Microalgae as a Potential Functional Ingredient: Evaluation of the Phytochemical Profile, Antioxidant Activity and In-Vitro Enzymatic Inhibitory Effect of Different Species

The functional food market has been in a state of constant expansion due to the increasing awareness of the impact of the diet on human health. In the search for new natural resources that could act as a functional ingredient for the food industry, microalgae represent a promising alternative, considering their high nutritional value and biosynthesis of numerous bioactive compounds with reported biological properties. In the present work, the phytochemical profile, antioxidant activity, and enzymatic inhibitory effect aiming at different metabolic disorders (Alzheimer’s disease, Type 2 diabetes, and obesity) were evaluated for the species Porphyridium purpureum, Chlorella vulgaris, Arthorspira platensis, and Nannochloropsis oculata. All the species presented bioactive diversity and important antioxidant activity, demonstrating the potential to be used as functional ingredients. Particularly, P. purpureum and N. oculata exhibited higher carotenoid and polyphenol content, which was reflected in their superior biological effects. Moreover, the species P. purpureum exhibited remarkable enzymatic inhibition for all the analyses.

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α-Glucosidase and α-Amylase Inhibitory Effect and Antioxidant Activity of Aerial Part from Linaria aegyptiaca L.

Current Enzyme Inhibition ◽

10.2174/1573408014666181022115524 ◽

2019 ◽

Vol 15 (1) ◽

pp. 22-27

Author(s):

Abir Bekhaoua ◽

Ihcen Khacheba ◽

Hadjer Boussoussa ◽

Mohamed Yousfi

Keyword(s):

Antioxidant Activity ◽

Aerial Part ◽

Biological Effects ◽

Antioxidant Properties ◽

Inhibitory Effect ◽

In Vitro Assays ◽

Inhibitory Effects ◽

Methanolic Extracts ◽

Large Genus

Background: The genus Linaria belongs to the Scrophulariaceae family. It is a large genus comprising about 200 species. Various parts of several Linaria species have been reported to exhibit various biological effects. In Algeria especially in the Sahara and steppe regions, the different species of Linaria have several uses in dietary application. Objective: The aims of this study are to evaluate the α-Glucosidase and α-Amylase inhibitory effects and the antioxidant activity using in vitro assays by an organic extract of the aerial part of Linaria aegyptiaca collected in two months, April and June, from southern Algeria. Methods: The extracts were obtained with successful maceration in (hexane, dichloromethane, acetone and methanol). The phenolics and flavonoids contents of L. aegyptiaca extracts were evaluated with Folin- Ciocalteu and aluminum chloride reagents, respectively. Then, we studied their inhibitory effects on α-Glucosidase and α-Amylase enzymes. The antioxidant potential was determined in vitro with DPPH, ABT and Phosphomolybdate tests. Results: The highest phenolic and flavonoid content were detected in the methanolic extracts of Linaria aegyptiaca collected in April. All the extracts showed good inhibitory activity on both enzymes, where the best activity was against α- amylase by acetonic extract collected in June with an IC50 = 95.03 μg/ml. The evaluation of antioxidant activity showed that all the extracts exhibited a good antioxidant capacity compared to standard antioxidants. Conclusion: The aim of this research is to establish the anti-diabetic properties and the probable alpha glucosidase and alpha amylase inhibitory activities of Algerian Linaria aegyptiaca species. These results show that this species has good antioxidant properties and a good potential for hyperglycemia management, too. The Algerian Linaria aegyptiaca can be considered as a natural source of anti-hyperglycemic treatment and might be interesting for the prospect of new molecules with antidiabetic effect.

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In vitro cytotoxicity assessment of ferulic, caffeic and p-coumaric acids on human renal cancer cells

Journal Biomedical and Biopharmaceutical Research ◽

10.19277/bbr.17.1.225 ◽

2020 ◽

Vol 17 (1) ◽

pp. 1-12

Author(s):

Rita Caparica ◽

André Rolim Baby ◽

Tânia Almeida ◽

João Guilherme Costa

Keyword(s):

Cancer Cells ◽

Renal Cancer ◽

Biological Effects ◽

Biological Properties ◽

In Vitro Cytotoxicity ◽

Hydroxycinnamic Acids ◽

Therapeutic Uses ◽

Cytotoxicity Assessment ◽

The Impact

Bioactive compounds from natural sources have been extensively studied as potential therapeutic agents, due to their chemical, structural, and biological properties. Among them, hydroxycinnamic acids emerge with a very interesting pharmacological potential to prevent and treat several diseases, including cancer. However, while some studies support their anticancer activity, other reports indicate otherwise. Since the impact of these compounds on renal cancer is not well established, further studies are needed to better understand their biological effects and their potential therapeutic uses in this cancer. In this work, the cytotoxicity of three hydroxycinnamic acids: ferulic, caffeic and p-coumaric acids, was evaluated on 786-O human renal cancer cells by MTT and CV assays. At concentrations up to 250 µM, none of the studied natural compounds showed cytotoxic effects to 786-O cell line. At higher concentrations (500 and 1000 µM), while ferulic acid also did not significantly influence the cell viability of 786-O cells, p-coumaric and caffeic acids decreased the renal cancer cells viability. Nevertheless, further studies on the biological activity of these compounds, using other methodologies, as well as using other cancer cell models, should be performed.

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Antioxidant Activity, Phenolic Content and Hematoprotective Effects of Cleome arabica Polyphenolic Leaf Extract

Phytothérapie ◽

10.3166/phyto-2019-0206 ◽

2019 ◽

Author(s):

C. Tigrine ◽

A. Kameli

Keyword(s):

Antioxidant Activity ◽

Biological Effects ◽

Reducing Power ◽

Hematological Toxicity ◽

Protective Effects ◽

Ferrous Ions ◽

Polyphenolic Extract ◽

Cleome Arabica

In this study a polyphenolic extract from Cleome arabica leaves (CALE) was investigated for its antioxidant activity in vitro using DPPH•, metal chelating and reducing power methods and for its protective effects against AraC-induced hematological toxicity in vivo using Balb C mice. Results indicated that CALE exhibited a strong and dose-dependent scavenging activity against the DPPH• free radical (IC50 = 4.88 μg/ml) and a high reducing power activity (EC50 = 4.85 μg/ml). Furthermore, it showed a good chelating effects against ferrous ions (IC50 = 377.75 μg/ml). The analysis of blood showed that subcutaneous injection of AraC (50 mg/kg) to mice during three consecutive days caused a significant myelosupression (P < 0.05). The combination of CALE and AraC protected blood cells from a veritable toxicity. Where, the number of the red cells, the amount of hemoglobin and the percentage of the hematocrite were significantly high. On the other hand, AraC cause an elevation of body temperature (39 °C) in mice. However, the temperature of the group treated with CALE and AraC remained normal and did not exceed 37.5 °C. The observed biological effects of CALE, in vitro as well as in vivo, could be due to the high polyphenol and flavonoid contents. In addition, the antioxidant activity of CALE suggested to be responsible for its hematoprotective effect.

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Curcumin-based antioxidant and glycohydrolase inhibitor compounds: Synthesis and in vitro appraisal of the dual activity against diabetes

Medicinal Chemistry ◽

10.2174/1573406416666200506083718 ◽

2020 ◽

Vol 16 ◽

Author(s):

Sajjad Esmaeili ◽

Nazanin Ghobadi ◽

Donya Nazari ◽

Alireza Pourhossein ◽

Hassan Rasouli ◽

...

Keyword(s):

Antioxidant Activity ◽

Enzyme Inhibitor ◽

Radical Scavenging Activity ◽

Curcuma Longa ◽

Radical Scavenging ◽

Reducing Power ◽

Inhibitory Effect ◽

Curcumin Derivatives ◽

Reducing Power Assay

Background: Curcumin, as the substantial constituent of the turmeric plant (Curcuma longa), plays a significant role in the prevention of various diseases, including diabetes. It possesses ideal structure features as enzyme inhibitor, including a flexible backbone, hydrophobic nature, and several available hydrogen bond (H-bond) donors and acceptors. Objective: The present study aimed at synthesizing several novel curcumin derivatives and further evaluation of these compounds for possible antioxidant and anti-diabetic properties along with inhibitory effect against two carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase, as these enzymes are therapeutic targets for attenuation of postprandial hyperglycemia. Methods: Therefore, curcumin-based pyrido[2,3-d]pyrimidine derivatives were synthesized and identified using an instrumental technique like NMR spectroscopy and then screened for antioxidant and enzyme inhibitory potential. Total antioxidant activity, reducing power assay and 1,1-diphenyl-2-picrylhydrazyl (DPPH• ) radical scavenging activity were done to appraisal the antioxidant potential of these compounds in vitro. Results: Compounds L6-L9 showed higher antioxidant activity while L4, L9, L12 and especially L8 exhibited the best selectivity index (lowest α-amylase/α-glucosidase inhibition ratio). Conclusion: These antioxidant inhibitors may be potential anti-diabetic drugs, not only to reduce glycemic index but also to limit the activity of the major reactive oxygen species (ROS) producing pathways.

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Chemical Composition, In Vitro and In Silico Antioxidant Potential of Melissa officinalis subsp. officinalis Essential Oil

Antioxidants ◽

10.3390/antiox10071081 ◽

2021 ◽

Vol 10 (7) ◽

pp. 1081

Author(s):

Matilda Rădulescu ◽

Călin Jianu ◽

Alexandra Teodora Lukinich-Gruia ◽

Marius Mioc ◽

Alexandra Mioc ◽

...

Keyword(s):

Antioxidant Activity ◽

Chemical Composition ◽

Essential Oil ◽

In Silico ◽

Antioxidant Properties ◽

Radical Scavenging ◽

Inhibitory Effect ◽

Melissa Officinalis ◽

Β Carotene

The investigation aimed to study the in vitro and in silico antioxidant properties of Melissa officinalis subsp. officinalis essential oil (MOEO). The chemical composition of MOEO was determined using GC–MS analysis. Among 36 compounds identified in MOEO, the main were beta-cubebene (27.66%), beta-caryophyllene (27.41%), alpha-cadinene (4.72%), caryophyllene oxide (4.09%), and alpha-cadinol (4.07%), respectively. In vitro antioxidant properties of MOEO have been studied in 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) free-radical scavenging, and inhibition of β-carotene bleaching assays. The half-maximal inhibitory concentration (IC50) for the radical scavenging abilities of ABTS and DPPH were 1.225 ± 0.011 μg/mL and 14.015 ± 0.027 μg/mL, respectively, demonstrating good antioxidant activity. Moreover, MOEO exhibited a strong inhibitory effect (94.031 ± 0.082%) in the β-carotene bleaching assay by neutralizing hydroperoxides, responsible for the oxidation of highly unsaturated β-carotene. Furthermore, molecular docking showed that the MOEO components could exert an in vitro antioxidant activity through xanthine oxidoreductase inhibition. The most active structures are minor MOEO components (approximately 6%), among which the highest affinity for the target protein belongs to carvacrol.

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Isobornylchalcones as Scaffold for the Synthesis of Diarylpyrazolines with Antioxidant Activity

Molecules ◽

10.3390/molecules26123579 ◽

2021 ◽

Vol 26 (12) ◽

pp. 3579

Author(s):

Svetlana A. Popova ◽

Evgenia V. Pavlova ◽

Oksana G. Shevchenko ◽

Irina Yu. Chukicheva ◽

Aleksandr V. Kutchin

Keyword(s):

Antioxidant Activity ◽

Antioxidant Properties ◽

Biological Properties ◽

High Reactivity ◽

Biologically Active ◽

Brain Lipids ◽

Wide Range ◽

Privileged Structure ◽

Vitro Model

The pyrazoline ring is defined as a “privileged structure” in medicinal chemistry. A variety of pharmacological properties of pyrazolines is associated with the nature and position of various substituents, which is especially evident in diarylpyrazolines. Compounds with a chalcone fragment show a wide range of biological properties as well as high reactivity which is primarily due to the presence of an α, β-unsaturated carbonyl system. At the same time, bicyclic monoterpenoids deserve special attention as a source of a key structural block or as one of the pharmacophore components of biologically active molecules. A series of new diarylpyrazoline derivatives based on isobornylchalcones with different substitutes (MeO, Hal, NO2, N(Me)2) was synthesized. Antioxidant properties of the obtained compounds were comparatively evaluated using in vitro model Fe2+/ascorbate-initiated lipid peroxidation in the substrate containing brain lipids of laboratory mice. It was demonstrated that the combination of the electron-donating group in the para-position of ring B and OH-group in the ring A in the structure of chalcone fragment provides significant antioxidant activity of synthesized diarylpyrazoline derivatives.

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Histological, Biomechanical, and Biological Properties of Genipin-Crosslinked Decellularized Peripheral Nerves

International Journal of Molecular Sciences ◽

10.3390/ijms22020674 ◽

2021 ◽

Vol 22 (2) ◽

pp. 674

Author(s):

Óscar Darío García-García ◽

Marwa El Soury ◽

David González-Quevedo ◽

David Sánchez-Porras ◽

Jesús Chato-Astrain ◽

...

Keyword(s):

Ex Vivo ◽

Nerve Repair ◽

Wistar Rat ◽

Biomechanical Properties ◽

Biological Properties ◽

Suitable Alternative ◽

Promising Alternative ◽

Histological Pattern ◽

The Impact

Acellular nerve allografts (ANGs) represent a promising alternative in nerve repair. Our aim is to improve the structural and biomechanical properties of biocompatible Sondell (SD) and Roosens (RS) based ANGs using genipin (GP) as a crosslinker agent ex vivo. The impact of two concentrations of GP (0.10% and 0.25%) on Wistar rat sciatic nerve-derived ANGs was assessed at the histological, biomechanical, and biocompatibility levels. Histology confirmed the differences between SD and RS procedures, but not remarkable changes were induced by GP, which helped to preserve the nerve histological pattern. Tensile test revealed that GP enhanced the biomechanical properties of SD and RS ANGs, being the crosslinked RS ANGs more comparable to the native nerves used as control. The evaluation of the ANGs biocompatibility conducted with adipose-derived mesenchymal stem cells cultured within the ANGs confirmed a high degree of biocompatibility in all ANGs, especially in RS and RS-GP 0.10% ANGs. Finally, this study demonstrates that the use of GP could be an efficient alternative to improve the biomechanical properties of ANGs with a slight impact on the biocompatibility and histological pattern. For these reasons, we hypothesize that our novel crosslinked ANGs could be a suitable alternative for future in vivo preclinical studies.

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Amorphous–Crystalline Calcium Phosphate Coating Promotes In Vitro Growth of Tumor-Derived Jurkat T Cells Activated by Anti-CD2/CD3/CD28 Antibodies

Materials ◽

10.3390/ma14133693 ◽

2021 ◽

Vol 14 (13) ◽

pp. 3693

Author(s):

Yurii P. Sharkeev ◽

Ekaterina G. Komarova ◽

Valentina V. Chebodaeva ◽

Mariya B. Sedelnikova ◽

Aleksandr M. Zakharenko ◽

...

Keyword(s):

T Cells ◽

Calcium Phosphate ◽

Biological Effects ◽

Electrical Potential ◽

Biological Properties ◽

Modern Trend ◽

Calcium Phosphate Coating ◽

Jurkat T Cells ◽

Micro Arc Oxidation

A modern trend in traumatology, orthopedics, and implantology is the development of materials and coatings with an amorphous–crystalline structure that exhibits excellent biocopatibility. The structure and physico–chemical and biological properties of calcium phosphate (CaP) coatings deposited on Ti plates using the micro-arc oxidation (MAO) method under different voltages (200, 250, and 300 V) were studied. Amorphous, nanocrystalline, and microcrystalline statesof CaHPO4 and β-Ca2P2O7were observed in the coatings using TEM and XRD. The increase in MAO voltage resulted in augmentation of the surface roughness Ra from 2.5 to 6.5 µm, mass from 10 to 25 mg, thickness from 50 to 105 µm, and Ca/P ratio from 0.3 to 0.6. The electrical potential (EP) of the CaP coatings changed from −456 to −535 mV, while the zeta potential (ZP) decreased from −53 to −40 mV following an increase in the values of the MAO voltage. Numerous correlations of physical and chemical indices of CaP coatings were estimated. A decrease in the ZP magnitudes of CaP coatings deposited at 200–250 V was strongly associated with elevated hTERT expression in tumor-derived Jurkat T cells preliminarily activated with anti-CD2/CD3/CD28 antibodies and then contacted in vitro with CaP-coated samples for 14 days. In turn, in vitro survival of CD4+ subsets was enhanced, with proinflammatory cytokine secretion of activated Jurkat T cells. Thus, the applied MAO voltage allowed the regulation of the physicochemical properties of amorphous–crystalline CaP-coatings on Ti substrates to a certain extent. This method may be used as a technological mechanism to trigger the behavior of cells through contact with micro-arc CaP coatings. The possible role of negative ZP and Ca2+ as effectors of the biological effects of amorphous–crystalline CaP coatings is discussed. Micro-arc CaP coatings should be carefully tested to determine their suitability for use in patients with chronic lymphoid malignancies.

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Distinct Chemistries Define the Diverse Biological Effects of Plasma Activated Water Generated with Spark and Glow Plasma Discharges

Applied Sciences ◽

10.3390/app11031178 ◽

2021 ◽

Vol 11 (3) ◽

pp. 1178

Author(s):

Evanthia Tsoukou ◽

Maxime Delit ◽

Louise Treint ◽

Paula Bourke ◽

Daniela Boehm

Keyword(s):

Mammalian Cells ◽

Biomedical Application ◽

Biological Effects ◽

Mode Of Delivery ◽

Chemical Species ◽

Resistant Bacteria ◽

Cytotoxic Activities ◽

Promising Alternative ◽

Plasma Activated Water

The spread of multidrug-resistant bacteria poses a significant threat to human health. Plasma activated liquids (PAL) could be a promising alternative for microbial decontamination, where different PAL can possess diverse antimicrobial efficacies and cytotoxic profiles, depending on the range and concentration of their reactive chemical species. In this research, the biological activity of plasma activated water (PAW) on different biological targets including both microbiological and mammalian cells was investigated in vitro. The aim was to further an understanding of the specific role of distinct plasma reactive species, which is required to tailor plasma activated liquids for use in applications where high antimicrobial activity is required without adversely affecting the biology of eukaryotic cells. PAW was generated by glow and spark discharges, which provide selective generation of hydrogen peroxide, nitrite and nitrate in the liquid. The PAW made by either spark or glow discharges showed similar antimicrobial efficacy and stability of activity, despite the very different reactive oxygen species (ROS) and reactive nitrogen species profiles (RNS). However, different trends were observed for cytotoxic activities and effects on enzyme function, which were translated through the selective chemical species generation. These findings indicate very distinct mechanisms of action which may be exploited when tailoring plasma activated liquids to various applications. A remarkable stability to heat and pressure was noted for PAW generated with this set up, which broadens the application potential. These features also suggest that post plasma modifications and post generation stability can be harnessed as a further means of modulating the chemistry, activity and mode of delivery of plasma functionalised liquids. Overall, these results further understanding on how PAL generation may be tuned to provide candidate disinfectant agents for biomedical application or for bio-decontamination in diverse areas.

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