Propolis Extracts Inhibit UV-Induced Photodamage in Human Experimental In Vitro Skin Models

The aim of this study was to assess the antioxidant, photoprotective, and antiaging effects of Greek propolis. Propolis was subjected to n-heptane or methanol extraction. Total phenolic/flavonoid content and antioxidant potential were determined in the extracts. Promising extracts were evaluated for their cytoprotective properties using human immortalized keratinocyte (HaCaT) or reconstituted human skin tissue following exposure to UVB. Assessment of cytotoxicity, DNA damage, oxidative status, and gene/protein expression levels of various matrix metalloproteinases (MMPs) were performed. The propolis methanolic fractions exhibited higher total phenolic and flavonoid contents and significant in vitro antioxidant activity. Incubation of HaCaT cells with certain methanolic extracts significantly decreased the formation of DNA strand breaks following exposure to UVB and attenuated UVB-induced decrease in cell viability. The extracts had no remarkable effect on the total antioxidant status, but significantly lowered total protein carbonyl content used as a marker for protein oxidation in HaCaT cells. MMP-1, -3, -7, and -9, monitored as endpoints of antiaging efficacy, were significantly reduced by propolis following UVB exposure in a model of reconstituted skin tissue. In conclusion, propolis protects against the oxidative and photodamaging effects of UVB and could be further explored as a promising agent for developing natural antiaging strategies

Toxicity Profiling of Biosurfactants Produced by Novel Marine Bacterial Strains

Surface active agents (SAAs), currently used in modern industry, are synthetic chemicals produced from non-renewable sources, with potential toxic impacts on humans and the environment. Thus, there is an increased interest for the identification and utilization of natural derived SAAs. As such, the marine environment is considered a promising source of biosurfactants with low toxicity, environmental compatibility, and biodegradation compared to their synthetic counterparts. MARISURF is a Horizon 2020 EU-funded project aiming to identify and functionally characterize SAAs, derived from a unique marine bacterial collection, towards commercial exploitation. Specifically, rhamnolipids produced by Marinobacter MCTG107b and Pseudomonas MCTG214(3b1) strains were previously identified and characterized while currently their toxicity profile was assessed by utilizing well-established methodologies. Our results showed a lack of cytotoxicity in in vitro models of human skin and liver as indicated by alamar blue and propidium iodide assays. Additionally, the use of the single gel electrophoresis assay, under oxidative stress conditions, revealed absence of any significant mutagenic/anti-mutagenic potential. Finally, both 2,2’-azino-bis (3-ethylbenzothiazoline-6-sulphonicacid) (ABTS) and 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) cell-free assays, revealed no significant anti-oxidant capacity for neither of the tested compounds. Consequently, the absence of significant cytotoxicity and/or mutagenicity justifies their commercial exploitation and potential development into industrial end-user applications as natural and environmentally friendly biosurfactants

Application of the technology of liposomes and dendrimers in the design and study of new chimeric nanosystems for the delivery of the anticancer drug doxorubicin

A plethora of drug molecules with significant biological activity, both in vitro and in vivo, have been found to be inactive during clinical trials. Nanotechnology seems to be the multiscientific field that will permit the clinical application of many of the above molecules. The formulation of a drug molecule with nanocarriers may alter the ADME (Administration, bioDistribution, Metabolism, Exertion) profile of the drug to a large extent. A new approach for nanocarrier design is the development of chimeric drug delivery systems that result from the combination of nanoparticles. The main representative category of chimeric drug delivery systems is liposomal locked-in dendrimers (LLDs) that result from the combination of liposomes and dendrimers. LLDs have been successfully developed in the past but there is a gap in the literature concerning the interactions of the parts of the final nanocarrier; information that is necessary for the rational design of such nanosystems. In the present study two new polyester-polyether dendrimers of generation one and two were synthesized. These dendrimers, as well as generation 3,5 commercial polyamidoamine (PAMAM) dendrimer, were incorporated into lipid bilayers or liposomes consisting of dipalmitoyl phosphatidylcholine and phosphatidylglcerol (DPPC-DPPG) and the interactions between dendrimers and lipids were studied with methods of thermal analysis, Raman spectroscopy and fluorescence spectroscopy. The derived information served as a basis for the incorporation of dendrimers into liposomes of various compositions and the final products (LLDs) were subjected to lyophilization. After reconstitution, the anticancer drug doxorubicin was loaded to both pure liposomes and LLDs and the interaction of the components of the final nanosystem, the in vitro release of doxorubicin and the in vitro pharmacological activity against human breast cancer cell lines were evaluated. The results that concern the interaction of the components of the nanocarrier were evaluated as very important and were correlated to the doxorubicin release rate.LLDs seem to be a very promising category of chimeric drug delivery systems. The rational choice of dendrimers and lipidic composition of liposomes may lead to original drug delivery sytems of the LLD category that may present controlled release rate and enhanced therapeutic index. The understanding of the dynamics and kinetics of the components of the LLD nanocarriers with thermal analysis and spectroscopic methods may lead to the development of novel drugs against cancer and other diseases.Μια πληθώρα φαρμακομορίων με σημαντική βιολογική δράση, τόσο in vitro όσο και in vivo, έχουν αποδειχτεί ανενεργά κατά τη διάρκεια των κλινικών δοκιμών. Η νανοτεχνολογία φαίνεται να είναι το διεπιστημονικό πεδίο το οποίο θα επιτρέψει την κλινική χρήση πολλών από αυτά τα μόρια καθώς η μορφοποίησή τους σε νανοφορείς μπορεί να μεταβάλλει σε μεγάλο βαθμό τα χαρακτηριστικά των φαρμακομορίων που σχετίζονται με την απορρόφηση, τη βιοκατανομή, το μεταβολισμό και την απέκκρισή τους από τον οργανισμό. Μία νέα προσέγγιση δημιουργίας νανοφορέων σε αυτή την κατεύθυνση είναι η ανάπτυξη χιμαιρικώνσυστημάτων μεταφοράς φαρμάκων, η οποία προκύπτει από το συνδυασμό νανοσωματιδίων. Κύριος εκπρόσωπος των χιμαιρικών συστημάτων μεταφοράς φαρμακομορίων είναι τα Λιποσωμιακά Εγκλεισμένα Δενδριμερή (ΛΕΔ) που προκύπτουν από το συνδυασμό ιποσωμάτων και δενδριμερών. Τα ΛΕΔ έχουν παρασκευαστεί με επιτυχία στο παρελθόν αλλά υπάρχει σημαντικό κενό στη βιβλιογραφία όσον αφορά τις αλληλεπιδράσεις των επιμέρους συστημάτων του τελικού νανοφορέα του φαρμακομορίου, πληροφορία απαραίτητη για τον ορθολογικό σχεδιασμό του.Στην παρούσα μελέτη έγινε σύνθεση νέων πολυεστερικών-πολυαιθερικών δενδριμερών πρώτης και δεύτερης γενιάς. Τα δενδριμερή αυτά, καθώς και το εμπορικό δενδριμερές της οικογένειας των πολυαμιδοαμινών (ΡΑΜΑΜ) γενιάς 3,5 ενσωματώθηκαν σε λιπιδικές διπλοστιβάδες ή λιποσώματα αποτελούμενα από διπαλμιτική φωσφατιδυλοχολίνη και φωσφατιδυλογλυκερόλη (DPPC-DPPG) και μελετήθηκαν οι αλληλεπιδράσεις δενδριμερών-λιπιδίων με μεθόδους θερμικής ανάλυσης, φασματοσκοπίας Raman και φασματοσκοπίας φθορισμού. Με βάση τις πληροφορίες που προέκυψαν, τα δενδριμερή ενσωματώθηκαν σε λιποσώματα διαφόρων συστάσεων και τα τελικά προϊόντα (ΛΕΔ) λυοφιλοποιήθηκαν. Μετά την ανάκτηση των ΛΕΔ από τα λυοφιλοποιημένα προϊόντα έγινε εγκλωβισμός του αντικαρκινικού φαρμάκου δοξορουβικίνη. Αξιολογήθηκε τόσο η αλληλεπίδραση των συστατικών του τελικού νανοφορέα ΛΕΔ όσο και η in vitro αποδέσμευση της δοξορουβικίνης και η in vitro φαρμακολογική δράση των σκευασμάτων σε ανθρώπινες καρκινικές σειρές. Τα αποτελέσματα που αφορούν την αλληλεπίδραση των συστατικών του νανοφορέα αξιολογήθηκαν ως πολύ σημαντικά και συσχετίστηκαν με το ρυθμό αποδέσμευσης της δοξορουβικίνης. Τα ΛΕΔ αποτελούν μία πολλά υποσχόμενη κατηγορία χιμαιρικών συστημάτων μεταφοράς φαρμακομορίων. Η ορθολογική επιλογή των δενδριμερών και της λιπιδικής σύστασης των λιποσωμάτων μπορεί να οδηγήσει στη δημιουργία πρωτότυπων συστημάτων μεταφοράς φαρμακομορίων της κατηγορίας των ΛΕΔ τα οποία να εμφανίζουν ελεγχόμενη αποδέσμευση και βελτιωμένη θεραπευτική αποτελεσματικότητα. Η κατανόηση της δυναμικής αλλά και της κινητικής των επιμέρους συστημάτων των ΛΕΔ νανοφορέων με μεθόδους θερμικής ανάλυσης και φασματοσκοπίας μπορεί να οδηγήσει στον σχεδιασμό καινοτόμων φαρμάκων κατάτου καρκίνου αλλά και άλλων νόσων

Medicinal plants in the treatment of skin diseases in Serbia during 19th and 20th century

The purpose of this study was to collect and analyse plant-based treatments applied in Serbian folk medicine for treating skin disorders during the nineteenth and early to mid-twentieth century. We have consulted the most relevant ethnographic literature that was in any larger segment devoted to the folk medicine. This investigation has identified 164 plant species from 63 families and one mushroom species as being applied in the treatment of ailments categorized as skin diseases in the International Classification of Primary Care. Frequently used families were: Asteraceae (14 taxa), Lamiaceae (13 taxa), Solanaceae (10 taxa) and Rosaceae (8 taxa). Among plant parts leaves were the most utilized (21%) followed by aerial parts, roots, fruits and seeds. Mostly plant species were applied externally (60.98%), 9.15% of mentioned species were used both internally and externally and 4.27% were administered only externally. Herbs were processed and taken in different ways and forms, both fresh and dry. As fresh they were directly applied, or previously mashed and mixed with water, milk, vinegar, oil, honey, lard and butter. In case of Arnica montana, Fumaria officinalis, Galium verum, and Conium maculatum juice squeezed from fresh parts of the plants was used. Skin problems recorded in our investigation could be divided in three main categories: hair problems, bites and inflammatory skin diseases such as eczema, psoriasis etc. After comparison with contemporary ethnobotanical investigations conducted on the territory of Serbia, we observed that significantly lower number of plant species was recorded in modern studies

Innovative Delivery Systems Loaded with Plant Bioactive Ingredients: Formulation Approaches and Applications

Plants constitute a rich source of diverse classes of valuable phytochemicals (e.g., phenolic acids, flavonoids, carotenoids, alkaloids) with proven biological activity (e.g., antioxidant, anti-inflammatory, antimicrobial, etc.). However, factors such as low stability, poor solubility and bioavailability limit their food, cosmetics and pharmaceutical applications. In this regard, a wide range of delivery systems have been developed to increase the stability of plant-derived bioactive compounds upon processing, storage or under gastrointestinal digestion conditions, to enhance their solubility, to mask undesirable flavors as well as to efficiently deliver them to the target tissues where they can exert their biological activity and promote human health. In the present review, the latest advances regarding the design of innovative delivery systems for pure plant bioactive compounds, extracts or essential oils, in order to overcome the above-mentioned challenges, are presented. Moreover, a broad spectrum of applications along with future trends are critically discussed

Photometric Analysis of Propolis from the Island of Samothraki, Greece. The Discovery of Red Propolis

Propolis presents notable and variable antioxidant activity depending on the territory and the local flora. As a result, propolis collected from areas presenting botanical diversity can become an intriguing research field. In the present study, we examined propolis from different areas of Samothraki, a small Greek island in the north-eastern Aegean Sea, considered a hot-spot of plant biodiversity. The analysis of propolis samples presented huge variability in the antioxidant activity, the total polyphenol content and the total flavonoids content. Propolis from two areas presented high antioxidant activity with a maximum at 1741.48 μmol of Trolox equivalents per gram of dry propolis weight, very high polyphenol content, 378.73 mg of gallic acid equivalents per gram of dry propolis weight, and high flavonoid content with a maximum concentration of 70.31 mg of quercetin equivalents per gram of dry propolis weight. The samples that presented the best qualitative characteristics were all red propolis which is a type that has never been reported in any part of Europe

Green extraction of caffeine from coffee pulp using a deep eutectic solvent (DES)

The objective of this work was the development of a green extraction method based on the use of a deep eutectic solvent (DES) to extract caffeine from coffee pulp (CP). Choline chloride and glycerol were used as hydrogen bond acceptor and hydrogen bond donor, respectively. ATR-FTIR and viscosity measurements were conducted for the characterization of DES mixtures. The effects of DES mixtures concentration (CDES), liquid-to-solid ratio (L/S), extraction temperature (T) on caffeine extraction yield (CCaf) and extract antiradical activity (AAR) were studied, and the extraction process was optimized. The optimum of extraction was achieved at a temperature of 55 °C, a solvent/pulp ratio of 47 mL/g, and a DES concentration of 70% w/v in aqueous solution. In addition, a mathematical model to describe the kinetic mechanisms of the extraction was developed, whereas the dependence of the best descriptive model constants on extraction variables was expressed by an appropriate model. These results would offer scientific reference for promoting the valorization of coffee pulp

Royal Jelly Components Encapsulation in a Controlled Release System—Skin Functionality, and Biochemical Activity for Skin Applications

Royal jelly is a yellowish-white substance with a gel texture that is secreted from the hypopharyngeal and mandibular glands of young worker bees. It consists mainly of water (50–56%), proteins (18%), carbohydrates (15%), lipids (3–6%), minerals (1.5%), and vitamins, and has many beneficial properties such as antimicrobial, anti-inflammatory, anticancer, antioxidant, antidiabetic, immunomodulatory, and anti-aging. Royal jelly has been used since ancient times in traditional medicine, cosmetics and as a functional food due to its high nutritional value. The main bioactive substances are royalactin, and 10-hydroxy-2-decenoic acid (10-HDA). Other important bioactive molecules with antioxidant and photoprotective skin activity are polyphenols. However, they present difficulties in extraction and in use as they are unstable physicochemically, and a higher temperature causes color change and component degradation. In the present study, a new encapsulation and delivery system consisting of liposomes and cyclodextrins incorporating royal jelly has been developed. The new delivery system aims to the elimination of the stability disadvantages of royal jelly’s sensitive component 10-HDA, but also to the controlled release of its ingredients and, more particularly, 10-HDA, for an enhanced bioactivity in cosmeceutical applications

Cyclodextrins for the Delivery of Bioactive Compounds from Natural Sources: Medicinal, Food and Cosmetics Applications

Cyclodextrins have gained significant and established attention as versatile carriers for the delivery of bioactive compounds derived from natural sources in various applications, including medicine, food and cosmetics. Their toroidal structure and hydrophobic cavity render them ideal candidates for encapsulating and solubilizing hydrophobic and poorly soluble compounds. Most medicinal, food and cosmetic ingredients share the challenges of hydrophobicity and degradation that can be effectively addressed by various cyclodextrin types. Though not new or novel—their first applications appeared in the market in the 1970s—their versatility has inspired numerous developments, either on the academic or industrial level. This review article provides an overview of the ever-growing applications of cyclodextrins in the delivery of bioactive compounds from natural sources and their potential application benefits