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Biological Activities of Natural Products
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Biological Activities of Natural Products

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (30 September 2020) | Viewed by 134120

Special Issue Editors

Prof. Dr. Halina Ekiert

E-Mail Website
Guest Editor
Head of Chair and Department of Pharmaceutical Botany, Pharmaceutical Faculty, Jagiellonian University, Medical College, Krakow, Poland
Interests: pharmaceutical botany; plant biotechnology (plant in vitro cultures, endogenic production of bioactive products; biotransformation of egzogenic substrates); phytochemistry (quantification of natural products, isolation of natural products); medicinal plants; cosmetic plants, biotechnology of mushrooms; mycochemistry (chemistry of fruitbodies of mushrooms and mycelial cultures); natural products; bioactive compounds (especially coumarins, phenolic acids, flavonoids, schisandra lignans, nonhalucinogenic indole compounds, and polysaccharides); ethnobotany; ethnopharmacology
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Agnieszka Szopa

E-Mail Website1 Website2
Guest Editor
Department of Pharmaceutical Botany, Medical College, Jagiellonian University, ul. Medyczna 9, 30-688 Kraków, Poland
Interests: plant biotechnology; phytochemistry; phytotherapy; lignans; polyphenols
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Natural products originating from the plant kingdom offer an unexplored wealth of potential valuable medicinal, health promoting and cosmetic applications.

In recent years, special attention has been given to natural products exhibiting antioxidant and antiproliferative/anticancer properties. They are of vital importance since they can be used in the treatment and prevention of different lifestyle diseases. Plant extracts and/or isolated compounds exhibiting other directions of biological activities, such as anti-inflammatory, immunostimulating or antimicrobial effects and also cardioprotective, neuroprotective, and antidiabetic activities, are also very significant.

The results of biological activity studies of to date unknown and/or uninvestigated natural products can broaden the range of professional phytotherapeutics available in different regions of the world, including Europe. The selection of plant-derived medicinal products can also be expanded through the verification of ethnobotanical and ethnopharmacological knowledge of various ethnic groups in the world.

In addition to plants, fruitbodies of mushrooms, algae, and lichens are rich and still unrecognized sources of natural products.

The main aim of the Special Issue on “Biological Activities of Natural Products” is to present the newest results of investigations and findings in the above-presented area. Results presenting the correlation between chemical composition of extracts and/or isolated compounds and their biological activity are particularly welcome. Research on antioxidant and antiproliferative/anticancer activities of extracts and/or isolated products will be preferentially considered. All research on other above-mentioned activities will also be expected with much interest. The results of biological activity studies documented in vitro and in vivo, and also results of clinical investigations, will be anticipated.

Original papers or review articles are welcome.

Dr. Agnieszka Szopa
Prof. Dr. Halina Ekiert
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Bioactive natural compounds
  • Antioxidants
  • Polyphenols
  • Antioxidant activity
  • Anticancer/antiproliferative activity
  • Anti-inflammatory activity
  • Immunostimulating activity
  • Antimicrobial activity
  • Other activities
  • In vitro approach
  • In vivo approach
  • Clinical investigations
  • Ethnopharmacological indications
  • Ethnobotanical indications

Published Papers (31 papers)

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Editorial

Jump to: Research, Review

7 pages, 221 KiB  
Editorial
Biological Activities of Natural Products
by Halina Maria Ekiert and Agnieszka Szopa
Molecules 2020, 25(23), 5769; https://doi.org/10.3390/molecules25235769 - 07 Dec 2020
Cited by 52 | Viewed by 4472
Abstract
Natural products and their biological activities are currently a subject of great interest in the pharmaceutical, health food, and cosmetics industries, and numbers of scientific studies in this field are increasing rapidly [...] Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)

Research

Jump to: Editorial, Review

18 pages, 1576 KiB  
Article
Health-Promoting Compounds in Stevia: The Effect of Mycorrhizal Symbiosis, Phosphorus Supply and Harvest Time
by Silvia Tavarini, Clarissa Clemente, Cecilia Bender and Luciana G. Angelini
Molecules 2020, 25(22), 5399; https://doi.org/10.3390/molecules25225399 - 18 Nov 2020
Cited by 11 | Viewed by 2167
Abstract
This work aimed to establish the synergic role of arbuscular mycorrhizal fungi (AMF) symbiosis, phosphorus (P) fertilization and harvest time on the contents of stevia secondary metabolites. Consequently, steviol glycosides (SVglys) concentration and profile, total phenols and flavonoids as well as antioxidant assays, [...] Read more.
This work aimed to establish the synergic role of arbuscular mycorrhizal fungi (AMF) symbiosis, phosphorus (P) fertilization and harvest time on the contents of stevia secondary metabolites. Consequently, steviol glycosides (SVglys) concentration and profile, total phenols and flavonoids as well as antioxidant assays, have been assessed in inoculated and no-inoculated plants, grown with or without P supply and collected at different growth stages(69, 89 and 123 days after transplanting).The obtained results suggest that the synthesis of stevia secondary metabolites is induced and/or modulated by all the investigated variability factors. In particular, AMF symbiosis promoted total SVglys content and positively influenced the concentration of some minor compounds (steviolbioside, dulcoside A and rebaudioside B), indicating a clear effect of mycorrhizal inoculation on SVglys biosynthetic pathway. Interestingly, only the mycorrhizal plants were able to synthesize rebaudioside B. In addition, P supply provided the highest levels of total phenols and flavonoids at leaf level, together with the maximum in vitro antioxidant activities (FRAP and ORAC). Finally, the harvest time carried out during the full vegetative phase enhanced the entire composition of the phytocomplex (steviolbioside, dulcoside A, stevioside, rebaudioside A, B, C. total phenols and flavonoids). Moreover, polyphenols and SVglys appeared to be the main contributors to the in vitro antioxidant capacity, while only total phenols mostly contributed to the cellular antioxidant activity (CAA). These findings provide original information about the role played by AMF in association with P supply, in modulating the accumulation of bioactive compounds during stevia growth. At the cultivation level, the control of these preharvest factors, together with the most appropriate harvest time, can be used as tools for improving the nutraceutical value of raw material, with particular attention to its exploitation as functional ingredient for food and dietary supplements and cosmetics. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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23 pages, 5414 KiB  
Article
Phytochemical and Biological Activity Studies on Nasturtium officinale (Watercress) Microshoot Cultures Grown in RITA® Temporary Immersion Systems
by Marta Klimek-Szczykutowicz, Michał Dziurka, Ivica Blažević, Azra Đulović, Sebastian Granica, Izabela Korona-Glowniak, Halina Ekiert and Agnieszka Szopa
Molecules 2020, 25(22), 5257; https://doi.org/10.3390/molecules25225257 - 11 Nov 2020
Cited by 14 | Viewed by 3043
Abstract
The main compounds in both extracts were gluconasturtiin, 4-methoxyglucobrassicin and rutoside, the amounts of which were, respectively, determined as 182.93, 58.86 and 23.24 mg/100 g dry weight (DW) in biomass extracts and 640.94, 23.47 and 7.20 mg/100 g DW in plant herb extracts. [...] Read more.
The main compounds in both extracts were gluconasturtiin, 4-methoxyglucobrassicin and rutoside, the amounts of which were, respectively, determined as 182.93, 58.86 and 23.24 mg/100 g dry weight (DW) in biomass extracts and 640.94, 23.47 and 7.20 mg/100 g DW in plant herb extracts. The antioxidant potential of all the studied extracts evaluated using CUPRAC (CUPric Reducing Antioxidant Activity), FRAP (Ferric Reducing Ability of Plasma), and DPPH (1,1-diphenyl-2-picrylhydrazyl) assays was comparable. The anti-inflammatory activity of the extracts was tested based on the inhibition of 15-lipoxygenase, cyclooxygenase-1, cyclooxygenase-2 (COX-2), and phospholipase A2. The results demonstrate significantly higher inhibition of COX-2 for in vitro cultured biomass compared with the herb extracts (75.4 and 41.1%, respectively). Moreover, all the studied extracts showed almost similar antibacterial and antifungal potential. Based on these findings, and due to the fact that the growth of in vitro microshoots is independent of environmental conditions and unaffected by environmental pollution, we propose that biomass that can be rapidly grown in RITA® bioreactors can serve as an alternative source of bioactive compounds with valuable biological properties. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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14 pages, 6500 KiB  
Article
Chemical Profile and Antimicrobial Activity of the Fungus-Growing Termite Strain Macrotermes Bellicosus Used in Traditional Medicine in the Republic of Benin
by Dima Hammoud Mahdi, Jane Hubert, Jean-Hugues Renault, Agathe Martinez, Andreas Schubert, Kathrin Monika Engel, Blaise Koudogbo, Zacharie Vissiennon, Virgile Ahyi, Karen Nieber and Cica Vissiennon
Molecules 2020, 25(21), 5015; https://doi.org/10.3390/molecules25215015 - 29 Oct 2020
Cited by 16 | Viewed by 3156
Abstract
The fungus growing termite species Macrotermes bellicosus (M. bellicosus) is used in nutrition and traditional medicine in the Republic of Benin for the treatment of infectious and inflammatory diseases. Previous findings demonstrated evidence of anti-inflammatory and spasmolytic properties of M. bellicosus [...] Read more.
The fungus growing termite species Macrotermes bellicosus (M. bellicosus) is used in nutrition and traditional medicine in the Republic of Benin for the treatment of infectious and inflammatory diseases. Previous findings demonstrated evidence of anti-inflammatory and spasmolytic properties of M. bellicosus. The aim of the present study was to evaluate the antimicrobial potential of different extracts of M. bellicosus samples and determine the chemical profile of an ethanolic M. bellicosus extract. Chemical profiling was conducted using centrifugal partition chromatography and 13C-NMR, followed by MALDI-TOF MS. Major identified compounds include hydroquinone (HQ), methylhydroquinone (MHQ), 3,4-dihydroxyphenethyl glycol (DHPG), N-acetyldopamine (NADA) and niacinamide. The fatty acid mixture of the extract was mainly composed of linoleic and oleic acid and highlights the nutritional purpose of M. bellicosus. Using the Kirby–Bauer disc diffusion and broth microdilution assay, an antibacterial activity of M. bellicosus samples was observed against various clinical strains with a highest growth inhibition of S. aureus. In addition, HQ and MHQ as well as fractions containing DHPG, niacinamide and NADA inhibited S. aureus growth. The reported antimicrobial activity of M. bellicosus and identified active substances provide a rationale for the traditional medicinal use of M. bellicosus. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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19 pages, 1188 KiB  
Article
Evaluation of Various Solvent Extracts of Tetrastigma leucostaphylum (Dennst.) Alston Leaves, a Bangladeshi Traditional Medicine Used for the Treatment of Diarrhea
by Sajib Rudra, Afroza Tahamina, Nazim Uddin Emon, Md. Adnan, Mohammad Shakil, Md. Helal Uddin Chowdhury, James W. Barlow, Mona S. Alwahibi, Mohamed Soliman Elshikh, Mohammad Omar Faruque and Shaikh Bokhtear Uddin
Molecules 2020, 25(21), 4994; https://doi.org/10.3390/molecules25214994 - 28 Oct 2020
Cited by 23 | Viewed by 3334
Abstract
Tetrastigma leucostaphylum (TL) is an important ethnic medicine of Bangladesh used to treat diarrhea and dysentery. Hence, current study has been designed to characterize the antidiarrheal (in vivo) and cytotoxic (in vitro) effects of T. leucostaphylum. A crude extract was prepared with [...] Read more.
Tetrastigma leucostaphylum (TL) is an important ethnic medicine of Bangladesh used to treat diarrhea and dysentery. Hence, current study has been designed to characterize the antidiarrheal (in vivo) and cytotoxic (in vitro) effects of T. leucostaphylum. A crude extract was prepared with methanol (MTL) and further partitioned into n-hexane (NTL), dichloromethane (DTL), and n-butanol (BTL) fractions. Antidiarrheal activity was investigated using castor oil induced diarrhea, enteropooling, and gastrointestinal transit models, while cytotoxicity was evaluated using the brine shrimp lethality bioassay. In antidiarrheal experiments, all doses (100, 200, and 400 mg/kg) of the DTL extract significantly reduced diarrheal stool frequency, volume and weight of intestinal contents, and gastrointestinal motility in mice. Similarly, in the cytotoxicity assay, all extracts exhibited activity, with the DTL extract the most potent (LC50 67.23 μg/mL). GC-MS analysis of the DTL extract identified 10 compounds, which showed good binding affinity toward M3 muscarinic acetylcholine, 5-HT3, Gut inhibitory phosphodiesterase, DNA polymerase III subunit alpha, and UDP-N-acetylglucosamine-1 carboxyvinyltransferase enzyme targets upon molecular docking analysis. Although ADME/T analyses predicted the drug-likeness and likely safety upon consumption of these bioactive compounds, significant toxicity concerns are evident due to the presence of the known phytotoxin, 2,4-di-tert-butylphenol. In summary, T. leucostaphylum showed promising activity, helping to rationalize the ethnomedicinal use and importance of this plant, its safety profile following both acute and chronic exposure warrants further investigation. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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15 pages, 1537 KiB  
Article
Constituents of Xerolekia speciosissima (L.) Anderb. (Inuleae), and Anti-Inflammatory Activity of 7,10-Diisobutyryloxy-8,9-epoxythymyl Isobutyrate
by Natalia Kłeczek, Janusz Malarz, Barbara Gierlikowska, Anna K. Kiss and Anna Stojakowska
Molecules 2020, 25(21), 4913; https://doi.org/10.3390/molecules25214913 - 23 Oct 2020
Cited by 8 | Viewed by 2874
Abstract
Xerolekia speciosissima (L.) Anderb., a rare plant from the north of Italy, is a member of the Inuleae-Inulinae subtribe of the Asteraceae. Despite its close taxonomic relationship with many species possessing medicinal properties, the chemical composition of the plant has remained unknown until [...] Read more.
Xerolekia speciosissima (L.) Anderb., a rare plant from the north of Italy, is a member of the Inuleae-Inulinae subtribe of the Asteraceae. Despite its close taxonomic relationship with many species possessing medicinal properties, the chemical composition of the plant has remained unknown until now. A hydroalcoholic extract from the aerial parts of X. speciosissima was analyzed by HPLC-DAD-MSn, revealing the presence of caffeic acid derivatives and flavonoids. In all, 19 compounds, including commonly found chlorogenic acids and less frequently occurring butyryl and methylbutyryl conjugates of dicaffeoylquinic and tricaffeoylhexaric acids, plus two flavonoids, were tentatively identified. Chromatographic separation of a hydroalcoholic extract from the capitula of the plant led to the isolation of (+)-dehydrodiconiferyl alcohol 4-O-β-glucopyranoside, quercimeritrin, astragalin, isoquercitrin, 6-hydroxykaempferol-7-O-β-glucoside, quercetagitrin, methyl caffeate, caffeic acid, protocatechuic acid, chlorogenic acid and 1,5-dicaffeoylquinic acid. Composition of a nonpolar extract from the aerial parts of the plant was analyzed by chromatographic methods supported with 1H-NMR spectroscopy. The analysis revealed the presence of loliolide, reynosin, samtamarine, 2,3-dihydroaromaticin, 2-deoxy-4-epi-pulchellin and thymol derivatives as terpenoid constituents of the plant. One of the latter compounds—7,10-diisobutyryloxy-8,9-epoxythymyl isobutyrate—at concentrations 0.5, 1.0 and 2.5 μM, significantly reduced IL-8, IL-1β and CCL2 excretion by LPS-stimulated human neutrophils. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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22 pages, 3730 KiB  
Article
Synthesis and Antiplasmodial Activity of Novel Fosmidomycin Derivatives and Conjugates with Artemisinin and Aminochloroquinoline
by Despina Palla, Antonia I. Antoniou, Michel Baltas, Christophe Menendez, Philippe Grellier, Elisabeth Mouray and Constantinos M. Athanassopoulos
Molecules 2020, 25(20), 4858; https://doi.org/10.3390/molecules25204858 - 21 Oct 2020
Cited by 10 | Viewed by 3287
Abstract
Malaria, despite many efforts, remains among the most problematic infectious diseases worldwide, mainly due to the development of drug resistance by Plasmodium falciparum. The antibiotic fosmidomycin (FSM) is also known for its antimalarial activity by targeting the non-mevalonate isoprenoid synthesis pathway, which is [...] Read more.
Malaria, despite many efforts, remains among the most problematic infectious diseases worldwide, mainly due to the development of drug resistance by Plasmodium falciparum. The antibiotic fosmidomycin (FSM) is also known for its antimalarial activity by targeting the non-mevalonate isoprenoid synthesis pathway, which is essential for the malaria parasites but is absent in mammalians. In this study, we synthesized and evaluated against the chloroquine-resistant P. falciparum FcB1/Colombia strain, a series of FSM analogs, derivatives, and conjugates with other antimalarial agents, such as artemisinin (ART) and aminochloroquinoline (ACQ). The biological evaluation revealed four new compounds with higher antimalarial activity than FSM: two FSM-ACQ derivatives and two FSM-ART conjugates, with 3.5–5.4 and 41.5–23.1 times more potent activities than FSM, respectively. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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21 pages, 7487 KiB  
Article
Formulation and Evaluation of Supramolecular Food-Grade Piperine HP β CD and TPGS Complex: Dissolution, Physicochemical Characterization, Molecular Docking, In Vitro Antioxidant Activity, and Antimicrobial Assessment
by Syed Sarim Imam, Sultan Alshehri, Talal Abdullah Alzahrani, Afzal Hussain and Mohammad A. Altamimi
Molecules 2020, 25(20), 4716; https://doi.org/10.3390/molecules25204716 - 14 Oct 2020
Cited by 23 | Viewed by 2435
Abstract
The purpose of the present study was to improve the aqueous solubility, dissolution, and antioxidant activity of the water-insoluble drug piperine (PIP). The study was performed by preparing PIP binary inclusion complex (PIP BIC) and piperine ternary inclusion complex (PIP TIC) by different [...] Read more.
The purpose of the present study was to improve the aqueous solubility, dissolution, and antioxidant activity of the water-insoluble drug piperine (PIP). The study was performed by preparing PIP binary inclusion complex (PIP BIC) and piperine ternary inclusion complex (PIP TIC) by different methods. The effect of a hydrophilic auxiliary substance (TPGS) was assessed with addition to PIP and hydroxypropyl beta cyclodextrin (HP β CD) complex. The phase solubility study was performed to evaluate the complexation efficiency and stability constant. The aqueous solubility, dissolution, physicochemical assessment, antioxidant activity, antimicrobial activity, and molecular docking were further evaluated to check the effect of the complexation of PIP. The stability constant (Ks) value was found to be 238 and 461 M−1 for the binary and ternary inclusion complex. The dissolution study results showed a marked enhancement of release in comparison to pure drug. XRD and SEM studies revealed the presence of more agglomerated and amorphous structures of PIP, which confirmed the formation of complexes. The results of DPPH radical scavenging and antimicrobial activity showed a significant (p < 0.05) enhancement in scavenging activity for PIP TIC (microwave irradiation (MI)). The docking studies have revealed that the binding affinity of TPGS at the PIP-HP β CD complex was −5.2 kcal/mol. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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16 pages, 8673 KiB  
Article
Extract Derived from Cedrus atlantica Acts as an Antitumor Agent on Hepatocellular Carcinoma Growth In Vitro and In Vivo
by Xiao-Fan Huang, Kai-Fu Chang, Shan-Chih Lee, Gwo-Tarng Sheu, Chia-Yu Li, Jun-Cheng Weng, Chih-Yen Hsiao and Nu-Man Tsai
Molecules 2020, 25(20), 4608; https://doi.org/10.3390/molecules25204608 - 10 Oct 2020
Cited by 14 | Viewed by 2343
Abstract
Cedrus atlantica is widely used in herbal medicine. However, the anti-cancer activity of C. atlantica extract (CAt extract) has not been clarified in hepatocellular carcinoma. In the study, we elucidated the anti-hepatoma capacity of CAt extract on HCC in vitro and in vivo. [...] Read more.
Cedrus atlantica is widely used in herbal medicine. However, the anti-cancer activity of C. atlantica extract (CAt extract) has not been clarified in hepatocellular carcinoma. In the study, we elucidated the anti-hepatoma capacity of CAt extract on HCC in vitro and in vivo. To explore the anti-hepatoma mechanisms of the CAt extract in vitro, HCC and normal cells were treated with the CAt extract, which showed marked inhibitory effects on HCC cells in a dose-dependent manner; in contrast, the CAt extract treatment was less cytotoxic to normal cells. In addition, our results indicate that the CAt extract induced apoptosis via caspase-dependent and independent apoptosis pathways. Furthermore, the CAt extract inhibited HCC tumor cell growth by restraining cell cycle progression, and it reduced the signaling of the AKT, ERK1/2, and p38 pathways. In the xenograft model, the CAt extract suppressed HCC tumor cell growth and prolonged lifespan by inhibiting PCNA protein expression, repressing part of the VEGF-induced autocrine pathway, and triggering strong expression of cleaved caspase-3, which contributed to cell apoptosis. Moreover, the CAt extract did not induce any obvious changes in pathological morphology or body weight, suggesting it had no toxicity. CAt extract exerted anti-tumor effects on HCC in vitro and in vivo. Thus, CAt extract could be used as a potential anti-cancer therapeutic agent against HCC. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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16 pages, 2548 KiB  
Article
A Bibenzyl Component Moscatilin Mitigates Glycation-Mediated Damages in an SH-SY5Y Cell Model of Neurodegenerative Diseases through AMPK Activation and RAGE/NF-κB Pathway Suppression
by Mei Chou Lai, Wayne Young Liu, Shorong-Shii Liou and I-Min Liu
Molecules 2020, 25(19), 4574; https://doi.org/10.3390/molecules25194574 - 07 Oct 2020
Cited by 10 | Viewed by 2584
Abstract
Moscatilin can protect rat pheochromocytoma cells against methylglyoxal-induced damage. Elimination of the effect of advanced glycation end-products (AGEs) but activation of AMP-activated protein kinase (AMPK) are the potential therapeutic targets for the neurodegenerative diseases. Our study aimed to clarify AMPK signaling’s role in [...] Read more.
Moscatilin can protect rat pheochromocytoma cells against methylglyoxal-induced damage. Elimination of the effect of advanced glycation end-products (AGEs) but activation of AMP-activated protein kinase (AMPK) are the potential therapeutic targets for the neurodegenerative diseases. Our study aimed to clarify AMPK signaling’s role in the beneficial effects of moscatilin on the diabetic/hyperglycemia-associated neurodegenerative disorders. AGEs-induced injury in SH-SY5Y cells was used as an in vitro neurodegenerative model. AGEs stimulation resulted in cellular viability loss and reactive oxygen species production, and mitochondrial membrane potential collapse. It was observed that the cleaved forms of caspase-9, caspase-3, and poly (ADP-ribose) polymerase increased in SH-SY5Y cells following AGEs exposure. AGEs decreased Bcl-2 but increased Bax and p53 expression and nuclear factor kappa-B activation in SH-SY5Y cells. AGEs also attenuated the phosphorylation level of AMPK. These AGEs-induced detrimental effects were ameliorated by moscatilin, which was similar to the actions of metformin. Compound C, an inhibitor of AMPK, abolished the beneficial effects of moscatilin on the regulation of SH-SY5Y cells’ function, indicating the involvement of AMPK. In conclusion, moscatilin offers a promising therapeutic strategy to reduce the neurotoxicity or AMPK dysfunction of AGEs. It provides a potential beneficial effect with AGEs-related neurodegenerative diseases. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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16 pages, 3726 KiB  
Article
Antrodia cinnamomea Extraction Waste Supplementation Promotes Thermal Stress Tolerance and Tissue Regeneration Ability of Zebrafish
by Chi-Chang Chang, Yung-Chuan Lu, Chih-Chun Wang, Tsui-Ling Ko, Jung-Ren Chen, Wei Wang, Ya-Ling Chen, Yu-Wen Wang, Tzu-Hsien Chang, Hsia-Fen Hsu and Jer-Yiing Houng
Molecules 2020, 25(18), 4213; https://doi.org/10.3390/molecules25184213 - 14 Sep 2020
Cited by 7 | Viewed by 2406
Abstract
Antrodia cinnamomea (AC) has been shown to have anti-inflammatory, anti-tumor, and immunomodulation activities. It is estimated that hundreds of metric tons of AC extraction waste (ACEW) are produced per year in Taiwan. This study aims to assess the feasibility of applying ACEW as [...] Read more.
Antrodia cinnamomea (AC) has been shown to have anti-inflammatory, anti-tumor, and immunomodulation activities. It is estimated that hundreds of metric tons of AC extraction waste (ACEW) are produced per year in Taiwan. This study aims to assess the feasibility of applying ACEW as feed supplement in the aquaculture industry. ACEW significantly inhibited the growth of microorganisms in the water tank, by around 39.4% reduction on the fifth day with feed supplemented of 10% ACEW. The feed conversion efficiency of zebrafish with 10% ACEW supplementation for 30 days was 1.22-fold compared to that of the control. ACEW dramatically improved the tolerances of zebrafish under the heat and cold stresses. When at water temperature extremes of 38 °C or 11 °C, compared to the 100% mortality rate in the control group, the 10% ACEW diet group still had 91.7% and 83.3% survival rates, respectively. In a caudal fin amputation test, the fin recovery of zebrafish was increased from 68.4% to 93% with 10% ACEW diet after 3-week regeneration. ACEW effectively down-regulated the gene expression of TNF-α, IL-1β, IL-6, and IL-10, and up-regulated the gene expression of IL-4/13A. Additionally, the supplement of ACEW in the feed can maintain and prevent the fish’s body weight from dropping too much under enteritis. Taken together, ACEW has beneficial potential in aquaculture. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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13 pages, 1065 KiB  
Article
Residual Larvicidal Activity of Quinones against Aedes aegypti
by Raquel L. Silva, Daniel P. Demarque, Renata G. Dusi, João Paulo B. Sousa, Lorena C. Albernaz and Laila S. Espindola
Molecules 2020, 25(17), 3978; https://doi.org/10.3390/molecules25173978 - 31 Aug 2020
Cited by 26 | Viewed by 3327
Abstract
The number of documented dengue cases has increased dramatically in recent years due to transmission through the Aedes aegypti mosquito bite. Vector control remains the most effective measure to protect against this and other arboviral diseases including Zika, chikungunya and (urban) yellow fever, [...] Read more.
The number of documented dengue cases has increased dramatically in recent years due to transmission through the Aedes aegypti mosquito bite. Vector control remains the most effective measure to protect against this and other arboviral diseases including Zika, chikungunya and (urban) yellow fever, with an established vaccine only available for yellow fever. Although the quinone class shows potential as leading compounds for larvicide development, limited information restricts the development of optimized structures and/or formulations. Thus, in this contribution we investigated the larvicidal and pupicidal activity of three quinone compounds isolated from a Connarus suberosus root wood ethyl acetate extract together with 28 quinones from other sources. Eight quinones demonstrated larvicidal activity, of which tectoquinone (4) proved to be the most active (LC50 1.1 µg/mL). The essential residual effect parameter of four of these quinones was evaluated in laboratory trials, with tectoquinone (4) and 2-ethylanthraquinone (7) presenting the most prolonged activity. In small-scale field residual tests, tectoquinone (4) caused 100% larvae mortality over 5 days, supporting its selection for formulation trials to develop a prototype larvicide to control Ae. aegypti. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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13 pages, 2447 KiB  
Article
Anti-Melanogenesis Activity of 6-O-Isobutyrylbritannilactone from Inula britannica on B16F10 Melanocytes and In Vivo Zebrafish Models
by Dae Kil Jang, Chau Ha Pham, Ik Soo Lee, Seung-Hyun Jung, Ji Hye Jeong, Han-Seung Shin and Hee Min Yoo
Molecules 2020, 25(17), 3887; https://doi.org/10.3390/molecules25173887 - 26 Aug 2020
Cited by 14 | Viewed by 3300
Abstract
A potential natural melanogenesis inhibitor was discovered in the form of a sesquiterpene isolated from the flowers of Inula britannica, specifically 6-O-isobutyrylbritannilactone (IBL). We evaluated the antimelanogenesis effects of IBL on B16F10 melanocytes and zebrafish embryos. As a result, we [...] Read more.
A potential natural melanogenesis inhibitor was discovered in the form of a sesquiterpene isolated from the flowers of Inula britannica, specifically 6-O-isobutyrylbritannilactone (IBL). We evaluated the antimelanogenesis effects of IBL on B16F10 melanocytes and zebrafish embryos. As a result, we found that 3-isobutyl-1-methylxanthine (IBMX)-induced melanin production was reduced in a dose-dependent manner in B16F10 cells by IBL. We also analyzed B16F10 cells that were and were not treated with IBMX, investigating the melanin concentration, tyrosinase activity, mRNA levels. We also studied the protein expressions of microphthalmia-associated transcription factor (MITF), tyrosinase, and tyrosinase-related proteins (TRP1, and TRP2). Furthermore, we found that melanin synthesis and tyrosinase expression were also inhibited by IBL through the modulation of the following signaling pathways: ERK, phosphoinositide 3-kinase (PI3K)/AKT, and CREB. In addition, we studied antimelanogenic activity using zebrafish embryos and found that the embryos had significantly reduced pigmentation in the IBL-treated specimens compared to the untreated controls. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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17 pages, 5968 KiB  
Article
Neuroprotective Effects of 7-Geranyloxycinnamic Acid from Melicope lunu ankenda Leaves
by Zeinab Abdulwanis Mohamed, Enas Mohamed Eliaser, Mohammed Sani Jaafaru, Norshariza Nordin, Costas Ioannides and Ahmad Faizal Abdull Razis
Molecules 2020, 25(16), 3724; https://doi.org/10.3390/molecules25163724 - 15 Aug 2020
Cited by 3 | Viewed by 2634
Abstract
Neurodegenerative diseases (NDDs) are chronic conditions that have drawn robust interest from the scientific community. Phytotherapeutic agents are becoming an important source of chemicals for the treatment and management of NDDs. Various secondary metabolites have been isolated from Melicope lunu-ankenda plant leaves, including [...] Read more.
Neurodegenerative diseases (NDDs) are chronic conditions that have drawn robust interest from the scientific community. Phytotherapeutic agents are becoming an important source of chemicals for the treatment and management of NDDs. Various secondary metabolites have been isolated from Melicope lunu-ankenda plant leaves, including phenolic acid derivatives. However, their neuroprotective activity remains unclear. Thus, the aim of this study is to elucidate the in vitro neuroprotective activity of 7-geranyloxycinnamic acid isolated from Melicope lunu-ankenda leaves. The neuroprotective activity was evaluated in differentiated human neuroblastoma (SH-SY5Y) cells by monitoring cell viability using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT). Moreover, the potential to impair apoptosis in differentiated cells was investigated employing the Annexin V-FITC assay, acridine orange and propidium iodide (AO/PI) staining, and fluorescence microscopy. Morphological assessment and ultrastructural analysis were performed using scanning and transmission electron microscopy to evaluate the effect of 7-geranyloxycinnamic acid on surface morphology and internal features of the differentiated cells. Pre-treatment of neuronal cells with 7-geranyloxycinnamic acid significantly protected the differentiated SH-SY5Y cells against H2O2-induced apoptosis. Cytoskeleton and cytoplasmic inclusion were similarly protected by the 7-geranyloxycinnamic acid treatment. The present findings demonstrate the neuroprotective potential of 7-geranyloxycinnamic acid against H2O2-induced neurotoxicity in neuronal cells, which is an established hallmark of neuronal disorders. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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14 pages, 1070 KiB  
Article
Immunomodulatory Activity and Phytochemical Profile of Infusions from Cleavers Herb
by Tetiana Ilina, Weronika Skowrońska, Natalia Kashpur, Sebastian Granica, Agnieszka Bazylko, Alla Kovalyova, Olga Goryacha and Oleh Koshovyi
Molecules 2020, 25(16), 3721; https://doi.org/10.3390/molecules25163721 - 14 Aug 2020
Cited by 16 | Viewed by 3919
Abstract
Extracts from aerial parts of G. aparine (cleavers) constitute a herbal remedy with monography in British Herbal Pharmacopeia. On the European market, there are several drugs and food supplements consisting of Galium extracts. In folk medicine, cleavers was used topically in Europe, Asia, [...] Read more.
Extracts from aerial parts of G. aparine (cleavers) constitute a herbal remedy with monography in British Herbal Pharmacopeia. On the European market, there are several drugs and food supplements consisting of Galium extracts. In folk medicine, cleavers was used topically in Europe, Asia, and the Americas to treat skin diseases. In several remedies, cleavers is also listed as an immunomodulatory active herb influencing the defense response of the human body. The aim of this study was to investigate the immunostimulatory activity and antioxidant potential in vitro of a raw infusion of cleavers and bioactive fractions. The functional activity of lymphocytes in the reaction of the lymphocyte blast transformation (RLBT) method was used for immunomodulatory activity assays and direct scavenging of 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO), and hydrogen peroxide (H2O2) was chosen for the examination of antioxidant activity. It was shown that both the raw extract and fractions show significant immunostimulatory and scavenging activities. The obtained data partially justify the traditional use of cleavers as topical remedy for skin infections and for wounds. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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19 pages, 2327 KiB  
Article
Achillea millefolium L. and Achillea biebersteinii Afan. Hydroglycolic Extracts–Bioactive Ingredients for Cosmetic Use
by Katarzyna Gaweł-Bęben, Marcelina Strzępek-Gomółka, Marcin Czop, Zuriyadda Sakipova, Kazimierz Głowniak and Wirginia Kukula-Koch
Molecules 2020, 25(15), 3368; https://doi.org/10.3390/molecules25153368 - 24 Jul 2020
Cited by 31 | Viewed by 4477
Abstract
Studies on hydroglycolic (HG) extracts of Achillea biebersteinii (AB)—a less investigated representative of the genus—were performed to determine their potential for cosmetic applications compared to the well-known Achillea millefolium (AM). Three types of water:polyethylene glycol extracts (1:1, 4:1, 6:1 v/v) [...] Read more.
Studies on hydroglycolic (HG) extracts of Achillea biebersteinii (AB)—a less investigated representative of the genus—were performed to determine their potential for cosmetic applications compared to the well-known Achillea millefolium (AM). Three types of water:polyethylene glycol extracts (1:1, 4:1, 6:1 v/v) were obtained from both species and analyzed for their composition by high performance liquid chromatography coupled with mass spectrometry (HPLC-ESI-Q-TOF-MS) and assayed for their biological activities. The study led to the identification of 11 metabolites from different natural product classes with the highest share corresponding to 5-caffeoylquinic acid, axillarin, coumaroylquinic acid isomers and 3-caffeoylquinic acid. The highest antiradical capacity in DPPH and ABTS scavenging assays was shown for HG 4:1 of AB and AM extracts. HG 1:1 extracts from both species inhibited monophenolase and diphenolase activity of tyrosinase, whereas AB HG 4:1 extract showed significant monophenolase inhibition. The highest sun protection factor (SPF) was determined for AM HG 4:1 extract, equal to 14.04 ± 0.17. The AB extracts were cytotoxic for both human keratinocytes HaCaT and A375 melanoma, however HG 1:1 and 4:1 extracts were more cytotoxic for cancer than for noncancerous cells. In conclusion, AB HG 1:1 and 4:1 extracts display significant potential as active cosmetic ingredients. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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15 pages, 3945 KiB  
Article
The Essential Oil of Cymbopogon citratus Stapt and Carvacrol: An Approach of the Antitumor Effect on 7,12-Dimethylbenz-[α]-anthracene (DMBA)-Induced Breast Cancer in Female Rats
by Juan Pedro Rojas-Armas, Jorge Luis Arroyo-Acevedo, Miriam Palomino-Pacheco, Oscar Herrera-Calderón, José Manuel Ortiz-Sánchez, Agustín Rojas-Armas, James Calva, Américo Castro-Luna and Julio Hilario-Vargas
Molecules 2020, 25(14), 3284; https://doi.org/10.3390/molecules25143284 - 20 Jul 2020
Cited by 37 | Viewed by 4815
Abstract
C. citratus essential oil and carvacrol have shown an antitumor effect on breast tumor cell lines; the main objective of this research was to evaluate the antitumor effect of the essential oil of Cymbopogon citratus (EOCc) and carvacrol on 7,12-dimethylbenz [a] anthracene (DMBA)-induced [...] Read more.
C. citratus essential oil and carvacrol have shown an antitumor effect on breast tumor cell lines; the main objective of this research was to evaluate the antitumor effect of the essential oil of Cymbopogon citratus (EOCc) and carvacrol on 7,12-dimethylbenz [a] anthracene (DMBA)-induced breast cancer in female rats. Cancer was induced by a single administration of DMBA at dose of 80 mg/kg body weight (BW). A total of 54 female Holtzman rats were randomly assigned into 9 groups (n = 6). Group I: PS (Physiological saline); Group II: DMBA; Groups III, IV, and V: DMBA + EOCc at doses of 50, 100 and 200 mg/kg/day BW, respectively; Groups VI, VII, and VIII: DMBA + carvacrol at doses of 50, 100 and 200 mg/kg/day BW, respectively; and group IX: DMBA + EOCc + carvacrol at doses of 100 mg/kg/day BW. The treatment lasted 14 weeks. As results, EOCc showed a reduction in tumors as well as necrosis and mitosis. Animals treated with carvacrol did not show necrosis, mitosis, or infiltration. Carvacrol at dose of 100 mg/kg/day BW revealed a significant decrease in the cumulative tumor volume down to 0.11 ± 0.05 cm3 compared to 0.38 ± 0.04 cm3 of the DMBA group (p < 0.01). It is concluded that EOCc and carvacrol had an antitumor effect on DMBA-induced breast cancer in female rats. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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19 pages, 5049 KiB  
Article
Huperzine A and Huperzine B Production by Prothallus Cultures of Huperzia selago (L.) Bernh. ex Schrank et Mart
by Wojciech J. Szypuła, Beata Wileńska, Aleksandra Misicka and Agnieszka Pietrosiuk
Molecules 2020, 25(14), 3262; https://doi.org/10.3390/molecules25143262 - 17 Jul 2020
Cited by 8 | Viewed by 4096
Abstract
This is the first report of an efficient and effective procedure to optimize the biosynthesis of huperzine A (HupA) and huperzine B (HupB) in vitro from Huperzia selago gametophytes. Axenic tissue cultures were established using spores collected from the sporophytes growing in the [...] Read more.
This is the first report of an efficient and effective procedure to optimize the biosynthesis of huperzine A (HupA) and huperzine B (HupB) in vitro from Huperzia selago gametophytes. Axenic tissue cultures were established using spores collected from the sporophytes growing in the wild. The prothalia were obtained after 7–18 months. Approximately 90 up to 100% of the gametophytes were viable and grew rapidly after each transfer on to a fresh medium every 3 months. The best biomass growth index for prothallus calculated on a fresh (FW) and dry weight (DW) basis, at 24 weeks of culture, was 2500% (FW) and 2200% (DW), respectively. The huperzine A content in the gametophytes was very high and ranged from 0.74 mg/g to 4.73 mg/g DW. The highest yield HupA biosynthesis at >4 mg/g DW was observed on W/S medium without growth regulators at 8 to 24 weeks of culture. The highest HupB content ranged from 0.10 mg/g to 0.52 mg/g DW and was obtained on the same medium. The results demonstrate the superiority of H. selago gametophyte cultures, with the level of HupA biosynthesis approximately 42% higher compared to sporophyte cultures and 35-fold higher than when the alkaloid was isolated from H. serrata, its current source for the pharmaceutical industry. Moreover, the biosynthesis of HupB was several-fold more efficient than in H. selago sporophytes growing in the wild. HPLC-HR-MS analyses of the extracts identified eight new alkaloids previously unreported in H. selago: deacetylfawcettine, fawcettimine, 16-hydroxyhuperzine B, deacetyllycoclavine, annopodine, lycopecurine, des-N-methylfastigiatine and flabelline. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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14 pages, 7366 KiB  
Article
Non-Cytotoxic Dibenzyl and Difluoroborate Curcuminoid Fluorophores Allow Visualization of Nucleus or Cytoplasm in Bioimaging
by Marco A. Obregón-Mendoza, Imilla I. Arias-Olguín, M. Mirian Estévez-Carmona, William Meza-Morales, Yair Alvarez-Ricardo, Rubén A. Toscano, Francisco Arenas-Huertero, Julia Cassani and Raúl G. Enríquez
Molecules 2020, 25(14), 3205; https://doi.org/10.3390/molecules25143205 - 14 Jul 2020
Cited by 4 | Viewed by 2612
Abstract
Curcumin, the most important secondary metabolite isolated from Curcuma longa, is known for its numerous purported therapeutic properties and as a natural dye. Herein, based on curcumin’s intrinsic fluorescence, a search for improved curcumin-based fluorophores was conducted. Within the set of semi-synthetic [...] Read more.
Curcumin, the most important secondary metabolite isolated from Curcuma longa, is known for its numerous purported therapeutic properties and as a natural dye. Herein, based on curcumin’s intrinsic fluorescence, a search for improved curcumin-based fluorophores was conducted. Within the set of semi-synthetic curcumin derivatives i.e. mono (1), di (2), tri (3), tetra (4) benzylated and dibenzyl-fluoroborate (5), the fluorescence properties of 2 and 5 in solution outstood with a two-fold quantum yield compared to curcumin. Furthermore, all benzylated derivatives showed a favorable minimal cytotoxic activity upon screening at 25 μM against human cancer and non-tumoral COS-7 cell lines, with a reduction of its cytotoxic effect related to the degree of substitution. Fluorophores 2 and 5 are versatile bioimaging tools, as revealed by Confocal Fluorescence Microscopy (CFM), and showed permeation of living cell membranes of astrocytes and astrocytomas. When 2 is excited with a 405- (blue) or 543-nm (green) laser, it is possible to exclusively and intensively visualize the nucleus. However, the fluorescence emission fades as the laser wavelength moves towards the red region. In comparison, 5 allows selective visualization of cytoplasm when a 560-nm laser is used, showing emission in the NIR region, while it is possible to exclusively observe the nucleus at the blue region with a 405-nm laser. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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20 pages, 3165 KiB  
Article
Potentilla alba Extracts Affect the Viability and Proliferation of Non-Cancerous and Cancerous Colon Human Epithelial Cells
by Klaudia Kowalik, Roman Paduch, Jakub W. Strawa, Adrian Wiater, Kamila Wlizło, Adam Waśko, Iwona Wertel, Anna Pawłowska, Monika Tomczykowa and Michał Tomczyk
Molecules 2020, 25(13), 3080; https://doi.org/10.3390/molecules25133080 - 06 Jul 2020
Cited by 12 | Viewed by 3583
Abstract
The aim of this study was to determine the anti-tumor activity of extracts isolated from Potentilla alba L. on human colon cancer cells of the HT-29 line and on non-cancer colon epithelial cells of the CCD 841 CoTr line. The research methods we [...] Read more.
The aim of this study was to determine the anti-tumor activity of extracts isolated from Potentilla alba L. on human colon cancer cells of the HT-29 line and on non-cancer colon epithelial cells of the CCD 841 CoTr line. The research methods we used to determine the cytotoxic and proliferative properties were 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and neutral red (NR) assays, the ability to produce nitric oxide, the Griess method, and the biochemical properties like 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP) methods indicating reduction activity of tested samples. In order to obtain a phytochemical profile of the different extracts an analytical method based on liquid chromatography-photodiode array detection-electrospray ionization ion-trap time-of-flight mass spectrometry (LC-PDA-ESI-MS/TOF) was applied. Finally, the effects of the extracts on the morphology and cell counts were assessed by May–Grünwald–Giemsa staining. After a comprehensive analysis of all the experiments, the extracts were found to demonstrate cytotoxic properties, they stimulated the division of non-cancer cells, and they were able to scavenge free radicals. In the NR method, the cell viability dropped to approximately 80% compared to the control. In the MTT assay, tumor cell proliferation decreased to 9.5% compared to the control. Therefore, we concluded that this plant has medical potential. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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12 pages, 2277 KiB  
Article
Extract of Juniperus indica Bertol Synergizes with Cisplatin to Inhibit Oral Cancer Cell Growth via Repression of Cell Cycle Progression and Activation of the Caspase Cascade
by Xiao-Fan Huang, Kai-Fu Chang, Shan-Chih Lee, Chia-Yu Li, Hung-Hsiu Liao, Ming-Chang Hsieh and Nu-Man Tsai
Molecules 2020, 25(12), 2746; https://doi.org/10.3390/molecules25122746 - 13 Jun 2020
Cited by 9 | Viewed by 2575
Abstract
Oral cancer—a type of head and neck cancer—is estimated to be the fifth most common cancer in Taiwan. However, efficacious therapies for oral cancer are still lacking due to drug resistance and recurrence. Consequently, the identification of new anticancer agents for clinical treatment [...] Read more.
Oral cancer—a type of head and neck cancer—is estimated to be the fifth most common cancer in Taiwan. However, efficacious therapies for oral cancer are still lacking due to drug resistance and recurrence. Consequently, the identification of new anticancer agents for clinical treatment is needed. Juniperus indica Bertol is a plant of the Juniperus genus often used as a treatment in traditional medicine due to its anti-inflammatory, antibacterial and diuretic functions. The biofunctions of Juniperus indica Bertol including its anticancer potential, have not been fully explored. As a result, the aim of this research was to investigate the anticancer activity of Juniperus indica Bertol extract (JIB extract) and determine whether JIB extract has synergistic effects with cisplatin in oral cancer. These results are the first to demonstrate that JIB extract exhibits anticancer capacity and synergizes with cisplatin to treat oral cancer. Our findings indicate that JIB extract has a potential to develop anticancer agent and chemo therapeutic adjuvant for oral cancer. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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15 pages, 1183 KiB  
Article
Evaluation of Antioxidant and Antibacterial Activities, Cytotoxicity of Acacia seyal Del Bark Extracts and Isolated Compounds
by Abdirahman Elmi, Rosella Spina, Arnaud Risler, Stéphanie Philippot, Ali Mérito, Raphaël E. Duval, Fatouma Mohamed Abdoul-latif and Dominique Laurain-Mattar
Molecules 2020, 25(10), 2392; https://doi.org/10.3390/molecules25102392 - 21 May 2020
Cited by 26 | Viewed by 4707
Abstract
Water extract of Acacia seyal bark is used traditionally by the population in Djibouti for its anti-infectious activity. The evaluation of in vitro antibacterial, antioxidant activities and cytotoxicity as well as chemical characterization of Acacia seyal bark water and methanolic extracts were presented. [...] Read more.
Water extract of Acacia seyal bark is used traditionally by the population in Djibouti for its anti-infectious activity. The evaluation of in vitro antibacterial, antioxidant activities and cytotoxicity as well as chemical characterization of Acacia seyal bark water and methanolic extracts were presented. The water extract has a toxicity against the MRC-5 cells at 256 μg/mL while the methanolic extract has a weak toxicity at the same concentration. The methanolic extract has a strong antioxidant activity with half maximal inhibitory concentration (IC50) of 150 ± 2.2 μg/mL using 1-diphenyl-2-picrylhydrazyl (DPPH) and IC50 of 27 ± 1.3 μg/mL using 2,2′-azino-bis 3-ethylbenzthiazoline-6-sulphonic acid (ABTS) radical methods. For ferric reducing/antioxidant power (FRAP) assay, the result is 45.74 ± 5.96 μg Vitamin C Equivalent (VCE)/g of dry weight (DW). The precipitation of tannins from methanol crude extract decreases the MIC from 64 µg/mL to 32 µg/mL against Staphylococcus aureus and Corynebacterium urealyticum. However, the antioxidant activity is higher before tannins precipitation than after (IC50 = 150 µg/mL for methanolic crude extract and 250 µg/mL after tannins precipitation determined by DPPH method). By matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS) analysis, the results showed that the condensed tannins consist of two types of catechin and gallocatechin-based oligomers. The fractionation led to the identification of three pure compounds: two flavanols catechin and epicatechin; one triterpene as lupeol; and a mixture of three steroids and one fatty acid: campesterol, stigmasterol, clionasterol, and oleamide. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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24 pages, 7277 KiB  
Article
Improving Regulation of Enzymatic and Non-Enzymatic Antioxidants and Stress-Related Gene Stimulation in Cucumber mosaic cucumovirus-Infected Cucumber Plants Treated with Glycine Betaine, Chitosan and Combination
by Ahmed R. Sofy, Rehab A. Dawoud, Mahmoud R. Sofy, Heba I. Mohamed, Ahmed A. Hmed and Noha K. El-Dougdoug
Molecules 2020, 25(10), 2341; https://doi.org/10.3390/molecules25102341 - 17 May 2020
Cited by 72 | Viewed by 5305
Abstract
Cucumber mosaic cucumovirus (CMV) is a deadly plant virus that results in crop-yield losses with serious economic consequences. In recent years, environmentally friendly components have been developed to manage crop diseases as alternatives to chemical pesticides, including the use of natural compounds such [...] Read more.
Cucumber mosaic cucumovirus (CMV) is a deadly plant virus that results in crop-yield losses with serious economic consequences. In recent years, environmentally friendly components have been developed to manage crop diseases as alternatives to chemical pesticides, including the use of natural compounds such as glycine betaine (GB) and chitosan (CHT), either alone or in combination. In the present study, the leaves of the cucumber plants were foliar-sprayed with GB and CHT—either alone or in combination—to evaluate their ability to induce resistance against CMV. The results showed a significant reduction in disease severity and CMV accumulation in plants treated with GB and CHT, either alone or in combination, compared to untreated plants (challenge control). In every treatment, growth indices, leaf chlorophylls content, phytohormones (i.e., indole acetic acid, gibberellic acid, salicylic acid and jasmonic acid), endogenous osmoprotectants (i.e., proline, soluble sugars and glycine betaine), non-enzymatic antioxidants (i.e., ascorbic acid, glutathione and phenols) and enzymatic antioxidants (i.e., superoxide dismutase, peroxidase, polyphenol oxidase, catalase, lipoxygenase, ascorbate peroxidase, glutathione reductase, chitinase and β-1,3 glucanase) of virus-infected plants were significantly increased. On the other hand, malondialdehyde and abscisic acid contents have been significantly reduced. Based on a gene expression study, all treated plants exhibited increased expression levels of some regulatory defense genes such as PR1 and PAL1. In conclusion, the combination of GB and CHT is the most effective treatment in alleviated virus infection. To our knowledge, this is the first report to demonstrate the induction of systemic resistance against CMV by using GB. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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19 pages, 2106 KiB  
Article
Elicitation-Based Method for Increasing the Production of Antioxidant and Bactericidal Phenolic Compounds in Dionaea muscipula J. Ellis Tissue
by Wojciech Makowski, Krzysztof Michał Tokarz, Barbara Tokarz, Rafał Banasiuk, Karolina Witek and Aleksandra Królicka
Molecules 2020, 25(8), 1794; https://doi.org/10.3390/molecules25081794 - 14 Apr 2020
Cited by 22 | Viewed by 4556
Abstract
The carnivorous plant Dionaea muscipula J. Ellis (Venus flytrap) is a widely known medical herb, capable of producing various phenolic compounds known for their strong antioxidant and antibacterial properties. In the pharmaceutical industry, Venus flytrap is grown in tissue cultures, as the natural [...] Read more.
The carnivorous plant Dionaea muscipula J. Ellis (Venus flytrap) is a widely known medical herb, capable of producing various phenolic compounds known for their strong antioxidant and antibacterial properties. In the pharmaceutical industry, Venus flytrap is grown in tissue cultures, as the natural population of D. muscipula is very limited. Here, we describe an improved method to increase the quantity and quality of phenolic compounds produced in D. muscipula. This is achieved by combining biotic elicitation (using Cronobacter sakazakii bacteria lysate) of D. muscipula cultured with rotary shaking (hydromechanical stress), which we describe here for the first time. The antibacterial activity and the antioxidant properties of the obtained compounds were studied on two antibiotic-resistant human pathogenic bacteria. The proposed plant culture conditions resulted in an increase in fresh weight, as well as a higher total phenolic content, in comparison to traditional tissue cultures on agar-solidified medium. With the use of high-performance liquid chromatography, we demonstrated that the described elicitation strategy leads to an increased synthesis of myricetin, caffeic acid, ellagic acid and plumbagin in D. muscipula tissue. We also found that a higher level of antioxidant activity, exhibited by the plant extract, corresponded with its higher phenylpropanoid content. The bactericidal activity of the extract against Staphylococcus aureus was dependent on the duration of plant culture under described elicitation conditions, whereas neither elicitation condition (duration or elicitor concentration) seemed relevant for the bactericidal activity of the extract towards Escherichia coli. This suggest that Gram-negative bacteria are less sensitive to compounds derived from Venus flytrap tissue. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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14 pages, 919 KiB  
Article
Acetylcholinesterase Inhibitors among Zingiber officinale Terpenes—Extraction Conditions and Thin Layer Chromatography-Based Bioautography Studies
by Lidia Czernicka, Agnieszka Ludwiczuk, Edward Rój, Zbigniew Marzec, Agata Jarzab and Wirginia Kukula-Koch
Molecules 2020, 25(7), 1643; https://doi.org/10.3390/molecules25071643 - 03 Apr 2020
Cited by 16 | Viewed by 3779
Abstract
Although numerous studies have been conducted on ginger extracts and fractions, the data on the pharmacological activity of single constituents of Zingiber officinale are still insufficient. To assess the antidementia properties of the plant, a thin layer chromatography (TLC)-based bioautography acetylcholinesterase inhibitory assay [...] Read more.
Although numerous studies have been conducted on ginger extracts and fractions, the data on the pharmacological activity of single constituents of Zingiber officinale are still insufficient. To assess the antidementia properties of the plant, a thin layer chromatography (TLC)-based bioautography acetylcholinesterase inhibitory assay was performed on the Zingiber officinale diethyl ether extract. It led to the recognition of three active inhibitors among volatile constituents of the plant: ar-curcumene (A), α-sesquiphellandrene (B) and a-zingiberene (C). The identification of the components was possible thanks to the application of a TLC–HPLC-MS interface analysis of active zones and the GC-MS qualitative analysis of the tested samples. Based on the obtained results, the influence of several extraction techniques (hydrodistillation—HD, pressurized liquid extraction or accelerated solvent extraction—ASE, shaking maceration–SM, supercritical fluid extraction–SFE, and ultrasound-assisted extraction—UAE) on the recovery of the active metabolites from plant material was assessed to deliver enriched extracts. As a result, HD and SFE, were found to be the most efficient methods to recover the volatile components and the concentrations of A, B, and C reached 0.51 ± 0.025, 0.77 ± 0.045, and 1.67 ± 0.11 percent, respectively. Only HD and SFE were found to recover monoterpene hydrocarbons from the plant matrix. The remaining techniques provided extracts rich in more complex constituents, like sesquiterpenes. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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14 pages, 1768 KiB  
Article
Assessment of Hepatoprotective Effect of Chokeberry Juice in Rats Treated Chronically with Carbon Tetrachloride
by Hanna Piotrowska-Kempisty, Michał Nowicki, Jadwiga Jodynis-Liebert, Monika Kurpik, Małgorzata Ewertowska, Teresa Adamska, Jan Oszmiański and Małgorzata Kujawska
Molecules 2020, 25(6), 1268; https://doi.org/10.3390/molecules25061268 - 11 Mar 2020
Cited by 12 | Viewed by 2729
Abstract
The aim of this study was to compare the protective effects of chokeberry juice and silymarin against chemical-induced liver fibrosis in rats. Liver fibrosis was induced by CCl4 administered two days a week for six weeks. Two groups of rats were co-treated [...] Read more.
The aim of this study was to compare the protective effects of chokeberry juice and silymarin against chemical-induced liver fibrosis in rats. Liver fibrosis was induced by CCl4 administered two days a week for six weeks. Two groups of rats were co-treated with chokeberry juice, 10 mL/kg/day. or silymarin as a positive control, 100 mg/kg/day for six weeks. Hepatic lipid peroxidation was suppressed by 50% and the activity of hepatic antioxidant enzymes was increased by 19%–173% in rats co-treated with CCl4 and substances tested as compared to rats administered CCl4 alone. Hepatic hydroxyproline was decreased by 24% only in rats treated with silymarin. The messenger RNA (mRNA) expression levels of fibrosis-related molecules, procollagen I, α-SMA, TIMP-1, TGFβ, and TNFα, which were significantly increased in the liver of CCl4-treated rats, were not modulated by substances tested. Histological evaluation revealed a slight protective effect of silymarin against fibrosis. However, in CCl4 + chokeberry-treated rats, the density of vacuolated hepatocytes was significantly lower than that in silymarin administered animals. Chokeberry juice did not demonstrate an antifibrotic effect in the applied experimental model of fibrosis, and the effect of the known antifibrotic agent, silymarin, was very limited. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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23 pages, 6113 KiB  
Article
The Effects of Houttuynia cordata Thunb and Piper ribesioides Wall Extracts on Breast Carcinoma Cell Proliferation, Migration, Invasion and Apoptosis
by Subhawat Subhawa, Teera Chewonarin and Ratana Banjerdpongchai
Molecules 2020, 25(5), 1196; https://doi.org/10.3390/molecules25051196 - 06 Mar 2020
Cited by 20 | Viewed by 4573
Abstract
Houttuynia cordata Thunb. (HCT) and Piper ribesioides Wall. (PR) are common herbs that are widely distributed throughout East Asia and possess various biological properties including anti-cancer effects. However, in breast cancer, their mechanisms responsible for anti-carcinogenic effects have not been clarified yet. In [...] Read more.
Houttuynia cordata Thunb. (HCT) and Piper ribesioides Wall. (PR) are common herbs that are widely distributed throughout East Asia and possess various biological properties including anti-cancer effects. However, in breast cancer, their mechanisms responsible for anti-carcinogenic effects have not been clarified yet. In this study, the inhibitory effects of HCT and PR ethanolic extracts on breast cancer cell proliferation, migration, invasion and apoptosis were examined. In MCF-7 and MDA-MB-231 cells, HCT and PR extracts at low concentrations can inhibit colony formation and induce G1 cell cycle arrest by downregulating cyclinD1 and CDK4 expression. Additionally, HCT and PR extracts also decreased the migration and invasion of both breast cancer cell lines through inhibition of MMP-2 and MMP-9 secretion. Moreover, the induction of apoptosis was observed in breast cancer cells treated with high concentrations of HCT and PR extracts. Not only stimulated caspases activity, but HCT and PR extracts also upregulated the expression of caspases and pro-apoptotic Bcl-2 family proteins in breast cancer cells. Altogether, these findings provide the rationale to further investigate the potential actions of HCT and PR extracts against breast cancer in vivo. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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19 pages, 2848 KiB  
Article
Elsholtzia ciliata (Thunb.) Hyl. Extracts from Different Plant Parts: Phenolic Composition, Antioxidant, and Anti-Inflammatory Activities
by Lauryna Pudziuvelyte, Mindaugas Liaudanskas, Aiste Jekabsone, Ilona Sadauskiene and Jurga Bernatoniene
Molecules 2020, 25(5), 1153; https://doi.org/10.3390/molecules25051153 - 05 Mar 2020
Cited by 38 | Viewed by 5926
Abstract
Polyphenols play an important role on the health-promoting properties of humans. Plants belonging to Lamiaceae family are known as rich source of phenolic compounds. The current work aimed to evaluate the phenolic compounds, antioxidant, and anti-inflammatory activity of Elsholtzia ciliata (Thunb.) Hyl. ethanolic [...] Read more.
Polyphenols play an important role on the health-promoting properties of humans. Plants belonging to Lamiaceae family are known as rich source of phenolic compounds. The current work aimed to evaluate the phenolic compounds, antioxidant, and anti-inflammatory activity of Elsholtzia ciliata (Thunb.) Hyl. ethanolic extracts from leaf, stem, flower, and whole herb. Twelve compounds were identified in ethanolic extracts using high-performance liquid chromatography (HPLC). The HPLC analysis revealed that chlorogenic acid, rosmarinic acid, and rutin were predominant compounds in ethanolicic extracts. Using HPLC-ABTS (2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)) post-column assay, avicularin, chlorogenic, and rosmarinic acids were identified as the predominant radical scavengers in all ethanolic extracts. All tested preparations significantly reduced the level of secretion of proinflammatory cytokines TNF-α, IL-6, and prostaglandin E2 induced by lipopolysaccharide treatment in mouse peritoneal macrophage cell culture. Stem and flower extracts were most efficient in reducing cytokine release, but leaf extract demonstrated stronger effect on prostaglandin E2 secretion. This is the first study exploring antioxidant efficiency by HPLC–ABTS post-column method and investigating anti-inflammatory activity of ethanolic extracts from E. ciliata different plant parts. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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Review

Jump to: Editorial, Research

32 pages, 1469 KiB  
Review
Significance of Artemisia Vulgaris L. (Common Mugwort) in the History of Medicine and Its Possible Contemporary Applications Substantiated by Phytochemical and Pharmacological Studies
by Halina Ekiert, Joanna Pajor, Paweł Klin, Agnieszka Rzepiela, Halina Ślesak and Agnieszka Szopa
Molecules 2020, 25(19), 4415; https://doi.org/10.3390/molecules25194415 - 25 Sep 2020
Cited by 66 | Viewed by 17639
Abstract
Artemisia vulgaris L. (common mugwort) is a species with great importance in the history of medicine and was called the “mother of herbs” in the Middle Ages. It is a common herbaceous plant that exhibits high morphological and phytochemical variability depending on the [...] Read more.
Artemisia vulgaris L. (common mugwort) is a species with great importance in the history of medicine and was called the “mother of herbs” in the Middle Ages. It is a common herbaceous plant that exhibits high morphological and phytochemical variability depending on the location where it occurs. This species is well known almost all over the world. Its herb—Artemisiae vulgaris herba—is used as a raw material due to the presence of essential oil, flavonoids, and sesquiterpenoids lactones and their associated biological activities. The European Pharmacopoeia has listed this species as a potential homeopathic raw material. Moreover, this species has been used in traditional Chinese, Hindu, and European medicine to regulate the functioning of the gastrointestinal system and treat various gynecological diseases. The general aim of this review was to analyze the progress of phytochemical and pharmacological as well as professional scientific studies focusing on A. vulgaris. Thus far, numerous authors have confirmed the beneficial properties of A. vulgaris herb extracts, including their antioxidant, hepatoprotective, antispasmolytic, antinociceptive, estrogenic, cytotoxic, antibacterial, and antifungal effects. In addition, several works have reviewed the use of this species in the production of cosmetics and its role as a valuable spice in the food industry. Furthermore, biotechnological micropropagation of A. vulgaris has been analyzed. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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16 pages, 446 KiB  
Review
One Hundred Faces of Geraniol
by Wanda Mączka, Katarzyna Wińska and Małgorzata Grabarczyk
Molecules 2020, 25(14), 3303; https://doi.org/10.3390/molecules25143303 - 21 Jul 2020
Cited by 70 | Viewed by 7378
Abstract
Geraniol is a monoterpenic alcohol with a pleasant rose-like aroma, known as an important ingredient in many essential oils, and is used commercially as a fragrance compound in cosmetic and household products. However, geraniol has a number of biological activities, such as antioxidant [...] Read more.
Geraniol is a monoterpenic alcohol with a pleasant rose-like aroma, known as an important ingredient in many essential oils, and is used commercially as a fragrance compound in cosmetic and household products. However, geraniol has a number of biological activities, such as antioxidant and anti-inflammatory properties. In addition, numerous in vitro and in vivo studies have shown the activity of geraniol against prostate, bowel, liver, kidney and skin cancer. It can induce apoptosis and increase the expression of proapoptotic proteins. The synergy of this with other drugs may further increase the range of chemotherapeutic agents. The antibacterial activity of this compound was also observed on respiratory pathogens, skin and food-derived strains. This review discusses some of the most important uses of geraniol. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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20 pages, 272 KiB  
Review
Fish By-Product Use as Biostimulants: An Overview of the Current State of the Art, Including Relevant Legislation and Regulations within the EU and USA
by Moses Madende and Maria Hayes
Molecules 2020, 25(5), 1122; https://doi.org/10.3390/molecules25051122 - 03 Mar 2020
Cited by 58 | Viewed by 8268
Abstract
Crop production systems have adopted cost-effective, sustainable and environmentally friendly agricultural practices to improve crop yields and the quality of food derived from plants. Approaches such as genetic selection and the creation of varieties displaying favorable traits such as disease and drought resistance [...] Read more.
Crop production systems have adopted cost-effective, sustainable and environmentally friendly agricultural practices to improve crop yields and the quality of food derived from plants. Approaches such as genetic selection and the creation of varieties displaying favorable traits such as disease and drought resistance have been used in the past and continue to be used. However, the use of biostimulants to promote plant growth has increasingly gained attention, and the market size for biostimulants is estimated to reach USD 4.14 billion by 2025. Plant biostimulants are products obtained from different inorganic or organic substances and microorganisms that can improve plant growth and productivity and abate the negative effects of abiotic stresses. They include materials such as protein hydrolysates, amino acids, humic substances, seaweed extracts and food or industrial waste-derived compounds. Fish processing waste products have potential applications as plant biostimulants. This review gives an overview of plant biostimulants with a focus on fish protein hydrolysates and legislation governing the use of plant biostimulants in agriculture. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products)
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