scholarly journals Synthesis, Structure and Evaluation of the N-(2-Acetyl-4-(styryl)phenyl)-4-benzenesulfonamide Derivatives for Anticholinesterase and Antioxidant Activities

Crystals ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 341
Author(s):  
Malose J. Mphahlele ◽  
Samantha Gildenhuys ◽  
Sizwe J. Zamisa
Keyword(s):  
Molecular Level ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
X Ray Diffraction ◽  
Enzymatic Assays ◽  
X Ray ◽  
Protein Ligand Interactions ◽  
Ligand Interactions

N-(2-Acetyl-4-bromophenyl)-4-methylbenzenesulfonamide (2) was transformed into 5-(4-methoxymethylstyryl)-2-(p-tolylsulfonamido)acetophenone (3a) and 5-(4- trifluoromethylstyryl)-2-(p-tolylsulfonamido)acetophenone (3b). Their structures were determined using a combination of NMR (1H & 13C) and mass spectroscopic as well as single crystal X-ray diffraction techniques. These compounds and the corresponding precursor, 2-amino-5-bromoacetophenone (1), were evaluated through enzymatic assays in vitro for inhibitory effect against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities as well as antioxidant effect through the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide (NO) free radical scavenging assays. Molecular docking was performed on 3a to determine plausible protein–ligand interactions on a molecular level. Their drug likeness properties (absorption, distribution, metabolism, and excretion) and ability to cross the blood–brain barrier (BBB) have also been predicted at theoretical level.

Aqueous extracts of avocado pear (Persea americana Mill.) leaves and seeds exhibit anti-cholinesterases and antioxidant activities in vitro

2016 ◽  
Vol 27 (2) ◽  
Author(s):  
Ganiyu Oboh ◽  
Veronica O. Odubanjo ◽  
Fatai Bello ◽  
Ayokunle O. Ademosun ◽  
Sunday I. Oyeleye ◽  
...  
Keyword(s):  
Leaf Extract ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
Seed Extract ◽  
Persea Americana ◽  
Dependent Manner ◽  
Natural Treatment

AbstractAvocado pear (The inhibitory effects of extracts on AChE and BChE activities and antioxidant potentials (inhibition of FeThe extracts inhibited AChE and BChE activities and prooxidant-induced TBARS production in a dose-dependent manner, with the seed extract having the highest inhibitory effect and the leaf extract exhibiting higher phenolic content and radical scavenging abilities, but lower Fe chelation ability compared with that of the seed. The phytochemical screening revealed the presence of saponins, alkaloids, and terpenoids in both extracts, whereas the total alkaloid profile was higher in the seed extract than in the leaf extract, as revealed by GC-FID.The anti-cholinesterase and antioxidant activities of avocado leaf and seed could be linked to their phytoconstituents and might be the possible mechanisms underlying their use as a cheap and natural treatment/management of AD. However, these extracts should be further investigated in vivo.

scholarly journals In vitro gastrointestinal digestion of a bisdemethoxycurcumin-rich Curcuma longa extract and its oral bioavailability in rats

2021 ◽  
Vol 45 (1) ◽  
Author(s):  
Venkataramana Heggar Sudeep ◽  
Kuluvar Gouthamchandra ◽  
Siddappa Chandrappa ◽  
Puttaswamy Naveen ◽  
Budanuru Reethi ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Curcuma Longa ◽  
Radical Scavenging ◽  
Relative Bioavailability ◽  
Inhibitory Effect ◽  
Gastrointestinal Digestion ◽  
Potential Health ◽  
Turmeric Extract ◽  
In Vitro Gastrointestinal Digestion

Abstract Background Nonetheless curcumin has potential health benefits, its low bioavailability limits the application of conventional turmeric extract with curcumin as major curcuminoid. This is a comparative study to assess the stability, bioaccessibility and biological activity of BDMC in standardized C. longa extract (REVERC3) relative to curcumin in regular turmeric extract (RTE). Here we report the preparation of a standardized Curcuma longa extract (REVERC3™) standardized to contain 75 ± 5 w/w % bisdemethoxycurcumin (BDMC), 1.2 ± 0.8 w/w % curcumin and 10 ± 5 w/w % demethoxycurcumin (DMC). The turmeric extracts were subjected to in vitro gastrointestinal digestion and the curcuminoids in undigested and digested samples were analyzed using HPLC to determine the bioaccessibility. Further, the undigested and digested samples were evaluated for lipase inhibition and antioxidant activities. Male Wistar rats were administered with single dose (1000 mg/kg) of standardized C. longa extract and RTE to determine the plasma concentration of BDMC and curcumin respectively at different time points using LCMS/MS. Results The bioaccessibility of BDMC was significantly higher than curcumin (p < 0.05). BDMC was found superior to curcumin having significant lipase inhibitory effect (p < 0.01), ABTS radical scavenging (p < 0.05), and nitric oxide scavenging activities (p < 0.01). Interestingly, the relative bioavailability of BDMC in standardized C. longa extract was 18.76 compared to curcumin. The Cmax of BDMC was 4.4-fold higher than curcumin. Conclusion BDMC is reported to have higher bioaccessibility and bioavailability than curcumin. Our findings rationalize use of BDMC-enriched standardized C. longa extract for improved physiological benefits counteracting the regular turmeric extract with less bioavailable curcumin as major curcuminoid.

scholarly journals In Vitro Studies of the Antimicrobial and Free-Radical Scavenging Potentials of Silver Nanoparticles Biosynthesized From the Extract of Desmostachya bipinnata

2018 ◽  
Vol 13 ◽  
pp. 117739011878287 ◽  
Author(s):  
Sitaramanjaneya Reddy Guntur ◽  
NS Sampath Kumar ◽  
Manasa M Hegde ◽  
Vijaya R Dirisala
Keyword(s):  
Silver Nanoparticles ◽  
Green Synthesis ◽  
Radical Scavenging ◽  
X Ray Diffraction ◽  
X Ray ◽  
Gram Positive Bacteria ◽  
Antimicrobial Studies ◽  
Hepg2 Cell Lines ◽  
Hydrazyl Radical

The aim of this study was to perform green synthesis of silver nanoparticles (AgNPs) from the leaf extract of Desmostachya bipinnata (Dharba), a medicinally important herb which is widely used across India. Synthesized AgNPs were analyzed by UV-Visible spectroscopy, X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), and energy dispersive X-ray spectroscopy (EDAX). The results have confirmed that green synthesis of AgNPs leads to the fabrication of sphere-shaped particles with a diameter of 53 nm. Furthermore, these AgNPs were subjected to antioxidant and antimicrobial studies against gram-negative and gram-positive bacteria, where AgNPs at a concentration of 20 mg/mL showed highest zone of inhibition. Synthesized AgNPs were evaluated for their antioxidant activity by 1, 1-diphenyl-2-picryl hydrazyl radical (DPPH), H2O2, and superoxide inhibiting assays; increasing concentration has showed increase in scavenging ability. Cell toxicity was assessed on HepG2 cell lines, and synthesized nanoparticles at a concentration of 128 μg/mL produced significant reduction in viability of Hep cells ( P < .05). The availability of Dharba throughout the year and the eco-friendly approach in the synthesis of AgNPs coupled with bioactivity has demonstrated its potential as a novel biomaterial which can be used for various biomedical applications.

In vitro Antioxidant and Antiproliferative Activity of the Stem Extracts from Graptopetalum paraguayense

2008 ◽  
Vol 36 (02) ◽  
pp. 369-383 ◽  
Author(s):  
Shu-Ju Chen ◽  
Jing-Gung Chung ◽  
Yun-Chin Chung ◽  
Su-Tze Chou
Keyword(s):  
Lipid Peroxidation ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
Hep G2 ◽  
Hep G2 Cells ◽  
Inhibition Concentration ◽  
G1 Phase Arrest ◽  
Antioxidant Reactions

This study was aimed to evaluate the antioxidant abilities of water (SGWE), 50% ethanolic (SGE50) and 95% ethanolic (SGE95) extracts from the stem of Graptopetalum paraguayense, and the extract with the highest antioxidant activity was assayed for its inhibitory effect on proliferation of human hepatoma (Hep G2) cell line. Antioxidant abilities of extracts were assessed their radical-scavenging abilities and effects on Fe /ascorbate-induced lipid peroxidation in a liposome model system. The results of this study showed that antioxidant activities were increased with the increase of the extracts concentrations, and the activities correlated with both the total phenol and anthocyanin contents. A comparison of the 50% inhibition concentration (IC50) values of different antioxidant reactions revealed that SGWE was the more effective at scavenging superoxide anion radical and preventing lipid peroxidation than SGE50 and SGE95 ( p < 0.05). The flow cytometry results indicated that SGWE lowered cell viability, and induced G1 phase arrest and apoptosis in Hep G2 cells. These results demonstrated the antioxidatant and anti-hepatoma potential of stem of Graptopetalum paraguayense.

Phenolic and Flavonoids Analysis of Pomegranate Peel Extracts and their Antiniflammatory and Antioxidant Activities

2019 ◽  
Vol 10 (01) ◽  
Author(s):  
Qabaha K. ◽  
Al-Rimawi F ◽  
Nusseibeh S. ◽  
Abbadi J J. ◽  
Abu-Lafi S.
Keyword(s):  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
Total Phenolic ◽  
Polymorphonuclear Cells ◽  
Pomegranate Peel ◽  
Radical Scavenging Ability ◽  
Pomegranate Peel Extract ◽  
Peel Extract

An in-vitro evaluation of the anti-inflammatory and antioxidant activities of pomegranate peel extract from Palestine were investigated. In parallel, the total phenolic content (TPC) and the total flavonoids content (TFC) were measured. The antioxidant activities were determined spectrophotometrically by DPPH, FRAP, CUPRAC and the ABTS methods. The phenolic and flavonoid contents were separated and partially identified using HPLC and LC-MS. In-vitro inhibitory effect of the extract on production of Interlukin-6 (Il-6) and Tumor Necrosis Factor-α (TNF-α) by Lipopolysacaride (LPS)-induced polymorphonuclear Cells (PMNCs) was evaluated. Pomegranate peel extract was found to have strong antiinflamatory activity as revealed by the reduction in the levels of IL-6 and TNF-alfa. It was also found that it is rich in phenoloic and flavonoids that enhanced its reducing activity and free radical scavenging ability.

scholarly journals RADICAL SCAVENGING AND DISINFECTANT EFFECT OF ESSENTIAL OIL FROM MOROCCAN MENTHA PULEGIUM

2016 ◽  
Vol 8 (9) ◽  
pp. 116 ◽  
Author(s):  
Marwa Chraibi ◽  
Kawtar Fikri Benbrahim ◽  
Douâae Ou-yahyia ◽  
Mounyr Balouiri ◽  
Abdellah Farah
Keyword(s):  
Essential Oil ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
Mentha Pulegium ◽  
Medicinal And Aromatic Plants ◽  
Scavenging Effect ◽  
Microdilution Method ◽  
Broth Microdilution Method

<p><strong>Objective: </strong>As part of the valorization of medicinal and aromatic plants in Morocco, this study aims to investigate the chemical composition, the antimicrobial and the antioxidant activities of <em>Mentha pulegium </em>essential oil.</p><p><strong>Methods: </strong>Essential oil of <em>M. pulegium </em>from Oued Laou region (Morocco) was screened for its antimicrobial activity against seven bacteria and two fungi using broth microdilution method. The radical scavenging effect was used to assess <em>in vitro </em>antioxidant capacity of this oil.</p><p><strong>Results: </strong>The tested essential oil exhibited strong inhibitory effect against all tested microorganisms with minimum inhibitory concentrations ranging from 0.003% to 1% (v/v) except for <em>Pseudomonas aeruginosa</em>. Moreover, the studied essential oil exhibited radical scavenging power with the half maximal inhibitory concentration of 2 mg/ml.</p><p><strong>Conclusion: </strong>These findings showed that the studied essential oil has both an antimicrobial and antioxidant potential, which is very rare. Thus, it reinforces its use as an effective, eco-friendly preservative agent in food and cosmetic field.</p><p> </p>

scholarly journals Synthesis of a Small Library of Nature-Inspired Xanthones and Study of Their Antimicrobial Activity

Molecules ◽  
2020 ◽  
Vol 25 (10) ◽  
pp. 2405 ◽  
Author(s):  
Diana I. S. P. Resende ◽  
Patrícia Pereira-Terra ◽  
Joana Moreira ◽  
Joana Freitas-Silva ◽  
Agostinho Lemos ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Biofilm Formation ◽  
Multidrug Resistant ◽  
Inhibitory Effect ◽  
X Ray Diffraction ◽  
X Ray ◽  
Xanthone Derivatives ◽  
Potent Inhibitory Effect ◽  
Resistant Strains

A series of thirteen xanthones 3–15 was prepared based on substitutional (appendage) diversity reactions. The series was structurally characterized based on their spectral data and HRMS, and the structures of xanthone derivatives 1, 7, and 8 were determined by single-crystal X-ray diffraction. This series, along with an in-house series of aminated xanthones 16–33, was tested for in-vitro antimicrobial activity against seven bacterial (including two multidrug-resistant) strains and five fungal strains. 1-(Dibromomethyl)-3,4-dimethoxy-9H-xanthen-9-one (7) and 1-(dibromomethyl)-3,4,6-trimethoxy-9H-xanthen-9-one (8) exhibited antibacterial activity against all tested strains. In addition, 3,4-dihydroxy-1-methyl-9H-xanthen-9-one (3) revealed a potent inhibitory effect on the growth of dermatophyte clinical strains (T. rubrum FF5, M. canis FF1 and E. floccosum FF9), with a MIC of 16 µg/mL for all the tested strains. Compounds 3 and 26 showed a potent inhibitory effect on two C. albicans virulence factors: germ tube and biofilm formation.

Comparative effects of berberine and piperine on the neuroprotective potential of neostigmine

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Stephen Adeniyi Adefegha ◽  
Ganiyu Oboh ◽  
Bathlomew Maduka Okeke
Keyword(s):  
Neurological Disorders ◽  
Antioxidant Activities ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Complementary Therapy ◽  
Inhibitory Effect ◽  
Distilled Water ◽  
Underlying Mechanisms ◽  
Reducing Properties

Abstract Objectives This study examined effect of berberine and piperine on neuroprotective potential of neostigmine in the management of neurological disorders. Methods Berberine and neostigmine were weighed (30 g), dissolved in distilled water (30 mL) separately, while, 30 mg piperine was dissolved in ethanol (0.45 mL), made up to 30 mL with distilled water. Antioxidant activities in 2, 2-diphenyl-1-picrylhydrazyl radical (DPPH), 2, 2-azinobis (3-ethylbenzothiazoline-6-sulfonate) radical (ABTS), Fe-chelation, ferric reducing properties (FRAP), nitric oxide (NO) and hydroxyl (OH) radical scavenging abilities and Fe2+, cisplatin and sodium nitroprusside (SNP) induced lipid peroxidation (LPO), and acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and monoamine oxidase (MAO) activities were assessed in vitro. Results The result revealed that tested compounds inhibited enzymes activities dose-dependently. However, berberine (IC50=0.17 mg/mL) had slight higher AChE inhibitory effect than piperine and neostigmine (p<0.05). Also, berberine had the highest BChE inhibitory effect (IC50=0.16 mg/mL) while piperine exhibited the highest MAO inhibitory effect (IC50=0.21 mg/mL). Berberine, piperine and neostigmine exhibited high antioxidant properties and inhibited Fe2+, cisplatin and SNP induced LPO. Conclusions Both alkaloids demonstrated antiradical scavenging ability comparable to neostigmine action against Alzheimer’s disease (AD). The modulatory and antioxidant berberine and piperine properties on these enzymes (AChE, BChE and MAO) could be possible underlying mechanisms in employing these compounds as a complementary therapy in neurodegenerative diseases (NDDs) management.

A New Purine Derivative from the Roots of Phyllanthus flexuosus

2018 ◽  
Vol 13 (1) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Guanlin Zhu ◽  
Hongying Wang ◽  
Kunrong Gan ◽  
Heng Gao ◽  
Wei Li
Keyword(s):  
Spectroscopic Analysis ◽  
Carcinoma Cell ◽  
Inhibitory Effect ◽  
X Ray Diffraction ◽  
Purine Derivative ◽  
X Ray ◽  
Carcinoma Cell Lines ◽  
Human Hepatocellular Carcinoma Cell ◽  
Different Levels

A new purine derivative, 1-methyl-3-isopentenylisoguanine (1), together with six known compounds (2-7), was isolated from the roots of Phyllanthus flexuosus. The newly isolated structure was established by means of extensive spectroscopic analysis and single-crystal X-ray diffraction experiment. All isolates were evaluated for their in vitro cytotoxicities against two human hepatocellular carcinoma cell lines (HepG2 and SMMC-7721) by CCK-8 assays. Among them, three cleistanthane diterpenes (2–4) exhibited different levels of cytotoxicities against these cells with IC50 values ranging from 27.34 to 53.28 μM. Furthermore, acetylcholinesterase inhibitory effect for the new purine derivative was also assessed.

scholarly journals Exploring Biological Activity of 4-Oxo-4H-furo[2,3-h]chromene Derivatives as Potential Multi-Target-Directed Ligands Inhibiting Cholinesterases, β-Secretase, Cyclooxygenase-2, and Lipoxygenase-5/15

Biomolecules ◽  
2019 ◽  
Vol 9 (11) ◽  
pp. 736
Author(s):  
Malose J. Mphahlele ◽  
Emmanuel N. Agbo ◽  
Samantha Gildenhuys ◽  
Itumeleng B. Setshedi
Keyword(s):  
Biological Activity ◽  
Radical Scavenging ◽  
Kinetic Studies ◽  
Halogen Bonding ◽  
Docking Studies ◽  
Cyclooxygenase 2 ◽  
Strong Electron ◽  
Protein Ligand Interactions ◽  
Ligand Interactions

A series of 5-oxo-5H-furo[3,2-g]chromene-6-carbaldehydes and their hydrazone derivatives were evaluated as potential multi-target-directed ligands in vitro against cholinesterases, β-secretase, cyclooxygenase-2, and lipoxygenase-15 (LOX-15), as well as for free radical-scavenging activities. The most active compounds against LOX-15 were also evaluated for activity against the human lipoxygenase-5 (LOX-5). Kinetic studies against AChE, BChE, and β-secretase (BACE-1) were performed on 2-(3-fluorophenyl)- (3b) and 2-(4-chlorophenyl)-6-[(4-trifluoromethylphenyl)hydrazonomethyl]furo[3,2-h]chromen-5-one (3e) complemented with molecular docking (in silico) to determine plausible protein-ligand interactions on a molecular level. The docking studies revealed hydrogen and/or halogen bonding interactions between the strong electron-withdrawing fluorine atoms of the trifluoromethyl group with several residues of the enzyme targets, which are probably responsible for the observed increased biological activity of these hydrazone derivatives. The two compounds were found to moderately inhibit COX-2 and lipoxygenases (LOX-5 and LOX-15). Compounds 3b and 3e were also evaluated for cytotoxicity against the breast cancer MCF-7 cell line and Hek293-T cells.

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