Antioxidant and Antimicrobial Potential of New Azetidin-2-One of Ferulic Acid

DRĂGAN, MARIA

doi:10.31925/farmacia.2019.5.6

Cited by 11 publications

(14 citation statements)

References 9 publications

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“…Based on the results obtained on in vitro anti-inflammatory evaluation studies which were previously published [7,8] and from the literature data regarding the anti-inflammatory potential and mechanism of ferulic acid, our azetidin-2-one derivatives of ferulic acid were included in a pharmacological screening test aimed to determine the in vivo anti-inflammatory effect.…”

Section: Discussionmentioning

confidence: 99%

“…In those studies, the in vitro antioxidant potential of the azetidin-2-one derivatives of ferulic acid was assessed using the total antioxidant capacity, total reducing power assays, and DPPH and ABTS .+ radicals scavenging assays. The results showed that all the investigated compounds possess a good antioxidant activity at low concentrations, a more intense effect than ferulic acid and a comparable effect with ascorbic acid, used as positive control, was found for compound 6b (R = 4-F) [7,8]. Additionally, the in vitro anti-inflammatory potential was investigated using bovine serum albumin denaturation and human red blood cell membrane stabilization assays.…”

Section: Compound -R Compound -R 6amentioning

confidence: 96%

“…-H 6d -NO 2 (2) 6b -F(4) 6e -Br(4) 6c -Cl(4) 6f -OH (2) The synthesis, spectral characterization, in vitro antioxidant and anti-inflammatory potential, and antimicrobial action have already been published [7,8].…”

Section: Compound -R Compound -R 6amentioning

confidence: 99%

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Biological Evaluation of Azetidine-2-One Derivatives of Ferulic Acid as Promising Anti-Inflammatory Agents

et al. 2020

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The purpose of this study was to evaluate the in vivo biological potential of new azetidine-2-one derivatives of ferulic acid (6a–f). First, the in vivo acute toxicity of azetidine-2-one derivatives of ferulic acid on Swiss white mice was investigated and, based on the obtained results, it can be stated that the studied derivatives belong to compounds with moderate toxicity. The in vivo anti-inflammatory potential of these derivatives was determined in a model of acute inflammation induced by carrageenan in rats and in a chronic inflammation model induced in rats using the granuloma test. In the acute inflammation model, all the studied compounds had a maximum anti-inflammatory effect 24 h after administration, which suggests that these compounds may be classified, from a pharmacokinetic point of view, in the category of long-acting compounds. The most active compound in the series was found to be compound 6b. In the case of the chronic inflammation model, it was observed that the studied compounds (6a–f) reduced the formation of granulation tissue compared to the control group, having an intense effect of inhibiting the proliferative component. The most important inhibitory effect of inhibiting the proliferative component was recorded for compound 6b. Additionally, the investigation of liver function was performed by determining the serum levels of liver enzymes aspartate transaminase (AST), alanine aminotransferase (ALT), lactate dehydrogenase (LDH) and bilirubin (total and direct). The results showed that, in the series of azetidin-2-one derivatives, the liver enzymes concentration values were close to those recorded for the reference anti-inflammatories (diclofenac sodium and indomethacin) and slightly higher compared to the values for the healthy control group. At the end of the experiment, the animals were euthanized and fragments of liver, lung, and kidney tissue were taken from all groups in the study. These were processed for histopathological examination, and we noticed no major changes in the groups treated with the azetidine 2-one derivatives of ferulic acid compared to the healthy groups.

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Section: Discussionmentioning

confidence: 99%

Section: Compound -R Compound -R 6amentioning

confidence: 96%

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Biological Evaluation of Azetidine-2-One Derivatives of Ferulic Acid as Promising Anti-Inflammatory Agents

et al. 2020

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“…The reagent contains the following substances: sulphuric acid 0.6 M, sodium phosphate 28 mM and ammonium molybdate 4 mM. The absorbance of the sample was measured at 695 nm, using a blank which contains 2% acetic acid (50 µL) and the reagent solution (2 mL); effective concentrations (EC50) were calculated [24,25].…”

Section: Research Regarding Antioxidant Assaysmentioning

confidence: 99%

“…The absorbance of each sample was measured at 700 nm, using a blank that contains all reagents and less stock solution. The effective concentrations (EC50) were calculated for this method (also [24]).…”

Section: Research Regarding Antioxidant Assaysmentioning

confidence: 99%

Designing of Chitosan Derivatives Nanoparticles with Antiangiogenic Effect for Cancer Therapy

et al. 2020

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Angiogenesis is a physiological process involving the growth of new blood vessels, which provides oxygen and required nutrients for the development of various pathological conditions. In a tumor microenvironment, this process upregulates the growth and proliferation of tumor cells, thus any stage of angiogenesis can be a potential target for cancer therapies. In the present study, chitosan and his derivatives have been used to design novel polymer-based nanoparticles. The therapeutic potential of these newly designed nanoparticles has been evaluated. The antioxidant and MTT assays were performed to know the antioxidant properties and their biocompatibility. The in vivo antiangiogenic properties of the nanoparticles were evaluated by using a chick Chorioallantoic Membrane (CAM) model. The obtained results demonstrate that chitosan derivatives-based nanostructures strongly enhance the therapeutic effect compared to chitosan alone, which also correlates with antitumor activity, demonstrated by the in vitro MTT assay on human epithelial cervical Hep-2 tumor cells. This study opens up new direction for the use of the chitosan derivatives-based nanoparticles for designing of antiangiogenic nanostructured materials, for future cancer therapy.While stimulation of angiogenesis in cancer leads to metastasis, the anti-angiogenic therapy proved to be an important approach against tumor growth. In this respect, it is a well-known fact that the consumption of antioxidants can be recommended to achieve the inhibition of angiogenesis or reversal of unwanted cell-cell adherence [1]. Several studies have been conducted to investigate the connection between antioxidants and pathological angiogenesis, thus leading to mixed conclusions from studies that have been associated with a lower total cancer incidence with the use of antioxidants [2], to studies that have highlighted the lack of any benefit of using antioxidants on the incidence of cancer [3]. All these results are, for certain ones, closely related with the type of antioxidant included in the study (alpha tocopherol, beta-carotene, ascorbic acid) and the investigated tumor location and not least the investigated pharmaceutical formulation. In this context, the use of antioxidants in the form of nanoparticles could improve the efficiency of this therapy due to specific surface area of nanostructures [4], thereby ensuring better contact with cells that would increase the chances of pathological angiogenesis inhibition. However, to have more success in cancer therapy, more studies should be conducted in this direction.Chitosan is a natural cationic polymer exhibits three chemical reactive sites including a primary amine and two primary or secondary hydroxyl groups for further modification [5][6][7]. Nano/microparticles coated with chitosan, synthesized through different techniques for encapsulation (chemical, physical and mechanical techniques), are in continuous development, aiming at the entrapment of bioactive substances, enzymes, hormones, antimicrobial agents, vitamins, mi...

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Rational Design of Multifunctional Ferulic Acid Derivatives Aimed for Alzheimer’s and Parkinson’s diseases

Guzmán‐López¹,

Reina²,

Hernández‐Ayala³

et al. 2023

Preprint

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Ferulic acid has numerous beneficial effects for human health, which are frequently attributed to its antioxidant behavior. In this report many of them are reviewed and 185 new ferulic acid derivatives are computationally designed, using the CADMA-Chem protocol. For the later, the chemical space was sampled and evaluated. To that purpose selection and elimination scores were used, which are built from a set of descriptors accounting for ADME properties, toxicity, and synthetic accessibility. After the first screening, 12 derivatives were selected and further investigated. Their potential role as antioxidants was predicted from reactivity indexes, directed related with the formal hydrogen atom transfer and the single electron transfer mechanisms. The best performing molecules were identified by comparisons with the parent molecule and two references: Trolox and alpha-tocopherol. Their potential as polygenic neuroprotectors was investigated through the interactions with enzymes directed related with the etiologies of Parkinson’s and Alzheimer’s diseases. They are acetylcholinesterase, catechol-O-methyltransferase, and monoamine oxidase B. Based on the obtained results, the most promising candidates (FA-26, FA-118, and FA-138) are proposed as multifunctional antioxidants with potential neuroprotective effects. The findings derived from this investigation are encouraging and might promote further investigations on these molecules.

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Antioxidant and Antimicrobial Potential of New Azetidin-2-One of Ferulic Acid

Cited by 11 publications

References 9 publications

Biological Evaluation of Azetidine-2-One Derivatives of Ferulic Acid as Promising Anti-Inflammatory Agents

Biological Evaluation of Azetidine-2-One Derivatives of Ferulic Acid as Promising Anti-Inflammatory Agents

Designing of Chitosan Derivatives Nanoparticles with Antiangiogenic Effect for Cancer Therapy

Rational Design of Multifunctional Ferulic Acid Derivatives Aimed for Alzheimer’s and Parkinson’s diseases

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