scholarly journals Characterization of Novel Synthetic Polyphenols: Validation of Antioxidant and Vasculoprotective Activities

Antioxidants ◽  
2020 ◽  
Vol 9 (9) ◽  
pp. 787 ◽  
Author(s):  
María Jesús Pérez de Vega ◽  
Silvia Moreno-Fernández ◽  
Gloria María Pontes-Quero ◽  
María González-Amor ◽  
Blanca Vázquez-Lasa ◽  
...  

Antioxidant compounds, including polyphenols, have therapeutic effects because of their anti-inflammatory, antihypertensive, antithrombotic and antiproliferative properties. They play important roles in protecting the cardiovascular and neurological systems, by having preventive or protective effects against free radicals produced by either normal or pathological metabolism in such systems. For instance, resveratrol, a well-known potent antioxidant, has a counteracting effect on the excess of reactive oxygen species (ROS) and has a number of therapeutic benefits, like anti-inflammatory, anti-cancer and cardioprotective activities. Based on previous work from our group, and on the most frequent OH substitutions of natural polyphenols, we designed two series of synthetically accessible bis-polyhydroxyphenyl derivatives, separated by amide or urea linkers. These compounds exhibit high antioxidant ability (oxygen radical absorbance capacity (ORAC) assay) and interesting radical scavenging activity (RSA) values (2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and α,α-diphenyl-β-picrylhydrazyl (DPPH) tests). Some of the best polyphenols were evaluated in two biological systems, endothelial cells (in vitro) and whole aorta (ex vivo), highly susceptible for the deleterious effects of prooxidants under different inflammatory conditions, showing protection against oxidative stress induced by inflammatory stimuli relevant in cardiovascular diseases, i.e., Angiotensin II and IL-1β. Selected compounds also showed strong in vivo antioxidant properties when evaluated in the model organism Saccharomyces cerevisiae.

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4114
Author(s):  
Maria Fernanda Taviano ◽  
Emilia Cavò ◽  
Vivienne Spadaro ◽  
Francesco Maria Raimondo ◽  
Vincenzo Musolino ◽  
...  

In a project designed to investigate the specific and infraspecific taxa of Matthiola endemic to Sicily (Italy) as new potential sources of bioactive compounds in this work, the infraspecific taxa of Matthiola fruticulosa were studied, namely, subsp. fruticulosa and subsp. coronopifolia. HPLC–PDA/ESI–MS and SPME–GC/MS analyses of hydroalcoholic extracts obtained from the aerial parts of the two subspecies led to the detection of 51 phenolics and 61 volatile components, highlighting a quite different qualitative–quantitative profile. The antioxidant properties of the extracts were explored through in vitro methods: 1,1-diphenyl-2-picrylhydrazyl (DPPH), reducing power and Fe2+ chelating activity assays. The results of the antioxidant tests showed that the extracts possess a different antioxidant ability: particularly, the extract of M. fruticulosa subsp. fruticulosa exhibited higher radical scavenging activity than that of subsp. coronopifolia (IC50 = 1.25 ± 0.02 mg/mL and 2.86 ± 0.05 mg/mL), which in turn displayed better chelating properties (IC50 = 1.49 ± 0.01 mg/mL and 0.63 ± 0.01 mg/mL). Lastly, Artemia salina lethality bioassay was performed for toxicity assessment. The results of the bioassay showed lack of toxicity against brine shrimp larvae for both extracts. The data presented indicate the infraspecific taxa of M. fruticulosa as new and safe sources of antioxidant compounds.


Antioxidants ◽  
2020 ◽  
Vol 9 (1) ◽  
pp. 55 ◽  
Author(s):  
Ana Carolina Ruberte ◽  
Sandra Ramos-Inza ◽  
Carlos Aydillo ◽  
Irene Talavera ◽  
Ignacio Encío ◽  
...  

Selenium compounds are pivotal in medicinal chemistry for their antitumoral and antioxidant properties. Forty seven acylselenoureas have been designed and synthesized following a fragment-based approach. Different scaffolds, including carbo- and hetero-cycles, along with mono- and bi-cyclic moieties, have been linked to the selenium containing skeleton. The dose- and time-dependent radical scavenging activity for all of the compounds were assessed using the in vitro 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) assays. Some of them showed a greater radical scavenging capacity at low doses and shorter times than ascorbic acid. Therefore, four compounds were evaluated to test their protective effects against H2O2-induced oxidative stress. One derivative protected cells against H2O2-induced damage, increasing cell survival by up to 3.6-fold. Additionally, in vitro cytotoxic activity of all compounds was screened against several cancer cells. Eight compounds were selected to determine their half maximal inhibitory concentration (IC50) values towards breast and lung cancer cells, along with their selectivity indexes. The breast cancer cells turned out to be much more sensitive than the lung. Two compounds (5d and 10a) stood out with IC50 values between 4.2 μM and 8.0 μM towards MCF-7 and T47D cells, with selectivity indexes greater than 22.9. In addition, compound 10b exhibited dual antioxidant and cytotoxic activities. Although further evidence is needed, the acylselenourea scaffold could be a feasible frame to develop new dual agents.


Marine Drugs ◽  
2021 ◽  
Vol 19 (2) ◽  
pp. 48
Author(s):  
Laura Micheli ◽  
Marzia Vasarri ◽  
Emanuela Barletta ◽  
Elena Lucarini ◽  
Carla Ghelardini ◽  
...  

Posidonia oceanica (L.) Delile is traditionally used for its beneficial properties. Recently, promising antioxidant and anti-inflammatory biological properties emerged through studying the in vitro activity of the ethanolic leaves extract (POE). The present study aims to investigate the anti-inflammatory and analgesic role of POE in mice. Inflammatory pain was modeled in CD-1 mice by the intraplantar injection of carrageenan, interleukin IL-1β and formalin. Pain threshold was measured by von Frey and paw pressure tests. Nociceptive pain was studied by the hot-plate test. POE (10–100 mg kg−1) was administered per os. The paw soft tissue of carrageenan-treated animals was analyzed to measure anti-inflammatory and antioxidant effects. POE exerted a dose-dependent, acute anti-inflammatory effect able to counteract carrageenan-induced pain and paw oedema. Similar anti-hyperalgesic and anti-allodynic results were obtained when inflammation was induced by IL-1β. In the formalin test, the pre-treatment with POE significantly reduced the nocifensive behavior. Moreover, POE was able to evoke an analgesic effect in naïve animals. Ex vivo, POE reduced the myeloperoxidase activity as well as TNF-α and IL-1β levels; further antioxidant properties were highlighted as a reduction in NO concentration. POE is the candidate for a new valid strategy against inflammation and pain.


2021 ◽  
Vol 17 ◽  
Author(s):  
Brahim Asseli ◽  
Reguia Mahfoudi ◽  
Amar Djeridane ◽  
Mohamed Yousfi

Background: Research on medicinal plant antioxidants has emerged as a potential therapeutic to prevent free radical generated damage in the human body. Hammada elegans Botsch (popularly known as “Ajram”) is a xerophytic plant widely found in Laghouat region, but there are only a few reports about the biological or chemical properties of these species. Hence, the aim of this study is to investigate the antioxidant and the antihemolytic activities of hexanic, acetonic, methanolic and aqueous extracts of aerial parts of Algerian Hammada elegans Botsch by employing different in vitro assay systems. Methods: The total phenolic content, the flavonoid content and the condensed tannin amount were analyzed using Folin-Ciocalteu, aluminum chloride and vanillin assays, respectively. The in vitro antioxidant capacity of extracts was assessed by CUPRAC, iron chelating, ABTS•+and antihemolytic assays, and was expressed as EC50 values. Results: Among the analyzed extracts, the aqueous extract had the highest phenolic, flavonoid and tannin contents. Also, this extract displayed the highest antioxidant capacities compared to the other extracts and standards. Its EC50 value for ABTS radical-scavenging activity was 0.265 ± 0.003 mg/L. Moreover, this extract showed high iron (II) chelating ability (EC50 = 0.958 ± 0.001 mg/L), and good antioxidant activity in the cupric ion reducing activity (CUPRAC) in a concentration dependent manner (EC50 were 0.709 ± 0.002 mg/L). Additionally, this extract had the best antihemolytic activity against AAPH-induced hemolysis (EC50=0.090 ± 0.004 mg/L). Conclusion: Our study revealed that the aqueous extract of Hammada elegans Botsch, is a potential source of antioxidants which possess a high protective effect of membrane against free radical.


Author(s):  
Iserhienrhien Lucky Osafanme ◽  
Okolie Paulinus Ngozi

Aim: This study investigated the phytochemical constituents and in vitro antioxidant properties of methanol and aqueous leaf extracts of Geophila obvallata using standard methods. Materials and Methods: The in vitro antioxidant assays carried out were 1, 1‐diphenyl‐2‐picrylhydrazyl (DPPH) radical scavenging ability, Nitric oxide (NO•) radical scavenging activity assay, 2, 2'-azino-bis (3-ethylbenzthiazoline-6-sulphonic acid) (ABTS•+) radical cation scavenging assay, ferric reducing properties and hydroxyl radical scavenging assays. Results: Phytochemical analysis revealed the presence of alkaloids, flavonoids, phenolic compounds, steroids, saponins, terpernoids and cardiac glycosides in both extracts. Relative to the aqueous extract, the methanol extract contained a higher amount of the secondary metabolites. However, both extracts exhibited appreciable and dose-dependent capacities for quenching DPPH, ABTS•+ and NO• free radicals, and potent ferric reducing ability to levels comparable to those of ascorbic acid. The crude methanol extract showed significantly increased (P<0.05) antioxidant activity than the aqueous extract. Conclusion: It was concluded that the extract possesses strong antioxidant properties due to its content of phytochemicals, and provides scientific basis for its ethno medicinal applications.


2020 ◽  
Vol 11 (4) ◽  
pp. 6262-6267
Author(s):  
Krishnamoorthy Meenakumari ◽  
Giridharan Bupesh ◽  
Mayur Mausoom Phukan

The foods from plants were known to ensure against degenerative diseases and maturing because of their antioxidant activitycredited to their high content. Information on antioxidant activity of Indian medicinal plant is abundant. To the best of our knowledge, biological properties have not been accounted in the literature for this species of . As a point, this is the first results to assess the anti-oxidant activity of the plant which belongs to the family . The antioxidant activity of Methanol, , Ethyl acetate and Aqueous extracts of E. was determined using the DPPH free radical scavenging activity, ABTS radical scavenging activity and reducing power assay. The DPPH scavenging activity showed higher activity observed in extract (63%) of E. than (54%), (44%) and aqueous (30%). the ABTS assay inhibition in extract (58%) than (43%), (38%) and aqueous (32%) extracts. The reducing power assay of different extracts was increased in extract (54%) than (40%), (34%) and aqueous (28%) extracts. Overall, the and ethyl acetate extract had higher antioxidant properties than other extract. However, in this study, extracts exhibit great potential for antioxidant activity and may be useful for their nutritional and medicinal functions.


2016 ◽  
Vol 2016 ◽  
pp. 1-11 ◽  
Author(s):  
Hamdy Abdelkader ◽  
Michael Longman ◽  
Raid G. Alany ◽  
Barbara Pierscionek

Purpose.L-Carnosine is a naturally occurring dipeptide which recently gained popularity as an anticataractogenic agent due to its purported antioxidant activities. There is a paucity of research and conclusive evidence to support such claims. This work offers compelling data that help clarify the mechanism(s) behind the anticataract properties of L-carnosine.Methods.Direct in vitro antioxidant free radical scavenging properties were assayed using three different antioxidant (TEAC, CUPRAC, and DPPH) assays. Indirect in vitro and ex vivo antioxidant assays were studied by measuring glutathione bleaching capacity and total sulfhydryl (SH) capacity of bovine lens homogenates as well as hydrogen-peroxide-stress assay using human lens epithelial cells. Whole porcine lenses were incubated in high galactose media to study the anticataract effects of L-carnosine. MTT cytotoxicity assays were conducted on human lens epithelial cells.Results.The results showed that L-carnosine is a highly potent antiglycating agent but with weak metal chelating and antioxidant properties. There were no significant decreases in lens epithelial cell viability compared to negative controls. Whole porcine lenses incubated in high galactose media and treated with 20 mM L-carnosine showed a dramatic inhibition of advanced glycation end product formation as evidenced by NBT and boronate affinity chromatography assays.Conclusion.L-Carnosine offers prospects for investigating new methods of treatment for diabetic cataract and any diseases that are caused by glycation.


2021 ◽  
Vol 25 (1) ◽  
pp. 75-79
Author(s):  
S.O. Olubodun ◽  
G.E. Eriyamremu ◽  
M.E. Ayevbuomwan ◽  
C.I. Nzoputa

The presence of various bioactive components makes it necessary to analyse plants for their potential to act as a source of useful treatments and cures for many inflammatory, infectious and pathogenic diseases. This study was carried out to determine phytochemicals and in-vitro antioxidant activities of the leaf extracts of Acalypha godseffiana. The leaves of A. godseffiana were collected, dried, pulverized and extracted separately with methanol and water using maceration method. The extract was concentrated in vacuo with rotary evaporator at 40oC. The extracts were subjected to quantitative phytochemical analysis and different anti-oxidant analytical procedures like FRAP, DPPH etc to determine the radical scavenging capabilities. The results of phytochemical analysis estimated the quantities and revealed the presence of alkaloids, flavonoids, tannins, saponins and terpenoids which varied in both extracts. The methanol and aqueous extracts exhibited antioxidant activities with relatively high IC50 (IC50 = 3.67 ìg/ml and 4.42ìg/ml respectively) which accounted for a low free radical-scavenging activity when compared with the reference antioxidant, vitamin C (IC50 = 1.51ìg/ml). The results of the study indicates that A. godseffiana leaf extracts contain secondary metabolites and possesses antioxidant properties.


Author(s):  
Mrinmoy Basak ◽  
Moksood Ahmed Laskar ◽  
Priyanka Goswami

Most of the synthetic drugs used at present as analgesic and anti-inflammatory agents cause many side effects and toxic effects. Many medicines of plant origin with analgesic and anti-inflammatory activity have been used since long time without adverse effects. The purpose of the study was to explore the anti-pyretic and anti-oxidant activity of fruits of Garcinia pedunculata. The fruit of G. pedunculata was collected from Shillong, Meghalaya and extraction is done by using methanol as a solvent. The methanol extract shows the presence of carbohydrate, glycoside, alkaloids, phenol and flavonoids. Acute anti-pyretic activity for the extract was investigated in pyrexia rat. Temperature level was determined after 1hours, 4 hours, 8 hours and 12 hours after giving the extract dose of 100mg/kg and 200mg/kg body weight, and it was found to produce a significant reduce in fever. DPPH radical scavenging activity (In-vitro anti-oxidant activity of G. pedunculata) of methanolic extract shows 38.31 as IC50 (µg/ml) whereas Ascorbic acid as standard in the same concentration shows 34.81 IC50 (µg/ml). The obtained result justified the traditional use of G. pedunculata as anti-pyretic and antioxidant purpose.


Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5295
Author(s):  
Xinyu Zhao ◽  
Ruyi Chen ◽  
Yueyue Shi ◽  
Xiaoxi Zhang ◽  
Chongmei Tian ◽  
...  

This study aimed to isolate, prepare and identify the main flavonoids from a standardized Smilax glabra flavonoids extract (SGF) using preparative HPLC, MS, 1H NMR and 13C NMR, determine the contents of these flavonoids using UPLC, then compare their pharmacological activities in vitro. We obtained six flavonoids from SGF: astilbin (18.10%), neoastilbin (11.04%), isoastilbin (5.03%), neoisoastilbin (4.09%), engeletin (2.58%) and (−)-epicatechin (1.77%). The antioxidant activity of six flavonoids were evaluated by determining the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical and 2,2′-Azinobis (3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt (ABTS+) radical scavenging activity and ferric reducing antioxidant power (FRAP). In addition, the anti-inflammatory activity of six flavonoids were evaluated by determining the production of cytokines (IL-1β, IL-6), nitric oxide (NO) using enzyme linked immunosorbent assay and the NF-κB p65 expression using Western blotting in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. The results showed that (−)-epicatechin, astilbin, neoastilbin, isoastilbin and neoisoastilbin had strong antioxidant activities, not only in DPPH and ABTS+ radicals scavenging capacities, but in FRAP system. Furthermore, all the six flavonoids could significantly inhibit the secretion of IL-1β, IL-6, NO (p < 0.01) and the protein expression of NF-κB p-p65 (p < 0.01) in LPS-stimulated RAW264.7 cells. This study preliminarily verified the antioxidant and anti-inflammatory activities of six flavonoids in S. glabra.


Sign in / Sign up

Export Citation Format

Share Document