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Bioactive Substances: Properties, Applications and or Toxicities

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A special issue of Applied Sciences (ISSN 2076-3417). This special issue belongs to the section "Environmental Sciences".

Deadline for manuscript submissions: closed (29 February 2020) | Viewed by 48346

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Prof. Dr. Caterina Faggio

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Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98168 Messina, Italy
Interests: cytotoxicity; oxidative stress markers; health status in shellfish and fish; ecophysiology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Bioactive substances demonstrate a wide range of biological, pharmacological and nutraceutical activities and are considered to have beneficial effects on nutrition and health. Bioactive substances are currently used in several product preparations, mainly as flavouring agents, fragrances, and functional additives in the cosmetic and pharmaceutical industries, as well their individual components. Moreover, these bioactive substances have been suggested for use in foodstuffs, as they are known to display ample properties. However, some of them may show potentially toxic mechanisms, and for this reason further research is still needed.

Prof. Dr. Caterina Faggio
Guest Editor

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Keywords

Bioactive substances
Waste products
Nanoparticles
Heavy metals
Algae
Nutraceuticals
Nutrition
Vertebrates
Invertebrates
Culture cells

Published Papers (10 papers)

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Research

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14 pages, 1915 KiB

Open AccessFeature PaperArticle

Antioxidant Properties of a Supercritical Fluid Extract of the Halophyte Mesembryanthemum nodiflorum L. from Sicilian Coasts: Nutraceutical and Cosmeceutical Applications

by Rosaria Arena, Simona Manuguerra, Edward Collins, Abdelkarim Mahdhi, Giuseppe Renda, Concetta Maria Messina and Andrea Santulli

Appl. Sci. 2020, 10(7), 2374; https://doi.org/10.3390/app10072374 - 31 Mar 2020

Cited by 5 | Viewed by 2529

Abstract

The aim of this paper was to obtain different extracts from the aerial parts of Mesembryanthemum nodiflorum, comparing traditional extraction (using solvents with increasing polarity such as hexane, ethanol 80%, acetone 70% and water) with an eco-friendly technique (supercritical fluid extraction (SFE)); to evaluate which extract showed a higher amount of antioxidants and then evaluate the bioactive properties in vitro, in human fibroblast (HS68). From the six extracts obtained it was observed that the solvent with the highest extraction efficiency was water, but the extracts in ethanol, N-hexane and SFE are those that showed the highest antioxidant activity (polyphenols, 1,1-Diphenyl-2-picrylhydrazyl (DPPH) and reducing power). On the basis of these results, the SFE extract was chosen to evaluate the antioxidant and anti-aging activity in vitro, by assessing cell vitality and molecular markers (MTT and immunoblotting assays). The results showed that the SFE extract exerted antioxidant activity in vitro, protecting cells from mortality induced by oxidative stress; this protection was also confirmed at the molecular level, by the levels of the protein integrin -1, that is able to prevent the negative effects of a stress situation, such as oxidative stress, that could promote aging and related diseases. This extract, obtained with an eco-friendly technique, given its beneficial properties, could be used for application in nutraceuticals and cosmeceuticals. Full article

(This article belongs to the Special Issue Bioactive Substances: Properties, Applications and or Toxicities)

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12 pages, 1144 KiB

Open AccessArticle

Evaluation of Tramadol Hydrochloride Toxicity to Juvenile Zebrafish—Morphological, Antioxidant and Histological Responses

by Lucie Plhalova, Pavla Sehonova, Jana Blahova, Veronika Doubkova, Frantisek Tichy, Caterina Faggio, Petra Berankova and Zdenka Svobodova

Appl. Sci. 2020, 10(7), 2349; https://doi.org/10.3390/app10072349 - 30 Mar 2020

Cited by 37 | Viewed by 3677

Abstract

The presence of pharmaceuticals in water bodies is associated with the increasing consumption of these substances and limited elimination from wastewater. Pharmaceutical residues and their metabolites may have an unfavorable impact on fish and other aquatic biota. As the purification of wastewater from tramadol is very limited and the knowledge on its effects on non-target organisms is low, we decided to assess the subchronic impact of tramadol hydrochloride on fish—on the mortality, growth and histopathology, together with the impact on selected indices of oxidative stress. The juvenile growth toxicity test was carried out on zebrafish (Danio rerio), in accordance with the Organisation for European Economic Cooperation Guidelines 215 (Fish, Juvenile Growth Test). The fish were exposed to a range of tramadol hydrochloride concentrations (0.2, 2, 20, 200 and 600 µg/L) for 28 days. The outcome of this study suggests that chosen concentrations of tramadol hydrochloride did not affect either mortality or growth (regarding weight, length and specific growth rate). However, the results of this study indicate that 28-day exposure can negatively influence selected indices of oxidative stress, which is a harmful imbalance between free radicals and antioxidants in an organism. A significant increase was observed in glutathione S-transferase activity in the experimental group exposed to 2 µg/L tramadol hydrochloride, compared to the control. Moreover, lipid peroxidation was observed in groups exposed to 20 and 200 µg/L, in comparison to the control. Full article

(This article belongs to the Special Issue Bioactive Substances: Properties, Applications and or Toxicities)

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13 pages, 1847 KiB

Open AccessFeature PaperArticle

Screening of Antioxidant Potentials and Bioactive Properties of the Extracts Obtained from Two Centaurea L. Species (C. kroumirensis Coss. and C. sicula L. subsp sicula)

by Nedra Dhouibi, Simona Manuguerra, Rosaria Arena, Abdelkarim Mahdhi, Concetta Maria Messina, Andrea Santulli and Hatem Dhaouadi

Appl. Sci. 2020, 10(7), 2267; https://doi.org/10.3390/app10072267 - 26 Mar 2020

Cited by 13 | Viewed by 2661

Abstract

Herbal medicines, dietary supplements, or infusions with health promoting effects can note strong consumer demand. Hence, researchers and scientists have been increasingly focusing on the promotion of medicinal plants. In this respect, the present study has the evaluation of the biological properties of different extracts (hexane, chloroform, methanol, ultrasonic, essential oil, and supercritical) obtained from two Centaurea species (C. kroumirensis (Coss.) and C. sicula L. subsp sicula) as purpose. Antioxidative activities were assessed by in vitro assays including total phenolic content, free radical scavenging assay and ferric ion reducing power. Among the fourteen extracts examined, the highest total phenolic content (TPC) and antioxidant abilities were recorded in ultrasonic ethanol extracts of both Centaurea species. Additionally, these extracts exhibited a noticeable strong protective effect of the human skin fibroblast cell line (HS-68) that was exposed to oxidative stress induced by hydrogen peroxide. According to our results, the sonication with ethanol might be an ideal, rapid, and eco-friendly extraction method for obtaining a polyphenol-rich extract that exhibited high antioxidant activity. The results presented herein suggest that Centaurea species could be promoted as an antioxidant resource that could be exploited for the development of nutraceuticals or in pharmacology industry. Full article

(This article belongs to the Special Issue Bioactive Substances: Properties, Applications and or Toxicities)

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10 pages, 724 KiB

Open AccessFeature PaperArticle

The Dietary Effect of Vitex agnus-castus Hydroalcoholic Extract on Growth Performance, Blood Biochemical Parameters, Carcass Quality, Sex Ratio and Gonad Histology in Zebrafish (Danio rerio)

by Tayebeh Enayat Gholampour, Raha Fadaei Raieni, Mojtaba Pouladi, Mohamad Larijani, Maria Pagano and Caterina Faggio

Appl. Sci. 2020, 10(4), 1402; https://doi.org/10.3390/app10041402 - 19 Feb 2020

Cited by 49 | Viewed by 4527

Abstract

The main purpose of this study was to consider the impact of Vitex agnus-castus hydroalcoholic extract, containing phytoestrogenic compounds on growth indices, sex ratio and histology of gonads of female Zebrafish. Fish larvae (4-day-old after hatching) were nourished with investigational diets (0 (control group T0), 5 g (T1), 10 g (T2) and 15 g (T3) kg⁻¹ food) from first active feeding for 90 days. The results showed that Condition Factor (CF), Food Conversion Rate (FCR), Body Weight Gain (BWG), and Specific Growth Rate (SGR) were affected meaningfully by hydroalcoholic extract of Vitex agnus-castus (p < 0.05). These factors were significantly higher in compare to T3 treatment (p < 0.05). With increasing concentration of the extract in the diet, the ratio of female to male increased Treatment of T3 resulted in 87.23% feminization. Overall, this study suggests the use of T3 treatment achieves the best reproduction performance and a higher percentage of females in zebrafish as a model for aquaculture species. According to the results, the lowest levels of glucose and cholesterol were observed in T3 treatment and showed a significant changes with the control and treatments (p < 0.05). Full article

(This article belongs to the Special Issue Bioactive Substances: Properties, Applications and or Toxicities)

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16 pages, 19666 KiB

Open AccessArticle

The Protective Effect of New Carnosine-Hyaluronic Acid Conjugate on the Inflammation and Cartilage Degradation in the Experimental Model of Osteoarthritis

by Rosalba Siracusa, Daniela Impellizzeri, Marika Cordaro, Alessio F. Peritore, Enrico Gugliandolo, Ramona D’Amico, Roberta Fusco, Rosalia Crupi, Enrico Rizzarelli, Salvatore Cuzzocrea, Susanna Vaccaro, Mariafiorenza Pulicetta, Valentina Greco, Sebastiano Sciuto, Antonella Schiavinato, Luciano Messina and Rosanna Di Paola

Appl. Sci. 2020, 10(4), 1324; https://doi.org/10.3390/app10041324 - 15 Feb 2020

Cited by 10 | Viewed by 4110

Abstract

Osteoarthritis (OA) is a disease that currently has no cure. There are numerous studies showing that carnosine and hyaluronic acid (HA) have a positive pharmacological action during joint inflammation. For this reason, the goal of this research was to discover the protective effect of a new carnosine conjugate with hyaluronic acid (FidHycarn) on the inflammatory response and on the cartilage degradation in an in vivo experimental model of OA. This model was induced by a single intra-articular (i.ar.) injection of 25 µL of normal saline with 1 mg of monosodium iodoacetate solution (MIA) in the knee joint of rats. MIA injection caused histological alterations and degradation of the cartilage, as well as behavioral changes. Oral treatment with FidHycarn ameliorated the macroscopic signs, improved thermal hyperalgesia and the weight distribution of the hind paw, and decreased histological and radiographic alterations. The oxidative damage was analyzed by evaluating the levels of nitrotyrosine and inducible nitric oxide synthase (iNOS) that were significantly reduced in FidHycarn rats. Moreover, the levels of pro-inflammatory cytokines and chemokines were also significantly reduced by FidHycarn. Therefore, for the first time, the effectiveness of oral administration of FidHycarn has been demonstrated in an osteoarthritis model. In conclusion, the new FidHycarn could represent an interesting therapeutic strategy to combat osteoarthritis. Full article

(This article belongs to the Special Issue Bioactive Substances: Properties, Applications and or Toxicities)

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10 pages, 2586 KiB

Open AccessFeature PaperArticle

Effect of Sowing Dates on Fatty Acids and Phytosterols Patterns of Carthamus tinctorius L.

by Jane Roche, Zephirin Mouloungui, Muriel Cerny and Othmane Merah

Appl. Sci. 2019, 9(14), 2839; https://doi.org/10.3390/app9142839 - 16 Jul 2019

Cited by 29 | Viewed by 2736

Abstract

Field experiments were carried out at the Regional Centre of Experimentation in Organic agriculture at Auch (near Toulouse, South west of France). Due to the high potential applications for its oil components such as fatty acids and phytosterols, safflower (Carthamus tinctorius L.) is considered as an emerging crop. Safflower plants, as many other oil crops, are submitted to environmental stresses that modify seed composition. Nevertheless, few reports are available about the effects of environmental conditions on fatty acid and phytosterol compositions in safflower. Different rainfall supplies can be managed by delaying the sowing dates. In this study, fatty acid and phytosterol contents have been evaluated in safflower seeds cultivated at two sowing dates (conventional and late) that led to a differential of rainfall during seed development. At harvest, seeds were used for oil extraction. Fatty acid composition was performed by using GC-FID. A set of seeds was dehulled to separate the almond (embryo) and hull to release the extraction and measurement of sterol contents in the two compartments by GC-FID. A delay of sowing increased the content of all sterol categories but induced a significant decrease in fatty acids. The ratio of saturated to unsaturated fatty acids increased under a delaying sowing. The repartition of phytosterols was ¾ and ¼ of total sterols in the embryo and the hull, respectively. These results could make the use of hull (considered as waste) possible, help breeders to improve safflower oil composition and develop new industrial applications. Full article

(This article belongs to the Special Issue Bioactive Substances: Properties, Applications and or Toxicities)

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11 pages, 691 KiB

Open AccessFeature PaperArticle

Pistacia Atlantica Desf., a Source of Healthy Vegetable Oil

by Amina Labdelli, Kamel Zemour, Valérie Simon, Muriel Cerny, Ahmed Adda and Othmane Merah

Appl. Sci. 2019, 9(12), 2552; https://doi.org/10.3390/app9122552 - 21 Jun 2019

Cited by 30 | Viewed by 5681

Abstract

Pistacia atlantica, which belongs to the Anacardiaceae family, is an important species for rural people in arid and semi-arid areas. The fruit, rich in oil, is used in traditional medicine for the treatment of various diseases. The oil extracted from this species growing in a northern area of Algeria and its fatty acid composition were previously studied. However, the largest areas where this species is present (traditional cultivation) is located in southern Algeria. Moreover, studies on oil fatty acid composition and essential oil were always conducted separately. This study was performed in order to assess the fatty acid and volatile organic compound composition of P. atlantica vegetable oil. The seeds were collected randomly from Djelfa (300 km South of Algiers, Algeria). Oil content and fatty acid composition were determined by Soxhlet extraction. The seeds contained high concentrations of oil (32–67%). The major fatty acids were oleic (39–49%), linoleic (23.6–31%), and palmitic (21.3–26.6%) acids. The ratio of polyunsaturated fatty acids (PUFA) to saturated fatty acids (SFA) indicated that the content of unsaturated fatty acids was approximately three times higher than that of SFA. This ratio is widely used in epidemiological studies and research on cardiovascular diseases, diabetes, and metabolic syndrome. The ratios of ω-acids, i.e., ω-9/ω-6 and ω-6/ω-3, were 1.3–2 and 18.5–38.3, respectively. Crushed seeds were analyzed by headspace solid-phase microextraction (SPME) coupled with gas chromatography–mass spectrometry. More than 40 compounds were identified, mainly monoterpenes (C₁₀H₁₆), such as α-terpinene and terpinolene, but also sesquiterpenes (C₁₅H₂₄) at lower levels. The value of this species as a source of healthy oil rich in ω-3 acid and its effects on cardiovascular disease risk are discussed. Full article

(This article belongs to the Special Issue Bioactive Substances: Properties, Applications and or Toxicities)

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17 pages, 1308 KiB

Open AccessArticle

Impact of Copper Oxide Nanoparticles on Enhancement of Bioactive Compounds Using Cell Suspension Cultures of Gymnema sylvestre (Retz.) R. Br

by Ill-Min Chung, Govindasamy Rajakumar, Umadevi Subramanian, Baskar Venkidasamy and Muthu Thiruvengadam

Appl. Sci. 2019, 9(10), 2165; https://doi.org/10.3390/app9102165 - 27 May 2019

Cited by 47 | Viewed by 4696

Abstract

Gymnema sylvestre is a plant that is enriched in bioactive compounds. In particular, gymnemic acids (GA) and phenolic compounds (PC) are pharmaceutically important. There is a commercial demand for naturally occurring bioactive compounds, but their availability is limited due to geographical and seasonal variations. The elicitation approach can enhance the biosynthesis of phytochemicals during in vitro culture of G. sylvestre. Here, to further improve gymnemic acid II (GA II) and phenolic compounds (PC) production by G. sylvestre, cell suspension cultures (CSC), which has attracted attention for the production of essential phytochemicals, was explored using copper oxide nanoparticles (CuO NPs). Callus was obtained on MS medium containing 2,4-dichlorophenoxyacetic acid, kinetin, phytoagar, and sucrose. Agar-free MS medium was used to initiate CSC, which was treated with three concentrations of CuO NPs (1, 3 or 5 mg/L). Treatment for 48 h with 3 mg/L CuO NPs resulted in the greatest yields of GA II, total phenolics, and flavonoids. The cultures also displayed pronounced antioxidant, antidiabetic, anti-inflammatory, antibacterial, antifungal, and anticancer activities. The use of CuO NPs (3 mg/L) significantly increased the production of GA II (nine-fold) and PC compared to unamended CSC. We propose that CSC and use of nanoparticles (NPs) as a new generation of elicitors, offer a suitable prospect for the production of bioactive compounds. Full article

(This article belongs to the Special Issue Bioactive Substances: Properties, Applications and or Toxicities)

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Review

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9 pages, 788 KiB

Open AccessReview

Mycoremediation of PCBs by Pleurotus ostreatus: Possibilities and Prospects

by Se Chul Chun, Manikandan Muthu, Nazim Hasan, Shadma Tasneem and Judy Gopal

Appl. Sci. 2019, 9(19), 4185; https://doi.org/10.3390/app9194185 - 08 Oct 2019

Cited by 26 | Viewed by 6337

Abstract

With the rising awareness on environmental issues and the increasing risks through industrial development, clean up remediation measures have become the need of the hour. Bioremediation has become increasingly popular owing to its environmentally friendly approaches and cost effectiveness. Polychlorinated biphenyls (PCBs) are an alarming threat to human welfare as well as the environment. They top the list of hazardous xenobiotics. The multiple effects these compounds render to the niche is not unassessed. Bioremediation does appear promising, with myco remediation having a clear edge over bacterial remediation. In the following review, the inputs of white-rot fungi in PCB remediation are examined and the lacunae in the practical application of this versatile technology highlighted. The unique abilities of Pleurotus ostreatus and its deliverables with respect to removal of PCBs are presented. The need for improvising P. ostreatus-mediated remediation is emphasized. Full article

(This article belongs to the Special Issue Bioactive Substances: Properties, Applications and or Toxicities)

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21 pages, 2548 KiB

Open AccessReview

Survey of Pharmacological Activity and Pharmacokinetics of Selected β-Adrenergic Blockers in Regard to Their Stereochemistry

by Ružena Čižmáriková, Ladislav Habala, Jindra Valentová and Mário Markuliak

Appl. Sci. 2019, 9(4), 625; https://doi.org/10.3390/app9040625 - 13 Feb 2019

Cited by 24 | Viewed by 10325

Abstract

The present survey concentrates on pharmacodynamics and pharmacokinetics of selected β-adrenergic blockers from the point of view of their stereochemistry. It could be shown that the activity in the arylaminoethanol and aryloxyaminopropanol group of β-blockers is higher in their (–)-enantiomers as compared with the (+)-enantiomers. The stereoisomers differ also in other types of bioactivity as well as in toxicity. The particular pharmacokinetic stages such as resorption, distribution, and metabolism are discussed in regard to their stereochemistry. Full article

(This article belongs to the Special Issue Bioactive Substances: Properties, Applications and or Toxicities)

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