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18 pages, 4116 KiB

Open AccessArticle

Development and Characterization of Biointeractive Gelatin Wound Dressing Based on Extract of Punica granatum Linn

by Marismar F. do Nascimento, Juliana C. Cardoso, Tarsizio S. Santos, Lívia A. Tavares, Tatiana N. Pashirova, Patricia Severino, Eliana B. Souto and Ricardo L. C. de Albuquerque-Junior

Pharmaceutics 2020, 12(12), 1204; https://doi.org/10.3390/pharmaceutics12121204 - 11 Dec 2020

Cited by 18 | Viewed by 2259

Abstract

Punica granatum Linn (pomegranate) extracts have been proposed for wound healing due to their antimicrobial, antioxidant, and anti-inflammatory properties. In this work, we designed biointeractive membranes that contain standard extracts of P. granatum for the purpose of wound healing. The used standard extract [...] Read more.

Punica granatum Linn (pomegranate) extracts have been proposed for wound healing due to their antimicrobial, antioxidant, and anti-inflammatory properties. In this work, we designed biointeractive membranes that contain standard extracts of P. granatum for the purpose of wound healing. The used standard extract contained 32.24 mg/g of gallic acid and 41.67 mg/g of ellagic acid, and it showed high antioxidant activity (the concentration of the extract that produces 50% scavenging (IC₅₀) 1.715 µg/mL). Compared to the gelatin-based membranes (GEL), membranes containing P. granatum extracts (GELPG) presented a higher maximal tension (p = 0.021) and swelling index (p = 0.033) and lower water vapor permeability (p = 0.003). However, no difference was observed in the elongation and elastic modulus of the two types of membranes (p > 0.05). Our wound-healing assay showed that a GELPG-treated group experienced a significant increase compared to that of the control group in their wound contraction rates on days 3 (p < 0.01), 7 (p < 0.001), and on day 14 (p < 0.001). The GELPG membranes promoted major histological changes in the dynamics of wound healing, such as improvements in the formation of granular tissue, better collagen deposition and arrangement, and earlier development of cutaneous appendages. Our results suggest that a biointeractive gelatin-based membrane containing P. granatum extracts has a promising potential application for dressings that are used to treat wounds. Full article

(This article belongs to the Special Issue Herbal Extracts and Natural Compounds: Nutraceutical and Pharmaceutical Aspects)

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11 pages, 1432 KiB

Open AccessArticle

Echinacea angustifolia DC. Lipophilic Extract Patch for Skin Application: Preparation, In Vitro and In Vivo Studies

by Dritan Hasa, Simon Žakelj, Iztok Grabnar, Francesco Cilurzo, Stefano Dall’Acqua, Antonella Riva, Beatrice Perissutti and Dario Voinovich

Pharmaceutics 2020, 12(11), 1096; https://doi.org/10.3390/pharmaceutics12111096 - 16 Nov 2020

Cited by 2 | Viewed by 2158

Abstract

Dodeca-2E,4E,8Z,10E/Z-tetraenoic isobutylamide (tetraene) is the main component of Echinacea angustifolia DC. lipophilic extract, the bioavailability and immunomodulatory effect after oral administration in soft gel capsules in healthy volunteers of which we have already [...] Read more.

Dodeca-2E,4E,8Z,10E/Z-tetraenoic isobutylamide (tetraene) is the main component of Echinacea angustifolia DC. lipophilic extract, the bioavailability and immunomodulatory effect after oral administration in soft gel capsules in healthy volunteers of which we have already demonstrated. In the present work, we assessed the transdermal administration as an alternative route of administration of such an alkamide. The first step, therefore, encompassed the preparation of a drug-in-adhesive patch with an area of 868 mm² and containing a dose of 0.64 mg of tetraene. In vitro skin permeation studies in Franz-type diffusion chambers resulted in a tetraene flux of (103 ± 10) ng × cm⁻² × h⁻¹ with a very good linearity (r = 0.99). The relatively low lag time of just 13 min indicates low binding and the accumulation of tetraene in the skin. Finally, the patch was administered to six healthy volunteers, and the pharmacokinetic analysis was performed by nonlinear mixed effects modelling with soft gel oral capsules serving as the reference formulation. The in vivo results correlated well with the in vitro permeation and indicated an initial burst tetraene absorption from the patch that was in parallel with the zero-order kinetics of absorption. The rate of the latter process was in good agreement with the one estimated in vitro. The tetraene absorption rate was therefore slow and prolonged with time, resulting in a bioavailability of 39% relative to the soft gel capsules and a very flat plasma concentration profile. Full article

(This article belongs to the Special Issue Herbal Extracts and Natural Compounds: Nutraceutical and Pharmaceutical Aspects)

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29 pages, 8315 KiB

Open AccessArticle

Blueberry Consumption Challenges Hepatic Mitochondrial Bioenergetics and Elicits Transcriptomics Reprogramming in Healthy Wistar Rats

by Sara Nunes, Sofia D. Viana, Inês Preguiça, André Alves, Rosa Fernandes, João S. Teodoro, Artur Figueirinha, Lígia Salgueiro, Sara Silva, Ivana Jarak, Rui A. Carvalho, Cláudia Cavadas, Anabela P. Rolo, Carlos M. Palmeira, Maria M. Pintado and Flávio Reis

Pharmaceutics 2020, 12(11), 1094; https://doi.org/10.3390/pharmaceutics12111094 - 14 Nov 2020

Cited by 5 | Viewed by 3889

Abstract

An emergent trend of blueberries’ (BB) “prophylactic” consumption, due to their phytochemicals’ richness and well-known health-promoting claims, is widely scaled-up. However, the benefits arising from BB indiscriminate intake remains puzzling based on incongruent preclinical and human data. To provide a more in-depth elucidation [...] Read more.

An emergent trend of blueberries’ (BB) “prophylactic” consumption, due to their phytochemicals’ richness and well-known health-promoting claims, is widely scaled-up. However, the benefits arising from BB indiscriminate intake remains puzzling based on incongruent preclinical and human data. To provide a more in-depth elucidation and support towards a healthier and safer consumption, we conducted a translation-minded experimental study in healthy Wistar rats that consumed BB in a juice form (25 g/kg body weight (BW)/day; 14 weeks’ protocol). Particular attention was paid to the physiological adaptations succeeding in the gut and liver tissues regarding the acknowledged BB-induced metabolic benefits. Systemically, BB boosted serum antioxidant activity and repressed the circulating levels of 3-hydroxybutyrate (3-HB) ketone bodies and 3-HB/acetoacetate ratio. Moreover, BB elicited increased fecal succinic acid levels without major changes on gut microbiota (GM) composition and gut ultra-structural organization. Remarkably, an accentuated hepatic mitochondrial bioenergetic challenge, ensuing metabolic transcriptomic reprogramming along with a concerted anti-inflammatory pre-conditioning, was clearly detected upon long-term consumption of BB phytochemicals. Altogether, the results disclosed herein portray a quiescent mitochondrial-related metabolomics and hint for a unified adaptive response to this nutritional challenge. The beneficial or noxious consequences arising from this dietary trend should be carefully interpreted and necessarily claims future research. Full article

(This article belongs to the Special Issue Herbal Extracts and Natural Compounds: Nutraceutical and Pharmaceutical Aspects)

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12 pages, 2431 KiB

Open AccessArticle

Carob Seeds: Food Waste or Source of Bioactive Compounds?

by Debora Santonocito, Giuseppe Granata, Corrada Geraci, Annamaria Panico, Edy Angela Siciliano, Giuseppina Raciti and Carmelo Puglia

Pharmaceutics 2020, 12(11), 1090; https://doi.org/10.3390/pharmaceutics12111090 - 13 Nov 2020

Cited by 29 | Viewed by 2790

Abstract

(1) Background: For centuries, carob fruit has been used in the food field, while carob seeds have been mainly considered as food waste. Nowadays, there has been considerable attention toward the recovery of the waste plant matrices as possible sources of functional compounds [...] Read more.

(1) Background: For centuries, carob fruit has been used in the food field, while carob seeds have been mainly considered as food waste. Nowadays, there has been considerable attention toward the recovery of the waste plant matrices as possible sources of functional compounds with health properties. Therefore, our goal was to evaluate the health properties of carob seed extracts, and to study the effects of the ripening process on the chemical composition of the extracts. (2) Methods: After the mechanical separation of seeds from carob fruit, an ultrasound-assisted extraction (UAE) was performed to maximize and preserve the quality of bioactive compounds. Seed extracts were characterized by high-performance liquid chromatography (HPLC) and liquid chromatography/mass spectrometry (LC/MS) for the content of bioactive polyphenols, and were finally analyzed by oxygen radical absorbance capacity (ORAC), NO Scavenger (NO) and advanced glyoxidation end products (AGEs) assays, in order to estimate the antioxidant potential of the active compounds. (3) Results: Although both seed extracts of carob unripe (CAR-UR) and ripe (CAR-R) showed an interesting antioxidant activity, CAR-R had greater activity due to the procyanidins content. (4) Conclusions: Based on the obtained results, carob seed extracts could be regarded as interesting source of bioactive antioxidant compounds for a potential application in nutraceutical and food supplement fields. Full article

(This article belongs to the Special Issue Herbal Extracts and Natural Compounds: Nutraceutical and Pharmaceutical Aspects)

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10 pages, 2452 KiB

Open AccessArticle

Quercetin Disaggregates Prion Fibrils and Decreases Fibril-Induced Cytotoxicity and Oxidative Stress

by Kun-Hua Yu and Cheng-I Lee

Pharmaceutics 2020, 12(11), 1081; https://doi.org/10.3390/pharmaceutics12111081 - 11 Nov 2020

Cited by 5 | Viewed by 2902

Abstract

Transmissible spongiform encephalopathies (TSEs) are fatal neurodegenerative diseases caused by misfolding and aggregation of prion protein (PrP). Previous studies have demonstrated that quercetin can disaggregate some amyloid fibrils, such as amyloid β peptide (Aβ) and α-synuclein. However, the disaggregating ability is unclear in [...] Read more.

Transmissible spongiform encephalopathies (TSEs) are fatal neurodegenerative diseases caused by misfolding and aggregation of prion protein (PrP). Previous studies have demonstrated that quercetin can disaggregate some amyloid fibrils, such as amyloid β peptide (Aβ) and α-synuclein. However, the disaggregating ability is unclear in PrP fibrils. In this study, we examined the amyloid fibril-disaggregating activity of quercetin on mouse prion protein (moPrP) and characterized quercetin-bound moPrP fibrils by imaging, proteinase resistance, hemolysis assay, cell viability, and cellular oxidative stress measurements. The results showed that quercetin treatment can disaggregate moPrP fibrils and lead to the formation of the proteinase-sensitive amorphous aggregates. Furthermore, quercetin-bound fibrils can reduce the membrane disruption of erythrocytes. Consequently, quercetin-bound fibrils cause less oxidative stress, and are less cytotoxic to neuroblastoma cells. The role of quercetin is distinct from the typical function of antiamyloidogenic drugs that inhibit the formation of amyloid fibrils. This study provides a solution for the development of antiamyloidogenic therapy. Full article

(This article belongs to the Special Issue Herbal Extracts and Natural Compounds: Nutraceutical and Pharmaceutical Aspects)

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13 pages, 1550 KiB

Open AccessArticle

Co-Microencapsulation of Flavonoids from Yellow Onion Skins and Lactic Acid Bacteria Lead to Multifunctional Ingredient for Nutraceutical and Pharmaceutics Applications

by Ștefania Adelina Milea, Mihaela Aida Vasile, Oana Crăciunescu, Ana-Maria Prelipcean, Gabriela Elena Bahrim, Gabriela Râpeanu, Anca Oancea and Nicoleta Stănciuc

Pharmaceutics 2020, 12(11), 1053; https://doi.org/10.3390/pharmaceutics12111053 - 04 Nov 2020

Cited by 16 | Viewed by 2537

Abstract

In this study, flavonoids extracted from yellow onion skins and Lactobacillus casei were encapsulated in a combination of whey protein isolate, inulin and maltodextrin with an encapsulation efficiency of 84.82 ± 0.72% for flavonoids and 72.49 ± 0.11% for lactic acid bacteria. The [...] Read more.

In this study, flavonoids extracted from yellow onion skins and Lactobacillus casei were encapsulated in a combination of whey protein isolate, inulin and maltodextrin with an encapsulation efficiency of 84.82 ± 0.72% for flavonoids and 72.49 ± 0.11% for lactic acid bacteria. The obtained powder showed a flavonoid content of 89.49 ± 4.12 mg quercetin equivalents/g dry weight (DW) and an antioxidant activity of 39.27 ± 0.45 mM Trolox/g DW. The powder presented a significant antidiabetic and anti-inflammatory potential, with an inhibitory effect on α-amylase, lipase and lipoxygenase of 76.40 ± 2.30%, 82.58 ± 3.36% and 49.01 ± 0.62%, respectively. The results obtained for in vitro digestion showed that the coating materials have a protective effect on the flavonoids release. Cytotoxicity results indicated that the powder was cytocompatible up to a concentration of 500 μg/mL. The functional potential of the powder was tested by adding in a selected food matrix, highlighting a good stability of the phytochemicals, whereas an increase with 1 log cell forming unit (CFU)/g DW was observed after 21 days of storage. The obtained results are promising in the valorization of natural antioxidants in combination with lactic acid bacteria in order to develop multifunctional ingredients with value-added for food and pharmaceutics applications. Full article

(This article belongs to the Special Issue Herbal Extracts and Natural Compounds: Nutraceutical and Pharmaceutical Aspects)

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15 pages, 6051 KiB

Open AccessArticle

Recycling of Almond By-Products for Intestinal Inflammation: Improvement of Physical-Chemical, Technological and Biological Characteristics of a Dried Almond Skins Extract

by Maria Rosaria Lauro, Stefania Marzocco, Shara Francesca Rapa, Teresa Musumeci, Virgilio Giannone, Patrizia Picerno, Rita Patrizia Aquino and Giovanni Puglisi

Pharmaceutics 2020, 12(9), 884; https://doi.org/10.3390/pharmaceutics12090884 - 17 Sep 2020

Cited by 7 | Viewed by 2460

Abstract

Background: Almond skins are rich in bioactive compounds that undergo oxidation/degradation phenomena and are poorly soluble in water, reducing in vivo absorption and bioavailability, factors that influence the pharmacological activity of an active product. We developed a dried acetonic almond skins extract/cyclodextrin complex [...] Read more.

Background: Almond skins are rich in bioactive compounds that undergo oxidation/degradation phenomena and are poorly soluble in water, reducing in vivo absorption and bioavailability, factors that influence the pharmacological activity of an active product. We developed a dried acetonic almond skins extract/cyclodextrin complex to improve extract solubility, dissolution rate and biological activity. Methods: A lyophilized acetonic almond skin extract was produced. To optimize complex formulation, phase solubility studies and complex characterization (absorption studies, differential scanning calorimetry (DSC), morphology, solubility studies) were performed. To evaluate a possible use in healthy products, tumor necrosis factor-α levels and reactive oxygen species release, as well as cicloxygenase-2 and inducible nitric oxide synthase expression in intestinal epithelial cells, were also evaluated. Results: Phase solubility studies showed a Bs-type profile. A 1:1 dried acetonic almond skins extract/cyclodextrin ratio was able to improve extract water solubility and dissolution rate (100% in 45 min). The UV-Vis spectra of complex revealed a hypsochromic and hyperchromic effect, probably due to a partial inclusion of extract in cyclodextrin cavity through weak bonds, confirmed by DSC and morphology studies. The technological improvement in the extract characteristics also led to better biological activity. In fact, the complex effectively reduces tumor necrosis factor-α levels with respect to the pure extract and significantly inhibits the reactive oxygen species release, even if only at the lower concentration of 5 μg/mL. Conclusion: The complex was able to overcome solubility problems and could be used in inflammatory disease. Full article

(This article belongs to the Special Issue Herbal Extracts and Natural Compounds: Nutraceutical and Pharmaceutical Aspects)

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22 pages, 3858 KiB

Open AccessArticle

Biological Evaluation of Black Chokeberry Extract Free and Embedded in Two Mesoporous Silica-Type Matrices

by Valentina Buda, Ana-Maria Brezoiu, Daniela Berger, Ioana Zinuca Pavel, Delia Muntean, Daliana Minda, Cristina Adriana Dehelean, Codruta Soica, Zorita Diaconeasa, Roxana Folescu and Corina Danciu

Pharmaceutics 2020, 12(9), 838; https://doi.org/10.3390/pharmaceutics12090838 - 01 Sep 2020

Cited by 16 | Viewed by 3754

Abstract

Black chokeberry fruits possess a wide range of biological activities, among which the most important that are frequently mentioned in the literature are their antioxidant, anti-inflammatory, anti-proliferative, and antimicrobial properties. The present paper reports, for the first time, the encapsulation of the ethanolic [...] Read more.

Black chokeberry fruits possess a wide range of biological activities, among which the most important that are frequently mentioned in the literature are their antioxidant, anti-inflammatory, anti-proliferative, and antimicrobial properties. The present paper reports, for the first time, the encapsulation of the ethanolic extract of Aronia melanocarpa L. fruits into two mesoporous silica-type matrices (i.e., pristine MCM-41 and MCM-41 silica decorated with zinc oxide nanoparticles). The aim of this work was to evaluate the antiradicalic capacity, the antimicrobial potential, and the effects on the cell viability on a cancer cell line (i.e., A375 human melanoma cell line) versus normal cells (i.e., HaCaT human keratinocytes) of black chokeberry extract loaded on silica-type matrices in comparison to that of the extract alone. The ethanolic polyphenolic extract obtained by conventional extraction was characterized by high-performance liquid chromatography with a photodiode array detector (HPLC–PDA) and spectrophotometric methods. The extract was found to contain high amounts of polyphenols and flavonoids, as well as good radical scavenging activity. The extract-loaded materials were investigated by Fourier transform infrared spectroscopy, N₂ adsorption–desorption isotherms, thermal analysis, and radical scavenger activity on solid samples. The black chokeberry extract, both free and loaded onto mesoporous silica-type matrices, exhibited a significant antioxidant capacity. Antibacterial activity was recorded only for Gram-positive bacteria, with a more potent antibacterial effect being observed for the extract loaded onto the ZnO-modified MCM-41 silica-type support than for the free extract, probably due to the synergistic effect of the ZnO nanoparticles that decorate the pore walls of silica. The cellular viability test (i.e., MTT assay) showed dose- and time-dependent activity regarding the melanoma cell line. The healthy cells were less affected than the cancer cells, with all tested samples showing good cytocompatibility at doses of up to 100 µg/mL. Improved in vitro antiproliferative and antimigratory (i.e., scratch assay) potential was demonstrated through the loading of black chokeberry extract into mesoporous silica-type matrices, and the screened samples exhibited low selectivity against the tested non-tumor cell line. Based on presented results, one can conclude that mesoporous silica-type matrices are good hosts for black chokeberry extract, increasing its antioxidant, antibacterial (on the screened strains), and in vitro antitumor (on the screened cell line) properties. Full article

(This article belongs to the Special Issue Herbal Extracts and Natural Compounds: Nutraceutical and Pharmaceutical Aspects)

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21 pages, 4382 KiB

Open AccessArticle

Schizonepeta Tenuifolia with Alpinia Oxyphylla Alleviates Atopic Dermatitis and Improves the Gut Microbiome in Nc/Nga Mice

by Ting Zhang, Jingyi Qiu, Xuangao Wu, Shaokai Huang, Heng Yuan and Sunmin Park

Pharmaceutics 2020, 12(8), 722; https://doi.org/10.3390/pharmaceutics12080722 - 31 Jul 2020

Cited by 8 | Viewed by 3413

Abstract

Atopic dermatitis (AD) is a chronic inflammatory skin disease that may be related to gut microbes. Schizonepeta Tenuifolia Briquet (STB) and Alpinia Oxyphylla Miquel (AOM) has traditionally been used for anti-inflammatory activity. We evaluated the effects of STB, AOM and STB+AOM extracts on [...] Read more.

Atopic dermatitis (AD) is a chronic inflammatory skin disease that may be related to gut microbes. Schizonepeta Tenuifolia Briquet (STB) and Alpinia Oxyphylla Miquel (AOM) has traditionally been used for anti-inflammatory activity. We evaluated the effects of STB, AOM and STB+AOM extracts on 2,4-dinitro-1-chlorobenzene (DNCB)-induced AD skin lesions in Nc/Nga mice and action mechanism was explored. AD lesions were induced in the dorsal skin of Nc/Nga mice by topical application of 1% followed by 0.2% DNCB. After DNCB was applied, the mice had topical applications of either 30% water, 0.01% dexamethasone, 30% STB, 30% AOM, 15% STB + 15% AOM extracts in butylene glycol (BG). Each group was also fed corresponding high-fat diets with 1% dextrin (AD-Con and AD-Positive), 1% STB (AD-STB), 1% AOM (AD-AOM) and 0.5% STB + 0.5% (AD-MIX). Normal-control mice had no DNCB application. The study evaluated the skin AD severity, scratching behavior and weight changes of AD mice for 5 weeks. Compared with AD-Con, AD-STB, AD-AOM and AD-MIX alleviated the clinical AD symptoms (erythema, pruritus, edema, erosion and lichenification and scratching behaviors), normalized immune chemistry (serum IgE concentration, mast cells and eosinophil infiltration), improved skin hyperplasia and enhanced the gut microbiome. AD-STB, AD-AOM, AD-MIX and AD-positive treatments inhibited cutaneous mRNA expression of TNF-α, IL-4 and IL-13 and serum IgE concentrations. AD-MIX most effectively reduced clinical AD symptoms and proinflammatory cytokines. AD-Positive also reduced them but serum GOT and GPT concentrations were abnormally high. AD-STB and AD-MIX increased the alpha-diversity of fecal bacteria and reduced the serum acetate concentration, compared to the AD-Con. In conclusion, the mixture of STB and AOM is effective for treating AD symptoms locally and systemically without adverse effects and are potential interventions for atopic dermatitis. Full article

(This article belongs to the Special Issue Herbal Extracts and Natural Compounds: Nutraceutical and Pharmaceutical Aspects)

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23 pages, 5443 KiB

Open AccessArticle

Study on Ajuga reptans Extract: A Natural Antioxidant in Microencapsulated Powder Form as an Active Ingredient for Nutraceutical or Pharmaceutical Purposes

by Tiziana Esposito, Francesca Sansone, Giulia Auriemma, Silvia Franceschelli, Michela Pecoraro, Patrizia Picerno, Rita P. Aquino and Teresa Mencherini

Pharmaceutics 2020, 12(7), 671; https://doi.org/10.3390/pharmaceutics12070671 - 17 Jul 2020

Cited by 14 | Viewed by 2994

Abstract

The administration of natural antioxidants is considered to be a prevention strategy for chronic diseases and a useful tool for the healthcare system to reduce the administration of expensive and often not effective treatments. The chemical characterization of a methanolic extract (AJ) of [...] Read more.

The administration of natural antioxidants is considered to be a prevention strategy for chronic diseases and a useful tool for the healthcare system to reduce the administration of expensive and often not effective treatments. The chemical characterization of a methanolic extract (AJ) of Ajuga reptans L. was performed, and its antioxidant activity was evaluated. AJ and the major compounds, characterized by chromatographic techniques as phenylpropanoids and iridoids, were able to reduce the Reactive Oxygen Species levels in cancer cell lines (melanoma, A375, cervical cancer, HeLa, and alveolar adenocarcinoma, A549), stimulated by E. coli lipopolysaccharide. However, a clinical translation of these results encountered a significant limitation represented by the poor water solubility and bioavailability of the extract and compounds. Consequently, a hydro-soluble powder system (AJEP₃) was developed by spray-drying encapsulating AJ into a multi-component solid matrix that is based on L-proline and hydroxyethylcellulose as loading and coating agents, and lecithin as solubility enhancer. The technological approach led to a satisfactory process yield (71.5%), encapsulation efficiency (99.9%), and stability. The in vitro water dissolution rate of the bioactive compounds appeared to be improved with respect to the extract, suggesting higher feasibility in the manufacturing and administration; even the in vitro biological activity of the produced multi-component AJEP₃ was clearly enhanced. Full article

(This article belongs to the Special Issue Herbal Extracts and Natural Compounds: Nutraceutical and Pharmaceutical Aspects)

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22 pages, 5605 KiB

Open AccessArticle

In Vitro Antigenotoxic, Antihelminthic and Antioxidant Potentials Based on the Extracted Metabolites from Lichen, Candelariella vitellina

by Islam El-Garawani, Mahmoud Emam, Waill Elkhateeb, Hesham El-Seedi, Shaden Khalifa, Salwa Oshiba, Shaimaa Abou-Ghanima and Ghoson Daba

Pharmaceutics 2020, 12(5), 477; https://doi.org/10.3390/pharmaceutics12050477 - 24 May 2020

Cited by 20 | Viewed by 3778

Abstract

Lichens have recently received great attention due to their pharmacological potentials. The antigenotoxic potential of C. vitellina extract (25 and 50 µg/mL) was assessed in normal human peripheral blood lymphocytes (HPBL) against Mitomycin C (MMC) co-treatments. Flow cytometric analyses of cell cycle distribution, [...] Read more.

Lichens have recently received great attention due to their pharmacological potentials. The antigenotoxic potential of C. vitellina extract (25 and 50 µg/mL) was assessed in normal human peripheral blood lymphocytes (HPBL) against Mitomycin C (MMC) co-treatments. Flow cytometric analyses of cell cycle distribution, as well as apoptosis (Annexin V/PI), revealed that the extract had significantly (p ≤ 0.05) ameliorated the MMC toxicity by reducing the apoptotic cells and normalized the cell cycle phases. C. vitellina exhibited antigenotoxicity by ameliorating the diminished mitotic index and DNA single-strand breaks caused by MMC. Herein, the hydromethanolic extract (80%) of Candelariella vitellina (Japan) lichen, exhibited very low cytotoxicity towards normal human peripheral lymphocytes (HPBL) with IC₅₀ >1000 µg/mL. In order to explore the antihelminthic effect, Echinococcus granulosus protoscoleces were used in vitro. Eosin staining revealed significant (p ≤ 0.05) dose and time-dependent scolicidal effects of the extract confirmed by degenerative alterations as observed by electron scan microscopy. Furthermore, primary and secondary metabolites were investigated using GC-MS and qualitative HPLC, revealing the presence of sugars, alcohols, different phenolic acids and light flavonoids. Significant antioxidant capacities were also demonstrated by DPPH radical-scavenging assay. In conclusion, the promising antigenotoxic, antihelminthic and antioxidant potentials of C. vitellina extract encourage further studies to evaluate its possible therapeutic potency. Full article

(This article belongs to the Special Issue Herbal Extracts and Natural Compounds: Nutraceutical and Pharmaceutical Aspects)

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17 pages, 3756 KiB

Open AccessArticle

Characterization of Phenolic Acid Antimicrobial and Antioxidant Structure–Property Relationships

by Jingyi Liu, Changling Du, Henry T. Beaman and Mary Beth B. Monroe

Pharmaceutics 2020, 12(5), 419; https://doi.org/10.3390/pharmaceutics12050419 - 02 May 2020

Cited by 77 | Viewed by 5931

Abstract

Plant-derived phenolic acids (PAs) are small molecules with antimicrobial, antioxidant, anti-inflammatory, and pro-coagulant properties. Their chemistry enables facile potential incorporation into biomaterial scaffolds to provide naturally-derived functionalities that could improve healing outcomes. While PAs have been previously characterized, their structure-property relationships in terms [...] Read more.

Plant-derived phenolic acids (PAs) are small molecules with antimicrobial, antioxidant, anti-inflammatory, and pro-coagulant properties. Their chemistry enables facile potential incorporation into biomaterial scaffolds to provide naturally-derived functionalities that could improve healing outcomes. While PAs have been previously characterized, their structure-property relationships in terms of antioxidant and antimicrobial properties are not well-understood, particularly in the context of their use in medical applications. To that end, a library of PAs with varied pendant groups was characterized here. It was found that increasing the number of radical-scavenging hydroxyl and methoxy groups on PAs increased antioxidant properties. All PAs showed some antimicrobial activity against the selected bacteria strains (Escherichia coli, Staphylococcus epidermidis (native and drug-resistant), and Staphylococcus aureus (native and drug-resistant)) at concentrations that are feasible for incorporation into polymeric biomaterials. In general, a trend of slightly decreased antimicrobial efficacy with increased number of pendant hydroxyl and methoxy groups was observed. The carboxylic acid group of a selection of PAs was modified with a polyurethane monomer analog. Modification did not greatly affect antioxidant or antimicrobial properties in comparison to unmodified controls, indicating that the carboxylic acid group of PAs can be altered without losing functionality. These results could be utilized for rational selection of phenolic moieties for use as therapeutics on their own or as part of a biomaterial scaffold with desired healing outcomes. Full article

(This article belongs to the Special Issue Herbal Extracts and Natural Compounds: Nutraceutical and Pharmaceutical Aspects)

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20 pages, 4293 KiB

Open AccessArticle

β-Sitosterol Loaded Nanostructured Lipid Carrier: Physical and Oxidative Stability, In Vitro Simulated Digestion and Hypocholesterolemic Activity

by Yasamin Soleimanian, Sayed Amir Hossein Goli, Jaleh Varshosaz, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Marzia Cirri and Francesca Maestrelli

Pharmaceutics 2020, 12(4), 386; https://doi.org/10.3390/pharmaceutics12040386 - 22 Apr 2020

Cited by 12 | Viewed by 4089

Abstract

The objective of the present study was to explore the potential of nanostructured lipid carriers (NLCs) for improving the oral delivery of β-sitosterol, a poorly water-soluble bioactive component with hypocholesterolemic activity. Two β-sitosterol formulations with different solid lipid compositions were prepared by melt [...] Read more.

The objective of the present study was to explore the potential of nanostructured lipid carriers (NLCs) for improving the oral delivery of β-sitosterol, a poorly water-soluble bioactive component with hypocholesterolemic activity. Two β-sitosterol formulations with different solid lipid compositions were prepared by melt emulsification, followed by the sonication technique, and the effect of storage conditions and simulated digestion on the physical, chemical and oxidative stability, bioaccessibility and release were extensively studied. Both NLC preparations remained relatively stable during the four weeks of storage at different conditions (4, 25 and 40 °C), with more superior stability at lower temperatures. The in vitro digestion experiment indicated a high physical stability after exposure to the simulated mouth and stomach stages and an improved overall β-sitosterol bioaccessibility at the end of the digestion. The NLCs presented an increased solubility and gradual release which could be justified by the remarkable affinity of β-sitosterol to the complex lipid mixture. An in vivo study demonstrated an improved reduction in the total cholesterol and low-density lipoprotein cholesterol plasma levels in mice compared with the drug suspension. These investigations evidenced the potential of the developed NLC formulations for the enhancement of solubility and in vivo performance of β-sitosterol. Full article

(This article belongs to the Special Issue Herbal Extracts and Natural Compounds: Nutraceutical and Pharmaceutical Aspects)

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0 pages, 3562 KiB

Open AccessArticle

RETRACTED: Optimized Icariin Phytosomes Exhibit Enhanced Cytotoxicity and Apoptosis-Inducing Activities in Ovarian Cancer Cells

by Nabil A. Alhakamy, Usama A. Fahmy, Shaimaa M. Badr-Eldin, Osama A. A. Ahmed, Hani Z. Asfour, Hibah M. Aldawsari, Mardi M. Algandaby, Basma G. Eid, Ashraf B. Abdel-Naim, Zuhier A. Awan, Nabil K. Alruwaili and Amir I. Mohamed

Pharmaceutics 2020, 12(4), 346; https://doi.org/10.3390/pharmaceutics12040346 - 11 Apr 2020

Cited by 64 | Viewed by 4657 | Retraction

Abstract

Icariin (ICA) is a flavonol glycoside that has pleiotropic pharmacological actions. It has cytotoxic effects against ovarian cancer cells and increases their chemosensitivity to chemotherapeutic drugs. Phytosomes are identified for their potential in drug delivery of cytotoxic agents. Thus, the purpose of this [...] Read more.

Icariin (ICA) is a flavonol glycoside that has pleiotropic pharmacological actions. It has cytotoxic effects against ovarian cancer cells and increases their chemosensitivity to chemotherapeutic drugs. Phytosomes are identified for their potential in drug delivery of cytotoxic agents. Thus, the purpose of this study was to determine the potential enhancement of ICA cytotoxicity activity in OVCAR-3 ovarian cancer cells via its formulation in phytosomes. ICA-phytosomal formulation was optimized using a Box–Behnken design. Particle size, shape, and in vitro drug release were used to characterize the optimized formula. The optimized formulation exhibited enhanced in vitro drug release. ICA-phytosomes exhibited enhanced cytotoxicity against ovarian cancer cells. Cell cycle analysis indicated accumulation of cells challenged with ICA-phytosomes in G2/M and pre-G1 phases. Staining of cells with annexin V indicated significant elevation of percentage cells with early and late apoptosis as well as total cell death. In addition, the formulation significantly disturbed mitochondrial membrane potential and cellular content of caspase 3. In addition, intracellular release of reactive oxygen species (ROS) was enhanced by ICA-phytosomes. In conclusion, phytosome formulation of ICA significantly potentiates its cytotoxic activities against OVCAR-3 cells. This is mediated, at least partly, by enhanced ICA cellular permeation, apoptosis, and ROS. Full article

(This article belongs to the Special Issue Herbal Extracts and Natural Compounds: Nutraceutical and Pharmaceutical Aspects)

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Open AccessArticle

Neuroprotective Effect of Bergamot Juice in 6-OHDA-Induced SH-SY5Y Cell Death, an In Vitro Model of Parkinson’s Disease

by Nadia Ferlazzo, Santa Cirmi, Alessandro Maugeri, Caterina Russo, Giovanni Enrico Lombardo, Sebastiano Gangemi, Gioacchino Calapai, Vincenzo Mollace and Michele Navarra

Pharmaceutics 2020, 12(4), 326; https://doi.org/10.3390/pharmaceutics12040326 - 05 Apr 2020

Cited by 25 | Viewed by 4538

Abstract

Much evidence suggests that both oxidative stress and apoptosis play a key role in the pathogenesis of Parkinson’s disease (PD). The present study aims to evaluate the protective effect of bergamot juice (BJ) against 6-hydroxydopamine (6-OHDA)- or H₂O₂-induced cell [...] Read more.

Much evidence suggests that both oxidative stress and apoptosis play a key role in the pathogenesis of Parkinson’s disease (PD). The present study aims to evaluate the protective effect of bergamot juice (BJ) against 6-hydroxydopamine (6-OHDA)- or H₂O₂-induced cell death. Treatment of differentiated SH-SY5Y human neuroblastoma cells with 6-OHDA or H₂O₂ resulted in cell death that was significantly reduced by the pre-treatment with BJ. The protective effects of BJ seem to correlate with the reduction of intracellular reactive oxygen species and nitric oxide generation caused by 6-OHDA or H₂O₂. BJ also attenuated mitochondrial dysfunction, caspase-3 activation, imbalance of pro- and anti-apoptotic proteins, MAPKs activation and reduced NF-ĸB nuclear translocation evoked by neurotoxic agents. Additionally, BJ exhibited excellent antioxidant capability in cell-free assays. Collectively, our results suggest that BJ exerts neuroprotective effect through the interplay with specific cell targets and its antioxidant activity, making it worthy of consideration for the management of neurodegenerative diseases. Full article

(This article belongs to the Special Issue Herbal Extracts and Natural Compounds: Nutraceutical and Pharmaceutical Aspects)

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Review

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34 pages, 711 KiB

Open AccessReview

Are Nutraceuticals Beneficial in Chronic Kidney Disease?

by Jacek Rysz, Beata Franczyk, Krzysztof Kujawski, Izabela Sacewicz-Hofman, Aleksanda Ciałkowska-Rysz and Anna Gluba-Brzózka

Pharmaceutics 2021, 13(2), 231; https://doi.org/10.3390/pharmaceutics13020231 - 06 Feb 2021

Cited by 7 | Viewed by 3623

Abstract

Chronic kidney disease (CKD) is a worldwide health problem in which prevalence is constantly rising. The pathophysiology of CKD is complicated and has not been fully resolved. However, elevated oxidative stress is considered to play a vital role in the development of this [...] Read more.

Chronic kidney disease (CKD) is a worldwide health problem in which prevalence is constantly rising. The pathophysiology of CKD is complicated and has not been fully resolved. However, elevated oxidative stress is considered to play a vital role in the development of this disease. CKD is also thought to be an inflammatory disorder in which uremic toxins participate in the development of the inflammatory milieu. A healthy, balanced diet supports the maintenance of a good health status as it helps to reduce the risk of the development of chronic diseases, including chronic kidney disease, diabetes mellitus, and hypertension. Numerous studies have demonstrated that functional molecules and nutrients, including fatty acids and fiber as well as nutraceuticals such as curcumin, steviol glycosides, and resveratrol not only exert beneficial effects on pro-inflammatory and anti-inflammatory pathways but also on gut mucosa. Nutraceuticals have attracted great interest recently due to their potential favorable physiological effects on the human body and their safety. This review presents some nutraceuticals in which consumption could exert a beneficial impact on the development and progression of renal disease as well cardiovascular disease. Full article

(This article belongs to the Special Issue Herbal Extracts and Natural Compounds: Nutraceutical and Pharmaceutical Aspects)

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