Two undescribed benzopyran derivatives from Ranunculus sceleratus L. with their in vitro anti-inflammatory activity in lipopolysaccharide-activated RAW 264.7 cells.

Previous studies on Ranunculus sceleratus L. have shown the existence of coumarins and their anti-inflammatory effect. Phytochemical work was conducted to investigate the bioactive compounds, leading to the isolation of two undescribed benzopyran derivatives, namely ranunsceleroside A (1) and B (3), together with two known coumarins (2, 4) from the whole plant of R. sceleratus L. All compounds were structurally identified by extensive spectroscopic analysis and then investigated for their inhibitory effect on nitric oxide (NO), tumor necrosis factor-α (TNF-α), interleukin-1ß (IL-1ß) and interleukin-6 (IL-6) production induced by lipopolysaccharide (LPS) in RAW 264.7 murine macrophages, repectively. As a result, compound 1-4 presented inhibitory effects on the production of NO, TNF-α, IL-1ß, and IL-6 in a concentration-dependent manner, which provides a potential chemical basis for the traditional use of R. sceleratus L. as an anti-inflammatory plant.

Borneol, a novel agent that improves central nervous system drug delivery by enhancing blood-brain barrier permeability.

The clinical application of central nervous system (CNS) drugs is limited by their poor bioavailability due to the blood-brain barrier (BBB). Borneol is a naturally occurring compound in a class of 'orifice-opening' agents often used for resuscitative purposes in traditional Chinese medicine. A growing body of evidence confirms that the 'orifice-opening' effect of borneol is principally derived from opening the BBB. Borneol is therefore believed to be an effective adjuvant that can improve drug delivery to the brain. The purpose of this paper is to provide a comprehensive review of information accumulated over the past two decades on borneol's chemical features, sources, toxic and kinetic profiles, enhancing effects on BBB permeability and their putative mechanisms, improvements in CNS drug delivery, and pharmaceutical forms. The BBB-opening effect of borneol is a reversible physiological process characterized by rapid and transient penetration of the BBB and highly specific brain regional distribution. Borneol also protects the structural integrity of the BBB against pathological damage. The enhancement of the BBB permeability is associated with the modulation of multiple ATP-binding cassette transporters, including P-glycoprotein; tight junction proteins; and predominant enhancement of vasodilatory neurotransmitters. Systemic co-administration with borneol improves drug delivery to the brain in a region-, dose- and time-dependent manner. Several pharmaceutical forms of borneol have been developed to improve the kinetic and toxic profiles of co-administered drugs and enhance their delivery to the brain. Borneol is a promising novel agent that deserves further development as a BBB permeation enhancer for CNS drug delivery.

Identification and determination of myriocin in Isaria cicadae and its allies by LTQ-Orbitrap-HRMS.

A hybrid linear ion trap-quadrupole-Orbitrap high-resolution mass spectrometry (LTQ-Orbitrap-HRMS) was used to qualitatively and quantitatively analyse the myriocin in Isaria cicadae and its allies. The samples were prepared with 95% methanol for 30 min by ultrasonic-assisted extraction. The target compound was purified by ODS solid-phase extraction (SPE) column. The enriched samples were identified by mass spectrometry. The results showed that the contents of myriocin in both wild and artificial Isaria cicadae were below the detection limit, while a strain of Ophiocordyceps longissima and Cordyceps cicadae Shing (Dujiaolong), both closely related to the Isaria cicadae, and its asexual mycelia are rich in myriocin. It suggests that it may be wrong to consider C. cicadae as I. cicadae's teleomorph in Genbank or Mycobank in many published reports based on chemical classification, and the species rich in myriocin is probably not Isaria cicadae.

[Study on Appraising Storage Periods of Moutan Cortex and Its Quality by Means of Colorimeter].

Objective: To examine the correlation between storage periods and L*, a* and b* color of Moutan Cortex. Methods: A optical density meter was used for the measurement of reflected light from sieved powder and section samples using the CIE 1976 L~*,a~*,b~* color system. The content of paeonol were determined by HPLC. The correlation between storage periods,paeonol content and color indices of Moutan Cortex was analyzed. Results: The measured color was significantly correlated with storage periods. The color of Moutan Cortex shift toward the red with the increase of storage periods. The storage periods were correlated with paeonol content. The measured color was equably correlated with paeonol content. Conclusion: The correlation between the color of Moutan Cortex and storage periods was found in this study. Measurment of the color of Moutan Cortex can be used to appraise its storage periods and quality.

[Research progress on meridian-guiding theory of traditional Chinese medicine].

Ancient materia medica and medical formularies were consulted to illustrate the development history of meridian-guiding theory of traditional Chinese medicine (TCM). The influences of various meridian-guiding drugs (Achyranthis Bidentatae Radix, borneol, Bupleuri Radix, Platycodon Radix) on the pharmacokinetic and pharmacodynamic characteristics of other drugs were summarized. Meridian-guiding drugs can promote the absorption and targeted distribution of other drugs and enhance the efficacy of injured tissues. The possible mechanisms of meridian-guiding are related with changing the component of cell membrane, inhibiting the efflux of P-gp, opening physiological barriers, modulating the levels of biochemicals, promoting microcirculation and adjusting the pH of targeted tissues. The chemical components of meridian-guiding drugs are the substance basis of meridian-guiding. The aim of exploring meridian-guiding chemicals is to find a natural targeted delivery system. At the present time, some progress has been made in the research on meridian-guiding field. However, further studies are required for the meridian-guiding theory of TCM.

Rapid Fabrication of Gold Nanoflowers Tuned by pH: Insights Into the Growth Mechanism.

We reported a one-pot, no added seeding and green method to synthesize gold nanoflowers, in which HAuC4 and H2O2 were added one by one into the alkaline protocatechuic aldehyde solution at room temperature. Au(III) was partially reduced by protocatechuic aldehyde to produce primary Au nanocrystals, and then Au nanocrystals agglomerated into loose flower-like nanoparticles as seeds, which catalyzed H2O2 reduction of the residual Au(III), thus accelerating the formation of compact 3D gold nanoflowers. The key synthesis strategy was to use protocatechuic aldehyde as a structure-induced agent to influence the growth of gold nanoflowers. The pH value of growth solution could tune the size and/or morphology of gold nanoflowers through its influence on the adhesion force of protocatechuic aldehyde on gold surfaces and the species type of Au(III) complexes. When the pH value of growth solution was above 7.26 (the pKa of protocatechuic aldehyde), the flower-like of gold nanostructural architectures with different sizes could be fabricated. The obtained gold nanoflowers had a large dimension of 198 and 157 nm at the pH of 7.6 and 8, respectively. Size control of gold nanoflowers can be accomplished in the growth solutions of pH 9.4-12.0 with a similar diameter around 60 nm. The as-synthesized gold nanoflowers exhibited good stability and have the prospects for surface-enhanced Raman scattering enhancement.

[Simultaneous determination of eight active components in Chrysanthemum indicum by HPLC].

This study is aimed to establish a high-performance liquid chromatography (HPLC) method for simultaneous determination of chlorogenic acid, caffeic acid, 1,3-dicaffeoylquinic acid, 3,5-dicaffeoylquinic acid, luteolin-7-O-beta-D-glucoside, 3,4-dicaffeoylquinic acid, linarin and luteolin in Chrysanthemum indicum. The separation was carried out on a Shim pack VP-ODS (4.6 mm x 250 mm, 5 microm) column eluting with mobile phases of methanol (A) and water containing 0.3% phosphoric acid (B) in gradient mode (0-9 min, 85% -80% B; 9-12 min, 80% -70% B; 12-15 min, 70% -65% B; 15-20 min, 65% -60% B; 20-23 min, 60% -55% B; 23-29 min, 55% -54.4% B; 29-32 min, 54.4% -45% B; 32-37 min, 45% -5% B; 37-45 min, 5% -85% B) at the flow rate of 1.0 mL x min(-1). The column temperature was 35 degrees C and the detection wavelength was set at 326 nm. The good separation of chlorogenic acid, caffeic acid, 1,3-dicaffeoylquinic acid, 3,5-dicaffeoylquinic acid, luteolin-7-O-beta-D-glucoside, 3,4-dicaffeoylquinic acid, linarin and luteolin was achieved within 40 min. Calibration curves of the eight effective components showed good linear relationship (r > 0.999 5, n = 7). The average recoveries were within 97.03%-102.3% (RSD < 2.0%, n = 6). The method is simple, accurate and repeatable and can be used for the quality control of Ch. indicum.

[Analysis of fingerprint and bioactive components of Bidens biternata by HPLC].

OBJECTIVE: To establish HPLC fingerprint of Bidens biternata from different habitats and determine the contents of hyperoside, isoquercetin, astragalin and bipinnatapolyacetylpside. METHODS: Analysis was carried on Hypersil ODS C18 column (4.6 mm x 250 mm, 5.0 microm) with acetonitrile and 3% acetic acid as the mobile phase in a gradient elution. The contents of 4 components were determined simultaneously. RESULTS: The fingerprint of 10 populations were established and the data were analyzed by the similarity evaluation software. There were almost no differences between the similarities of 10 population, but the contents of 4 main compoerls were different among them. CONCLUSION: This method is stable and reliable which could be applied in quality assessment.

Pharmacokinetics and blood-brain barrier penetration of (+)-catechin and (-)-epicatechin in rats by microdialysis sampling coupled to high-performance liquid chromatography with chemiluminescence detection.

(+)-Catechin (C) and (-)-epicatechin (EC), as the basic monomer units of flavanols, can be widely found in natural products or medicinal herbs. Recent pharmacological studies have revealed that C and EC exhibit good neuroprotective effects. However, there is little information about pharmacokinetic profiles in the brain and in vivo BBB penetration of C and EC. In this paper, an ultrasensitive method using high-performance liquid chromatography (HPLC) with chemiluminescence (CL) detection was developed for the analysis of microdialysis samples. The detection limits for C and EC in Ringer's solution were 1.0 and 1.2 ng/mL, respectively. The intraday and interday accuracies for C and EC in Ringer's solution ranged from -3.0 to 4.4%, and the intraday and interday precisions were below 5.2%. The mean in vivo recoveries of C and EC in microdialysis probes were 33.7% and 26.5% in blood while 38.3% and 29.1% in brain. Pharmacokinetic parameters were estimated using the statistical moment method after iv administration (C and EC, 20 mg/kg of body weight) in rats. Brain-to-blood (AUC(brain)/AUC(blood)) distribution ratios were 0.0726 ± 0.0376 for C and 0.1065 ± 0.0531 for EC, indicating that C and EC could pass through the BBB, which is further evidence of their neuroprotective effects.

A novel on-line gold nanoparticle-catalyzed luminol chemiluminescence detector for high-performance liquid chromatography.

A novel on-line gold nanoparticle-catalyzed luminol-H(2)O(2) chemiluminescence (CL) detector for high-performance liquid chromatography (HPLC) was established, in which gold nanoparticles were produced by the on-line reaction of H(2)O(2), NaHCO(3)-Na(2)CO(3) (buffer solution of luminol), and HAuCl(4). Eight phenolic compounds (gallic acid, protocatechuic acid, protocatechuic aldehyde, 2,5-dihydroxybenzoic acid, caffeic acid, 2,3-dihydroxybenzoic acid, (+)-catechin, and (-)-epicatechin) were chosen as the model compounds. Every separated phenolic compound in the column eluent strongly enhanced the CL signal of on-line gold nanoparticle-catalyzed luminol system. The CL and UV-visible absorption spectra and transmission electron microscopy studies were carried out, and the CL enhancement mechanism was ascribed to that the presence of phenolic compound promoted the on-line formation of 38-nm-diameter gold nanoparticles, which better catalyzed the luminol-H(2)O(2) CL reaction. The effects of methanol and phosphoric acid in the proposed HPLC configuration were performed by two gradient elution programs, and the baseline profile revealed that on-line gold nanoparticle-catalyzed luminol-H(2)O(2) CL detector had better compatibility than 38 nm gold colloids-luminol-H(2)O(2) CL detector. The proposed CL detector exhibits excellent analytical performance with the low detection limit (S/N=3) of 0.53-0.97 ng/mL (10.6-19.4 pg) phenolic compounds, and offers a new strategy for developing on-line nanoparticle-catalyzed CL detector for HPLC with sensitive analysis.

Pharmacokinetics of phenolic compounds of Danshen extract in rat blood and brain by microdialysis sampling.

AIM OF THE STUDY: To evaluate the pharmacokinetics of phenolic compounds after oral administration of Danshen extract in rat brain. MATERIALS AND METHODS: Blood and brain microdialysis probes were inserted into jugular vein and cerebral cortex of rat under anesthesia and perfused with ringer's solution at the rate of 2.0 and 0.8 µL/min, respectively. Blank microdialysates were collected after 2h post-implantation equilibrium time. Danshen extract (danshensu 40 mg/kg BW, protocatechuic aldehyde 149 mg/kg BW, and salvianolic acid B 50mg/kg BW) was administrated intragastrically, and then blood and brain microdialysates were collected at 15 and 30 min time intervals for 4h, respectively. The concentrations of phenolic compounds were determined by high-performance liquid chromatography coupled with chemiluminescence detection. Pharmacokinetic parameters were estimated using non-compartmental methods. RESULTS: Danshensu and protocatechuic acid could be detected in both blood and brain microdialysates, while protocatechuic aldehyde and salvianolic acid B were not detected. Brain-to-blood (AUC(brain)/AUC(blood)) distribution ratio were 0.25±0.04 and 0.09±0.02 for danshensu and protocatechuic acid, respectively. CONCLUSIONS: Danshensu can readily permeate the blood brain barrier after oral administration of Danshen extract, and protocatechuic acid is a potential oxidative metabolite of protocatechuic aldehyde.

Chemiluminescence screening assay for diethylstilbestrol in meat.

A simple, rapid, and sensitive flow injection method with chemiluminescence detection was developed for the screening of meat samples containing diethylstilbestrol, based on the enhancement by diethylstilbestrol of the cerium(IV)-rhodamine 6G chemiluminescence system in sulfuric acid medium. Under the optimal conditions, the chemiluminescence intensity was linear for the diethylstilbestrol concentration in four types of meat (chicken, beef, mutton, and pork) matrix, with the linear ranges of CL detection more than three orders of magnitude and the detection limits (3σ) in the range 0.75-1.12pg/mL. The relative standard deviations for intra-day and inter-day precision were less than 3.0%. The proposed method was found to be highly reliable for screening purpose and successfully applied to the screening of diethylstilbestrol residue in four types of meat samples, with the good quantitative recoveries for the different concentration levels varied from 93.1% to 104.5%. The mechanism of this chemiluminescence reaction has also been proposed.