Liposomal and Nanostructured Lipid Nanoformulations of a Pentacyclic Triterpenoid Birch Bark Extract: Structural Characterization and In Vitro Effects on Melanoma B16-F10 and Walker 256 Tumor Cells Apoptosis.

: Pentacyclic triterpenoids are increasingly studied as anticancer agents with many advantages compared to synthetic chemotherapeutics. The aim of this study was to prepare liposomal and nanostructured lipid formulations including a standardized extract of silver birch () outer bark (TTs) and to evaluate their potential as anticancer agents in vitro, using Melanoma B16-F10 and Walker carcinoma cells. : Appropriate solvents were selected for efficient TTs extraction, and original recipes were used to obtain Pegylated liposomes and nanolipid complexes with entrapped TTs, comparative to pure standards (betulinic acid and doxorubicin) in similar conditions.

Stability and Bioaccessibility of Carotenoids from Sea Buckthorn Pomace Encapsulated in Alginate Hydrogel Beads.

Carotenoids, the natural pigments that confer the bright orange color of sea buckthorn berries, are also associated with several health benefits, such as antioxidant activity and skin and eye protection. Due to their lipophilic nature and localization, carotenoids are largely retained in the sea buckthorn pomace (SBP) resulting from juice production. Carotenoids from SBP (70.

Sonochemical synthesis, optical properties and DFT studies on novel (N-arylamino)phenothiazinium dyes suitable for fluorescence cells imaging.

Novel (N-arylamino)phenothiazinium dyes containing meta-substituted-arylamine auxochrome units were successfully obtained by applying a sonochemical protocol designed for a more efficient energy usage in the preparation of methylene blue (MB) analogues. Single crystal X-ray diffraction analysis revealed the spatial arrangement in aggregated crystalline state of (N-(meta-bromoaryl)amino)phenothiazinium dye with minor variances induced by the nature of the halogenide counterion (iodide or chloride). The optical UV-vis properties of the novel (N-arylamino)phenothiazinium dyes were comparable to those of the parent MB, with the longest wavelength absorption maxima situated in the visible range (640-680 nm), large molar extinction coefficients (log ε = 4.

Antioxidant, Enzyme Inhibitory, and Protective Effect of Extract.

The present study aimed to investigate the chemical content of Romanian juneberries (), their effect on antioxidant and enzyme inhibition activities, and their bioaccessibility after simulated in-vitro digestion. In extract (AME), 16 polyphenolic compounds were identified by LC-ESI+-MS analysis. The most representative compounds found in the extract were cyanidin-galactoside, 3,4-dihydroxy-5-methoxybenzoic acid, feruloylquinic acid, and kaempferol, all belonging to the anthocyanins, phenolic acids, and flavonols subclasses.

Pentacyclic Triterpenoid Phytochemicals with Anticancer Activity: Updated Studies on Mechanisms and Targeted Delivery.

Pentacyclic triterpenoids (TTs) represent a unique family of phytochemicals with interesting properties and pharmacological effects, with some representatives, such as betulinic acid (BA) and betulin (B), being mainly investigated as potential anticancer molecules. Considering the recent scientific and preclinical investigations, a review of their anticancer mechanisms, structure-related activity, and efficiency improved by their insertion in nanolipid vehicles for targeted delivery is presented. A systematic literature study about their effects on tumor cells in vitro and in vivo, as free molecules or encapsulated in liposomes or nanolipids, is discussed.

NIR photothermal-activable drug-conjugated microcapsules for in vitro targeted delivery and release: An alternative treatment of diabetic retinopathy.

Diabetic retinopathy (DR) is one of the most serious complications of diabetes, which leads to blindness. By addressing the traditional treatment limitations, we developed a novel light-responsive targeted polymeric microcapsule able to encapsulate a near infrared (NIR) photoactive fluorophore - Indocyanine Green, owing to its photothermal properties. Moreover, for an efficient in vitro targeted drug delivery, the fluorescent microsystem was conjugated with a therapeutic agent, i.

Resveratrol: Its Path from Isolation to Therapeutic Action in Eye Diseases.

Due to the confirmed therapeutic potential of resveratrol (Rv) for eye diseases, namely its powerful anti-angiogenic and antioxidant effects, this molecule must be studied more deeply. Nowadays, the pharmaceutic and pharmacokinetic available studies offer a troubling picture because of its low stability and bioavailability. To overcome this problem, researchers started to design and create different delivery systems that could improve the delivery amount of Rv.

Hybrid polymeric therapeutic microcarriers for thermoplasmonic-triggered release of resveratrol.

Diabetic retinopathy (DR) is a severe ocular complication that causes retinal damage, being one of the leading causes of blindness globally, thus the development of new strategies to prevent and treat DR as well as other degenerative diseases is highly desired. This work is focused on the design and fabrication of an ingenious model of polymeric microcapsules (MC) for controlled drug delivery in human retina cells able to carry therapeutic resveratrol (RSV) molecules in tandem with active anisotropic gold bipyramidal nanoparticles (AuBPs) as efficient photothermal agents. Specifically, MC were developed via a Layer-by-Layer deposition technique, by successively adding oppositely charged polyelectrolytes on a RSV-conjugated calcium carbonate (CaCO) core.

Anthocyanins as Key Phytochemicals Acting for the Prevention of Metabolic Diseases: An Overview.

Anthocyanins are water-soluble pigments present in fruits and vegetables, which render them an extensive range of colors. They have a wide distribution in the human diet, are innocuous, and, based on numerous studies, have supposed preventive and therapeutical benefits against chronic affections such as inflammatory, neurological, cardiovascular, digestive disorders, diabetes, and cancer, mostly due to their antioxidant action. Despite their great potential as pharmaceutical applications, they have a rather limited use because of their rather low stability to environmental variations.

Real-time fluorescence imaging of anthocyanins complexed with diphenylboric acid 2-aminoethyl inside B16-F10 melanoma cells.

Anthocyanins (AN), natural compounds daily consumed by humans, have outstanding therapeutical potential if administered topically in melanoma pathology. However, the search for efficient therapy development is still in progress, owing to the lack of complete understanding of the AN intracellular path, once they are uptaken by the cells. This target is constrained by the need for an imaging strategy that would enable their intracellular detection and localization in-situ.

Fluorescent Polyelectrolyte System to Track Anthocyanins Delivery inside Melanoma Cells.

Over the past decades, there has been a growing interest in using natural molecules with therapeutic potential for biomedical applications. In this context, our aim is focused on anthocyanins (AN) as molecules with anticancer properties that could be used in melanoma local therapies. Due to their susceptibility to environmental changes, current study is based on the design and development of a fluorescent system for carrying and trafficking AN inside melanoma cells.

Novel (Phenothiazinyl)Vinyl-Pyridinium Dyes and Their Potential Applications as Cellular Staining Agents.

We report here the synthesis and structural characterization of novel cationic (phenothiazinyl)vinyl-pyridinium (PVP) dyes, together with optical (absorption/emission) properties and their potential applicability as fluorescent labels. Convective heating, ultrasound irradiation and mechanochemical synthesis were considered as alternative synthetic methodologies proficient for overcoming drawbacks such as long reaction time, nonsatisfactory yields or solvent requirements in the synthesis of novel dye (E)-1-(3-chloropropyl)-4-(2-(10-methyl-10H-phenothiazin-3-yl)vinyl)pyridin-1-ium bromide and its -alkyl-2-methylpyridinium precursor . The geometry of the newly synthesized (E)-4-(2-(7-bromo-10-ethyl-10H-phenothiazin-3-yl)vinyl)-1-methylpyridin-1-ium iodide and (E)-1-methyl-4-(2-(10-methyl-10H-phenothiazin-3-yl)vinyl)pyridin-1-ium tetrafluoroborate was confirmed by single crystal X-ray diffraction.

Comparative analysis of some bioactive compounds in leaves of different Aloe species.

Although a vast number of Aloe species are known, only the Aloe vera and Aloe arborescens species are currently used by cosmetic and pharmaceutical industries. Therefore, the current study aims to complete the existent literature data with new information on the phytochemical composition of some lesser-known Aloe species, with the main focus on carotenoids and fatty acids. Among the analyzed species, Aloe aculeata and Aloe ferox had the highest content in carotenoids, the major pigments being lutein and β-carotene (according to HPLC analysis).

ICG-loaded gold nano-bipyramids with NIR activatable dual PTT-PDT therapeutic potential in melanoma cells.

A great amount of effort is directed towards the progress of cancer treatment approaches aspiring to develop non-invasive, targeted and highly efficient therapies. In this context, Photothermal (PTT) and Photodynamic (PDT) Therapies were proven as promising. This work aims to integrate the therapeutic activities of two near-infrared (NIR) photoactive biomaterials - gold nano-bipyramids (AuBPs) and Indocyanine Green (ICG) - into one single targeted hybrid nanosystem able to operate as dual PTT-PDT agent with higher efficiency compared with each one alone.

Cellular Internalization of Beta-Carotene Loaded Polyelectrolyte Multilayer Capsules by Raman Mapping.

Raman mapping is becoming a very useful tool in investigating cells and cellular components, as well as bioactive molecules intracellularly. In this study, we have encapsulated beta-carotene using a layer-by-layer technique, as a way to enhance its stability and bioavailability. Further, we have used Raman mapping to characterize the as-obtained capsules and monitor their uptake by the human retinal epithelial D407 cells.

Sea Buckthorn Oil as a Valuable Source of Bioaccessible Xanthophylls.

Sea buckthorn oil, derived from the fruits of the shrub, also termed seaberry or sandthorn, is without doubt a strikingly rich source of carotenoids, in particular zeaxanthin and β-carotene. In the present study, sea buckthorn oil and an oil-in-water emulsion were subjected to a simulated gastro-intestinal in vitro digestion, with the main focus on xanthophyll bioaccessibility. Zeaxanthin mono- and di-esters were the predominant carotenoids in sea buckthorn oil, with zeaxanthin dipalmitate as the major compound (38.

Warfarin-Capped Gold Nanoparticles: Synthesis, Cytotoxicity, and Cellular Uptake.

Currently, research studies on nanoparticle cytotoxicity, uptake or internalization into the body's cells are of great interest for the improvement of diagnostic and therapeutic applications. We report here the synthesis and characterization of very stable novel warfarin-capped gold nanoparticles with an average diameter of 54 ± 10 nm which were prepared using sodium warfarin as a reducing agent. The nanoparticles were tested in terms of cytotoxicity and cellular internalization in vitro on two cell lines: normal lung fibroblast HFL-1 and human retinal pigment epithelial D407 cells.

Phytochemical Characterization of Commercial Processed Blueberry, Blackberry, Blackcurrant, Cranberry, and Raspberry and Their Antioxidant Activity.

Being delicious and containing strong disease-fighting agents, berries represent an increasing proportion of fruits consumed nowadays in our diet. However, berries are highly perishable as fresh and, therefore, they are usually processed into various products to extend their shelf-life and availability throughout the year. Among the fruit-containing products, jam is one of the most common due to its nourishing properties, its low production costs, and its accessibility for a lengthy period.

Resveratrol-delivery vehicle with anti-VEGF activity carried to human retinal pigmented epithelial cells exposed to high-glucose induced conditions.

As an integrated approach to defeat diabetic retinopathy, a common complication of diabetes leading to vision loss, a delivery vehicle able to transport resveratrol (Rv) directly into retina pigmented epithelial D407 cells was designed. Rv, a molecule with known therapeutic potential, was successfully inserted into a microcapsule based on porous CaCO templates revealing an encapsulation efficiency of 96.8 ± 4.

Antiangiogenic cytokines as potential new therapeutic targets for resveratrol in diabetic retinopathy.

Diabetes mellitus (DM) affects >350 million people worldwide. With many complications that can reduce the patient's quality of life, vision loss is one of the most debilitating disorders it can cause. Active research in the field of diabetes includes microvascular complications in diabetic retinopathy (DR).

Melanoma Inhibition by Anthocyanins Is Associated with the Reduction of Oxidative Stress Biomarkers and Changes in Mitochondrial Membrane Potential.

Anthocyanins are water soluble pigments which have been proved to exhibit health benefits. Several studies have investigated their effects on several types of cancer, but little attention has been given to melanoma. The phytochemical content of nine different berry samples was assessed by liquid chromatography followed by electrospray ionization mass spectrometry (LC-ESI-MS).

Antiproliferative and Apoptotic Potential of Cyanidin-Based Anthocyanins on Melanoma Cells.

Elderberries are known for their high anthocyanins content, which have been shown to possess anti-proliferative and anti-cancer effects. Anthocyanins enriched extract (AEE) was obtained from elderberries and was characterized by LC/DAD/ESI-MS analysis. Five cyanidin-based anthocyanins were identified, among which Cy-3--samb was the major compound (51%).

Chokeberry Anthocyanin Extract as Pancreatic β-Cell Protectors in Two Models of Induced Oxidative Stress.

The aim of this study was to investigate the protective effects of a chokeberry anthocyanin extract (CAE) on pancreatic β-cells (βTC3) exposed to hydrogen peroxide- (H2O2-) and high glucose- (HG-) induced oxidative stress conditions. In order to quantify individual anthocyanins high performance liquid chromatography (HPLC) coupled to photodiode array (PDA) was used. The identification of the fragment ion pattern of anthocyanins was carried out by electrospray ionization mass spectrometry (LC-ESI-MS).

Antiproliferative and antioxidant properties of anthocyanin rich extracts from blueberry and blackcurrant juice.

The present study was aimed at evaluating the antiproliferative potential of anthocyanin-rich fractions (ARFs) obtained from two commercially available juices (blueberry and blackcurrant juices) on three tumor cell lines; B16F10 (murine melanoma), A2780 (ovarian cancer) and HeLa (cervical cancer). Individual anthocyanin determination, identification and quantification were done using HPLC-MS. Antioxidant activity of the juices was determined through different mechanism methods such as DPPH and ORAC.