scholarly journals Pleiotropic Properties of Valsartan: Do They Result from the Antiglycooxidant Activity? Literature Review and In Vitro Study

2021 ◽  
Vol 2021 ◽  
pp. 1-20
Author(s):  
Kacper Maksymilian Mil ◽  
Małgorzata Ewa Gryciuk ◽  
Cezary Pawlukianiec ◽  
Małgorzata Żendzian-Piotrowska ◽  
Jerzy Robert Ładny ◽  
...  

Valsartan belongs to angiotensin II type 1 (AT1) receptor blockers (ARB) used in cardiovascular diseases like heart failure and hypertension. Except for its AT1-antagonism, another mechanism of drug action has been suggested in recent research. One of the supposed actions refers to the positive impact on redox balance and reducing protein glycation. Our study is aimed at assessing the antiglycooxidant properties of valsartan in an in vitro model of oxidized bovine serum albumin (BSA). Glucose, fructose, ribose, glyoxal (GO), methylglyoxal (MGO), and chloramine T were used as glycation or oxidation agents. Protein oxidation products (total thiols, protein carbonyls (PC), and advanced oxidation protein products (AOPP)), glycooxidation products (tryptophan, kynurenine, N-formylkynurenine, and dityrosine), glycation products (amyloid-β structure, fructosamine, and advanced glycation end products (AGE)), and albumin antioxidant activity (total antioxidant capacity (TAC), DPPH assay, and ferric reducing antioxidant power (FRAP)) were measured in each sample. In the presence of valsartan, concentrations of protein oxidation and glycation products were significantly lower comparing to control. Moreover, albumin antioxidant activity was significantly higher in those samples. The drug’s action was comparable to renowned antiglycation agents and antioxidants, e.g., aminoguanidine, metformin, Trolox, N-acetylcysteine, or alpha-lipoic acid. The conducted experiment proves that valsartan can ameliorate protein glycation and oxidation in vitro in various conditions. Available animal and clinical studies uphold this statement, but further research is needed to confirm it, as reduction of protein oxidation and glycation may prevent cardiovascular disease development.

2020 ◽  
Vol 13 (9) ◽  
pp. 240 ◽  
Author(s):  
Cezary Pawlukianiec ◽  
Małgorzata Ewa Gryciuk ◽  
Kacper Maksymilian Mil ◽  
Małgorzata Żendzian-Piotrowska ◽  
Anna Zalewska ◽  
...  

Meloxicam is a non-steroidal anti-inflammatory drug, which has a preferential inhibitory effect to cyclooxyganase-2 (COX-2). Although the drug inhibits prostaglandin synthesis, the exact mechanism of meloxicam is still unknown. This is the first study to assess the effect of meloxicam on protein glyco-oxidation as well as antioxidant activity. For this purpose, we used an in vitro model of oxidized bovine serum albumin (BSA). Glucose, fructose, ribose, glyoxal and methylglyoxal were used as glycating agents, while chloramine T was used as an oxidant. We evaluated the antioxidant properties of albumin (2,2-di-phenyl-1-picrylhydrazyl radical scavenging capacity, total antioxidant capacity and ferric reducing antioxidant power), the intensity of protein glycation (Amadori products, advanced glycation end products) and glyco-oxidation (dityrosine, kynurenine, N-formylkynurenine, tryptophan and amyloid-β) as well as the content of protein oxidation products (advanced oxidation protein products, carbonyl groups and thiol groups). We have demonstrated that meloxicam enhances the antioxidant properties of albumin and prevents the protein oxidation and glycation under the influence of various factors such as sugars, aldehydes and oxidants. Importantly, the antioxidant and anti-glycating activity is similar to that of routinely used antioxidants such as captopril, Trolox, reduced glutathione and lipoic acid as well as protein glycation inhibitors (aminoguanidine). Pleiotropic action of meloxicam may increase the effectiveness of anti-inflammatory treatment in diseases with oxidative stress etiology.


Antioxidants ◽  
2020 ◽  
Vol 10 (1) ◽  
pp. 32
Author(s):  
Pattamaporn Aksornchu ◽  
Netima Chamnansilpa ◽  
Sirichai Adisakwattana ◽  
Thavaree Thilavech ◽  
Charoonsri Choosak ◽  
...  

Antidesma bunius (L.) spreng (Mamao) is widely distributed in Northeastern Thailand. Antidesma bunius has been reported to contain anthocyanins, which possess antioxidant and antihypertensive actions. However, the antidiabetic and antiglycation activity of Antidesma bunius fruit extract has not yet been reported. In this study, we investigated the inhibitory activity of anthocyanin-enriched fraction of Antidesma bunius fruit extract (ABE) against pancreatic α-amylase, intestinal α-glucosidase (maltase and sucrase), protein glycation, as well as antioxidant activity. A liquid chromatography-tandem mass spectrometry (LC-MS/MS) chromatogram revealed that ABE contained phytochemical compounds such as cyanidin-3-glucoside, delphinidin-3-glucoside, ellagic acid, and myricetin-3-galactoside. ABE inhibited intestinal maltase and sucrase activity with the IC50 values of 0.76 ± 0.02 mg/mL and 1.33 ± 0.03 mg/mL, respectively. Furthermore, ABE (0.25 mg/mL) reduced the formation of fluorescent AGEs and the level of Nε-carboxymethyllysine (Nε-CML) in fructose and glucose-induced protein glycation during four weeks of incubation. During the glycation process, the protein carbonyl and β-amyloid cross structure were decreased by ABE (0.25 mg/mL). In addition, ABE exhibited antioxidant activity through DPPH radical scavenging activity and Trolox equivalent antioxidant capacity (TEAC) with the IC50 values 15.84 ± 0.06 µg/mL and 166.1 ± 2.40 µg/mL, respectively. Meanwhile, ferric reducing antioxidant power (FRAP) showed an EC50 value of 182.22 ± 0.64 µg/mL. The findings suggest that ABE may be a promising agent for inhibiting carbohydrate digestive enzyme activity, reducing monosaccharide-induced protein glycation, and antioxidant activity.


Author(s):  
Patel M G. ◽  
Prajapati D. P.

Non enzymatic glycation is a chain reaction between reducing sugars and the free amino groups of proteins, involved in severity of diabetes and diabetic complications. Litchi chinensis used as consumed fruit and as a drug to treat certain diseases. In this study the antioxidative effects of L.chinensis and also its effect against protein oxidation and advanced glycation end products. The antioxidant potential of aqueous fruit pericarp extract of L.chinensis (APLC) was evaluated in vitro using a model of fructose-mediated protein glycation. The antioxidant activity of APLC conducted for superoxide, hydroxyl, hydrogen peroxide, nitric oxide radical scavenging activities and also demonstrated antioxidant activity with Fe+2 chelating activity, ferric reducing antioxidant power (FRAP) and Trolox equivalent antioxidant capacity (TEAC) were applied. Fructose (100mM) increased fluorescence intensity of glycated bovine serum albumin (BSA) in terms of total AGEs during 21 days of exposure. Moreover, fructose caused more protein carbonyl (PCO) formation in native BSA. The APLC prevents oxidative protein damages including effect on PCO formation which are believed to form under the glycoxidation process. The APLC at different concentrations (25-250µg/ml) has significantly decreased the formation of AGEs in term of the fluorescence intensity of glycated BSA.


Author(s):  
Swathi Putta ◽  
Eswar Kumar Kilari

Non enzymatic glycation is a chain reaction between reducing sugars and the free amino groups of proteins, involved in severity of diabetes and diabetic complications. Litchi chinensis used as consumed fruit and as a drug to treat certain diseases. In this study the antioxidative effects of L.chinensis and also its effect against protein oxidation and advanced glycation end products. The antioxidant potential of aqueous fruit pericarp extract of L.chinensis (APLC) was evaluated in vitro using a model of fructose-mediated protein glycation. The antioxidant activity of APLC conducted for superoxide, hydroxyl, hydrogen peroxide, nitric oxide radical scavenging activities and also demonstrated antioxidant activity with Fe+2 chelating activity, ferric reducing antioxidant power (FRAP) and Trolox equivalent antioxidant capacity (TEAC) were applied. Fructose (100mM) increased fluorescence intensity of glycated bovine serum albumin (BSA) in terms of total AGEs during 21 days of exposure. Moreover, fructose caused more protein carbonyl (PCO) formation in native BSA. The APLC prevents oxidative protein damages including effect on PCO formation which are believed to form under the glycoxidation process. The APLC at different concentrations (25-250µg/ml) has significantly decreased the formation of AGEs in term of the fluorescence intensity of glycated BSA.


2012 ◽  
Vol 2 (12) ◽  
pp. 58-59
Author(s):  
suvarna M N Vinay ◽  
◽  
Ramesh B S Ramesh B S ◽  
Venkatachalapathy R Venkatachalapathy R ◽  
Makari Hanumantappa K ◽  
...  

2020 ◽  
Vol 16 ◽  
Author(s):  
Benedetta Bocchini ◽  
Bruna Goldani ◽  
Fernanda S.S. Sousa ◽  
Paloma T. Birmann ◽  
Cesar A. Brüning ◽  
...  

Background: Quinoline derivatives have been attracted much attention in drug discovery and synthetic derivatives of these scaffolds present a range of pharmacological activities. Therefore, organoselenium compounds are valuable scaffolds in organic synthesis because their pharmacological activities and their use as versatile building blocks for regio-, chemio-and stereoselective reactions. Thus, the synthesis of selenium-containing quinolines has great significance, and their applicability range from simple antioxidant agents, to selective DNA-binding and photocleaving agents. Objective: In the present study we describe the synthesis and antioxidant activity in vitro of new 7-chloroN(arylselanyl)quinolin-4-amines 5 by the reaction of 4,7-dichloroquinoline 4 with (arylselanyl)-amines 3. Methods: For the synthesis of 7-chloro-N(arylselanyl)quinolin-4-amines 5, we performed the reaction of (arylselanyl)- amines 3 with 4,7-dichloroquinoline 4 in the presence of Et3N at 120 °C in a sealed tube. The antioxidant activities of the compounds 5 were evaluated by the following in vitro assays: 2,2- diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, 2,2-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS), ferric ion reducing antioxidant power (FRAP), nitric oxide (NO) scavenging and superoxide dismutase-like activity (SOD-Like). Results: 7-Chloro-N(arylselanyl)quinolin-4-amines 5a-d has been synthesized in yields ranging from 68% to 82% by the reaction of 4,7-dichloroquinoline 4 with arylselanyl-amines 3a-d using Et3N as base, at 120 °C, in a sealed tube for 24 hours and tolerates different substituents, such as -OMe and -Cl, in the arylselanyl moiety. The obtained compounds 5a-d presented significant results with respect to the antioxidant potential, which had effect in the tests of inhibition of radical’s DPPH, ABTS+ and NO, as well as in the test that evaluates the capacity (FRAP) and in the superoxide dismutase-like activity assay (SOD-Like). It is worth mentioning that 7-chloro-N(arylselanyl)quinolin-4-amine 5b presented excellent results, demonstrating a better antioxidant capacity when compared to the others. Conclusion: According to the obtained results 7-chloro-N(arylselanyl)quinolin-4-amines 5 were synthesized in good yields by the reaction of 4,7-dichloroquinoline with arylselanyl-amines and tolerates different substituents in the arylselanyl moiety. The tested compounds presented significant antioxidant potential in the tests of inhibition of DPPH, ABTS+ and NO radicals, as well as in the FRAP and superoxide dismutase-like activity assays (SOD-Like).


2018 ◽  
Vol 10 (1) ◽  
pp. 407
Author(s):  
Dewi Kumala Putri ◽  
Berna Elya ◽  
Nuraini Puspitasari

Objective: To assess the antioxidant activity from another part of the plant, in this study, leaf extracts in n-hexane were fractionated.Methods: Ten fractions were obtained and tested in vitro for antioxidant activity using two methods, 1,1-diphenyl-2-picrylhydrazyl (DPPH) and ferricreducing antioxidant power (FRAP), to identify the most active fraction.Results: The IC50 of the most active fraction was 36.24 μg/mL using the DPPH method, and the EC50 was 39.54 μg/mL using the FRAP method. Themost active fraction was also shown to contain terpenoids.Conclusion: The most active fraction of an n-hexane extract of the leaves of Gacinia bancana Miq., which was tested by both DPPH and FRAP methodshad antioxidant activities with IC50 and EC50 values of 36.2482 μg/mL and 39.5442 μg/mL, respectively. Phytochemical screening showed that activefraction contains terpenoids.


Botanica ◽  
2020 ◽  
Vol 26 (1) ◽  
pp. 76-87
Author(s):  
Aziza Lfitat ◽  
Hind Zejli ◽  
Abdelkamel Bousselham ◽  
Yassine El Atki ◽  
Badiaa Lyoussi ◽  
...  

AbstractWe conducted this study to determine and compare the content of phenolic compounds and flavonoids in the argan and olive leaves as well as their antioxidant capacity in aqueous, methanolic, and ethyl acetate extracted fractions. In vitro antioxidant activity was evaluated in comparison with synthetic antioxidants by assessing DPPH• radical scavenging capacity, ferric reducing antioxidant power, scavenging ability by inhibiting the β-carotene/linoleic acid emulsion oxidation, and by the ABTS radical scavenging activity assay. Total phenolic content in argan samples ranged from 221.69 ± 2.07 to 1.32 ± 0.01 mg GAE/g DW and in olive samples from 144.61 ± 0.82 to 1.21 ± 0.02 mg GAE/g DW. Total flavonoids content in argan samples varied from 267.37 ± 1.12 to 25.48 ± 0.02 mg QE/g DW, while in olives from 96.06 ± 0.78 to 10.63 ± 0.05 mg QE/g DW. In vitro antioxidant studies strongly confirmed the antioxidant potency of argan and olive leaves and their richness in secondary metabolites that are effective in free radicals scavenging and metal chelating capacities, indicating their antioxidant power.


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