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A special issue of Molecules (ISSN 1420-3049).

Deadline for manuscript submissions: closed (31 December 2018) | Viewed by 36690

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Prof. Dr. Paula B. Andrade

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REQUIMTE/LAQV, Laboratory of Pharmacognosy, Faculty of Pharmacy, University of Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal
Interests: metabolite profiling of natural matrices; natural agents for inflammation; neurodegenerative disorders
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Dr. Patrícia Valentão

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REQUIMTE/LAQV, Laboratory of Pharmacognosy, Faculty of Pharmacy, University of Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal
Interests: narural products; primary and secondary metabolites; bioactivity
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The search for novel bioactive compounds in natural sources has been increasingly receiving a great amount of attention, driven by the need of finding alternatives with higher efficacy, and less undesirable effects than those currently used in therapeutics. Despite the historical value of terrestrial species, plants, in particular, being the most prolific source of bioactive molecules, sea contains a genetic diversity that is superior to land, comprising living organisms that could be responsible for the production of unknown compounds that might give a significant contribution to drug discovery.

This Special Issue will focus several aspects related to the bioactivity of both plant and animal species, covering from well characterized extracts to isolated compounds, primary and secondary metabolism, bioavailability and toxicological features, by exploring the relevant current scientific research to provide a general perspective of this broad area.

Prof. Dr. Paula B. Andrade
Prof. Dr. Patrícia Valentão
Guest Editors

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Keywords

Natural products
Plants
Macroinvertebrates
Seaweeds
Bioactivity
Drug discovery

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Published Papers (7 papers)

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Research

16 pages, 3447 KiB

Open AccessArticle

Anti-Arthritis Effect through the Anti-Inflammatory Effect of Sargassum muticum Extract in Collagen-Induced Arthritic (CIA) Mice

by Hyelin Jeon, Weon-Jong Yoon, Young-Min Ham, Seon-A Yoon and Se Chan Kang

Molecules 2019, 24(2), 276; https://doi.org/10.3390/molecules24020276 - 13 Jan 2019

Cited by 20 | Viewed by 4901

Abstract

(1) Background: Rheumatoid arthritis is a chronic autoimmune disease that causes progressive articular damage and functional loss. It is characterized by synovial inflammation that leads to progressive cartilage destruction. For this reason, research on functional foods that reduce the inflammatory response are under progress. (2) Methods: We focused on the anti-inflammatory effects of Sargassum muticum, and confirmed the effect of the extract on the collagen-induced arthritis (CIA) DBA/1J mice model. (3) Results: The extract was given at concentrations of 50, 100, and 200 mg/kg, and the arthritis score and edema volume of the experimental group were significantly different from the CIA group. The level of interleukin (IL)-6, tumor necrosis factor (TNF)-α, and interferon (IFN)-γ were determined in serum and lymphocytes. The expression of these cytokines in the serum remarkably decreased from S. muticum extract (SME)100 mg/kg, and decreased from SME 200 mg/kg in lymphocytes. Also, immunohistochemical analysis of IL-6 and TNF-α in the joints revealed that the inflammatory response was noticeably lower when treated with S. muticum extract. (4) Conclusions: This study provides results of the experiment of S. muticum extract treatment in a mouse model. The treatment was found to contribute to the alleviation of edema and symptoms by reducing the expression of inflammatory cytokines. It was concluded that it may be a useful substance to help in the mitigation of arthritis symptoms. Full article

(This article belongs to the Special Issue Biological Potential of Marine and Terrestrial Species)

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15 pages, 4676 KiB

Open AccessArticle

Cuscuta chinensis and C. campestris Attenuate Scopolamine-Induced Memory Deficit and Oxidative Damage in Mice

by Ming-Kuem Lin, Meng-Shiou Lee, Hui-Chi Huang, Tun-Jen Cheng, Yih-Dih Cheng and Chi-Rei Wu

Molecules 2018, 23(12), 3060; https://doi.org/10.3390/molecules23123060 - 22 Nov 2018

Cited by 24 | Viewed by 4419

Abstract

The seeds of Cuscuta chinensis Lam. and C. campestris Yuncker have been commonly used as Chinese medical material for preventing aging. Our previous studies have found that C. chinensis and C. campestris possess anti-inflammatory activities in rodents. However, their other biological activities, such as memory-improving properties, have not yet been explored. In the present study, we examined the memory-improving effects of the extracts of C. chinensis and C. campestris on scopolamine (SCOP)-induced memory deficit and explored their underlying mechanism in mice. Both Cuscuta species improved SCOP-induced memory deficits in the passive avoidance test, elevated plus-maze, and spatial performance test of the Morris water maze in mice. In addition, compared with mice injected with SCOP, mice pretreated with both Cuscuta species stayed for a longer time on the platform for the probe test of the Morris water maze. Moreover, both Cuscuta species reduced brain acetylcholinesterase activity and malondialdehyde levels that were increased by SCOP, and the species restored the activities of antioxidant enzymes (superoxide dismutase and catalase) and the levels of glutathione that were decreased by SCOP in the brains of mice. Both Cuscuta species further decreased brain interleukin-1β and tumor necrosis factor-α levels that were elevated by SCOP. We demonstrated that both Cuscuta species exhibited a protective activity against SCOP-induced memory deficit, cholinergic dysfunction, oxidative damage, and neuroinflammation in mice, and C. campestris has better potential than C. chinensis. In addition, we provided evidence that the seeds of C. campestris can be used as Cuscutae Semen in Traditional Chinese Medicine. Full article

(This article belongs to the Special Issue Biological Potential of Marine and Terrestrial Species)

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17 pages, 5465 KiB

Open AccessArticle

Anti-Bacterial Adhesion Activity of Tropical Microalgae Extracts

by Claudia Zea-Obando, Alina Tunin-Ley, Jean Turquet, Gérald Culioli, Jean-François Briand, Alexis Bazire, Karine Réhel, Fabienne Faÿ and Isabelle Linossier

Molecules 2018, 23(9), 2180; https://doi.org/10.3390/molecules23092180 - 29 Aug 2018

Cited by 14 | Viewed by 5070

Abstract

The evolution of regulations concerning biocidal products aimed towards an increased protection of the environment (e.g., EU Regulation No 528/2012) requires the development of new non-toxic anti-fouling (AF) systems. As the marine environment is an important source of inspiration, such AF systems inhibiting the adhesion of organisms without any toxicity could be based on molecules of natural origin. In this context, the antibiofilm potential of tropical microalgal extracts was investigated. The tropics are particularly interesting in terms of solar energy and temperatures which provide a wide marine diversity and a high production of microalgae. Twenty microalgal strains isolated from the Indian Ocean were studied. Their extracts were characterized in terms of global chemical composition by high resolution magic angle spinning (HR-MAS) and nuclear magnetic resonance (NMR) spectroscopy, toxicity against marine bacteria (viability and growth) and anti-adhesion effect. The different observations made by confocal laser scanning microscopy (CLSM) showed a significant activity of three extracts from Dinoflagellate strains against the settlement of selected marine bacteria without any toxicity at a concentration of 50 μg/mL. The Symbiodinium sp. (P-78) extract inhibited the adhesion of Bacillus sp. 4J6 (Atlantic Ocean), Shewanella sp. MVV1 (Indian Ocean) and Pseudoalteromonas lipolytica TC8 (Mediterranean Ocean) at 60, 76 and 52%, respectively. These results underlined the potential of using microalgal extracts to repel fouling organisms. Full article

(This article belongs to the Special Issue Biological Potential of Marine and Terrestrial Species)

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16 pages, 4822 KiB

Open AccessArticle

Synergistic Effect of Bioactive Anticarcinogens from Soybean on Anti-Proliferative Activity in MDA-MB-231 and MCF-7 Human Breast Cancer Cells In Vitro

by Yingying Zhu, Yang Yao, Zhenxing Shi, Nadia Everaert and Guixing Ren

Molecules 2018, 23(7), 1557; https://doi.org/10.3390/molecules23071557 - 27 Jun 2018

Cited by 42 | Viewed by 5342

Abstract

Consumption of soybean products has been implicated in the prevention of breast cancer. This study provides insights into the anti-proliferative activity of 12 anticarcinogens from soybean by single or two-way combination treatment against MCF-7 and MDA-MB-231 human breast cancer cells. Results showed that genistein, daidzein, glycitein, genistin and dainzin showed stronger anti-proliferative activity against MCF-7 cells with EC₅₀ values of 66.98 ± 4.87 μM, 130.14 ± 2.10 μM, 190.67 ± 5.65 μM, 72.82 ± 2.66 μM and 179.21 ± 6.37 μM, respectively. There is a synergistic effect of combination treatment of genistin plus daidzin in MCF-7 cells with combination index at inhibition of 50% (CI₅₀) of 0.89 ± 0.12. Genistein, glycitein, genistin and β-sitosterol were demonstrated to have a stronger anti-proliferative activity against MDA-MB-231 cells with EC₅₀ values of 93.75 ± 5.15 μM, 142.67 ± 5.88 μM, 127.82 ± 4.70 μM and 196.28 ± 4.45 μM. The synergistic effect was observed in the mixture of genistein plus genistin, genistein plus β-sitosterol or β-sitosterol plus genistin with CI₅₀ values of 0.56 ± 0.13, 0.54 ± 0.20 and 0.45 ± 0.12, respectively. These bioactive anticarcinogens were able to inhibit invasion and migration of breast cancer cells and the combination treatments enhanced the inhibitory effect. Regulation of PI3K/Akt/mTORpathway seems to be the main mechanisms involved in the anticancer activity. Full article

(This article belongs to the Special Issue Biological Potential of Marine and Terrestrial Species)

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19 pages, 1106 KiB

Open AccessArticle

Phenolic and Nonpolar Fractions of Elaeagnus rhamnoides (L.) A. Nelson Extracts as Virulence Modulators—In Vitro Study on Bacteria, Fungi, and Epithelial Cells

by Barbara Różalska, Beata Sadowska, Jerzy Żuchowski, Marzena Więckowska-Szakiel, Aleksandra Budzyńska, Urszula Wójcik and Anna Stochmal

Molecules 2018, 23(7), 1498; https://doi.org/10.3390/molecules23071498 - 21 Jun 2018

Cited by 23 | Viewed by 4929

Abstract

Butanol extracts from leaves, twigs, and fruits of Elaeagnus rhamnoides (L.) A. Nelson (sea buckthorn, SBT) were fractionated into phenolic and nonpolar lipid components, the chemical composition of which was analyzed. Assuming that an effect on natural microbiota and host epithelial cells needs to be assessed, regardless of the purpose of using SBT formulations in vivo, the minimal inhibitory/biocidal/fungicidal concentrations (MICs/MBCs/MFCs) of the fractions and reference phytocompounds were screened, involving 17 species of Gram-positive and Gram-negative bacteria and Candida species. The MICs of SBT extracts were in the range of 0.25–2.0 mg∙mL⁻¹. Since direct antimicrobial activity of the extracts was quite low and variable, the impact of subMIC on the important in vivo persistence properties of model microorganisms S. aureus and C. albicans was evaluated. Tests for adhesion and biofilm formation on an abiotic surface and on surfaces conditioned with fibrinogen, collagen, plasma, or artificial saliva showed the inhibitory activity of the fractions. The effects on fluorescein isothiocyanate (FITC)-labeled staphylococci adhesion to fibroblasts (HFF-1) and epithelial cells (Caco-2), and on fungal morphogenesis, indicated that SBT extracts have high antivirulence potential. Cytotoxicity tests (MTT reduction) on the standard fibroblast cell line showed variable biological safety of the fractions depending on their composition and concentration. The new information afforded by this study, additional to that already known, is of potential practical value in the application of SBT-derived preparations as antivirulence agents. Full article

(This article belongs to the Special Issue Biological Potential of Marine and Terrestrial Species)

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12 pages, 2005 KiB

Open AccessArticle

Identification of a 3-Alkylpyridinium Compound from the Red Sea Sponge Amphimedon chloros with In Vitro Inhibitory Activity against the West Nile Virus NS3 Protease

by Aubrie O’Rourke, Stephan Kremb, Brendan M. Duggan, Salim Sioud, Najeh Kharbatia, Misjudeen Raji, Abdul-Hamid Emwas, William H. Gerwick and Christian R. Voolstra

Molecules 2018, 23(6), 1472; https://doi.org/10.3390/molecules23061472 - 18 Jun 2018

Cited by 15 | Viewed by 5125

Abstract

Viruses are underrepresented as targets in pharmacological screening efforts, given the difficulties of devising suitable cell-based and biochemical assays. In this study we found that a pre-fractionated organic extract of the Red Sea sponge Amphimedon chloros was able to inhibit the West Nile Virus NS3 protease (WNV NS3). Using liquid chromatography–mass spectrometry (LC-MS) and nuclear magnetic resonance (NMR) spectroscopy, the identity of the bioactive compound was determined as a 3-alkylpyridinium with m/z = 190.16. Diffusion Ordered Spectroscopy (DOSY) NMR and NMR relaxation rate analysis suggest that the bioactive compound forms oligomers of up to 35 kDa. We observed that at 9.4 μg/mL there was up to 40–70% inhibitory activity on WNV NS3 protease in orthogonal biochemical assays for solid phase extracts (SPE) of A. chloros. However, the LC-MS purified fragment was effective at inhibiting the protease up to 95% at an approximate amount of 2 µg/mL with negligible cytotoxicity to HeLa cells based on a High-Content Screening (HCS) cytological profiling strategy. To date, 3-alkylpyridinium type natural products have not been reported to show antiviral activity since the first characterization of halitoxin, or 3-alkylpyridinium, in 1978. This study provides the first account of a 3-alkylpyridinium complex that exhibits a proposed antiviral activity by inhibiting the NS3 protease. We suggest that the here-described compound can be further modified to increase its stability and tested in a cell-based assay to explore its full potential as a potential novel antiviral capable of inhibiting WNV replication. Full article

(This article belongs to the Special Issue Biological Potential of Marine and Terrestrial Species)

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13 pages, 17318 KiB

Open AccessArticle

Sinularin Selectively Kills Breast Cancer Cells Showing G2/M Arrest, Apoptosis, and Oxidative DNA Damage

by Hurng-Wern Huang, Jen-Yang Tang, Fu Ou-Yang, Hui-Ru Wang, Pei-Ying Guan, Chiung-Yao Huang, Chung-Yi Chen, Ming-Feng Hou, Jyh-Horng Sheu and Hsueh-Wei Chang

Molecules 2018, 23(4), 849; https://doi.org/10.3390/molecules23040849 - 8 Apr 2018

Cited by 47 | Viewed by 5778 | Correction

Abstract

The natural compound sinularin, isolated from marine soft corals, is antiproliferative against several cancers, but its possible selective killing effect has rarely been investigated. This study investigates the selective killing potential and mechanisms of sinularin-treated breast cancer cells. In 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H- tetrazolium, inner salt (MTS) assay, sinularin dose-responsively decreased the cell viability of two breast cancer (SKBR3 and MDA-MB-231) cells, but showed less effect on breast normal (M10) cells after a 24 h treatment. According to 7-aminoactinomycin D (7AAD) flow cytometry, sinularin dose-responsively induced the G2/M cycle arrest of SKBR3 cells. Sinularin dose-responsively induced apoptosis on SKBR3 cells in terms of a flow cytometry-based annexin V/7AAD assay and pancaspase activity, as well as Western blotting for cleaved forms of poly(ADP-ribose) polymerase (PARP), caspases 3, 8, and 9. These caspases and PARP activations were suppressed by N-acetylcysteine (NAC) pretreatment. Moreover, sinularin dose-responsively induced oxidative stress and DNA damage according to flow cytometry analyses of reactive oxygen species (ROS), mitochondrial membrane potential (MitoMP), mitochondrial superoxide, and 8-oxo-2′-deoxyguanosine (8-oxodG)). In conclusion, sinularin induces selective killing, G2/M arrest, apoptosis, and oxidative DNA damage of breast cancer cells. Full article

(This article belongs to the Special Issue Biological Potential of Marine and Terrestrial Species)

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