Research

Jump to: Review

20 pages, 2425 KiB

Open AccessArticle

Zeaxanthin-Rich Extract from Superfood Lycium barbarum Selectively Modulates the Cellular Adhesion and MAPK Signaling in Melanoma versus Normal Skin Cells In Vitro

by Diana Cenariu, Eva Fischer-Fodor, Adrian Bogdan Țigu, Andrea Bunea, Piroska Virág, Maria Perde-Schrepler, Vlad-Alexandru Toma, Andrei Mocan, Ioana Berindan-Neagoe, Adela Pintea, Gianina Crișan, Mihai Cenariu and Alma Maniu

Molecules 2021, 26(2), 333; https://doi.org/10.3390/molecules26020333 - 11 Jan 2021

Cited by 19 | Viewed by 2815

Abstract

The concern for implementing bioactive nutraceuticals in antioxidant-related therapies is of great importance for skin homeostasis in benign or malignant diseases. In order to elucidate some novel insights of Lycium barbarum (Goji berry) activity on skin cells, the present study focused on its [...] Read more.

The concern for implementing bioactive nutraceuticals in antioxidant-related therapies is of great importance for skin homeostasis in benign or malignant diseases. In order to elucidate some novel insights of Lycium barbarum (Goji berry) activity on skin cells, the present study focused on its active compound zeaxanthin. By targeting the stemness markers CD44 and CD105, with deep implications in skin oxidative stress mechanisms, we revealed, for the first time, selectivity in zeaxanthin activity. When applied in vitro on BJ human fibroblast cell line versus the A375 malignant melanoma cells, despite the moderate cytotoxicity, the zeaxanthin-rich extracts 1 and 2 were able to downregulate significantly the CD44 and CD105 membrane expression and extracellular secretion in A375, and to upregulate them in BJ cells. At mechanistic level, the present study is the first to demonstrate that the zeaxanthin-rich Goji extracts are able to influence selectively the mitogen-activated protein kinases (MAPK): ERK, JNK and p38 in normal BJ versus tumor-derived A375 skin cells. These results point out towards the applications of zeaxanthin from L. barbarum as a cytoprotective agent in normal skin and raises questions about its use as an antitumor prodrug alone or in combination with standard therapy. Full article

(This article belongs to the Special Issue Natural Product Pharmacology and Medicinal Chemistry II)

► Show Figures

Figure 1

14 pages, 5201 KiB

Open AccessArticle

Anti-Inflammatory and Neuromodulatory Effects Induced by Tanacetum parthenium Water Extract: Results from In Silico, In Vitro and Ex Vivo Studies

by Lucia Recinella, Annalisa Chiavaroli, Viviana di Giacomo, Marco Daniel Antolini, Alessandra Acquaviva, Sheila Leone, Luigi Brunetti, Luigi Menghini, Gunes Ak, Gokhan Zengin, Simonetta Cristina Di Simone, Claudio Ferrante and Giustino Orlando

Molecules 2021, 26(1), 22; https://doi.org/10.3390/molecules26010022 - 23 Dec 2020

Cited by 14 | Viewed by 3405

Abstract

Tanacetum parthenium (feverfew) has traditionally been employed as a phytotherapeutic remedy in the treatment of migraine. In this study, a commercial T. parthenium water extract was investigated to explore its anti-inflammatory and neuromodulatory effects. Isolated mouse cortexes were exposed to a K⁺ [...] Read more.

Tanacetum parthenium (feverfew) has traditionally been employed as a phytotherapeutic remedy in the treatment of migraine. In this study, a commercial T. parthenium water extract was investigated to explore its anti-inflammatory and neuromodulatory effects. Isolated mouse cortexes were exposed to a K⁺ 60 mM Krebs-Ringer buffer and treated with T. parthenium water extract. The prostaglandin E₂ (PGE₂) level, brain-derived neurotrophic factor (BDNF), interleukin-10 (IL-10), and IL-1β gene expression were evaluated in the cortex. The effects on dopamine (DA) release and dopamine transporter (DAT) gene expression were assayed in hypothalamic HypoE22 cells. A bioinformatics analysis was conducted to further investigate the mechanism of action. The extract was effective in reducing cortex PGE₂ release and IL-1β gene expression. In the same experimental system, IL-10 and BDNF gene expressions increased, and in HypoE22 cells, the extract decreased the extracellular dopamine level and increased the DAT gene expression due to the direct interaction of parthenolide with the DAT. Overall, the present findings highlight the efficacy of T. parthenium water extract in controlling the inflammatory pathways that occur during cortical-spreading depression. Additionally, the inhibition of the hypothalamic DA release observed in this study further supports the role of dopaminergic pathways as key targets for novel pharmacological approaches in the management of migraine attacks. Full article

(This article belongs to the Special Issue Natural Product Pharmacology and Medicinal Chemistry II)

► Show Figures

Figure 1

15 pages, 764 KiB

Open AccessArticle

Biological Activities of Selected Plants and Detection of Bioactive Compounds from Ardisia elliptica Using UHPLC-Q-Exactive Orbitrap Mass Spectrometry

by Pei Lou Wong, Nurul Azila Fauzi, Siti Norhamimah Mohamed Yunus, Nur Ashikin Abdul Hamid, Siti Zulaikha Abd Ghafar, Awanis Azizan, Nur Khaleeda Zulaikha Zolkeflee and Faridah Abas

Molecules 2020, 25(13), 3067; https://doi.org/10.3390/molecules25133067 - 06 Jul 2020

Cited by 6 | Viewed by 3367

Abstract

Plants and plant-based products have been used for a long time for medicinal purposes. This study aimed to determine the antioxidant and anti-α-glucosidase activities of eight selected underutilized plants in Malaysia: Leucaena leucocephala, Muntingia calabura, Spondias dulcis, Annona squamosa, Ardisia elliptica, Cynometra cauliflora, [...] Read more.

Plants and plant-based products have been used for a long time for medicinal purposes. This study aimed to determine the antioxidant and anti-α-glucosidase activities of eight selected underutilized plants in Malaysia: Leucaena leucocephala, Muntingia calabura, Spondias dulcis, Annona squamosa, Ardisia elliptica, Cynometra cauliflora, Ficus auriculata, and Averrhoa bilimbi. This study showed that the 70% ethanolic extract of all plants exhibited total phenolic content (TPC) ranging from 51 to 344 mg gallic acid equivalent (GAE)/g dry weight. A. elliptica showed strong 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide (NO) scavenging activities, with half maximal inhibitory concentration (IC₅₀) values of 2.17 and 49.43 μg/mL, respectively. Most of the tested plant extracts showed higher inhibition of α-glucosidase enzyme activity than the standard, quercetin, particularly A. elliptica, F. auriculata, and M. calabura extracts with IC₅₀ values of 0.29, 0.36, and 0.51 μg/mL, respectively. A total of 62 metabolites including flavonoids, triterpenoids, benzoquinones, and fatty acids were tentatively identified in the most active plant, i.e., A. elliptica leaf extract, by using ultra-high-performance liquid chromatography (UHPLC)–electrospray ionization (ESI) Orbitrap MS. This study suggests a potential natural source of antioxidant and α-glucosidase inhibitors from A. elliptica. Full article

(This article belongs to the Special Issue Natural Product Pharmacology and Medicinal Chemistry II)

► Show Figures

Figure 1

17 pages, 5298 KiB

Open AccessArticle

In Vivo Wound Healing and In Vitro Anti-Inflammatory Activity Evaluation of Phlomis russeliana Extract Gel Formulations

by Mehmet Evren Okur, Ayşe Esra Karadağ, Neslihan Üstündağ Okur, Yağmur Özhan, Hande Sipahi, Şule Ayla, Benay Daylan, Betül Demirci and Fatih Demirci

Molecules 2020, 25(11), 2695; https://doi.org/10.3390/molecules25112695 - 10 Jun 2020

Cited by 26 | Viewed by 4623

Abstract

The air-dried aerial parts of Phlomis russeliana (Sims) Lag. Ex Benth. was extracted by methanol and fractionated by n-hexane, dichloromethane, and ethyl acetate, respectively. The wound healing properties of P. russeliana extract gel was evaluated using the in vivo excisional wound model [...] Read more.

The air-dried aerial parts of Phlomis russeliana (Sims) Lag. Ex Benth. was extracted by methanol and fractionated by n-hexane, dichloromethane, and ethyl acetate, respectively. The wound healing properties of P. russeliana extract gel was evaluated using the in vivo excisional wound model using Balb-c mice. Initially, the P. russeliana methanol extract showed LOX inhibitory activity at IC₅₀ = 23.2 µg/mL, whereas the DPPH^• assay showed IC₅₀ = 0.89 mg/mL, and the ABTS^• assay showed IC₅₀ = 0.99 mg/mL, respectively. In addition, a remarkable anti-inflammatory activity was observed in the cell culture assay. Thereafter, activity-guided fractionation was performed by LOX enzyme inhibition assays, and the structures of the two most active fractions were revealed by both GC–FID and GC/MS analyses, simultaneously. Phytol and 1-heptadecanoic acid were characterized as the active constituents. Moreover, the P. russeliana extract gel formulation was applied for in vivo tests, where the new gel formulation supported the in vitro anti-inflammatory activity findings. As a conclusion, this experimental results support the wound healing evidence based on the ethnobotanical application of Phlomis species with further potential. Full article

(This article belongs to the Special Issue Natural Product Pharmacology and Medicinal Chemistry II)

► Show Figures

Figure 1

22 pages, 17009 KiB

Open AccessArticle

Panax quinquefolium L. Ginsenosides from Hairy Root Cultures and Their Clones Exert Cytotoxic, Genotoxic and Pro-Apoptotic Activity towards Human Colon Adenocarcinoma Cell Line Caco-2

by Ewa Kochan, Adriana Nowak, Małgorzata Zakłos-Szyda, Daria Szczuka, Grażyna Szymańska and Ilona Motyl

Molecules 2020, 25(9), 2262; https://doi.org/10.3390/molecules25092262 - 11 May 2020

Cited by 12 | Viewed by 3302

Abstract

American ginseng, Panax quinquefolium (L.), is traditionally used in folk medicine. It exhibits a range of anti-inflammatory, hepatoprotective, anti-diabetic, anti-obesity, anti-hyperlipidemic and anti-carcinogenic effects. Its main components are ginsenosides, also known as panaxosides or triterpene saponins. In order to obtain high yields of [...] Read more.

American ginseng, Panax quinquefolium (L.), is traditionally used in folk medicine. It exhibits a range of anti-inflammatory, hepatoprotective, anti-diabetic, anti-obesity, anti-hyperlipidemic and anti-carcinogenic effects. Its main components are ginsenosides, also known as panaxosides or triterpene saponins. In order to obtain high yields of ginsenosides, different methods of controlled production are involved, i.e., with hairy root cultures. However, they are still employed under in vitro conditions. Our studies revealed that hairy root cultures subjected to an elicitation process can be considered as a potent source of ginsenosides. The present study examines the biological activity of ginseng hairy root cultures against the Caco-2 human adenocarcinoma cell line. Among our six different clones of P. quinquefolium hairy roots, extracts B and Be (treated with elicitor) were the strongest inhibitors of the cellular metabolic activity. While all extracts induced DNA damage, B and Be also generated reactive oxygen species (ROS) in a concentration-dependent manner, which was correlated with the depletion of the mitochondrial membrane potential and induction of apoptosis. These findings indicate that further research concerning P. quinquefolium hairy root cultures should focus on the activity of rare ginsenosides and other biologically active compound profiles (i.e., phenolic compounds). Full article

(This article belongs to the Special Issue Natural Product Pharmacology and Medicinal Chemistry II)

► Show Figures

Graphical abstract

21 pages, 1340 KiB

Open AccessArticle

Walnut (Juglans regia L.) Septum: Assessment of Bioactive Molecules and In Vitro Biological Effects

by Marius Emil Rusu, Ionel Fizesan, Anca Pop, Andrei Mocan, Ana-Maria Gheldiu, Mihai Babota, Dan Cristian Vodnar, Ancuta Jurj, Ioana Berindan-Neagoe, Laurian Vlase and Daniela-Saveta Popa

Molecules 2020, 25(9), 2187; https://doi.org/10.3390/molecules25092187 - 07 May 2020

Cited by 42 | Viewed by 4429

Abstract

Walnut (Juglans regia L.) septum represents an interesting bioactive compound source by-product. In our study, a rich phenolic walnut septum extract, previously selected, was further examined. The tocopherol content determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS) revealed higher amounts of α-tocopherol compared [...] Read more.

Walnut (Juglans regia L.) septum represents an interesting bioactive compound source by-product. In our study, a rich phenolic walnut septum extract, previously selected, was further examined. The tocopherol content determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS) revealed higher amounts of α-tocopherol compared to γ- and δ-tocopherols. Moreover, several biological activities were investigated. The in vitro inhibiting assessment against acetylcholinesterase, α-glucosidase, or lipase attested a real management potential in diabetes or obesity. The extract demonstrated very strong antimicrobial potential against Staphylococcus aureus, Pseudomonas aeruginosa and Salmonella enteritidis. It also revealed moderate (36.08%) and strong (43.27%) antimutagenic inhibitory effects against TA 98 and TA 100 strains. The cytotoxicity of the extract was assessed on cancerous (A549, T47D-KBluc, MCF-7) and normal (human gingival fibroblasts (HGF)) cell lines. Flow cytometry measurements confirmed the cytotoxicity of the extract in the cancerous cell lines. Additionally, the extract demonstrated antioxidant activity on all four cell types, as well as anti-inflammatory activity by lowering the inflammatory cytokines (interleukin-6 (IL-6), interleukin-8 (IL-8), interleukin-1 β (IL-1β)) evaluated in HGF cells. To the best of our knowledge, most of the cellular model analyses were performed for the first time in this matrix. The results prove that walnut septum may be a potential phytochemical source for pharmaceutical and food industry. Full article

(This article belongs to the Special Issue Natural Product Pharmacology and Medicinal Chemistry II)

► Show Figures

Graphical abstract

19 pages, 1270 KiB

Open AccessArticle

Phytocomplex Characterization and Biological Evaluation of Powdered Fruits and Leaves from Elaeagnus angustifolia

by Simone Carradori, Francesco Cairone, Stefania Garzoli, Giancarlo Fabrizi, Antonia Iazzetti, Anna Maria Giusti, Luigi Menghini, Sengul Uysal, Gunes Ak, Gokhan Zengin and Stefania Cesa

Molecules 2020, 25(9), 2021; https://doi.org/10.3390/molecules25092021 - 26 Apr 2020

Cited by 21 | Viewed by 3839

Abstract

Fully ripe fruits and mature leaves of Elaeagnus angustifolia were harvested and analyzed by means of analytical and biological tests to better comprehend the chemical composition and therapeutic/nutraceutical potential of this plant. Fruits and leaves were dried and the obtained powders were analyzed [...] Read more.

Fully ripe fruits and mature leaves of Elaeagnus angustifolia were harvested and analyzed by means of analytical and biological tests to better comprehend the chemical composition and therapeutic/nutraceutical potential of this plant. Fruits and leaves were dried and the obtained powders were analyzed to study their color character and (via headspace gas chromatography) describe the chemical profile. Subsequently, they were submitted to a chloroform–methanol extraction, to a hydroalcoholic extraction procedure assisted or not by microwaves, and to an extraction with supercritical CO₂, assisted or not by ethanol as the co-solvent, to detect the polyphenolic and the volatile content. The resulting extracts were evaluated in terms of chlorophyll and carotenoid content, polyphenolic content, volatile fraction, total phenolic content, total flavonoid content, antioxidant activity, radical scavenging activity, and enzymatic inhibition activity. The results confirmed the correlation between the chemical composition and the high antioxidant potential of leaf extracts compared to the fruit extracts in terms of the phenolic and pigment content. A promising effect against tyrosinase emerged for all the extracts, suggesting a therapeutic/nutraceutical use for this plant. Conversely, the volatile content from both natural matrices was similar. Full article

(This article belongs to the Special Issue Natural Product Pharmacology and Medicinal Chemistry II)

► Show Figures

Figure 1

13 pages, 2736 KiB

Open AccessArticle

Natural Compounds Rosmarinic Acid and Carvacrol Counteract Aluminium-Induced Oxidative Stress

by Juste Baranauskaite, Ilona Sadauskiene, Arunas Liekis, Arturas Kasauskas, Robertas Lazauskas, Ugne Zlabiene, Ruta Masteikova, Dalia M. Kopustinskiene and Jurga Bernatoniene

Molecules 2020, 25(8), 1807; https://doi.org/10.3390/molecules25081807 - 15 Apr 2020

Cited by 25 | Viewed by 3482

Abstract

Aluminum accumulation, glutathione (GSH) and malondialdehyde (MDA) concentrations as well as catalase (CAT) and superoxide dismutase (SOD) activities were determined in erythrocytes and brain and liver homogenates of BALB/c mice treated with Al³⁺ (7.5 mg/kg/day (0.15 LD₅₀) as AlCl₃ [...] Read more.

Aluminum accumulation, glutathione (GSH) and malondialdehyde (MDA) concentrations as well as catalase (CAT) and superoxide dismutase (SOD) activities were determined in erythrocytes and brain and liver homogenates of BALB/c mice treated with Al³⁺ (7.5 mg/kg/day (0.15 LD₅₀) as AlCl₃ (37.08 mg/kg/day), whereas HCl (30.41 mg/kg/day) was used as Cl⁻ control, the treatments were performed for 21 days, i.p., in the presence and absence of rosmarinic acid (0.2805 mg/kg/day (0.05 LD₅₀), 21 days, i.g.) or carvacrol (0.0405 mg/kg/day (0.05 LD₅₀), 21 days, i.g.). The treatment with AlCl₃ increased GSH concentration in erythrocytes only slightly and had no effect on brain and liver homogenates. Rosmarinic acid and carvacrol strongly increased GSH concentration in erythrocytes but decreased it in brain and liver homogenates. However, AlCl₃ treatment led to Al accumulation in mice blood, brain, and liver and induced oxidative stress, assessed based on MDA concentration in the brain and liver. Both rosmarinic acid and carvacrol were able to counteract the negative Al effect by decreasing its accumulation and protecting tissues from lipid peroxidation. AlCl₃ treatment increased CAT activity in mice brain and liver homogenates, whereas the administration of either rosmarinic acid or carvacrol alone or in combination with AlCl₃ had no significant effect on CAT activity. SOD activity remained unchanged after all the treatments in our study. We propose that natural herbal phenolic compounds rosmarinic acid and carvacrol could be used to protect brain and liver against aluminum induced oxidative stress leading to lipid peroxidation. Full article

(This article belongs to the Special Issue Natural Product Pharmacology and Medicinal Chemistry II)

► Show Figures

Figure 1

Review

Jump to: Research

19 pages, 666 KiB

Open AccessReview

Antimicrobials from Venomous Animals: An Overview

by Tania Yacoub, Mohamad Rima, Marc Karam, Jean-Marc Sabatier and Ziad Fajloun

Molecules 2020, 25(10), 2402; https://doi.org/10.3390/molecules25102402 - 21 May 2020

Cited by 52 | Viewed by 7670

Abstract

The inappropriate or excessive use of antimicrobial agents caused an emerging public health problem due to the resulting resistance developed by microbes. Therefore, there is an urgent need to develop effective antimicrobial strategies relying on natural agents with different mechanisms of action. Nature [...] Read more.

The inappropriate or excessive use of antimicrobial agents caused an emerging public health problem due to the resulting resistance developed by microbes. Therefore, there is an urgent need to develop effective antimicrobial strategies relying on natural agents with different mechanisms of action. Nature has been known to offer many bioactive compounds, in the form of animal venoms, algae, and plant extracts that were used for decades in traditional medicine. Animal venoms and secretions have been deeply studied for their wealth in pharmaceutically promising molecules. As such, they were reported to exhibit many biological activities of interest, such as antibacterial, antiviral, anticancer, and anti-inflammatory activities. In this review, we summarize recent findings on the antimicrobial activities of crude animal venoms/secretions, and describe the peptides that are responsible of these activities. Full article

(This article belongs to the Special Issue Natural Product Pharmacology and Medicinal Chemistry II)

► Show Figures

Graphical abstract

Journal Menu

Journal Browser

Natural Product Pharmacology and Medicinal Chemistry II

Share This Special Issue

Special Issue Editors

Special Issue Information

Published Papers (9 papers)

Research

Review

Further Information

Guidelines

MDPI Initiatives

Follow MDPI