scholarly journals Anti-Oxidant and Tyrosinase Inhibitory In Vitro Activity of Amino Acids and Small Peptides: New Hints for the Multifaceted Treatment of Neurologic and Metabolic Disfunctions

Antioxidants ◽  
2018 ◽  
Vol 8 (1) ◽  
pp. 7 ◽  
Author(s):  
Grazia Luisi ◽  
Azzurra Stefanucci ◽  
Gokhan Zengin ◽  
Marilisa Dimmito ◽  
Adriano Mollica

Oxidative damage is among the factors associated with the onset of chronic pathologies, such as neurodegenerative and metabolic diseases. Several classes of anti-oxidant compounds have been suggested as having a protective role against cellular stressors, but, in this perspective, peptides’ world represents a poorly explored source. In the present study, the free radical scavenging properties, the metal ion reducing power, and the metal chelating activity of a series of sulfurated amino acids and tripeptides were determined in vitro through canonical assays (DPPH, ABTS, CUPRAC, FRAP, PM, and EECC) and estimated in comparison with the corresponding activities of synthetic peptide semicarbazones, incorporating the peculiar non-proteinogenic amino acid, tert-leucine (tLeu). The compounds exhibited remarkable anti-oxidant properties. As expected, sulfurated compounds 1–5 were found to be the most efficient radical scavengers and strongest reductants. Nevertheless, tLeu-containing peptides 7 and 8 disclosed notable metal reducing and chelating activities. These unprecedented results indicate that tLeu-featuring di- and tripeptide backbones, bearing the semicarbazone chelating moiety, are compatible with the emergence of an anti-oxidant potential. Additionally, when tested against a panel of enzymes usually targeted for therapeutic purposes in neurodegenerative and metabolic disorders, all samples were found to be good inhibitors of tyrosinase.

2021 ◽  
Vol 26 ◽  
pp. 2515690X2110366
Author(s):  
Hope Onohuean ◽  
Abdullateef I. Alagbonsi ◽  
Ibe M. Usman ◽  
Keneth Iceland Kasozi ◽  
Athanasios Alexiou ◽  
...  

Background. Annona muricata and Khaya grandifoliola are ethnomedicinally used for the treatment of malaria and have been experimentally shown to have an anti-plasmodial effect, but the mechanisms involved are not fully understood. This study investigated the effect of the ethanol extracts of their leaves on parasitemia, radical scavenging and cytokines in Plasmodium berghei ANKA-infected BALB/c mice. Methods. BALB/c mice were infected with P. berghei and treated with chloroquine, A. muricata or K. grandifoliola extract for 4 days. The percentage of parasitemia and the level of cytokine expression were determined after treatment. Trace element, phytochemical and nitric oxide (NO) scavenging activity, 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging properties assays were done to study the antioxidant effects of AN and KG in vitro. Results. P. berghei consistently increased parasitemia in BALB/c mice. The tested doses (100-, 200-, and 400 mg/kg) of A. muricata and K. grandifoliola attenuated the P. berghei-induced elevation of parasitemia and cytokines (TNF-α, IL-5, and IL-6) in vivo during the experimental period, though not as much as chloroquine. Moreover, both extracts scavenged the DPPH and NO radicals, though A. muricata had more anti-oxidant effect than K. grandifoliola in-vitro. Conclusion. The ethanol extracts of A. muricata and K. grandifoliola reduce parasitemia in P. berghei-treated mice BALB/c by scavenging free radicals and reducing cytokines, though the extracts were not as effective as chloroquine.


Author(s):  
Suseela V. ◽  
Sushmita L. ◽  
Bharatkumar R. ◽  
Nirmaladevi R.

The present study was carried out to elucidate the in vitro free radical scavenging potential of various extracts of Tabebuia roseo-alba leaves. Assays for radical scavenging, such as DPPH, ABTS+, hydroxyl, hydrogen peroxide, superoxide, nitric oxide assay and reducing power activity were performed using standard protocols and the results were compared with standard ascorbic acid. Among the various extracts used the ethanolic extract of T. roseo-alba exhibited efficient scavenging potential with lowest EC50 value proving its antioxidant potential. Leaves of T. roseo-alba have strong free radical scavenging properties and thus can be used as a potential antioxidant to resolve diseases that are associated with oxidative stress including diabetes and other age related disorders.


2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Shashank Kumar ◽  
Ramesh Kumar ◽  
Astha Dwivedi ◽  
Abhay K. Pandey

The present study reports thein vitroantioxidant, antibacterial, and cytotoxic potential ofSyngonium podophyllum(SP) andEichhornia crassipes(EC) leaf aqueous extracts as well as theirin vivoeffect on oxidative stress and hepatic biomarkers in isoniazid induced rats. Phytochemical screening of extracts revealed the presence of flavonoids, terpenoids, reducing sugars, alkaloids, and saponins. Phenolic content in SP and EC extracts was5.36±0.32and10.63±0.13 mg PGE/g, respectively, while flavonoid content was1.26±0.03and0.51±0.03 μg QE/mg, respectively. EC extract exhibited comparatively better antioxidant activity as indicated by reducing power (0.197–0.775), DPPH radical scavenging potential (11%–96%), and metal ion chelating ability (42%–93%). Both the extracts provided 13%–65% protection against lipid peroxidation in rat tissue (liver, kidney, and brain) homogenate. SP and EC extracts exhibited 51% and 43% cytotoxicity against lung cancer (NCI-H322) cell line, respectively. Both extracts demonstrated considerable antibacterial activity againstProteus vulgaris,Salmonella typhi, andBordetella bronchiseptica. Coadministration ofE. crassipesextract with isoniazid in rats accounted for 46% decrease in malondialdehyde content and 21% increase in FRAP value of plasma. It also mitigated the isoniazid induced alterations in serum enzymes (SGOT, SGPT, and ALP), total bilirubin, creatinine, and hemoglobin contents.S. podophyllumextract was found to be hepatotoxic.


2016 ◽  
Vol 11 ◽  
pp. S61-S67 ◽  
Author(s):  
Jinpeng Wang ◽  
Lian Zhang ◽  
Zhengyu Jin

Low-molecular-weight chondroitin sulfate was obtained by degradation of chondroitin sulfate using hyaluronidase. Then, separated with sephadex G25, DEAE-52, and finally purified with AKATA superpeptide separation system and fluorescence-assisted carbohydrate electrophoresis. The main compo-nents detected by high performance gel-filtration chromatography were disaccharide, tetrasaccharide, hexasaccharide with molecular weight of 521, 1024 and 1527 Da, respectively. The anti-oxidant activity of these three oligosaccharides in vitro showed that the reducing power (maximum value at 10 mg/mL) and superoxide anion radical scavenging abilities were increased (maximum value at 4 mg/mL) with an increased in their concentration. There were no significant differences of the anti-oxidant properties between those three oligosaccharides. 


Author(s):  
Nongalleima Khumukcham ◽  
T Ajungla ◽  
Chingakham Brajakishore Singh

Objective: The present investigation was designed for Gas Chromatography Mass Spectrometry (GCMS) based metabolite profiling of Citrus macroptera Montruz. Leaves and peel oils followed by assessment of in vitro antioxidant and anti-inflammatory activity.Methods: Essential oil was extracted from leaves and peels of Citrus macroptera Montruz. The oil samples were subjected to GCMS analysis using Shimadzu GCMS-QP2010 equiped with an AOC-2oi auto-injector and AOC-2os autosampler units. In vitro antioxidant activities were evaluated using DPPH radical scavenging, reducing power and nitric oxide reducing method. In vitro anti-inflammatory activity was evaluated using protease inhibitory assay, heat induced haemolysis and albumin denaturation assay.Results: Both the peels and leaves of Citrus macroptera Montruz. Yielded good amount of essential oil. 57 compounds each were identified from leaves as well as peel of C. macroptera. 10 common compounds have been detected in both the oil samples. Peels oil showed IC50 at 118.07 µg/ml and that of leaves showed IC50 at 252.93 µg/ml in DPPH (1, 1-diphenyl-2-picrylhydrazyl) assay. In reducing assay, peel and leaves oil showed IC50 at 122.5 µg/ml and 208.24 µg/ml. In albumin denaturation, the peels showed IC50 at 73.91 µg/ml and that of leaves showed IC50 at 87.48 µg/ml.Conclusion: The oil yield denotes peel as better source of volatile oil than leaves. Essential oil of peel showed more anti-oxidant and anti-inflammatory activity than that of leaves essential oil.


2018 ◽  
Vol 7 (3) ◽  
pp. 263-269
Author(s):  
Saraswathi K ◽  
◽  
Rajesh V ◽  
Saranya R ◽  
Arumugam P ◽  
...  

Plants have been used for thousands of years to flavour and conserve food, to treat health disorders and to prevent diseases including epidemics. The knowledge of the anti-oxidant properties has been a promising method of assessing free radicals damage. The aim of the present study was to evaluate the antioxidant activities of leaves of Canavalia cathartica and to identify the bioactive compounds by performing GC-MS analysis resulting in the presence of volatile and semi volatile compounds. The IC50 of DPPH˙ radical, ABTS˙+ radical cation, Nitric oxide radical scavenging assays were 84.03, 51.18 and 351.78µg/mL concentration respectively. Also, the IC50 of Phosphomolybdenum reduction and ferric reducing power assay were 81.53 and 87.64µg/mL concentration respectively. The results of this study portray the effective antioxidant activity of Canavalia cathartica and further studies are required to isolate the active compounds from various parts of this species and their mode of action. From the study it can be concluded that the plant might be promising as a curative for many diseases associated with free radicals


2018 ◽  
Vol 15 (2) ◽  
pp. 127-135 ◽  
Author(s):  
Parvesh Singh ◽  
Nomandla Ngcoya ◽  
Ramgopal Mopuri ◽  
Nagaraju Kerru ◽  
Neha Manhas ◽  
...  

Background: Diabetes Mellitus (DM) is a complex metabolic disease illustrated by abnormally high levels of plasma glucose or hyperglycaemia. Accordingly, several α-glucosidase inhibitors have been developed for the treatment of diabetes and other degenerative disorders. While, a coumarin ring has the privilege to represent numerous natural and synthetic compounds with a wide spectrum of biological activities e.g. anti-cancer, anti-HIV, anti-viral, anti-malarial, anti-microbial, anti-convulsant, anti-hypertensive properties. Besides this, coumarins have also shown potential to inhibit α-glucosidase leading to a generation of new promising antidiabetic agents. However, the testing of O-substituted coumarins for α-glucosidase inhibition has evaded the attention of medicinal chemists. Methods: For O-alkylation/acetylation reactions, the hydroxyl coumarins (A-B) initially activated by K2CO3 in dry DMF were reacted with variedly substituted haloalkanes at room temperature under nitrogen. The synthesized compounds were tested for their α-glucosidase (from Saccharomyces cerevisiae) inhibitory activity and anti-oxidant activity using DPPH radical scavenging activity. In silico docking simulations were conducted using CDocker module in DS (Accelrys) to explore the binding modes of the representative compounds in the catalytic site of α-glucosidase. Results: All the coumarin analogues (A1, B1, A2-A10, B2-B8) including their precursors (A-B) were evaluated for their in vitro α-glucosidase inhibition using acarbose as a standard inhibitor. All the mono O-alkylated coumarins (except A1) showed significant (p <0.05) α-glucosidase inhibition relative to the hydroxyl coumarin (A) with IC50 values ranging between 11.084±0.117 to 145.24± 29.22 µg/mL. Compound 7-(benzyloxy)-4, 5-dimethyl-2H-chromen-2-one (A9) bearing a benzyl group (Ph-CH2-) at position 7 showed a remarkable (p <0.05) increase in the activity (IC50 = 11.084±0.117 µg/mL), almost four-fold more than acarbose (IC50 = 40.578±5.999 µg/mL). The introduction of –NO2 group dramatically improved the anti-oxidant activity of coumarin, while the O-alkylation/acetylation decreased the activity. Conclusion: The present study describes the synthesis of functionalized coumarins and their evaluation for α-glucosidase inhibition and antioxidant activity under in vitro conditions. Based on IC50 data, the mono O-alkylated coumarins were observed to be stronger inhibitors of α-glucosidase with respect to their bis O-alkylated analogues. Coumarin (A9) bearing O-benzyloxy group displayed the strongest α-glucosidase inhibition, even higher than the standard inhibitor acarbose. The coumarin (A10) bearing –NO2 group showed the highest anti-oxidant activity amongst the synthesized compounds, almost comparable to the ascorbic acid. Finally, in silico docking simulations revealed the role of hydrogen bonding and hydrophobic forces in locking the compounds in catalytic site of α-glucosidase.


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.


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