Rosehip Extract-Loaded Liposomes for Potential Skin Application: Physicochemical Properties of Non- and UV-Irradiated Liposomes

In the present study, rosehip (Rosa canina L.) extract was successfully encapsulated in phospholipid liposomes using a single-step procedure named the proliposome method. Part of the obtained liposomes was subjected to UV irradiation and non-treated (native) and UV-irradiated liposomes were further characterized in terms of encapsulation efficiency, chemical composition (HPLC analysis), antioxidant capacity, particle size, PDI, zeta potential, conductivity, mobility, and antioxidant capacity. Raman spectroscopy as well as DSC analysis were applied to evaluate the influence of UV irradiation on the physicochemical properties of liposomes. The encapsulation efficiency of extract-loaded liposomes was higher than 90%; the average size was 251.5 nm; the zeta potential was -22.4 mV; and the conductivity was found to be 0.007 mS/cm. UV irradiation did not cause a change in the mentioned parameters. In addition, irradiation did not affect the antioxidant potential of the liposome-extract system. Raman spectroscopy indicated that the extract was completely covered by the lipid membrane during liposome entrapment, and the peroxidation process was minimized by the presence of rosehip extract in liposomes. These results may guide the potential application of rosehip extract-loaded liposomes in the food, pharmaceutical, or cosmetic industries, particularly when liposomal sterilization is needed

‐sitosterol and gentisic acid loaded 1,2‐dipalmitoyl‐sn‐glycero‐3‐phosphocholine liposomal particles

The aim of the present study was the examination of the impact of -sitosterol andgentisic acid on the characteristics of 1,2-dipalmitoyl-sn-glycero-3-phosphocholine(DPPC) liposomal particles: (a) bilayer permeability (fluorescence spectroscopy),(b) particle size, polydispersity index (PDI) and zeta potential (photon correlationspectroscopy) and (c) thermal properties (differential scanning calorimetry). -sitosterol induced the increase of liposomal bilayer rigidity, due to rearranging ofthe phospholipid chains, while gentisic acid enhanced the membrane fluidity, dueto the reduced orderliness and the increase of phospholipid dynamics. The inclusionof -sitosterol in liposomes caused a significant increase in particle diameterand PDI, while the encapsulation of gentisic acid did not have influence on particlesize distribution. Apart from that, the presence of -sitosterol resulted in thesignificant zeta potential increase, and thus a better stability of liposomal spheres(in the absence and in the presence of gentisic acid). -sitosterol decreased maintransition temperature (Tm) and phase transition enthalpy (H), and caused thedisappearance of the pre-transition peak as well, whereas the presence of gentisicacid produced a slight decrease in Tm and increase of H. Therefore, gentisic acidhad more favourable, stabilizing interactions with phospholipids than -sitosterol.Thus, it can be concluded that -sitosterol is located in the bilayer interior betweenphospholipids acyl chains, and gentisic acid is incorporated near the outer leaflet ofthe phospholipid membrane, next to the polar head groups. -sitosterol and gentisicacid loaded DPPC liposomal particles have a potential to be used in food andpharmaceutical products, due to the important individual and possible synergisticbeneficial health properties of -sitosterol and gentisic acid

A prospective, randomized, double-blind, placebo-controlled trial of polyphenols on the outcomes of inflammatory factors and oxidative stress in patients with type 2 diabetes mellitus

Type 2 diabetes mellitus (T2DM) is commonly associated with hyperglycemia, dyslipidemia, oxidative stress and inflammation which are well known cardiovascular risk factors. Pomegranate peel polyphenols have a proven hypolipemic, antioxidant and anti-inflammatory activity. However, there is a lack of clinical studies that would confirm its antioxidant and anti-inflammatory effects in diabetic patients. The potential of pomegranate peel extract (PoPEx) to counteract inflammation and oxidative stress in T2DM patients was investigated. For this purpose, a randomized, double-blind placebo-controlled study involving adult T2DM patients treated with PoPEx or placebo for eight-weeks was conducted. Methods: Patients were randomly divided into two groups: the first group (n = 30) received capsules containing PoPEx 250 mg twice daily, while the placebo group (n = 30) received placebo capsules twice daily. Plasma concentration of inflammatory factors (interleukin 6 (IL-6), tumor necrosis factor α (TNF-α) and high sensitivity C reactive protein (hsCRP)), oxidative stress biomarkers (thiobarbituric acid reactive substances (TBARS), nitrites (NO2−), superoxide anion radical (O2−), hydrogen peroxide (H2O2), total antioxidant capacity (TAC)), homocysteine and lipid profile were analyzed. Results: The PoPEx treatment showed a significant reduction of inflammatory factors (IL-6, TNF-α, hsCRP), oxidative stress biomarkers (TBARS, NO2−, O2−) and homocysteine, while the TAC was increased. Moreover, a significant improvement in lipid profile was observed in the PoPEx group. Additional analysis showed a significant inverse correlation between the decrements of all measured inflammatory markers and TAC in the PoPEx group. Conclusions: The study demonstrated that eight-week-long PoPEx administration had favorable effects on inflammatory status and oxidative stress biomarkers in diabetic patients

Fucus spiralis extract and fractions: Anticancer and pharmacological potentials

Purpose: Sea macroalgae are an important source of biologically highly valuable compounds. The main aim of this study was to investigate the in vitro anticancer properties and chemical composition of the dichloromethane-methanol extract and three fractions of the Fucus spiralis from coastline of Morocco. Methods: Fractions were made from dichloromethane: methanol (1:1) extract of Fucus spiralis: petroleum-ether, ethyl-acetate and n-butanol. Extract and fractions were screened for in vitro cytotoxicity by MTT assay against human cervical adenocarcinoma (HeLa), colorectal adenocarcinoma (LS-174T), lung carcinoma (A549), and normal human lung fibroblasts (MRC-5). Cell cycle distribution of the HeLa cells was evaluated using flow cytometry. Acridine orange (AO)-ethidium bromide (EB) staining was used to assess morphological changes of HeLa cells under fluorescence microscope. Anti-migration and anti-angiogenic properties were investigated using scratch and tube formation assays against human endothelium-derived permanent EA.hy926 cell line. Antidiabetic activity was tested using anti-α-glucosidase assay. Antimicrobial effect was tested using micro- dilution method. Results: Petroleum-ether fraction оf Fucus spiralis rich in fatty acids exerted the highest cytotoxicity against HeLa cells. Ethyl-acetate and petroleum-ether fractions induced the highest accumulation of the HeLa cells in sub-G1 and G2/M phases. Extract and fractions showed proapoptotic effect on HeLa cells under fluorescent microscope. They exhibited antimigratory and antiangiogenic effects in vitro. IC50 value for α-glucosidase inhibitory activity was much stronger than standard acarbose. n-Butanol fraction exerted the highest antibacterial and antifungal activity. Conclusions: The investigation of various biological activities of the extract and fractions obtained from Fucus spiralis may suggest a promising anticancer and pharmacological potential of this edible macroalga

Chemical Profiling and Assessment of Antineurodegenerative and Antioxidant Properties of Veronica teucrium L. and Veronica jacquinii Baumg.

Neuroprotective potential of V. teucrium and V. jacquinii methanol extracts was analyzed. Chemical analysis of investigated extracts showed the presence of phenolic acid derivatives, flavonoids and one secoiridoid. The detected flavonoids derived from flavones (luteolin and isoscutellarein in V. jacquinii; apigenin, isoscutellarein and luteolin in V. teucrium) and flavonol (quercetin in V. jacquinii). Acteoside was the dominant compound in V. jacquinii, while plantamajoside and isoscutellarein 7-O-(6‴-O-acetyl)-ß-allosyl (1‴?2‴)-ß-glucoside were the major phenolics in V. teucrium. Additionally, the antineurodegenerative activity was tested at concentrations of 25, 50, and 100 µg/ml using acetylcholinesterase (AChE) and tyrosinase (TYR) assays. The inhibition of both enzymes was achieved with the investigated extracts, ranging from 22.78 to 35.40% for AChE and from 9.57 to 16.38% for TYR. There was no statistical difference between the activities of the analyzed extracts. Our data indicate that V. teucrium and V. jacquinii may have beneficial effects against Alzheimer's and Parkinson's disease.The authors are grateful to Fundac ~ao para a Ci^encia e a Tecnologia (FCT, Portugal) for financial support to CIMO (strategic project PEst-OE/AGR/UI0690/2011). J. C. M. Barreira and M. I. Dias thank FCT, POPH-QREN, and FSE for their grants (SFRH/BPD/72802/2010 and SFRH/BD/84485/2012, respectively). The GIP-USAL is financially supported by the Spanish Government through the project AGL2015-64522-C2-2-R. The authors are also grateful to the Serbian Ministry of Education, Science and Technological Development for financial support (Grant Numbers 173032, 173029, and 46013).info:eu-repo/semantics/publishedVersio

Seasonal variation in biopharmaceutical activity and fatty acid content of endemic Fucus virsoides algae from Adriatic Sea

Macroalgae from Fucus genus are a valuable source of bioactive components as they are abundant in complex polysaccharides, fatty acids and polyphenols. In this work, the biological activity and chemical composition of extracts and fractions obtained from endemic Fucus virsoides J. Agardh species collected in the summer and in the fall were investigated. From dichloromethane:methanol (1:1) extract three fractions were made: petroleum-ether, ethyl-acetate and n-butanol. The aim of the study was to examine the influence of the seasonal variations on algal composition and activity. The significant seasonal variation in content and biological activity of Fucus virsoides samples was found. Fall extract and fractions exerted higher cytotoxic effects on cancer cell lines in comparison with summer extract and fractions. The examined extracts and fractions showed higher cytotoxic activity towards cancer cells compared to normal fibroblast MRC5 cells. Morphological evaluation and cell cycle distribution analysis demonstrated their proapoptotic activity in human cervical adenocarcinoma HeLa cells. Fall extract and fractions better suppressed the migration and tube formation of EA.hy926 cells in comparison with summer extract and fractions. Fall extract and fractions were more potent in inhibition of α-glucosidase enzymatic activity. Ethyl-acetate fractions, from both seasons, exhibited the best antibacterial and antifungal activity on all tested bacteria and fungi. In conclusion, the two fall fractions ethyl-acetate and petroleum-ether rich in polyphenols and polyunsaturated fatty acids, were the most active and exhibited prominent anticancer and anti-α-glucosidase activities

Phenolic compounds and carotenoids in pumpkin fruit and related traditional products

Pumpkin fruit is used in a diet since ancient times especially in rural communities. The major contributory factors of nutritional and medicinal value of pumpkins are carotenoids, polysaccharides, vitamins, minerals, and phenolic compounds. Due to a very large fruit that it is not easy to consume a whole as well as short shelf-life of fresh-cut pumpkin, different ways of conserving and processing are performed. In our study, total carotenoids, total phenolics and individual phenolics in fresh pumpkin and pumpkin traditional products such as sweet in wine, jam and juice, which are typical for northern parts of Serbia, were studied. Total carotenoids ranged from 27.6 μg/g of pumpkin sweet in wine to 86.3 μg/g of fresh fruit, while the amount of total phenolics varied between 93.0 μg GAE/g of pumpkin juice and 905.9 μg GAE/g of fresh fruit. Eight phenolic compounds were identified in the investigated samples and among them phenolic acids dominated. Among flavonoids, flavanon glycoside hesperidin was detected. [Projekat Ministarstva nauke Republike Srbije, br. 46013

Crataegus orientalis leaves and berries: Phenolic profiles, antioxidant and anti-inflammatory activity

The present study was designed to define the phenolic content, antioxidant and anti-inflammatory activity of Crateagus orientalis Pall. Ex M. Bieb., traditionally used by local people in southern parts of F.Y.R. Macedonia. The presence and content of 7 phenolics in ethanolic extracts of leaves and berries were studied using HPLC-DAD, where the most dominant compounds were hyperoside, isoquercitrin and chlorogenic acid. The leaf extract was more effective as a DPPH radical scavenger (IC50 = 29.7 μg/g) than the berry extract, as well as in the relative reducing power on Fe3+. Anti-inflammatory potential was studied by means of cyclooxygenase-1 (COX-1) and 12-lipoxygenase (12-LOX) inhibitory activity; both extracts evinced activity. Furthermore, C. orientalis leaf extract showed a concentration dependent inhibition of COX-1 pathway products 12-HHT and TXB2, reaching IC50 values below the lowest applied concentration (68.9% and 55.2% of 12-HHT and TXB2 production inhibition, respectively, at concentration of 0.4 mg/mL). Although inhibitors such as acetylsalicylic acid and quercetin showed higher activity, this study demonstrates that the investigated extracts are potential anti-inflammatory agents.Natural Product Communications (2017), 12(2): 159-16

β‐sitosterol and gentisic acid loaded1,2‐dipalmitoyl‐sn‐glycero‐3‐phosphocholine liposomal particles

The aim of the present study was the examination of the impact of β-sitosterol and gentisic acid on the characteristics of 1,2-dipalmitoyl-sn-glycero-3-phosphocholine(DPPC) liposomal particles: (a) bilayer permeability (fluorescence spectroscopy),(b) particle size, polydispersity index (PDI) and zeta potential (photon correlation spectroscopy) and (c) thermal properties (differential scanning calorimetry).β-sitosterol induced the increase of liposomal bilayer rigidity, due to rearranging of the phospholipid chains, while gentisic acid enhanced the membrane fluidity, due to the reduced orderliness and the increase of phospholipid dynamics. The inclusion of β-sitosterol in liposomes caused a significant increase in particle diameter and PDI, while the encapsulation of gentisic acid did not have influence on particle size distribution. Apart from that, the presence ofβ-sitosterol resulted in the significant zeta potential increase, and thus a better stability of liposomal spheres(in the absence and in the presence of gentisic acid). β-sitosterol decreased main transition temperature (Tm) and phase transition enthalpy (∆H), and caused the disappearance of the pre-transition peak as well, whereas the presence of gentisic acid produced a slight decrease in Tm and increase of ∆H. Therefore, gentisic acid had more favourable, stabilizing interactions with phospholipids thanβ-sitosterol. Thus, it can be concluded that β-sitosterol is located in the bilayer interior between phospholipids acyl chains, and gentisic acid is incorporated near the outer leaflet of the phospholipid membrane, next to the polar head groups.β-sitosterol and gentisic acid loaded DPPC liposomal particles have a potential to be used in food and pharmaceutical products, due to the important individual and possible synergistic beneficial health properties ofβ-sitosterol and gentisic acid

Ultrasound Extraction of Polyphenolic Compounds from Thymus serpyllum

Aromatic plant species of family Lamiaceae are important medicinal plants because of their antioxidant, antimicrobial, antispasmodic, expectorant, stimulant and diuretic properties. In this study T. serpyllum herba was evaluated as a source of polyphenolic compounds, which are extracted by the application of ultrasound probe instead of the traditional solvent extraction. Ultrasound extraction has become a good alternative extraction method when compared to classical methods due to its high efficiency, low energy and solvent consumption. Ultrasound assisted extraction is a well established method in the processing of plant material, particularly to extract bioactive substances such as polyphenols. Optimization of the extraction was carried out through varying degrees of fragmentation (0.3, 0.7 and 1.5), time of extraction (3, 7 and 10 minutes) and ratio drugs:solvent (1:10, 1:20 and 1:30) in 30% ethanol as an extraction medium. Extraction efficiency was expressed via total polyphenols content (Folin-Ciocalteu method) and antioxidant activity (DPPH method). The highest total polyphenols content and antioxidant activity were recorded in extract with a degree of fragmentation of 0.3 and ratio drug:solvent 1:30 after 3 minutes, 23.03 mg/L GA and IC50 3.00 mg/ml, respectively. The lowest total polyphenols content and antioxidant capacity were obtained in extract with a degree of fragmentation of 1.5 and ratio drug:solvent 1:10 (12.06 mg/L GA and IC50 4.78 mg/ml, respectively). This study found that both total polyphenols and antioxidant activities determined were significantly affected by the degree of fragmentation and ratio drugs:solvent. Also, the levels of total soluble phenolic compounds were positively correlated with free radical scavenging activities against DPPH radicals