Ferulic acid reduces inflammatory response induced by radiation through Sirt1-NLRP3 pathway

Objective:A model of inflammatory damage was induced by radiation to investigate whether ferulic acid(FA)can reduce the inflammatory response through the Sirt1-NLRP3 inflammatory pathway.This will help discover radiation-protective drugs and elucidate the molecular mechanisms related to radiation-induced inflammatory damage.Methods:A mouse model of radiation-induced immunoinflammatory injury was established to verify the anti-inflammatory effects of FA in vivo.C57BL/6J mice were randomly divided into six groups,and 5 Gy whole-body irradiation was used for modeling.Mice were administered a gastric solvent,amifostine,or 25,50,or 100 mg/kg FA daily for 12 days,consecutively,before irradiation.The serum of mice was collected 24 hour after irradiation to observe the content of inflammatory factors interleukin(IL)-1β,IL-18,IL-6,and tumor necrosis factor(TNF)-α.The spleen and thymus tissues of mice were weighed and the organ index was calculated for pathological testing and immunofluorescence detection.Results:FA reduced the radiation-induced decrease in the spleen and thymus indices.FA significantly reduced the secretion of inflammatory factors in the serum and reversed the radiation-induced reduction in lymphocytes in the spleen and thymus of mice.FA activated Sirt1 and inhibited the expression of the NLRP3 inflammasome to alleviate the inflammatory response.Conclusions:FA reduced radiation-induced inflammation in animals,possibly by activating Sirt1 and reducing nucleotide oligomerization domain(NOD)-like receptor thermal protein domain associated protein 3(NLRP3)inflammasome expression,thereby reducing the secretion of inflammatory factors.

Integrated mass spectrometry imaging reveals spatial-metabolic alteration in diabetic cardiomyopathy and the intervention effects of ferulic acid

Diabetic cardiomyopathy(DCM)is a metabolic disease and a leading cause of heart failure among people with diabetes.Mass spectrometry imaging(MSI)is a versatile technique capable of combining the molecular specificity of mass spectrometry(MS)with the spatial information of imaging.In this study,we used MSI to visualize metabolites in the rat heart with high spatial resolution and sensitivity.We optimized the air flow-assisted desorption electrospray ionization(AFADESI)-MSI platform to detect a wide range of metabolites,and then used matrix-assisted laser desorption ionization(MALDI)-MSI for increasing metabolic coverage and improving localization resolution.AFADESI-MSI detected 214 and 149 metabolites in positive and negative analyses of rat heart sections,respectively,while MALDI-MSI detected 61 metabolites in negative analysis.Our study revealed the heterogenous metabolic profile of the heart in a DCM model,with over 105 region-specific changes in the levels of a wide range of metabolite classes,including carbohydrates,amino acids,nucleotides,and their derivatives,fatty acids,glycerol phospholipids,carnitines,and metal ions.The repeated oral administration of ferulic acid during 20 weeks significantly improved most of the metabolic disorders in the DCM model.Our findings provide novel insights into the molecular mechanisms underlying DCM and the potential of ferulic acid as a therapeutic agent for treating this condition.

Protective effects of ferulic acid against ionizing radiation-induced oxidative damage in rat lens through activating Nrf2 signal pathway

AIM: To examine the protection of ferulic acid(FA) against ionizing radiation(IR)-induced lens injury in rats, as well as the underlying mechanisms.METHODS: FA(50 mg/kg) was administered to rats for 4 consecutive days before they were given 10 Gy γ-radiation, as well as for 3 consecutive days afterward. Two weeks after radiation, the eye tissues were collected. Histological alterations were evaluated by hematoxylineosin staining. Enzyme linked immunosorbent assay(ELISA) was utilized to assess the activities of glutathione reductase(GR) and superoxide dismutase(SOD), as well as the levels of glutathione(GSH) and malondialdehyde(MDA) in the lenses. The protein and m RNA levels of Bcl-2, caspase-3, Bax, heme oxygenase-1(HO-1), and glutamatecysteine ligase catalytic subunit(GCLC) were quantified using Western blot and quantitative reverse transcription polymerase chain reaction, respectively. With nuclear extracts, the nuclear factor erythroid-2 related factor(Nrf2) protein expressions in the nuclei were also measured.RESULTS: Rats exposed to IR showed lens histological alterations which could be alleviated by FA. FA treatment reversed apoptosis-related markers in IR-induced lens, as evidenced by lower levels of Bax and caspase-3 and higher level of Bcl-2. Furthermore, IR induced oxidative damage manifested by decreased GSH level, increased MDA level, and decreased SOD and GR activities. FA boosted nuclear translocation of Nrf2 and increased the expressions of HO-1 and GCLC to inhibit oxidative stress, as evidenced by an increase in GSH, a decrease in MDA, and an increase in GR and SOD activities.CONCLUSION: FA may work well in preventing and treating IR-induced cataract through promoting the Nrf2 signal pathway to attenuate oxidative damage and cell apoptosis.

Quantitative Extraction of p-Coumaric Acid and Ferulic Acid in Different Gramineous Materials and Structural Changes of Residual Alkali Lignin

Ferulic acid(FA)and p-coumaric acid(pCA)in bagasse,wheat straw,corn straw,and corncob were extracted by alkaline hydrolysis and characterized by gas chromatography(GC)and gas chromatography-mass spectrometry(GC-MS).It was found that the FA and most of the pCA in gramineous biomass could be dissociated and released after being treated with 1 M NaOH at 100℃for 4 h.The yields of pCA/FA in bagasse,wheat straw,corn straw,and corncob determined by GC-FID are 39.8/11.5,13.7/11.0,28.0/11.0,and 35.1/14.5 mg/g,respectively.The raw materials and the treated solid residues were characterized by gel-state 2D Heteronuclear Single Quantum Coherence Nuclear Magnetic Resonance(2D HSQC NMR).It was found that only a small amount of lignin was detected in the residue after alkali treatment,indicating that the alkali treatment conditions can effectively cleave the FA and pCA.Additionally,the lignin in the alkali solution was recovered and characterized by 2D HSQC NMR.The FA was not able to be detected by NMR,whereas a small amount of pCA remained in the alkali lignin.This study reveals the structural change of residual lignins during the quantitative isolation of FA and pCA,which is essential for the selective isolation of pCA/FA and valorization of residual alkali lignin.

Inhibitory Effect of Ferulic Acid on Oxidation of L-DOPA Catalyzed by Mushroom Tyrosinase

The inhibitory effect of ferulic acid on the diphenolase activity of mushroom tyrosinase and the kinetic behavior were studied with L-3,4-dihydroxyphenylalanine （L-DOPA） as substrate. The inhibitor concentration leading to 50% relative activity lost （IC50） was estimated to be 0.15 mmol·L^-1. The inhibition mechanism obtained from Lineweaver-Burk plots shows that ferulic acid is a competitive inhibitor and the inhibition of tyrosinase by ferulic acid is a reversible reaction. The equilibrium constant for ferulic acid binding with the tyrosinase was determined to be 0.25 mmol·L^-1 for diphenolase. Keywords tyrosinase, ferulic acid, kinetics, inhibition, L-DOPA, diphenolase

Biodegradation of ferulic acid by a newly isolated strain of Cupriavidus sp. B-8

As a major component of lignin and abundantly existing in softwood and hardwood, ferulic acid has been used as a lignin-related compound for lignin biodegradation study. Biodegradation of ferulic acid by Cupriavidus sp. B-8, a newly isolated strain, was studied. This strain is able to utilize a wide range of lignin-related aromatic compounds as the sole carbon and energy source, including guaiacol, veratric acid, vanillic acid, cinnamic acid, p-coumaric acid, ferulic acid, and sinapic acid. In addition, the effects of different concentrations of ferulic acid on growth of Cupriavidus sp. B-8 were studied. The growth of Cupriavidus sp. B-8 is better under the condition of lower concentration. High-performance liquid chromatography （HPLC） analysis reveals that above 95% of ferulic acid is degraded within 12 h by Cupriavidus sp. B-8. Based on identification of biodegradation intermediates and further metabolites, the biodegradation pathway of ferulic acid by Cupriavidus sp. B-8 was proposed. Ferulic acid is initially converted to 4-vinylguaiacol, and further oxidized to vanillic acid and protocatechuic acid.

Ferulic acid alleviates lipopolysaccharide-induced depression-like behavior by inhibiting inflammation and apoptosis

Objective:To identify the anti-depressive effect of ferulic acid(FA)in mice exposed to lipopolysaccharide(LPS)and explore its molecular mechanisms.Methods:The mice were divided into 5 groups as follows:Control,LPS,LPS+SP,LPS+FA,and LPS+FA+anisomycin.The LPS+FA and LPS+FA+anisomycin groups were administered with FA(100 mg/kg,i.p.)once daily continuously for 7 days,and the other groups received an equivalent volume of saline.On the 7 th day,LPS(0.1 mg/m L,i.p.)was injected in all mice except the control group 30 min after FA or saline administration.The LPS+SP and LPS+FA+anisomycin groups were intravenously administered with SP600125[c-Jun N-terminal kinase(JNK)inhibitor](100μL/site,i.v.)and anisomycin(JNK activator)(100μL/site,i.v.)15 min before LPS,respectively.The depressive behaviors were assessed by open field test,sucrose preference test,and forced swimming test at 24 h post-LPS administration.Tumor necrosis factor-α(TNF-α)and interleukin-1β(IL-1β)levels in plasma were measured by ELISA.The levels of phospho-JNK,TNF-α,IL-1β,Bcl-2,Bax,cytochrome c and caspase-3 were evaluated by Western blotting.Results:FA alleviated depression symptoms caused by LPS in mice,including increasing sucrose water consumption in sucrose preference test and reducing the immobility time in forced swimming test.FA could inhibit upregulated levels of phospho-JNK,TNF-α,and IL-1β.FA also markedly decreased Bax,caspase-3,and cytochrome c,and increased Bcl-2 levels.Besides,SP600125 showed neuroprotective effect similar to FA which was attenuated by anisomycin.Conclusions:FA attenuates inflammation and apoptosis by inhibiting LPS-induced activation of JNK to alleviate depressionlike behaviors.

In vitro and in vivo effects of ferulic acid on gastrointestinal motility:Inhibition of cisplatin-induced delay in gastric emptying in rats

AIM: To study the effects of ferulic acid on gastrointe-stinal motility both in vitro and in vivo.METHODS: Ferulic acid induced concentration-dependent stimulation of the basal tone of isolated guinea pig ileum (2-20 μmol/L) and isolated rat fundus (0.05-0.4 mmol/L). RESULTS: Ferulic acid significantly accelerated the gastrointestinal transit and gastric emptying in rats in a dose-dependent manner (50-200 mg/kg, po). Cisplatin (2.5-20 mg/kg, ip) induced a dose-dependent delay in gastric emptying in rats. Pretreatment with ferulic acid dose-dependently, significantly reversed the cisplatin-induced delay in gastric emptying. CONCLUSION: The endogenous prostaglandins (PGs) are involved in mediating the stimulant effects of ferulic acid. This effect of dietary ferulic acid may help improve other accompanying gastrointestinal symptoms such as abdominal discomfort and also may protect against emesis induced by cytotoxic drugs.

Anti-insulin resistant effect of ferulic acid on high fat diet-induced obese mice

Objective: To evaluate the insulin sensitivity action of ferulic acid(FA) in skeletal muscle and hypothalamus of high-fat diet(HFD)-induced obese mice. Methods: Obese mouse model was induced by HFD(45 kcal% lard fat) for 16 weeks. After 8 weeks of HFD feeding, these obese mice were orally treated with FA at doses of 25 and 50 mg/kg/day for 8 weeks. At the end of all treatments, the epididymal fat, pancreas, skeletal muscle and hypothalamus were removed for biochemical parameter and protein expression examinations. Results: FA treatment significantly decreased leptin level in fat tissue and insulin level in pancreas(P < 0.05). Interestingly, obese mice treated with FA increased the protein expressions of insulin receptor substrate-1, phosphatidylinositol 3-kinase, and phosphorylated-protein kinase B in both muscle and brain(P < 0.05). The phosphorylations of adenosine monophosphate-activated protein kinase and acetyl-CoA carboxylase in muscle, and leptin receptor protein in hypothalamus were also increased(P < 0.05). The pancreatic islets histology showed smaller size in obese mice treated with FA compared to untreated obese mice. Conclusions: These findings indicate the beneficial effect of FA in improving insulin resistance in HFD-induced obese mice. These effects are probably mediated via modulating the insulin receptor substrate/phosphatidylinositol 3-kinase/protein kinase B or adenosine monophosphate-activated protein kinase pathways.

Antibacterial activity and inhibition against Staphylococcus aureus NorA efflux pump by ferulic acid and its esterified derivatives

Objective:To evaluate the inhibitory activity of ferulic acid and four of its esterified derivatives(methyl,ethyl,propyl,and butyl)against resistance mechanisms in Staphylococcus aureus strains.Methods:Ferulic acid derivatives were obtained by esterification with methanol,ethanol,propanol,and butanol,and then characterized by hydrogen and carbon-13 nuclear magnetic resonance analysis.The minimum inhibitory concentrations(MIC)of ferulic acid and its esterified derivatives,ethidium bromide,and norfloxacin were obtained using the microdilution test,while the efflux pump inhibition test was conducted by examining reduction in the MICs of norfloxacin and ethidium bromide.Molecular docking was also carried out using the Schrodinger Suite 2015 molecular modeling software.A three-dimensional model of NorA efflux pump was generated using I-TASSER.The best scoring model was used as a receptor for ligand-receptor docking.Results:The methyl and butyl ester derivatives did not demonstrate significant antimicrobial activity.However,a significant synergic effect was evidenced when norfloxacin was combined with the ethyl and propyl esterified derivatives.The docking study demonstrated favorable energy of interaction between ferulate derivatives and NorA,and amino acid residues TYR57,TYR58,and LEU255 were present commonly in stabilizing all complexes.The PCA analysis corroborated the docking hypothesis that the lipophilic character and hydrogen bond interactions were the most relevant characteristics involved with NorA inhibitors.The pharmacokinetic parameters of ferulic acid derivatives showed good ADMET properties,demonstrating that they can be easily absorbed and have no effect or inhibit the cytochrome P450 enzyme complex,revealing their potential as drug candidates.Conclusions:This study provides strong evidence that the molecular basis for this activity is potentially due to the NorA efflux pump.

Determination of Volatile Oil and Ferulic Acid in Different Parts of Wild Ferula sinkiangensis K. M. Shen and Ferula fukanensis K. M.Shen Cultivars

[Objectives] To increase the reserves distribution and planting area of Ferula resources,protect wild Ferula resources,make comparative analysis on wild and cultivated varieties of Ferula medicinal materials,and provide references for quality evaluation of Ferula herbs collected from cultivation environment. [Methods] Volatile oil determination and high performance liquid chromatography were used to measure volatile oil and ferulic acid in different parts of wild and cultivated varieties of Ferula. [Results] In the volatile oil measured from artificially pressed Ferula lipid,wild varieties in different places conformed to the pharmacopoeia standard( volatile oil content ≥10%); in cultivated varieties,F. fukanensis K. M. Shen and F. sinkiangensis K. M. shen reached the pharmacopoeia standard. According to measurement results of ferulic acid,the ferulic acid content of roots and leaves of Altay,Fukang,and Yining cultivars were higher than that of wild varieties. [Conclusions]The ferulic medicinal herbs collected from artificial cultivation environment have considerable prospect,and many parts of Ferula herbs can be used for raw materials for preparation of extracts.

Effects of ferulic acid on antioxidant activity in Angelicae Sinensis Radix, Chuanxiong Rhizoma, and their combination

The present study aimed at exploring different roles of the same compound in different environment, using preparative HPLC, and the significance to investigating bio-active constituents in traditional Chinese medicine （TCM） on the basis of holism. In this study, the depletion of target component ferulic acid （FA） by using preparative HPLC followed by antioxidant activity testing was applied to investigate the roles of FA in Angelicae Sinansis Radix （DG）, Chuanxiong Rhizoma （CX） and their combination （GX）. The antioxidant activity was performed by 1, 1-diphenyl-2-picrylhydrazyl （DPPH） radical-scavenging activity testing. FA was successfully and exclusively depleted from DG, CX, and GX, respectively. By comparing the effects of the samples, it was found that FA was one of the main antioxidant constituents in DG, CX and GX, and the roles of FA were DG 〉 CX 〉 GX. Furthermore, the effects of FA varied at different doses in these herbs. This study provided a reliable and effective approach to clarifying the contribution of same compound in different TCMs to their bio-activities. The role of a constituent in different TCMs might be different, and a component with the same content might have different effects in different chemical environments. Furthermore, this study also suggested the potential utilization of preparative HPLC in the characterization of the roles of multi-ingredients in TCM.

Probiotic effect of ferulic acid esterase-producing Lactobacillus plantarum inoculated alfalfa silage on digestion,antioxidant,and immunity status of lactating dairy goats

A feeding experiment was conducted to determine the effects of inoculating alfalfa silage with a ferulic acid esterase-producing inoculum on feed digestibility,rumen fermentation,antioxidant,and immunity status of lactating dairy goats.Twenty dairy goats were distributed into 2 experimental groups consisting of control diet(Lp MTD/1,including Lactobacillus plantarum MTD/1 inoculated silage)against diet containing silage treated with ferulic acid esterase-producing L.plantarum A1(Lp A1).Alfalfa silage inoculated with a ferulic acid esterase-producing Lp A1 had better fermentation quality than the Lp MTD/1inoculation.The application of Lp A1 improved silage antioxidant capacity as indicated by greater total antioxidant capacity(T-AOC),superoxide dismutase(SOD)and glutathion peroxidase(GSH-Px)activities in Lp A1 treated silage versus Lp MTD/1 treatment.Compared with Lp MTD/1 treated group,inoculation of silage with Lp A1 increased apparent total tract digestibility of dietary dry matter,organic matter and crude protein,and ruminal concentrations of total volatile fatty acids,acetate,propionate and isobutyrate as well.The results of current study also demonstrated improved antioxidant capacity and immune performance of dairy goats with Lp A1 inoculation.Feeding Lp A1-treated silage increased dairy goats’serum antioxidase activity,such as T-AOC,SOD,GSH-Px and catalase,and the serum concentration of immunoglobulin A,while decreased tumor necrosis factor a,interleukin(IL)-2 and IL-6.In addition,compared with Lp MTD/1,diet containing alfalfa silage inoculated with Lp A1 endowed dairy goats’milk with greater fat and protein contents,improved dairy goat milk quality without affecting feed efficiency.

Ferulic acid prevents liver injury and increases the anti-tumor effect of diosbulbin B in vivo

The present study is designed to investigate the protection by ferulic acid against the hepatotoxicity induced by diosbulbin B and its possible mechanism, and further observe whether ferulic acid augments diosbulbin B- induced anti-tumor activity. The results show that ferulic acid decreases diosbulbin B-increased serum alanine transaminase/aspartate transaminase （ALT/AST） levels. Ferulic acid also decreases lipid peroxide （LPO） levels which are elevated in diosbulbin B-treated mice. Histological evaluation of the liver demonstrates hydropic degeneration in diosbulbin B-treated mice, while ferulic acid reverses this injury. Moreover, the activities of copper- and zinc-containing superoxide dismutase （CuZn-SOD） and catalase （CAT） are decreased in the livers of diosbulbin B-treated mice, while ferulic acid reverses these decreases. Further results demonstrate that the mRNA expressions of CuZn-SOD and CAT in diosbulbin B-treated mouse liver are significantly decreased, while ferulic acid prevents this decrease. In addition, ferulic acid also augments diosbulbin B-induced tumor growth inhibition compared with diosbulbin B alone. Taken together, the present study shows that ferulic acid prevents diosbulbin B-induced liver injury via ameliorating diosbulbin B-induced liver oxidative stress injury and augments diosbulbin B-induced anti-tumor activity.

Dietary ferulic acid and vanillic acid on inflammation,gut barrier function and growth performance in lipopolysaccharide-challenged piglets

Ferulic acid(FA)and vanillic acid(VA)are considered as major phenolic metabolites of cyanidin 3-glucoside,a polyphenol that widely exists in plants that possess a protective effect against oxidative stress and inflammation in our previous study.This study aimed to investigate the effect of FA and VA on inflammation,gut barrier function,and growth performance in a weaned piglet model challenged with lipopolysaccharide(LPS).Thirty-six piglets(PIC 337×C48,28 d of age)were randomly allocated into 3 treatments with 6 replicate pens(2 piglets per pen).They were fed with a basal diet or a diet containing 4,000 mg/kg of FA or VA.Dietary supplementation of VA significantly increased average daily gain(ADG)(P<0.05).Both FA and VA decreased serum levels of thiobarbituric acid reactive substances(TBARS),interlukin(IL)-1β,IL-2,IL-6,and tumor necrosis factor(TNF)-α(P<0.05),and enhanced the expression of tight junction protein oclaudin(P<0.05).Analysis of gut microbiota indicated that both FA and VA increased the Firmicutes/Bacteroidetes ratio alongside reducing the relative abundance of the Prevotellaceae family including Prevotella 9 and Prevotella 2 genera,but enriched the Lachoiraceaea family including the Lachnospiraceae FCS020 group(P<0.05).Moreover,VA reduced the relative abundance of Prevotella 7 and Prevotella 1 but enriched Lachnospira,Eubacterium eligens group,and Eubacterium xylanophilum group(P<0.05),while FA showed a limited effect on these genera.The results demonstrated that both VA and FA could alleviate inflammation and oxidative stress,but only VA has a significant positive effect on the growth performance of LPS-challenged piglets potentially through modulating gut microbiota.

Scavenging activity and mechanism study of ferulic acid against reactive carbonyl species acrolein

Acrolein,known as one of the most common reactive carbonyl species,is a toxic small molecule affecting human health in daily life.This study is focused on the scavenging abilities and mechanism of ferulic acid and some other phenolic acids against acrolein.Among the 13 phenolic compounds investigated,ferulic acid was found to have the highest efficiency in scavenging acrolein under physiological 8nditions.Ferulic acid remained at(3.04±1.89)%and acrolein remained at(29.51±4.44)%after being incubated with each other for 24 h.The molecular mechanism of the detoxifying process was also studied.Detoxifying products,namely 2-methoxy-4-vinyIphenol(product 21)and 5-(4-hydroxy-3-methoxyphenyl)pent-4-enal(product 22),were identified though nuclear magnetic resonanee(NMR)and gas chromatography-mass spectrometry(GC-MS),after the scavenging process.Ferulic acid showed significant activity in scavenging acrolein under physiological conditions.This study indicates a new method for inhibiting damage from acrolein.

Development of a new ferulic acid certified reference material for use in clinical chemistry and pharmaceutical analysis

This study compares the results of three certified methods, namely differential scanning calorimetry (DSC), the mass balance (MB) method and coulometric titrimetry (CT), in the purity assessment of ferulic acid certified reference material (CRM). Purity and expanded uncertainty as determined by the three methods were respectively 99.81%, 0.16%; 99.797, 0.16%; and 99.81%, 0.26% with, in all cases, a coverage factor (k) of 2 (P=95%). The purity results are consistent indicating that the combination of DSC, the MB method and CT provides a confident assessment of the purity of suitable CRMs like ferulic acid. (C) 2015 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.

Ferulic acid mediates prebiotic responses of cereal-derived arabinoxylans on host health

Dietary fiber is named as “the 7th nutrient” for humans, which is beneficial to improve intestinal healthand prevent metabolic disease of the host. Mechanisms of dietary fiber administration on improved hosthealth are mediated by short chain fatty acids (SCFA), which are reported to activate G protein-coupledreceptors (GPR) and suppress activity of histone deacetylase (HDAC) to down-regulate expression ofnuclear factor-к-gene binding (NF-кB) signaling. Arabinoxylan is fermented by gut microbiota to produceSCFA and improved microbial community composition, intestinal barrier functions and host health.Interestingly, the latest publications have observed that ferulic acid combined with the arabinose inarabinoxylans from various cereal grains can be released through gut microbial fermentation. Ferulic acidcan improve antioxidase activity and decrease reactive oxygen species (ROS) concentration by activatingthe signaling pathway of Kelch-like ECH-associated protein-1 and nuclear factor E2-related factor-2(Keap1-Nrf2). However, the role of ferulic acid in cooperation with SCFA produced from microbialfermentation of cereal-derived arabinoxylan to regulate the intestinal health and host metabolisms, hasbeen widely unclear. This review summarizes the potential mechanisms of ferulic acid from microbialfermentation of cereal-derived arabinoxylans on immunological functions and physiological metabolismsof the host. The evidence presented in the review indicates that dietary supplementation withcereal-derived arabinoxylans improves antioxidant capacity of intestinal epithelial cells due to theproduction of ferulic acid and SCFA from microbial fermentation. Ferulic acid can cooperate with SCFA toregulate intestinal integrity and immunological functions of the host. Peroxisome proliferator activatedreceptorg (PPARg) may play an important role in integrating ferulic acid and SCFA to regulate host healthand metabolism.

Photosensitive damage of lysozyme caused by pazufloxacin and the protective effect of ferulic acid

Laser flash photolysis and sodium dodecyl sulfate-polyacrylamide gel electrophoresis(SDS-PAGE) experiments were carried out to study the photosensitive damage induced by pazufloxacin(PAX) and the protection of lysozyme(Lyso) by ferulic acid(FCA), an active antioxidant. Transient absorption spectra revealed electron transfer from Lyso and FCA to 3PAX*, with respective bimolecular reaction rate constants of 6.3×107 and 1.4×1010 dm3/(mol s). A pulse radiolysis study was also performed to investigate the formation of Lyso radical cations. Results showed that FCA effectively inhibited the cross-linking of protein induced by fluoroquinolones. Finally, a mechanism of the protective effect of FCA on Lyso was proposed.

Design and synthesis of the ring-opened derivative of 3-n-butylphthalide-ferulic acid-glucose trihybrids as potential anti-ischemic agents

To improve aqueous solubility and anti-ischemic activity of 3-n-butylphthalide(NBP),we designed and synthesized the ring-opened derivative of NBP-ferulic acid-glucose trihybrids(S1-S8).These hybrids inhibited adenosine diphosphate(ADP)-or arachidonic acid(AA)-induced platelet aggregation,among them,S2 was 30-fold more water-soluble,and over 10-fold more potent in inhibition of platelet aggregation,as well as reduced ROS generation and protected primary neuronal cells from OGD/Rinduced damage,in comparison with NB P.Additionally,S2 was more active than its three moieties alone or in combination,suggesting that the activity of S2 may be attributed to the synergistic effects of these moieties.Importantly,in vivo studies indicated that S2 not only possessed good pharmacokinetic profile,but also improved NBP distribution in rodent brain,suggesting that the glucose moiety in S2 may be recognized by glucose transporter 1(GLUT1)on blood-brain barrier(BBB),promoting it to penetrate through BBB.Our findings suggest that S2 may be a promising candidate for the intervention of ischemic stroke,warranting further study.