scholarly journals Physico-Chemical and Pharmaco-Technical Characterization of Inclusion Complexes Formed by Rutoside with β-Cyclodextrin and Hydroxypropyl-β-Cyclodextrin Used to Develop Solid Dosage Forms

Processes ◽  
2020 ◽  
Vol 9 (1) ◽  
pp. 26
Author(s):  
Teodora Balaci ◽  
Bruno Velescu ◽  
Oana Karampelas ◽  
Adina Magdalena Musuc ◽  
George Mihai Nițulescu ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Molar Ratio ◽  
Mechanical Resistance ◽  
Direct Compression ◽  
Active Ingredients ◽  
Compression Process ◽  
Antioxidant Power

The aim of our study was to obtain rutoside (RUT) inclusion complexes in β-cyclodextrin (β-CD) and in hydroxypropyl-β-cyclodextrin (HP-β-CD), in a 1:1 molar ratio, using the lyophilization method of complexation in solution. The complexes were confirmed and characterized, in comparison with the raw materials and their simple physical mixtures, by SEM, DSC, and FT-IR analyses. The antioxidant activity of the compounds was assessed by using the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) and 2’-azino-bis(3-ethylbenzothiazolin-6-sulfonic) acid (ABTS) radicals, determining the radical scavenging activity, and by ferric reducing antioxidant power (FRAP) assay. The results revealed superior antioxidant ability for the inclusion complexes towards rutoside alone. The inclusion complexes were used as active ingredients in formulations of immediate-release tablets. The preformulation studies were performed on the powders for direct compression obtained after mixing the active ingredients with the excipients (Avicel PH 102, Polyplasdone XL-10, magnesium stearate, and talc). The materials were assessed for particle size, flowability, compressibility, and moisture content, establishing they are suitable for a direct compression process. The tablets were characterized regarding their pharmaco-technical properties and the results proved that the formulations lead to high-quality delivery systems, showing a good mechanical resistance with a low friability, excellent disintegration times, and satisfying dissolution rate. The performances were very similar for both formulations and the physico-mechanical properties of the tablets are not influenced by type of the used cyclodextrin, but the RUT- HP-β-CD tablets presented a higher dissolution rate.

scholarly journals Determination of formation constants and structural characterization of cyclodextrin inclusion complexes with two phenolic isomers: carvacrol and thymol

2016 ◽  
Vol 12 ◽  
pp. 29-42 ◽  
Author(s):  
Miriana Kfoury ◽  
David Landy ◽  
Steven Ruellan ◽  
Lizette Auezova ◽  
Hélène Greige-Gerges ◽  
...  
Keyword(s):  
Inclusion Complexes ◽  
Food Systems ◽  
Antioxidant Activities ◽  
Chemical Shifts ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Aqueous Solubility ◽  
Formation Constants ◽  
Molar Ratio ◽  
Phase Solubility

Carvacrol and thymol have been widely studied for their ability to control food spoilage and to extend shelf-life of food products due to their antimicrobial and antioxidant activities. However, they suffer from poor aqueous solubility and pronounced flavoring ability that limit their application in food systems. These drawbacks could be surpassed by encapsulation in cyclodextrins (CDs). Applications of their inclusion complexes with CDs were reported without investigating the inclusion phenomenon in deep. In this study, inclusion complexes were characterized in terms of formation constants (K f), complexation efficiency (CE), CD:guest molar ratio and increase in bulk formulation by using an UV–visible competitive method, phase solubility studies as well as 1H and DOSY 1H NMR titration experiments. For the first time, a new algorithmic treatment that combines the chemical shifts and diffusion coefficients variations for all guest protons was applied to calculate K f. The position of the hydroxy group in carvacrol and thymol did not affect the stoichiometry of the inclusion complexes but led to a different binding stability with CDs. 2D ROESY NMR experiments were also performed to prove the encapsulation and illustrate the stable 3D conformation of the inclusion complexes. The structural investigation was accomplished with molecular modeling studies. Finally, the radical scavenging activity of carvacrol and thymol was evaluated by the ABTS radical scavenging assay. An improvement of this activity was observed upon encapsulation. Taken together, these results evidence that the encapsulation in CDs could be valuable for applications of carvacrol and thymol in food.

Assessment of antioxidant and antibacterial activities of crude extracts of verbena officinalis Linn root or Atuch (Amharic)

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Antioxidant Activity ◽  
Methanolic Extract ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Dry Weight ◽  
Antimicrobial Activities ◽  
Total Flavonoid ◽  
Root Extract ◽  
Antioxidant Power ◽  
Crude Extracts

Verbena officinalis Linn is a traditionally known medicinal plant which is used against a number of diseases including inflammatory conditions. In this study its antioxidant activity (reducing powers, 2, 2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activities), ferric reduction activity potential (FRAP), total flavonoid concentration and antimicrobial activities of 80%, 90%, 100% methanol and chloroform extracts of V. officinalis Linn root and 90% and100% methanol leaf extracts were determined. Its antioxidant activity increases with increase in amount of extract (10% to 40%v/v). Total flavonoid content (TFC) varied from 73.32±0.002 mgQE/100g of dry weight (90% methanol) to 42.39±0.032 mgQE/100g dry weight (chloroform), 2,2-diphenyl-1-picrylhydrazyl (DPPH), radical scavenging activity (%) was varied between 87.39% (90% methanol) to 45.57% (chloroform) while Ferric reducing antioxidant power was observed between 372.93±0.04 mgAAE/100 g extract (90% methanol) to 129.41±0.026 mgAAE/100 g chloroform in the root extract. The methanolic extract of the leaf showed less antioxidant activity than the methanolic extract of the root. Crude extracts of V. officinalis root showed various degree of antimicrobial activity towards drug resistance microbial pathogens. Growth inhibition tests against bacterial pathogens demonstrated concentration dependence. Moreover, gram positive bacteria were more susceptible to V. officinalis root extract when compared to gram negative bacteria. In general V. officinalis root and leave extracts possess strong antioxidant and antimicrobial activities.

Biological Activities of Carlina Oxide Isolated from the Roots of Carthamus caeruleus

2020 ◽  
Vol 10 (2) ◽  
pp. 145-152 ◽  
Author(s):  
Imane Rihab Mami ◽  
Rania Belabbes ◽  
Mohammed El Amine Dib ◽  
Boufeldja Tabti ◽  
Jean Costa ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Essential Oil ◽  
Skin Diseases ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Penicillium Expansum ◽  
Natural Food ◽  
Antioxidant Power

Background: Carthamus caeruleus belongs to the Asteraceae family. The roots are traditionally used as healing agents. They help to heal burns and treat skin diseases. They are also used against joint inflammation and are very effective against diseases such as irritable bowel syndrome for cancer patients. Objectives: The purpose of this work was i) to study the chemical composition of i) the essential oil and hydrosol extract of Carthamus caeruleus, ii) to isolate the major component of both extracts and iii) to evaluate their antioxidant, antifungal and insecticidal activities. Methods: The essential oil and hydrosol extract obtained from the roots were studied by GC and GC/MS. The antioxidant activities were performed using two different methods i) Radical scavenging activity (DPPH) and ii) the Ferric-Reducing Antioxidant Power (FRAP), using BHT as a positive control. Whereas, the antifungal activity of the essential oil and Carlina oxide was investigated against plant fungi. The fumigation toxicity of C. caeruleus essential oil besides Carlina oxide was evaluated against adults of Bactrocera oleae better known as the olive fly. Results: The essential oil and hydrosol extract were mainly represented by acetylenic compounds such as carline oxide and 13-methoxy carline oxide. Carlina oxide was isolated and identified by 1H and 13C NMR spectroscopic means. The results showed that Carlina oxide presented interesting antioxidant and antifungal properties, while C. caeruleus root essential oil had better insecticidal activity. Furthermore, Carlina oxide has demonstrated promising in vivo antifungal activity to control infection of apples by Penicillium expansum. Conclusion: Carlina oxide can be used as a natural food preservative and alternative to chemical fungicides to protect stored apple against Penicillium expansum.

scholarly journals Comparison of Phenolic Contents and Scavenging Activities of Miang Extracts Derived from Filamentous and Non-Filamentous Fungi-Based Fermentation Processes

Antioxidants ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1144
Author(s):  
Aliyu Dantani Abdullahi ◽  
Pratthana Kodchasee ◽  
Kridsada Unban ◽  
Thanawat Pattananandecha ◽  
Chalermpong Saenjum ◽  
...  
Keyword(s):  
Filamentous Fungi ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Protective Effects ◽  
Tea Leaves ◽  
Antioxidant Power ◽  
Phenolic Contents ◽  
Ic50 Values ◽  
Ferric Reducing Antioxidant Power ◽  
The Impact

The study investigated the impact of the fermentation process on the phenolic contents and antioxidant and anti-inflammatory activities in extracts of Miang, an ethnic fermented tea product of northern Thailand. The acetone (80%) extraction of Miang samples fermented by a non-filamentous fungi-based process (NFP) and filamentous fungi-based process (FFP) had elevated levels of total polyphenols, total tannins, and condensed tannins compared to young and mature tea leaves. The antioxidant studies also showed better the half-maximal inhibitory concentration (IC50) values for fermented leaves in both 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging activity assays as well as improved ferric reducing antioxidant power (FRAP) compared to young and mature tea leaves. Extracts of NFP and FFP samples at concentrations of 50 and 100 ppm showed better protective effects against hydrogen peroxide (H2O2)-induced intracellular reactive oxygen species (ROS) production in HT-29 colorectal cells without exerting cytotoxicity. Additionally, lipopolysaccharide (LPS)-induced production of nitric oxide (a proinflammatory mediator as well as a reactive nitrogen species) was also inhibited by these fermented Miang extracts with an IC50 values of 17.15 μg/mL (NFP), 20.17 μg/mL (FFP), 33.96 μg/mL (young tea leaves), and 31.33 μg/mL (mature tea leaves). Therefore, both NFP-Miang and FFP-Miang showed the potential to be targeted as natural bioactive functional ingredients with preventive properties against free radical and inflammatory-mediated diseases.

scholarly journals Optimization of Lutein Recovery from Tetraselmis suecica by Response Surface Methodology

Biomolecules ◽  
2021 ◽  
Vol 11 (2) ◽  
pp. 182
Author(s):  
Kang Hyun Lee ◽  
Ye Won Jang ◽  
Hansol Kim ◽  
Jang-Seu Ki ◽  
Hah Young Yoo
Keyword(s):  
Response Surface Methodology ◽  
Response Surface ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
High Energy ◽  
Solid Loading ◽  
Control Group ◽  
Energy Yield ◽  
Tetraselmis Suecica ◽  
Antioxidant Power

Microalgae have been attracting attention as feedstock for biorefinery because they have various advantages, such as carbon fixation, high growth rate and high energy yield. The bioactive compounds and lutein contained in microalgae are known to be beneficial for human health, especially eye and brain health. In this study, in order to improve the recovery of bioactive extracts including lutein from Tetraselmis suecica with higher efficiency, an effective solvent was selected, and the extraction parameters such as temperature, time and solid loading were optimized by response surface methodology. The most effective solvent for lutein recovery was identified as 100% methanol, and the optimum condition was determined (42.4 °C, 4.0 h and 125 g/L biomass loading) by calculation of the multiple regression model. The maximum content of recovered lutein was found to be 2.79 mg/mL, and the ABTS radical scavenging activity (IC50) and ferric reducing antioxidant power (FRAP) value were about 3.36 mg/mL and 561.9 μmol/L, respectively. Finally, the maximum lutein recovery from T. suecica through statistical optimization was estimated to be 22.3 mg/g biomass, which was 3.1-fold improved compared to the control group.

scholarly journals Inhibitory Effect of Antidesma bunius Fruit Extract on Carbohydrate Digestive Enzymes Activity and Protein Glycation In Vitro

Antioxidants ◽  
2020 ◽  
Vol 10 (1) ◽  
pp. 32
Author(s):  
Pattamaporn Aksornchu ◽  
Netima Chamnansilpa ◽  
Sirichai Adisakwattana ◽  
Thavaree Thilavech ◽  
Charoonsri Choosak ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Radical Scavenging Activity ◽  
Digestive Enzyme ◽  
Radical Scavenging ◽  
Protein Glycation ◽  
Trolox Equivalent Antioxidant Capacity ◽  
Fruit Extract ◽  
Antioxidant Power ◽  
Ic50 Values

Antidesma bunius (L.) spreng (Mamao) is widely distributed in Northeastern Thailand. Antidesma bunius has been reported to contain anthocyanins, which possess antioxidant and antihypertensive actions. However, the antidiabetic and antiglycation activity of Antidesma bunius fruit extract has not yet been reported. In this study, we investigated the inhibitory activity of anthocyanin-enriched fraction of Antidesma bunius fruit extract (ABE) against pancreatic α-amylase, intestinal α-glucosidase (maltase and sucrase), protein glycation, as well as antioxidant activity. A liquid chromatography-tandem mass spectrometry (LC-MS/MS) chromatogram revealed that ABE contained phytochemical compounds such as cyanidin-3-glucoside, delphinidin-3-glucoside, ellagic acid, and myricetin-3-galactoside. ABE inhibited intestinal maltase and sucrase activity with the IC50 values of 0.76 ± 0.02 mg/mL and 1.33 ± 0.03 mg/mL, respectively. Furthermore, ABE (0.25 mg/mL) reduced the formation of fluorescent AGEs and the level of Nε-carboxymethyllysine (Nε-CML) in fructose and glucose-induced protein glycation during four weeks of incubation. During the glycation process, the protein carbonyl and β-amyloid cross structure were decreased by ABE (0.25 mg/mL). In addition, ABE exhibited antioxidant activity through DPPH radical scavenging activity and Trolox equivalent antioxidant capacity (TEAC) with the IC50 values 15.84 ± 0.06 µg/mL and 166.1 ± 2.40 µg/mL, respectively. Meanwhile, ferric reducing antioxidant power (FRAP) showed an EC50 value of 182.22 ± 0.64 µg/mL. The findings suggest that ABE may be a promising agent for inhibiting carbohydrate digestive enzyme activity, reducing monosaccharide-induced protein glycation, and antioxidant activity.

scholarly journals Changes in Amino Acid Profiles and Bioactive Compounds of Thai Silk Cocoons as Affected by Water Extraction

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 2033
Author(s):  
Chuleeporn Bungthong ◽  
Sirithon Siriamornpun
Keyword(s):  
Amino Acids ◽  
Amino Acid ◽  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Silk Protein ◽  
Extraction Time ◽  
Antioxidant Power ◽  
Silk Cocoon ◽  
Amino Acid Profiles

Silk proteins have many advantageous components including proteins and pigments. The proteins—sericin and fibroin—have been widely studied for medical applications due to their good physiochemical properties and biological activities. Various strains of cocoon display different compositions such as amino-acid profiles and levels of antioxidant activity. Therefore, the objectives of this study were to find a suitable silk protein extraction method to obtain products with chemical and biological properties suitable as functional foods in two strains of Bombyx mori silk cocoon (Nangsew strains; yellow cocoon) and Samia ricini silk cocoon (Eri strains; white cocoon) extracted by water at 100 °C for 2, 4, 6 and 8 h. The results showed that Nangsew strains extracted for 6 h contained the highest amounts of protein, amino acids, total phenolics (TPC) and total flavonoids (TFC), plus DPPH radical-scavenging activity, ABTS radical scavenging capacity, and ferric reducing antioxidant power (FRAP), anti-glycation, α-amylase and α-glucosidase inhibition. The longer extraction time produced higher concentrations of amino acids, contributing to sweet and umami tastes in both silk strains. It seemed that the bitterness decreased as the extraction time increased, resulting in improvements in the sweetness and umami of silk-protein extracts.

scholarly journals Grape Canes from Typical Cultivars of Campania (Southern Italy) as a Source of High-Value Bioactive Compounds: Phenolic Profile, Antioxidant and Antimicrobial Activities

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2746
Author(s):  
Giuseppe Squillaci ◽  
Carla Zannella ◽  
Virginia Carbone ◽  
Paola Minasi ◽  
Veronica Folliero ◽  
...  
Keyword(s):  
Southern Italy ◽  
Radical Scavenging Activity ◽  
Antiviral Agents ◽  
Radical Scavenging ◽  
Antimicrobial Activities ◽  
Total Phenolic ◽  
Antioxidant Power ◽  
Herpes Simplex Viruses ◽  
Ferric Reducing Antioxidant Power ◽  
Antioxidant And Antimicrobial Activities

The purpose of the current study was to determine the phenolic composition, antioxidant, and antimicrobial activities in grape cane extracts from typical cultivars of Southern Italy. Aqueous extracts at different pHs (1–13) were prepared from “Aglianico”, “Fiano”, and “Greco” grape canes. The results demonstrated that an alkaline pH (13.00) produced the best polyphenol-rich extracts, as the total phenolic content was more than double when compared to the respective extracts prepared at pH 1.00. “Greco” grape canes gave the highest quantity of phenolic compounds at each pH, ranging from 42.7 ± 0.4 to 104.3 ± 3.0 mg Gallic Acid Equivalents (GAE)/g Dry Extract (DE) from pH 1.00 to 13.00. The Radical Scavenging Activity (RSA) and the Ferric Reducing Antioxidant Power (FRAP) were measured. The highest antioxidant activity was showed by “Greco” extract at pH 7.00. Seventy-five compounds were identified in the extracts by HPLC-MS with six of them described for the first time in grape canes. Procyanidins were highly abundant in extracts at pH 7.00, whereas stilbenoids were the most represented compounds at pH 13.00. Very strong antiviral activity against herpes simplex viruses was recorded for the extracts at pH 7.00 and 13.00 that were active in the early stages of infection by acting directly against the viral particles. The overall results suggest that grape canes, currently underutilized, can be usefully valorised by providing active extracts to use as antioxidant and antiviral agents.

scholarly journals Composition, antimicrobial and antioxidant activity of the extracts of Eryngium palmatum Pančić and Vis. (Apiaceae)

2014 ◽  
Vol 9 (2) ◽  
pp. 149-155 ◽  
Author(s):  
Mirjana Marčetić ◽  
Silvana Petrović ◽  
Marina Milenković ◽  
Marjan Niketić
Keyword(s):  
Antioxidant Activity ◽  
Methanol Extract ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Chloroform Extract ◽  
Volatile Fraction ◽  
Scavenging Activity ◽  
Antioxidant Power ◽  
Aerial Parts ◽  
Antimicrobial And Antioxidant Activity

AbstractThe chemical composition, antimicrobial and antioxidant activity of Eryngium palmatum, an endemic plant species from the Balkan Peninsula, were investigated. The flavonoids apigenin (9.5±0.3 mg g−1) and apigenin 7-O-glucoside (2.4±0.1 mg g−1) were determined in a methanol extract of aerial parts using HPLC analysis. The methanol extract of roots contained catechin (5.0±0.1 mg g−1), epicatechin (2.9±0.1 mg g−1), chlorogenic acid (1.6±0.0 mg g−1), gallic acid (0.9±0.0 mg g−1) and rosmarinic acid (0.9±0.2 mg g−1). GC-FID and GCMS analysis of a chloroform extract of aerial parts showed that the main volatile constituents were falcarinol, linoleic acid, hexadecanoic acid and methyl linoleate (comprising 32.6%; 24.4%; 19.9; 13.2% of the volatile fraction, respectively), while octanoic acid, tetradecanol and dodecanol dominated in the chloroform extract of the roots (34.9%; 25.8%; 22.2% of the volatile fraction, respectively). Investigation of antimicrobial activity by broth microdilution showed that the methanol and chloroform extracts of aerial parts and roots exerted a significant effect (MIC 3.5–15.6 μg mL−1) against tested Gram-positive and Gram-negative bacteria. The methanol extracts of aerial parts or roots exerted moderate ferric reducing antioxidant power, DPPH radical scavenging activity and hydroxyl radical scavenging activity.

Synthesis and Biological Activities of Hydroxytyrosol Ester Derivatives

2020 ◽  
Vol 42 (1) ◽  
pp. 109-109
Author(s):  
Hao Zang Hao Zang ◽  
Qian Xu Qian Xu ◽  
Luyun Zhang Luyun Zhang ◽  
Guangqing Xia Guangqing Xia ◽  
Jiaming Sun and Junyi Zhu Jiaming Sun and Junyi Zhu
Keyword(s):  
Ascorbic Acid ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Acetylcholinesterase Inhibition ◽  
Hydroxyl Group ◽  
Scavenging Activity ◽  
Antioxidant Power ◽  
Better Than

A series of hydroxytyrosol (HT) derivatives were synthesized by modification of alcohol hydroxyl group of HT, twenty-five target compounds were obtained and characterized by NMR and HRMS. The antioxidant activities of those compounds were evaluated in three different assays. Except 3e and 3y, all other compounds demonstrated significant 2,2and#39;-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) free radical cation scavenging activity ranging from IC50 3.4 to 24.4 μM, which were more potent than L-ascorbic acid (IC50=24.8 μM). Compounds 3b-3d, 3f-3k, 3m-3x were better than Trolox (18.3 M). Moreover, the ferric reducing antioxidant power (FRAP) of all compounds were discovered to be more potent than L-ascorbic acid (40.7 mmol/g), except 3e, all other compounds (141.5-202.1 mmol/g) were better than Trolox (94.7 mmol/g). Compounds 3a-3d, 3f-3j, 3l-3m, 3o, 3q, 3t, 3v-3y exhibited more potent hydroxyl radical scavenging activity (IC50=245.1-475.1 M) than L-ascorbic acid (554.4 M) and Trolox (500.4 M). Compounds 3q, 3t and 3y exhibited more potent -Glucosidase inhibition activity (39.1-52.4 M) than Acarbose (60.9 M). Compounds 3a, 3d, 3f-3m, 3s-3t, 3v-3y showed some acetylcholinesterase inhibition activities, compounds 3a, 3d, 3f-3j, 3l-3m, 3o-3p, 3s-3t, 3w showed some butyrylcholinesterase inhibition activities.

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