Pharmaceutics

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17 pages, 2953 KiB

Open AccessArticle

Eudraguard^® Natural and Protect: New “Food Grade” Matrices for the Delivery of an Extract from Sorbus domestica L. Leaves Active on the α-Glucosidase Enzyme

by Maria Rosaria Lauro, Patrizia Picerno, Silvia Franceschelli, Michela Pecoraro, Rita Patrizia Aquino and Rosario Pignatello

Pharmaceutics 2023, 15(1), 295; https://doi.org/10.3390/pharmaceutics15010295 - 16 Jan 2023

Cited by 3 | Viewed by 2029

Abstract

(1) Background: Eudraguard^® Natural (EN) and Protect (EP) are polymers regulated for use in dietary supplements in the European Union and the United States to carry natural products, mask unpleasant smells and tastes, ameliorate product handling, and protect products from moisture, light, [...] Read more.

(1) Background: Eudraguard^® Natural (EN) and Protect (EP) are polymers regulated for use in dietary supplements in the European Union and the United States to carry natural products, mask unpleasant smells and tastes, ameliorate product handling, and protect products from moisture, light, and oxidation. Moreover, EN and EP can control the release of encapsulated compounds. The aim of this work was the development, preparation, and control of Eudraguard^® spray-drying microparticles to obtain powders with easy handling and a stable dietary supplement containing a polar functional extract (SOE) from Sorbus domestica L. leaves. (2) Methods: SOE was characterized using HPLC, NMR, FTIR, DSC, and SEM methods. Furthermore, the SOE’s antioxidant/free radical scavenging activity, α-glucosidase inhibition, MTT assay effect on viability in normal cells, and shelf life were evaluated in both the extract and final formulations. (3) Results: The data suggested that SOE, rich in flavonoids, is a bioactive and safe extract; however, from a technological point of view, it was sticky, difficult to handle, and had low aqueous solubility. Despite the fact that EN and EP may undergo changes with spray-drying, they effectively produced easy-to-handle micro-powders with a controlled release profile. Although EN had a weaker capability to coat SOE than EP, EN acted as a substrate that was able to swell, drawing in water and improving the extract solubility and dissolution/release; however, EP was also able to carry the extract and provide SOE with controlled release. (4) Conclusion: Both Eudraguard^® products were capable of carrying SOE and improving its antioxidant and α-glucosidase inhibition activities, as well as the extract stability and handling. Full article

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

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15 pages, 1800 KiB

Open AccessArticle

Crocus sativus L. Petal Extract Inhibits Inflammation and Osteoclastogenesis in RAW 264.7 Cell Model

by Ciriana Orabona, Elena Orecchini, Claudia Volpi, Federico Bacaloni, Eleonora Panfili, Cinzia Pagano, Luana Perioli and Maria Laura Belladonna

Pharmaceutics 2022, 14(6), 1290; https://doi.org/10.3390/pharmaceutics14061290 - 17 Jun 2022

Cited by 11 | Viewed by 2361

Abstract

The dried stigmas of Crocus sativus L. (Iridaceae) are traditionally processed to produce saffron, a spice widely used as a food coloring and flavoring agent, which is important in the pharmaceutical and textile dye-producing industries. The labor-intensive by-hand harvesting and the use of [...] Read more.

The dried stigmas of Crocus sativus L. (Iridaceae) are traditionally processed to produce saffron, a spice widely used as a food coloring and flavoring agent, which is important in the pharmaceutical and textile dye-producing industries. The labor-intensive by-hand harvesting and the use of only a small amount of each flower cause saffron to be the most expensive spice in the world. Crocus sp. petals are by-products of saffron production and represent an interesting raw material for the preparation of extracts intended for health protection in the perspective of a circular economy. In the present study, ethanolic extract from Crocus sativus L. petals (Crocus sativus L. petal extract, CsPE) was tested on macrophages by in vitro models of inflammation and osteoclastogenesis. The extract was found to be endowed with anti-inflammatory activity, significantly reducing the nitric oxide production and IL-6 release by RAW 264.7 murine cells. Moreover, CsPE demonstrated an anti-osteoclastogenic effect, as revealed by a complete inhibition of tartrate-resistant acid phosphatase (TRAP)-positive osteoclast formation and a decreased expression of key osteoclast-related genes. This study, which focuses on the macrophage as the target cell of the bioactive extract from Crocus sativus L. petals, suggests that the petal by-product of saffron processing can usefully be part of a circular economy network aimed at producing an extract that potentially prevents bone disruption. Full article

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

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18 pages, 7856 KiB

Open AccessArticle

Hepatoprotective Effect of Carob Pulp Flour (Ceratonia siliqua L.) Extract Obtained by Optimized Microwave-Assisted Extraction

by Nikola Martić, Jana Zahorec, Nebojša Stilinović, Bojana Andrejić-Višnjić, Branimir Pavlić, Nebojša Kladar, Dragana Šoronja-Simović, Zita Šereš, Miodrag Vujčić, Olga Horvat and Aleksandar Rašković

Pharmaceutics 2022, 14(3), 657; https://doi.org/10.3390/pharmaceutics14030657 - 17 Mar 2022

Cited by 17 | Viewed by 3434

Abstract

To examine antioxidant capacity and the hepatoprotective effect of carob pulp flour, microwave-assisted extraction was performed. The influence of ethanol concentration (0–40% w/w), extraction time (5–25 min) and irradiation power (400–800 W) on DPPH, FRAP and ABTS antioxidant activity of [...] Read more.

To examine antioxidant capacity and the hepatoprotective effect of carob pulp flour, microwave-assisted extraction was performed. The influence of ethanol concentration (0–40% w/w), extraction time (5–25 min) and irradiation power (400–800 W) on DPPH, FRAP and ABTS antioxidant activity of carob pulp flour extract was evaluated. The strongest influence was that of the ethanol concentration, followed by extraction time. Optimal process parameters for maximizing total antioxidant activity were determined, using response surface methodology: ethanol concentration 40%, time 25 min and power 800 W. Carob extract obtained at optimal conditions (CE) was analyzed in vivo using a paracetamol-induced hepatotoxicity model in mice. Treatment with CE attenuated the parameters of liver injury, especially aspartate and alanine aminotransferase activity, and prevented paracetamol-induced increase in malondialdehyde levels. Pretreatment with CE reversed the activities of superoxide dismutase, catalase, glutathione peroxidase and glutathione S-transferase enzymes after the high dose of paracetamol in the liver. Hepatotoxicity induced using a toxic dose of paracetamol was also seen through histopathological alterations, which were significantly reduced in the groups treated with CE prior to paracetamol. Still, the number of Kupffer cells and macrophages did not differ among groups. Finally, pretreatment of mice with CE and paracetamol significantly decreased the expression of cytochrome P450 2E1 (CYP2E1) in hepatocytes. Full article

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

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12 pages, 1999 KiB

Open AccessArticle

Dihydroauroglaucin Isolated from the Mediterranean Sponge Grantia compressa Endophyte Marine Fungus Eurotium chevalieri Inhibits Migration of Human Neuroblastoma Cells

by Marzia Vasarri, Giovanni Andrea Vitale, Giovanna Cristina Varese, Emanuela Barletta, Maria Valeria D’Auria, Donatella de Pascale and Donatella Degl’Innocenti

Pharmaceutics 2022, 14(3), 616; https://doi.org/10.3390/pharmaceutics14030616 - 11 Mar 2022

Cited by 4 | Viewed by 2592

Abstract

Cancer cell migration is a hallmark of the aggressiveness and progression of malignancies such as high-risk neuroblastoma. Given the lack of effective therapeutic solutions to counteract cancer progression, basic research aims to identify novel bioactive molecules with inhibitory potential on cancer cell migration. [...] Read more.

Cancer cell migration is a hallmark of the aggressiveness and progression of malignancies such as high-risk neuroblastoma. Given the lack of effective therapeutic solutions to counteract cancer progression, basic research aims to identify novel bioactive molecules with inhibitory potential on cancer cell migration. In this context, this work investigated the role of members of the salicylaldehyde secondary metabolite set from the sponge endophyte fungus Eurotium chevalieri MUT 2316 as potential inhibitors of human neuroblastoma SH-SY5Y cell migration. Since tetrahydroauroglaucin (TAG) and dihydroauroglaucin (DAG) were isolated in large amounts, both were evaluated for their anticancer properties towards SH-SY5Y cells. Both molecules were found to be non-cytotoxic by MTT assay and cytofluorimetric analysis. Moreover, DAG showed efficacy in inhibiting the highly migratory phenotype of SH-SY5Y cells by wound healing assay; whereas TAG, although structurally similar to DAG, showed no anti-migratory effect. Therefore, this work provides good reasons to conduct further in vitro and in vivo studies focusing on DAG as a potentially useful migrastatic natural marine molecule. Full article

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

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17 pages, 648 KiB

Open AccessArticle

Unique Phenanthrenes from Juncus ensifolius and Their Antiproliferative and Synergistic Effects with the Conventional Anticancer Agent Doxorubicin against Human Cancer Cell Lines

by Dóra Stefkó, Norbert Kúsz, Nikoletta Szemerédi, Anita Barta, Gabriella Spengler, Róbert Berkecz, Judit Hohmann and Andrea Vasas

Pharmaceutics 2022, 14(3), 608; https://doi.org/10.3390/pharmaceutics14030608 - 10 Mar 2022

Cited by 4 | Viewed by 2126

Abstract

Phenanthrenes are the main special metabolites of Juncaceae species from phytochemical, pharmacological, and chemotaxonomical points of view. The present study focused on the isolation, structure determination, and pharmacological investigation of phenanthrenes from Juncus ensifolius. Nineteen compounds, including 17 phenanthrenes, were identified from [...] Read more.

Phenanthrenes are the main special metabolites of Juncaceae species from phytochemical, pharmacological, and chemotaxonomical points of view. The present study focused on the isolation, structure determination, and pharmacological investigation of phenanthrenes from Juncus ensifolius. Nineteen compounds, including 17 phenanthrenes, were identified from the methanol extract of the plant. Thirteen compounds, namely, ensifolins A–M (1–13), were obtained for the first time from natural sources. Four phenanthrenes [2-hydroxy-1,7-dimethyl-5-vinyl-9,10-dihydrophenanthrene (14), juncuenin B (15), juncatrin B (16), and sylvaticin A (17)], 4-hydroxybenzaldehyde (18) and luteolin (19) were isolated for the first time from J. ensifolius. Ensifolins A (1) and B (2) are structurally unique phenanthrenes, considering that they are flavonoid- (1) or benzaldehyde-adducts (2). The antiproliferative activity of all isolated compounds against HeLa, COLO 205, and COLO 320 cancer cells and a non-tumor (MRC-5) cell line was tested using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) viability assay. The luteolin-substituted phenanthrene ensifolin A (1) proved to be the most active against all three cancer cell lines (IC₅₀ values 3.9–12.7 μM) and showed good selectivity (SI = 4.95) in the case of COLO 205. The best selectivity was recorded for ensifolins D (4, SI > 5.15, HeLa), H (8, SI > 8.13, HeLa), and 17 (SI > 9.43, HeLa). The synergistic activity of the compounds with doxorubicin was also tested on HeLa cells, and ensifolins E (5) and H (8) exhibited very strong synergism (CI < 0.1). In conclusion, these phenanthrenes are worthy of further investigation. Full article

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

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16 pages, 10598 KiB

Open AccessArticle

Carotenoids from Persimmon (Diospyros kaki Thunb.) Byproducts Exert Photoprotective, Antioxidative and Microbial Anti-Adhesive Effects on HaCaT

by Sara Gea-Botella, Bryan Moreno-Chamba, Laura de la Casa, Julio Salazar-Bermeo, Nuria Martí, María Concepción Martínez-Madrid, Manuel Valero and Domingo Saura

Pharmaceutics 2021, 13(11), 1898; https://doi.org/10.3390/pharmaceutics13111898 - 8 Nov 2021

Cited by 6 | Viewed by 3001

Abstract

Persimmon (Diospyros kaki Thunb.) fruits are a remarkable source of carotenoids, which have shown protective effects against UV radiation in bacteria, fungi, algae, and plants. The aim of this study was to analyze the photoprotection provided by an acetone extract, rich in [...] Read more.

Persimmon (Diospyros kaki Thunb.) fruits are a remarkable source of carotenoids, which have shown protective effects against UV radiation in bacteria, fungi, algae, and plants. The aim of this study was to analyze the photoprotection provided by an acetone extract, rich in carotenoids and obtained from byproducts derived from the persimmon juice industry, against UV-induced cell death in the keratinocyte HaCaT cell line. For this purpose, the cytotoxicity and phototoxicity of carotenoid extract, as well as its intracellular reactive oxygen species (ROS) scavenging and anti-adhesive activities towards HaCaT cells, were evaluated. The in vitro permeation test provided information about the permeability of the carotenoid extract. Persimmon extracts, rich in carotenoids (PEC), were absorbed by HaCaT keratinocyte cells, which reduced the UV-induced intracellular ROS production in treated cells. Thus, PEC exerted a photoprotective and regenerative effect on UV-irradiated HaCaT cells, and this protection was UV dose-dependent. No cytotoxic effect was observed in HaCaT cultures at the concentration tested. PEC treatment also stimulated the adhesion capacity of skin microbiome to HaCaT cells, while exhibiting a significant anti-adhesive activity against all tested pathogens. In conclusion, PEC showed potential for use as a functional ingredient in skin-care products. Full article

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

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13 pages, 3126 KiB

Open AccessArticle

Broad Spectrum Antiviral Properties of Cardiotonic Steroids Used as Potential Therapeutics for Emerging Coronavirus Infections

by Young-Hee Jin, Sangeun Jeon, Jihye Lee, Seungtaek Kim, Min Seong Jang, Chul Min Park, Jong Hwan Song, Hyoung Rae Kim and Sunoh Kwon

Pharmaceutics 2021, 13(11), 1839; https://doi.org/10.3390/pharmaceutics13111839 - 2 Nov 2021

Cited by 17 | Viewed by 2510

Abstract

Cardiotonic steroids are steroid-like natural compounds known to inhibit Na⁺/K⁺-ATPase pumps. To develop a broad-spectrum antiviral drug against the emerging coronavirus infection, this study assessed the antiviral properties of these compounds. The activity of seven types of cardiotonic steroids [...] Read more.

Cardiotonic steroids are steroid-like natural compounds known to inhibit Na⁺/K⁺-ATPase pumps. To develop a broad-spectrum antiviral drug against the emerging coronavirus infection, this study assessed the antiviral properties of these compounds. The activity of seven types of cardiotonic steroids against the MERS-CoV, SARS-CoV, and SARS-CoV-2 coronavirus varieties was analyzed using immunofluorescence antiviral assay in virus-infected cells. Bufalin, cinobufagin, and telocinobufagin showed high anti-MERS-CoV activities (IC₅₀, 0.017~0.027 μM); bufalin showed the most potent anti-SARS-CoV and SARS-CoV-2 activity (IC₅₀, 0.016~0.019 μM); cinobufotalin and resibufogenin showed comparatively low anti-coronavirus activity (IC₅₀, 0.231~1.612 μM). Differentially expressed genes in Calu3 cells treated with cinobufagin, telocinobufagin, or bufalin, which had high antiviral activity during MERS-CoV infection were analyzed using QuantSeq 3′ mRNA-Seq analysis and data showed similar gene expression patterns. Furthermore, the intraperitoneal administration of 10 mg/kg/day bufalin, cinobufagin, or digitoxin induced 100% death after 1, 2, and 4 days in 5-day repeated dose toxicity studies and it indicated that bufalin had the strongest toxicity. Pharmacokinetic studies suggested that telocinobufagin, which had high anti-coronavirus activity and low toxicity, had better microsomal stability, lower CYP inhibition, and better oral bioavailability than cinobufagin. Therefore, telocinobufagin might be the most promising cardiotonic steroid as a therapeutic for emerging coronavirus infections, including COVID-19. Full article

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

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18 pages, 3988 KiB

Open AccessArticle

In Vitro Gingival Wound Healing Activity of Extracts from Reynoutria japonica Houtt Rhizomes

by Izabela Nawrot-Hadzik, Adam Matkowski, Artur Pitułaj, Barbara Sterczała, Cyprian Olchowy, Anna Szewczyk and Anna Choromańska

Pharmaceutics 2021, 13(11), 1764; https://doi.org/10.3390/pharmaceutics13111764 - 22 Oct 2021

Cited by 11 | Viewed by 2802

Abstract

Rhizomes of Reynoutria japonica Houtt. are a traditional Chinese medicinal herb (Polygoni cuspidati rhizoma, hu zhang) used for treatment of numerous diseases including wound healing support. The aim of this study was to provide evidence for the value of this herbal [...] Read more.

Rhizomes of Reynoutria japonica Houtt. are a traditional Chinese medicinal herb (Polygoni cuspidati rhizoma, hu zhang) used for treatment of numerous diseases including wound healing support. The aim of this study was to provide evidence for the value of this herbal drug’s traditional use as a gingival healing treatment as well as to obtain the most active extract. In vitro studies were performed using primary human gingival fibroblasts (HGFs) with determination of viability (MTT assay), cell proliferation (the confocal laser scanning microscope (CLSM) was used to visualize histone 3 expression), cell migration (wound healing assay), and evaluation of the expression of collagen type III (immunocytochemical staining) after incubation with extracts from R. japonica rhizomes (25% or 40% ethanol or 60% acetone). In addition to these extracts, commercial dental rinse (containing chlorhexidine digluconate 0.2%) was tested as the gold standard of choice for gum healing in dental practice. The studied extracts were qualitatively and quantitatively characterized using the validated HPLC/DAD/ESI-HR-QTOF-MS method. Total phenols and tannins content were determined using the Folin–Ciocalteu assay. Low concentration of all extracts after 24 h incubation caused significant increase in HGF viability. This effect was most pronounced at a concentration of 50 µg/mL, which was selected for further experiments. All extracts (at 50 µg/mL) stimulated HGF to proliferate, migrate, and increase collagen III synthesis, but with different strength. The highest stimulated proliferation and migration activity was observed after incubation with 25% EtOH, which according to phytochemical analysis may be related to the highest content of resveratrol and an appropriate composition of procyanidins. The 25% EtOH extract from R. japonica rhizomes appears to be a promising gingival wound healing agent worthy of animal and clinical trials. Full article

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

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16 pages, 1505 KiB

Open AccessArticle

A Novel Curcumin-Mycophenolic Acid Conjugate Inhibited Hyperproliferation of Tumor Necrosis Factor-Alpha-Induced Human Keratinocyte Cells

by Yonelian Yuyun, Pahweenvaj Ratnatilaka Na Bhuket, Wiwat Supasena, Piyapan Suwattananuruk, Kemika Praengam, Opa Vajragupta, Chawanphat Muangnoi and Pornchai Rojsitthisak

Pharmaceutics 2021, 13(7), 956; https://doi.org/10.3390/pharmaceutics13070956 - 25 Jun 2021

Cited by 9 | Viewed by 2843

Abstract

Curcumin (CUR) has been used as adjuvant therapy for therapeutic application in the treatment of psoriasis through several mechanisms of action. Due to the poor oral bioavailability of CUR, several approaches have been developed to overcome the limitations of CUR, including the prodrug [...] Read more.

Curcumin (CUR) has been used as adjuvant therapy for therapeutic application in the treatment of psoriasis through several mechanisms of action. Due to the poor oral bioavailability of CUR, several approaches have been developed to overcome the limitations of CUR, including the prodrug strategy. In this study, CUR was esterified with mycophenolic acid (MPA) as a novel conjugate prodrug. The MPA-CUR conjugate was structurally elucidated using FT-IR, ¹H-NMR, ¹³C-NMR, and MS techniques. Bioavailable fractions (BFs) across Caco-2 cells of CUR, MPA, and MPA-CUR were collected for further biological activity evaluation representing an in vitro cellular transport model for oral administration. The antipsoriatic effect of the BFs was determined using antiproliferation and anti-inflammation assays against hyperproliferation of tumor necrosis factor-alpha (TNF-α)-induced human keratinocytes (HaCaT). The BF of MPA-CUR provided better antiproliferation than that of CUR (p < 0.001). The enhanced hyperproliferation suppression of the BF of MPA-CUR resulted from the reduction of several inflammatory cytokines, including IL-6, IL-8, and IL-1β. The molecular mechanisms of anti-inflammatory activity were mediated by an attenuated signaling cascade of MAPKs protein, i.e., p38, ERK, and JNK. Our results present evidence for the MPA-CUR conjugate as a promising therapeutic agent for treating psoriasis by antiproliferative and anti-inflammatory actions. Full article

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

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18 pages, 7207 KiB

Open AccessArticle

Co-Delivery of Berberine Chloride and Tariquidar in Nanoliposomes Enhanced Intracellular Berberine Chloride in a Doxorubicin-Resistant K562 Cell Line Due to P-gp Overexpression

by Giulia Vanti, Marcella Coronnello, Daniele Bani, Antonella Mannini, Maria Camilla Bergonzi and Anna Rita Bilia

Pharmaceutics 2021, 13(3), 306; https://doi.org/10.3390/pharmaceutics13030306 - 26 Feb 2021

Cited by 25 | Viewed by 3170

Abstract

The MDR phenomenon has become a major obstacle in the treatment of cancers, and among the strategies to reverse it, the inhibition of P-gp function and expression is essential to increase for effective anticancer drugs. In the present paper, the co-delivery of berberine [...] Read more.

The MDR phenomenon has become a major obstacle in the treatment of cancers, and among the strategies to reverse it, the inhibition of P-gp function and expression is essential to increase for effective anticancer drugs. In the present paper, the co-delivery of berberine chloride and tariquidar loaded nanoliposomes was investigated with the aim of enhancing solubility and improving desired effects for the antineoplastic drug and the P-gp inhibitor. Developed nanoliposomes were loaded with the electron-dense enzyme horseradish peroxidase, and analyzed by TEM to investigate their ability to enter in both K562 and K562/DOXO cell lines. Receptor-mediated endocytosis was evidenced for both cell lines. Nanoliposomes were loaded with tariquidar, berberine chloride, or both, maintaining chemical and physical characteristics—i.e., size, homogeneity, and encapsulation efficiency—and high suitability for parenteral administration. Tariquidar was able to reverse the MDR in the K562/DOXO cell line. Tariquidar- and berberine chloride-loaded nanoliposomes showed a significant increase of berberine chloride accumulation in tumor cells, which could be correlated with resensitization of the resistant cells to the antitumor agent. These results suggest that the co-delivery of the P-gp inhibitor, tariquidar, and the cytotoxicity inducer, berberine chloride, looks like a promising approach to overcome the MDR. Full article

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

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Review

Jump to: Research

23 pages, 1599 KiB

Open AccessReview

An Updated Systematic Review of Vaccinium myrtillus Leaves: Phytochemistry and Pharmacology

by Ruxandra Ștefănescu, Eszter Laczkó-Zöld, Bianca-Eugenia Ősz and Camil-Eugen Vari

Pharmaceutics 2023, 15(1), 16; https://doi.org/10.3390/pharmaceutics15010016 - 21 Dec 2022

Cited by 12 | Viewed by 2595

Abstract

Bilberry leaves are used in many countries in traditional medicine for treating a wide variety of diseases. Due to the high therapeutic potential of Vaccinium myrtillus (VM) leaves, this review aims to present the latest knowledge on the phytochemical profile, as well as [...] Read more.

Bilberry leaves are used in many countries in traditional medicine for treating a wide variety of diseases. Due to the high therapeutic potential of Vaccinium myrtillus (VM) leaves, this review aims to present the latest knowledge on the phytochemical profile, as well as the therapeutic effects of this herbal drug. The review was conducted according to the Prisma guidelines, and the scientific databases were searched using combinations of the following keywords: “Vaccinium myrtillus”, “leaves”, “bilberry”. Recent research was focused on the influence of abiotic factors on the phytochemical composition, and it seems that there are significant differences between the herbal drugs collected from different countries. The phytochemical composition is correlated with the broad spectrum of pharmacological effects. The paper outlines the potent antimicrobial activity of VM extracts against multidrug-resistant bacterial strains, and also the pathways that are modulated by the unique “cocktail” of phytoconstituents in different metabolic alterations. Reviewing the research articles published in the last 10 years, it seems that bilberry leaves have been slightly forgotten, although their phytochemical and pharmacological characteristics are unique. Full article

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

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12 pages, 1885 KiB

Open AccessReview

Natural Products from Mangroves: An Overview of the Anticancer Potential of Avicennia marina

by Federico Cerri, Marco Giustra, Yaprak Anadol, Giulia Tomaino, Paolo Galli, Massimo Labra, Luca Campone and Miriam Colombo

Pharmaceutics 2022, 14(12), 2793; https://doi.org/10.3390/pharmaceutics14122793 - 14 Dec 2022

Cited by 8 | Viewed by 3223

Abstract

Exploring the potential of natural extracts for pharmaceutical applications in the treatment of different diseases is an emerging field of medical research, owing to the tremendous advantages that they can offer. These include compound sustainability due to the natural origin and virtually unlimited [...] Read more.

Exploring the potential of natural extracts for pharmaceutical applications in the treatment of different diseases is an emerging field of medical research, owing to the tremendous advantages that they can offer. These include compound sustainability due to the natural origin and virtually unlimited availability. In addition, they contribute to promoting the countries in which they are extracted and manufactured. For this reason, wild active compounds derived from plants are attracting increasing interest due to their beneficial properties. Among them, Avicennia marina has been recently recognized as a potential source of natural substances with therapeutic activities for anti-cancer treatment. A. marina beneficially supplies different chemical compounds, including cyclic triterpenoids, flavonoids, iridoids, naphtaquinones, polyphenols, polysaccharides, and steroids, most of them exhibiting potent antitumor activity. The in vivo and in vitro studies on different models of solid tumors demonstrated its dose-dependent activity. Moreover, the possibility to formulate the A. marina extracted molecules in nanoparticles allowed researchers to ameliorate the therapeutic outcome of treatments exploiting improved selectivity toward cancer cells, thus reducing the side effects due to nonspecific spread. Full article

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

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17 pages, 1311 KiB

Open AccessReview

The Role of Glucosinolates from Cruciferous Vegetables (Brassicaceae) in Gastrointestinal Cancers: From Prevention to Therapeutics

by Catarina Melim, Maria R. Lauro, Isabel M. Pires, Paulo J. Oliveira and Célia Cabral

Pharmaceutics 2022, 14(1), 190; https://doi.org/10.3390/pharmaceutics14010190 - 14 Jan 2022

Cited by 29 | Viewed by 6080

Abstract

The gastrointestinal (GI) tract is composed of rapidly renewing cells, which increase the likelihood of cancer. Colorectal cancer is one of the most frequently diagnosed GI cancers and currently stands in second place regarding cancer-related mortality. Unfortunately, the treatment of GI is limited, [...] Read more.

The gastrointestinal (GI) tract is composed of rapidly renewing cells, which increase the likelihood of cancer. Colorectal cancer is one of the most frequently diagnosed GI cancers and currently stands in second place regarding cancer-related mortality. Unfortunately, the treatment of GI is limited, and few developments have occurred in the field over the years. With this in mind, new therapeutic strategies involving biologically active phytocompounds are being evaluated as anti-cancer agents. Vegetables such as broccoli, brussels sprouts, cabbage, cauliflower, and radish, all belonging to the Brassicaceae family, are high in dietary fibre, minerals, vitamins, carotenoids, polyphenols, and glucosinolates. The latter compound is a secondary metabolite characteristic of this family and, when biologically active, has demonstrated anti-cancer properties. This article reviews the literature regarding the potential of Cruciferous vegetables in the prevention and/or treatment of GI cancers and the relevance of appropriate compound formulations for improving the stability and bioaccessibility of the major Cruciferous compounds, with a particular focus on glucosinolates. Full article

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

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32 pages, 920 KiB

Open AccessReview

Red Seaweed-Derived Compounds as a Potential New Approach for Acne Vulgaris Care

by Adriana P. Januário, Rafael Félix, Carina Félix, João Reboleira, Patrícia Valentão and Marco F. L. Lemos

Pharmaceutics 2021, 13(11), 1930; https://doi.org/10.3390/pharmaceutics13111930 - 15 Nov 2021

Cited by 11 | Viewed by 4831

Abstract

Acne vulgaris (AV) is a chronic skin disease of the pilosebaceous unit affecting both adolescents and adults. Its pathophysiology includes processes of inflammation, increased keratinization, sebum production, hormonal dysregulation, and bacterial Cutibacterium acnes proliferation. Common AV has been treated with antibiotics since the [...] Read more.

Acne vulgaris (AV) is a chronic skin disease of the pilosebaceous unit affecting both adolescents and adults. Its pathophysiology includes processes of inflammation, increased keratinization, sebum production, hormonal dysregulation, and bacterial Cutibacterium acnes proliferation. Common AV has been treated with antibiotics since the 1960s, but strain resistance has emerged and is of paramount concern. Macroalgae are known producers of substances with bioactive properties, including anti-viral, antibacterial, antioxidant, and anti-inflammatory properties, among several others. In particular, red algae are rich in bioactive compounds such as polysaccharides, phenolic compounds, lipids, sterols, alkaloids, and terpenoids, conferring them antioxidant, antimicrobial, and anti-inflammatory activities, among others. Thus, the exploration of compounds from marine resources can be an appealing approach to discover new treatment options against AV. The aim of this work is to provide an overview of the current knowledge of the potentialities of red macroalgae in the treatment of AV by reviewing the main therapeutic targets of this disease, and then the existence of compounds or extracts with bioactive properties against them. Full article

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

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