The extracted and purified ferulic acid residue from Radix angelicae sinensis was quantified by an established HPLC system composed of the following conditions: reversed phase column C-18 Purosphere 4.6mm 1D x 250 mm (5mm); mobile phase: acetonitrile/potassium dihydrophosphate 10 mM/L (15/85); pH: 4.5; flow rate: 1.2 mL/min; column temperature: 30oC. The results showed that the method can meet the following criteria: Rs > 1.5, RSD < 2%, N > 1 000, Tf in the range 0.8-1.2
Coumaric Acids ; Drugs ; Chinese Herbal

p-coumaric acid is one of the aromatic compounds that are widely used in food, cosmetics and medicine due to its properties of antibacterium, antioxidation and cardiovascular disease prevention. Tyrosine ammonia-lyase (TAL) catalyzes the deamination of tyrosine to p-coumaric acid. However, the lack of highly active and specific tyrosine ammonia lyase limits cost-effective microbial production of p-coumaric acid. In order to improve biosynthesis efficiency of p-coumaric acid, two tyrosine ammonia-lyases, namely Fc-TAL2 derived from Flavobacterium columnare and Fs-TAL derived from Flavobacterium suncheonense, were selected and characterized. The optimum temperature (55 ℃) and pH (9.5) for Fs-TAL and Fc-TAL2 are the same. Under optimal conditions, the specific enzyme activity of Fs-TAL and Fc-TAL2 were 82.47 U/mg and 13.27 U/mg, respectively. Structural simulation and alignment analysis showed that the orientation of the phenolic hydroxyl group of the conserved Y50 residue on the inner lid loop and its distance to the substrate were the main reasons accounting for the higher activity of Fs-TAL than that of Fc-TAL2. The higher activity and specificity of Fs-TAL were further confirmed via whole-cell catalysis using recombinant Escherichia coli, which could convert 10 g/L tyrosine into 6.2 g/L p-coumaric acid with a yield of 67.9%. This study provides alternative tyrosine ammonia-lyases and may facilitate the microbial production of p-coumaric acid and its derivatives.
Ammonia-Lyases/chemistry* ; Coumaric Acids ; Escherichia coli/genetics* ; Tyrosine

OBJECTIVETo prepare sustained-release pellets of active components from Ligusticun chuanxiong by coating in the fluid-bed.

METHODThe fast-release pellets were prepared by the extrusion-spheronization process. The coating formulation was optimized with the release of ferulic acid as criteria. The micromeritic properties and drug dissolution behaviors of the prepared pellets were evaluated.

RESULTThe pellets presented perfect sphericity. The obviously sustained-release effects were shown in 12 h. The coating weight gain was the major factor impacting drug release.

CONCLUSIONThe coating pellets show the obviously sustained-release effects.

OBJECTIVETo systematically review the efficacy and safety of sodium ferulate (SF) for the treatment of diabetic nephropathy.

METHODSBy computerized retrieving the Cochrane Library, MEDLINE, EMBASE, CNKI, VIP, CBM (theses, conference and internet materials), as well as data from internet materials regarding randomized controlled clinical trials of sodium ferulate for the treatment of diabetic nephropathy were collected completely. Data were strictly extracted using the simple evaluation method recommended in Cochrane Handbook and Meta-analysis was performed using Revman 5.0 software.

RESULTSFourteen randomized controlled trials involving 906 patients met the inclusion criteria. Meta-analysis showed that as compared with the control group, the effects in SF group were superior in terms of reducing urinary albumin excretion rate (UAER) at early stage [WMD = 16.08, 95% confidence interval (95% CI): 11.01 to 21.15] and clinical stage (WMD = 82.66, 95% CI: 66.95 to 98.37), urinary endothelin/endothelin-1 (ET/ET-1, WMD = 10.78, 95% CI: 8.18 to 13.39), levels of serum creatinine (SCr, WMD = 6.42, 95% CI: 1.83 to 11.01), blood urea nitrogen (BUN, SMD = 1.45, 95% CI: 0.19 to 2.71) and total cholesterol (TC, WMD = 0.84, 95% CI: 0.56 to 1.21, as well as in increasing high density lipoprotein-cholesterol (HDL-C, WMD = 0.17, 95% CI: 0.09 to 0.26), showing significant difference between groups. However, the effects of SF were insignificantly different to those of control in reducing fasting blood glucose (FBG, WMD = 0.17, 95% CI: -0.03 to 0.37) and triglyceride (TG, SMD = -0.13, 95% CI -0.49 to 0.23).

CONCLUSIONSAt present the evidences show that SF is superior to the conventional treatment in reducing UAER, ET, SCr, BUN, TC and increasing HDL-C, but there is no evidence to show that SF is superior in reducing FBG and TG. However, the evidence is not strong enough due to the low quality of included literature. More large-scale, multi-center, randomized trials are needed to confirm the efficacy and safety of SF in treating diabetic nephropathy.

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 conditions. 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-vinylphenol (product 21) and 5-(4-hydroxy-3-methoxyphenyl)pent-4-enal (product 22), were identified though nuclear magnetic resonance (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.
Acrolein/toxicity* ; Coumaric Acids/pharmacology* ; Glutathione/physiology* ; Hydroxybenzoates/pharmacology* ; Magnetic Resonance Spectroscopy ; Structure-Activity Relationship

OBJECTIVE: To investigate the effect of ferulic acid, a natural compound, on pancreatic beta cell viability, Ca²⁺ channels, and insulin secretion. METHODS: We studied the effects of ferulic acid on rat insulinoma cell line viability using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide viability assay. The whole-cell patch-clamp technique and enzyme-linked immunosorbent assay were also used to examine the action of ferulic acid on Ca²⁺ channels and insulin secretion, respectively. RESULTS: Ferulic acid did not affect cell viability during exposures up to 72 h. The electrophysiological study demonstrated that ferulic acid rapidly and concentration-dependently increased L-type Ca²⁺ channel current, shifting its activation curve in the hyperpolarizing direction with a decreased slope factor, while the voltage dependence of inactivation was not affected. On the other hand, ferulic acid have no effect on T-type Ca²⁺ channels. Furthermore, ferulic acid significantly increased insulin secretion, an effect inhibited by nifedipine and Ca²⁺-free extracellular fluid, confirming that ferulic acid-induced insulin secretion in these cells was mediated by augmenting Ca²⁺ influx through L-type Ca²⁺ channel. Our data also suggest that this may be a direct, nongenomic action. CONCLUSION This is the first electrophysiological demonstration that acute ferulic acid treatment could increase L-type Ca²⁺ channel current in pancreatic β cells by enhancing its voltage dependence of activation, leading to insulin secretion.
Rats ; Animals ; Insulin Secretion ; Insulin/pharmacology* ; Insulin-Secreting Cells/metabolism* ; Coumaric Acids/metabolism* ; Calcium/metabolism*

OBJECTIVETo establish a quality control method of Fuan oral liquid.

METHODSHigh-performance capillary electrophoresis (HPCE) was used to determine the content of feruild acid in Herba taraxaci, and thin-layer chromatography (TLC) was performed to identify Herba taraxaci and Bupleurum chinense. The condition of HPCE was optimized with a fuse silica capillary tube (70 microm x 60 cm) and 20 mmol/L sodium tetraborate buffer (pH9.18) at a constant voltage of 12 kV and temperature at 25 degrees celsius;, with the detection wavelength at 313 nm.

RESULTSClear spots were displayed on TLC. The calibration curve was linear in the range of 8-40 microg/ml for ferulic acid (Y=360.5-207.4, r=0.9997, n=5). The average recovery rate exceeded 95% with a RSD<3% (n=3).

CONCLUSIONThis method is simple and specific with a good reproducibility for quality control of Fuan oral liquid.

OBJECTIVETo study relationships between the main active ingredients and physical and chemical parameters of dangguibuxue decoction, and to explore the feasibility of characterization the quality of decoction by physical and chemical parameters.

METHODSolutions of ferulic acid and astragaloside with different concentrations were prepared, of which physical and chemical parameters such as surface tension, pH value and conductivity, etc were determined at 25 degrees C. And polynomial regression analysis was used to analyze these data.

RESULTWith the increase of concentration of ferulic acid, pH value was decreased and conductivity was increased. And surface tension was decreased in the aqueous solution of astragaloside. In the combined solution of ferulic acid and astragaloside, ferulic acid was the main influencing pH value and conductivity, while astragaloside was the main factor influencing surface tension.

CONCLUSIONOn one hand, astragaloside concentration has a significant correlation with surface tension, but almost no correlation with pH value and conductivity. On the other hand, ferulic acid concentration has a strong correlation with pH value and conductivity, but almost no correlation with surface tension. In addition, each parameter has strong anti-interference ability and almost didn't change with the addition of another material. These preliminary results suggested that such characteristic parameters could be used to characterize the decoction quality.

In order to investigate the characteristics of transdermal delivery of ferulic acid under the treated of microneedle arrays and the influence on permeability of rat skin capillaries, improved Franz-cells were used in the transdermal delivery experiment with the rat skin of abdominal wall and the length of microneedle arrays, different insertion forces, retention time were studied in the influence of characteristics of transdermal delivery of FA. The amount of FA was determined by HPLC system. Intravenous injection Evans blue and FA was added after microneedle arrays treated. Established inflammation model was built by daubing dimethylbenzene. The amount of Evans blue in the rat skin was read at 590 nm wavelength with a Multiskan Go microplate reader. Compared with passive diffusion group the skin pretreated with microneedle arrays had a remarkable enhancement of FA transport (P <0.01). The accumulation of FA increased with the enhancement of insertion force as to as the increase of retention time. Microneedle arrays with different length had a remarkable enhancement of FA transport, but was not related to the increase of the length. The research of FA on the reduce of permeability of rat skin capillaries indicated that the skin pretreated with microneedle arrays could reduce the content of Evans blue in the skins of rat significantly compared with the untreated group. The permeation rate of ferulic acid transdermal delivery had remarkable increase under the treated of microneedle arrays and the length of microneedle arrays ,the retention time so as to the insertion force were important to the transdermal delivery of ferulic acid.
Administration, Cutaneous ; Animals ; Coumaric Acids ; administration & dosage ; pharmacokinetics ; Male ; Needles ; Rats ; Rats, Sprague-Dawley ; Skin Absorption

Preparative HPLC was used to prepare ferulic acid, senkyunolide I and senkyunolide H from Ligusticum chuanxiong. The separation was conducted on a Shim-Pack Prep-ODS (20.0 mm x 250 mm, 5 microm) column with the mobile phase of methanol-0.2% glacial acetic acid (50:50)at the flow rate of 5 mL x min(-1). The detection wavelength was 278 nm, and the purity of each compound was detected by HPLC analysis. Spectral data analyses including UV, ESI-MS and NMR were used to identify their structures. This method is simple, fast, which is suitable for preparation of standard reference of ferulic acid, senkyunolide I and senkyunolide H from L. chuanxiong and can meet the requirement of new drug research and development.
Benzofurans ; chemistry ; isolation & purification ; Chromatography, High Pressure Liquid ; methods ; Coumaric Acids ; chemistry ; isolation & purification ; Ligusticum ; chemistry