Antioxidant and Antisteatotic Activities of Fucoidan Fractions from Marine and Terrestrial Sources

Fucoidan is a fucose-rich sulfated polysaccharide typically found in the cell wall of marine algae but also recently isolated from terrestrial sources. Due to a variety of biological activities, including antioxidant properties, fucoidan exhibits an attractive therapeutic potential against a wide array of metabolic diseases associated with oxidative stress. We used FTIR, 1H NMR and 13C NMR spectroscopy to investigate the structural features of a fucoidan fraction extracted from the brown alga Cystoseira compressa (CYS). The antioxidant potential of CYS was measured by DPPH, ABTS and FRAP assays, which revealed a radical scavenging capacity that was confirmed in in vitro cellular models of hepatic and endothelial cells. The same antioxidant effects were observed for another fucoidan fraction previously identified in the terrestrial tree Eucalyptus globulus (EUC). Moreover, in hepatic cells, CYS and EUC exhibited a significant antisteatotic action, being able to reduce intracellular triglyceride content through the regulation of key genes of hepatic lipid metabolism. EUC exerted stronger antioxidant and antisteatotic effects as compared to CYS, suggesting that both marine and terrestrial sources should be considered for fucoidan extraction and therapeutic applications.

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Antioxidant and Antisteatotic Activities of a New Fucoidan Extracted from Ferula hermonis Roots Harvested on Lebanese Mountains

Molecules ◽

10.3390/molecules26041161 ◽

2021 ◽

Vol 26 (4) ◽

pp. 1161

Author(s):

Zeinab El Rashed ◽

Giulio Lupidi ◽

Hussein Kanaan ◽

Elena Grasselli ◽

Laura Canesi ◽

...

Keyword(s):

Therapeutic Potential ◽

Biological Activities ◽

Radical Scavenging ◽

Bioactive Compound ◽

13C Nmr Spectroscopy ◽

Antioxidant Property ◽

Structural Features ◽

Water Soluble ◽

Cellular Models

Fucoidan is a fucose-rich sulfated polysaccharide with attractive therapeutic potential due to a variety of biological activities, including antioxidant action. Fucoidan is typically found in the cell wall of marine brown algae, but extra-algal sources have also been discovered. In the present work, for the first time we extracted a water soluble fucoidan fraction from the roots of the terrestrial shrub Ferula hermonis. This fucoidan fraction was termed FUFe, and contained fucose, glucose, sulfate, smaller amounts of monosaccharides such as galactose and mannose, and a minor quantity of proteins. FUFe structural features were investigated by FTIR, 1H NMR and 13C NMR spectroscopy. The antioxidant property of FUFe was measured by DPPH, ABTS and FRAP assays, which revealed a high radical scavenging capacity that was confirmed in in vitro cellular models. In hepatic and endothelial cells, 50 μg/mL FUFe could reduce ROS production induced by intracellular lipid accumulation. Moreover, in hepatic cells FUFe exhibited a significant antisteatotic action, being able to reduce intracellular triglyceride content and to regulate the expression of key genes of hepatic lipid metabolism. Altogether, our results candidate FUFe as a possible bioactive compound against fatty liver disease and related vascular damage.

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In Vitro and In Vivo Immunomodulator Activities of Allium sativum L.

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2018/4984659 ◽

2018 ◽

Vol 2018 ◽

pp. 1-10 ◽

Cited By ~ 9

Author(s):

Mouna Moutia ◽

Norddine Habti ◽

Abdallah Badou

Keyword(s):

Immune Cells ◽

Allium Sativum ◽

Therapeutic Potential ◽

Inflammatory Diseases ◽

Biological Activities ◽

Antioxidant Properties ◽

Allergic Airway Inflammation ◽

Cytokine Gene Expression

Allium Sativum L. (garlic), which is a species of the onion family, Alliaceae, is one of the most used plants in traditional medicine worldwide. More than 200 chemicals with diverse properties have been found in garlic extracts. Several garlic compounds were suggested to be efficient in improving various pathologies including certain types of cancer. This paper is an overview of data about garlic biological activities in vitro and/or in vivo on immune cells, on the development of certain inflammatory diseases, and on different types of carcinomas and sarcomas. Garlic and its compounds were found to have notable antioxidant properties. Garlic therapeutic potential has also been studied in several inflammatory diseases such as allergic-airway inflammation, inflammatory bowel disease, arthritic rheumatism, and atherosclerosis. Furthermore, garlic was found to be able to maintain the immune system homeostasis and to exhibit beneficial effects on immune cells especially through regulation of proliferation and cytokine gene expression. Finally, we will show how major garlic components such as sulfur compounds and polyphenols might be responsible for the garlic biological activities revealed in different situations. If identified, specific compounds present in garlic could potentially be used in therapy.

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In Vitro Antioxidant Activities of Methanolic Extracts of Caesalpinia volkensii Harms., Vernonia lasiopus O. Hoffm., and Acacia hockii De Wild

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2020/3586268 ◽

2020 ◽

Vol 2020 ◽

pp. 1-10

Author(s):

Beatrice Muthoni Guchu ◽

Alex King’ori Machocho ◽

Stephen Kiruthi Mwihia ◽

Mathew Piero Ngugi

Keyword(s):

Oxidative Stress ◽

Therapeutic Potential ◽

Antioxidant Activities ◽

Antioxidant Properties ◽

Radical Scavenging ◽

Antioxidant Power ◽

Chain Reactions ◽

Methanolic Extracts ◽

Ferric Reducing Antioxidant Power

Oxidative stress is the result of the disparity between pro-oxidants and antioxidants in an organism, and it is important in the pathogenesis of several degenerative disorders, such as arthritis, Alzheimer’s, cancer, and cardiovascular diseases. Free radicals can damage biomolecules, such as nucleic acids, lipids, proteins, polyunsaturated fatty acids, and carbohydrates, and the DNA leading to mutations. The use of antioxidants is effective in delaying the oxidation of biomolecules. Antioxidants are complexes found in the food that can retard or deter oxidation by preventing the initiation and propagation of oxidizing chain reactions. Medicinal plants have been used for centuries by man to manage diseases and have a host of antioxidant complexes. Traditionally, Caesalpinia volkensii, Vernonia lasiopus, and Acacia hockii have folkloric remedies against associated oxidative stress-mediated complications. However, the upsurge in its use has not been accompanied by scientific validations to support these claims. In this study, in vitro antioxidant activity of Caesalpinia volkensii, Vernonia lasiopus, and Acacia hockii collected from Embu County (Kenya) were determined by radical scavenging activities of 1,1-diphenyl-2-picrylhydrazyl (DPPH) and hydroxyl radical in addition to ferric reducing antioxidant power analyzed against that of L-ascorbic acid as the standard. The obtained results revealed remarkable antioxidant activities of the studied plant extracts as evidenced by the low IC50 and EC50 values. These antioxidant activities could be due to the presence of antioxidants phytochemicals such as flavonoids, phenols, terpenoids, and saponins among others. Therefore, the therapeutic potential of this plant could be due to their antioxidant properties. This study recommends bioassay of the extracts against oxidative stress-related disorders for development of phytomedicine with antioxidant properties.

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Citrus limon from Tunisia: Phytochemical and Physicochemical Properties and Biological Activities

BioMed Research International ◽

10.1155/2018/6251546 ◽

2018 ◽

Vol 2018 ◽

pp. 1-10 ◽

Cited By ~ 7

Author(s):

Mohamed Makni ◽

Raoua Jemai ◽

Walid Kriaa ◽

Yassine Chtourou ◽

Hamadi Fetoui

Keyword(s):

Biological Activities ◽

Antioxidant Properties ◽

Radical Scavenging ◽

Reducing Power ◽

Citrus Limon ◽

Strand Breakage ◽

Antibacterial And Antioxidant Activity

Natural plant extracts contain a variety of phenolic compounds which are assigned various biological activities. Our work aims to make a quantitative and qualitative characterization of the Zest (ZL) and the Flesh (FL) of lemon (Citrus limon), to valorize the pharmacological uses of lemon, by evaluating in vitro activities (DPPH, free radical scavenging and reducing power). The antibacterial, antifungal, and antiproliferative activities were sought in the ability of Citrus limon extracts to protect DNA and protein. We found that the ZL contains high amounts of phenolics responsible for the important antioxidant properties of the extract. However, the FL is richer in flavonoids than the ZL. The FL extract was also found to be more effective than the ZL in protecting plasmid DNA against the strand breakage induced by hydroxyl radicals. We also concluded that the FL extract exhibited potent antibacterial activity unlike ZL. Analysis by LC/MS-MS identified 6 compounds (Caffeoyl N-Tryptophan, Hydroxycinnamoyl-Oglucoside acid, Vicenin 2, Eriocitrin, Kaempferol-3-O- rutinoside, and Quercetin-3-rutinoside). These preliminary results showed that Citrus limon has antibacterial and antioxidant activity in vitro. It would be interesting to conduct further studies to evaluate the in vivo potential in an animal model.

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Anti-inflammatory Activity of Mollugo cerviana Methanolic Extract in LPS-induced Acute Inflammatory RAW 264.7 Macrophages

Combinatorial Chemistry & High Throughput Screening ◽

10.2174/1386207324666210302101204 ◽

2021 ◽

Vol 24 ◽

Author(s):

Robina Antony ◽

Jijin Raveendran ◽

Prabath Gopalakrishnan Biju

Keyword(s):

Acute Inflammation ◽

Methanolic Extract ◽

Therapeutic Potential ◽

Indian Subcontinent ◽

Antioxidant Properties ◽

Radical Scavenging ◽

Raw 264.7 Cells ◽

Raw 264.7 ◽

Anti Inflammatory

Background: The management of acute inflammation, which arises from complex biological responses to harmful stimuli, is an important determinant in recovery of the system from an otherwise detrimental outcome such as septicemia. However, the side effects and limitations of current therapeutics necessitate the development of newer and safer alternatives. Mollugo cerviana is a common medicinal herb of the Indian subcontinent and has been traditionally used for its fever mitigating, anti-microbial and hepatoprotective action. We have already reported the rich presence of radical scavenging phytochemicals in the plant extracts and their strong antioxidant properties. Objective: In the present study, we have evaluated the anti-inflammatory effects of methanolic extract (ME) of the areal parts of M. cerviana in a lipopolysaccharide (LPS)-induced acute inflammatory cell culture model. Method: RAW 264.7 mouse macrophages cell were stimulated by the bacterial endotoxin LPS at a concentration of 1 µg/mL. Cytotoxicity and anti-inflammatory potential of ME were carried out. Results: M. cerviana extract concentration up to 150 µg/ml was found to be non-toxic to cells (MTT and NRU assay). LPS induces acute inflammation by binding to TLR-4 receptors, initiating downstream signalling cascade that result in pro-inflammatory cytokine secretion. Extract treatment at 100 µg/ml suppressed LPS-induced gene expression (qPCR) and secretion (ELISA) of pro-inflammatory cytokines IL-1β, IL-6 and TNF-α, and the chemokine CCL2, indicating a dampening of the acute inflammatory cascade. LPS-induced elevation of ROS level (DCFDA method) was significant reduced by extract treatment. Nitric oxide production, as indicated by nitrite level, was significantly reduced post extract treatment. Conclusion: From this study, it is demonstrated that M. cerviana methanolic extract has potent anti-inflammatory effect in the in vitro acute inflammation model of LPS-stimulated RAW 264.7 cells. There is not reported study so far on the anti-inflammatory properties of M. cerviana in an LPS-induced acute inflammatory model which closely mimics a human bacteremia response. Hence, this study highlights the therapeutic potential of this extract as a source of anti-inflammatory lead molecules.

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Bioactive Algal-Derived Polysaccharides: Multi-Functionalization, Therapeutic Potential and Biomedical Applications

Current Pharmaceutical Design ◽

10.2174/1381612825666190618152133 ◽

2019 ◽

Vol 25 (11) ◽

pp. 1147-1162 ◽

Cited By ~ 9

Author(s):

Ida Idayu Muhamad ◽

Nabilah Zulkifli ◽

Suguna a/p Selvakumaran ◽

Nurul Asmak Md Lazim

Keyword(s):

Biomedical Applications ◽

Therapeutic Potential ◽

Biomedical Application ◽

Biological Activities ◽

Algal Species ◽

Structural Features ◽

Sulfated Polysaccharides ◽

Wide Range

Background: In recent decades, there has been an increased interest in the utilization of polysaccharides showing biological activity for various novel applications owing to their biocompatibility, biodegradability, non-toxicity, and some specific therapeutic activities. Increasing studies have started in the past few years to develop algal polysaccharides-based biomaterials for various applications. Methods: Saccharide mapping or enzymatic profiling plays a role in quality control of polysaccharides. Whereby, in vitro and in vivo tests as well as toxicity level discriminating polysaccharides biological activities. Extraction and purification methods are performed in obtaining algal derived polysaccharides followed by chromatographic profiles of their active compounds, structural features, physicochemical properties, and reported biological activities. Results: Marine algae are capable of synthesizing Glycosaminoglycans (GAGs) and non-GAGs or GAG mimetics such as sulfated glycans. The cell walls of algae are rich in sulfated polysaccharides, including alginate, carrageenan, ulvan and fucoidan. These biopolymers are widely used algal-derived polysaccharides for biological and biomedical applications due to their biocompatibility and availability. They constitute biochemical compounds that have multi-functionalization, therapeutic potential and immunomodulatory abilities, making them promising bioactive products and biomaterials with a wide range of biomedical applications. Conclusion: Algal-derived polysaccharides with clearly elucidated compositions/structures, identified cellular activities, as well as desirable physical properties have shown the potential that may create new opportunities. They could be maximally exploited to serve as therapeutic tools such as immunoregulatory agents or drug delivery vehicles. Hence, novel strategies could be applied to tailor multi-functionalization of the polysaccharides from algal species with vast biomedical application potentials.

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Digestibility and Bioavailability of the Active Components ofErica australisL. Aqueous Extracts and Their Therapeutic Potential as Acetylcholinesterase Inhibitors

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2015/854373 ◽

2015 ◽

Vol 2015 ◽

pp. 1-7 ◽

Cited By ~ 1

Author(s):

Pilar Dias ◽

Pedro L. Falé ◽

Alice Martins ◽

Amélia P. Rauter

Keyword(s):

Therapeutic Potential ◽

Cell Model ◽

Biological Activities ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Acetylcholinesterase Inhibitors ◽

Biological Properties ◽

Aqueous Extracts ◽

Active Components

Erica australisL. (Ericaceae) is used in traditional medicine to treat many free-radical related ailments. In the present work, the stability and biological activity of the plant aqueous extracts submitted to anin vitrodigestive process were investigated. Chemical stability was monitored by HPLC-DAD and LC-MS/MS, while the bioactivities were evaluated through the inhibition of acetylcholinesterase (AChE) and DPPH radical scavenging activity. Both extracts, whose main components were flavonol glycosides, inhibited AChE, showing IC50values of 257.9 ± 6.2 µg/mL and 296.8 ± 8.8 µg/mL for the decoction and for the infusion, respectively. Significant radical scavenging activities were also revealed by both extracts, as denoted by the IC50values for the decoction, 6.7 ± 0.1 µg/mL, and for the infusion, 10.5 ± 0.3 µg/mL. After submission to gastric and pancreatic juices, no remarkable alterations in the composition or in the bioactivities were observed, suggesting that the extracts may pass through the gastrointestinal tract, keeping their composition and therefore their biological properties. Moreover, the bioavailability of the components of both extracts, as studied in a Caco-2 cell model, showed that compounds can permeate the membrane, which is a condition to exert their biological activities. Our results add further support to the potential ofE. australisfor its antioxidant and neuroprotective properties.

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Synthesis, Molecular Docking Analysis, and Evaluation of Antibacterial and Antioxidant Properties of Stilbenes and Pinacol of Quinolines

Advances in Pharmacological and Pharmaceutical Sciences ◽

10.1155/2021/6635270 ◽

2021 ◽

Vol 2021 ◽

pp. 1-17

Author(s):

Zeleke Digafie ◽

Yadessa Melaku ◽

Zerihun Belay ◽

Rajalakshmanan Eswaramoorthy

Keyword(s):

Molecular Docking ◽

Biological Activities ◽

Antioxidant Properties ◽

Radical Scavenging ◽

Inhibition Zone ◽

Positive Control ◽

Health Concern ◽

Diffusion Method ◽

E Coli

Emergence of antimicrobial resistance to standard commercial drugs has become a critical public health concern worldwide. Hence, novel antimicrobials with improved biological activities are urgently needed. In this regard, a series of quinoline-stilbene derivatives were synthesized from substituted quinoline and benzyltriphenylphosphonium chloride using Wittig reaction. Furthermore, a novel pinacol of quinoline was synthesized by pinacolinazation of 2-methoxyquinoline-3-carbaldehyde which was achieved by aluminum powder-potassium hydroxide reagent combination at ambient temperature in methanol. The structures of the synthesized compounds were established based on their spectral data. The antibacterial activities of the synthesized compounds were evaluated in vitro by the paper disc diffusion method against two Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis) and two Gram-negative bacteria (Escherichia coli and Salmonella typhimurium). The best activity was displayed by compound 19 against E. coli with an inhibition zone of 16.0 ± 0.82 mm and 14.67 ± 0.94 mm at 500 and 250 μg/mL, respectively. This is close to ciprofloxacin which is used as a positive control. The results of in silico molecular docking evaluation of the compounds against E. coli DNA gyraseB were in good agreement with the in vitro antibacterial analysis. Compounds 19 (−6.9 kcal/mol) and 24 (−7.1 kcal/mol) showed the maximum binding affinity close to ciprofloxacin (−7.3 kcal/mol) used as positive control. Therefore, the antibacterial activity displayed by these compounds is encouraging for further investigation to improve the activities of quinoline-stilbenes by incorporating various bioisosteric groups in one or more positions of the phenyl nuclei for their potential pharmacological use. Findings of the DPPH radical scavenging assay indicated that some of the quinolone stilbenes and pinacol possess moderate antioxidant properties compared to ascorbic acid used as a natural antioxidant.

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Extraction, Chemical Composition, Antioxidant Property and In vitro Anticancer Activity of Silymarin from Silybum Marianum On Kb and A549 Cell Lines

Current Drug Discovery Technologies ◽

10.2174/1570163817666200827111127 ◽

2020 ◽

Vol 17 ◽

Author(s):

Mojgan Azadpour ◽

Mohammad Mehdi Farajollahi ◽

Ali Mohammad Varzi ◽

Pejman Hashemzadeh ◽

Hossein Mahmoudvand ◽

...

Keyword(s):

Anticancer Activity ◽

Cell Lines ◽

A549 Cell ◽

Hplc Analysis ◽

Antioxidant Properties ◽

Radical Scavenging ◽

Antioxidant Property ◽

Silybum Marianum ◽

Stable Free Radical

Introduction: This study aimed to evaluate the antioxidant property of silymarin (SM) extracted from the seed of Silybum marianum and its anticancer activity on KB and A549 cell lines following 24, 48, and 72 h of treatment. Methods: Ten grams of powdered S. marianum seeds were defatted using n-hexane for 6 hours and then extracted by methanol. The silymarin extracted of extraction components The extracted components of silymarin were measured by spectrophotometric assay and HPLC analysis. 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, phenol content, total flavonoid content, and total antioxidant capacity were measured to detect the antioxidant properties of SM. The anticancer activity of the SM on cell lines evaluated by MTT. Results: In HPLC analysis, more than 50% of the peaks were related to silibin A and B. SM was reducedDPPH (the stable free radical) with a 50% inhibitory concentration (IC50) of 6.56 μg/ ml in comparison with butylated hydroxyl toluene (BHT), which indicated an IC50 of ~3.9 μg/ ml.The cytotoxicity effect of SM on the cell lines was studied by MTT assay. The cytotoxicity effect of the extracted silymarin on KB and A549 cell lines was observed up to 80 and 70% at 156 and 78 µg/ml, respectively. The IC50 value of the extracted SM on KB and A549 cell lines after 24 hours of treatment was seen at 555 and 511 µg/ml, respectively. Conclusion: Due to the good antioxidant and anticancer properties of the isolated silymarin, its use as an anticancer drug is suggested.

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α-Glucosidase Inhibition, Antioxidant and Docking Studies of Hydroxycoumarins and their Mono and Bis O-alkylated/acetylated Analogs

Letters in Drug Design & Discovery ◽

10.2174/1570180814666170602081941 ◽

2018 ◽

Vol 15 (2) ◽

pp. 127-135 ◽

Cited By ~ 3

Author(s):

Parvesh Singh ◽

Nomandla Ngcoya ◽

Ramgopal Mopuri ◽

Nagaraju Kerru ◽

Neha Manhas ◽

...

Keyword(s):

In Silico ◽

Biological Activities ◽

Wide Spectrum ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Catalytic Site ◽

Docking Simulations ◽

In Silico Docking ◽

Anti Oxidant

Background: Diabetes Mellitus (DM) is a complex metabolic disease illustrated by abnormally high levels of plasma glucose or hyperglycaemia. Accordingly, several α-glucosidase inhibitors have been developed for the treatment of diabetes and other degenerative disorders. While, a coumarin ring has the privilege to represent numerous natural and synthetic compounds with a wide spectrum of biological activities e.g. anti-cancer, anti-HIV, anti-viral, anti-malarial, anti-microbial, anti-convulsant, anti-hypertensive properties. Besides this, coumarins have also shown potential to inhibit α-glucosidase leading to a generation of new promising antidiabetic agents. However, the testing of O-substituted coumarins for α-glucosidase inhibition has evaded the attention of medicinal chemists. Methods: For O-alkylation/acetylation reactions, the hydroxyl coumarins (A-B) initially activated by K2CO3 in dry DMF were reacted with variedly substituted haloalkanes at room temperature under nitrogen. The synthesized compounds were tested for their α-glucosidase (from Saccharomyces cerevisiae) inhibitory activity and anti-oxidant activity using DPPH radical scavenging activity. In silico docking simulations were conducted using CDocker module in DS (Accelrys) to explore the binding modes of the representative compounds in the catalytic site of α-glucosidase. Results: All the coumarin analogues (A1, B1, A2-A10, B2-B8) including their precursors (A-B) were evaluated for their in vitro α-glucosidase inhibition using acarbose as a standard inhibitor. All the mono O-alkylated coumarins (except A1) showed significant (p <0.05) α-glucosidase inhibition relative to the hydroxyl coumarin (A) with IC50 values ranging between 11.084±0.117 to 145.24± 29.22 µg/mL. Compound 7-(benzyloxy)-4, 5-dimethyl-2H-chromen-2-one (A9) bearing a benzyl group (Ph-CH2-) at position 7 showed a remarkable (p <0.05) increase in the activity (IC50 = 11.084±0.117 µg/mL), almost four-fold more than acarbose (IC50 = 40.578±5.999 µg/mL). The introduction of –NO2 group dramatically improved the anti-oxidant activity of coumarin, while the O-alkylation/acetylation decreased the activity. Conclusion: The present study describes the synthesis of functionalized coumarins and their evaluation for α-glucosidase inhibition and antioxidant activity under in vitro conditions. Based on IC50 data, the mono O-alkylated coumarins were observed to be stronger inhibitors of α-glucosidase with respect to their bis O-alkylated analogues. Coumarin (A9) bearing O-benzyloxy group displayed the strongest α-glucosidase inhibition, even higher than the standard inhibitor acarbose. The coumarin (A10) bearing –NO2 group showed the highest anti-oxidant activity amongst the synthesized compounds, almost comparable to the ascorbic acid. Finally, in silico docking simulations revealed the role of hydrogen bonding and hydrophobic forces in locking the compounds in catalytic site of α-glucosidase.

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