In-vitro Antioxidant and Cytotoxicity Studies of <i>Annona squamosa</i> Linn.

n-Hexane, chloroform and methanol soluble extracts of the leaves of Annona squamosa were screened fortheir possible antioxidant activitiy by DPPH free radical scavenging and cytotoxicity by brine shrimp lethalitybioassay. In DPPH radical scavenging assay, methanol soluble extract was found to be the most potent withan IC50 value of 103.5 μg/ml. The amount of total phenolics was also found to the highest in the methanolsoluble extract (283.16 ± 8.90 mg/g), followed by chloroform soluble extract (216.90 ± 4.48 mg/g). Here BHTand ascorbic acid were used as standards with IC50 values 8.2 μg/ml and 25 μg/ml respectively. In the brineshrimp lethality bioassay, the most significant cytotoxicity was observed with chloroform soluble extract withan LC50 of 4.16 μg/ml where vincristine sulphate was used as standard (LC50 0.29 μg/ml).Key Words: Annona squamosa; DPPH; Folin-Ciocalteu Reagent; Phenolic Contents; Brine ShrimpDOI: 10.3329/sjps.v2i1.5813Stamford Journal of Pharmaceutical Sciences Vol.2(1) 2009: 32-36

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

Antioxidants ◽

10.3390/antiox10071144 ◽

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.

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Survey of Phenolic Acids, Flavonoids and In Vitro Antioxidant Potency Between Fig Peels and Pulps: Chemical and Chemometric Approach

Molecules ◽

10.3390/molecules26092574 ◽

2021 ◽

Vol 26 (9) ◽

pp. 2574

Author(s):

Lahcen Hssaini ◽

Francisca Hernandez ◽

Manuel Viuda-Martos ◽

Jamal Charafi ◽

Rachid Razouk ◽

...

Keyword(s):

Phenolic Acids ◽

Radical Scavenging ◽

Fruit Peel ◽

Mean Values ◽

Local Cultivar ◽

Ic50 Values ◽

The Mean ◽

Lipid Peroxidation Inhibition ◽

Almost All

In the present study, chromatic coordinates, phenolic acids, flavonoids and antioxidant capacity assessed by 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonate (ABTS) and lipid peroxidation inhibition capacity (LPIC) essays and their relative IC50 were investigated in 25 fig cultivars growing in Morocco. The aims of this study were to determine (i) the variation in these compounds among light and dark-colored cultivars, (ii) their partitioning between fruit peel and pulp and (iii) to display network connections among these variables. Twelve phenolic compounds (PCs) were isolated in peel extract versus eight in pulp samples. Anthocyanins, mainly cyanidin-3,5-diglucoside and cyanidin-3-O-rutinoside, were the predominant compounds in peels, where the mean concentrations were 75.90 ± 18.76 and 77.97 ± 18.95 µg/g dw, respectively. On the other hand, (−)-epicatechin and cyanidin-3-O-rutinoside were the major compounds in the pulp extracts, where the mean values were 5.23 ± 4.03 and 9.01 ± 5.67 µg/g dw, respectively. A two-dimensional hierarchically clustered heatmap was applied to the dataset to explore correlations in the dataset and similarities between cultivars, without dimensionality reduction. Results showed that anthocyanins, particularly pelargonidin-3-O-rutinoside, cyanidin-3,5-diglucoside and cyanidin-3-O-rutinoside, were the main contributors to the peels’ free radical scavenging capacity. This capacity was particularly higher in the peel of dark-colored figs compared to the fruit pulp. The local cultivar “INRA 1301” showed the most promising phenolic profile due to its very high levels of almost all detected PCs, especially (−)-epicatechin, quercetin-3-O-rutinoside, quercetin-3-O-glucoside, cyanidine-3,5-diglucoside, cyanidine-3-O-rutinoside and pelargonidin-3-O-rutinoside (54.66, 141.08, 35.48, 494.08, 478.66, 12.56 µg/g dw, respectively). Having the darkest figs in the collection (L* = 25.72, c* = 22.09 and h° = 20.99), this cultivar has also combined promising IC50 values, which were of 19.85, 40.58 and 124.78 µg/mL for DPPH, ABTS and LPIC essays, respectively.

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

Antioxidants ◽

10.3390/antiox10010032 ◽

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.

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Synthesis and Antioxidant Properties of Novel 2-(2,4-Dioxothiazolidin-5-ylidene)-Acetamides Containing 1,3,4-Thia/Oxadiazole Moieties

Biointerface Research in Applied Chemistry ◽

10.33263/briac125.67106722 ◽

2021 ◽

Vol 12 (5) ◽

pp. 6710-6722

Keyword(s):

Ascorbic Acid ◽

Acetyl Chloride ◽

Antioxidant Properties ◽

Radical Scavenging ◽

Scavenging Effect ◽

Highly Active ◽

Ethanol Medium ◽

Ic50 Value ◽

Radical Scavenging Ability

A series of novel 1,3,4-thia(oxa)diazole substituted 2-(2,4-dioxothiazolidine-5-ylidene)-acetamides 3a-c, 4 and 5a-k have been synthesized following the acylation reaction of 2-amino-5-aryl-1,3,4-oxadiazoles, 5-amino-1,3,4-thiadiazole-2-thiol and it’s S-alkylated derivatives with 2-(2,4-dioxothiazolidine-5-ylidene)acetyl chloride in dioxane medium. The functionalization of compounds 3b, 3c, 5d and 5e was carried out on their N3 position under N-alkylation conditions with N-aryl-2-chloroacetamides in DMF/ethanol medium yielded the corresponding 2,4-dioxothiazolidine-3,5-diacetic acid diamides 6a-e and 7a-b. The structures of target compounds were confirmed by using 1H NMR spectroscopy and elemental analysis. The antioxidant activity evaluation in vitro of the synthesized compounds was performed by the method of scavenging effect on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals. As a result, the highly active compound 4, namely 2-(2,4-dioxothiazolidin-5-ylidene)-N-(5-mercapto-[1,3,4]thiadiazol-2-yl)acetamide was found to be the most efficient candidate among all compounds with a radical scavenging ability of 88.9%, which was comparable that for ascorbic acid (92.7%). The experimentally calculated IC50 value of 43.1 µM for compound 4 was lower than for ascorbic acid (50.5 µM).

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Functional Effects of Pomegranate Peel Extracts on Milk: Antibacterial Measurements, Antioxidant Activities, and Photochemical Characterizations

Journal of Biobased Materials and Bioenergy ◽

10.1166/jbmb.2021.2097 ◽

2021 ◽

Vol 15 (5) ◽

pp. 571-579

Author(s):

Rokayya Sami ◽

Ebtihal Khojah ◽

Mona Alharbi ◽

Amina A. M. Al-Mushhin ◽

Mohammed Saeed Alkaltham ◽

...

Keyword(s):

Antioxidant Activities ◽

Radical Scavenging ◽

Water Extract ◽

Ethanol Extract ◽

Inhibition Zone ◽

Pomegranate Peel ◽

Bacteria Growth ◽

Wonderful Variety ◽

Ic50 Values

Consumers are interested in antimicrobial by-products from natural sources. The present study aims to estimate the antibacterial effects of different concentrations and solvent extracts such as methanol, ethanol, and water extract of pomegranate peels with the milk quality application in-vitro. Listeria monocytogens, E. coli, Salmonella, and Staphylococcus aureus were used as bacteria growth indicators in two pomegranate varieties (i.e., Wonderful and Francis). Besides, evaluating somephysical characterization, antibacterial and antioxidant activities. Results showed that the highest inhibition zone of 18.88 mm was observed with 90% ethanol extract of Wonderful variety against Listeria monocytogens, at 0, 12.5, 25, and 50 mg/mL concentrations, while the lowest inhibition zone of 11.29 mm was observed with 90% methanol extract of Francis variety, at 12.5 mg/mL concentration. The milk treated with WPE of Wonderful variety maintained the bacterial growth from 1.19 ±0.29 x 109 to 1.43 x 1011 CFU/mL at 4 °C. Punicalagin was the most abundant polyphenolic compound (165.05–190.43 µg/mL) followed by gallic acid (153.08–177.65 µg/mL), and p-Hydroxybenzoic acid (91.29–92.5 mg/mL). Acetaldehyde (23.09–27.15 PPM), followed by acetoin (9.65–15.33 PPM) were the most predominant volatile compounds. The WPE treated milk maintained the sensory evaluations such as taste, color, texture, and overall acceptance longer time longer time (i.e., 144 h) than FPE treated milk (i.e., 168 h) at 4°C. DPPH and ABTS radical scavenging of capacity (IC50 values) of FPE treated milk were found to be lower than WPE treated milk (i.e., 159.65 µg/mL and 131.87 µg/mL), respectively. While, FPE treated milk reported a higher viscosity content than WPE treated milk (13.11 cP). In conclusion, pomegranate peel extracts especially Wonderful variety may be used to prolong the shelf-life of milk in dairy products manufacturers.

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IN-SILICO AND IN VITRO ASSESSMENT OF SYNTHESIZED DIAZENYLSULFONAMIDES AS APOPTOSIS INDUCERS AND RADICAL SCAVENGERS

INDIAN DRUGS ◽

10.53879/id.57.06.12458 ◽

2020 ◽

Vol 57 (06) ◽

pp. 49-59

Author(s):

Priyambada Kshiroda Nandini Sarangi ◽

Jyotirmaya Sahoo ◽

Chita Ranjan Sahoo ◽

Sudhir Kumar Paidesetty ◽

Guru Prasad Mohanta

Keyword(s):

Cell Line ◽

Cancer Cell ◽

Radical Scavenging ◽

Cancer Cell Line ◽

Scavenging Effect ◽

Ic50 Values ◽

Radical Scavenging Effect ◽

The Individual ◽

Mcf 7

A series of eight quinoline-thiazole hybrid-bearing diazenylsulfonamides, 4a-4h, were synthesized and characterized by UV-Vis, FT/IR, 1H NMR and lC-MS. These compounds were formed when two prepared intermediate precursors of Schiff-base compounds, (E)-N-((2-chloroquinolin-3-yl)methylene)-4phenylthiazol-2-amine (3a) and (E)-N-((2-chloroquinolin-3-yl)methylene)-4-chlorophenylthiazol-2-amine (3b) were converted to the corresponding diazenyl compounds 4a-4h by treating and coupling with the individual diazonium salts of sulfa-drugs. The results of in vitro cytotoxic activity of the synthesized compounds in two cancer cell lines MCF 7 (human breast cancer cell line) and K562 (myelogenousleukemia cell line) have shown the IC50 values as given: 4b against MCF 7 19.52 and against K562 20.55µM; 4d against MCF 7 15.96 and against K562 13.05µM. Moreover, the compound 4-(((Z)-(2-chloroquinolin-3yl)(4-phenylthiazol-2-ylimino)methyl)diazenyl)benzenesulfonic acid (4d) induced maximum percentage of apoptosis. Furthermore, the in vitro antioxidant activity study revealed that among all the synthesized compounds, compound 4d has an excellent radical scavenging effect. Molecular docking was additionally performed to investigate the binding affinity of H-bonding interaction of synthesized compounds with a targeted enzyme and to compare it with the anticancer drugs, dasatinib, bosutinib and dacarbazine.

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Structurally Simple Phenanthridine Analogues Based on Nitidine and Their Antitumor Activities

Molecules ◽

10.3390/molecules24030437 ◽

2019 ◽

Vol 24 (3) ◽

pp. 437

Author(s):

Shu-Qin Qin ◽

Lian-Chun Li ◽

Jing-Ru Song ◽

Hai-Yun Li ◽

Dian-Peng Li

Keyword(s):

Anticancer Agents ◽

Human Cancer ◽

A549 Cells ◽

Anticancer Activities ◽

Human Cancer Cell Lines ◽

Ic50 Value ◽

Ic50 Values ◽

Diphenyl Tetrazolium Bromide ◽

Conjugated Compounds

A series of novel structurally simple analogues based on nitidine was designed and synthesized in search of potent anticancer agents. The antitumor activity against human cancer cell lines (HepG2, A549, NCI-H460, and CNE1) was performed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay in vitro. The results showed that some of them had good anticancer activities, especially derivatives with a [(dimethylamino)ethyl]amino side chain in the C-6 position. Planar conjugated compounds 15a, 15b, and 15c, with IC50 values of 1.20 μM, 1.87 μM, and 1.19 μM against CNE1 cells, respectively, were more active than nitidine chloride. Compound 15b and compound 15c with IC50 values of 1.19 μM and 1.37 μM against HepG2 cells and A549 cells demonstrated superior activities to nitidine. Besides, compound 5e which had a phenanthridinone core displayed extraordinary cytotoxicity against all test cells, particularly against CNE1 cells with the IC50 value of 1.13 μM.

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EVALUATION OF IN VITRO ANTIOXIDANT AND α-AMYLASE INHIBITORY ACTIVITY OF PHYLLANTHUS INDOFISCHERI BENNET

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2016v8i11.14013 ◽

2016 ◽

Vol 8 (11) ◽

pp. 131 ◽

Cited By ~ 1

Author(s):

Kalpana S ◽

Ramakrushna B. ◽

Anitha S.

Keyword(s):

Inhibitory Activity ◽

Colorimetric Method ◽

Radical Scavenging ◽

Total Flavonoid ◽

Aluminium Chloride ◽

Total Phenolic ◽

Total Flavonoid Content ◽

Flavonoid Content ◽

Ic50 Values

Objective: The present study evaluates the antioxidant and α-amylase inhibitory activity of leaf and bark extracts of Phyllanthus indofischeri with methanol and water as solvents. In addition to this, the total phenolic content and total flavonoid content was determined.Methods: The total phenolic and total flavonoid content of the extracts was determined by folin ciocaletus reagent method and aluminium chloride colorimetric method respectively. The antioxidant and α-amylase inhibitory activity were measured by various assays, including α, α-diphenyl-ẞ-dipicryl-hydrazyl (DPPH) free radical scavenging, 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulphonicacid) (ABTS) radical scavenging, superoxide radical scavenging, total antioxidant capacity by phosphomolybdate method and porcine pancreatic α-amylase inhibitory assay. The IC50 values were calculated and compared with standards such as gallic acid, ascorbic acid and α-acarbose.Results: The results illustrated that all the extracts of Phyllanthus indofischeri exhibit significant antioxidant and α-amylase inhibitory activity. Among the extracts, methanolic leaf extract showed high levels of activity followed by bark water extract.Conclusion: Phyllanthus indofischeri extracts had shown antioxidant and α-amylase inhibitory activity. On the basis of these results, Phyllanthus indofischeri can be used as a natural antioxidant and hypoglycemic agent against various disorders related to oxidative stress; and the isolation of bioactive compounds was warranted.

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Synthesis, Antimicrobial Activity and Molecular Docking of Novel Thiourea Derivatives Tagged with Thiadiazole, Imidazole and Triazine Moieties as Potential DNA Gyrase and Topoisomerase IV Inhibitors

Molecules ◽

10.3390/molecules25122766 ◽

2020 ◽

Vol 25 (12) ◽

pp. 2766 ◽

Cited By ~ 1

Author(s):

Heba E. Hashem ◽

Abd El-Galil E. Amr ◽

Eman S. Nossier ◽

Elsayed A. Elsayed ◽

Eman M. Azmy

Keyword(s):

Antimicrobial Activity ◽

Molecular Docking ◽

Antimicrobial Agents ◽

Biological Activities ◽

Topoisomerase Iv ◽

Thiourea Derivatives ◽

E Coli ◽

Cytotoxicity Studies ◽

Ic50 Values

To develop new antimicrobial agents, a series of novel thiourea derivatives incorporated with different moieties 2–13 was designed and synthesized and their biological activities were evaluated. Compounds 7a, 7b and 8 exhibited excellent antimicrobial activity against all Gram-positive and Gram-negative bacteria, and the fungal Aspergillus flavus with minimum inhibitory concentration (MIC) values ranged from 0.95 ± 0.22 to 3.25 ± 1.00 μg/mL. Furthermore, cytotoxicity studies against MCF-7 cells revealed that compounds 7a and 7b were the most potent with IC50 values of 10.17 ± 0.65 and 11.59 ± 0.59 μM, respectively. On the other hand, the tested compounds were less toxic against normal kidney epithelial cell lines (Vero cells). The in vitro enzyme inhibition assay of 8 displayed excellent inhibitory activity against Escherichia coli DNA B gyrase and moderate one against E. coli Topoisomerase IV (IC50 = 0.33 ± 1.25 and 19.72 ± 1.00 µM, respectively) in comparison with novobiocin (IC50 values 0.28 ± 1.45 and 10.65 ± 1.02 µM, respectively). Finally, the molecular docking was done to position compound 8 into the E. coli DNA B and Topoisomerase IV active pockets to explore the probable binding conformation. In summary, compound 8 may serve as a potential dual E. coli DNA B and Topoisomerase IV inhibitor.

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Phenolic Profile, Antioxidant, and Antidiabetic Potential Exerted by Millet Grain Varieties

Antioxidants ◽

10.3390/antiox9030254 ◽

2020 ◽

Vol 9 (3) ◽

pp. 254 ◽

Cited By ~ 4

Author(s):

Fred Kwame Ofosu ◽

Fazle Elahi ◽

Eric Banan-Mwine Daliri ◽

Ramachandran Chelliah ◽

Hun Ju Ham ◽

...

Keyword(s):

Radical Scavenging Activity ◽

Advanced Glycation Endproducts ◽

Radical Scavenging ◽

Total Phenolic ◽

Phenolic Profile ◽

Glycation Endproducts ◽

Total Antioxidant ◽

Ic50 Values

This study evaluated the potential antioxidant and antidiabetic properties in vitro of four millet grain varieties cultivated in South Korea. The free fractions were tested for their total antioxidant capacity using 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS+) and 2,2′-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assays, followed by α-glucosidase, α-amylase, and advanced glycation endproducts (AGEs) formation inhibition assays. The total phenolics, flavonoids, and condensed tannins in the free fractions ranged from 107.8 to 136.4 mg ferulic acid equivalent (FAE)/100 g, 101.3 to 115.8 mg catechin equivalent (CE)/100 g, and 17.65 to 59.54 mg catechin equivalent (CE)/100 g, respectively. Finger Italian millet had the highest total phenolic content (136.4 mg FAE/100 g) and flavonoid content (115.8 mg CE/100 g). Barnyard and finger Italian millet showed the highest DPPH (IC50 = 359.6 µg/mL and 436.25 µg/mL, respectively) and ABTS radical scavenging activity (IC50 = 362.40 µg/mL and 381.65 µg/mL, respectively). Similarly, finger Italian millet also exhibited significantly lower IC50 values for the percentage inhibition of α-glucosidase (18.07 µg/mL) and α-amylase (10.56 µg/mL) as compared with acarbose (IC50 = 59.34 µg/mL and 27.73 µg/mL, respectively) and AGEs formation (33.68 µg/mL) as compared with aminoguanidine (AG) (52.30 µg/mL). All eight phenolic compounds identified in finger Italian millet were flavonoids, with flavanols being the predominant subclass. Taken together, millet flavonoids play important roles in the prevention and management of type 2 diabetes, and hence finger Italian millet has the potential to be developed as a functional food.

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