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Ferulic acid-and 4-vinylguaiacol-induced apoptosis on HCT-116 and HT-29 human colorectal cancer cells. HCT-116 and HT-29 cells were treated with different concentrations of ferulic acid or 4-vinylguaiacol for 48 h. The cells were stained with a DNA specific dye, Hoechst 33258, and imaged at ×20 magnification in a fluorescence microscope. Apoptotic cells are indicated with arrows.
Source publication
Ferulic acid, a hydroxycinnamic acid, is abundant in vegetables, grains, and medicinal plants. Emerging evidence suggests that ferulic acid may exert beneficial effects against colorectal cancer. However, the anticancer activity of ferulic acid is relatively low, and its metabolism after oral administration is largely unknown. In this study, mimick...
Context in source publication
Context 1
... test whether or not the decrease in cell viability observed after treatment with ferulic acid and 4-vinylguaiacol was due to apoptosis, HCT-116 and HT-29 cells were stained with Hoechst 33258 dye after exposure to the compounds for 48 h. The dye stains condensed the chromatin of apoptotic cells more brightly than the chromatin of normal cells ( Figure 5). ...
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Citations
... They found that 4-VG down-regulated the expression of some key pro-inflammatory mediators such as nitric oxide, prostaglandins (PGE 2 ), iNOS and COX-2, through the suppression of (i) NF-κB and MAPK pathway activation, and (ii) histone H3 hyper-acetylation. In addition, antiproliferative effects were found on the two colorectal cancer cell lines HCT-116 and HT-29 [59], on benzo[a]pyrene-treated mouse fibroblast NIH 3T3 cells [60], as well as on human breast cancer MCF-7 cells [61] and human pancreatic cancer Panc-1 cells [62]. Finally, Rubab et al. [63] identified 4-VG as one of the main contributors of the strong antibacterial and antifungal effect of red cabbage (Brassica oleracea var. ...
p-Hydroxycinnamic acids, such as sinapic, ferulic, p-coumaric and caffeic acids, are among the most abundant phenolic compounds found in plant biomass and agro-industrial by-products (e.g. cereal brans, sugar-beet and coffee pulps, oilseed meals). These p-hydroxycinnamic acids, and their resulting decarboxylation products named vinylphenols (canolol, 4-vinylguaiacol, 4-vinylphenol, 4-vinylcatechol), are bioactive molecules with many properties including antioxidant, anti-inflammatory and antimicrobial activities, and potential applications in food, cosmetic or pharmaceutical industries. They were also shown to be suitable precursors of new sustainable polymers and biobased substitutes for fine chemicals such as bisphenol A diglycidyl ethers. Non-oxidative microbial decarboxylation of p-hydroxycinnamic acids into vinylphenols involves cofactor-free and metal-independent phenolic acid decarboxylases (EC 4.1.1 carboxyl lyase family). Historically purified from bacteria (Bacillus, Lactobacillus, Pseudomonas, Enterobacter genera) and some yeasts (e.g. Brettanomyces or Candida), these enzymes were described for the decarboxylation of ferulic and p-coumaric acids into 4-vinylguaiacol and 4-vinylphenol, respectively. The catalytic mechanism comprised a first step involving p-hydroxycinnamic acid conversion into a semi-quinone that then decarboxylated spontaneously into the corresponding vinyl compound, in a second step. Bioconversion processes for synthesizing 4-vinylguaiacol and 4-vinylphenol by microbial decarboxylation of ferulic and p-coumaric acids historically attracted the most research using bacterial recombinant phenolic acid decarboxylases (especially Bacillus enzymes) and the processes developed to date included mono- or biphasic systems, and the use of free- or immobilized cells. More recently, filamentous fungi of the Neolentinus lepideus species were shown to natively produce a more versatile phenolic acid decarboxylase with high activity on sinapic acid in addition to the others p-hydroxycinnamic acids, opening the way to the production of canolol by biotechnological processes applied to rapeseed meal. Few studies have described the further microbial/enzymatic bioconversion of these vinylphenols into valuable compounds: (i) synthesis of flavours such as vanillin, 4-ethylguaiacol and 4-ethylphenol from 4-vinylguaiacol and 4-vinylphenol, (ii) laccase-mediated polymer synthesis from canolol, 4-vinylguaiacol and 4-vinylphenol.
... 19 Potential mechanisms associated with ferulic acid, the predominant polyphenol in wheat, 8 include transformation by intestinal microflora and probiotics to 4-vinylguaiacol, with both compounds demonstrating in vitro anti-proliferative effects against human CRC cell lines HT-29 and HCT-116. 20 Lignan metabolites enterolactone and enterodiol also inhibited growth of human colonic cancer SW480 cells. 21 What remains unclear is whether the protective effects against CRC observed with grain polyphenols in experimental models are seen in populations. ...
... 4230 (12) 830 (12) 783 (11) 896 (13) 902 (13) 819 (12) High intake (>40 g/d) 2485 (7) 678 (10) 502 (7) 501 (7) 404 (6) 400 (6) Physical activity score, n (%) 0 7748 (22) 2262 (32) 1660 (24) 1397 (20) 1216 (17) 1213 (17) >0 to <4 7156 (20) 1496 (21) 1498 (21) 1437 (20) 1352 (19) 1373 (19) 4 to ...
Background
Cereal‐derived polyphenols have demonstrated protective mechanisms in colorectal cancer (CRC) models; however, confirmation in human studies is lacking. Therefore, this study examined the association between cereal polyphenol intakes and CRC risk in the Melbourne Collaborative Cohort Study (MCCS), a prospective cohort study in Melbourne, Australia that recruited participants between 1990 and 1994 to investigate diet–disease relationships.
Methods
Using food frequency questionnaire diet data matched to polyphenol data, dietary intakes of alkylresorcinols, phenolic acids, lignans, and total polyphenols from cereals were estimated. Hazard ratios (HRs) and 95% confidence intervals for CRC risk were estimated for quintiles of intake with the lowest quintile as the comparison category, using multivariable adjusted Cox proportional hazards models with age as the time axis adjusted for sex, socio‐economic status, alcohol consumption, fibre intake, country of birth, total energy intake, physical activity and smoking status.
Results
From 35,245 eligible adults, mean (SD) age 54.7 (8.6) years, mostly female (61%) and Australian‐born (69%), there were 1394 incident cases of CRC (946 colon cancers and 448 rectal cancers). Results for total cereal polyphenol intake showed reduced HRs in Q2 (HR: 0.80; 95% CI, 0.68–0.95) and Q4 (HR: 0.75; 95% CI, 0.62–0.90), and similar for phenolic acids. Alkylresorcinol intake showed reduced HR in Q3 (HR: 0.80; 95% CI, 0.67–0.95) and Q4 (HR: 0.79; 95% CI, 0.66–0.95).
Conclusions
Overall, the present study showed little evidence of association between intakes of cereal polyphenols and CRC risk. Future investigations may be useful to understand associations between cereal‐derived polyphenols and additional cancers in different populations.
... Canan et al. [53] observed that FA can inhibit cell proliferation by increasing the gene expression of TP53 and decreasing the gene expression of CDK2, CDK,4 and CDK6 in prostate cancer PC-3 cells, thus leading to cell cycle arrest in PC-3 cells. Luo et al. [54] found that FA can significantly reduce the number of S phase and G 2 /M phase cells in HCT116 and HT-29 colorectal cancer cells and increase the proportion of G1 phase cells in these two cancer cell lines, which reflects its antitumor cell proliferation ability. ...
Cancer is a significant disease that poses a major threat to human health. The main therapeutic methods for cancer include traditional surgery, radiotherapy, chemotherapy, and new therapeutic methods such as targeted therapy and immunotherapy, which have been developed rapidly in recent years. Recently, the tumor antitumor effects of the active ingredients of natural plants have attracted extensive attention. Ferulic acid (FA), (3-methoxy-4-hydroxyl cinnamic), with the molecular formula is C10H10O4, is a phenolic organic compound found in ferulic, angelica, jujube kernel, and other Chinese medicinal plants but is also, abundant in rice bran, wheat bran, and other food raw materials. FA has anti-inflammatory, analgesic, anti-radiation, and immune-enhancing effects and also shows anticancer activity, as it can inhibit the occurrence and development of various malignant tumors, such as liver cancer, lung cancer, colon cancer, and breast cancer. FA can cause mitochondrial apoptosis by inducing the generation of intracellular reactive oxygen species (ROS). FA can also interfere with the cell cycle of cancer cells, arrest most cancer cells in G0/G1 phase, and exert an antitumor effect by inducing autophagy; inhibiting cell migration, invasion, and angiogenesis; and synergistically improving the efficacy of chemotherapy drugs and reducing adverse reactions. FA acts on a series of intracellular and extracellular targets and is involved in the regulation of tumor cell signaling pathways, including the phosphatidylinositol 3 kinase (PI3K)/protein kinase B (AKT), B-cell lymphoma-2 (Bcl-2), and tumor protein 53 (P53) pathways and other signaling pathways. In addition, FA derivatives and nanoliposomes, as platforms for drug delivery, have an important regulatory effect on tumor resistance. This paper reviews the effects and mechanisms of antitumor therapies to provide new theoretical support and insight for clinical antitumor therapy.
... Wu pill can help prevent colitis-related CRC by regulating the intestinal microbiota (210). However, ferulic acid needs to be metabolized by intestinal flora, and its product has stronger anticancer activity than its mother, which is used to treat chemical resistance CRC (211). Yi-Yi-Fu-Zi-Bai-Jiang-San has no direct inhibitory effect on CRC, but it significantly improves the intestinal bacteria composition and tumor immune infiltration of CRC tumorbearing mice and inhibits the tumor growth after fecal bacteria transplantation treatment with the intestinal flora regulated by this compound (212). ...
In recent years, the incidences and mortalities from colorectal cancer (CRC) have been increasing; therefore, there is an urgent need to discover newer drugs that enhance drug sensitivity and reverse drug tolerance in CRC treatment. With this view, the current study focuses on understanding the mechanism of CRC chemoresistance to the drug as well as exploring the potential of different traditional Chinese medicine (TCM) in restoring the sensitivity of CRC to chemotherapeutic drugs. Moreover, the mechanism involved in restoring sensitivity, such as by acting on the target of traditional chemical drugs, assisting drug activation, increasing intracellular accumulation of anticancer drugs, improving tumor microenvironment, relieving immunosuppression, and erasing reversible modification like methylation, have been thoroughly discussed. Furthermore, the effect of TCM along with anticancer drugs in reducing toxicity, increasing efficiency, mediating new ways of cell death, and effectively blocking the drug resistance mechanism has been studied. We aimed to explore the potential of TCM as a sensitizer of anti-CRC drugs for the development of a new natural, less-toxic, and highly effective sensitizer to CRC chemoresistance.
... Another of the compounds present is sesaminol, which has been shown to have an in vitro neuroprotective effect, in addition, this same compound has good antioxidant, anti-collagenase, and antihyaluronidase activity, which makes it a candidate for cosmetic or nutraceutical applications (Kaji et al., 2020). On the other hand, some compounds found in polyembryonic genotypes have activities of interest, such as 4-vinylguaiacol, which has more powerful antioxidant and anticancer activities than ferulic acid, which can be helpful in treatments as an anticancer metabolite for cells resistant to chemotherapy (Luo et al., 2021;Sudhagar et al., 2018), and matairesinol which has different activities such as antiangiogenic, antioxidant, anticancer and antifungal activities, and can also suppress neuroinflammation (Mahajan et al., 2021;Xu et al., 2017). the proportion of fat is altered. ...
The growing demand for foods with better characteristics has led to the search for new alternatives, one of these being sprouts, of which polyembryonic maize kernels have been little studied. The objective of this work was to evaluate the morphological changes, as well as the physicochemical, techno-functional, phytochemical, and antioxidant properties of polyembryonic (Pem) and non-polyembryonic (NPem) corn sprouts at different germination times (0, 5, 10, and 15 days). Different analytical techniques as well as “green” extraction technique (Microwave-ultrasound) with various solvents were used to obtain phytochemicals. PEm “normal high polyembryony” (NAP) and NPEm “landrace” (CRO) maize showed higher growth (up to 24.7 and 30.6 cm) and moisture content (up to 89.5 and 87.7%). Overall protein content increased by up to 51% relative to the initial value, with higher PEm content (15.0 and 14.5% in “brachytic high polyembryony” (BAP) and NAP maize respectively). Fibre and protein content were negatively correlated with starch content. Likewise, the techno-functional properties improved, with higher values for NAP, BAP and CRO at 10 and 15 days of germination. PEm presented higher yields (13 times higher), higher content of hydrolysable polyphenols (553.08 ± 44.68 mg/100 g (BAP)) at 1/16 concentrations of 70% EtOH, and higher content of condensed tannins (1623.38 mg/100 g (NAP)) at 1/8 and 30% EtOH concentrations. Finally, PEm showed higher antioxidant activity which can be attributed to the content and presence of different polyphenols. The results indicate that sprouts produced from polyembryonic maize kernels present better physicochemical, phytochemical, techno-functional and antioxidant properties.
... As per the studies and indications of this anti-cancer drug, cyclophosphamide is usually preferred to be administered in the morning time. Because after its administration fluid intake should be proper by the patient to enhance diuresis to decrease the chances of toxicity in the urinary tract (Schoch et al., [58]). ...
... On the contrary, (40 mg/kg) ferulic acid showed no momentous effect to limit inflammation induced by cyclophosphamide in mice (Muronetz et al., [36]). These effects are harmonized with prior experiments (Liu et al., [67] and Rinwa et al., [58]). ...
... Steps involved in Rotarod apparatus test TAIL SUSPENSION TEST: ( Shao et al.,[58]) individually hanged withhold tails, at a height of 40 cm with the help of adhesive tape. The Tail was on hold for a time of 6 minutes. ...
Cyclophosphamide (CP) is a distinguished anticancer and immune subduing
medicament. Conversely, regardless of its pervasive proven use, it retains limitations of
neurotoxicity. Therefore, in the current study, ferulic acid (FA) has been sightseeing for
probable neuroprotective effects in contradiction to cyclophosphamide-prompted
neurotoxicity in the Swiss Albino mice. Mice were alienated into five groups (n=7) and
treated with FA for fourteen days and a single dose of CP was administered on the seventh
day. Animals were imperilled to neurobehavioral tests such as Rota rod test, Tail
suspension test, and Y-maze test. On day fifteenth, animals were forgone and brain was
detached and used for biochemical analysis. CP administration likewise condensed the
activity of antioxidant enzyme (GSH), and increased lipid peroxidation i.e., MDA and
pro-inflammatory cytokines (TNF-α and IL-1β). Furthermore, CP administration
amplified the level of acetylcholine esterase (AchE). Treatment with FA knowingly
overturned these behavioral and biochemical markers in the direction of the ordinary and
moderated cyclophosphamide-influenced neurotoxic demonstration. Contrariwise,
supplementary in-depth studies are obligatory to bring FRA from bench to bedside that
it be used as an adjuvant among chemotherapeutically treated patients.
... Among them, more than half of the components have an anticancer effect (Table 1). 4-vinyl-2-methoxyphenol and β-amyrin have a significant inhibitory effect on colorectal cancer HT-29 cells [40,41]. This provides a theoretical basis for R. molle as a potential anticancer drug. ...
Rhododendron molle G. Don is one example of traditional Chinese medicine with important medicinal value. In this study, the effects of methanol extract of R. molle leaves (RLE) on colorectal cancer HT-29 cells and its potential molecular mechanism were investigated. MTT analysis showed that RLE could significantly inhibit the cell viability and migration of HT-29 cells in a concentration-dependent manner. Cell cycle analyses via flow cytometer suggested that RLE induced DNA fragmentation, indicative of apoptosis, and arrest at the S phase in HT-29 cells. Quantitative real-time PCR (qRT-PCR) analysis showed that RLE could upregulate the mRNA expression of p53 and p21 in HT-29 cells, which would result in HT-29 cells being blocked in S phase. Meanwhile, RLE could upregulate the expression of Bax, and downregulate the expression of Bcl-2, which would induce cell apoptosis. Further western blot analysis showed that the protein expression changes of Bax and P53 were basically consistent with the results of qRT-PCR. In addition, GC-MS analysis detected 17 potential anticancer components in R. molle. These results indicate that R. molle has significant anticancer activity, which provides some useful information for further study and clinical application for R. molle.
Ferulic acid (FA) is a hydroxycinnamic acid known for its strong antioxidant activity and potential benefits for intestinal health. However, its poor water solubility and instability limit its effectiveness. To address these issues, different ways have been explored to protect FA against degradation and further exert its potential benefits. This review discusses the absorption and metabolism of FA in the gut, as well as its potential impact on intestinal health. It also compares different intestinal delivery systems, such as nanoparticles, electrospun nanofibers, microcapsules, cross‐linked polymer gels, and Pickering emulsions, which can improve the solubility, stability, and bioavailability of FA in the gastrointestinal tract. This comprehensive review provides valuable insights for using FA in food, pharmaceutical, and nutraceuticals products.
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.
