Activity Of Ferulic Acid Research Articles

Effects of temperature and solvent polarity on the thermodynamic and photophysical properties of ferulic acid using density functional theory (DFT)

Ferulic acid (FA) possesses diverse biological properties and is extensively utilized in pharmaceuticals, cosmetics, and the food industry due to its non-toxic nature. However, environmental factors such as temperature and solvent polarity play a significant role in influencing the thermodynamic and photophysical properties of drugs, particularly during the drug optimization and design phases. This study investigates the impact of temperature and solvent polarity on the thermodynamic and optical properties of FA using density functional theory (DFT) with the B3LYP functional approach and the 6-311++G(d, p) basis set under various solvent and gas conditions. Additionally, vertical UV-vis absorption and emission spectra of FA in different solvent polarities and gas phases were analyzed using time-dependent density-functional theory (TDDFT) with the B3LYP method and the 6-31++G(d, p) basis set. Applying Koopman's theory, the chemical activity of FA was assessed based on the highest occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital (LUMO) values. The findings indicate that an increase in temperature within the range of 100–1000 K leads to elevated enthalpy, heat capacity, and entropy due to molecular vibrational activity, resulting in FA degradation and instability. Furthermore, thermodynamic parameters, HOMO and LUMO values, and the chemical activity of FA were also influenced by different solvent polarities. The absorption and emission spectra of FA exhibited a red shift due to interactions with solvents and solutes. Overall, this study analyzed the significance of environmental factors such as temperature and solvent polarity in pharmaceutical design and optimization processes to enhance drug efficacy and stability.

An approach for an enhanced anticancer activity of ferulic acid-loaded polymeric micelles via MicroRNA-221 mediated activation of TP53INP1 in caco-2 cell line

Ferulic acid (FA) has powerful antioxidant and antitumor activities, but it has low bioavailability owing to its poor water solubility. Our aim is to formulate polymeric mixed micelles loaded with FA to overcome its poor solubility and investigate its potential anticancer activity via miRNA-221/TP53INP1 axis-mediated autophagy in colon cancer. A D-optimal design with three factors was used for the optimization of polymeric mixed micelles by studying the effects of each of total Pluronics mixture (mg), Pluronic P123 percentage (%w/w), and drug amount (mg) on both entrapment efficiency (EE%) and particle size. The anticancer activity of FA and Tocopheryl polyethylene glycol 1000 succinate (TPGS) mixed micelles formula (O2) was assessed by MTT and flow cytometry. O2 showed an EE% of 99.89%, a particle size of 13.86 nm, and a zeta potential of − 6.02 mv. In-vitro drug release studies showed a notable increase in the release rate of FA from O2, as compared to the free FA. The (IC50) values for FA from O2 and free FA were calculated against different cell lines showing a prominent IC50 against Caco-2 (17.1 µg/ml, 191 µg/ml respectively). Flow cytometry showed that FA caused cell cycle arrest at the G2/M phase in Caco-2. RT-PCR showed that O2 significantly increased the mRNA expression level of Bax and CASP-3 (4.72 ± 0.17, 3.67 ± 0.14), respectively when compared to free FA (2.59 ± 0.13, 2.14 ± 0.15), while miRNA 221 levels were decreased by the treatment with O2 (0.58 ± 0.02) when compared to free FA treatment (0.79 ± 0.03). The gene expression of TP53INP1 was increased by the treatment with O2 compared to FA at P < 0.0001. FA-loaded TPGS mixed micelles showed promising results for enhancing the anticancer effect of FA against colorectal cancer, probably due to its enhanced solubility. Thus, FA-loaded TPGS mixed micelles could be a potential therapeutic agent for colorectal cancer by targeting miRNA-221/TP53INP1 axis-mediated autophagy.

Mitigating effect of ferulic acid on di-(2-ethylhexyl) phthalate-induced neurocognitive dysfunction in male rats with a comprehensive in silico survey

Di-(2-ethylhexyl) phthalate (DEHP) is the most abundant phthalate threatening public health-induced neurotoxicity. This neurotoxicity is associated with behavioral and biochemical deficits in male rats. Our study investigated the neuroprotective effect of ferulic acid (FA) on male rats exposed to DEHP. Thirty-two male Wistar rats were assigned to four groups. Group I control rats received corn oil, group II intoxicated rats received 300 mg/kg of DEHP, group III received 300 mg/kg of DEHP + 50 mg/kg of FA, and group IV received 50 mg/kg of FA, all agents administrated daily per os for 30 days. Anxiety-like behavior, spatial working memory, and recognition memory were assessed. Also, brain oxidative stress biomarkers, including brain malondialdehyde (MDA), reduced glutathione (GSH), nitric oxide (NO), superoxide dismutase (SOD), brain-derived neurotrophic factor (BDNF) as well as heme oxygenase-1 (HO-1) were measured. Moreover, brain histopathology examinations associated with immunohistochemistry determination of brain caspase-3 were also evaluated. Furthermore, docking simulation was adapted to understand the inhibitory role of FA on caspase-3 and NO synthase. Compared to DEHP-intoxicated rats, FA-treated rats displayed improved cognitive memory associated with a reduced anxious state. Also, the redox state was maintained with increased BNDF levels. These changes were confirmed by restoring the normal architecture of brain tissue and a decrement in the immunohistochemistry caspase-3. In conclusion, FA has potent antioxidant and antiapoptotic properties that confirm the neuroprotective activity of FA, with a possible prospect for its therapeutic capabilities and nutritional supplement value.

Alkyl ferulic acid esters: Evaluating their structure and antibacterial properties.

Ferulic acid (FA) is a natural antibacterial agent rich in plants, FA has excellent antioxidant and antibacterial properties. However, because of its short alkane chain and large polarity, FA is difficult to penetrate the soluble lipid bilayer in the biofilm to enter the cell to play an inhibitory role, limiting its biological activity. To improve the antibacterial activity of FA, with the catalytic condition of Novozym 435, four alkyl ferulic acid esters (FCs) with different alkyl chain lengths were obtained by fatty alcohols (including 1-propanol (C3), 1-hexanol (C6), nonanol (C9), and lauryl alcohol (C12)) modification. The effect of FCs on P. aeruginosa was determined by Minimum inhibitory concentrations (MIC), minimum bactericidal concentrations (MBC), Growth curves, alkaline phosphatase (AKP) activity, crystal violet method, scanning electron microscopy (SEM), membrane potential, PI, cell contents leakage. Results showed that the antibacterial activity of FCs increased after esterification, and the antibacterial activity significantly increased and then decreased with the extension of the alkyl chain of the FCs. Hexyl ferulate (FC6) showed the best antibacterial activities against E. coli and P. aeruginosa (MIC for E. coli was 0.5 mg/ml, MIC for P. aeruginosa was 0.4 mg/ml). And Propyl ferulate (FC3) and FC6 showed the best antibacterial activities S. aureus and B. subtilis (MIC for S. aureus was 0.4 mg/ml, The MIC of B. subtilis was 1.1 mg/ml). In addition, the growth, AKP activity, bacterial biofilm, bacterial cell morphology, membrane potential and cell contents leakage of P. aeruginosa after different FCs were investigated, which found that FCs could damage the cell wall of P. aeruginosa and showed different effects on the P. aeruginosa cell biofilm. FC6 showed the best inhibition on the biofilm formation of P. aeruginosa cells, which caused the surface of P. aeruginosa cells to be rough and wrinkled. Some P. aeruginosa cells showed aggregation and adhesion, even rupture. The membrane hyperpolarization was obvious, which appeared as holes, leading to cell contents leakage (protein and nucleic acid). All these results concluded that the antibacterial activities FCs against foodborne pathogens depended on different fatty alcohol esterification of FA. FC6 showed the best inhibition on P. aeruginosa due to its effect on P. aeruginosa cell walls and biofilms and the leak of the cell contents. This study provides more practical methods and a theoretical basis for giving full play to the bacteriostatic effect of plant FA.

Antifungal activity and inhibitory mechanisms of ferulic acid against the growth of Fusarium graminearum

Fusarium graminearum is a pathogen that can infect wheat, corn and other grain crops, resulting in a reduction in grain yield and nutritional value and even causing serious harm to public health. Ferulic acid (FA) is popularly extracted from a variety of traditional Chinese medicines, such as ferula, asafoetida and angelica, and is a promising fungicide for the preservation of foods due to its antibacterial, antioxidant and anti-inflammatory functions. Based on its efficacy, the inhibitory activity of FA against F. graminearum was evaluated and the involved mechanism was investigated as well. The EC50 and EC90 values were approximately 20 μg/mL and 100 μg/mL, respectively, according to the mycelial dry weight test. TEM and SEM analyses after FA treatment revealed that the cell membrane of hyphae was impaired and showed the following characteristics: coarse surface with wrinkles, blurry ultrastructure edges, and cytoplasmic leakage. In addition, cell integrity and permeability analyses were performed to identify its antifungal mechanism. After FA treatment, the fluorescence intensity of mycelia after PI staining increased significantly (p < 0.001), and the high concentration group showed a continuous rise in extracellular relative conductivity and more significant leakage of nucleic acids and protein. Moreover, FA inhibited ergosterol synthesis in the F. graminearum cell membrane, which confirmed that the target site of FA antifungal action was the cell membrane.

Fucoidan-ferulic acid nanoparticles alleviate cisplatin-induced acute kidney injury by inhibiting the cGAS-STING pathway

Fucoidan (FU) is a natural sulfated polysaccharide with certain biological activity and has been shown to be an excellent nano-delivery material. In this study, ferulic acid (FA)-loaded FU nanoparticles (FA/FU NPs) were prepared and their nephroprotective mechanism was investigated. With a particle size of 158.6 ± 4.5 nm, FA/FU NPs increased the antioxidant activity of FA in vitro, possibly related to the increased dispersity of FA. In vitro results demonstrated that FA/FU NPs significantly protected human renal proximal tubule (HK−2) cells from cisplatin-induced damage, possibly by suppressing cisplatin-induced DNA damage and activating the cGAS-STING pathway. Furthermore, in vivo experiments confirmed that FA/FU NPs protected mice from cisplatin-induced acute kidney injury (AKI). Mechanistic studies confirmed that FA/FU NPs exerted nephroprotective effects by reducing MDA activity and increasing GSH and SOD activity. Our results demonstrated the potential of FU for delivering poorly soluble drug FA and protecting against cisplatin-induced AKI.

Loading ferulic acid into β-cyclodextrin nanosponges; antibacterial activity, controlled release and application in pomegranate juice as a copigment agent

Ferulic acid (FA) is a natural antioxidant with antimicrobial activity and its application is restricted due to poor water solubility. To overcome this limitation, FA was entrapped into cyclodextrin nanosponges (CD-NSs). The antibacterial activity of FA was assessed using the microdilution method which showed a higher antibacterial activity after encapsulation. A controlled release of FA was observed in simulated gastrointestinal environment and food simulants. Furthermore, the application of FA-loaded nanosponges (FA-NS) was investigated in pomegranate juice (PJ). Anthocyanins are the main phenolic compounds of PJ that are sensitive to different environmental conditions. Copigmentation of anthocyanins with other phenolic acids can help to improve their stabilization. The antioxidant activity and phenolic content of all PJ samples (free PJ and PJ containing pure FA and FA-NS) were enhanced during storage while the anthocyanin content of all PJ samples was lessened during the storage. However, the samples containing FA-NS compared to the other samples could better preserve the anthocyanin content. Enhanced solubility of FA after incorporation into CD-NSs can induce higher interaction of FA with other components in PJ and improve their stability to preserve during the storage. These results may pave the way for the application of FA-NS as a copigment agent in juices containing anthocyanins to improve their stability during storage.

In Search of Resistance Against Fusarium Ear Rot: Ferulic Acid Contents in Maize Pericarp Are Associated With Antifungal Activity and Inhibition of Fumonisin Production.

Fusarium verticillioides is a fungal pathogen of maize that causes seedling blight, stem rot, and Fusarium ear rot. Fungal infestation of maize kernels and ears affects grain quality from the ensuing mycotoxin buildup. Among the mycotoxins produced by F. verticillioides, fumonisins accumulate to high levels in Fusarium-infected maize kernels, fumonisin B1 (FB1) being the most abundant in naturally infected maize. Achieving resistance to Fusarium ear rot has been challenging, as various environmental factors facilitate fungal infection. Among the maize grain components that contribute to resistance to F. verticillioides infection, the pericarp is the first barrier faced by the fungus and thus plays a key role. Phenolic acids are major constituents of maize pericarp, of which ferulic acid (FA) is the predominant molecular species. In this work, we explored the relationship between FA levels, fungal infection, and FB1 production in 51 maize genotypes and whether the antioxidant activity of FA might play a role. We confirmed that FA is a major component of the seed pericarp, whose levels as bound FA varied between 4.5 and 26.3 mg/g across maize genotypes. We selected two pools of five maize varieties, with contrasting FA contents: low FA (LFA; 6.14 ± 0.40 mg/g) and high FA (HFA; 15.49 ± 1.31 mg/g). In vitro, HFA extracts inhibited fungal growth with effects comparable to FA concentrations in the 0.25–0.50 mM range. We also established a kernel assay to study F. verticillioides colonization and FB1 production in the LFA and HFA genotypes. Fungal colonization was significantly lower in HFA genotypes relative to LFA genotypes, based on ergosterol levels. Moreover, FB1 production was also inhibited in the HFA genotypes. Importantly, the antioxidant activity of maize pericarp extracts was associated with FA contents, with HFA extracts exhibiting a greater antioxidant activity than LFA extracts. Overall, our results highlight the role of FA and its antioxidant activity on resistance to Fusarium ear rot and provide the basis of a phenotypic trait that can be deployed for breeding selection.

Ferulic Acid From Plant Biomass: A Phytochemical With Promising Antiviral Properties.

Plant biomass is a magnificent renewable resource for phytochemicals that carry bioactive properties. Ferulic acid (FA) is a hydroxycinnamic acid that is found widespread in plant cell walls, mainly esterified to polysaccharides. It is well known of its strong antioxidant activity, together with numerous properties, such as antimicrobial, anti-inflammatory and neuroprotective effects. This review article provides insights into the potential for valorization of FA as a potent antiviral agent. Its pharmacokinetic properties (absorption, metabolism, distribution and excretion) and the proposed mechanisms that are purported to provide antiviral activity are presented. Novel strategies on extraction and derivatization routes, for enhancing even further the antiviral activity of FA and potentially favor its metabolism, distribution and residence time in the human body, are discussed. These routes may lead to novel high-added value biorefinery pathways to utilize plant biomass toward the production of nutraceuticals as functional foods with attractive bioactive properties, such as enhancing immunity toward viral infections.

Virtual prediction of purple rice ferulic acid as anti-inflammatory of TNF-α signaling

Purple rice is one of the main sources of ferulic acid (FA). Some studies reported anti-inflammatory properties of FA, but the interaction of FA with TNF-α signaling has not been elucidated. TNF-α is a target for anti-inflammatory drug research due to its major role in the inflammatory process. This study aims to investigate the interaction of FA with TNF-α and TNF-α receptor (TNFR) through in silico study and evaluate the drug-like properties and biological activity of FA. The interactions among FA (CID 445858), TNF-α (2AZ5), and TNFR (1NCF) were docked by Hex 8.0.0 Cuda, then visualized by Discovery Studio 2020 and LigPlot V.1.4.5. Apigenin-7-glucuronide (AG, CID 5319484) was used as the positive control. The drug-like properties were predicted by Lipinski’s rule of five and the biological activity was analyzed by PASS online. FA showed good properties as a drug-like molecule and biological activity as an anti-inflammatory. FA also showed good interaction with TNF-α and TNFR. FA bound to TNF-α at Asn92(B), Val91(B), Leu93(B), Phe124(B), Phe124(D), and Leu93(D) residues with docking energy of -214.6 kJ/mol, and bound to TNFR at Pro16(A), Glu56(B), Cys55(B), Glu54(B) residues with docking energy of -191.1 kJ/mol. FA could inhibit TNF-α – TNFR interaction by binding to TNFR at Glu54 residue, the same inhibition mechanism to AG which bind to TNFR at Glu54 and Val90. The current study shows that FA has the potential as an anti-inflammatory of TNF-α signaling and can be developed as an oral anti-inflammatory drug candidate.

MICROBIAL PRODUCTION OF FERULIC ACID AND OPTIMIZATION OF THE MEDIUM PARAMETERS USING FRACTIONAL FACTORIAL DESIGN

Phenolics are widely distributed in plant kingdom and are therefore, an integral part of the diet, with significant amounts being reported in vegetables, fruits, and beverages. Various phenolic compounds have attracted the attention of food and medical scientists because of their fragrance, aroma, antioxidant, anti-inflammatory properties and ability to combat human diseases. Of these, Ferulic Acid (FA), a hydroxy cinnamic acid (related to trans-cinnamic acid), being natural, is of great demand in the food industry. As a component of lignin, FA is a precursor in the manufacture of other aromatic compounds. In our study, FA was produced using Lactobacillus spp. isolates and standard culture of Lactobacillus plantarum ATCC 8014. FA was extracted and partially characterized using Thin Layer Chromatography (TLC), Absorption maxima (λm) analysis and High Performance Liquid Chromatography (HPLC). Further, optimization of the fermentation medium was done using Factorial Fractional Design (FFD). Preliminary confirmation of the extracted FA was done using TLC, spectral analysis and purity assessed by HPLC. FA could be produced using Lactobacillus sp. and agro industrial waste viz., wheat bran, leading to a cost-effective protocol and product. Further, medium was optimized for the production of FA using FFD and it was observed that medium containing5.75% Wheat bran &amp; 0.18% Tween 80 is optimum for the production of FA. The antimicrobial activity of FA was noteworthy against Aspergillus flavus and E. coli.

MICROBIAL PRODUCTION OF FERULIC ACID AND OPTIMIZATION OF THE MEDIUM PARAMETERS USING FRACTIONAL FACTORIAL DESIGN

Phenolics are widely distributed in plant kingdom and are therefore, an integral part of the diet, with significant amounts being reported in vegetables, fruits, and beverages. Various phenolic compounds have attracted the attention of food and medical scientists because of their fragrance, aroma, antioxidant, anti-inflammatory properties and ability to combat human diseases. Of these, Ferulic Acid (FA), a hydroxy cinnamic acid (related to trans-cinnamic acid), being natural, is of great demand in the food industry. As a component of lignin, FA is a precursor in the manufacture of other aromatic compounds. In our study, FA was produced using Lactobacillus spp. isolates and standard culture of Lactobacillus plantarum ATCC 8014. FA was extracted and partially characterized using Thin Layer Chromatography (TLC), Absorption maxima (λm) analysis and High Performance Liquid Chromatography (HPLC). Further, optimization of the fermentation medium was done using Factorial Fractional Design (FFD). Preliminary confirmation of the extracted FA was done using TLC, spectral analysis and purity assessed by HPLC. FA could be produced using Lactobacillus sp. and agro industrial waste viz., wheat bran, leading to a cost-effective protocol and product. Further, medium was optimized for the production of FA using FFD and it was observed that medium containing5.75% Wheat bran &amp; 0.18% Tween 80 is optimum for the production of FA. The antimicrobial activity of FA was noteworthy against Aspergillus flavus and E. coli.

Ferulic Acid and Salicylic Acid Foliar Treatments Reduce Short-Term Salt Stress in Chinese Cabbage by Increasing Phenolic Compounds Accumulation and Photosynthetic Performance.

Salinity stress is one of the most damaging abiotic stresses to plants, causing disturbances in physiological, biochemical, and metabolic processes. The exogenous application of natural metabolites is a useful strategy to reduce the adverse effects of stress on crops. We investigated the effect of foliar application of salicylic acid (SA) and ferulic acid (FA) (10–100 μM) on short-term salt-stressed (150 mM NaCl, 72 h) Chinese cabbage plants. Subsequently, proline level, photosynthetic performance, phenolic metabolites with special focus on selected phenolic acids (sinapic acid (SiA), FA, SA), flavonoids (quercetin (QUE), kaempferol (KAE)), and antioxidant activity were investigated in salt-stressed and phenolic acid-treated plants compared with the corresponding controls. Salt stress caused a significant increase in SA and proline contents, a decrease in phenolic compounds, antioxidant activity, and photosynthetic performance, especially due to the impairment of PSI function. SA and FA treatments, with a concentration of 10 μM, had attenuated effects on salt-stressed plants, causing a decrease in proline and SA level, and indicating that the plants suffered less metabolic disturbance. Polyphenolic compounds, especially FA, SiA, KAE, and QUE, were increased in FA and SA treatments in salt-stressed plants. Consequently, antioxidant activities were increased, and photosynthetic performances were improved. FA resulted in a better ameliorative effect on salt stress compared to SA.

Anxiolytic activity of ferulic acid in the light-dark test in zebrafish

The anxiety disorders belong to a group of mental disorders in which the patients present excessive fear and worry. Studies with ferulic acid have shown positive results on treating depressive symptoms. As many antidepressive drugs are effective in treating anxiety, the objective of the present study was to evaluate ferulic acid’s anxiolytic activity and possible mechanism of action in the light-dark test in zebrafish. To evaluate anxiolytic activity, the light-dark preference test was performed after exposure of the animals to ferulic acid or positive control (clonazepam or fluoxetine). Ferulic acid increased the time spent in the clear compartment at concentrations of 250 and 500 mg/L, not differing from the groups exposed to clonazepam or fluoxetine. To evaluate the possible mechanism of action, pre-exposure to flumazenil was carried out, followed by exposure to ferulic acid or positive control, with subsequent testing. Pre-exposure to flumazenil caused a significant reduction in the time spent in the clear compartment of ferulic acid and clonazepam groups but did not alter the effect of exposure to fluoxetine. These results suggest that ferulic acid promotes an anxiolytic effect, possibly through an action at the benzodiazepine binding site at the GABAA receptor.

Ferulic Acid Activity in Topical Formulations: Technological and Scientific Prospecting.

Ferulic acid is a phenolic compound widely distributed in monocotyledons, with several applications, especially in pharmaceutical and dermo-cosmetic industries. It has proven antioxidant and anti- inflammatory activities, among others, which are mainly ascribed to its molecular structure. The main factor that can lead to serious skin damages like inflammation, dryness, wrinkles, and cancer is the exposure to UV radiation that is responsible for an increased level of radical oxygen species. This review aims to evaluate the application of ferulic acid in topical formulations and the technologies used to enhance its bioavailability and stability, as well as to get a clearer picture of its effects by in vivo and in vitro studies. It covers technological publications in the WIPO, EPO, INPI, and USPTO databases and scientific publications in the PubMed, Web of Sciences, and Science Direct databases, exploring the trend and application of this compound by country and year of publication. Both the scientific and technological analyses showed the importance and tendency in the association of the Ferulic Acid and other vitamins and actives. The synergic effect certainly provides a better result, performance, and stability of the compounds, which cleared the great spectrum and applicability of the Ferulic Acid in topical formulations. The present literature survey revealed that ferulic acid exerts an important activity in several formulations for topical application and improved the stability and bioavailability when combined with new technologies and methods, showing an open path to target the treatment of skin disorders.

Ferulic Acid Prevents Angiogenesis Through Cyclooxygenase-2 and Vascular Endothelial Growth Factor in the Chick Embryo Chorioallantoic Membrane Model.

This study was designed to verify the antiangiogenic activity of ferulic acid (FA) and its potency to inhibit cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF) expression in the chorioallantoic membrane (CAM) model. Moreover, we verified its mechanism of action by docking the molecule on COX-2, tyrosine kinase, and VEGF-2 proteins in silico. An antiangiogenesis assay of FA at doses of 30, 60, and 90 μg was performed using the CAM of chicken eggs that were 9 days old and stimulated by 60 ng of basic fibroblast growth factor. Celecoxib (60 μg) was used as the reference drug. The inhibitory activity on VEGF and COX-2 expression was determined by immunohistochemistry assay. Molecular docking of FA was accomplished by Molegro Virtual Docker program ver. 5.5 on COX-2 enzyme (PDB ID 1CX2), tyrosine kinase receptor (PDB ID 1XKK), and VEGF-2 receptor (PDB ID 4ASD). FA at doses of 30, 60, and 90 μg significantly prevented angiogenesis in the CAM model, which was represented as inhibitory activity against endothelial cells of blood vessels (42.6-70.7%) and neovascularization (43.0-86.6%). The inhibitory activity of FA against VEGF expression was stronger than its action on COX-2 expression. Molecular docking on VEGF-2 receptor resulted in an RS value of FA of -73.844 kcal/mol and for celecoxib it was -94.557 kcal/mol. The RS value on tyrosine kinase of FA was -84.954 kcal/mol, while on celecoxib it was -93.163 kcal/mol. Docking on COX-2 receptor gave an RS value of FA of -73.416 kcal/mol, while for celecoxib it was -118.107 kcal/mol. Reductions in VEGF-2 and COX-2 expression due to treatment with FA at the dose range 30-90 μg appeared to be related to angiogenesis inhibition, which was shown by two parameters, namely inhibition of neovascularization and endothelial cell growth in blood vessels. It was concluded that FA is a promising antiangiogenic therapeutic agent especially at the early stage, and this activity can arise from inhibitory action on COX-2 and VEGF-2 proteins.

Comparison of Antiaging and Antioxidant Activities of Protocatechuic and Ferulic Acids

Background: Skin-aging is a progressive changes in the skin combine with cumulative extrinsic factors which are mostly caused by free radicals caused by exposure to lots of free radicals molecules from pollutant, wrongly food intake, or too much sun bathing. These free radicals can be tackled by a treatment using antioxidants. Prevention of aging can be done by escalating antioxidant intake. Protocatechuic acid (PCA) and Ferulic acid (FA) have been known for their scavenging properties on free radicals and antiaging activity. Antioxidant and antiaging activity of both compounds have not been compared comprehensively before. Hence, current study was conducted to compare the potential of PCA and FA for their antioxidant and antiaging activities using various methods.Materials and Methods: Antioxidant analysis of PCA and FA was conducted using H2O2 scavenging assay, 2,2’-azinobis-3-ethylbenzo-thiazoline-6-sulfonic acid (ABTS), 2,2-diphenyl-1-picrylhydrazil (DPPH), and ferric reducing antioxidant power (FRAP). Meanwhile, antiaging activities of PCA and FA were examined using inhibitory activities of tyrosinase, collagenase, elastase, hyaluronidase and tyrosinase.Results: IC50 of scavenging activity of ABTS were 125.18 µg/mL (PCA) and 35.55 µg/mL (FA), inhibition activity of collagenase were 126.16 µg/mL (PCA) and 52.85 µg/mL (FA) and inhibition activity of tyrosinase were 246.42 µg/mL (PCA), 253.58 µg/mL (FA).Conclusion: In conclusion, FA has better ABTS scavenging and collagenase inhibition activities compared to PCA. Meanwhile, PCA has better activity of tyrosinase inhibition than FA.Keywords: antioxidant, antiaging, ferulic acid, protocatechuic acid

Ferulic acid isolated from propolis inhibits porcine parvovirus replication potentially through Bid-mediate apoptosis

Propolis from honeybee hives, which is a traditional Chinese medicine, is widely used in veterinary clinics. Many compounds have been identified and isolated from propolis. Ferulic acid (FA), one of the propolis components, previous studies have proven that it has antiviral effects. To study the mechanism of FA antiviral effects, experiments such as immunofluorescence, quantitative real-time PCR and immunoblotting were introduced. In porcine kidney (PK-15) cells, PPV infection induced the expression of the proapoptotic genes Bid, Bad, Bim and Bak, disrupted mitochondrial membrane potential, promoted mitochondria-mediated, caspase-dependent apoptotic signaling and induced apoptosis. Furthermore, the infected PK-15 cells had increased intracellular reactive oxygen species (ROS) generation. FA treatment, however, reversed these effects and increased cell viability. FA treatment also significantly decreased the PPV-induced expression of Bid, Cyt-c and Apaf-1, suggesting that ROS were involved in the activation of the mitochondria-mediated apoptosis pathway. This in vitro study showed that the antiviral activity of FA was probably associated with inhibiting the replication of PPV by blocking proapoptotic factors such as Bid, Bcl-2 and Mcl-1, and attenuating the mitochondria-mediated response by inhibiting the activation of the Bid-related signaling pathway. Pharmacological inhibitors inhibited PPV-induced apoptosis by blocking Bid, and also suppressed the expression of Caspase family proteins in ppv-induced apoptosis. Taken together, our results suggested that PPV induced PK-15 cell apoptosis via activation of Bid and Bid-related signaling pathways and that the mitochondria act as the mediators of these pathways. FA effectively and extensively attenuated this PPV action, and thus is a potential antiviral agent against PPV.

Antioxidative potential of ferulic acid phenoxyl radical

The vast majority of previous studies dealing with antioxidant potency of (poly)phenols does not investigate the fate of phenoxyl radical obtained after single free radical scavenging. We investigated possible pathways of inactivation of ferulic acid phenoxyl radical (FAPR) using DFT method. Direct coupling with a set of 10 physiologically important free radicals, H-atom donation and dimerization were analysed by estimation of Gibbs free energy changes related to these processes. The former two processes are thermodynamically feasible to inactivate more dangerous free radicals such as hydroxyl, alkoxyl and carbon-centered radicals. Among dimerization reactions, the least energy demanding is formation of C-5−C-5 dimer of ferulic acid (FA), which has higher antiradical potency than FA itself. Obtained results reveal that FAPR, a priori considered as stable and unreactive, may contribute to the overall antioxidant activity of FA. This is a beneficial behavior, which makes FA a particularly valuable protector against oxidative stress. Hence, the contribution of phenoxyl radicals to the antioxidant activity of (poly)phenolic compounds should be taken into account, what has been scarcely considered until now.

The Temperature Effect on Ultrasonic-assisted of Synthesis Methyl Ferulate and Its Antiplatelet Assay

&lt;p&gt;Ferulic acid (FA) has been reported to have antiplatelet activity through indirectly inhibiting P2Y12 receptor. In order to increase the activity of FA, by improving its lipophilicity, so that it is easier to enter the cell, synthesis methyl ferulate was conducted through Fisher esterification. Ultrasonic waves were utilized as source of energy emitted through water as the medium at two various of temperature, i.e., 55 °C and 65 °C. The purposes of this study are to produce methyl ferulate and to determine the reaction constant rate (&lt;em&gt;k&lt;/em&gt;) and its energy activation (&lt;em&gt;E&lt;sub&gt;a&lt;/sub&gt;&lt;/em&gt;), at temperature of 55 °C and 65 °C. Moreover, the biological activity as antiplatelet was investigated at dose 20 mg/kg BW. The antiplatelet assay was conducted by clotting time and bleeding time methods. The results were analyzed by one way ANOVA program (&lt;em&gt;P&lt;/em&gt;&amp;lt;0.05). The yield of methyl ferulate are 50.3% and 67.1% at 55 °C and 65 °C, respectively. The &lt;em&gt;k&lt;/em&gt; value at 55°C is 4x10&lt;sup&gt;-5&lt;/sup&gt; cons&lt;sup&gt;-1&lt;/sup&gt;min&lt;sup&gt;-1&lt;/sup&gt;, while that of at 65 °C is 9x10&lt;sup&gt;-5&lt;/sup&gt; cons&lt;sup&gt;-1&lt;/sup&gt;min&lt;sup&gt;-1&lt;/sup&gt;. The clotting time and bleeding time of methyl ferulate obtained were 265 sec and 175 sec, respectively. The antiplatelet activity of methyl ferulate is better than ferulic acid.&lt;/p&gt;