scholarly journals Synthesis, Characterization, Hydrolytic Cleavage, and Biological Activity Studies of 2-[(1e)-N-{2-[(2-{(Z)-[1-(2-Hydroxyphenyl)Ethylidene] Amino}Ethyl)Amino]Ethyl}Ethanimidoyl]Phenol

2019 ◽  
Vol 9 (5-s) ◽  
pp. 25-29
Author(s):  
Kamel Mokhnache ◽  
Soraya Madoui ◽  
Hanane Khither ◽  
El-Khamsa Soltani ◽  
Noureddine Charef ◽  
...  

A Schiff base ligand 2-[(1E)-N-{2-[(2-{(Z)-[1-(2-hydroxyphenyl) ethylidene] amino}ethyl)amino]ethyl} ethanimidoyl]phenol L was hydrolyzed by copper cation which lead to formation of 8,8-dichloro-2H,3H,5H,6H-1,3-diaza-2-cupracyclopenta[1,3-a]1,3-diaza-2-cupracyclopentane hydrate (Complex), characterized by UV, IR, Powder XRD and by elemental analysis. In vitro antioxidant and anticoagulant, activities of L were evaluated. Antioxidant potential of L was assessed by DPPH scavenging, β-carotene bleaching test, hydroxyl radical scavenging method, ABTS radical scavenging test, and by reducing power test. In vitro anticoagulant effect of L at the 84 µg/mL; showed the maximum prolongation of plasma recalcification time which is comparable with that of the anticoagulant drug; heparin. In conclusion, results of the present investigation indicate that the ligand L can be a potential anticoagulant agent. Keywords: Schiff base; Antioxidant; Free radicals; Anticoagulant.

Author(s):  
Raj Kumar Tiwari ◽  
Udayabanu Malairaman ◽  
Silpi Chanda

Objective: The intent  of this report  was to investigate the effect of aqueous root extract of Clerodendrum serratum L. for antioxidant activity using divergent models viz. DPPH scavenging assay, Superoxide scavenging assay and Ferric Reducing Antioxidant Power (FRAP) assay.Materials and Methods: The root of C. serratum was extracted using water. The yield of aqueous extract was 10%w/w. The outcome was examined statistically by the regression method.Results and discussions: The IC50 values are 85.43 µg/ml and 107.59 µg/ml for DPPH radical scavenging and Superoxide scavenging assay respectively whereas  FRAP showed significant reducing power activity with increased concentration of sample. The pilot study showed, a significant correlation existed between concentrations of the extract and percentage engrossment of free radicals.Conclusion: The antioxidant property may be corresponding to the polyphenols and flavonoids adjacent in the extract. These results clearly revealed that C. serratum might be effective against diseases analogous with free radical mediated. Keywords Clerodendrum serratum, DPPH, Superoxide, FRAP, Rutin, Antioxidant


Food Research ◽  
2021 ◽  
Vol 5 (6) ◽  
pp. 187-196
Author(s):  
R. Ghosh ◽  
P. Barua ◽  
O. Sikder ◽  
S. Saha ◽  
S. Mojumder ◽  
...  

Phenolic content and antioxidant activity of two common fruits of Bangladesh, namely Phyllunthus emblica and Elaeocarpus floribundus, were measured in water, methanol, ethanol, acetone and hexane extracts. Several in vitro models including phosphomolybdenum assay, DPPH free radical scavenging assay, FRAP assay and reducing power assay were used to assess the antioxidant activity of these extracts in comparison with reference antioxidants. Between the two fruits, P. emblica showed higher phenolic content and antioxidant activity in all the solvents used. In the DPPH scavenging assay, the activity of P. emblica extracts was close to reference antioxidants, ascorbic acid and BHT. Besides, considering the solvents used, extracts of both fruits had the highest phenolic and antioxidant activity in polar solvents. The correlation coefficient between total phenolics and antioxidant activities was found statistically significant. These findings suggest that P. emblica could be an excellent antioxidant resource for industries like food, pharmaceutical, and cosmetics.


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.


Plants ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 124
Author(s):  
Haidy A. Gad ◽  
Nilufar Z. Mamadalieva ◽  
Stefan Böhmdorfer ◽  
Thomas Rosenau ◽  
Gokhan Zengin ◽  
...  

The compositions of volatile components in the aerial parts of six Astragalus species, namely A. campylotrichus (Aca), A. chiwensis (Ach), A. lehmannianus (Ale), A. macronyx (Ama), A. mucidus (Amu) and A. sieversianus (Asi), were investigated using gas chromatograph-mass spectrometry (GC-MS) analysis. Ninety-seven metabolites were identified, accounting for 73.28, 87.03, 74.38, 87.93, 85.83, and 91.39% of Aca, Ach, Ale, Ama, Amu and Asi whole oils, respectively. Sylvestrene was the most predominant component in Asi, Amu and Ama, with highest concentration in Asi (64.64%). In addition, (E)-2-hexenal was present in a high percentage in both Ale and Ach (9.97 and 10.1%, respectively). GC-MS based metabolites were subjected to principal component analysis (PCA) and hierarchal cluster analysis (HCA) to explore the correlations between the six species. The PCA score plot displayed clear differentiation of all Astragalus species and a high correlation between the Amu and Ama species. The antioxidant activity was evaluated in vitro using various assays, phosphomolybdenum (PM), 2,2 diphenyl-1-picryl-hydrazyl-hydrate (DPPH), 2,2-azino bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), cupric reducing antioxidant capacity (CUPRAC), ferric reducing power (FRAP) and ferrous ion chelation (FIC) assays. In addition, the potential for the volatile samples to inhibit both acetyl/butyrylcholinesterases (AChE, BChE), α- amylase, α-glucosidase and tyrosinase was assessed. Most of the species showed considerable antioxidant potential in the performed assays. In the DPPH assay, Ama exhibited the maximum activity (24.12 ± 2.24 mg TE/g sample), and the volatiles from Amu exhibited the highest activity (91.54 mgTE/g oil) in the ABTS radical scavenging assay. The effect was more evident in both CUPRAC and FRAP assays, where both Ale and Ama showed the strongest activity in comparison with the other tested species (84.06, 80.28 mgTE/g oil for CUPRAC and 49.47, 49.02 mgTE/g oil for FRAP, respectively). Asi demonstrated the strongest AChE (4.55 mg GALAE/g oil) and BChE (3.61 mg GALAE/g oil) inhibitory effect. Furthermore, the best tyrosinase inhibitory potential was observed for Ale (138.42 mg KAE/g). Accordingly, Astragalus species can be utilized as promising natural sources for many medicinally important components that could be tested as drug candidates for treating illnesses such as Alzheimer’s disease, diabetes mellitus and oxidative stress-related diseases.


2019 ◽  
Vol 5 (1) ◽  
Author(s):  
Praneetha Pallerla ◽  
Narsimha Reddy Yellu ◽  
Ravi Kumar Bobbala

Abstract Background The objective of the study is to evaluate the hepatoprotective activity of methanolic extract fractions of Lindernia ciliata (LC) and development of qualitative analytical profile of the bioactive fraction using HPLC fingerprinting analysis. All the fractions of methanolic extract of Lindernia ciliata (LCME) are assessed for their total phenolic, flavonoid contents and in vitro antioxidant properties by using DPPH, superoxide, nitric oxide, hydroxyl radical scavenging activities and reducing power assay. Acute toxicity study was conducted for all the fractions and the two test doses 50 and 100 mg/kg were selected for the hepatoprotective study. Liver damage was induced in different groups of rats by administering 3 g/kg.b.w.p.o. paracetamol and the effect of fractions were tested for hepatoprotective potential by evaluating serum biochemical parameters and histology of liver of rats. The effective fraction was evaluated for its antihepatotoxic activity against D-Galactosamine (400 mg/kg b.w. i.p.) and in vivo antioxidant parameters viz., Glutathione (GSH), Melondialdehyde (MDA) and Catalase (CAT) levels are estimated using liver homogenate. Results Among all the fractions, butanone fraction of LCME, (BNF-LCME) has shown better hepatoprotective activity and hence it is selected to evaluate the antihepatotoxicity against D-GaIN. The activity of BNF-LCME is well supported in in vitro and in vivo antioxidant studies and may be attributed to flavonoidal, phenolic compounds present in the fraction. Hence, BNF-LCME was subjected to the development of qualitative analytical profile using HPLC finger printing analysis. Conclusions All the fractions of LCME exhibited significant hepatoprotective activity and BNF-LCME (50 mg/kg) was identified as the most effective fraction.


Molecules ◽  
2019 ◽  
Vol 24 (6) ◽  
pp. 1109 ◽  
Author(s):  
Stefania Sut ◽  
Gokhan Zengin ◽  
Filippo Maggi ◽  
Mario Malagoli ◽  
Stefano Dall’Acqua

Triterpene acid and phenolic constituents from nine ancient varieties of apple (Malus domestica) fruits cultivated in Fanna, Friuli Venezia Giulia region, northeast Italy, were analyzed and compared with four commercial apples (‘Golden Delicious’, ‘Red Delicious’, ‘Granny Smith’ and ‘Royal Gala’). Total phenolic and flavonoid contents were measured by spectrophotometric assays. The quali-quantitative fingerprint of secondary metabolites including triterpene acid was obtained by LC-DAD-(ESI)-MS and LC-(APCI)-MS, respectively. Based on the two LC-MS datasets, multivariate analysis was used to compare the composition of ancient fruit varieties with those of four commercial apples. Significant differences related mainly to the pattern of triterpene acids were found. Pomolic, euscaphyc, maslinic and ursolic acids are the most abundant triterpene in ancient varieties pulps and peels, while ursolic and oleanolic acids were prevalent in the commercial fruits. Also, the content of the phenolic compounds phloretin-2-O-xyloglucoside and quercetin-3-O-arabinoside was greater in ancient apple varieties. The antioxidant (radical scavenging, reducing power, metal chelating and phosphomolybdenum assays) and enzyme inhibitory effects (against cholinesterase, tyrosinase, amylase and glucosidase) of the samples were investigated in vitro. Antioxidant assays showed that the peels were more active than pulps. However, all the samples exhibited similar enzyme inhibitory effects. Ancient Friuli Venezia Giulia apple cultivars can be a source of chlorogenic acid and various triterpene acids, which are known for their potential anti-inflammatory activity and beneficial effects on lipid and glucose metabolism. Our results make these ancient varieties suitable for the development of new nutraceutical ingredients.


INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (04) ◽  
pp. 59-64
Author(s):  
Pratibha Thaware ◽  
Pushpa Karale ◽  
Mahesh Karale ◽  
Pranati Chavan

The objective of this study was to evaluate the phytochemical and pharmacological screening of fruit extracts of Aegle marmelos using various in vitro methods. The antioxidant activity of the extracts was evaluated by using DPPH free radical scavenging and reducing power method, while well diffusion method was used for antimicrobial activity. Phytochemical screening indicated the presence of flavonoids, and phenolics were abundantly present in methanolic and aqueous extracts of A. marmelos. Methanolic extract showed significant antioxidant potential, which was however inferior to that of ascorbic acid. The methanolic extract showed maximum zone of inhibition against the S. aureus (18 mm) and it was higher than that of the standard tetracycline. The HPLC data predict that the presence of scopoletin, marmelosin and umbelliferone, which may contribute to their pharmacological action.


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


2021 ◽  
Vol 18 ◽  
Author(s):  
Nayla Javed ◽  
Shakeel Ijaz ◽  
Naveed Akhtar ◽  
Haji Muhammad Shoaib Khan

Background: Arctostaphylos uva-ursi (AUU) being rich in polyphenols and arbutin is known to have promising biological activities and can be a potential candidate as a cosmaceutical. Ethosomes encourage the formation of lamellar-shaped vesicles with improved solubility and entrapment of many drugs including plant extracts. Objective: The objective of this work was to develop an optimized nanostructured ethosomal gel formulation loaded with AUU extract and evaluated for skin rejuvenation and depigmentation. Methods: AUU extract was tested for phenolic and flavonoid content, radical scavenging potential, reducing power activity, and in-vitro SPF (sun protection factor) estimation. AUU loaded 12 formulations were prepared and characterized by SEM (scanning electron microscopy), vesicular size, zeta potential, and entrapment efficiency (%EE). The optimized formulation was subjected to non-invasive in-vivo investigations after incorporating it into the gel system and ensuring its stability and skin permeation. Results: Ethosomal vesicles were spherical in shape and Zeta size, zeta potential, PDI (polydispersity index), % EE and in-vitro skin permeation of optimized formulation (F3) were found to be 114.7nm, -18.9mV, 0.492, 97.51±0.023%, and 79.88±0.013% respectively. AUU loaded ethosomal gel formulation was stable physicochemically and exhibited non-Newtonian behavior rheologically. Moreover, it significantly reduced skin erythema, melanin as well as sebum level and improved skin hydration and elasticity. Conclusion: A stable AUU based ethosomal gel formulation could be a better vehicle for phytoextracts than conventional formulations for cosmeceutical applications such as for skin rejuvenation and depigmentation etc.


2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Kenza Ammor ◽  
Dalila Bousta ◽  
Sanae Jennan ◽  
Bahia Bennani ◽  
Abdellah Chaqroune ◽  
...  

The aim of this study is to investigate in vitro antioxidant and antibacterial activities of the aqueous and hydroethanolic extracts for aerial parts of Herniaria hirsuta. Extracts were screened for their possible antioxidant activities by three tests: DPPH free radical-scavenging, reducing power, and molybdenum systems. The screening of antibacterial activity of extracts was individually evaluated against sixteen bacteria species using a disc diffusion method. Flavonoids, total phenols, and tannins content were performed for both extracts. It shows higher content in the hydroethanolic extract. The hydroethanolic extract showed a significant antioxidant activity for the three methods studies to the aqueous extract, but nonsignificant results compared to the reference (BHT). However, both extracts have negative effect on the strains studies for the antibacterial activity.


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