Current Herbal-medicine News Results

Tracing Origins of Complex Pharmaceutical Preparations Using Surface Desorption Atmospheric Pressure Chemical Ionization Mass Spectrometry.

Anal Chem. 2010 Sep 1;
Zhang X, Jia B, Huang K, Hu B, Chen R, Chen H

A novel strategy to trace the origins of commercial pharmaceutical products has been developed based on the direct chemical profiling of the pharmaceutical products by surface desorption atmospheric pressure chemical ionization mass spectrometry (DAPCI-MS). Besides the unambiguous identification of active drug components, various compounds present in the matrixes are simultaneously detected without sample pretreatment, providing valuable information for drug quality control and origin differentiation. Four sources of commercial amoxicillin products made by different manufacturers have been successfully differentiated. This strategy has been extended to secerning six sources of Liuwei Dihuang Teapills, which are herbal medicine preparations with extremely complex matrixes. The photolysis status of chemical drug products and the inferior natural herd medicine products prepared with different processes (e.g., extra heating) were also screened using the method reported here. The limit of detection achieved in the MS/MS experiments was estimated to be 1 ng/g for amoxicillin inside the capsule product. Our experimental data demonstrate that DAPCI-MS is a useful tool for rapid pharmaceutical analysis, showing promising perspectives for tracking the entire pharmaceutical supply chain to prevent counterfeit intrusions.

Anaphylactoid-like reactions in a patient with HyperLp(a)lipidemia undergoing LDL apheresis with dextran sulfate adsorption and herbal therapy with the spice turmeric.

J Clin Apher. 2010 Aug 30;
Adamski J, Jamensky L, Ross J, Siegel DL, Sachais BS

Elevated Lipoprotein (a) (Lp(a)) levels are associated with atherosclerosis and are independent risk factors for coronary artery disease and stroke [Ariyo et al., N Engl J Med 2003;349:2108-2115; Price et al., Atherosclerosis 2001;157:241-249]. Low-density lipoprotein (LDL)-apheresis is the most effective therapy for reducing Lp(a) levels [Parker, Chem Phys Lipids 1994;67-68:331-338; Stefanutti et al., Transfus Apher Sci 2010;42:21-26]. Dextran sulfate-cellulose adsorption (Liposorber(R)) removes both LDL and Lp(a) particles with minimal effect on high-density lipoprotein levels. During the procedure, high levels of bradykinin are generated as the kallikrein-kinin system is activated by contact with the negatively charged dextran-sulfate cellulose [Krieter et al., Artif Organs 2005;29:47-52]. Bradykinin is a potent vasodilator and a substrate of the angiotension converting enzyme (ACE). ACE inhibitors are contraindicated for apheresis procedures because these drugs prevent bradykinin degradation, which causes anaphylatoid reactions characterized by hypotension, bradycardia, dyspnea, and flushing [Owen and Brecher, Transfusion 1994;34:891-894]. Turmeric is a yellow spice that is used as an herbal remedy to treat a myriad of conditions ranging from abdominal pain to pulmonary infections. Scientific investigations of the ethnomedicinal properties of curcumin, the major derivative of turmeric, suggest that this compound has anti-inflammatory, antioxidant, and antineoplastic properties [Lobo et al., J Pharm Pharmacol 2009;61:13-21]. We report a case of a patient undergoing Liposorber(R) therapy for treatment of hyperLp(a)lipidemia who had three episodes of anaphylactoid-like reactions after starting therapy with the spice turmeric. J. Clin. Apheresis, 2010. (c) 2010 Wiley-Liss, Inc.

Imperatorin sustained-release tablets: In Vitro and pharmacokinetic studies.

Arch Pharm Res. 2010 Aug; 33(8): 1209-16
Pan J, Lu W, Li C, Wang S, He L

We prepared and evaluated imperatorin (IMP) sustained-release tablets. IMP is an active compound in Angelica dahuricae, a Chinese herbal medicine. We used different polymers, such as hydroxypropyl methylcellulose (HPMC K4M, K15M, and K100M), carbopol 934P, sodium carboxymethyl cellulose (CMC-Na), and their combinations to prepare the matrix tablets and achieve the desired sustained release profile. The in vitro release profiles of these formulations were examined and fit to various kinetic release models. We also tested the effects of polymer combination ratios on the in vitro release rate. In vivo studies were performed for the optimized formulation in six beagle dogs, and pharmacokinetic parameters were compared with plain IMP tablets. IMP sustained-release tablets exhibited a more sustained plasma concentration than the plain tablets, with a relative bioavailability of 127.25%. The in vitro releases rates and in vivo absorption correlated for the initial 8 hours. These results demonstrate that the sustained-release tablet system can effectively control the release of IMP.

Using Herbal Remedies to Maintain Optimal Weight.

J Nurse Pract. 2010 Feb; 6(2): 153-154
Koithan M, Niemeyer K

Xanthine oxidase inhibitory properties of Czech medicinal plants.

J Ethnopharmacol. 2010 Aug 25;
Havlik J, Huebra RG, Hejtmankova K, Fernandez J, Simonova J, Melich M, Rada V

ETHNOPHARMACOLOGICAL RELEVANCE: The plant species screened within this research were selected based on their use in traditional herbal medicine of Czech Republic and Middle-East Europe region with indications related to rheumatism, arthritis and gout. AIM OF THE STUDY: This study aimed screening of plant extracts from traditionally used Czech medicinal plants for their xanthine oxidase inhibitory properties. MATERIALS AND METHODS: Methylene chloride-methanolic and two ethanolic extracts of 27 plant species were screened for in vitro xanthine oxidase inhibitory activity using a spectrophotometric method. RESULTS: Around 50% of the species exhibited some degree of xanthine oxidase inhibitory properties at 200mug/mL, showing a moderate correlation (r=0.59) with total phenol content. The most active were methylene chloride-methanolic extracts of Populus nigra and Betula pendula, with IC(50) of 8.3 and 25.9mug/mL, respectively, followed by 80% ethanolic extract of Caryophyllus aromaticus and Hypericum perforatum, both under 50mug/mL. CONCLUSIONS: Populus nigra and Betula pendula were identified as species with the highest xanthine oxidase inhibitory potential in our study. This correlates with the ethnobotanical data on their use in Central European folklore and provides the basis for further investigation on these plants.

The neuroprotective effects of Tanshinone IIA on beta-amyloid-induced toxicity in rat cortical neurons.

Neuropharmacology. 2010 Aug 24;
Liu T, Jin H, Sun QR, Xu JH, Hu HT

Oxidative stress caused by amyloid beta-peptide (Abeta) may play an important role in the pathogenesis of Alzheimer disease (AD). Abeta is known to be directly responsible for the production of reactive oxygen species (ROS) and induction of apoptosis. Tanshinone IIA (Tan IIA) is extracted from a traditional herbal medicine Salvia miltiorrhiza BUNGE, which has been shown to protect against oxidative stress and cell death. In this study, we investigated the neuroprotective effect of Tan IIA against Abeta(25-35)-induced cell death in cultured cortical neurons. Exposure of cortical neurons to 30 muM Abeta(25-35) caused a significant viability loss, cell apoptosis and decreased activities of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) as well as increased levels of malondialdehyde (MDA) production. In parallel, Abeta(25-35) significant increased the intracellular ROS elevation and decreased mitochondrial membrane potential (MMP). However, pretreatment of the cells with Tan IIA prior to Abeta(25-35) exposure suppressed these Abeta(25-35)-induced cellular events noticeably. In addition, Tan IIA reduced the Abeta(25-35)-induced increase of caspase-3 activity, and reduced cytochrome c translocation into the cytosol from mitochondria. Furthermore, Tan IIA also ameliorated the Abeta(25-35)-induced Bcl-2/Bax ratio reduction in cortical neurons. Taken together, these data indicate that Tan IIA protected cultured cortical neurons against Abeta(25-35)-induced neurotoxicity through its antioxidative potential. Our results strongly suggest that Tan IIA may be effective in treating AD associated with oxidative stress.

Analysis of marker compounds with anti-platelet aggregation effects in mailuoning injection using platelet binding assay combined with HPLC-DAD-ESI-MS and solid-phase extraction technique.

Phytochem Anal. 2010 Aug 26;
Yu L, Li Y, Fan H, Duan J, Zhu Q, Li S

Introduction - Mailuoning is prepared from a traditional formula of Chinese medicines and widely used as an antithrombotic agent. In this study, the platelet binding assay was used as a novel biospecific separation and analysis method to explore its active constituents, which could be considered as marker compounds for quality control.Objective - To establish a rapid and simple method to predict marker compounds in herbal medicine injection and evaluate the effects of those compounds.Material and methods - Platelets were used to bind and separate constituents. Binding constituents were analysed and taken as potential active compounds for further evaluation. Solid-phase-extraction was adopted to improve sensitivity. HPLC-DAD and ESI-MS were used to determine the binding constituents.Results - Five compounds were extracted through the platelet binding process and identified as neochlorogenic acid, caffeic acid, isochlorogenic acid and their isomers. Caffeic acid was selected for the flow cytometric assay to test its effect on platelets activation, which was determined by CD62P (P-selectin) expression. The results indicated that caffeic acid could significantly inhibit platelet activation while chlorogenic acid did not.Conclusion - Caffeic acid could be considered as a marker compound of Mailuoning injection due to its anti-platelet effect. The study also suggested that platelet binding assay combined with some preconcentration technique could be efficiently used to predict anti-platelet compounds in complicated herbal medicines. Copyright (c) 2010 John Wiley & Sons, Ltd.

Systematic characterisation of secondary metabolites from Ixeris sonchifolia by the combined use of HPLC-TOFMS and HPLC-ITMS.

Phytochem Anal. 2010 Aug 26;
Shi P, Zhang Y, Qu H, Fan X

Introduction - Ixeris sonchifolia (Bunge) Hance, a folk medicine, has been widely used in China for its anti-inflammatory and haemostatic effects. However, the miscellaneous component composition of this herbal medicine is not well known.Objective - To develop a fast and comprehensive analytical method for the characterisation of various components from I. Sonchifolia, as a tool for the quality control of the herb and its related preparations.Methodology - Ixeris sonchifolia samples were extracted with 60% aqueous methanol, purified by solid-phase extraction and then analysed by the combinatorial use of HPLC-TOFMS and HPLC-ITMS.Results - A total of six sesquiterpene lactones, six phenolic acids and seven flavonoids were identified or tentatively characterised. Five of them were reported for the first time in I. sonchifolia and, in particular, two amino acid-sesquiterpene lactone conjugates, 11,13-dihydro-13-prolyl-ixerin Z and 11,13-dihydro-13-prolyl-ixerin Z(1), that were first found in this plant source.Conclusion - A global profile of I. sonchifolia constituents was described, which could be useful for the quality control of this herb and its related preparations. The employed combination of HPLC-TOFMS and HPLC-ITMS could also be a promising tool for the analysis of other herbal medicines containing sesquiterpene lactones, phenolic acids or flavonoids. Copyright (c) 2010 John Wiley & Sons, Ltd.

Inhibitory effects of zingerone, a pungent component of Zingiber officinale Roscoe, on colonic motility in rats.

J Nat Med. 2010 Aug 27;
Iwami M, Shiina T, Hirayama H, Shima T, Takewaki T, Shimizu Y

Ginger (rhizome of Zingiber officinale Roscoe) is an herbal medicine for the treatment of gastrointestinal disorders including constipation and diarrhea. Zingerone is a likely active constituent responsible for the antidiarrheal activity of ginger. The current study was designed to characterize pharmacological actions of zingerone on colonic motility. To evaluate pharmacological effects of zingerone on colonic motility, we used isolated colonic segments from rats, in which mechanical responses were recorded in the longitudinal direction. In addition, we evaluated the effects on colonic motility in vivo by measuring intraluminal pressure changes and expelled fluid volume from the colon in anesthetized rats. Zingerone was applied to the lumen of the colon to allow the drug to access from the mucosal side. Zingerone inhibited spontaneous contractile movements in the isolated colonic segments in a dose-dependent manner. The inhibitory effects of zingerone on colonic movements were not affected by pretreatment with capsazepine, a typical antagonist of transient receptor potential vanilloid 1. In addition, tetrodotoxin, a blocker of voltage-dependent sodium channels on neurons, did not affect the suppression of colonic movements by zingerone, suggesting that zingerone acts on the smooth muscles directly. Zingerone also attenuated colonic motility in vivo without affecting blood pressure and heart rate. The effects were reversible and reproducible. Our findings suggest that zingerone can inhibit colonic motility via direct action on smooth muscles. Zingerone might exert beneficial therapeutic effects on hypermotility-induced diarrhea by abrogating excessive gastrointestinal motility.

Mitochondrial-mediated apoptosis in lymphoma cells by the diterpenoid lactone Andrographolide, the active component of Andrographis paniculata.

Clin Cancer Res. 2010 Aug 26;
Yang S, Evens AM, Prachand S, Singh AT, Bhalla S, David K, Gordon LI

PURPOSE: Andrographolide is a diterpenoid lactone isolated from Andrographis paniculata, an herbal medicine used in Asia. It has anti-inflammatory, antihypertensive, anti-viral and immuno-stimulant properties. Furthermore, it has been shown to inhibit cancer cell proliferation and induce apoptosis in leukemia and solid tumor cell lines. EXPERIMENTAL DESIGN: We studied the Burkitt p53 mutated Ramos cell line, the mantle-cell lymphoma (MCL) line Granta, the follicular lymphoma (FL) cell line HF-1 and the diffuse large B-cell lymphoma (DLBCL) cell line SUDHL4, as well as primary cells from patients with FL, DLBCL, and MCL. RESULTS: We found that andrographolide resulted in dose- and time-dependent cell death as measured by MTT. Andrographolide significantly increased reactive oxygen species (ROS) production in all cell lines. To determine mechanism of cell death, we measured apoptosis by Annexin-V/propidium iodide (PI) in the presence and absence of the antioxidant N-acetyl-L-cysteine (NAC), the glutathione-depleting agent buthionine sulfoxamine (BSO), or caspase inhibitors. We found that apoptosis was greatly enhanced by BSO, blocked by NAC, and accompanied by PARP cleavage and activation of caspases 3, 8 and 9. We measured BAX conformational change, and mitochondrial membrane potential, and using mouse embryonic fibroblast (MEF) Bax/Bak double knockouts (MEFBax-/-/Bak-/-), we found that apoptosis was mediated through mitochondrial pathways, but dependent on caspases in both cell lines and in patient samples. CONCLUSIONS: Andrographolide caused ROS-dependent apoptosis in lymphoma cell lines and in primary tumor samples, which was enhanced by depletion of GSH and inhibited by NAC or the pan-caspase inhibitor Z-VAD-FMK. Further studies of diterpenoid lactones in lymphoma are warranted.

Effects of oral dosage form and storage period on the antioxidant properties of four species used in traditional herbal medicine.

Phytother Res. 2010 Aug 24;
Guimarães R, Barreira JC, Barros L, Carvalho AM, Ferreira IC

Herbal infusions and decoctions in water are some of the most commonly consumed beverages in the world. Although water is not a good solvent for many of the active components in herbs, liquid preparations are rich in several bioactive compounds. Most of them have powerful antioxidant activity and have been related to medicinal herbs' properties. Herein, decoctions and infusions in water of lemon-verbena (Aloysia citrodora) aerial parts and leaves, fennel (Foeniculum vulgare), pennyroyal (Mentha pulegium) and spearmint (Mentha spicata) aerial parts with different periods of storage (0, 30, 60 and 120 days), were prepared. The effects of the method of preparation and storage period on their antioxidant properties were analysed. For all the analysed species, infusions gave better results than the corresponding decoctions. Spearmint infusions showed the highest antioxidant properties, at all the storage periods, probably due to the highest levels and synergy between phenolics, flavonoids and ascorbic acid found in this sample. Linear discriminant analysis confirmed that the length of storage period has a significant influence on the antioxidant activity and antioxidant content. Flavonoids and reducing sugars proved to be the parameters that most highly contributed to cluster individual groups according to different periods of storage. Copyright (c) 2010 John Wiley & Sons, Ltd.

Case reports of adverse effects of herbal medicinal products (HMPs): A quality assessment.

Phytomedicine. 2010 Aug 23;
Hung SK, Hillier S, Ernst E

BACKGROUND: Case reports provide essential information on adverse effects. Yet there is little consistency in the quality and format of reporting them. AIM: In this study, we aimed to assess the quality of case reports of adverse effect of herbal medicinal products (HMPs) published during three time periods, 1986-1988, 1996-1998, and 2006-2008. METHODS: We conducted literature searches in four major databases: Medline, EMBASE, AMED, and CINALH. Each case report was subject to specific inclusion criteria related to the intervention (i.e. herbal medicine) and outcome measurement (i.e. adverse effect). A 21-item scale was used to assess the quality of all included reports. Each report was categorised into low quality (score between 0 and 14), lower medium quality (score between 15 and 21), upper medium quality (score between 22 and 28), and high quality (score between 29 and 42). RESULTS: In total, 137 case reports were included. The percentage of high quality case reports rose from 0% in 1986-1988 to 27.9% in 1996-1998 and 34.2% in 2006-2008; conversely, the percentages of low quality case reports dropped from 13.3% in 1986-1988 to 0% in 1996-1998 and 2.5% in 2006-2008. CONCLUSION: These findings are consistent with the notion that the quality of case reports is improving. However, due to several caveats, our data should be interpreted with caution.

Fingerprinting Analysis of Saposhnikovia divaricata using H Nuclear Magnetic Resonance Spectroscopy and High Performance Liquid Chromatography.

J Integr Plant Biol. 2010 Sep 1; 52(9): 782-92
Xin YY, Deng AJ, Du GH, Zhang JL, Qin HL

The (1)H nuclear magnetic resonance ((1)H NMR) fingerprints of fractionated non-polar and polar extracts (control substance for plant drug [CSPD] A and B) from the roots of 12 specimens of Saposhnikovia divaricata (Turcz.) Schischk were achieved with Fourier Transform (FT)-NMR spectrometer and assigned by comparison to each other and to the (1)H NMR spectra of the isolated individual compounds. These fingerprints were found to be uniform in terms of the specificity for the implication of all 12 specimens being systematically of the same origin. The uniformity was further affirmed by high performance liquid chromatography (HPLC), which also revealed exactly identical specificity for the identified S. divaricata species with the (1)H NMR appearances of corresponding CSPD on the part of the composition of characteristic constituents when comparing to corresponding individual compounds. This investigation unambiguously shows that the specific signals from the chemotaxonomically significant compounds of chromones and coumarins in S. divaricata are exhibited distinctively in the composite features of both (1)H NMR fingerprints and HPLC profiles. The (1)H NMR and HPLC profiles established can successfully be used as reference for the authentication of the origin of S. divaricata species as well as for chemotaxonomic studies.

A randomized, controlled clinical trial on the clinical, microbiological, and staining effects of a novel 0.05% chlorhexidine/herbal extract and a 0.1% chlorhexidine mouthrinse adjunct to periodontal surgery.

J Clin Periodontol. 2010 Aug 25;
Duss C, Lang NP, Cosyn J, Persson GR

Duss C, Lang NP, Cosyn J, Persson GR. A randomized, controlled clinical trial on the clinical, microbiological, and staining effects of a novel 0.05% chlorhexidine/herbal extract and a 0.1% chlorhexidine mouthrinse adjunct to periodontal surgery. J Clin Periodontol 2010; doi: 10.1111/j.1600-051X.2010.01609.x. Abstract Background: Chlorhexidine (CHX) rinsing after periodontal surgery is common. We assessed the clinical and microbiological effects of two CHX concentrations following periodontal surgery. Materials and methods: In a randomized, controlled clinical trial, 45 subjects were assigned to 4 weeks rinsing with a 0.05 CHX/herbal extract combination (test) or a 0.1% CHX solution. Clinical and staining effects were studied. Subgingival bacteria were assessed using the DNA-DNA checkerboard. Statistics included parametric and non-parametric tests (p<0001 to declare significance at 80% power). Results: At weeks 4 and 12, more staining was found in the control group (p<0.05 and p<0.001, respectively). A higher risk for staining was found in the control group (crude OR: 2.3:1, 95% CI: 1.3 to 4.4, p<0.01). The absolute staining reduction in the test group was 21.1% (9 5% CI: 9.4-32.8%). Probing pocket depth (PPD) decreases were significant (p<0.001) in both groups and similar (p=0.92). No rinse group differences in changes of bacterial counts for any species were found between baseline and week 12. Conclusions: The test CHX rinse resulted in less tooth staining. At the study endpoint, similar and high counts of periodontal pathogens were found.

Dichloromethane fraction from Gardenia jasminoides: DNA topoisomerase 1 inhibition and oral cancer cell death induction.

Pharm Biol. 2010 Aug 25;
Lim W, Kim O, Jung J, Ko Y, Ha J, Oh H, Lim H, Kwon H, Kim I, Kim J, Kim M, Kim S, Kim BK, Kim S, Kang BC, Choi H, Kim O

Context: A growing body of evidence shows that compounds of plant origin have the ability to prevent cancer. The fruit of gardenia, Gardenia jasminoides Ellis (Rubiaceae), has long been used as a food additive and herbal medicine, and its pharmacological actions, such as protective activity against oxidative damage, cytotoxic effect, and anti-inflammatory and anti-tumor activity, have already been reported. Objective: The purpose of the present study was to investigate the presence of DNA topoisomerase 1 inhibitor in various solvent fractions of Gardenia extract and examine the induction of oral cancer cell death upon treatment with Gardenia extract. Materials and methods: The methanol extract of Gardenia was partitioned with n-hexane, dichloromethane, ethyl acetate, n-butanol, and water. Results: In the DNA topoisomerase 1 assay, n-hexane and dichloromethane fractions inhibited topoisomerase 1 and led to a decrease in the cell viability of KB cells. The dichloromethane fraction (0.1 mg/mL) also showed 77% inhibition of cell viability in KB cells compared with HaCaT cells. Treatment with dichloromethane fraction led to apoptotic cell death as evidenced by flow cytometric analysis and morphological changes. In addition, treatment with Gardenia extract dichloromethane fraction led to the partial increase of caspase-3, caspase-8 and caspase-9 activities and the cleavage of poly (ADP-ribose) polymerase. Conclusion: Taken together, these results suggest that the dichloromethane fraction from Gardenia extract induces apoptotic cell death by DNA topoisomerase 1 inhibition in KB cells. These findings suggest the possibility that Gardenia extract could be developed as an anticancer modality.

Chemoprevention of a flavonoid fraction from Rhus verniciflua Stokes on aflatoxin B(1)-induced hepatic damage in mice.

J Appl Toxicol. 2010 Aug 24;
Choi KC, Chung WT, Kwon JK, Jang YS, Yu JY, Park SM, Lee JC

Since aflatoxin B(1) (AFB(1))-mediated hepatic damage is related to the production of AFB(1)-8,9-epoxide and reactive oxygen species, bioactive compounds having antioxidant potentials are suggested to be capable of reducing AFB(1)-induced toxicity. We previously purified a mixture of flavonoids that we named RCMF (Rhus verniciflua Stokes chloroform-methanol fraction), from a traditional Korean food additive and herbal medicine. RCMF exhibited various biological effects, including antioxidant and antitumor activities. In this study, we examined whether RCMF protects against AFB(1)-induced liver injury using in vitro and in vivo systems. Pretreatment of HepG2 cells with RCMF significantly reduced AFB(1)-stimulated production of ROS and malondialdehyde (MDA) to the control levels. RCMF also prevented the reduction in HepG2 cell viability caused by AFB(1). Oral administration of RCMF to mice significantly suppressed an AFB(1)-induced increase in serum levels of alanine aminotransferase, alkaline phosphatase and lactate dehydrogenase. It also prevented MDA formation and blocked decreases in glutathione levels and superoxide dismutase activities in the livers of AFB(1)-treated mice. In addition, RCMF supplementation prevented an AFB(1)-induced decrease in serum titers of IgA and IgG1. Collectively, these results suggest that RCMF attenuates AFB(1)-mediated damage to the liver, and that this effect is at least partially related to the restoration of antioxidant defense systems and an increase in AFB(1)-GSH conjugate formation. Copyright (c) 2010 John Wiley & Sons, Ltd.

The Chinese Herbal Medicine Sophora Flavescens Activates Pregnane X Receptor.

Drug Metab Dispos. 2010 Aug 24;
Wang L, Li F, Lu J, Li G, Li D, Zhong XB, Guo GL, Ma X

Sophora flavescens (SF) is an herbal medicine widely used for the treatment of viral hepatitis, cancer, viral myocarditis, gastrointestinal hemorrhage and skin diseases. It was recently reported that SF upregulates cytochrome P450 3A (CYP3A) expression. The mechanism of SF-induced CYP3A expression is unknown. In the current study, we tested the hypothesis that SF-induced CYP3A expression is mediated by the activation of pregnane X receptor (PXR). We used two cell lines, DPX2 and HepaRG, to investigate the role of PXR in SF-induced CYP3A expression. The DPX2 cell line is derived from HepG2 cells with the stable transfection of human PXR and a luciferase reporter gene linked with a human PXR response element identified in the CYP3A4 gene promoter. In DPX2 cells, SF activated PXR in a concentration-dependent manner. We used a metabolomic approach to identify the chemical constituents in SF, which were further analyzed for their effect on PXR activation and CYP3A regulation. One chemical in SF, N-methylcytisine, was identified as an individual chemical that activated PXR. HepaRG is a highly differentiated hepatoma cell line that mimics human hepatocytes. In HepaRG cells, N-methylcytisine significantly induced CYP3A4 expression, and this induction was suppressed by the PXR antagonist sulforaphane. These results suggest that SF induces CYP3A expression via the activation of PXR.

Analysis of Biliary Excretion of Icariin in Rats.

J Agric Food Chem. 2010 Aug 24;
Wu YT, Lin CW, Lin LC, Chiu AW, Chen KK, Tsai TH

Icariin is a bioactive herbal ingredient isolated from Epimedii Herba. This study evaluates the distribution of icariin in rats by microdialysis sampling and high-performance liquid chromatography with ultraviolet detection (HPLC-UV). Microdialysis probes were simultaneously placed in the jugular vein, brain striatum, and bile duct of each anesthetized rat for sampling after the administration of icariin (dose = 10 or 20 mg/kg) via the femoral vein. The role of P-glycoprotein (P-gp) on icariin distribution was assessed by pretreatment with cyclosporine (CsA, dose = 20 mg/kg). This study is the first report of the biliary excretion of icarin in rats, defined as the blood-to-bile distribution (k value), calculated by dividing the area under the concentration-time curve (AUC) of icariin in bile by that in blood (k = AUC(bile)/AUC(blood)). The k values were 19.0 +/- 5.9 and 18.8 +/- 3.8 at the doses of 10 and 20 mg/kg, respectively. The decreased biliary excretion of icariin due to pretreatment with CsA was evidenced by the reduced k values (18.8 +/- 3.8 vs 9.9 +/- 1.9, p = 0.005). This work demonstrates that biliary excretion is the major elimination pathway for icariin disposition and that transporters, such as P-gp, might be related to icariin's biliary excretion.

Self-reported competence of Estonian community pharmacists in relation to herbal products: findings from a health-system in transition.

Phytother Res. 2010 Aug 23;
Volmer D, Lilja J, Hamilton D, Bell JS, Veski P

Recent health-system reforms in Estonia have resulted in an increased emphasis on primary health care and evidence-based medicine. Community pharmacies are the primary source of herbal products, and pharmacists have an important role in ensuring the safe and effective use of herbal products. The objective of this study was to explore the self-reported competence of pharmacists and the self-reported provision of community pharmacy services in relation to herbal products. A survey instrument was mailed to a random sample of 154 (50%) community pharmacies in Estonia in February 2005. Responses were received from 114 pharmacists and six assistant pharmacists (response rate 77.9%). Among the respondents, 64.1% self-evaluated their knowledge of herbal products as good or excellent. However, only 35.0% reported they experienced no problems in counselling about herbal products, while only 35.8% recognized the importance of continuing education. Pharmacists attached a high level of importance to providing information about herbal products' mode of action, administration, potential side-effects and interactions. There was an apparent mismatch between pharmacists' self-reported competence and their self-reported provision of advice about herbal products. Health system reforms in Estonia may need to be accompanied by enhanced training for pharmacists to provide advice about the safe and appropriate use of herbal products. Copyright (c) 2010 John Wiley & Sons, Ltd.

Echinacea and trypanasomatid parasite interactions: growth-inhibitory and anti-inflammatory effects of Echinacea.

Pharm Biol. 2010 Sep; 48(9): 1047-52
Canlas J, Hudson JB, Sharma M, Nandan D

CONTEXT/OBJECTIVE: Herbal preparations derived from various species and parts of Echinacea (Asteraceae) have been advocated for various medical applications, as a result of the many antimicrobial and immunomodulatory activities attributed to them. MATERIALS AND METHODS: In order to investigate their effects on parasites, four preparations of Echinacea, with distinct chemical compositions, were evaluated for growth inhibition of three species of trypanosomatids: Leishmania donovani, Leishmania major, and Trypanosoma brucei. In addition one Echinacea preparation was tested for anti-inflammatory activity in cell culture models designed to measure pro-inflammatory cytokines induced by L. donovani. RESULTS AND DISCUSSION: All Echinacea preparations inhibited growth of the organisms, though with different relative potencies, and in some cases morphological changes were observed. However, there was no obvious correlation with the composition of the marker compounds, alkylamides, caffeic acid derivatives, and polysaccharides. L. donovani stimulated the production of the pro-inflammatory cytokines IL-6 and IL-8 in human bronchial epithelial cells and in human skin fibroblasts, but in both cases the standardized ethanol extract of E. purpurea (L.) Moench (Echinaforce) abolished the stimulation, indicating anti-inflammatory activity of this extract. CONCLUSIONS: Thus various Echinacea extracts can inhibit the proliferation of these parasites and at least one can reverse the pro-inflammatory activity of Leishmania donovani.