Background Oxidative stress significantly impacts growth performance and liver function in piglets.Ferulic acid(FA)works as an antioxidant,however,the role and mechanism of FA in the regulation of diquat-induced oxida...Background Oxidative stress significantly impacts growth performance and liver function in piglets.Ferulic acid(FA)works as an antioxidant,however,the role and mechanism of FA in the regulation of diquat-induced oxidative stress in piglets are less known.This study was designed to investigate the effects of FA on growth performance and antioxi-dant capacity in piglets with diquat challenge.Methods Thirty-two healthy DLY(Duroc×Landrace×Yorkshire)piglets(13.24±0.19 kg)were randomly divided into one of two diets including 0 or 4 g/kg FA for 14 d.On d 15,all pigs were intraperitoneally injected diquat or sterile saline.Results Dietary supplementation with ferulic acid(FA)significantly improved the average daily gain(ADG)and decreased feed-gain ratio(F/G)of piglets.Here,dietary FA supplementation reduced serum aspartate aminotrans-ferase(AST),alanine aminotransferase(ALT)activities in diquat challenged piglets.Furthermore,diquat infusion increased reactive oxygen radicals(ROS)level in liver,decreased the activities of total superoxide dismutase(T-SOD)and glutathione peroxidase(GSH-Px),total antioxidant capacity(T-AOC)and increased malondialdehyde(MDA)con-tent in the liver and serum.Supplementation with FA significantly increased T-AOC and T-SOD activities and decreased MDA and ROS levels.FA down-regulated gene and protein expression of Keap1,and up-regulated protein expression of Nrf2 and HO-1 in the liver of piglets with diquat challenge.Importantly,diquat challenge increased the ratio of late apoptosis,increased serum levels of IL-1β,IL-18 and lactate dehydrogenase(LDH),and up-regulated pyroptosis-related genes in the liver.FA supplementation reduced the ratio of late apoptosis and down-regulated mRNA expression of Caspase-1.Accordingly,FA addition reduced concentration of IL-1β,IL-18,and LDH under diquat challenge.Conclusions Diquat-induced oxidative stress reduced growth performance and impaired liver function in piglets.Dietary FA supplementation enhanced the antioxidant capacity and reduced the degree of hepatocyte pyroptosis,thereby alleviating the oxidative damage in the liver and mitigating the impact of diquat on growth performance of piglets.展开更多
Extensive use of avermectin(AVM)in agriculture can seriously contaminate fish in aquaculture.Ferulic acid(FA)is a strong antioxidant sourced from plants and is widely applied in food and medicine,but its protective fu...Extensive use of avermectin(AVM)in agriculture can seriously contaminate fish in aquaculture.Ferulic acid(FA)is a strong antioxidant sourced from plants and is widely applied in food and medicine,but its protective function on the immunological damage caused by AVM is still lacking.In this study,carp were chronically exposed to(1/1096 hr LC_(50))AVM for 30 day(s),with a dietary supplement of FA(400 mg/kg)to assess its effects on carp spleen.The experimental groups(n=10)included:control,AVM-exposed(2.404μg/L),FA+AVM co-treated,and FA alone.Long-term AVM exposure altered spleen tissue,reducing serum complement C3(p<0.01)and immunoglobulin M levels(p<0.001),and increasing proinflammatory tnf-α(p<0.001),il-6(p<0.001),il-1β(p<0.001),and inos mRNA levels,whilst down-regulating the anti-inflammatory tgf-β(p<0.05).Additionally,it disrupted the balance of oxidative stress indicators such asMDA(p<0.001),T-AOC,GSH,and CAT,leading to spleen tissue apoptosis(42.4%).However,the addition of FA reversed these conditions,elevated the anti-inflammatory factor,and improved spleen immune function following chronic exposure to AVMin carp.Moreover,the ability to restore oxidative homeostasis in carp by adjusting the Nrf2/NQO-1 axis protected the health of spleen tissues.This discovery also supports the development of fish feed for aquaculture.展开更多
To test and study the Syndrome and Treatment Pharmacokinetics (S & TRK),we studied the pharmacokinetics of ferulic acid in healthy and blood stasis (microcirculation dysfunction)rabbits by RP-HPLC. After a single ...To test and study the Syndrome and Treatment Pharmacokinetics (S & TRK),we studied the pharmacokinetics of ferulic acid in healthy and blood stasis (microcirculation dysfunction)rabbits by RP-HPLC. After a single intravenous injection offenilic acid(5mg/kg)to healthy and blood stasis rabbits, compartment model of ferulic acid serum concentration was fitted and then pharmacokinetic parameters were calculated with a MCPKP program on a COMPAQ 386 compute Important parameters are as follows: In healthy rabbits V_B=0.9525±0.0211 L/kg,V_1=0.2462±0.0381 L/kg, CL_B=1.8133±0.9512 L/h·kg, T_(1/2β)=0.3639±0913, AUC=2.7566±0.8232 μg·h/ml; In blood stasis rabbits V_B=0.7882±0.0321 L/kg,V_1=0.1966±0.0537 L/kg,CL_B=0.8820±0.5481 L/h·kg,T_(1/2β)=0.6193±0.1216 h, AUC=5.6690±2.3541μg·h/ml.Through this experiment we found the sig-nificant differences in the FA's pharmacokinetic parameters between healthy and blood stasis rabbits.The results obtained correspond with S & TPK.展开更多
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 lea...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展开更多
Objective A strain of Aspergillus niger(A. niger), capable of releasing bound phenolic acids from wheat bran, was isolated. This strain was identified by gene sequence identification. The antioxidant and anti-inflamma...Objective A strain of Aspergillus niger(A. niger), capable of releasing bound phenolic acids from wheat bran, was isolated. This strain was identified by gene sequence identification. The antioxidant and anti-inflammatory capacity of ferulic acid released from wheat bran by this A. niger strain(FA-WB) were evaluated. Methods Molecular identification techniques based on PCR analysis of specific genomic sequences were conducted; antioxidant ability was examined using oxygen radical absorbance capacity(ORAC), cellular antioxidant activity(CAA) assays, and erythrocyte hemolysis assays. RAW264.7 cells were used as a model to detect anti-inflammatory activity. Results The filamentous fungal isolate was identified to be A. niger. ORAC and CAA assay showed that FA-WB had better antioxidant activity than that of the ferulic acid standard. The erythrocyte hemolysis assay results suggested that FA-WB could attenuate AAPH-induced oxidative stress through inhibition of reactive oxy gen species(ROS) generation. FA-WB could significantly restore the AAPH-induced increase in intracellular antioxidant enzyme activities to normal levels as well as inhibit the intracellular malondialdehyde formation. TNF-?, IL-6, and NO levels indicated that FA-WB can inhibit the inflammation induced by lipopolysaccharide(LPS). Conclusion Ferulic acid released from wheat bran by a new strain of A. niger had good anti-inflammatory activity and better antioxidant ability than standard ferulic acid.展开更多
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...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.展开更多
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...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.展开更多
Objective:To investigate the effects of the active ingredients combined therapy on inflammatory factors interleukin 1 beta(IL-1β)and neuropeptide Y(NPY)based on pharmacodynamics in rats.Methods:The animal model was b...Objective:To investigate the effects of the active ingredients combined therapy on inflammatory factors interleukin 1 beta(IL-1β)and neuropeptide Y(NPY)based on pharmacodynamics in rats.Methods:The animal model was built by transient middle cerebral artery occlusion(MCAO).The method for evaluating the concentrations of the FA-Pr-AI components in rat plasma was established by using HPLC and the expression levels of IL-1βand NPY were determined by ELISA.A new mathematics method of the trend of percentage rate of change(PRC)was used to assess the correlation between pharmacokinetics(PK)and pharmacodynamics(PD).Results:FA-Pr-Al in combination reduced neurological deficits,decreased infarct volume and inhibited the expression levels of IL-1βand NPY(all P<0.05)compared with the model group.FA,Pr and Al all displayed two compartment open models in rats.Clockwise hysteresis loops were obtained by time-concentration-effect curves.IL-1βand NPY level changes in the plasma followed an opposite trend to the plasma concentration tendency after C_(max)was reached.Astragaloside's PRC value was significantly higher than those of FA and puerarin between 120 to 180 min.Conclusions:The pharmacokinetics of FA-PrAl in combination were closely related its pharmacodynamics in treating ischemia/reperfusion injury,and the components of FA-Pr-Al may have a synergistic pharmacological effect.Astragaloside may play a more pronounced role in regulating IL-1βand NPY levels compared with puerarin or FA.展开更多
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 som...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.展开更多
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 ...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.展开更多
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...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.展开更多
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....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.展开更多
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) ...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.展开更多
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 ...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.展开更多
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 adenosin...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.展开更多
According to WHO, cancer is a leading cause of death worldwide, accounting for 8.2 million deaths in 2012. Among several factors involved in the pathogenesis of cancer, free radical formation followed by damage to DNA...According to WHO, cancer is a leading cause of death worldwide, accounting for 8.2 million deaths in 2012. Among several factors involved in the pathogenesis of cancer, free radical formation followed by damage to DNA and cell protein is one of the causes. Natural plant products have gained enormous interest in the prevention or treatment of chronic diseases. Ferulic acid, like other phenolic acids (caffeic acid, sinapic acid) possess anti cancer activity. A series of ferulic esters (FE1 - FE11) and ferulic amides (FA1 - FA10) were synthesized and evaluated for their cytotoxic activity.展开更多
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 de...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.展开更多
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...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.展开更多
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...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.展开更多
[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 provi...[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.展开更多
基金Sichuan Science and Technology Program(No.2021ZDZX0009).
文摘Background Oxidative stress significantly impacts growth performance and liver function in piglets.Ferulic acid(FA)works as an antioxidant,however,the role and mechanism of FA in the regulation of diquat-induced oxidative stress in piglets are less known.This study was designed to investigate the effects of FA on growth performance and antioxi-dant capacity in piglets with diquat challenge.Methods Thirty-two healthy DLY(Duroc×Landrace×Yorkshire)piglets(13.24±0.19 kg)were randomly divided into one of two diets including 0 or 4 g/kg FA for 14 d.On d 15,all pigs were intraperitoneally injected diquat or sterile saline.Results Dietary supplementation with ferulic acid(FA)significantly improved the average daily gain(ADG)and decreased feed-gain ratio(F/G)of piglets.Here,dietary FA supplementation reduced serum aspartate aminotrans-ferase(AST),alanine aminotransferase(ALT)activities in diquat challenged piglets.Furthermore,diquat infusion increased reactive oxygen radicals(ROS)level in liver,decreased the activities of total superoxide dismutase(T-SOD)and glutathione peroxidase(GSH-Px),total antioxidant capacity(T-AOC)and increased malondialdehyde(MDA)con-tent in the liver and serum.Supplementation with FA significantly increased T-AOC and T-SOD activities and decreased MDA and ROS levels.FA down-regulated gene and protein expression of Keap1,and up-regulated protein expression of Nrf2 and HO-1 in the liver of piglets with diquat challenge.Importantly,diquat challenge increased the ratio of late apoptosis,increased serum levels of IL-1β,IL-18 and lactate dehydrogenase(LDH),and up-regulated pyroptosis-related genes in the liver.FA supplementation reduced the ratio of late apoptosis and down-regulated mRNA expression of Caspase-1.Accordingly,FA addition reduced concentration of IL-1β,IL-18,and LDH under diquat challenge.Conclusions Diquat-induced oxidative stress reduced growth performance and impaired liver function in piglets.Dietary FA supplementation enhanced the antioxidant capacity and reduced the degree of hepatocyte pyroptosis,thereby alleviating the oxidative damage in the liver and mitigating the impact of diquat on growth performance of piglets.
基金supported by the National Natural Science Foundation of China(No.81773968)the Priority Academic Program Development of Jiangsu Higher Education Institutions of China.
文摘Extensive use of avermectin(AVM)in agriculture can seriously contaminate fish in aquaculture.Ferulic acid(FA)is a strong antioxidant sourced from plants and is widely applied in food and medicine,but its protective function on the immunological damage caused by AVM is still lacking.In this study,carp were chronically exposed to(1/1096 hr LC_(50))AVM for 30 day(s),with a dietary supplement of FA(400 mg/kg)to assess its effects on carp spleen.The experimental groups(n=10)included:control,AVM-exposed(2.404μg/L),FA+AVM co-treated,and FA alone.Long-term AVM exposure altered spleen tissue,reducing serum complement C3(p<0.01)and immunoglobulin M levels(p<0.001),and increasing proinflammatory tnf-α(p<0.001),il-6(p<0.001),il-1β(p<0.001),and inos mRNA levels,whilst down-regulating the anti-inflammatory tgf-β(p<0.05).Additionally,it disrupted the balance of oxidative stress indicators such asMDA(p<0.001),T-AOC,GSH,and CAT,leading to spleen tissue apoptosis(42.4%).However,the addition of FA reversed these conditions,elevated the anti-inflammatory factor,and improved spleen immune function following chronic exposure to AVMin carp.Moreover,the ability to restore oxidative homeostasis in carp by adjusting the Nrf2/NQO-1 axis protected the health of spleen tissues.This discovery also supports the development of fish feed for aquaculture.
文摘To test and study the Syndrome and Treatment Pharmacokinetics (S & TRK),we studied the pharmacokinetics of ferulic acid in healthy and blood stasis (microcirculation dysfunction)rabbits by RP-HPLC. After a single intravenous injection offenilic acid(5mg/kg)to healthy and blood stasis rabbits, compartment model of ferulic acid serum concentration was fitted and then pharmacokinetic parameters were calculated with a MCPKP program on a COMPAQ 386 compute Important parameters are as follows: In healthy rabbits V_B=0.9525±0.0211 L/kg,V_1=0.2462±0.0381 L/kg, CL_B=1.8133±0.9512 L/h·kg, T_(1/2β)=0.3639±0913, AUC=2.7566±0.8232 μg·h/ml; In blood stasis rabbits V_B=0.7882±0.0321 L/kg,V_1=0.1966±0.0537 L/kg,CL_B=0.8820±0.5481 L/h·kg,T_(1/2β)=0.6193±0.1216 h, AUC=5.6690±2.3541μg·h/ml.Through this experiment we found the sig-nificant differences in the FA's pharmacokinetic parameters between healthy and blood stasis rabbits.The results obtained correspond with S & TPK.
基金Supported by the Natural Science Foundation of Guangdong Province (No. 011563, No. 04020114).
文摘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
基金financially supported by the Science and Technology Planning Project of Guangdong Province [Nos.2016A040402020,2016B010121014]
文摘Objective A strain of Aspergillus niger(A. niger), capable of releasing bound phenolic acids from wheat bran, was isolated. This strain was identified by gene sequence identification. The antioxidant and anti-inflammatory capacity of ferulic acid released from wheat bran by this A. niger strain(FA-WB) were evaluated. Methods Molecular identification techniques based on PCR analysis of specific genomic sequences were conducted; antioxidant ability was examined using oxygen radical absorbance capacity(ORAC), cellular antioxidant activity(CAA) assays, and erythrocyte hemolysis assays. RAW264.7 cells were used as a model to detect anti-inflammatory activity. Results The filamentous fungal isolate was identified to be A. niger. ORAC and CAA assay showed that FA-WB had better antioxidant activity than that of the ferulic acid standard. The erythrocyte hemolysis assay results suggested that FA-WB could attenuate AAPH-induced oxidative stress through inhibition of reactive oxy gen species(ROS) generation. FA-WB could significantly restore the AAPH-induced increase in intracellular antioxidant enzyme activities to normal levels as well as inhibit the intracellular malondialdehyde formation. TNF-?, IL-6, and NO levels indicated that FA-WB can inhibit the inflammation induced by lipopolysaccharide(LPS). Conclusion Ferulic acid released from wheat bran by a new strain of A. niger had good anti-inflammatory activity and better antioxidant ability than standard ferulic acid.
基金supported by National Key Technology R&D Program(No.2008BAI51B01)the Specialized Research Fund for the Doctoral Program of Higher Education of China(No.20113237110010)A Project Funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions(PAPD)
文摘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.
基金Project supported by the Program for New Century Excellent Talents in University(No.NCET-11-1054)the National Natural Science Foundation of China(No.81322053)the Program for Changjiang Scholars and Innovative Research Team in University(No.PCSIRTIRT1071),China
文摘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.
基金supported by the National Science Foundation of China(81274176)the Clinical Medicine Special Foundation of China(12012064)+1 种基金the National Science Foundation of Province(LY13H280008)the Science and Technology Department of public welfare project(2014C33212)
文摘Objective:To investigate the effects of the active ingredients combined therapy on inflammatory factors interleukin 1 beta(IL-1β)and neuropeptide Y(NPY)based on pharmacodynamics in rats.Methods:The animal model was built by transient middle cerebral artery occlusion(MCAO).The method for evaluating the concentrations of the FA-Pr-AI components in rat plasma was established by using HPLC and the expression levels of IL-1βand NPY were determined by ELISA.A new mathematics method of the trend of percentage rate of change(PRC)was used to assess the correlation between pharmacokinetics(PK)and pharmacodynamics(PD).Results:FA-Pr-Al in combination reduced neurological deficits,decreased infarct volume and inhibited the expression levels of IL-1βand NPY(all P<0.05)compared with the model group.FA,Pr and Al all displayed two compartment open models in rats.Clockwise hysteresis loops were obtained by time-concentration-effect curves.IL-1βand NPY level changes in the plasma followed an opposite trend to the plasma concentration tendency after C_(max)was reached.Astragaloside's PRC value was significantly higher than those of FA and puerarin between 120 to 180 min.Conclusions:The pharmacokinetics of FA-PrAl in combination were closely related its pharmacodynamics in treating ischemia/reperfusion injury,and the components of FA-Pr-Al may have a synergistic pharmacological effect.Astragaloside may play a more pronounced role in regulating IL-1βand NPY levels compared with puerarin or FA.
基金Project supported by the National Natural Science Foundation of China(Nos.21327010 and 21372199)
文摘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.
文摘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.
基金supported by the Six Talent Peaks Project of Jiangsu Province(YY-042)Xuzhou Science&Technology Plan Project(KC16SG250)
文摘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.
基金Project(50925417)supported by the National Science Fund for Distinguished Young Scholars of ChinaProject(50830301)supported by the National Natural Science Foundation of ChinaProject(2011467062)supported by National Research Fund for Public Benefit(Environmental Protection)Industries,China
文摘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.
基金supported by the Faculty of Medicine Research Fund(GEN2-01/2016),Thammasat University,Thailand
文摘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.
基金supported by the National Natural Science Foundation of China(Grant Nos.:21927808 and 81803483).
文摘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.
基金the National Natural Science Foundation of China(Nos.81773573,81822041,21977116 and 81673305)National Science&Technology Major Project“Key New Drug Creation and Manufacturing Program”(No.2018ZX09711002006-013)+2 种基金the open project of State Key Laboratory of Natural Medicines(No.SKLNMZZCX201824)State Key Laboratory of Pathogenesis,Prevention and Treatment of High Incidence Diseases in Central Asia Fund(No.SKL-HIDCA-2018-1)Part of the work was supported by Postgraduate Research&Practice Innovation Program of Jiangsu Province(No.KYCX18_0795)。
文摘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.
文摘According to WHO, cancer is a leading cause of death worldwide, accounting for 8.2 million deaths in 2012. Among several factors involved in the pathogenesis of cancer, free radical formation followed by damage to DNA and cell protein is one of the causes. Natural plant products have gained enormous interest in the prevention or treatment of chronic diseases. Ferulic acid, like other phenolic acids (caffeic acid, sinapic acid) possess anti cancer activity. A series of ferulic esters (FE1 - FE11) and ferulic amides (FA1 - FA10) were synthesized and evaluated for their cytotoxic activity.
文摘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.
基金Supported by Medical Science Foundation of Military for Young Scholars (No.19QNP064)Natural Science Foundation of Jiangsu Province (No.BK20191233)Jiangsu Funding Program for Excellent Postdoctoral Talent (No.2022ZB702)。
文摘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.
基金grateful for the financial support for this work from the National Natural Science Foundation of China(31870560,22108088)the State Key Laboratory of Pulp and Paper Engineering(South China University of Technology),No.202105.
文摘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.
基金Supported by Traditional Chinese Medicine Project of Ministry of Industry and Information Technology"Wild Tending and Artificial Cultivation Base Construction of Endangered Medicinal Material Ferula"(2015)Yili Botanical Garden Planning and Design and Pre-construction Project(20130122-1)
文摘[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.
