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Antioxidant Properties of Ferulic Acid and Its Possible Application


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Ferulic acid has low toxicity and possesses many physiological functions (anti-inflammatory, antioxidant, antimicrobial activity, anticancer, and antidiabetic effect). It has been widely used in the pharmaceutical, food, and cosmetics industry. Ferulic acid is a free radical scavenger, but also an inhibitor of enzymes that catalyze free radical generation and an enhancer of scavenger enzyme activity. Ferulic acid has a protective role for the main skin structures: keratinocytes, fibroblasts, collagen, elastin. It inhibits melanogenesis, enhances angiogenesis, and accelerates wound healing. It is widely applied in skin care formulations as a photoprotective agent, delayer of skin photoaging processes, and brightening component. Nonetheless, its use is limited by its tendency to be rapidly oxidized.
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Review Article
Skin Pharmacol Physiol 2018;31:332–336
Antioxidant Properties of Ferulic Acid
and Its Possible Application
Kamila Zduńska Agnieszka Dana Anna Kolodziejczak Helena Rotsztejn
Chair of Cosmetology, Department of Cosmetology and Aesthetic Dermatology, Faculty of Pharmacy, Medical
University of Łódź, Łódź, Poland
Received: February 22, 2018
Accepted after revision: July 2, 2018
Published online: September 20, 2018
Kamila Zduńska
Department of Cosmetology and Aesthetic Dermatology, Faculty of Pharmacy
Medical University of Łódź, Muszyńskiego 1 Street
PL–91-151 Łódź (Poland)
E-Mail kamila.zdunska @
© 2018 S. Karger AG, Basel
DOI: 10.1159/000491755
Ferulic acid antioxidant · Photoaging
Ferulic acid has low toxicity and possesses many physiologi-
cal functions (anti-inflammatory, antioxidant, antimicrobial
activity, anticancer, and antidiabetic effect). It has been
widely used in the pharmaceutical, food, and cosmetics in-
dustry. Ferulic acid is a free radical scavenger, but also an
inhibitor of enzymes that catalyze free radical generation
and an enhancer of scavenger enzyme activity. Ferulic acid
has a protective role for the main skin structures: keratino-
cytes, fibroblasts, collagen, elastin. It inhibits melanogenesis,
enhances angiogenesis, and accelerates wound healing. It is
widely applied in skin care formulations as a photoprotec-
tive agent, delayer of skin photoaging processes, and bright-
ening component. Nonetheless, its use is limited by its ten-
dency to be rapidly oxidized. © 2018 S. Karger AG, Basel
Properties of Ferulic Acid
Ferulic acid ([E]-3-[4-hydroxy-3-methoxy-phenyl]
prop-2-enoic acid) (Fig.1) belongs to the phenolic acid
group commonly found in plant tissues [1]. Phenolic ac-
ids are secondary metabolites of varying chemical struc-
tures and biological properties. The plants are mainly
found in bound form as ester or glycosides, lignin com-
ponents, and hydrolysis tannins [2, 3]. In terms of chem-
ical structure, they can be divided into derivatives of cin-
namic and benzoic acid, varying in number and substitu-
tion of hydroxyl and methoxy groups, and phenolic acids
of unusual character. An additional group is the depside,
which is a combination of two or more phenolic acids [2].
Ferulic acid, like caffeic, p-coumaric, synapine, syryte,
and vanillin acids, is the most common cinnamic acid de-
rivative [3].
Ferulic acid is most commonly found in whole grains,
spinach, parsley, grapes, rhubarb, and cereal seeds, main-
ly wheat, oats, rye, and barley (Table 1). One of the most
important role of phenolic acids, especially cinnamic acid
derivatives, is their antioxidant activity, which depends
primarily on the number of hydroxyl and methoxy groups
attached to the phenyl ring [3, 4]. Ferulic acid is more eas-
ily absorbed into the body and stays in the blood longer
than any other phenolic acids. Ferulic acid is considered
to be a superior antioxidant [5]. Ferulic acid has low tox-
icity and possesses many physiological functions, includ-
ing anti-inflammatory, antimicrobial, anticancer (for
instance lung, breast, colon and skin cancer), anti-ar-
rhythmic, and antithrombotic activity, and it also dem-
onstrated antidiabetic effects and immunostimulant
properties, and it reduces nerve cell damage and may help
Ferulic Acid Properties and Application
Skin Pharmacol Physiol 2018;31:332–336
DOI: 10.1159/000491755
to repair damaged cells. Furthermore, it is a sports sup-
plement because it can neutralize free radicals in muscle
tissue (alleviate muscle fatigue). It has been widely used
in pharmaceutics and food. Moreover, it is widely applied
in skin care formulations as a photoprotective agent (sun-
screens), delayer of skin photoaging processes, and
brightening component. Nonetheless, its use is limited by
its tendency to be rapidly oxidized [3, 5–7].
Antioxidative Activity of Ferulic Acid
The antioxidant action mechanism of ferulic acid is
complex, mainly based on the inhibition of the formation
of reactive oxygen species (ROS) or nitrogen, but also the
neutralization (“sweeping”) of free radicals. In addition,
this acid is responsible for chelating protonated metal
ions, such as Cu(II) or Fe(II) [8, 9]. Ferulic acid is not only
a free radical scavenger, but also an inhibitor of enzymes
that catalyze free radical generation and an enhancer of
scavenger enzyme activity. It is directly related to its
chemical structure [3, 10–12]. Its antioxidating proper-
ties are primarily related to scavenging of free radicals,
binding transition metals such as iron and copper, and
lipid peroxidation prevention. The mechanism of anti-
oxidative activity of ferulic acid is the ability to form sta-
ble phenoxyl radicals, by the reaction of the radical mol-
ecule with the molecule of antioxidant. This makes it dif-
ficult to initiate a complex reaction cascade leading to the
generation of free radicals. This compound may also act
as hydrogen donor, giving atoms directly to the radicals.
This is particularly important for the protection of cell
membrane lipid acids, from undesired autoxidation pro-
cesses. As a secondary antioxidant, ferulic acids and their
related compounds are able to bind transition metals
such as iron and copper [13]. This prevents the formation
of toxic hydroxyl radicals, which lead to cell membrane
peroxidation [14].
Free radicals may also be formed through natural hu-
man physiological processes, such as cell respiration pro-
cess. These reactions are catalyzed by some enzymes,
among others xanthine oxidase and cyclooxygenase-2
[15]. It is suggested that inhibition of this enzyme could
prevent the changes caused by oxidative stress, including
photophobia [16]. Literature data report high efficacy of
ferulic acid and its derivatives in reducing xanthine oxi-
dase and cyclooxygenase activity. It is therefore believed
that ferulic acid reduces the amount of ROS produced by
the enzyme-catalyzed transformation [17].
Ferulic Acid as an Antioxidant against Negative UV
Highly exposed to UV-induced oxidative stress are ke-
ratinocytes and fibroblasts. ROS damage cells by the pro-
cess of lipid peroxidation, amino acid nitration, and even
DNA alterations, leading to cell death. Ferulic acid exhib-
its protective antioxidant properties, relative to various
skin structures and skin cells. Pluemsamran and partners
[18] proved that human endothelial cells and keratino-
cytes are much less susceptible to UVA-induced free rad-
ical damage when exposed to ferulic acid prior to irradia-
tion. It is believed that fibroblasts are exposed to UVA,
and the oxidative stress associated with it is greater than
that of the more superficially exposed keratinocytes. The
human fibroblast test showed that ferulic acid, adminis-
tered prior to exposure to UVA radiation, significantly re-
duced its adverse effects. It prevents UV-induced cell cycle
alterations and DNA damage and regulates the expression
of DNA repair genes. Hahn and partners [19] have shown
that intracellular ROS production is nearly 2-fold lower in
fibroblasts, which after irradiation with UVA, have ferulic
acid applied. Similar effects, in the form of protection
against free radical damage, have been observed in UVB-
exposed fibroblasts. In their research, Ambothi and Naga-
rajan [20] demonstrated the protective role of ferulic acid
applied to cells 30 min prior to exposure to UVB. Com-
pared to non-antioxidant-exposed cells, cytotoxicity, lipid
Fig. 1. Chemical structure of ferulic acid.
Table 1. Average ferulic acid content in plant-delivered foods
Foods Ferulic acid content, mg\kg
(in liquid mg/dm3)
Black currant 15
Black berry 10
Spinach 110
Tomatoes 700
Cucurbit 220
Wheat flour 150
Wheat bran 700
Oatmeal 145
Skin Pharmacol Physiol 2018;31:332–336
DOI: 10.1159/000491755
peroxidation, DNA alteration, antioxidant enzyme de-
cline, and reduced ROS production have been observed.
As UVB-induced ROS are one of the factors contributing
significantly to the development of skin cancer, ferulic
acid, which is known to lower their levels, has been found
to be a promising anticancer substance [20]. In another
study on human fibroblasts, ferulic acid proved to be an
effective substance that protects heat shock proteins from
degradation caused by hydrogen peroxide. As a result, the
cell-treated assay, prior to UV irradiation, showed signif-
icantly greater cell survival and less ROS-induced damage.
It has been proven to be closely related to significantly in-
creased levels of protective heat shock proteins compared
to the ferulic acid trial [21].
The activation of MMP-2 and MMP-9 under the influ-
ence of UVB radiation leads to photosaturation and ini-
tiation of photocancerogenesis processes [22]. Staniforth
et al. [23] have proven that these processes are effectively
prevented by the application of ferulic acid, just after ex-
posure to UVB radiation. Studies conducted on mice
showed a decrease in MMP-2 and MMP-9 activity by 37
and 83%, respectively, compared to the non-antioxidant-
exposed group [23]. Ferulic acid administered before ir-
radiation causes reduced cytotoxicity, less stimulation of
MMP-1 matrix metalloproteinases, and the generation of
ROS, compared to those exposed without antioxidant.
Also, the level of endogenous antioxidants, glutathione
and catalase, declined less and restored faster in the probe
with ferulic acid. The antioxidant tested proved to be ef-
fective not only for its free radical scavenging capacity but
also for its protective effect on the intracellular antioxi-
dant system [18]. Bian and partners [24] have demon-
strated a high efficacy of ferulic acid in the prevention of
H2O2-induced damage in human embryonic kidney cells.
Ferulic acid application, before exposure to H2O2, in-
creased cell survival and antioxidant enzyme levels (cata-
lase, superoxide dismutase). It has been stated that natu-
ral antioxidants such as ferulic acid can prevent adverse
changes in the body resulting from oxidative stress, in-
cluding collagen degradation [24].
Kawaguchi et al. [25] in their study on human fibro-
blasts showed that the main cause of elastosis (accumula-
tion of tropoelastin aggregates in skin reticular layer) are
free oxygen radicals. In the cells exposed to ROS, a sig-
nificant increase in tropoelastin mRNA expression was
observed. This process was reduced when the fibroblasts
were treated with catalase referred to as free radical scav-
engers. On this basis, the authors suggest that the use of
antioxidants such as ferulic acid could prevent the unfa-
vorable elastosis phenomenon [25, 26].
Angiogenesis Effect
In light of current knowledge, ferulic acid is believed
to have an angiogenesis effect by affecting the activity of
the main factors involved in it, i.e., vascular endothelial
growth factor (VEGF), platelet derived growth factor
(PDGF), and hypoxia-inducible factor 1 (HIF-1). Lin and
partners [27] in their research conducted using human
umbilical vein endothelial cells have shown that ferulic
acid enhances VEGF and PDGF expression and increases
the amount of hypoxia induced HIF-1, which generates
hypoxia-responsive responses. The authors believe that
ferulic acid is an effective substance that promotes the
formation of new vessels, as evidenced in both in vivo and
in vitro studies [27, 28].
Regeneration and Wound Healing Effect
The experiment conducted with the use of diabetic rats
demonstrated that ferulic acid accelerates the regenera-
tion and healing of wounds. The wound contraction per-
centage in rats to whom ferulic acid ointment was given
was 27% after 4 days, while in the group which did not
receive it, only 14% was administered after 4 days. After
16 days, rats treated with ferulic acid were almost com-
pletely healed (96%). In a control group that used an oint-
ment with 1% soframycin, standardized for treatment of
difficult-to-heal wounds, the wound was healed in 83%
after 16 days. There was also a faster onset of granulomas
in the ferulic acid group and faster epithelialization com-
pared to the control group [29]. Ghaisas and partners
[30], in a similar study, in addition to faster shrinking of
the wound and increased epithelialization, observed an
increased hydroxyproline and hydroxylysine synthesis
(major amino acids involved in wound healing, which are
the precursors of collagen), in the skin of diabetic rats to
whom ferulic acid was given. Moreover, it has been shown
that the use of ferulic acid ointment during healing inhib-
its lipid peroxidation and increases catalase, superoxide
dismutase, and glutathione. The authors suggest that this
phenomenon also significantly accelerates shrinkage of
the wound [30].
The Use of Ferulic Acid in Cosmetology and Aesthetic
Prevention of skin aging processes is one of the main
issues in contemporary cosmetology and aesthetic medi-
cine. Protection against the effects of external factors such
as UV radiation, air pollution, and free radical scavenging
plays an important role. The compounds with proven an-
tioxidative efficacy include ferulic acid. Initially, it was
used in cosmetics as a stabilizer of other commonly known
Ferulic Acid Properties and Application
Skin Pharmacol Physiol 2018;31:332–336
DOI: 10.1159/000491755
antioxidants such as vitamin C and vitamin E. Research
shows, though, that this compound is not only used as an
additional compound, but also an active ingredient with
antioxidative properties, which supports intracellular an-
tioxidant defense systems. Thanks to this, ferulic acid has
a protective role for the main skin structures (keratino-
cytes, fibroblasts, collagen, elastin), which is used in anti-
aging cosmetic formulations. Due to its ability to inhibit
the main enzyme of melanogenesis (tyrosinase), it is also
used in anti-blemish cosmetic formulations.
Ferulic acid is used in skin-lightening preparations be-
cause it inhibits tyrosinase activity (an enzyme involved
in melanogenesis) and inhibits melanocytic proliferation
[31, 32]. Staniforth et al. [23] noted that ferulic acid ab-
sorbs UV (290–320 nm). In order to increase the lighten-
ing effect, ferulic acid can be combined with other com-
pounds that also have a brightening effect, but by other
processes such as niacinamide (inhibits the movement of
melanosomes from melanocytes to keratinocytes). Saint-
Leger et al. [33] reported better effects of ferulic acid after
adding to it a keratolytic agent such as lipohydroxycar-
Ferulic acid is widely applied in skin care formulations
as a delayer of skin photoaging processes and photopro-
tective agent. Its application as a topical antioxidant has
become an important administration route due to main-
taining a high local concentration and the low cutaneous
metabolism [3]. Moreover, local ferulic acid penetrates
deeply into the skin, both acidic and neutral pH, in dis-
sociated and non-dissociated form [34]. Saija et al. [35]
studied the penetration of ferulic and caffeic acid soluble
in saturated aqueous solutions (pH 3 and pH 7.2) by a hu-
man skin cut in the Franz cells. It turned out that these
acids, regardless of pH, penetrated the stratum corneum.
It was noted that ferulic acid has a slightly better penetra-
tion capacity, which was explained by the known higher
lipophilicity of this acid. Research on phenolic antioxi-
dants has shown that ferulic acid improves the chemical
stability of L-ascorbic acid and α-tocopherol prepara-
tions, thereby increasing its photoprotection properties.
Ferulic acid is used in the production of face masks, as
well as antioxidant, protective, and moisturizing creams/
lotions. The recommended acid concentration in cosmet-
ic products of this type is from 0.5 to 1%. Ferulic acid is
also used in medical cosmetology and aesthetics salons. It
is most often used at a concentration of 12% and in com-
bination with vitamins C and hyaluronic acid. Ferulic
acid is used in the following procedures: microneedling
and non-needle mesotherapy, chemical peels, and groom-
ing treatments. Indications for the use of ferulic acid in-
clude skin aging and photoaging, hyperpigmentation
(melasma), seborrheic skin, and acne.
Research conducted so far has shown that ferulic acid
has strong antioxidant properties, which is directly in-
volved with its protective role to cellular structures and
inhibition of melanogenesis. It is increasingly used in cos-
metic preparations, mainly to inhibit photostage. At the
same time, it helps to reduce fine wrinkles and existing
discoloration. Good penetration into the skin, compati-
bility with many cosmetic formulas, and stabilizing prop-
erties of other ingredients make ferulic acid an increas-
ingly used compound in cosmetology.
This work was supported by statutory research activity of the
Department of Cosmetology and Aesthetic Dermatology, Faculty
of Pharmacy, Medical University of Lodz, No. 503/3-066-01/503-
Disclosure Statement
The authors declare no conflict of interest.
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... Ferulic acid (FA), commonly abundant in oranges, tomatoes, spinach, grains, and wheat bran, and largely used in the cosmetics and food industries, is one of the most studied phenolic acids for its neuroprotective, antioxidant, and anti-inflammatory effects [329][330][331][332][333]. Due to its structure, FA is a strong free-radical scavenger; moreover, it also inhibits ROS formation by reducing pro-oxidant enzyme levels and promoting antioxidant enzyme activities [330]. ...
... Ferulic acid (FA), commonly abundant in oranges, tomatoes, spinach, grains, and wheat bran, and largely used in the cosmetics and food industries, is one of the most studied phenolic acids for its neuroprotective, antioxidant, and anti-inflammatory effects [329][330][331][332][333]. Due to its structure, FA is a strong free-radical scavenger; moreover, it also inhibits ROS formation by reducing pro-oxidant enzyme levels and promoting antioxidant enzyme activities [330]. ...
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Citation: Varesi, A.; Campagnoli, L.I.M.; Carrara, A.; Pola, I.; Floris, E.; Ricevuti, G.; Chirumbolo, S.; Pascale, A. Non-Enzymatic Antioxidants against Alzheimer's Disease: Prevention, Diagnosis and Therapy. Abstract: Alzheimer's disease (AD) is a neurodegenerative disorder characterized by progressive memory loss and cognitive decline. Although substantial research has been conducted to elucidate the complex pathophysiology of AD, the therapeutic approach still has limited efficacy in clinical practice. Oxidative stress (OS) has been established as an early driver of several age-related diseases, including neurodegeneration. In AD, increased levels of reactive oxygen species mediate neuronal lipid, protein, and nucleic acid peroxidation, mitochondrial dysfunction, synaptic damage, and inflammation. Thus, the identification of novel antioxidant molecules capable of detecting, preventing, and counteracting AD onset and progression is of the utmost importance. However, although several studies have been published, comprehensive and up-to-date overviews of the principal anti-AD agents harboring antioxidant properties remain scarce. In this narrative review, we summarize the role of vitamins, minerals, flavonoids, non-flavonoids, mitochondria-targeting molecules, organosulfur compounds, and carotenoids as non-enzymatic antioxidants with AD diagnostic, preventative, and therapeutic potential, thereby offering insights into the relationship between OS and neurodegeneration.
... Ferulic acid has been shown to have many beneficial health effects including antioxidant properties (Zduńska et al. 2018). The antioxidant mechanisms of this compound are complex and are mainly centered on the inhibition of reactive oxygen or nitrogen species and the neutralization of free radicals. ...
... The antioxidant mechanisms of this compound are complex and are mainly centered on the inhibition of reactive oxygen or nitrogen species and the neutralization of free radicals. Due to its antioxidant activities, this compound is extensively used in cosmetic products for skin care (Zduńska et al. 2018). In addition, dietary ferulic acid enhanced antioxidant capacity and lipid metabolism in weaned piglets in an experiment (Wang et al. 2020). ...
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Simple phenolic acids are considered the most common and widely studied bioactive compounds belonging to plants’ secondary metabolites. The simple phenolic acids can be classified as hydroxybenzoic (gallic, protocatechuic, p-hydroxybenzoic, and syringic acids) and hydroxycinnamic acids (p-coumaric, caffeic, ferulic, and sinapic acids) and present high commercial value. This review comprehensively discussed the trends, classification, sources, biosynthesis, and biological properties of hydroxybenzoic and hydroxycinnamic acids, focusing on the antioxidant, anticancer, antitumor, anti-diabetic, anti-inflammatory, antimicrobial, anticholesterolemic, antimutagenic, and antihypertensive activities. The findings obtained support the application of simple phenolic acids in the cosmetic, food, pharmaceutical, and health industries and provide future perspectives and guidance for the exploration of simple phenolic acids from plants and fruit sources.
... Ferulic acid is a natural phenolic compound found in vegetables, fruits, cereals, coffee beans, and various Chinese medicine herbs (Mancuso & Santangelo, 2014). Ferulic acid is known to have antioxidant, anti-in ammatory, antithrombotic, anticancer, antidiabetic, and neuroprotective activities (Zduńska, Dana, Kolodziejczak, & Rotsztejn, 2018). However, relevant studies on its effects on AD are limited (Zhou, Shi, Hou, & Li, 2020). ...
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Atopic dermatitis (AD) is a prevalent skin ailment in Asia, and the currently available clinical interventions provide only limited respite while potentially leading to undesired or severe side effects. This investigation explores ferulic acid's potential as an innovative and efficacious remedy for AD. Ferulic acid, recognized for its diverse pharmacological and biological attributes, underwent evaluation through both cellular and in vivo studies. The outcomes revealed that ferulic acid adeptly mitigated the inflammatory retort associated with AD by quelling the activation of the TRPV1 and HMGB1 signaling pathways—both tied to the Transient Receptor Potential Cation Channel, Subfamily V, Member 1 (TRPV1) and High Mobility Group Protein 1 (HMGB1). In a BALB/c mouse model, ferulic acid demonstrated significant amelioration of AD symptoms prompted by DNCB, including the reduction of skin barrier impairment, diminished ear and skin epidermal thickness, curbed mast cell infiltration, and decreased spleen and lymph node dimensions. These findings underscore the potential of ferulic acid as a viable treatment avenue for AD. The multifaceted attributes of ferulic acid, its confirmed pharmacological and biological merits, and its demonstrated effectiveness in assuaging AD's inflammatory responses, as validated by cellular and in vivo investigations, collectively propose its significant promise as a compelling substitute in the therapeutic landscape for AD. Running head: Ferulic acid inhibits inflammation in AD
... One of the phenolic compounds is ferulic acid. Ferulic acids have low toxicity and are extensively utilised in the pharmaceutical, food, and cosmetics industries [56]. Additionally, it has been discovered that ferulic acid is a good precursor in the creation of vanillin, the primary component of vanilla flavour, which is widely used in the food, beverage, pharmaceutical, and cosmetics industries [57]. ...
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Cassava peel has been a notable agricultural waste material to researchers because of its potential to produce sugar, a valuable product in the food, agricultural, and cosmetic industries. The peels constitute lignin, hemicellulose, and cellulose, also known as lignocellulosic biomass. Cassava peels must undergo a pre-treatment method to separate the lignocellulosic material effectively. This study aims to investigate the optimal chemical pre-treatment methods and optimal pre-treatment concentration to produce sugar from cassava peel. Cassava peels were pre-treated with sodium hydroxide, sulphuric acid, and methanol with a catalyst (organosolv). Then, enzymatic hydrolysis was performed using cellulase to hydrolyze cellulose to glucose. The glucose yield is quantified using Dinitrosalicylic Acid Assay and a portable blood glucometer. The results showed that pre-treatment using sodium hydroxide at a concentration of 0.05 M at 121°C for 15 minutes gave the highest glucose yield of 4.53±1.20 mg/ml. Glucose produced from 0.05 M sulphuric acid (H2SO4) and 0.2 M organosolv sodium methoxide (MeOH+NaOAc) were 3.55±0.68 mg/ml and 3.29±0.93 mg/ml, respectively. Statistical analysis showed that the effect of different pre-treatment methods and pre-treatment concentrations had a significant glucose yield (P<0.05). Similarly, there was a significant difference (P<0.05) in the glucose yield under different pre-treatment concentrations. Further study on mechanical-assisted chemical pre-treatment methods is recommended.
... Ferulic acid has been studied for its potential to improve cardiovascular health by reducing blood pressure, inhibiting the formation of blood clots, and improving lipid levels in the blood [84]. Additionally, some research suggests that ferulic acid may have anti-cancer, antioxidant, anti-inflammatory, and antimicrobial properties [85]. Ferulic acid has been shown to have photoprotective effects, helping to protect the skin from UV damage and reduce the risk of skin cancer [86]. ...
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Culinary herbs and spices are widely used in daily diets. Pakistan’s flora is enriched with phytochemicals due to a diverse range of land. Phytochemicals, including volatile and non-volatile compounds, have captured much interest due to their numerous health advantages and significance in daily diet. The present study aimed to conduct in-depth metabolomic profiling of Pakistani-grown fenugreek leaves (Trigonella foenum-graecum), fennel seeds (Foeniculum vulgare), mint leaves (Mentha royleana), coriander seeds (Coriandrum sativum) and basil leaves (Ocimum basilicum) by using liquid chromatography–mass spectrometry (LC-MS/MS) and gas chromatography–mass spectrometry (GC-MS). The first study was conducted to optimize extraction using different solvents (methanol, ethanol, chloroform, acetone, and water). Total phenolic content (TPC), total flavonoid content (TFC), and total condensed tannins (TCT) were quantified along with the antioxidant and anti-diabetic activities. The highest TPC (125.42 ± 10.89 mg GAE/g) and the highest antioxidant and anti-diabetic potential were quantified in mint. Seventy-one phytochemical metabolites were identified using LC-MS/MS, while forty-nine volatile constituents were identified using GC-MS. A positive correlation was identified between phenolic contents and their biological activities. Furthermore, molecular docking helped to find drug molecules with more excellent anti-diabetic activity based on their binding affinities. This study suggests that selected herbs and spices from Pakistan have significant nutraceutical and phytopharmaceutical potential. This study could further help in drug discovery.
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Purpose of the review Ferulic acid (FA), which occurs naturally as the feruloylated sugar ester in grains, fruits, and vegetables, is critical for combating oxidative stress and alleviating neurodegenerative diseases resulting from free radical-generated protein aggregates in brain cells. However, FA cannot be absorbed in conjugated form. Therefore, strategies to improve the bioavailability of FA are gaining more importance. Ferulic acid esterases (FAE) of the gut microbiota are critical enzymes that facilitate FA release from feruloylated sugar ester conjugates and influence systemic health. This review provides insight into a nutrition-based approach to preventing neurodegenerative disorders such as Alzheimer’s and Parkinson’s by altering the diversity of FAE-producing gut microbiota. Recent findings The human gut is a niche for a highly dense microbial population. Nutrient components and the quality of food shape the gut microbiota. Microbiota–diet–host interaction primarily involves an array of enzymes that hydrolyse complex polysaccharides and release covalently attached moieties, thereby increasing their bio-accessibility. Moreover, genes encoding polysaccharide degrading enzymes are substrate inducible, giving selective microorganisms a competitive advantage in scavenging nutrients. Summary Nutraceutical therapy using specific food components holds promise as a prophylactic agent and as an adjunctive treatment strategy in neurotherapeutics, as it results in upregulation of polysaccharide utilisation loci containing fae genes in the gut microbiota, thereby increasing the release of FA and other antioxidant molecules and combat neurodegenerative processes.
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Hassawi rice is an Indica variety cultivated in Saudi Arabia with a higher nutritional value than the commercial Basmati rice varieties. The present study has investigated the feasibility of combining Hassawi rice flour (HRF) or husk (HRHF), an abundant byproduct, with wheat flour to produce nutritious economical pan bread. To achieve this aim, the physicochemical properties of HRF and HRHF were assessed using techniques such as UPLC-tandem MS, ICP-OES, and colorimeter. The proximate composition (moisture, crude fiber, and ash) and mineral contents of HRHF are significantly (p < 0.05) higher than HRF. On the other hand, the compounds p-coumaric acid, vanillic acid, γ- and δ-tocotrienols, and γ-oryzanol were unique to HRF. We further determined the changes in sensory, technological, and physicochemical properties of wheat flour bread substituted with 5%, 10%, and 15% of HRF or HRHF. The rheological tests showed that the addition of HRF and HRHF increased dough development and stability time. Further, substituting wheat flour for HRF and HRHF at levels higher than 10% affected sensory attributes, such as color, taste, odor, flavor, and appearance. These changes, however, were not always at a significant level. The causes of the differences in properties between control and fortified bread samples were investigated by chemometric methods. Samples of bread +HRF at 5 and 10% had comparable overall profiles to the control. On the other hand, bread +HRHF samples proved to retain higher concentrations of bioactive molecules compared to the control bread. Our findings shed light on the possible use of rice husk fibers in baking goods, notably pan bread. Furthermore, by integrating rice husk fibers into baked goods, we may boost their health
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Surface-Enhanced Raman Spectroscopy (SERS) is a powerful surface-sensitive technique to study the vibrational properties of analytes at very low levels of concentration. In particular, detection of bioactive molecules, specifically antioxidants, is an area of interest to gain insights into the reproducible and quantitative SERS-determination. In this study, SERS measurements were systematically evaluated for ferulic acid, p-coumaric acid, caffeic acid and sinapic acid. The study objective in this research was to: 1) prepare and characterize SERS-active silver colloids; 2) cluster the as-obtained colloids through Principal Component Analysis on the basis of concentration and nanoparticle size; and 3) develop a highly sensitive SERS-based method for phenolic antioxidant detection. The reliability of the proposed method was demonstrated through detection of the phenolic antioxidants evaluated at low levels of concentration. In particular, sinapic acid was evaluated for the first time, with a limit of detection of 2.5 × 10⁻⁹ M.
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Background Approximately 90%~99% of ultraviolet A (UVA) ray reaches the Earth's surface. The deeply penetrating UVA rays induce the formation of reactive oxygen species (ROS), which results in oxidative stress such as photoproducts, senescence, and cell death. Thus, UVA is considered a primary factor that promotes skin aging. Objective Researchers investigated whether pretreatment with ferulic acid protects human dermal fibroblasts (HDFs) against UVA-induced cell damages. Methods HDF proliferation was analyzed using the water-soluble tetrazolium salt assay. Cell cycle distribution and intracellular ROS levels were assessed by flow cytometric analysis. Senescence was evaluated using a senescence-associated β-galactosidase assay, while Gadd45α promoter activity was analyzed through a luciferase assay. The expression levels of superoxide dismutase 1 (SOD1), catalase (CAT), xeroderma pigmentosum complementation group A and C, matrix metalloproteinase 1 and 3, as well as p21 and p16 were measured using quantitative real-time polymerase chain reaction. Results Inhibition of proliferation and cell cycle arrest were detected in cells that were irradiated with UVA only. Pretreatment with ferulic acid significantly increased the proliferation and cell cycle progression in HDFs. Moreover, ferulic acid pretreatment produced antioxidant effects such as reduced DCF intensity, and affected SOD1 and CAT mRNA expression. These effects were also demonstrated in the analysis of cell senescence, promoter activity, expression of senescent markers, and DNA repair. Conclusion These results demonstrate that ferulic acid exerts protective effects on UVA-induced cell damages via anti-oxidant and stress-inducible cellular mechanisms in HDFs.
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Ferulic acid (4-hydroxy-3-methoxycinnamic acid) is a phytochemical constituent from the polyphenols group commonly found in whole grains, spinach, parsley, grapes and rhubarb. It has been widely applied in skin care formulations as photoprotective agent and delayer of cutaneous photoaging processes. This work aims to establish a protocol to the development of cosmetic formulations using thermoanalytical techniques (TG/DTG and DSC) and Pearson’s correlation by FTIR data, in order to evaluate the compatibility between ferulic acid and excipients used in skin care formulations. The results obtained from the thermoanalytical techniques indicated compatibility between ferulic acid and the following excipients: passion fruit seed oil, Carbopol® Ultrez 30, EDTA, Crodabase CR2®, Crodamol™ GTCC and Dow Corning® RM 2051. Nevertheless, the analysis also demonstrated the possibility of some interaction between ferulic acid and the following excipients: glyceryl stearate, Rapithix® A-60 and Optiphen®. To validate these results, it was demonstrated by Pearson’s correlation that passion fruit seed oil, Carbopol® Ultrez 30, EDTA, Crodabase CR2®, Crodamol™ GTCC, Dow Corning® RM 2051, glyceryl stearate and Rapithix® A-60 do not have any incompatibility that may compromise ferulic acid properties. Finally, it was also proved a meaningful incompatibility between ferulic acid and Optiphen® using Pearson’s correlation. Thus, it is not recommended to use Optiphen® in the development of cosmetic formulations to carry ferulic acid.
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Background and aims The main aims of the present study were to formulate an anti-age cream based on vegetal ingredients and ferulic acid and to evaluate the physical characteristics and the efficacy of the cream. Methods The active ingredients were Centella asiatica oil, Spilanthes acmella oil, Zingiber officinale extract and ferulic acid. Formulation 1 (F1) was prepared using glyceryl stearate and Ceteareth-25® as emulsifiers and Formulation 2 (F2) using glyceryl stearate and potassium cetyl phosphate, all other ingredients remaining the same. The physical characterization of the creams was performed and the following parameters were analyzed: viscosity, oil droplet size, polydispersity index; also, texture analysis was performed. The anti-aging effect of the F2 was evaluated by assessing the cutaneous density before and after cream application using DUB-cutis® scanner. Results The mean diameter of oil drops was 10.26±4.72 mm (F1) and 22.72±7.93 mm (F2) and the polydispersity index was 35.4% and 45.7%, respectively. The mean values for consistency were 594.7±10.3 g (F1) and 300.5±14.5 g (F2), the average values for adhesion were 15.61±0.8 mJ (F1) and 22.25±4.3 mJ (F2), for firmness were 51.2±0.8 g (F1) and 30.3±4.3 g (F2) and the spreadability had values between 72.63 mm2 (F1) and 73.3 mm2 (F2). In vivo study revealed that the mean values of the cutaneous density increased from 9.21±1.39 % to 12.50±1.44 % after 8 weeks of cream application. The herbal ingredients incorporated in the O/W cream base for the antioxidant activity and anti-wrinkle effect, induced changes of the cutaneous density, an important parameter which quantifies the regeneration process of the skin. Conclusions An anti-age cream containing herbal active ingredients and ferulic acid with appropriate physical characteristics was obtained. In vivo study of clinical efficacy revealed a positive effect on skin density, which increased after 8 weeks of cream application.
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The ferulic and gallic acid related compounds from natural origin were studied against xanthine oxidase and cyclooxygenase-2 along with their anti-inflammatory activity. The compounds gallic acid, ferulic acid, caffeic acid and p-coumaric acid revealed promising anti-inflammatory activity (30–40% TNF-α and 60–75% IL-6 inhibitory activity at 10μM). Bioavailability of compounds were checked by in vitro cytotoxicity using CCK-8 cell lines and confirmed to be nontoxic, but found toxic at higher concentration (50μM). Gallic, ferulic, caffeic acid was demonstrated potential dual inhibition toward xanthine oxidase and cyclooxygenase-2 as calculated by IC50: 68, 70.2, and 65μg/ml (xanthine oxidase) and 68.5, 65.2, and 62.5μg/ml (cyclooxygenase-2), respectively. The structure activity relationship and in silico drug relevant properties (HBD, HBA, PSA, cLogP, ionization potential, molecular weight, EHOMO and ELUMO) further confirmed that the compounds were potential candidates for future drug discovery study, which was expected for further rational drug design against xanthine oxidase and cyclooxygenase.
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Natural lipids, rich in mono-and polyunsaturated fatty acids, are basic components of food; they significantly impact the accurate functioning of human organism. Unfortunately, those lipids are characterized by instability owing to their high susceptibility to oxidation processes. Many treatment procedures are applied to eliminate those adverse changes. In spite of their many advantages, the currently used commercial antioxidants may arouse controversy attributed to the undesirable biological activity or low stability under the food processing conditions. Therefore, there are attempts at searching for new antioxidants that might be an alternative to the presently used antioxidants. The objective of the research study was to develop a method to synthesize long-chain alkyl esters of ferulic acid. The antioxidants produced were identified based on the results of spectroscopic investigations and elemental analysis. A thermal analysis of esters was performed, which comprised thermogravimetry (TG) and differential scanning calorimetry (DSC). The results obtained were compared with the results obtained for the free ferulic acid and with data in the reference literature on commercial antioxidants. In the research study, the antioxidant activity of tetradecyl ferulate and of BHT were pre-compared.
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Most anti-angiogenic therapies currently being evaluated target the vascular endothelial growth factor (VEGF) pathway; however, the tumor vasculature can acquire resistance to VEGF-targeted therapy by shifting to other angiogenesis mechanisms. Therefore, other therapeutic agents that block non-VEGF angiogenic pathways need to be evaluated. Here, we identified ferulic acid as a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor and a novel agent with potential anti-angiogenic and anti-cancer activities. Ferulic acid demonstrated inhibition of endothelial cell proliferation, migration and tube formation in response to basic fibroblast growth factor 1 (FGF1). In ex vivo and in vivo angiogenesis assays, ferulic acid suppressed FGF1-induced microvessel sprouting of rat aortic rings and angiogenesis. To understand the underlying molecular basis, we examined the effects of ferulic acid on different molecular components and found that ferulic acid suppressed FGF1-triggered activation of FGFR1 and phosphatidyl inositol 3-kinase (PI3K)-protein kinase B (Akt) signaling. Moreover, ferulic acid directly inhibited proliferation and blocked the PI3K-Akt pathway in melanoma cell. In vivo, using a melanoma xenograft model, ferulic acid showed growth-inhibitory activity associated with inhibition of angiogenesis. Taken together, our results indicate that ferulic acid targets the FGFR1-mediated PI3K-Akt signaling pathway, leading to the suppression of melanoma growth and angiogenesis.
Antioxidant, anticarcinogenic, and antimicrobial properties have been reported for ferulic acid (FA), therefore, its application interests both food and agriculture research. FA was immobilized in different chitosan (CS) matrices, physicochemicaly characterized and the effect on Aspergillus parasiticus ecological parameters evaluated. Nanoparticles (Nparticles), microparticles (Mparticles) and microcapsules (Mcapsules) of 35–40 nm, 30–40 μm, and 20 μm, respectively were obtained; FA incorporation in matrices affected their morphology, physicochemical properties, and their fungistatic effect. The effect of the particles was dependent on the matrix exposed. Nparticles and Mparticles showed high FA immobilization efficiency as well as a good fungistatic effect against A. parasiticus: Radial growth at 168 h was 28.46 ± 1.01 and 28.84 ± 1.36 and the inhibition of spore germination at 30 h was 57.44 ± 0.22 and 55.74 ± 2.19, for Nparticles and Mparticles, respectively compared with control cultures. Abnormalities in mycelium, hyphae, and spores morphology were observed, as well as low sporulation due particle interaction with the fungus.