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Vinegar-baked Radix Bupleuri (VBRB) is usually used to focus other drugs effect on liver in traditional Chinese medicine (TCM). However, no sufficient scientific data are available to support this concept. In this paper, the liver targeting enhancing effect of VBRB on rhein was investigated. 432 of rats were divided into two large groups according to the dose of rhein, low dose group of rhein (LDGR) and high dose group of rhein (HDGR). In each group, the rats were further divided into four subgroups, rhein control and rhein co-administered with three different doses of VBRB peroral. Concentrations of rhein and its metabolite in different tissues were determined by HPLC. Compared to the control group, VBRB significantly increased the distribution of both rhein and its metabolite in liver and meanwhile decreased their distribution in other tissues, indicating a strong liver targeting enhancing effect. This liver targeting effect of VBRB depended on the dose of VBRB and rhein. Low and high dose of VBRB had a more strong effect than medium dose in HDGR; high dose of rhein was more sensitive than low dose of rhein (P <0.05). Rhein existed in two forms after peroral administration in vivo. It was found that the liver targeting effect of VBRB was more remarkable with the native form of rhein compared to its derivative form. The results of this paper demonstrated that co-administration with VBRB is a simple and efficiencient method for liver targeting therapy, and the meridine guide theory of TCM was credible. [Copyright &y& Elsevier]

Abstract: Ethnopharmacological relevance: In Mexico, Opuntia streptacantha is used as part of a traditional medicine in the treatment of diabetes mellitus. Several studies have reported an anti-hyperglycemic effect from the plant, but none have focused on finding a mechanism of action to explain these results. This paper focuses on one of the most recurrent hypotheses for the effect of O. streptacantha: the mechanism of action is the hydrolysis of disaccharides, either by enzymatically inhibiting the alpha glucosidase inhibitors (AGIs) or mechanically acting as a barrier. Materials and methods: To test our hypothesis, three different experiments were performed. A maltose tolerance test was carried out using the total extract (TE) and the juice of the plant. Six different extracts were tested in a free-enzyme assay, four of which were aqueous extracts varying according to the procedure of removing the insoluble particles in an attempt to reduce the loss of the water-soluble compounds. The main component of the total extract, a derivative of (4-hydroxy)-phenyl acetic acid, was also tested. For both the maltose tolerance test and the free-enzyme assay, acarbose was used as a control drug. Finally, an everted small intestine assay was also performed. Results and conclusions: The maltose tolerance test confirmed that an anti-hyperglycemic effect occurs at doses of 100mg/kg TE and 4mL/kg juice. No inhibition on AGIs was observed in the free-enzyme assay, and neither a mechanic nor enzymatic effect on disaccharide hydrolysis was observed in the everted intestine assay. Conclusions: The anti-hyperglycemic effect of O. streptacantha was confirmed, and the results presented here contribute to the understanding that this effect is not due to the action on alpha-glucosidases or related to the intestinal hydrolysis of disaccharides. [Copyright &y& Elsevier]

Abstract: Ethnopharmacological relevance: Persicae Semen (Taoren) and Carthami Flos (Honghua) used in pair which is named as Taoren–Honghua (TH) herb pair has been used in traditional Chinese medicine (TCM) for promoting blood circulation to dissipate blood stasis for many years in China. Aim of the study: This paper investigated the effects of TH and its main components amygdalin and hydroxysafflor yellow A (HSYA) on hemorheological disorders of blood stasis in rats. Materials and methods: Rats were randomly divided into seven groups (control group, model group, TH group, amygdalin group, HSYA group, amygdalin+HSYA group, and aspirin group) with eight animals in each, whose gender was equally distributed throughout groups. All treatments were performed by gavage and administered seven times with an interval of 12h. After the fifth administration, the model rats except those in control group with blood stasis were established by being placed in ice-cold water during the interval between two injections of adrenaline hydrochloride (Adr); and blood samples were collected 30min after the last administration on the following day. Results: TH could significantly decrease whole blood viscosity (WBV), plasma viscosity (PV) and packed cell volume (PCV). It also significantly prolonged thrombin time (TT) and thromboplastin time (APTT), increased prothrombin time (PT) and lowered fibrinogen content (FIB). HSYA which significantly decreased WBV and PV had no effect on plasma coagulation parameters. Amygdalin could significantly decrease PV, prolong APTT and decrease FIB, showing few effects on WBV. TH and its main components amygdalin and HSYA could significantly reduce platelet aggregation and protect vascular endothelial cells. Based on the above results, amygdalin and HSYA were responsible for the main curative effects of TH and usually had synergetic effects, such as decreasing PV and platelet aggregation percentage. Conclusions: The study may provide scientific information to further understanding of the mechanism(s) of TH and its main components in activating blood circulation to dissipate blood. It may also create valuable insight into the possible effects and utilization of TH and its components as a feasible alternative therapeutic agent for patients with hemorheological disorders. [Copyright &y& Elsevier]

Abstract: Schizonepetin, a natural monoterpene from Herba Schizonepetae, is a potential antiviral agent. In this paper, a simple, rapid and sensitive HPLC-UV method was first developed and validated for the determination of schizonepetin in rat plasma and tissue homogenates after oral and intravenous administration. The results showed that schizonepetin was absorbed and eliminated rapidly, and its oral absolute bioavailability in rats achieved about 75%. The drug distributed widely in various tissues of rats, and had no long-term accumulation in vivo. The research provides reliable scientific data for designing drug treatment regimens of schizonepetin. [Copyright &y& Elsevier]

Abstract: Background: Paeonia lactiflora root (baishao in Chinese) is a commonly used herb in TCM. Research has shown baishao to have positive pharmacological actions, including, particularly, anti-inflammatory properties. In this paper we studied the influence of baishao extract on cAMP-phosphodiesterase (PDE) activity and related anti-inflammatory action to identify new pharmacologic action for its clinically widespread use. Methods: PDE activity was calculated by cAMP change examined with HPLC, respiratory burst of neutrophils was detected with method of cytochrome C reduction, elastase release was indicated with the substrate reduction, rat arthritis model was caused by complete Freund''s adjuvant, mouse capillary permeability model was made by acetic acid, and chemical constituents of baishao extract was identified by HPLC, mass spectroscopy and NMR spectrum. Results: Baishao extract had significant inhibition on cAMP-PDE activity (p <0.01), had dose dependent restraint on neutrophils respiratory burst (p <0.001), had inhibition at low concentration and promotion at high concentration on elastase release (p <0.05), and had obvious restraint on local inflammation of animal model (p <0.01). Analysis of HPLC, mass spectroscopy and NMR spectrum showed baishao extract mainly had five components (identified as gallic acid, paeoniflorin sulfonate, albiflorin, paeoniflorin and benzoic acid), among which gallic acid had the largest inhibition on cAMP-PDE activity. Conclusion: The anti-inflammatory effects of baishao may be mediated, at least in part, through its gallic acid content, and this effect may be regulated in part by an inhibition on cAMP-PDE. [Copyright &y& Elsevier]

Abstract: Aim of this study: Corn silk is a traditional herbal medicine in China, which has been used in many parts of the world for the treatment of edema as well as for cystitis, gout, kidney stones, nephritis, prostatitis and similar ailments. However, there is little scientific evidence about its safety. As a part of its safety assessment, a subchronic toxicity was performed in this paper. Methods: The subchronic toxicity was investigated in male and female Wistar rats by dietary administration at concentrations of 0.5%, 2.0% and 8.0% (w/w) for 90 days. Overall health, body weight, food consumption, hematology, blood chemistry, organ weights, gross and microscopic appearance of tissues were compared between test and control groups. Results: A number of significant differences were seen between groups, but none of them was considered to be adverse. Based on the present study, the no-observed-adverse-effect level (NOAEL) of corn silk is at least 8.0% which corresponds to a mean daily corn silk intake of approximately 9.354 and 10.308g/day/kg body weight for males and females, respectively. Conclusion: The results obtained in the present study suggest that consumption of corn silk has no adverse effects and support the safety of corn silk for humans. [Copyright &y& Elsevier]

Abstract: Ethnopharmacological relevance: Swertia chirayita, a medicinal herb endemic to the Tibetan region, is used as a special remedy for liver disorders. The hepatoprotective activity of its plant extracts has been associated with its antioxidant activity. This paper aims to investigate the in vitro and in vivo antioxidant effects of Swertia chirayita extracts (SCE). Materials and methods: Antioxidant ability of Swertia chirayita was investigated by employing several established in vitro methods. In vivo antioxidant activity was tested against CCl4-induced toxicity in mice. The levels and activities of malondialdehyde (MDA) and antioxidant enzymes, including superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH), were then assayed using standard procedures. Results: SCE exhibited strong antioxidant ability in vitro. The liver and kidney of CCl4-intoxicated animals exhibited a significant (p <0.001) decrease in SOD, CAT, and GSH levels. Additionally, these organs exhibited a significant (p <0.001) increase in MDA level. CCl4 did not exhibit toxicity on mice treated with SCE and Vitamin E. The effects of Swertia chirayita (three dosages) were comparable to those of Vitamin E, except in MDA level in the liver and GSH level in the kidney (p <0.05). Conclusion: This study suggests that the ethanolic extract of Swertia chirayita possesses in vitro and in vivo antioxidant effects. This supports the traditional use of Swertia chirayita in Tibetan medicine to cure liver diseases. [Copyright &y& Elsevier]

Abstract: Phlomis umbrosa Turcz has been used as the traditional medicine for thousands of years in China. In this paper, the acetic acid-induced writhing test, the hot plate test, the carrageenan-induced paw edema test, the xylene-induced ear swelling test, and the acetic acid-induced Evans blue leakage and leukocyte infiltration test were used to investigate the antinociceptive and anti-inflammatory activities of the aqueous extract of this plant (25, 50 and 100mg/kg i.p.). Good dose-dependent effects were obtained in most of these tests, except in the hot plate test and the acetic acid-induced Evans blue leakage test. TLC and HPLC analyses showed iridoid glucosides were the main compositions of this extract. These findings suggested that the aqueous extract of P. umbrosa has significant antinociceptive and anti-inflammatory activities. [Copyright &y& Elsevier]

Abstract: Aim of the study: Species of Lychnophora are used in Brazilian folk medicine as analgesic and anti-inflammatory agents. Chlorogenic acid (CGA) and their analogues are important components of polar extracts of these species, as well in several European and Asian medicinal plants. Some of these phenolic compounds display anti-inflammatory effects. In this paper we report the isolation of CGA from Lychnophora salicifolia and its effects on functions involved in neutrophils locomotion. Materials and methods: LC–MS n data confirmed the presence of CGA in the plant. Actions of CGA were investigated on neutrophils obtained from peritoneal cavity of Wistar rats (4h after 1% oyster glycogen solution injection; 10ml), and incubated with vehicle or with 50, 100 or 1000μM CGA in presence of lipopolysaccharide from Escherichia coli (LPS, 5μg/ml). Nitric oxide (NO; Griess reaction); prostaglandin E2 (PGE2), interleukin-1β (IL-1β) and tumor necrosis factor-α [TNF-α; enzyme-linked immunosorbent assay (EIA)]; protein (flow cytometry) and gene (RT-PCR) expression of L-selectin, β2integrin and platelet-endothelial cell adhesion molecule-1 (PECAM-1) were quantified. In vitro neutrophil adhesion to primary culture of microvascular endothelial cell (PMEC) and neutrophil migration in response to formyl-methionil-leucil-phenilalanine (fMLP, 10−8M, Boyden chamber) was determined. Results: CGA treatment did not modify the secretion of inflammatory mediators, but inhibited L-selectin cleavage and reduced β2 integrin, independently from its mRNA synthesis, and reduced membrane PECAM-1 expression; inhibited neutrophil adhesion and neutrophil migration induced by fMLP. Conclusions: Based on these findings, we highlight the direct inhibitory actions of CGA on adhesive and locomotion properties of neutrophils, which may contribute to its anti-inflammatory effects and help to explain the use of Lychnophora salicifolia as an anti-inflammatory agent. [Copyright &y& Elsevier]

Abstract: Ethnopharmacological relevance: Traditional Chinese medicine (TCM) has been used in clinical practice for several thousand years. TCM has played an indispensable role in the prevention and treatment of diseases, especially the complicated and chronic ones. Pharmacokinetic study on active constituents in herbal preparations is a good way for us to explain and predict a variety of events related to the efficacy and toxicity of TCM. Aim of the study: A selective and sensitive HPLC–MS/MS method was first developed and validated for the determination of luteolin, kaempferol, apigenin, quercetol, and isorhamnetin in rat plasma. Materials and methods: The LC system consisted of an Agilent Technologies Series 1200 system (Agilent, USA) equipped with an automatic degasser, a quaternary pump, and an autosampler. Chromatographic separations were performed on a Waters SunFire™ C18 column (150mm×4.6mm, 5μm), and the column temperature was maintained at 25°C and the sample injection volume was 20μL. The current LC–MS/MS assay was validated for linearity, intra-day and inter-day precisions, accuracy, extraction recovery and stability. Results: The validated method was successfully applied to monitoring the concentrations and pharmacokinetic studies of five flavone compounds in rat plasma after a single oral administration of Verbena officinalis L. extract with a dosage of 8.0mL/kg. The time to reach the maximum plasma concentration (T max1) was 0.48±2.14h for luteolin, 0.25±0.13h for kaempferol, 0.97±1.08h for apigenin, 1.04±4.25h for quercetol and 0.25±0.16h for isorhamnetin, and the maximum plasma concentration (T max2) was 3.97±1.48h, 4.05±0.46h, 4.33±0.58h, 2.99±0.48h and 4.02±0.34h. The elimination half-time (t 1/2) of luteolin, kaempferol, apigenin, quercetol and isorhamnetin was 4.02±0.81, 7.65±0.71, 3.30±0.83, 4.55±0.49 and 5.56±1.32h, respectively. Conclusions: This paper described a simple, sensitive and validated LC–MS/MS method for simultaneous determination of luteolin, kaempferol, apigenin, quercetol and isorhamnetin in rat plasma after oral administration of V. officinalis L. extract, and investigated on their pharmacokinetic studies as well, with a short run time of 5min. [Copyright &y& Elsevier]

Abstract: Ethnopharmacological relevance: Jiang-Zhi-Ning (JZN) is composed of four Chinese herbs, i.e., Fleeceflower Root, Fructus Crataegi, Folium Nelumbinis and Semen Cassiae. It was used to strengthen blood circulation of coronary artery, arrhythmia and hyperlipidemia. Aim of the study: The main objective of this paper is to evaluate lipid-lowering and antioxidant activities of extract and effective fraction of JZN by using in vitro experiments on hyperlipidemic rats. Moreover, in vivo experiments on cells were performed to investigate lipid-lowering and antioxidant activities of effective fraction and active constituents of JZN. Materials and method: Wistar rats with high fat diet-induced hyperlipidemia were used as in vitro models to study biological effects of lipid-lowering and antioxidant activities of extract and effective fraction of JZN. Serum total cholesterol (TC), triglyceride (TG), low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), Coronary Index and Atherogenic Index were investigated to evaluate lipid-lowering effects of extract and effective fraction of JZN. Serum total nitric oxide synthase (NOS), nitric oxide (NO), endothelin-1 (ET-1), malondialdehyde (MDA), superoxide dismutase (SOD) and total antioxidant capacity (T-AOC) were detected to measure antioxidant effects of extract and effective fraction of JZN. Furthermore, oxidized low-density lipoprotein (Ox-LDL) injured human umbilical vein endothelial cell (HUVEC) model was employed as in vivo experiment to study lipid-lowering and antioxidant effects of effective fraction and active constituents of JZN. NO, ET-1, MDA SOD and T-AOC in HUVECs or culture media were investigated to evaluate antioxidant activity of effective fraction and active constituents of JZN. Using human hepatoma cell line Bel-7402, reverse transcription polymerase chain reaction (RT-PCR) technology was performed to investigate cholesterol metabolism effects of effective fraction and active constituents of JZN. Expressions of low density lipoprotein receptor (LDL-R), 3-hydroxy-3-methyl-HMG-coenzyme A reductase (HMG-CoAR), and cholesterol 7α-hydroxylase (CYP7A1) mRNA of the liver cells were investigated to evaluate JZN on associated receptor and enzymes of cholesterol metabolism. High-performance liquid chromatography (HPLC) and spectrophotometry were used to study the impact of effective fraction and active constituents of JZN on synthesis and translation of cholesterol during the process of metabolism by measuring inside and extracellular contents of total bile acid (TBA) of Bel-7402. Results: Extract and effective fraction of JZN significantly reduced contents of TC, TG and LDL-C, CRI and AI in hyperlipidemic rats as well as significantly increased contents of HDL-C in the rats. Moreover, they significantly enhanced the activity of NOS and increased contents of NO. They also caused significant reductions in contents of ET-1 and MDA as well as significant increase in SOD activity and T-AOC in the hyperlipidemic rats. Several indicators were found to be concentration-dependent. As far as in vivo experiments to investigate biological activities of effective fraction and active constituents of JZN were concerned, it was found that they restored and enhanced the vitality of HUVECs with a concentration-dependent manner as well as content of NO in the culture media of HUVEC. They caused reductions in the contents of ET-1 in the culture media of HUVEC and contents of MDA in HUVECs. They also caused an increase in the vitality of SOD and T-AOC in HUVECs. Furthermore, they enhanced LDL-RmRNA expression, with a concentration-dependent manner. Low and medium concentrations of effective fraction and active constituents of JZN could inhibit expression of HMG-CoAR mRNA. High concentration counterpart could enhance expression of the HMG-CoAR mRNA. They enhanced expression of CYP7A1 mRNA in a concentration-dependent manner. Finally, they caused reductions in the contents of cholesterol in Bel-7402. They also increased intercellular content of total bile acid as well as lowered extracellular contents of TBA in the cells in a concentration-dependent manner. Conclusion: We demonstrated for the first time lipid-lowering and antioxidant activities of extract and effective fractions as well as active constituents of JZN. Active constituents of JZN had the same biological effects with effective fraction and extract of JZN. Therefore, this study supports its ethnopharmacological use in Traditional Chinese Medicine to manage hyperlipidemia and paves a basis for establishing quality control method of Chinese medicine. [Copyright &y& Elsevier]

Abstract: In this paper, microdialysis combined with ultra performance liquid chromatography/mass spectrometry (UPLC-MS) was applied for the determination of ligustilide in freely moving rats'' brain. The extracellular unbound ligustilide could be detected in rat brain within the first time interval (0–20min) after nasal administration but not after oral administration. This result showed that ligustilide could quickly enter the brain after nasal administration; which implied that ligustilide may have a rapid onset of action. This work demonstrated the potential application of microdialysis combined with UPLC-MS in pharmacokinetic studies. Furthermore, the advantage that fewer animals used in the microdialysis experiment was confirmed. [Copyright &y& Elsevier]

Abstract: Tripterygium Glycosides (TG) is effective in the treatment of patients with a variety of inflammatory and autoimmune diseases, especially rheumatoid arthritis (RA) in clinical. Wilforlide A (T1) serves as a quality control standard of TG that be listed in Drug Standard of Ministry of Public Health of the People''s Republic of China. The pharmacologic actions of T1 remain to be unidentified. In this paper, we studied the anti-inflammatory and immune suppressive effect of T1, and compared it with Triptolide (TP), which believed to be the major active component of TG. Carrageenan-induced rat pedal swelling, tampon-induced rat granulation, and mice ear inhibition rate of swelling trail results show that high-dose T1 has obvious anti-inflammatory effect. Colorimetric detection contents of hemolysin, carbon elimination from plasma of mice, mice delayed hypersensitivity immune, and organ index were measured. The results show that T1 has no significant immune suppressive activity, and there has a significant difference with TP and TG. Therefore, we think the content of TP also should be controlled as a supplement standard in order to ensure safe and effective medication. [Copyright &y& Elsevier]

Aim of the study: This paper aimed to elucidate the traditional use of Rosmarinus officinalis through the investigation of cholinergic activities and neuronal differentiation in rat pheochromocytoma PC12 cells. These effects were examined in relation to the plant''s habitat, the extraction procedure, and the major active compounds of R. officinalis. Materials and methods: Cell viability, cell differentiation, acetylcholinesterase (AChE) activity, total choline, acetylcholine (ACh) and extracellular signal-regulated kinases (ERK1/2) were determined in PC12 cells treated with extracts and HPLC-identified polyphenols of R. officinalis originated from Tunisian semi-arid and subhumid area in comparison with nerve growth factor (NGF). Results: R. officinalis extracts potentiated cell differentiation and significantly enhanced AChE activity in PC12 cells. The highest AChE activity was induced by semi-arid hydro-ethanolic extract (137% of control). Among HPLC-identified and screened polyphenols, carnosic acid (CA) and rosmarinic acid (RA) significantly induced cell differentiation, increased ACh level, and enhanced AChE activity in PC12 cells. U0126, inhibitor of ERK1/2, significantly reduced CA and RA effects on cell differentiation and AChE activity. Conclusions: R. officinalis’ CA and RA exhibited neurotrophic effects in PC12 cells through cell differentiation induction and cholinergic activities enhancement. These effects could be regulated by mitogen-activated protein kinase (MAPK), ERK1/2 signaling pathway. [Copyright &y& Elsevier]