scholarly journals Antioxidant Properties of Synthesized Bicyclic Thiazolopyrimidine Derivatives as Possible Therapeutic Agents

2018 ◽  
Vol 9 (1) ◽  
pp. 113 ◽  
Author(s):  
Darinka Gjorgieva Ackova ◽  
Jelena Kotur-Stevuljevic ◽  
Chandra Bhushan Mishra ◽  
Pratibha Mehta Luthra ◽  
Luciano Saso

Oxidant/antioxidant imbalance in the body has been implicated as one of the pathophysiological mechanisms leading to disease development. Therefore, we searched for a good antioxidant candidate that can be used as a therapeutic agent alone or in combination with other reported drugs. Earlier, we reported the A2A receptor antagonist properties of 7-Imino-3-substituted-2-thioxo-3,7-dihydro-2H-thiazolo[4,5-d]pyrimidin-6-yl)-urea derivatives (compounds 1–12) and the neuroprotective effect of compound 2. Therefore, in the present work, the antioxidant potential of compounds 1–12 was studied. Compounds 1–12 were screened using different (red/ox) tests, such as the Ferric Reducing Antioxidant Power (FRAP) assay, to determine total antioxidant activity, redox status tests (with and without prooxidants) such as Advanced Oxidation Protein Products (AOPP) and Total Oxidative Status (TOS) which measures H2O2 and lipid hydroperoxides, Paraoxonase-1 Enzyme Activity (PON1), Total SH-groups content, and Total Antioxidative Status (TAS) for antioxidant determination. The Prooxidative Score, Antioxidative Score, and Oxy Score were also calculated. From the obtained results, compounds 6 (8720 FRAP value and 39.31 Oxy Score) and 12 (7866 FRAP value and 36.41 Oxy Score) were found to possess significant antioxidant activity with reasonable potential for therapeutic activity.

2019 ◽  
Vol 9 (5) ◽  
pp. 1-8
Author(s):  
Lazare Belemnaba ◽  
Madi Soubeiga ◽  
Geoffroy G. Ouédraogo ◽  
Tata Kadiatou Traoré ◽  
Mathieu Nitiéma ◽  
...  

Aims: This study investigated the antioxidant activity and the 90 days subchronic toxicity of the standardized LAMIC phytomedicine prototype based on aqueous extracts from Lannea microcarpa trunk bark. Methods: Three spectrophotometric methods were used to evaluated the antioxidant activity of LAMIC which were 2,2-Diphenyl-1-picrylhydrazyl (DPPH) free radical, 2,2’-azinobis(3-ethylbenzolin-6-sulphonate) (ABTS) radical scavenging assays and ferric reducing antioxidant power (FRAP) assays. For the standardized LAMIC subchronic toxicity study, male and female Wistar rats were used by daily oral administration at doses of 500, 1000 and 1500 mg/kg bw consecutively for 90 days. Results: The LAMIC extract exhibit better inhibitory activity against DPPH radical than ABTS radical with respective IC50 values of 45.38±3.21 µg/mL and 66.45±18.76 µg/mL, while FRAP assay exhibit antioxidant activity of 211.34±15.92 mmol EAA/g. Subchronic oral administration of LAMIC was well-tolerated at all tested doses. No behavioral and physiological changes and mortality were observed. The LAMIC extract did not present any impact on general hematological parameters and biochemical parameters. Moreover, no significant changes were raised in organ and body weight of treated groups compared to the Control group. Conclusion: These results support that LAMIC prototype was a valuable source of natural antioxidants and no toxicity was associated to its long terms oral consumption in rats indicating a potential application as a cardiovascular protective formulation. Keywords: LAMIC–Lannea microcarpa–Standardization–Antioxidant–Subchronic toxicity.  


2015 ◽  
Vol 1113 ◽  
pp. 471-476
Author(s):  
Ummi Kalthum Ibrahim ◽  
Muhammad Ihsan Sobri Yusof ◽  
Khairul Anuar Ahmad Zamil ◽  
Nadia Kamarrudin ◽  
Siti Noor Suzila Maqsood-Ul-Haque ◽  
...  

The purpose of this study is to investigate the antioxidant properties and total phenolic content in local fruit wastes. Watermelon rinds, mango and banana peels were selected in the experiment. Two parameters involved were the extraction time and temperature. All samples had undergone drying process in an oven at 40°C for 24 hours before being extracted with 80%, v/v methanol on a hot plate together with magnetic stirrer. The extraction time was ranged from 20 to 40 minutes and the extraction temperature was from 30 to 60°C. Ferric Reducing Antioxidant Power (FRAP) assay and Folin-Ciocalteu reagent were used for antioxidant analysis and phenolic content determination, respectively. UV-Vis spectrophotometer was used to detect the antioxidant activity at 593 nm and 765 nm for phenolic content. Response Surface Method was used to find the best extraction condition. The best extraction conditions were found at extraction temperature and time of 58.93°C and 37.86 minutes, respectively.


Author(s):  
Hadi Shariati ◽  
Mohammad Hassanpour ◽  
Gholamreza Sharifzadeh ◽  
Asghar Zarban ◽  
Saeed Samarghandian ◽  
...  

Objective: The present study has been carried out to evaluate the diuretic and antioxidant properties of pine herb in an animal model. Materials and Methods: 45 adult male rats were randomly divided into nine groups including: groups I (the negative control), groups II (positive control, furosemide 10 mg/kg), groups III to VIII (treatment groups received 100, 200, 400 mg/kg of the aqueous extracts of bark and fruit) and group IX received the combination of aqueous extract of bark (100 mg/kg) and the fruit (100 mg/kg). The urine output, glomerular filtration rate (GFR), electrolytes, urea, and creatinine levels were evaluated . Furthermore, the phenolic content and antioxidant activity of both extracts were also assessed using 2, 2-diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP) and Folin–Ciocalteu methods. Results: The aqueous extracts of the pine bark and fruit increased the urinary output in a dose-dependent manner. The combination of the two extracts compared to the other extracts alone significantly increased the serum potassium level. This study also showed each extract increase creatinine clearance in a dose-dependent manner (p<0.01 and p<0.05). The increase of GFR in the combination group was not significant. The current data showed a significant increase in the total phenolic content in pine bark extract in compared with the fruit extract. Conclusion: The pine bark and fruit can be useful in the prevention and treatment of kidney stones due to the high antioxidant activity.


2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Chandravadivelu Gopi ◽  
Magharla Dasaratha Dhanaraju

Abstract Background The main aim of this work was to synthesise a novel N-(substituted phenyl)-2-(3-(hydroxyimino) methyl)-1H-indol-1-yl) acetamide derivatives and evaluate their antioxidant activity. These compounds were prepared by a condensation reaction between 1H-indole carbaldehyde oxime and 2-chloro acetamide derivatives. The newly synthesised compound structures were characterised by FT-IR, 1H-NMR, mass spectroscopy and elemental analysis. Furthermore, the above-mentioned compounds were screened for antioxidant activity by using ferric reducing antioxidant power (FRAP) and 1,1-diphenyl-2-picrylhydrazyl (DPPH) methods. Result The antioxidant activity result reveals that most of the compounds were exhibiting considerable activity in both methods and the values are very closer to the standards. Among the synthesised compounds, compound 3j, 3a and 3k were shown remarkable activity at low concentration. Conclusion Compounds 3j, 3a and 3k were shown highest activity among the prepared analogues due to the attachment of halogens connected at the appropriate place in the phenyl ring. Hence, these substituted phenyl rings considered as a perfect side chain for the indole nucleus for the development of the new antioxidant agents.


Processes ◽  
2021 ◽  
Vol 9 (8) ◽  
pp. 1262
Author(s):  
Shonisani Eugenia Ramashia ◽  
Felicia Matshepho Mamadisa ◽  
Mpho Edward Mashau

This study investigated the impact of Parinari curatellifolia peel flour on the nutritional, physical and antioxidant properties of formulated biscuits. Biscuits enriched with 5%, 10%, 15% and 20% of Parinari (P). curatellifolia peel flour were formulated and characterised. Thermal, physicochemical, polyphenolic compounds and antioxidant properties of flour and biscuits were determined. The incorporation of P. curatellifolia peel flour significantly increased (p < 0.05) thermal properties (onset, peak and conclusion temperatures) of flour. However, enthalpy of gelatinisation, viscosity and pH of flour samples decreased. Nutritional analysis revealed an increase in ash (0.74% to 2.23%) and crude fibre contents (0.39% to 2.95%) along with an increase of P. curatellifolia peel flour levels. Protein content and carbohydrates decreased while moisture content was insignificantly affected by the addition of P. curatellifolia peel flour. The L*, b* values and whiteness index of formulated biscuits decreased while parameter a* value (10.76 to 21.89) and yellowness index (69.84 to 102.71) decreased. Physical properties such as diameter (3.57 mm to 3.97 mm), spread ratio (2.67 to 3.45) and hardness (1188.13 g to 2432.60 g) increased with the inclusion levels of peel flour while weight and thickness decreased. The inclusion of P. curatellifolia improved the polyphenolic compounds and antioxidant activity of biscuits with values of total flavonoids content ranging from 0.028 to 0.104 mg CE/g, total phenolic content increasing from 20.01 mg to 48.51 mg GAE/g, ferric reducing antioxidant power (FRAP) increasing from 108.33 mg to 162.67 mg GAE/g and DPPH (2,2-diphenyl-1-picrylhydrazyl) from 48.70% to 94.72%. These results lead to the recommendation of the utilisation of P. curatellifolia peel flour to enhance the nutritional value, polyphenolic compounds and antioxidant activity of bakery products such as biscuits.


Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 1906
Author(s):  
Phraepakaporn Kunnaja ◽  
Sunee Chansakaow ◽  
Absorn Wittayapraparat ◽  
Pedcharada Yusuk ◽  
Seewaboon Sireeratawong

In Thailand, people in the highland communities whose occupational exposure to pesticides used the root of Litsea martabanica as a detoxifying agent. However, the scientific data to support the traditional use of this plant are insufficient. This study aimed to evaluate the antioxidant activity and anti-pesticide potential of L. martabanica root extract. Antioxidant properties were investigated by 2,2′-diphenyl-1-picrylhydrazyl (DPPH) assay, superoxide radicals scavenging assay, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay, ferric reducing antioxidant power (FRAP), and total phenolic content determination. In all assays, L. martabanica extracts and their fractions exhibited high antioxidant activities differently. The water extract is traditionally used as a detoxifying agent. Therefore, it was chosen for in vivo experiments. The rats received the extract in a way that mimics the traditional methods of tribal communities followed by chlorpyrifos for 16 days. The results showed that acetylcholinesterase activity decreases in pesticide-exposed rats. Treatment with the extract caused increasing acetylcholinesterase activity in the rats. Therefore, L. martabanica extract may potentially be used as a detoxifying agent, especially for the chlorpyrifos pesticide. The antioxidant properties of L. martabanica may provide a beneficial effect by protecting liver cells from damage caused by free radicals. Histopathology results revealed no liver cell necrosis and showed the regeneration of liver cells in the treatment group. L. martabanica extract did not cause changes in behavior, liver weight, hematological and biochemical profiles of the rats.


2009 ◽  
Vol 27 (Special Issue 1) ◽  
pp. S213-S216 ◽  
Author(s):  
D. Komes ◽  
D. Horžić ◽  
A. Belščak ◽  
K. Kovačević Ganič ◽  
A. Baljak

Caffeine-containing products have been consumed for hundreds of years for their pleasant flavor and stimulating effects. In recent years, caffeine received increasing attention in food and pharmaceutical industries, due to its pharmacological properties which comprise stimulation of the central nervous system, peripheral vasoconstriction, relaxation of the smooth muscle and myocardial stimulation. The aim of this study was to determine the content of caffeine in five types of tea (white, yellow, green, oolong, black) and two types of maté tea (green maté and roasted maté tea). The content of caffeine was determined by using four different methods: extraction with chloroform, micromethod, method with lead-acetate and high performance liquid chromatography method (HPLC-PDA). The antioxidant capacity of teas as well as of the extracted (“raw”) caffeine was determined by using two methods: reactions with 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) radical (ABTS assay) and Ferric reducing antioxidant power (FRAP assay). The content of caffeine has been associated with plant origin and growth conditions, as well as processing conditions. By applying all four methods, the highest content of caffeine was determined in white tea, whereas maté and roasted maté tea were characterised with the lowest content of caffeine. Spectrophotometric micro-method has proven to be the best alternative to the HPLC method. The highest antioxidant capacity was determined in yellow tea, while the lowest was determined in roasted maté tea. In comparison to the antioxidant capacity of teas, the antioxidant capacity of extracted (“raw”) caffeine is almost negligible, and does not contribute to the overall antioxidant properties of tea.


2021 ◽  
Vol 332 ◽  
pp. 08005
Author(s):  
Aminah Dalimunthe ◽  
Dewi Pertiwi ◽  
Mahatir Muhammad ◽  
Denny Satria

Free radicals also play a role in the pathology of various degenerative diseases such as cancer, rheumatism, coronary heart disease, cataracts, and others. Free radicals can come from within the body (endogenous) and outside the body (exogenous). Litsea cubeba (Lour,) is a Lauraceae family plant which have contents volatile oils which used as antimicrobial, anticancer on breast cancer, pesticide, antideppressants, antiinflammation, antioxidant, and neuro pharmacology. The extract was prepared using water with the soxhletation method. The antioxidant activity was determined with the 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2’-Azinobis [3-ethylbenzothiazoline-6)-sulfonic acid] -diammonium salt (ABTS) and Ferric Reducing Antioxidant Power (FRAP) methods. Total flavonoid and total phenolic content were determined with colorimetric methods. Antioxidant activity measured as IC50 was 23.37 ± 0.42 µg/mL; 111.21 ± 0.42 and 109.01 ± 0.28 respectively. The extract was found to contain high levels of total phenolic (282.93 ± 0.33 mg GAE/g) and total flavonoid 7.49 ± 0.51 mg QE/g). The results reveal that ethanol extract of Litsea cubeba Lour. Bark has antioxidant potential. The further analysis is to isolation antioxidant compound.


Author(s):  
CAROLINE JEBA R ◽  
INDHUJA D

Objectives: Antioxidant activity was studied in naturally dried seed extract and hot air oven dried extract of Actinidia deliciosa and Psidium guajava using ferric reducing antioxidant power (FRAP) assay method. Methods: The dried powdered seed of A. deliciosa and P. guajava 10 g was dissolved in 100 ml of ethanol in four different conical flasks S1 (for naturaly dried seeds of A. deliciosa), S2 (for hot air oven-dried seeds of A. deliciosa), S3 (for naturally dried seeds of P. guajava), and S4 (for hot air oven-dried seeds of P. guajava). The extract was carried out in shaker at 120 rpm for 72 h at room temperature by mild shaking. The extract was taken out and centrifuged at 4000 rpm for 10 min, the supernatant was taken out. The supernatant was placed in a water bath at 95°C for the solvent to evaporate and stored at room temperature. Results: According to the FRAP results, P. guajava which was naturally dried and extracted has shown the highest antioxidant activity (sample 3) then followed by the samples S4, S1, and S2. The least activity is observed in the sample (S2). Conclusion: By comparing the antioxidant activity between the A. deliciosa and P. guajava with the help of FRAP assay results, P. guajava has the highest amount of vitamin C (responsible for antioxidant activity) when compared to that of the A. deliciosa.


Molecules ◽  
2020 ◽  
Vol 25 (16) ◽  
pp. 3648
Author(s):  
Lucia Godočiková ◽  
Eva Ivanišová ◽  
Grzegorz Zaguła ◽  
Luis Noguera-Artiaga ◽  
Ángel A. Carbonell-Barrachina ◽  
...  

The biological activity of chocolates gains more and more attention of consumers. Its antioxidant properties depend, among other factors, mainly on the origin of cocoa and the characteristics that this origin gives to the final product. Therefore, the aim of the study was to measure and compare the total content of polyphenols, antioxidant activity, and key odorants of commercial chocolates made from blend cocoa with single-origin ones. The highest content of polyphenols was found in 90% blend cocoa chocolate and single-origin samples, while the lowest content was exhibited by 100% chocolate from blend cocoa mass. The highest antioxidant activity measured by 2,2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) and ferric reducing antioxidant power (FRAP) assays was observed in the sample of chocolate with 90% cocoa solids from blend mass, followed by single-origin chocolates. A high positive correlation between ABTS assay and the total polyphenol and phenolic acids’ content, as well as among the total content of polyphenols, flavonoids, and phenolic acids was found. Mineral composition analysis showed that dark chocolate is a valuable source of some elements, especially Mg, Fe, and Zn. Potentially toxic elements were not detected or below permitted limits. Moreover, it was noticed that the main volatile compound in all tested samples was acetic acid, but pyrazines were considered the most important group of chocolate odorants.


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