Propolis is a bee-produced substance rich in bioactive compounds, which has been utilized widely in folk medicine, in food supplement and cosmetology areas because of its biological properties, ...(antibacterial, antiviral, antioxidant, anti-inflammatory, etc.). The subject of this study is associated with the chemical analysis and the biological evaluation of 16 propolis samples from the northeast Aegean region Greek islands, a well-recognized geographic area and the homeland of rich flora as a crossroads between Europe and Asia. Our study resulted in the detection of a significant percentage of diterpenes by gas chromatography-mass spectrometry (GC-MS), while flavonoids were identified in low percentages among studied samples. Furthermore, the DPPH assay highlighted that eight of the samples (Lesvos and Lemnos origin) demonstrated a promising antioxidant profile, further verified by their total phenolic content (TPC). Additionally, the propolis samples most rich in diterpenes showed significant antibacterial and fungicidal properties against human pathogenic microorganisms, proving them to be a very interesting and promising crude material for further applications, concluding that floral diversity is the most responsible for the bioactivity of the propolis samples.
Thiazolin-4-ones and their derivatives represent important heterocyclic scaffolds with various applications in medicinal chemistry. For that reason, the synthesis of two 5-substituted ...thiazolidin-4-one derivatives was performed. Their structure assignment was conducted by NMR experiments (2D-COSY, 2D-NOESY, 2D-HSQC and 2D-HMBC) and conformational analysis was conducted through Density Functional Theory calculations and 2D-NOESY. Conformational analysis showed that these two molecules adopt exo conformation. Their global minimum structures have two double bonds (C=N, C=C) in Z conformation and the third double (C=N) in E. Our DFT results are in agreement with the 2D-NMR measurements. Furthermore, the reaction isomerization paths were studied via DFT to check the stability of the conformers. Finally, some potential targets were found through the SwissADME platform and docking experiments were performed. Both compounds bind strongly to five macromolecules (triazoloquinazolines, mglur3, Jak3, Danio rerio HDAC6 CD2, acetylcholinesterase) and via SwissADME it was found that these two molecules obey Lipinski’s Rule of Five.
Throughout centuries, traditional herbal medicine and the employment of medicinal plants have constituted an important tool for the treatment and prevention of numerous diseases. The present study ...focuses on the collection of ethnopharmacological data regarding the uses of medicinal plants for the treatment of dermatological ailments in various villages of Mount Pelion, Greece. More specifically, the study area is represented by the city of Volos and villages located in Central West Pelion and has not been investigated up to now. The information on the medicinal uses of the various species was obtained through extensive semi-structured interviews or the completion of specific questionnaires by the informants. Although the Covid-19 pandemic caused difficulties and obstacles in carrying out this research procedure, 60 informants were recruited and interviewed (36 women and 24 men). Their age range was between 31 and 97 years and their educational level was characterized by great diversity (primary, secondary, and higher education). The elaboration of the gathered information included the calculation of some quantitative indices, such as Fidelity Level (FL), and Informant Consensus Factor (FIC). Moreover, the relative importance of each reported species was identified by calculating the Use Value (UV). The interviews revealed 38 plant taxa belonging to 27 plant families reported to be used in the study area exclusively against skin diseases. The plant family mostly mentioned by the informants was Hypericaceae, followed by Plantaginaceae and Amaryllidaceae, while among the most popular methods of application are cataplasms, compresses, and topical application of decoction or raw plant material. Some of the most cited species are
Hypericum perforatum
L.,
Quercus coccifera
L., and
Plantago
sp., traditionally used to treat skin problems such as eczema, wounds, and insect stings. The present ethnopharmacological study is the first documentation of ethnobotanical knowledge of this area that points out the traditional uses of medicinal plants against skin ailments.
In this study, the black fertile (BSs) and the red unfertile seeds (RSs) of the Greek endemic
subsp.
(Stearn) Tzanoud were studied for the first time. Nine phenolic derivatives,
-resveratol,
...-resveratrol-4'-O-β-d-glucopyranoside,
-
-viniferin,
-gnetin H, luteolin, luteolin 3'-O-β-d-glucoside, luteolin 3',4'-di-O-β-d-glucopyranoside, and benzoic acid, along with the monoterpene glycoside paeoniflorin, have been isolated and structurally elucidated. Furthermore, 33 metabolites have been identified from BSs through UHPLC-HRMS, including 6 monoterpene glycosides of the paeoniflorin type with the characteristic cage-like terpenic skeleton found only in plants of the genus
, 6 gallic acid derivatives, 10 oligostilbene compounds, and 11 flavonoid derivatives. From the RSs, through HS-SPME and GC-MS, 19 metabolites were identified, among which nopinone, myrtanal, and
-myrtanol have been reported only in peonies' roots and flowers to date. The total phenolic content of both seed extracts (BS and RS) was extremely high (up to 289.97 mg GAE/g) and, moreover, they showed interesting antioxidative activity and anti-tyrosinase properties. The isolated compounds were also biologically evaluated. Especially in the case of
-gnetin H, the expressed anti-tyrosinase activity was higher than that of kojic acid, which is a well-known whitening agent standard.
The aim of the present study was the phytochemical analysis of the aerial parts of
Mill., a herb from Boraginaceae plant family not previously studied. The methanol (ME) and aqueous extracts (WE) of ...the aerial parts were assayed for their total phenolic and flavonoid content and antioxidant properties, using free radical scavenging (DPPH, ABTS), reducing power (FRAP, CUPRAC), phosphomolybdenum and metal chelating assays. The extracts displayed considerable free radical scavenging activity against DPPH and ABTS radicals, with potential values of 46.88 and 68.31 mg TE/g extract for ME, and 93.43 and 131.48 mg TE/g extract for WE, respectively. Key clinical enzymes involved in neurodegenerative diseases AChE and BChE, diabetes (α-amylase and α-glucosidase) and skin whitening (tyrosinase) were also assayed. The phytochemical profile of the studied species was determined through UHPLC-HRMS, whereby 26 secondary metabolites were identified, three of which (luteolin-7-glucoside, lithospermic and rosmarinic acids) were isolated and structurally determined by NMR spectral means.
was found to harbor bioactive metabolites and could, hence, serve as a source of biological activities which could be further explored and exploited for potential applications.
The structure assignment and conformational analysis of the thiosemicarbazones, DKI21 and DKI24, were performed through homonuclear and heteronuclear 2D Nuclear Magnetic Resonance (NMR) spectroscopy ...(2D-COSY, 2D-NOESY, 2D-ROESY, 2D-HSQC, and 2D-HMBC) and quantum mechanics (QM) calculations, using Functional Density Theory (DFT). In addition, utilizing a combination of 2D-NOESY and 2D-ROESY spectra an exo structure was established for both of the analogs. This experimental results were confirmed by theoretical mechanistic studies, as the lowest minima conformations derived through DFT calculations were compatible with the spatial correlations observed in the 2D-NOESY and 2D-ROESY spectra. Finally, molecular binding experiments were performed to detect the potential targets for DKI21 and DKI24, derived from SwissAdme. In silico molecular binding experiments showed favorable binding energy values for the most of the enzymes studied. The ADMET calculations, using the preADMET and pKCSm software, showed that the two molecules appear as possible drug leads.
Organometallic complexes of the formula Ru(N^N)(p-cymene)ClX (N^N = bidentate polypyridyl ligands, p-cymene = 1-methyl-4-(1-methylethyl)-benzene, X = counter anion), are currently studied as possible ...candidates for the potential treatment of cancer. Searching for new organometallic compounds with good to moderate cytotoxic activities, a series of mononuclear water-soluble ruthenium(II)–arene complexes incorporating substituted pyridine–quinoline ligands, with pending -CH2OH, -CO2H and -CO2Me groups in the 4-position of quinoline ring, were synthesized, for the first time, to study their possible effect to modulate the activity of the ruthenium p-cymene complexes. These include the Ru(η6-p-cymene)(pqhyme)ClX (X = Cl− (1-Cl), PF6− (1-PF6), pqhyme = 4-hydroxymethyl-2-(pyridin-2-yl)quinoline), Ru(η6-p-cymene)(pqca)ClCl ((2-Cl), pqca = 4-carboxy-2-(pyridin-2-yl)quinoline), and Ru(η6-p-cymene)(pqcame)ClX (X = Cl− (3-Cl), PF6− (3-PF6), pqcame = 4-carboxymethyl-2-(pyridin-2-yl)quinoline) complexes, respectively. Identification of the complexes was based on multinuclear NMR and ATR-IR spectroscopic methods, elemental analysis, conductivity measurements, UV–Vis spectroscopic, and ESI-HRMS techniques. The solid-state structures of 1-PF6 and 3-PF6 have been elucidated by single-crystal X-ray diffraction revealing a three-legged piano stool geometry. This is the first time that the in vitro cytotoxic activities of these complexes are studied. These were conducted in HEK293T (human embryonic kidney cells) and HeLa cells (cervical cancer cells) via the MTT assay. The results show poor in vitro anticancer activities for the HeLa cancer cell lines and 3-Cl proved to be the most potent (IC50 > 80 μΜ). In both cell lines, the cytotoxicity of the ligand precursor pqhyme is significantly higher than that of cisplatin.
Chemical composition of propolis depends on the plant source and thus on the geographic and climatic characteristics of the site of collection. The aim of this study was to investigate the chemical ...profile of Greek and Chinese propolis extracts from different regions and suggest similarities and differences between them. Untargeted ultrahigh-performance liquid chromatography coupled to hybrid quadrupole-Orbitrap mass spectrometry (UHPLC-HRMS) method was developed and 22 and 23 propolis samples from Greece and China, respectively, were analyzed. The experimental data led to the observation that there is considerable variability in terms of quality of the distinctive propolis samples. Partial least squares - discriminant analysis (PLS-DA) and orthogonal partial least squares-discriminant analysis (OPLS-DA) models were constructed and allowed the identification of significant features for sample discrimination, adding relevant information for the identification of class-determining metabolites. Chinese samples overexpressed compounds that are characteristic of the poplar type propolis, whereas Greek samples overexpress the latter and the diterpenes characteristic of the Mediterranean propolis type.
A review research was conducted to provide an overview of the ethnobotanical knowledge of medicinal plants and traditional medical practices for the treatment of skin disorders in Albania, Cyprus, ...Greece, and Turkey. The geographical and ecological characteristics of the Balkan Peninsula and Mediterranean Sea, along with the historical connection among those countries, gave rise to the development of a distinct flora and to the uses of common medicinal plants against various skin ailments, respectively. The review focuses on the detailed study of 128 ethnobotanical surveys conducted in these areas and the species used for skin ailments were singled out. The analysis showed that 967 taxa belonging to 418 different genera and 111 different families are used in the treatment of skin related problems. The majority of the plants belong to the families of Asteraceae (11.7%), Lamiaceae (7.4%), Rosaceae (6.7%), Plantaginaceae (5.4%), and Malvaceae (3.8%). Their usage is internal or external to treat ailments such as wounds and burns (22.1%), hemorrhoids (14.7%), boils, abscesses, and furuncles (8.2%). Beside specific skin disorders, numerous species appeared to be used for their antifungal, antimicrobial, and antiseptic activity (9.1%). Literature evaluation highlighted that, the most commonly used species are
Plantago major
L. (Albania, Turkey),
Hypericum perforatum
L. (Greece, Turkey),
Sambucus nigra
L. (Cyprus, Greece),
Ficus carica
L. (Cyprus, Turkey),
Matricaria chamomilla
L. (Cyprus, Greece), and
Urtica dioica
L. (Albania, Turkey), while many medicinal plants reported by interviewees were common in all four countries. Finally, to relate this ethnopharmacological knowledge and trace its expansion and diversification through centuries, a comparison of findings was made with the use of the species mentioned in Dioscorides’ “
De Materia Medica”
for skin disorders. This work constitutes the first comparative study performed with ethnobotanical data for skin ailments gathered in the South Balkan and East Mediterranean areas. Results confirm the primary hypothesis that people in Albania, Cyprus, Greece, and Turkey are closely related in terms of traditionally using folk medicinal practices. Nevertheless, more field studies conducted, especially in remote places of these regions, can help preserve the traditional medical knowledge, aiming at the discovery of new phytotherapeutics against dermatological diseases.
The volatiles of different aerial parts of three kumquat species (Fortunella margarita Swingle–Nagami, Fortunella japonica Swingle–Marumi, and Fortunella crassifolia Swingle–Meiwa) growing in Greece ...were analyzed via GC-MS and evaluated for their antimicrobial properties against nine human pathogenic microorganisms. A total number of 23 compounds were identified in the peel, 38 in the leaves, and 30 in the flowers of the examined species. Limonene was the dominant metabolite in the peels of all three species, germacrene-D was present in the leaves of Nagami and Marumi kumquats, while limonene was the most abundant in the flower of Marumi and Meiwa kumquat but with significant differences in the composition of the total fracture of the essential oil, since compounds with high antimicrobial activity were only present in the flower of Meiwa kumquat. The essential oils from the leaf and peel of the three kumquat species were either inactive or showed weak antimicrobial activity, respectively, against Gram-positive and Gram-negative bacterial strains and pathogenic fungi. Only the essential oil from the flower of F. crassifolia Swingle (Meiwa) showed a stronger effect (MIC values 3.5–7.48 mg/mL) against all the assayed microorganisms. Furthermore, through multivariate statistical analysis, we studied the relationships between the samples regarding their origin (species and plant part), as well as between the chemical composition of the corresponding essential oils and their antimicrobial activity. Considering its chemical profile and antimicrobial activity, the Greek Meiwa flowers’ essential oil seemed a promising essential oil for further exploitation in the food and/or medicinal industry.
PDF
