Antioxidant and Cardioprotective Evaluation of Some N-(3-Chloro-2-oxo-4-
arylazetidin-1-yl)-2-[(4-oxo-2-aryl-4H-chromen-7-yl)oxy]acetamide Derivatives

A series of N-(3-chloro-2-oxo-4-arylazetidin-1-yl)-2-[(4-oxo-2-aryl-4H-chromen-7-yl)oxy]acetamide derivatives [SLP VI 1(a-d)-2(a-d)] were synthesized from 7-hydroxy flavone derivatives through the intermediate Schiff bases. The synthesized compounds were investigated for in vitro antioxidant property by DPPH radical scavenging assay. The title compounds with good antioxidant potency were further evaluated for possible cardioprotective effect by doxorubicin induced cardiotoxicity. All biochemical changes were normalized after oral administration of the test compounds at the dose of 50 μg/kg. The results showed the significant (p < 0.05) increase in antioxidant enzymes catalase and superoxide dismutase in heart tissue homogenates. These observations enable us to conclude that the synthesized derivatives SLP VI 1b, VI 1c, VI 2b and VI 2d have cardioprotective activity against doxorubicin induced cardiotoxicity. Further, an attempt has been made to perform in silico studies on the synthesized compounds to predict the interaction between test ligands and prospective cardiovascular protein targets using molecular docking tools. The title compounds have good binding affinity with MAPkinase P38 and PKCβ cardiovascular targets.

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Fortification of a Desert Using Nanoencapsulated Supercritical Carbon Dioxide Extract of Small Cardamom Seeds: A Nutraceutical Custard with Antioxidant Synergy

Recent Patents on Biotechnology ◽

10.2174/1872208315666210913100153 ◽

2021 ◽

Vol 15 ◽

Author(s):

Kaninika Paul ◽

Dipshikha Tamili ◽

Paramita Bhattacharjee

Keyword(s):

Radical Scavenging Activity ◽

Radical Scavenging ◽

Control Sample ◽

Reducing Power ◽

Antioxidant Property ◽

Total Phenolic ◽

Antioxidant Potency ◽

Spray Dried

Background: 1,8 cineole-rich supercritical CO2 extract of small cardamom seeds of Alleppey green variety exhibiting prominent antioxidant property was microencapsulated and utilized in formulating an antioxidant-rich custard. However, the antioxidant potency of the prepared custard was not appreciable. To redress the phytochemical loss during custard preparation, custard using nanoliposomes was formulated. Patents related to 1,8 cineole-rich food products have been revised thoroughly. Objective: The objective of the current study is to examine whether nanoencapsulation-mediated entrapment of antioxidants is more effective in fortifying a dessert, namely custard, vis-à-vis microencapsulated (spray dried)-mediated enhancement of antioxidative potency in the same. Methods: Our previous investigations have established that nanoliposome of 1,8 cineole-rich supercritical CO2 extract of small cardamom seeds effectively redresses type 2 diabetes and hypercholesterolemia. In the current investigation, this pre-characterized nanoliposome which exhibited appreciable in vitro and in vivo antioxidant efficacy has been utilized at varying concentrations for fortification of a custard. The designer custard samples have been characterized for their sensory and physicochemical properties, identification of the cardamom antioxidants therein and determination of the synergistic efficacy value of the identified antioxidants. Results: The custard formulated with 0.3% nanoliposomes exhibited appreciable antioxidant potency in terms of DPPH radical scavenging activity (304.58±1.09 mg/ml) and reducing power (0.020±0.001 mg BHT/g custard), conferred by its total phenolic content (0.049±0.004 mg GAE/g custard). It also had relatively more stable textural attributes vis-à-vis the control sample (formulated with the non-encapsulated native extract). GC-MS analysis of the nanoliposome-fortified custard confirmed retention of the spice antioxidants namely1,8- cineole, α-terpinyl acetate, α-terpineol and linalool and its synergistic efficacy value being greater than unity, attested to a synergistic presence of cardamom antioxidants therein. The newly formulated custard retained more than 4.5 times of 1,8-cineole (5.05 mg/g custard) vis-à-vis the custard sample (1.12 mg/g custard) prepared with a microencapsulated (spray-dried) formulation of the extract. Additionally, absence of heavy metals in the formulated custard confirmed it to be safe for consumption. Conclusion: This is the first study on application of nanoliposomes of spiceuticals in formulation of a dessert, and more emphatically on use of a ‘green’ supercritical CO2 extract of spice antioxidants in fortification of a dessert to achieve antioxidant synergy.

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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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ASSESSMENT OF PHYTOCHEMICALS, TOTAL PHENOL, FLAVONOID CONTENT AND IN VITRO ANTIOXIDANT PROPERTY OF LARGE CARDAMOM EXTRACTS

INDIAN DRUGS ◽

10.53879/id.58.10.12627 ◽

2021 ◽

Vol 58 (10) ◽

pp. 34-41

Author(s):

Kanthlal S. K. ◽

Jipnomon Joseph ◽

Bindhu P. Paul ◽

Vijayakumar M ◽

Rema Shree A. B. ◽

...

Keyword(s):

Antioxidant Activity ◽

Antioxidant Activities ◽

Radical Scavenging ◽

Reducing Power ◽

Antioxidant Property ◽

Bioactive Constituents ◽

Preliminary Assessment ◽

Reducing Power Assay ◽

Large Cardamom

Amomum subulatum, commonly known as large or black cardamom, is a commonly used spice in Indian kitchens and is traditionally used to treat various ailments. To add more knowledge about the medicinal values of the fruit, this study was conducted to evaluate the in vitro antioxidant activities of aqueous, methanol, ethanol, hydro alcohol, ethyl acetate, acetone and chloroform extracts of the fruit. Preliminary assessment was done to detect the presence of phytoconstituents using identification tests. The antioxidant activity was measured by employing methods such as diphenylpicrylhydrazyl (DPPH) radical scavenging assay, total antioxidant activity equivalent to ascorbic acid, reducing power assay and superoxide anion scavenging assay. The antioxidant activities were compared with their respective phenol and flavonoid contents. Preliminary assessment revealed that large cardamom fruit is a good source of all the bioactive constituents as well as phenol and flavonoid essential for medicinal values. The extract obtained by polar solvents showed the highest antioxidant efficacy in relation to its phenol content. Also, all the solvent-soluble fractions showed a concentration-dependent antioxidant effect. Results from our study prove that large cardamom can alleviate oxidative stress, suggesting the potential of large cardamom as a functional food

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Analysis of the oxidative stress inhibition potentials of Artemisia annua and its bioactive compounds through in vitro and in silico studies

Journal of Pharmacy & Bioresources ◽

10.4314/jpb.v18i3.9 ◽

2021 ◽

Vol 18 (3) ◽

pp. 245-259

Author(s):

Stephen Adakole Ejembi ◽

Titilayo Omolara Johnson ◽

Jonathan Dingkwoet Dabak ◽

Augustina Oduje Akinsanmi ◽

Jane-Rose Ifuanyachi Oche ◽

...

Keyword(s):

Oxidative Stress ◽

Bioactive Compounds ◽

Artemisia Annua ◽

Antioxidant Activities ◽

Protein Targets ◽

Active Involvement ◽

In Silico Studies ◽

Plateau State ◽

Antioxidant Mechanisms

Oxidative stress overwhelms the antioxidant mechanisms of living systems, with active involvement in the pathogenesis of several diseases. Natives of Gangnim in the Plateau State of Nigeria may be unknowingly endowed with some protective advantages against oxidative stress for their habitual consumption of Artemisia annua tea. The antioxidant activities of A. annua extracts were determined using in vitro methods and the inhibitory potentials of twenty-nine (29) bioactive compounds of the plant against oxidative stress target proteins were assessed through molecular docking analysis. These extracts showed significantly high activities in scavenging nitric oxide, 2,2-diphenyl-1-picrylhydrazyl (DPPH) and reducing ferric (Fe3+) to ferrous (Fe2+) iron. Virtually, none of the bioactive compounds binds to the active site of the antioxidant protein targets. Rather, 72.41, 93.10 and 75.86% of these compounds bind with high binding affinity to the activator binding sites of superoxide dismutase (SOD), glutathione peroxidase (GSH-Px) and catalase (CAT) respectively. 7,8-dimethylalloxazine (-8.10 kcal/mol) ranked highest as a prospective inhibitor of xanthine oxidase (XOX). The antioxidant activity exhibited by the extracts of the locally cultivated A. annua and the molecular interactions of its bioactive compounds against the protein targets used predict that oxidative stress inhibition could be effectively achieved with these phytochemicals.

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Rice Germosprout Extract Protects Erythrocytes from Hemolysis and the Aorta, Brain, Heart, and Liver Tissues from Oxidative StressIn Vitro

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2016/9587020 ◽

2016 ◽

Vol 2016 ◽

pp. 1-9 ◽

Cited By ~ 1

Author(s):

Shahdat Hossain ◽

Sujan Bhowmick ◽

Marzan Sarkar ◽

Mehedi Hassan ◽

Jakir Hussain ◽

...

Keyword(s):

Oxidative Stress ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Lipid Peroxide ◽

Erythrocyte Membranes ◽

Total Polyphenols ◽

Tissue Homogenates ◽

Antioxidative Effects ◽

Gallic Acid Equivalent

Identifying dietary alternatives for artificial antioxidants capable of boosting antihemolytic and antioxidative defense has been an important endeavor in improving human health. In the present study, we studied antihemolytic and antioxidative effects of germosprout (i.e., the germ part along with sprouted stems plus roots) extract prepared from the pregerminated rice. The extract contained considerable amounts of antioxidantβ-carotene (414±12 ng/g of extract) and phytochemicals such as total polyphenols (12.0±1.1 mg gallic acid equivalent/g of extract) and flavonoids (11.0±1.4 mg catechin equivalent/g of extract). The antioxidant potential of the extract was assessed by its DPPH- (2,2-diphenyl-1-picrylhydrazyl-) free radical scavenging activity where we observed that germosprout extract had considerable antioxidative potentials. To evaluate antihemolytic effect of the extract, freshly prepared erythrocytes were incubated with either peroxynitrite or Fenton’s reagent in the absence or presence of the extract. We observed that erythrocytes pretreated with the extract exhibited reduced degree ofin vitrohemolysis. To support the proposition that germosprout extract could act as a good antioxidative agent, we also inducedin vitrooxidative stress in erythrocyte membranes and in the aorta, brain, heart, and liver tissue homogenates in the presence of the extract. As expected, germosprout extract decreased oxidative stress almost to the same extent as that of vitamin E, as measured by lipid peroxide levels, in all the mentioned tissues. We conclude that rice germosprout extract could be a good natural source of antioxidants to reduce oxidative stress-induced hemolysis and damage of blood vessels and other tissues.

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In vitro antioxidant, antiglycation, and MGO scavenging effects of Leonurus sibiricus water extract

Asia Pacific Journal of Molecular Biology and Biotechnology ◽

10.35118/apjmbb.2021.029.4.08 ◽

2021 ◽

pp. 84-95

Author(s):

Xiu Qing Chong ◽

Kirtani AP Anamalay ◽

Okechukwu Patrick Nwabueze ◽

Hor Kuan Chan

Keyword(s):

Radical Scavenging Activity ◽

Radical Scavenging ◽

Water Extract ◽

Antioxidant Property ◽

Future Research ◽

Total Phenolic ◽

Bioactive Constituents ◽

Bioactive Component ◽

Glycation End Products

Recently, extensive research has been conducted to evaluate the inhibitory activity of different plant species on the advanced glycation end products (AGEs). L. sibiricus is a traditional herb that has been used for postpartum confinement meals in Sarawak, Malaysia and pharmacologically possess anti-hemorrhagic, antioxidant, anti-diabetic, and anti-cancer. The aim of this research was to evaluate the antioxidant, anti-AGEs, and preliminary biochemical screening of bioactive component present in L. sibiricus in water extract. Free radical scavenging activity of L. sibiricus was evaluated via DPPH, hydroxyl radical, nitric oxide, lipid peroxidation, chelating capacity, and total phenolic content was evaluated comparing with gallic acid. Inhibition of formation AGEs by L. sibiricus was evaluated using BSA-MGO, BSA-glucose and MGO scavenging assays. Flavonoids, phenols, saponins, alkaloids, phytosterol, and diterpenoids were identified in L. sibiricus extract. It also seems to inhibit early and late formation of AGE and MGO scavenging ability. L. sibiricus was able to inhibit the formation of early and late formation of AGE through the scavenging of the formation of reactive dicarbonyl intermediates and reduce the formation of methylquinoxaline adducts through the scavenge of MGO. The inhibition of AGEs formation by L. sibiricus maybe due its antioxidant property and the presence phytochemical bioactive constituents which has been previously reported to possess antioxidant and anti-AGE activity. Future research is ongoing to identify the adducts formed because of MGO scavenging by L. sibiricus using HPLC.

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HINOKITIOL-AMELIORATED DIETHYLNITROSAMINE-INDUCED HEPATOCARCINOGENESIS THROUGH ANTIOXIDANT MECHANISM IN RATS: IN VITRO AND IN VIVO STUDY

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i6.21950 ◽

2018 ◽

Vol 11 (6) ◽

pp. 232 ◽

Cited By ~ 1

Author(s):

Mohamed Zerein Fathima ◽

Mohamed Nainar ◽

Somasundaram I ◽

Shanmugarajan Ts

Keyword(s):

Biochemical Parameters ◽

Radical Scavenging ◽

Antioxidant Property ◽

Treated Group ◽

Enzymatic Antioxidants ◽

Glutathione S Transferase ◽

Antioxidant Mechanism ◽

Single Intraperitoneal Injection

Objective: Chemoprevention seems to be the best strategy for lowering the incidence of liver cancer. Therefore, this study has been initiated to investigate the hinokitiol (HIOL) supplementation which could prevent oxidative stress induced by hepatocarcinogen, diethylnitrosamine (DEN) in rats.Methods: The biochemical parameters such as tissue damaging enzymes, namely, alanine transaminase (ALT), alkaline phosphatase (ALP), aspartate aminotransferase (AST), and attack-free period and enzymatic antioxidants, namely, glutathione (GSH), catalase (CAT), glutathione peroxidase (GPx), glutathione-S-transferase (GST), glutathione reductase (GR), superoxide dismutase (SOD), and histopathological changes were estimated.Results: DEN-treated rats shows increased ALT, ALP, and AST and decreased GSH, GST, CAT, GPx, GR, and SOD activities in liver tissues. The DEN-treated group (200 mg/kg body weight single intraperitoneal injection) with phenobarbital 0.05% orally showed the severe histopathological lesions in liver tissue. Whereas, the groups received HIOL along with DEN shown a comparatively lesser damage. Here, the HIOL supplementation ameliorated the biochemical parameters as well as evoked enzymatic antioxidants in DEN-induced rats to the control values.Conclusion: The HIOL possesses potent antioxidant property, in this credence to that conception, the treatment with HIOL may prevent the development of chemical-induced hepatocarcinogenesis in rats by free radical scavenging mechanism.

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An Insight into the Discovery of Potent Antifilarial Leads Against Lymphatic Filariasis

Current Drug Targets ◽

10.2174/1389450120666191204152415 ◽

2020 ◽

Vol 21 (7) ◽

pp. 657-680

Author(s):

Pone Kamdem Boniface ◽

Ferreira Igne Elizabeth

Keyword(s):

Lymphatic Filariasis ◽

In Vivo Studies ◽

Protein Targets ◽

Scientific Databases ◽

Naturally Occurring ◽

In Silico Studies ◽

Antifilarial Activity ◽

Insight Into

Background and Objectives: Lymphatic filariasis is a neglected tropical disease caused by infection with filarial worms that are transmitted through mosquito bites. Globally, 120 million people are infected, with nearly 40 million people disfigured and disabled by complications such as severe swelling of the legs (elephantiasis) or scrotum (hydrocele). Current treatments (ivermectin, diethylcarbamazine) have limited effects on adult parasites and produce side effects; therefore, there is an urgent to search for new antifilarial agents. Numerous studies on the antifilarial activity of pure molecules have been reported accross the recent literature. The present study describes the current standings of potent antifilarial compounds against lymphatic filariasis. Methods: A literature search was conducted for naturally occurring and synthetic antifilarial compounds by referencing textbooks and scientific databases (SciFinder, PubMed, Science Direct, Wiley, ACS, SciELO, Google Scholar, and Springer, among others) from their inception until September 2019. Results: Numerous compounds have been reported to exhibit antifilarial acitivity in adult and microfilariae forms of the parasites responsible for lymphatic filariasis. In silico studies of active antifilarial compounds (ligands) showed molecular interactions over the protein targets (trehalose-6-phosphate phosphatase, thymidylate synthase, among others) of lymphatic filariasis, and supported the in vitro results. Conclusion: With reference to in vitro antifilarial studies, there is evidence that natural and synthetic products can serve as basic scaffolds for the development of antifilarial agents. The optimization of the most potent antifilarial compounds can be further performed, followed by their in vivo studies.

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In- vitro Antioxidant and Cardio-protective effect of Delonix elata (L.) Leaf extract against Doxorubicin induced toxicity in H9c2 Cardio-myocyte cell line

Research Journal of Pharmacy and Technology ◽

10.52711/0974-360x.2021.00980 ◽

2021 ◽

pp. 5635-5641

Author(s):

Archana V ◽

Indumathy R

Keyword(s):

Reactive Oxygen Species ◽

Protective Effect ◽

Cell Viability ◽

Leaf Extract ◽

Radical Scavenging ◽

Reactive Oxygen ◽

Ethanolic Extract ◽

Antioxidant Property ◽

Oxygen Species

Objective: The aim of this study is to evaluate the protective effect of Delonix elata (L.) leaf extract against doxorubicin-induced cardiotoxicity in H9c2 cells. Methods: Doxorubicin has been used to treat cancer, but its clinical uses are limited because of its dose-dependent cardiotoxicity. Reactive oxygen species play an important role in the pathological process of cardiotoxicity. The various extracts (pet.ether, ethyl acetate and ethanol) of Delonix elata leaves antioxidant property was evaluated by SOD antioxidant assay and DPPH free radical scavenging assay. The cells were incubated with different concentrations of various extracts of Delonix elata leaves for 2 hr, followed by incubation with 5µM doxorubicin for 24 hr. Cell viability was determined by using MTT assay, respectively. Results: The various extracts of Delonix elata leaves exhibits antioxidant activity. The Doxorubicin significantly decreased cell viability which was accompanied by an increased ROS production. Pre-treatment with various extracts of Delonix elata leaves increased the viability ofcells and inhibit the generation of reactive oxygen species. Conclusion: In this study, findings how that Delonix elata leaf extract exhibited a protective effect against oxidative stress-induced cardiomyocyte damage. The ethanolic extract of Delonix elata leaves possesses significant antioxidant and cardioprotective activity.

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COMPARATIVE EVALUATION OF ANTIDIABETIC AND ANTIOXIDANT POTENCY OF DIFFERENT EXTRACTS OBTAINED FROM MEMECYLON SPECIES

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2017v9i2.15695 ◽

2017 ◽

Vol 9 (2) ◽

pp. 187

Author(s):

Tumkur Ramasetty Bharathi ◽

Harishchandra Sripathy Prakash

Keyword(s):

Antioxidant Activities ◽

Antioxidant Properties ◽

Radical Scavenging ◽

Reducing Power ◽

Methanol Extracts ◽

Soxhlet Apparatus ◽

Antioxidant Potency ◽

Reducing Power Assay ◽

Different Doses

Objective: Memecylon species is being extensively used in traditional medicine for the treatment of skin disorders and it is proved to possess antidiabetic and anti-inflammatory properties. The present investigation was to study the effect of different solvent extracts of five Memecylon species such as M. umbellatum, M. talbotianum, M. edule, M. malabaricum and M. wightii on antidiabetic and antioxidant effects.Methods: Plant extracts were prepared using soxhlet apparatus using different solvents such as hexane, ethyl acetate, methanol and water and obtained extracts were subjected to antidiabetic (α-amylase and α-glucosidase inhibition assays) and antioxidant (2, 2-Diphenyl-2-Picryl Hydrazyl hydrate (DPPH), 2,2-Azino-bis (3-ethyl benzothiazoline-6-Sulfonic acid)diammonium salt (ABTS), Superoxide radical scavenging assay (SRSA) and reducing power assays) evaluated at different doses.Results: Methanol extracts of all five Memecylon species exhibited effective antidiabetic and antioxidant properties among them methanol extracts of M. malabaricum and M. talbotianum have highest biological activity. For α-amylase IC50 value for both M. malabaricum and M. talbotianum was found to be 100 and 130 µg/reaction and IC50 value for α-glucosidase was found to be 6.1 and 7.8 µg/reaction respectively. For DPPH the IC50value was found to be 190 µg/reaction, for ABTS 31-39 µg/reaction, for SRSA 950-1200 µg/reaction and for reducing power assay 420-490 µg/reaction respectively.Conclusion: The results indicate that methanol extracts of M. malabaricum and M. talbotianum possess potent in vitro antidiabetic and antioxidant activities compared to other Memecylon species.

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