scholarly journals Docking Studies, Synthesis, Characterization and Evaluation of Their Antioxidant and Cytotoxic Activities of Some Novel Isoxazole-Substituted 9-Anilinoacridine Derivatives

2012 ◽  
Vol 2012 ◽  
pp. 1-6 ◽  
Author(s):  
R. Kalirajan ◽  
M. H. Mohammed Rafick ◽  
S. Sankar ◽  
S. Jubie

A convenient synthesis of novel isoxazole-substituted 9-anilinoacridine derivatives5a–jwas reported. The compounds were confirmed by physical and analytical data and screened forin vitroantioxidant activity by DPPH method, reducing power assay and total antioxidant capacity method. The cytotoxic activity of the compounds was also studied in HEp-2 cell line. The docking studies of the synthesized compounds were performed towards the key nucleoside dsDNA by using AutoDock vina 4.0 programme. All the isoxazole-substituted compounds have significant activities.

2021 ◽  
Vol 18 (21) ◽  
pp. 35
Author(s):  
Manuel Rodrigues ◽  
Basavaraju Bennehalli ◽  
Vagdevi Hosadu Manjappaiah ◽  
Shruthi Anantha

In the present study, a set of different benzoxazole derivatives has been synthesized from ethyl acetoacetate, ethoxymethylene malononitrile, NaNO2, and organic acids. Analytical instruments like proton NMR (1H), carbon NMR (13C), infrared spectroscopy (IR), and LC-MS mass spectrometry were used for structural characterization. Synthesized molecules were evaluated for In-vitro antioxidant property (DPPH assay, Total antioxidant & reducing power method) and anti-diabetic property (alpha-amylase & alpha-glucosidase assay). In silico, studies against Human pancreatic alpha-amylase (PDB ID: 3BAW) have been carried out to get the binding approach of the ligand towards the protein. The results demonstrated that compounds namely 5b, 6b, 3b and 4b had potent antioxidant and anti-diabetic activity compared with ascorbic acid and acarbose. HIGHLIGHTS Anti-oxidant (DPPH assay, Total antioxidant and Reducing power) and Anti-diabetic (alpha-amylase & alpha-glucosidase assay) activities performed for synthesized molecules Sulfonamide substitutions are more potent towards biological activities In silico docking studies correlate with in vitro studies The small three-dimensional, stable structure and its ability to form hydrogen bonding the molecules show good activity towards antioxidant and anti-diabetic GRAPHICAL ABSTRACT


2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Praveena Bhatt ◽  
Gilbert Stanley Joseph ◽  
Pradeep Singh Negi ◽  
Mandyam Chakravarthy Varadaraj

The stem of Indian borage (Plectranthus amboinicus) was found to be an antioxidant rich fraction as evaluated byin vitromodels such as DPPH free radical scavenging, reducing power assay, superoxide anion radical scavenging, and total antioxidant capacity. The extract also exhibited antiplatelet aggregation ability, antibacterial activity, and antiproliferative effect against cancer cell lines: Caco-2, HCT-15, and MCF-7. Phytochemical evaluation of the extract revealed the occurrence of total phenolics (49.91 mg GAE/g extract), total flavonoids (26.6 mg RE/g extract), and condensed tannins (0.7 mg TAE/g extract). Among the major phenolics, rosmarinic acid (6.160 mg/g extract) was predominant, followed by caffeic acid (0.770 mg/g extract), rutin (0.324 mg/g extract), gallic acid (0.260 mg/g extract), quercetin (0.15 mg/g extract), andp-coumaric acid (0.104 mg/g extract). The appreciable biological activity and presence of biomolecules in the methanolic extract of stem indicate its potential application as functional food ingredients and nutraceuticals.


Author(s):  
JENSON JACOB ◽  
MEENU JOHN

Objective: The aim of this study was focussed on phytochemical analysis, in vitro antioxidant activities of different solvent extracts of Hypoestes phyllostachya leaf. Methods: The leaves were washed efficiently, shade dried and coarsely powdered. The powdered leaf material of Hypoestes phyllostachya was successively extracted with hexane, chloroform, methanol and water using Soxhlet apparatus. Preliminary phytochemical screenings for polyphenolics, proteins, phytosteroids, flavonoids, tannins, glycosides, alkaloids carbohydrates, polyphenolics, saponins were done by following standard procedure. In vitro antioxidant activities of various solvent extracts were assessed using DPPH, ABTS, Hydroxy radical, total antioxidant capacity and reducing power assay. Polyphenolics and flavonoids were also estimated. Results: The results showed that most of the phytochemical compounds such as carbohydrates, proteins, steroids, fixed oils and fatty acids, flavonoids, alkaloids, saponins, tannins, polyphenolics and glycosides present in the methanolic and aqueous extract of Hypoestes phyllostachya. The in vitro antioxidant activity of Hypoestes phyllostachya leaf clearly showed that it has better antioxidant activity, which was confirmed by different assays. Conclusion: From this work, it can be concluded that Hypoestes phyllostachya has the potential to be a good antioxidant but have only a lesser amount of flavonoids and polyphenolic contents. This was the first report on the pharmacological activity of the Hypoestes phyllostachya.


Author(s):  
Hemlata Bhatt ◽  
Sarla Saklani ◽  
Kumud Upadhayay

Objective: To evaluate the phytochemical, physicochemical, antimicrobial and in-vitro antioxidant activity of Clamentis montana (Family: Rananculaceae).Methods: The extracts were evaluated for antibacterial activity against S. aureus, B. subtilis, E. coli, P. aeruginosa by cup plate method. In-vitro antioxidant activity was done by DPPH, ferrous chelating and reducing power assay method. The physicochemical parameter like a loss on drying, total ash value, foreign matter, etc. was evaluated by standard protocol.Results: The extract showed significant antibacterial activity against all test strains when compared with standard drugs amoxicillin. The extract showed significant antioxidant activity by DPPH method, reducing power assay and ferrous chelating method.Conclusion: The extract showed a dose-dependent significant antibacterial and antioxidant activity.


2016 ◽  
Vol 2016 ◽  
pp. 1-6 ◽  
Author(s):  
Hamayun Khan ◽  
Hazrat Amin ◽  
Asad Ullah ◽  
Sumbal Saba ◽  
Jamal Rafique ◽  
...  

Two important biologically active compounds were isolated fromMallotus philippensis. The isolated compounds were characterized using spectroanalytical techniques and found to be bergenin (1) and 11-O-galloylbergenin (2). Thein vitroantioxidant and antiplasmodial activities of the isolated compounds were determined. For the antioxidant potential, three standard analytical protocols, namely, DPPH radical scavenging activity (RSA), reducing power assay (RPA), and total antioxidant capacity (TAC) assay, were adopted. The results showed that compound2was found to be more potent antioxidant as compared to1. Fascinatingly, compound2displayed better EC50results as compared toα-tocopherol while being comparable with ascorbic acid. The antiplasmodial assay data showed that both the compound exhibited good activity against chloroquine sensitive strain ofPlasmodium falciparum(D10) and IC50values were found to be less than 8 μM. Thein silicomolecular docking analyses were also performed for the determination of binding affinity of the isolated compounds usingP. falciparumproteins PfLDH and Pfg27. The results showed that compound2has high docking score and binding affinity to both protein receptors as compared to compound1. The demonstrated biological potentials declared that compound2could be the better natural antioxidant and antiplasmodial candidate.


2020 ◽  
Vol 16 ◽  
Author(s):  
Sajjad Esmaeili ◽  
Nazanin Ghobadi ◽  
Donya Nazari ◽  
Alireza Pourhossein ◽  
Hassan Rasouli ◽  
...  

Background: Curcumin, as the substantial constituent of the turmeric plant (Curcuma longa), plays a significant role in the prevention of various diseases, including diabetes. It possesses ideal structure features as enzyme inhibitor, including a flexible backbone, hydrophobic nature, and several available hydrogen bond (H-bond) donors and acceptors. Objective: The present study aimed at synthesizing several novel curcumin derivatives and further evaluation of these compounds for possible antioxidant and anti-diabetic properties along with inhibitory effect against two carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase, as these enzymes are therapeutic targets for attenuation of postprandial hyperglycemia. Methods: Therefore, curcumin-based pyrido[2,3-d]pyrimidine derivatives were synthesized and identified using an instrumental technique like NMR spectroscopy and then screened for antioxidant and enzyme inhibitory potential. Total antioxidant activity, reducing power assay and 1,1-diphenyl-2-picrylhydrazyl (DPPH• ) radical scavenging activity were done to appraisal the antioxidant potential of these compounds in vitro. Results: Compounds L6-L9 showed higher antioxidant activity while L4, L9, L12 and especially L8 exhibited the best selectivity index (lowest α-amylase/α-glucosidase inhibition ratio). Conclusion: These antioxidant inhibitors may be potential anti-diabetic drugs, not only to reduce glycemic index but also to limit the activity of the major reactive oxygen species (ROS) producing pathways.


INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (10) ◽  
pp. 34-41
Author(s):  
Kanthlal S. K. ◽  
Jipnomon Joseph ◽  
Bindhu P. Paul ◽  
Vijayakumar M ◽  
Rema Shree A. B. ◽  
...  

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


Plants ◽  
2022 ◽  
Vol 11 (2) ◽  
pp. 208
Author(s):  
Ahlam Elwekeel ◽  
Dalia El Amir ◽  
Enas I. A. Mohamed ◽  
Elham Amin ◽  
Marwa H. A. Hassan ◽  
...  

The current study accentuates the significance of performing the multiplex approach of LC-HRESIMS, biological activity, and docking studies in drug discovery, taking into consideration a review of the literature. In this regard, the investigation of antioxidant and cytotoxic activities of Trigonella stellata collected from the Egyptian desert revealed a significant antioxidant capacity using DPPH with IC50 = 656.9 µg/mL and a moderate cytotoxicity against HepG2, MCF7, and CACO2, with IC50 values of 53.3, 48.3, and 55.8 µg/mL, respectively. The evaluation of total phenolic and flavonoid contents resulted in 32.8 mg GAE/g calculated as gallic acid equivalent and 5.6 mg RE/g calculated as rutin equivalent, respectively. Chemical profiling of T. stellata extract, using LC-HRESIMS analysis, revealed the presence of 15 metabolites, among which eleven compounds were detected for the first time in this species. Interestingly, in vitro testing of the antidiabetic activity of the alcoholic extract noted an α-glucosidase enzyme inhibitory activity (IC50 = 559.4 µg/mL) better than that of the standard Acarbose (IC50 = 799.9 µg/mL), in addition to a moderate inhibition of the α-amylase enzyme (IC50 = 0.77 µg/mL) compared to Acarbose (IC50 = 0.21 µg/mL). α-Glucosidase inhibition was also virtualized by binding interactions through the molecular docking study, presenting a high binding activity of six flavonoid glycosides, as well as the diterpenoid compound graecumoside A and the alkaloid fenugreekine. Taken together, the conglomeration of LC-HRESIMS, antidiabetic activity, and molecular docking studies shed light on T. stellata as a promising antidiabetic herb.


2018 ◽  
Vol 7 (2) ◽  
pp. 191-198
Author(s):  
Shruti Gupta ◽  
◽  
Kishori G Apte ◽  
◽  

Sesbania grandiflora Linn. is perennial branching, small erect quick-growing short-lived soft-wooded tree, mostly cultivated in southeast Asian countries including India and grows primarily in hot, humid environments. This study investigated on phytochemical values- total phenolic flavonoid, tannins and saponin contents for Sesbania grandiflora leaf extracts. The total antioxidant capacity, DPPH, reducing power, superoxide scavenging and Iron chelating effects were examined by established methods. In-vitro cytotoxicity by brine shrimp bioassay. Both the extracts of Sesbania grandiflora were found to possess moderate to high amounts of phytochemical contents. The total phenolic, flavonoid and saponin contents were found significantly higher in EQSG whereas tannins were more in AQSG. The EQSG and AQSG possessed low IC50 for H2O2 Scavenging (32.9, 27.3µg/ml), TAC (35.6, 41.8µg/ml) and moderate for DPPH (114.9, 113µg/ml) and reducing power (176.3, 181.6µg/ml) respectively. The Brine shrimp lethality bioassay showed a significantly high LC50 value with EQSG (10313µg/ml) and AQSG (12773µg/ml) compared to cyclophosphamide (110µg/ml) in cytotoxic assay. The results evidenced the potential of Sesbania grandiflora Linn. as potent drug with antioxidant and cytotoxic activity and could be useful for preparation of nutraceuticals for pharmaceutical use in the treatment of various human diseases and its complications


2020 ◽  
Vol 11 (4) ◽  
pp. 6262-6267
Author(s):  
Krishnamoorthy Meenakumari ◽  
Giridharan Bupesh ◽  
Mayur Mausoom Phukan

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.


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