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

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
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.

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

2018 ◽  
Vol 15 (2) ◽  
pp. 127-135 ◽  
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.

Polyphenol Contents, Antioxidant and Antibacterial Activities of Aqueous Algerian Propolis Extracts

2021 ◽  
Author(s):  
E.K. Soltani ◽  
K. Zaim ◽  
K. Mokhnache ◽  
N. Haichour ◽  
S. Mezaache-Aichour ◽  
...  
Keyword(s):  
Aqueous Extract ◽  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Antibacterial Properties ◽  
Natural Antioxidants ◽  
Antibacterial Activities ◽  
Antimicrobial Activities ◽  
Biological Properties ◽  
Aqueous Extracts

The propolis, an extremely complex resinous material, exhibits valuable pharmacological and biological properties, mainly attributed to the presence of polyphenols. The composition of propolis depends on time, vegetation, and the area of collection. Total flavonoid and polyphenol contents of aqueous extracts of propolis samples from different areas of Algeria, determined by using aluminum chloride and Folin–Ciocalteu colorimetric methods, were in the range of 3.047 ± 0.004–5.273 ± 0.013 mg/g and 96.833 ± 0.027–458.833 ± 0.0005 mg/g crude extract of propolis, respectively. This study examined the antioxidant and antimicrobial activities of propolis. Aqueous extracts of propolis were obtained in order to evaluate their antioxidant activities by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging, β-carotene and electrochemical assays. All tested propolis samples had relatively strong antioxidant activities, which were also correlated with the total polyphenol and flavonoid content present. The percentage of inhibition of lipid peroxidation of linoleic acid emulsion during 24 h varied between 86.04 ± 0.42 and 90.60 ± 3.77% among the tested samples. The highest DPPH radical scavenging activity was observed by ABAL (Ain Abassa Aqueous Extract) with IC50 = 8.49 ± 5.07 10−5 μg/ml, and the lowest was observed by SAL (Setif Aqueous Extract) with IC50 of 21.16 ± 0.0001 μg/ml. The most important antibacterial activity was obtained with Ain Abassa extract; the zones of inhibition obtained for this excerpt vary from 15.22 to 15.5 mm. Followed by the Setif extract with areas of 12.33 to 12.75 mm, the Tizi-Ouzou extract with areas of 10.11 to 11.11 mm. This study will bring an innovation for further studies with regard to the antioxidant and antibacterial properties of the aqueous extracts of propolis. This study corroborates that Algerian propolis is a rich source of natural antioxidants, properties which could be used in the prevention of different diseases, both in humans and in animals.

scholarly journals Determination of in vitro antioxidant activity of the leaves extracts of Ehretia pubescens

2020 ◽  
Vol 11 (4) ◽  
pp. 6262-6267
Author(s):  
Krishnamoorthy Meenakumari ◽  
Giridharan Bupesh ◽  
Mayur Mausoom Phukan
Keyword(s):  
Antioxidant Activity ◽  
Ethyl Acetate ◽  
Radical Scavenging Activity ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Biological Properties ◽  
Scavenging Activity ◽  
Reducing Power Assay

The foods from plants were known to ensure against degenerative diseases and maturing because of their antioxidant activitycredited to their high content. Information on antioxidant activity of Indian medicinal plant is abundant. To the best of our knowledge, biological properties have not been accounted in the literature for this species of . As a point, this is the first results to assess the anti-oxidant activity of the plant which belongs to the family . The antioxidant activity of Methanol, , Ethyl acetate and Aqueous extracts of E. was determined using the DPPH free radical scavenging activity, ABTS radical scavenging activity and reducing power assay. The DPPH scavenging activity showed higher activity observed in extract (63%) of E. than (54%), (44%) and aqueous (30%). the ABTS assay inhibition in extract (58%) than (43%), (38%) and aqueous (32%) extracts. The reducing power assay of different extracts was increased in extract (54%) than (40%), (34%) and aqueous (28%) extracts. Overall, the and ethyl acetate extract had higher antioxidant properties than other extract. However, in this study, extracts exhibit great potential for antioxidant activity and may be useful for their nutritional and medicinal functions.

scholarly journals Chemical Profiling and Biological Properties of Extracts from Different Parts of Colchicum Szovitsii Subsp. Szovitsii

Antioxidants ◽  
2019 ◽  
Vol 8 (12) ◽  
pp. 632 ◽  
Author(s):  
Gabriele Rocchetti ◽  
Biancamaria Senizza ◽  
Gokhan Zengin ◽  
Murat Ali Okur ◽  
Domenico Montesano ◽  
...  
Keyword(s):  
Biological Activities ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Extraction Methods ◽  
Biological Properties ◽  
Leaf Extracts ◽  
Orthogonal Projections ◽  
Antioxidant Power ◽  
Latent Structures

Like other members of the Colchicum genus, C. szovitsii subsp. szovitsii is also of medicinal importance in Turkish traditional medicine. However, its biological properties have not been fully investigated. Herein, we focused on the evaluation of the in vitro antioxidant and enzyme inhibitory effects of flower, root and leaf extracts, obtained using different extraction methods. In addition, a comprehensive (poly)-phenolic and alkaloid profiling of the different extracts was undertaken. In this regard, ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC-QTOF-MS) allowed us to putatively annotate 195 polyphenols and 87 alkaloids. The most abundant polyphenols were flavonoids (83 compounds), whilst colchicine and 2-demethylcolchicine were some of the most widespread alkaloids in each extract analyzed. However, our findings showed that C. szovitsii leaf extracts were a superior source of both total polyphenols and total alkaloids (being, on average 24.00 and 2.50 mg/g, respectively). Overall, methanolic leaf extracts showed the highest (p < 0.05) ferric reducing antioxidant power (FRAP) reducing power (on average 109.52 mgTE/g) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging (on average 90.98 mgTE/g). Interestingly, each C. szovitsii methanolic extract was more active than the water extracts when considering enzymatic inhibition such as against tyrosinase, glucosidase, and acetylcholinesterase (AChE). Strong correlations (p < 0.01) were also observed between polyphenols/alkaloids and the biological activities determined. Multivariate statistics based on supervised orthogonal projections to latent structures discriminant analysis (OPLS-DA) allowed for the detection of those compounds most affected by the different extraction methods. Therefore, this is the first detailed evidence showing that C. szovitsii subsp. szovitsii might provide beneficial effects against oxidative stress and the associated chronic diseases. Nevertheless, the detailed mechanisms of action need to be further investigated.

scholarly journals Effect of Chitosan Nanoparticle-Loaded Thymus serpyllum on Hydrogen Peroxide-Induced Bone Marrow Stromal Cell Damage

2019 ◽  
Vol 2019 ◽  
pp. 1-12
Author(s):  
Salma Baig ◽  
Ainnul Hamidah Syahadah Azizan ◽  
Hanumantha Rao Balaji Raghavendran ◽  
Elango Natarajan ◽  
Sangeetha Naveen ◽  
...  
Keyword(s):  
Hydrogen Peroxide ◽  
Cell Death ◽  
Cell Damage ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Potential Candidate ◽  
Protective Effects ◽  
Active Components ◽  
Thymus Serpyllum

We have determined the protective effects of Thymus serpyllum (TS) extract and nanoparticle-loaded TS on hydrogen peroxide-induced cell death of mesenchymal stromal cells (MSCs) in vitro. Gas chromatography–mass spectroscopy confirmed the spectrum of active components in the extract. Out of the three different extracts, the hexane extract showed significant free radical scavenging activity. Treatment of MSCs with H2O2 (hydrogen peroxide) significantly increased intracellular cell death; however, pretreatment with TS extract and nanoparticle-loaded TS (200 μg/ml) suppressed H2O2-induced elevation of Cyt-c and MMP13 and increased the survival rates of MSCs. H2O2-induced (0.1 mM) changes in cytokines were attenuated in the extract and nanoparticles by pretreatment and cotreatment at two time points (p<0.05). H2O2 increased cell apoptosis. In contrast, treatment with nanoparticle-loaded TS suppressed the percentage of apoptosis considerably (p<0.05). Therefore, TS may be considered as a potential candidate for enhancing the effectiveness of MSC transplantation in cell therapy.

scholarly journals Antioxidant Activity of Metabolites from Coleonema Album (Rutaceae)

2006 ◽  
Vol 1 (5) ◽  
pp. 1934578X0600100 ◽  
Author(s):  
Lindy L. Esterhuizen ◽  
Riaan Meyer ◽  
Ian A. Dubery
Keyword(s):  
Antioxidant Activity ◽  
South African ◽  
Structural Information ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Active Components ◽  
Bioassay Guided Fractionation ◽  
The Relationship

Coleonema album, a member of the South African ‘Fynbos’ biome, was evaluated for its antioxidant and free radical scavenging activity. Ethanol- and acetone-based extracts from plant material obtained from two different geographical areas were analysed. A bioassay-guided fractionation methodology was followed for screening of active compounds. The 1,1-diphenyl-2-picrylhydrazyl (DPPH)-TLC method revealed the presence of a number of antioxidants which were quantified by the DPPH-spectrophotometric assay and the oxygen radical absorbance capacity (ORAC) assay. The C. album extracts possessed significant in vitro antioxidant activity, a large portion of which appeared to be contributed by the phenolic compounds. In contrast, the reducing power of the extracts could not be correlated with the observed antioxidant activity. Identification and structural information of the active components were obtained by a combination of preparative TLC and LC-MS which revealed the presence of coumarin aglycones and glycosides. The results of this study indicate that C. album contains strong antioxidants that warrant further investigation into the relationship between the structure and activity of the active coumarin metabolites.

scholarly journals Phytochemical, in-vitro biological and chemo-preventive profiling of Arisaema jacquemontii Blume tuber extracts

2019 ◽  
Vol 19 (1) ◽  
Author(s):  
Saira Tabassum ◽  
Muhammad Zia ◽  
Esperanza J. Carcahe de Blanco ◽  
Riffat Batool ◽  
Roohi Aslam ◽  
...  
Keyword(s):  
Cell Lines ◽  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Scavenging Activity ◽  
Zone Of Inhibition ◽  
Meoh Extract ◽  
Etoac Extract

Abstract Background Arisaema jacquemontii is traditionally used in treatment of different diseases. In this study, phytochemical, in vitro biological and chemo-preventive screening of A. jacquemontii was carried out to explore its pharmacological potential. Methods The dried tuber of A. jacquemontii was extracted in 11 organic solvent mixture of different polarity. The extracts were screened for phytochemical assays (phenolics and flavonoids), antioxidants potential (free radical scavenging activity, total antioxidant activity, reducing power), biological activities (antibacterial, antifungal, cytotoxic, antileishmanial, protein kinase inhibition), and chemopreventive activities using different cell lines through standard protocols. Results Significant amount phenolic contents were determined in EtOH and MeOH extracts (210.3 ± 3.05 and 193.2 ± 3.15 μg GAE/mg, respectively). Maximum flavonoid content was determined in MeOH extract (22.4 ± 4.04 μg QE/mg). Noteworthy, DPPH scavenging activity was also recorded for MeOH extract (87.66%) followed by MeOH+EtOAc extract (85.11%). Considerable antioxidant capacity (7.8 ± 0.12 μg AAE/mg) and reducing power (3.1 ± 0.15 μg AAE/mg) was observed in extract of MeOH. The LC50 against brine shrimp and leishmanial parasite was found 9.01 and 12.87 μg/mL for n-Hex and CHCl3 extracts, respectively. The highest zone of inhibition against Streptomyces hyphae formation (12.5 ± 1.77 mm) by n-Hex extract. Growth zone of inhibition 13.8 ± 1.08 mm was recorded for EtOAc and MeOH extracts, respectively against Micrococcus luteus while 10.0 ± 0.11 mm for MeOH extract against Aspergillus flavus. In-vitro cytotoxic assay showed that n-Hex extract had higher cytotoxicity against DU-145 prostate cancer and HL-60 cancer cell lines. NF-kB and MTP potential showed 34.01 and 44.87 μg/mL for n-Hex and CHCl3 extracts, respectively in chemo-preventive potential. Conclusion The study concludes that Arisaema jacquemontii bears significant phytochemical activity and pharmacological activities, this plant can be further explored for isolation of active component against a number of aliments.

scholarly journals Antioxidant, Antidiabetic, and Anticholinesterase Activities and Phytochemical Profile of Azorella glabra Wedd

Plants ◽  
2019 ◽  
Vol 8 (8) ◽  
pp. 265 ◽  
Author(s):  
Immacolata Faraone ◽  
Dilip K. Rai ◽  
Daniela Russo ◽  
Lucia Chiummiento ◽  
Eloy Fernandez ◽  
...  
Keyword(s):  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Ethanol Extract ◽  
Flowering Plant ◽  
Acetylcholinesterase Inhibition ◽  
Neutral Radical ◽  
Phytochemical Profile

Oxidative stress is involved in different diseases, such as diabetes and neurodegenerative diseases. The genus Azorella includes about 70 species of flowering plant species; most of them are commonly used as food and in particular as a tea infusion in the Andean region of South America in folk medicine to treat various chronic diseases. Azorella glabra Wedd. aerial parts were firstly analyzed for their in vitro antioxidant activity using different complementary assays. In particular, radical scavenging activity was tested against biological neutral radical DPPH; ferric reducing power and lipid peroxidation inhibitory capacity (FRAP and Beta-Carotene Bleaching tests) were also determined. The Relative Antioxidant Capacity Index (RACI) was used to compare data obtained by different assays. Then, the inhibitory ability of samples was investigated against α-amylase and α-glucosidase enzymes involved in diabetes and against acetylcholinesterase and butyrylcholinesterase enzymes considered as strategy for the treatment of Parkinson’s or Alzheimer’s diseases. Moreover, the phytochemical profile of the sample showing the highest RACI (1.35) and interesting enzymatic activities (IC50 of 163.54 ± 9.72 and 215.29 ± 17.10 μg/mL in α-glucosidase and acetylcholinesterase inhibition, respectively) was subjected to characterization and quantification of its phenolic composition using LC-MS/MS analysis. In fact, the ethyl acetate fraction derived from ethanol extract by liquid/liquid extraction showed 29 compounds, most of them are cinnamic acid derivatives, flavonoid derivatives, and a terpene. To the best of our knowledge, this is the first report about the evaluation of significant biological activities and phytochemical profile of A. glabra, an important source of health-promoting phytochemicals.

Evaluation of In-vitro cytotoxic and antioxidant activity of methanolic extracts of Ipomoea carnea and Alternanthera sessilis

2016 ◽  
Vol 5 (08) ◽  
pp. 4763 ◽  
Author(s):  
Anushi Jain ◽  
Soumen Roy ◽  
Ambika Joshi* ◽  
Nitesh Joshi
Keyword(s):  
Antioxidant Activity ◽  
Therapeutic Potential ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Assay Method ◽  
Leaf Extracts ◽  
Alternanthera Sessilis ◽  
Cytotoxicity Activity ◽  
Ipomoea Carnea

Ipomoea carnea and Alternanthera sessilis are two common weeds in India which have shown to possess several medicinal properties. The present study pertains to assess the antioxidant and cytotoxicity activity of the leaf extracts of these plants. The extraction of leaf content of the plants was carried out by soxhlet method using methanol. The in vitro cytotoxicity assay was performed in vitro on vero cell line by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay method. In vitro antioxidant activity was carried out by DPPH radical scavenging method. The cytotoxicity activity for I. Carnea i.e. IC50 (50% growth inhibition) value was found to be 1mg/ml and the IC50 of A.sessilis was found to be 6.5mg/ml. The antioxidant activity of I. Carnea i.e. IC50 value was found to be 1200ug/ml whereas that of A. sessilis was found to be 400ug/ml. The cytotoxic activity was higher for Ipomoea extracts as compared to Alternanthera extracts. However, the DPPH free radical scavenging activity was higher for Alternanthera sessilis extracts as compared to Ipomoea carnea extracts. Both showed high in vitro activity, which indicates the therapeutic potential of these plants.

scholarly journals Muscari comosum L. Bulb Extracts Modulate Oxidative Stress and Redox Signaling in HepG2 Cells

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 416
Author(s):  
Fabiana Giglio ◽  
Maria Antonietta Castiglione Morelli ◽  
Ilenia Matera ◽  
Chiara Sinisgalli ◽  
Rocco Rossano ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Hepg2 Cells ◽  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Redox Homeostasis ◽  
Folk Medicine ◽  
Radical Scavenging ◽  
In Vitro Assays ◽  
South Italy

Muscari comosum L. bulbs are commonly used as food in South Italy and also in folk medicine. By evaluating in vitro antioxidant activity and biological activities of their aqueous and methanol extracts, we shed light on the potential role, including both the nutraceutical and health benefits, of this plant. Total polyphenol content (TPC) and total flavonoid content (TFC) were evaluated by the Folin–Ciocalteu method and by the aluminum chloride method, respectively. Antioxidant activity was investigated by three in vitro assays and relative antioxidant capacity index (RACI) was calculated to compare results obtained by different tests. The extracts were tested to evaluate their possible involvement in redox homeostasis, using the human hepatoma (HepG2) cell line used as model. The extracts exhibited concentration/solvent dependent radical scavenging activity, as well as dysregulation of some genes involved in redox pathways by promoting Nrf2, SOD-2, GPX1, ABCC6 and ABCG2 expression. NMR metabolomics analysis suggests that HepG2 cells treated with Muscari comosum extracts experience changes in some metabolites involved in various metabolic pathways.

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