Eugenol restrains abdominal aortic aneurysm progression with down-regulations on NF-κB and COX-2.

Abdominal aortic aneurysm (AAA) is a lethal disease without available medicine for treatment. This study aimed to evaluate the efficiency of eugenol (4-allyl-2-methoxyphenol) against AAA and the underlying mechanism. Eugenol is the major bioactive component of clove. A mouse AAA model was established through porcine pancreatic elastase (PPE) incubation peri-adventitially and 1% 3-aminopropanonitrile (BAPN) diet. Continuous AAA progression from day 0 to day 15 was observed after PPE plus BAPN treatment, according to the AAA diameter and histopathological evaluation. Accompanying with AAA progression, sustained increased expressions of CD68, COX-2 and NF-κB were observed through immunofluorescence assay. After elucidation the efficiency of eugenol against AAA progression by AAA diameter, hematoxylin-eosin staining and orcein staining, the down-regulations of eugenol on COX-2 and NF-κB were further detected by immunohistochemistry and western blot. Eugenol not only blocked AAA expansion and protected the integrity of aortic structure in a dose-dependent manner, but also held high oral bioavailability. Excellent efficiency, high oral bioavailability and down-regulation on COX-2/NF-κB endowed eugenol great potential for future AAA therapy.

Cannabisin D from Sinomenium Acutum Inhibits Proliferation and Migration of Glioblastoma Cells through MAPKs Signaling.

Glioblastoma is the most common and malignant tumor in human central nervous system with poor prognosis. From the dried stem of Sinomenium acutum, an herbal medicine, five compounds (sinomenine, syringin, corchoionoside C, protocatechuic acid and cannabisin D) were isolated, characterized and subjected to cytotoxicity screening on U-87 and U-251 glioblastoma cells. Cannabisin D presented effective inhibitory effects on the proliferation and migration of glioblastoma cells. By flow cytometry, real-time PCR and Western blotting, cell apoptosis and cell cycle arrest were proved to contribute to the anti-glioblastoma effects. Further, the activation of MAPKs signaling (p38 MAPK, p42/p44 MAPK and SAPK/JNK) was observed in glioblastoma cells upon cannabisin D treatment by Western blotting, indicating the involvement of MAPKs signaling in the inhibitory effects of cannabisin D. These data suggested that S. acutum is a novel natural source of cannabisin D and cannabisin D is a novel anti-glioblastoma agent candidate.

Characteristics of petroleum-contaminated groundwater during natural attenuation: a case study in northeast China.

The objective of this study was to investigate a petroleum-contaminated groundwater site in northeast China. We determined the physicochemical properties of groundwater that contained total petroleum hydrocarbons (TPH) with a view to developing a scientifically robust strategy for controlling and remediating pollution of groundwater already contaminated with petroleum. Samples were collected at regular intervals and were analyzed for dissolved oxygen (DO), iron (Fe3+), sulfate (SO42-), electrical conductivity (Eh), pH, hydrogen carbonate (HCO3-), and enzyme activities of catalase (CAT), peroxidase (HRP), catechol 1,2-dioxygenase (C12O), and catechol 2,3-dioxygenase (C23O). We used factor analysis in SPSS to determine the main environmental characteristics of the groundwater samples. The results confirmed that the study site was slightly contaminated and that TPH levels were decreasing slightly. Some of the physicochemical variables showed regular fluctuations; DO, Fe3+, and SO42- contents decreased gradually, while the concentrations of one of the microbial degradation products, HCO3-, increased. Microorganism enzyme activities decreased gradually. The microbiological community deteriorated noticeably during the natural attenuation process, so microbiological degradation of pollutants receded gradually. The HCO3- content increased and the pH and Eh decreased gradually. The groundwater environment tended to be reducing.

Development of a UPLC-MS/MS Method for Simultaneous Determination of Six Flavonoids in Rat Plasma after Administration of Maydis stigma Extract and Its Application to a Comparative Pharmacokinetic Study in Normal and Diabetic Rats.

Maydis stigma is an important medicine herb used in many parts of the world for treatment of diabetes mellitus, which main bioactive ingredients are flavonoids. This paper describes for the first time a study on the comparative pharmacokinetics of six active flavonoid ingredients of Maydis stigma in normal and diabetic rats orally administrated with the decoction. Therefore, an efficient and sensitive ultra high performance liquid chromatography coupled to tandem mass spectrometry (UPLC-MS/MS) method for the simultaneous determination of six anti-diabetic ingredients (cynaroside, quercetin, luteolin, isorhamnetin, rutin and formononetin) of Maydis stigma in rat plasma has been developed and validated in plasma samples, which showed good linearity over a wide concentration range (r² > 0.99), and gave a lower limit of quantification of 1.0 ng·mL-1 for the analytes. The intra- and interday assay variability was less than 15% for all analytes. The mean extraction recoveries and matrix effect of analytes and IS from rats plasma were all more than 85.0%. The stability results showed the measured concentration for six analytes at three QC levels deviated within 15.0%. The results indicated that significant differences in the pharmacokinetic parameters of the analytes were observed between the two groups of animals, whereby the absorptions of these analytes in the diabetic group were all significantly higher than those in the normal group, which provides an experimental basis for the role of Maydis stigma in anti-diabetic treatment.

Separation and purification of epigallocatechin-3-gallate (EGCG) from green tea using combined macroporous resin and polyamide column chromatography.

Epigallocatechin-3-gallate (EGCG) is a major bioactive ingredient of green tea that produces beneficial neuroprotective effects. In this paper, to optimize the EGCG enrichment, thirteen macroporous resins with different chemical and physical properties were systemically evaluated. Among the thirteen tested resins, the H-bond resin HPD826 exhibited best adsorption/desorption capabilities and desorption ratio, as well as weakest affinity for caffeine. The absorption of EGCG on the HPD826 resin followed the pseudo-second-order kinetics and Langmuir isotherm model. The separation parameters of EGCG were optimized by dynamic adsorption/desorption experiments with the HPD826 resin column. Under the optimal condition, the content of EGCG in the 30% ethanol eluent increased by 5.8-fold from 7.7% to 44.6%, with the recovery yield of 72.1%. After further purification on a polyamide column, EGCG with 74.8% purity was obtained in the 40-50% ethanol fraction with a recovery rate of 88.4%. In addition, EGCG with 95.1% purity could be easily obtained after one-step crystallization in distilled water. Our study suggests that the combined macroporous resin and polyamide column chromatography is a simple method for large-scale separation and purification of EGCG from natural plants for food and pharmaceutical applications.

A metabonomic analysis of serum from rats treated with ricinine using ultra performance liquid chromatography coupled with mass spectrometry.

A metabonomic approach based on ultra performance liquid chromatography coupled with mass spectrometry (UPLC/MS) was used to study the hepatotoxicity of ricinine in rats. Potential biomarkers of ricinine toxicity and toxicological mechanism were analyzed by serum metabonomic method. The significant differences in the metabolic profiling of the control and treated rats were clear by using the principal components analysis (PCA) of the chromatographic data. Significant changes of metabolite biomarkers like phenylalanine, tryptophan, cholic acid, LPC and PC were detected in the serum. These biochemical changes were related to the metabolic disorders in amino acids and phospholipids. This research indicates that UPLC/MS-based metabonomic analysis of serum samples can be used to predict the hepatotoxicity and further understand the toxicological mechanism induced by ricinine. This work shows that metabonomics method is a valuable tool in drug mechanism study.

Alteration of amino acid neurotransmitters in brain tissues of immature rats treated with realgar.

Realgar is a traditional Chinese medicine, which has been used for thousands of years and are claimed to have therapeutic effects. The toxicity from realgar or realgar-containing traditional medicines has raised public concern. However, the neurotoxicity induced by realgar is less reported. Amino acid neurotransmitters are closely linked to the vulnerability of the immature brain to neuronal injury. The investigation of amino acid neurotransmitters is important to understand the evolution of developmental brain damage. An improved HPLC-UV method was developed and applied to analyzing amino acid neurotransmitters of aspartate, glutamate, glutamine, homocysteine, serine, glycine, γ-aminobutyric acid and taurine in brain tissues of immature rats after the treatment of realgar. Significant changes of these amino acid neurotransmitters were observed in realgar treated groups. Negative correlations were found between the levels of some amino acids and the contents of arsenic in brain tissues. The result indicates that the neurotoxicity induced by realgar is associated with its effects on amino acid neurotransmitters.

LC determination of luteolin-7-O-ß-D-glucoside and apigenin-7-O-ß-D-glucoside in rat plasma after administration of Humulus scandens extract and its application to pharmacokinetic studies.

The present study was to investigate the pharmacokinetics of luteolin-7-O-ß-D-glucoside (LGL) and apigenin-7-O-ß-D-glucoside (AGL) in rat plasma after intravenous administration of the Humulus scandens extract (HSE). A simple and accurate high-performance liquid chromatographic (HPLC) method was successfully developed for simultaneous determination of LGL and AGL in rat plasma after the plasma protein was precipitated with methanol. HPLC analysis was performed on a C18 column with UV detection at 350 nm and a mobile phase of methanol-0.2% phosphoric acid (1 : 1, v/v). Calibration curves of LGL and AGL were linear over the concentration range of 0.16-20.0 and 0.06-7.20 µg mL⁻¹, respectively. The accuracy and precision of the two analytes at low, medium and high concentrations were within the range of -3.4% to 8.1%. The relative standard deviations (RSDs) of the intra- and inter-day precisions were less than 11.7% and 10.0%, respectively. The extraction recoveries (n = 5) varied from 91.9% to 104.1% for LGL and from 92.6% to 109.3% for AGL. The method was fully validated and successfully applied to a pharmacokinetic study of LGL and AGL in rat plasma after the intravenous administration of HSE.