scholarly journals Biochemical Constituents of Phaleria macrocarpa (Leaf) Methanolic Extract Inhibit ROS Production in SH-SY5Y Cells Model

2020 ◽  
Vol 2020 ◽  
pp. 1-7
Author(s):  
Ibrahim Maina Hassan ◽  
Wan Norhamidah Wan Ibrahim ◽  
Ferdaus Binti Mohamat Yusuf ◽  
Siti Aqlima Ahmad ◽  
Syahida Ahmad

Background. Reactive oxygen species generation in mammalian cells profoundly affects several critical cellular functions, and the lack of efficient cellular detoxification mechanisms which remove these radicals may lead to several human diseases. Several studies show that ROS is incriminated as destructive agents in the context of the nervous system especially with advance in age leading to neurodegeneration. Current treatments of this disease are not effective and result in several side effects. Thus, the search for alternative medicines is in high demand. Therefore, the aim of this study is to evaluate the reactive oxygen inhibitory effect of Phaleria macrocarpa 80% (leaf) extract. Methods. The leaf was extracted with 80% methanol. Cytotoxicity studies were carried out using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), and ROS inhibitory activities were evaluated using dichlorofluorescein diacetate (DCF-DA) assay in the SH-SY5Y cells model. Results. The result revealed ROS inhibitory activities of the crude extract with highly significant differences at p < 0.001 between the group that were treated with crude extract only, the group treated with crude extract and exposed to H2O2, and the group exposed to H2O2 only as well as the group that were maintained in complete media. Bioactive compounds show the presence of vitexin and isovitexin following the HPLC method. Conclusion. High antioxidant activities and low toxicity effect of this crude revealed its high benefit to be used as natural medicine/supplements.

2011 ◽  
Vol 4 (1) ◽  
pp. 15-19 ◽  
Author(s):  
Antonin Lojek ◽  
Milan Číž ◽  
Michaela Pekarová ◽  
Gabriela Ambrožová ◽  
Ondřej Vašíček ◽  
...  

Modulation of metabolic activity of phagocytes by antihistaminesThe purpose of the study was to investigate the effects of H1-antihistamines of the 1stgeneration (antazoline, bromadryl, brompheniramine, dithiaden, cyclizine, chlorcyclizine, chlorpheniramine, clemastine) and the 2ndgeneration (acrivastine, ketotifen, and loratadine) on the respiratory burst of phagocytes. Reactive oxygen species generation in neutrophils isolated from rat blood was measured using luminol-enhanced chemiluminescence. Changes in nitrite formation and iNOS protein expression by RAW 264.7 macrophages were analysed using Griess reaction and Western blotting. The antioxidative properties of drugs in cell-free systems were detected spectrophotometrically, luminometrically, fluorimetrically, and amperometrically. The majority of the H1-antihistamines tested (bromadryl, brompheniramine, chlorcyclizine, chlorpheniramine, clemastine, dithiaden, and ketotifen) exhibited a significant inhibitory effect on the chemiluminescence activity of phagocytes. H1-antihistamines did not show significant scavenging properties against superoxide anion and hydroxyl radical, thus this could not contribute to the inhibition of chemiluminescence. H1-antihistamines had a different ability to modulate nitric oxide production by LPS-stimulated macrophages. Bromadryl, clemastine, and dithiaden were the most effective since they inhibited iNOS expression, which was followed by a significant reduction in nitrite levels. H1-antihistamines had no scavenging activity against nitric oxide. It can be concluded that the effects observed in the H1-antihistamines tested are not mediated exclusively via H1-receptor pathway or by direct antioxidative properties. Based on our results, antihistamines not interfering with the microbicidal mechanisms of leukocytes (antazoline, acrivastine and cyclizine) could be used preferentially in infections. Other antihistamines should be used, under pathological conditions accompanied by the overproduction of reactive oxygen species.


Cells ◽  
2018 ◽  
Vol 7 (12) ◽  
pp. 274 ◽  
Author(s):  
Saima Kausar ◽  
Feng Wang ◽  
Hongjuan Cui

Mitochondria are dynamic cellular organelles that consistently migrate, fuse, and divide to modulate their number, size, and shape. In addition, they produce ATP, reactive oxygen species, and also have a biological role in antioxidant activities and Ca2+ buffering. Mitochondria are thought to play a crucial biological role in most neurodegenerative disorders. Neurons, being high-energy-demanding cells, are closely related to the maintenance, dynamics, and functions of mitochondria. Thus, impairment of mitochondrial activities is associated with neurodegenerative diseases, pointing to the significance of mitochondrial functions in normal cell physiology. In recent years, considerable progress has been made in our knowledge of mitochondrial functions, which has raised interest in defining the involvement of mitochondrial dysfunction in neurodegenerative diseases. Here, we summarize the existing knowledge of the mitochondrial function in reactive oxygen species generation and its involvement in the development of neurodegenerative diseases.


Horticulturae ◽  
2021 ◽  
Vol 7 (12) ◽  
pp. 555
Author(s):  
Vo Thi Tu Anh ◽  
Dai Thi Xuan Trang ◽  
Kaeko Kamei ◽  
Tran Chi Linh ◽  
Nguyen Huan Pham-Khanh ◽  
...  

The flowers of M. velutina were extracted with ethanol to obtain a crude extract that was consecutively extracted using n-hexane, dichloromethane, ethyl acetate and water. The crude extract and fractions were studied for the chemical composition and antioxidant and antidiabetic activities. The extracts had various phytoconstituents, namely steroids, flavonoids, tannins, saponins, alkaloids and glycosides. The aqueous extract had the highest total polyphenol (12.6 mg GAE/g extract) and total flavonoid (205.6 mg QE/g extract) content. The aqueous extract exhibited the strongest antioxidant activities in the ferric reducing antioxidant power assay (EC50 = 4.0 µg/mL), reducing power assay (EC50 = 78.1 µg/mL), 2,2-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid radical cation assay (EC50 = 48.2 µg/mL), total antioxidant capacity assay (EC50 = 8.7 µg/mL) and 1,1-diphenyl-2-picrylhydrazyl assay (EC50 = 9.3 µg/mL). The aqueous extract showed the strongest inhibitory effect on the activity of α-amylase (IC50 = 376.6 μg/mL) and α-glucosidase (IC50 = 69.7 μg/mL). The results showed that the aqueous extract of M. velutina flowers can be a promising candidate for the control of diabetes and oxidative stress. This is the first report about the chemical components and antioxidant and antidiabetic activities of M. velutina flower extracts.


The eff ect of the non-opiate analog of leu-enkephalin (peptide NALE: Phe – D – Ala – Gly – Phe – Leu – Arg) on the reactive oxygen species generation in the heart of albino rats in the early postnatal period was studied. Peptide NALE was administered intraperitoneally in the dose of 100 μ/kg daily from 2 to 6 days of life. Reactive oxygen species generation was assessed by chemiluminescence in the heart homogenates of 7-day-old animals. Decreasing of reactive oxygen species generation nearly by 30 % and an increasing in antioxidant system activity by the 20-27 %, compared with the control parameters, were found. The antioxidant eff ect of peptide NALE is associated with the presence of the amino acid Arg in the structure of the peptide. An analogue of NALE peptide, devoid of Arg (peptide Phe – D – Ala – Gly – Phe – Leu – Gly), had a signifi cant lower antioxidant eff ect. The NO-synthase inhibitor NG-nitro-L-arginine methyl ester (L-NAME) in the dose 50 mg/kg, administered with NALE peptide, reduced the severity of the NALE antioxidant eff ect. The results of the study suggest that the pronounced antioxidant eff ect of NALE peptide in the heart of albino rats, at least in part, is due to the interaction with the nitric oxide system.


2019 ◽  
Vol 16 (3) ◽  
pp. 256-272
Author(s):  
Uzma Salar ◽  
Khalid Mohammed Khan ◽  
Syeda Abida Ejaz ◽  
Abdul Hameed ◽  
Mariya al-Rashida ◽  
...  

Background: Alkaline Phosphatase (AP) is a physiologically important metalloenzyme that belongs to a large family of ectonucleotidase enzymes. Over-expression of tissue non-specific alkaline phosphatase has been linked with ectopic calcification including vascular and aortic calcification. In Vascular Smooth Muscles Cells (VSMCs), the high level of Reactive Oxygen Species (ROS) resulted in the up-regulation of TNAP. Accordingly, there is a need to identify highly potent and selective inhibitors of APs for treatment of disorders related to hyper activity of APs. </P><P> Methods: Herein, a series of coumarinyl alkyl/aryl sulfonates (1-40) with known Reactive Oxygen Species (ROS) inhibition activity, was evaluated for alkaline phosphatase inhibition against human Tissue Non-specific Alkaline Phosphatase (hTNAP) and Intestinal Alkaline Phosphatase (hIAP). </P><P> Results: With the exception of only two compounds, all other compounds in the series exhibited excellent AP inhibition. For hIAP and hTNAP inhibition, IC50 values were observed in the range 0.62-23.5 &#181;M, and 0.51-21.5 &#181;M, respectively. Levamisole (IC50 = 20.21 &#177; 1.9 &#181;M) and Lphenylalanine (IC50 = 100.1 &#177; 3.15 &#181;M) were used as standards for hIAP and hTNAP inhibitory activities, respectively. 4-Substituted coumarinyl sulfonate derivative 23 (IC50 = 0.62 &#177; 0.02 &#181;M) was found to be the most potent hIAP inhibitor. Another 4-substituted coumarinyl sulfonate derivative 16 (IC50 = 0.51 &#177; 0.03 &#181;M) was found to be the most active hTNAP inhibitor. Some of the compounds were also found to be highly selective inhibitors of APs. Detailed Structure-Activity Relationship (SAR) and Structure-Selectivity Relationship (SSR) analysis were carried out to identify structural elements necessary for efficient and selective AP inhibition. Molecular modeling and docking studies were carried out to rationalize the most probable binding site interactions of the inhibitors with the AP enzymes. In order to evaluate drug-likeness of compounds, in silico ADMETox evaluation was carried out, most of the compounds were found to have favorable ADME profiles with good predicted oral bioavailability. X-ray crystal structures of compounds 38 and 39 were also determined. </P><P> Conclusion: Compounds from this series may serve as lead candidates for future research in order to design even more potent, and selective inhibitors of APs.


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