oil-in-water (O/W) emulsions of essential oils and diethyl ether fractions were obtained by the self-emulsification method, followed by droplet size, polydispersity index, and zeta potential value measurements. The in vitro antibacterial effects of the emulsions and binary combinations (10:90, 20:80, 30:70, 40:60, 50:50, 60:40, 70:30, 80:20, 90:10, v:v) against Staphylococcus aureus were determined by microdilution. In addition, the in vitro anti-biofilm, antioxidant, and anti-inflammatory effects of emulsion formulations were evaluated. According to the experimental results, fractionation and emulsification enhanced essential oil in vitro antibacterial, anti-inflammatory, and antioxidant effects due to increased solubility and nano-sized droplets. Among 22 different emulsion combinations, 1584 test concentrations resulted in 21 cases of synergistic effects. The mechanism of the increase in biological activities was hypothesized to be higher solubility and stability of the essential oil fractions. Food and pharmaceutical industries may benefit from the procedure proposed in this study.

An Investigation Into the Degree of Sinus Mucosal Delivery of Inhaled Black Cumin Volatile and Peppermint Essential Oils.

The aim of this study was to investigate the quantity of volatile components reaching the sinus mucosa (SM) by inhalation, which is responsible for the therapeutic effect, as a first step toward targeted drug design. In this study, 18 Wistar-Albino female rats with an average weight between 200 and 250 g were used. The rats to be used in the study were randomized: Black cumin (BC) essential oil group (group 1) (n = 6), Peppermint essential oil (PEO) group (group 2) (n = 6), and Control (group 3) (n = 6). Volatile oils were inhaled in group 1 and 2; in the control group volatile oils were not inhaled. In all groups, SM was removed and essential volatile oil composition was determined. In group 1, α-pinene was identified as the principal component in the gas phase from five different glass bottles containing SM. The data obtained were evaluated using the single sample T-test and results show that the α-pinene component in the group of inhaled BC essential oil reached significance (P < .001) when compared with the control group. The active component of the BC essential oil could not be identified as thymoquinone. In group 2, eucalyptol (1,8-cineole) was identified as the principal component in the gas phase from five different glass bottles containing SM. The data obtained were evaluated using the single sample T-test and it was found that the eucalyptol component in the group which inhaled PEO reached statistical significance (P < .001) compared with the control group. In group 3, no volatile oil compounds were detected. We have demonstrated that both oils (BC and peppermint) are delivered to the SM. There is a need for the optimum dose to be clarified by different methods of measurement than those used in the spectrometric data we have obtained. We are convinced that our work will lead to pharmacological, toxicological, and subsequent clinical trials in this area.

Secondary metabolites from Verbascum bugulifolium Lam. and their bioactivities.

Five iridoid glycosides catalpol (1), specioside (2), ajugol (3), ajugoside (4), 8-O-acetylharpagide (5), two phenylethanoid glycosides, verbascoside (6) and glucopyranosyl-(1→Gi-6)-martynoside (7), four flavonoids, luteolin (8), luteolin 7-O-ß-glucopyranoside (9), luteolin 7-O-rutinoside (10), apigenin 7-O-rutinoside (11), quercetin 3-O-rutinoside (12) and ß-sitosterol (13) were isolated from the aerial parts of Verbascum bugulifolium Lam. for the first time. Their structures were elucidated by NMR and MS experiments. The extracts, and the isolates were evaluated for their in vitro antioxidant (DPPH•, ABTS• and CUPRAC), anti-inflammatory (LOX inhibition) and antimicrobial activities. Compounds 6 and 8 showed the highest antioxidant activity in all tests, where luteolin (8) showed the relatively best anti-inflammatory activity compared to other samples with 54.1 ± 5.0% inhibition at 1 µg/mL. All the tested compounds showed weak antimicrobial activity against tested microorganisms. This is the first phytochemical and bioactivity study on V. bugulifolium.[Figure: see text].

Secondary metabolites from the aerial parts of Sideritis germanicopolitana and their in vitro enzyme inhibitory activities.

Three iridoid glycosides, 5-allosyloxy-aucubine (1), melittoside (2), ajugol (3), five phenylethanoid glycosides, verbascoside (4), martynoside (5), leucoseptoside A (6), lamalboside (7), decaffeoylverbascoside (8), four flavonoids, xanthomicrol (9), isoscutellarein 7-O-[6'''-O-acetyl-ß-allopyranosyl-(1→2)]-ß-glucopyranoside (10), 4'-O-methylisoscutellarein 7-O-[6'''-O-acetyl-ß-allopyranosyl-(1→2)]-ß-glucopyranoside (11), 3'-hydroxy-4'-O-methylisoscutellarein 7-O-[6'''-O-acetyl-ß-allopyranosyl-(1→2)]-ß-glucopyranoside (12), and two lignan glycosides dehydrodiconiferylalcohol 4-O-ß-D-glucopyranose (13) and pinoresinol 4'-O-ß-glucopyranoside (14) were isolated from the aerial parts of Sideritis germanicopolitana. Their structures were determined on the basis of detailed NMR and HRESIMS analyses. To our knowledge, all compounds are being reported for the first time from S. germanicopolitana, while the isolated lignans (13 and 14) are new for the genus Sideritis. In vitro evaluation of AChE, BChE and LOX inhibitory effects of all the tested compounds (1-14) resulted in low to moderate activities.

Synergistic antibacterial combination of Lavandula latifolia Medik. essential oil with camphor.

Combination of various compounds and essential oils for pharmaceutical formulations withdraw attention. In this present study, it was aimed to evaluate the in vitro potential synergistic antibacterial effect of Lavandula latifolia (spike lavender) essential oil with camphor by using the checkerboard method against the human pathogens; Staphylococcus aureus and Listeria monocytogenes. Pharmacopoeia quality L. latifolia essential oil and racemic camphor were analyzed and verified by GC-FID and GC/MS, simultaneously. In vitro antibacterial activity of essential oil and camphor (MIC range: 0.16-20 mg/mL) and standard antimicrobial clarithromycin (MIC range: 0.125-16 µg/mL) were carried out by broth microdilution against S. aureus and L. monocytogenes standard strains, respectively. Resulting antibacterial effects were evaluated for their fractional inhibitory concentrations (FICs) as antagonistic, additive and synergistic effects. The analytical results showed that the major component of essential oil was linalool (45.2%) and 1,8-cineole (25.6%). Antibacterial effects of essential oil were determined as MIC 1.25-5 mg/mL. As a result of the experiments, L. latifolia essential oil-camphor combinations were identified as "synergistic (FIC ≤ 0.5), and additive (0.5 < FIC ≤ 1)" in the respective combinations, suggesting further evaluation for formulations for potential antimicrobial applications in food and pharmaceuticals.

Albumin Based Nanoparticles for Detection of Pancreatic Cancer Cells.

BACKGROUND: Molecular imaging of cancer cells using effective drug targeting systems are most interested research area in recent years. Albumin protein is a soluble and most abundant protein in circulatory system. It has a ligand-binding function and acts as a transport protein. Researchers are interested in developing albumin based nanostructured specific anti-tumor drugs in cancer therapy. Pancreatic cancer treatment or drug design for targeted pancreatic cancer cell has great importance due to it has a high mortality rate comparing other cancer types. OBJECTIVE: In this article, our goal is to develop new targeting nanoparticles based on the conjugation of albumin and Hyaluronic Acid (HA) for pancreatic cancer cells. METHOD: In this article, we proposed a new technique for conjugation of albumin (BSA) and HA in nano formation. Firstly, cationic BSA is synthesized. Then, BSA-HA conjugation is obtained by interacted cationic BSA with 1000 ppm HA. Secondly, nano BSA-HA particles and nano BSA particles were synthesized according to AmiNoAcid Decorated and Light Underpinning Conjugation Approach (ANADOLUCA) method which provides a special cross-linking strategy for biomolecules using ruthenium-based amino acid monomer haptens. After characterization studies, in vitro cytotoxic activity of synthesized nano BSA-HA particles were determined for PANC-1 ATCC® CRL146 cells. RESULTS: According to the data, nano BSA and nano BSA-HA particles synthesized uniquely using special ruthenium-based amino acid decorated cross-linking agent, (MATyr)2-Ru-(MATyr)2.based on ANDOLUCA method. Characterization results showed that there was not any change in protein folding structures during nano formation process. In addition, nano protein particles gained fluorescence feature. When interacting synthesized nano BSA and nano BSA-HA particles with pancreatic cells, it was found that BSA nanoparticles were usually around cells and membranes, but BSA-HA nanoparticles were identified around the cells, in the cytoplasm inside the cell, and next to the cell nucleus. So, nano BSA-HA particles could be used as cancer cell imaging agent for PANC-1 ATCC® CRL146 cells. CONCLUSION: The satisfactory conclusion of this study is that synthesized nano BSA-HA particles are fundamental materials for targeting pancreatic cancer cells due to HA receptors located on pancreatic cancer cells and imaging agents due to fluorescence feature of the BSA-HA nanoparticles.

Anti-inflammatory and antibacterial evaluation of Thymus sipyleus Boiss. subsp. sipyleus var. sipyleus essential oil against rhinosinusitis pathogens.

Thymus sipyleus Boiss. subsp. sipyleus var. sipyleus of the Lamiaceae, locally known as thyme scented lemon, which is an endemic taxon collected from Sivas in Anatolia, was investigated in this study due to its folk medicine use against rhinosinusitis. The aromatic characteristics of the plant material gave the idea for the detailed evaluation of the volatiles and essential oil thereof. Consequently, the oil was obtained by Clevenger type hydrodistillation followed by gas chromatography-flame ionization detector (GC-FID) and gas chromatography/mass spectrometry (GC/MS) analyses for phytochemical characterization. To confirm the folk medicinal use against sinusitis, in vitro antimicrobial activities of the essential oil was evaluated by agar diffusion, microdilution and vapour diffusion methods against selected rhinosinusitis associated strains such as Staphylococcus aureus, methicillin-resistant S. aureus (MRSA), S. epidermidis, Streptococcus pyogenes, S. pneumoniae, Pseudomonas aeruginosa, Haemophilus influenzae and Moraxella catarrhalis. Additionally, the in vitro anti-inflammatory activity was evaluated by 5-lipoxygenase (5-LOX) inhibitory effect of the essential oil spectrophotometrically. Furthermore, the composition of the volatiles of the vapour phase of the oil was determined by headspace-solid phase microextraction (HS-SPME-GC/MS) after 15 min and 24 h in accordance with antimicrobial vapour diffusion method conditions, respectively. According to the analytical results, the main component was determined as thymol (66.2%). Whereas in the HS-SPME method p-cymene (26.1%) and γ-terpinene (26%) were identified as the main volatile components within the 15. min., and thymol (75.3%) after 24 h, respectively. The antibacterial activity against rhinosinusitis pathogens varied between 160 and 1250 µg/mL minimum inhibitory concentrations, with the best inhibitory effects observed against the S. aureus, S. pyogenes and M. catarrhalis. The anti-inflammatory activity of the oil was determined as 12.1 ±â€¯1.8% in 100 µg/mL. The results showed the in vitro antimicrobial and anti-inflammatory potential of the oil also in vapour phase against sinusitis supporting the traditional use.

Secondary Metabolites from the Leaves of Digitalis viridiflora.

A new phenylethanoid glycoside, named digiviridifloroside (1), was isolated from the leaves of Digitalis viridiflora Lindley along with a known phenylethanoid glycoside, calceolarioside A (2), two flavonoid glycosides, scutellarein 7-Ο-ß-D-glucopyranoside (3) and hispidulin 7-0-ß-D-glucopyranoside (4), two cleroindicins, cleroindicins B (5) and F (6), a nucleoside, adenosine (7), as well as a mixture of ß-glucopyranosyl-(1-6)-4-O-caffeoyl-α/ß glucopyranose and 3,4-dihydroxyphenylethanol. The structure of the new compound was established as 3,4-dihydroxy-ß-phenylethoxy-6-O-(E)-feruloyl-ß- glucopyranosyl-(l->6)-4-0-(E)-caffeoyl-ß-glucopyranoside (1) based on extensive ID- and 2D-NMR spectroscopy, as well. as HR-ESI-MS. Digiviridifloroside represents a rare type of phenylethanoid glycoside which bears two aromatic acyl units in its structure. In addition to phytochemical studies, the isolates were evaluated for their in vitro antimicrobial activities against three pathogenic bacteria and three yeast strains using a microdilution method. Among the tested compounds, 5 exhibited moderate antibacterial activity against Bacillus cereus NRRLB 3711 with a MIC value of 25 µg/mL, whereas compounds 5 and 6 showed relatively high anticandidal activity against Candida strains with MIC values down to 12.5 µg/mL, in comparison to the standard antimicrobial compounds.