scholarly journals Novel N,N′-Disubstituted Acylselenoureas as Potential Antioxidant and Cytotoxic Agents

Antioxidants ◽  
2020 ◽  
Vol 9 (1) ◽  
pp. 55 ◽  
Author(s):  
Ana Carolina Ruberte ◽  
Sandra Ramos-Inza ◽  
Carlos Aydillo ◽  
Irene Talavera ◽  
Ignacio Encío ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Radical Scavenging Activity ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Cytotoxic Agents ◽  
Cytotoxic Activities ◽  
Protective Effects ◽  
Selenium Compounds ◽  
Ic50 Values

Selenium compounds are pivotal in medicinal chemistry for their antitumoral and antioxidant properties. Forty seven acylselenoureas have been designed and synthesized following a fragment-based approach. Different scaffolds, including carbo- and hetero-cycles, along with mono- and bi-cyclic moieties, have been linked to the selenium containing skeleton. The dose- and time-dependent radical scavenging activity for all of the compounds were assessed using the in vitro 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) assays. Some of them showed a greater radical scavenging capacity at low doses and shorter times than ascorbic acid. Therefore, four compounds were evaluated to test their protective effects against H2O2-induced oxidative stress. One derivative protected cells against H2O2-induced damage, increasing cell survival by up to 3.6-fold. Additionally, in vitro cytotoxic activity of all compounds was screened against several cancer cells. Eight compounds were selected to determine their half maximal inhibitory concentration (IC50) values towards breast and lung cancer cells, along with their selectivity indexes. The breast cancer cells turned out to be much more sensitive than the lung. Two compounds (5d and 10a) stood out with IC50 values between 4.2 μM and 8.0 μM towards MCF-7 and T47D cells, with selectivity indexes greater than 22.9. In addition, compound 10b exhibited dual antioxidant and cytotoxic activities. Although further evidence is needed, the acylselenourea scaffold could be a feasible frame to develop new dual agents.

scholarly journals Antibacterial, antioxidant and cytotoxic activities of different fractions of acetone extract from flowers of Dipterocarpus intricatus Dyer (Dipterocarpaceae)

2021 ◽  
Vol 8 (2) ◽  
pp. 273-277
Author(s):  
Hong Thia Le ◽  
Thao Nguyen Luu ◽  
Huynh Mai Thu Nguyen ◽  
Dang HoaiTrang Nguyen ◽  
Pham Tan Quoc Le ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Salmonella Enteritidis ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Acetone Extract ◽  
Cytotoxic Agents ◽  
Diffusion Method ◽  
Cytotoxic Activities ◽  
Ic50 Values ◽  
First Time

This study has shown for the first time the antimicrobial, antioxidant and cytotoxicity of 3 fractions of acetone extract, including hexane, chloroform and ethyl acetate from flowers of Dipterocarpus intricatus. Antibacterial test using disc diffusion method showed that the chloroform and ethyl acetate fractions inhibited the growth of all the tested bacteria, including Escherichia coli, Pseudomonas aeruginosa, Salmonella enteritidis, Salmonella typhimurium, Bacillus cereus and Staphylococcus aureus while the hexane fraction showed the antibacterial activity against B. cereus and S. enteritidis. Antioxidant activity and cancer cell resistance of those extracts were conducted using DPPH and MTT methods respectively. As a result, the DPPH radical scavenging activity of the hexane, chloroform and ethyl acetate fractions were determined with the IC50 values of 0.508, 0.22 and 0.075 mg/mL respectively while the cytotoxicity to HepG2 cell line of those fractions was 163.3 ppm, 106.7 ppm and 459.3 ppm. These results suggested the potential application of these fractions isolated from D. intricatus flowers as the natural antimicrobial, antioxidant and cytotoxic agents for medicine.

scholarly journals Characterization of Novel Synthetic Polyphenols: Validation of Antioxidant and Vasculoprotective Activities

Antioxidants ◽  
2020 ◽  
Vol 9 (9) ◽  
pp. 787 ◽  
Author(s):  
María Jesús Pérez de Vega ◽  
Silvia Moreno-Fernández ◽  
Gloria María Pontes-Quero ◽  
María González-Amor ◽  
Blanca Vázquez-Lasa ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Radical Scavenging Activity ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Antioxidant Compounds ◽  
Therapeutic Effects ◽  
Protective Effects ◽  
Therapeutic Benefits ◽  
Anti Inflammatory

Antioxidant compounds, including polyphenols, have therapeutic effects because of their anti-inflammatory, antihypertensive, antithrombotic and antiproliferative properties. They play important roles in protecting the cardiovascular and neurological systems, by having preventive or protective effects against free radicals produced by either normal or pathological metabolism in such systems. For instance, resveratrol, a well-known potent antioxidant, has a counteracting effect on the excess of reactive oxygen species (ROS) and has a number of therapeutic benefits, like anti-inflammatory, anti-cancer and cardioprotective activities. Based on previous work from our group, and on the most frequent OH substitutions of natural polyphenols, we designed two series of synthetically accessible bis-polyhydroxyphenyl derivatives, separated by amide or urea linkers. These compounds exhibit high antioxidant ability (oxygen radical absorbance capacity (ORAC) assay) and interesting radical scavenging activity (RSA) values (2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and α,α-diphenyl-β-picrylhydrazyl (DPPH) tests). Some of the best polyphenols were evaluated in two biological systems, endothelial cells (in vitro) and whole aorta (ex vivo), highly susceptible for the deleterious effects of prooxidants under different inflammatory conditions, showing protection against oxidative stress induced by inflammatory stimuli relevant in cardiovascular diseases, i.e., Angiotensin II and IL-1β. Selected compounds also showed strong in vivo antioxidant properties when evaluated in the model organism Saccharomyces cerevisiae.

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 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.

Strong antihemolytic and antioxidant properties of aqueous extract from Algerian Hammada elegans (Bge.) Botsch (Chenopodiaceae)

2021 ◽  
Vol 17 ◽  
Author(s):  
Brahim Asseli ◽  
Reguia Mahfoudi ◽  
Amar Djeridane ◽  
Mohamed Yousfi
Keyword(s):  
Free Radical ◽  
Aqueous Extract ◽  
Radical Scavenging Activity ◽  
Condensed Tannin ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Total Phenolic ◽  
Dependent Manner ◽  
Vitro Assay

Background: Research on medicinal plant antioxidants has emerged as a potential therapeutic to prevent free radical generated damage in the human body. Hammada elegans Botsch (popularly known as “Ajram”) is a xerophytic plant widely found in Laghouat region, but there are only a few reports about the biological or chemical properties of these species. Hence, the aim of this study is to investigate the antioxidant and the antihemolytic activities of hexanic, acetonic, methanolic and aqueous extracts of aerial parts of Algerian Hammada elegans Botsch by employing different in vitro assay systems. Methods: The total phenolic content, the flavonoid content and the condensed tannin amount were analyzed using Folin-Ciocalteu, aluminum chloride and vanillin assays, respectively. The in vitro antioxidant capacity of extracts was assessed by CUPRAC, iron chelating, ABTS•+and antihemolytic assays, and was expressed as EC50 values. Results: Among the analyzed extracts, the aqueous extract had the highest phenolic, flavonoid and tannin contents. Also, this extract displayed the highest antioxidant capacities compared to the other extracts and standards. Its EC50 value for ABTS radical-scavenging activity was 0.265 ± 0.003 mg/L. Moreover, this extract showed high iron (II) chelating ability (EC50 = 0.958 ± 0.001 mg/L), and good antioxidant activity in the cupric ion reducing activity (CUPRAC) in a concentration dependent manner (EC50 were 0.709 ± 0.002 mg/L). Additionally, this extract had the best antihemolytic activity against AAPH-induced hemolysis (EC50=0.090 ± 0.004 mg/L). Conclusion: Our study revealed that the aqueous extract of Hammada elegans Botsch, is a potential source of antioxidants which possess a high protective effect of membrane against free radical.

Synthesis and Evaluation of bis-Schiff Bases of Carbohydrazide as Antioxidant and Cytotoxic Agents

2021 ◽  
Vol 18 ◽  
Author(s):  
Sarosh Iqbal ◽  
Shumaila Kiran ◽  
Shahida Perveen ◽  
Rizwana Malik ◽  
Muhammad Taha ◽  
...  
Keyword(s):  
Schiff Bases ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Cytotoxic Agents ◽  
Scavenging Activity ◽  
Standard Drug ◽  
Age Related ◽  
Dpph Radical Scavenging ◽  
Better Than

Background & Introduction : Antioxidants are known to prevent oxidative stress-induced damage to the biomolecules and thus, delay the onset of cancers and many age-related diseases. Therefore, the development of novel and potent antioxidants is justified. Method: During this study, we synthesized symmetrical bis-Schiff bases of carbohydrazide 1-27, and evaluated their in vitro antioxidative activity and cytotoxic activity. Results: Among synthesized compounds, six compounds 20 (IC50 = 12.89 ± 0.02 µM), 16 (IC50 = 14.32 ± 0.43 µM), 17 (IC50 = 18.52 ± 0.83 µM), 19 (IC50 = 22.84 ± 0.62 µM), 24 (IC50 = 35.1 ± 0.82 µM) and 15 (IC50 = 40.03 ± 1.06 µM) showed an excellent 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, better than the standard butylatedhydroxyanisole (BHA) (IC50 = 44.6 ± 0.6 µM). Likewise, two compounds 16 (IC50 = 4.3 ± 1.3 µM) and 20 (IC50 = 6.6 ± 1.6 µM) showed oxidative burst scavenging activity better than the standard drug ibuprofen (IC50 = 11.2 ± 1.9 µM). Some synthesized compounds showed good to moderate toxicity against prostate cancer (PC-3) cell lines. Conclusion: This study has identified potent antioxidants and good cytotoxic agents with the potential to further investigate.

scholarly journals Phytochemical Screening and in vitro Antioxidant Properties of Methanol and Aqueous Leaf Extracts of Geophila obvallata

2018 ◽  
pp. 1-11
Author(s):  
Iserhienrhien Lucky Osafanme ◽  
Okolie Paulinus Ngozi
Keyword(s):  
Aqueous Extract ◽  
Methanol Extract ◽  
Radical Scavenging Activity ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Scientific Basis ◽  
Phytochemical Analysis ◽  
Leaf Extracts ◽  
Reducing Ability

Aim: This study investigated the phytochemical constituents and in vitro antioxidant properties of methanol and aqueous leaf extracts of Geophila obvallata using standard methods. Materials and Methods: The in vitro antioxidant assays carried out were 1, 1‐diphenyl‐2‐picrylhydrazyl (DPPH) radical scavenging ability, Nitric oxide (NO•) radical scavenging activity assay, 2, 2'-azino-bis (3-ethylbenzthiazoline-6-sulphonic acid) (ABTS•+) radical cation scavenging assay, ferric reducing properties and hydroxyl radical scavenging assays. Results: Phytochemical analysis revealed the presence of alkaloids, flavonoids, phenolic compounds, steroids, saponins, terpernoids and cardiac glycosides in both extracts. Relative to the aqueous extract, the methanol extract contained a higher amount of the secondary metabolites. However, both extracts exhibited appreciable and dose-dependent capacities for quenching DPPH, ABTS•+ and NO• free radicals, and potent ferric reducing ability to levels comparable to those of ascorbic acid. The crude methanol extract showed significantly increased (P<0.05) antioxidant activity than the aqueous extract. Conclusion: It was concluded that the extract possesses strong antioxidant properties due to its content of phytochemicals, and provides scientific basis for its ethno medicinal applications.

scholarly journals Antioxidant, Cytotoxic Activities and Total Phenolic Content of Four Indonesian Medicinal Plants

2012 ◽  
Vol 2 (4) ◽  
Author(s):  
Waras Nurcholis ◽  
Bambang Pontjo Priosoeryanto ◽  
Edy Djauhari Purwakusumah ◽  
Takeshi Katayama ◽  
Toshisada Suzuki
Keyword(s):  
Free Radical ◽  
Medicinal Plants ◽  
Total Phenolic Content ◽  
Phenolic Content ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Total Phenolic ◽  
Cytotoxic Activities ◽  
Ic50 Values ◽  
Ethanol Extracts

The crude ethanol extracts of four Indonesian medicinal plants namely Curcuma xanthorrhiza Roxb.,Phyllanthus niruri Linn., Andrographis paniculata Ness., and Curcuma aeruginosa Roxb. wereexamined for their antioxidant (radical scavenging) activity using 2, 2-diphenyl-2-picrylhydrazyl(DPPH) free radical and cytotoxicity using brine shrimp lethality test (BSLT). The total phenoliccontent was used the Folin-Ciocalteu method. IC50 values for DPPH radical scavenging activityranged from 14.5 to 178.5 μg/ml, with P. niruri having the lowest value and therefore the mostpotent, and C. aeruginosa having the highest value. LC50 values for BSLT ranged from 210.3 to593.2 μg/ml, with C. xanthorrhiza and A. paniculata having the lowest and highest values,respectively. The total phenolic content of the Indonesian plants ranged from 133.0 ±3.7 to863.3±54.7 mg tannic acid equivalent per 1 g extract, with C. aeruginosa and P. niruri having thelowest and highest values, respectively. A positive correlation between free radical scavengingactivity and the content of phenolic compounds was found in the four of Indonesian medicinal plants.

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.

In vitro antioxidant activity and phytochemical analyses of Acalypha godseffiana (Euphobiaceae) leaf extracts

2021 ◽  
Vol 25 (1) ◽  
pp. 75-79
Author(s):  
S.O. Olubodun ◽  
G.E. Eriyamremu ◽  
M.E. Ayevbuomwan ◽  
C.I. Nzoputa
Keyword(s):  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Antioxidant Vitamin ◽  
Phytochemical Analysis ◽  
Leaf Extracts ◽  
Anti Oxidant ◽  
In Vitro Antioxidant Activity

The presence of various bioactive components makes it necessary to analyse plants for their potential to act as a source of useful treatments and cures for many inflammatory, infectious and pathogenic diseases. This study was carried out to determine phytochemicals and in-vitro antioxidant activities of the leaf extracts of Acalypha godseffiana. The leaves of A. godseffiana were collected, dried, pulverized and extracted separately with methanol and water using maceration method. The extract was concentrated in vacuo with rotary evaporator at 40oC. The extracts were subjected to quantitative phytochemical analysis and different anti-oxidant analytical procedures like FRAP, DPPH etc to determine the radical scavenging capabilities. The results of phytochemical analysis estimated the quantities and revealed the presence of alkaloids, flavonoids, tannins, saponins and terpenoids which varied in both extracts. The methanol and aqueous extracts exhibited antioxidant activities with relatively high IC50 (IC50 = 3.67 ìg/ml and 4.42ìg/ml respectively) which accounted for a low free radical-scavenging activity when compared with the reference antioxidant, vitamin C (IC50 = 1.51ìg/ml). The results of the study indicates that A. godseffiana leaf extracts contain secondary metabolites and possesses antioxidant properties.

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