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Background: Echinococcosis, coenurosis and cysticercosis are debilitating diseases which prevail in China. Immunological diagnosis of metacestodosis is important in disease control. The 8-kDa glycoproteins from taeniid cestodes have successfully been used for diagnosis of human cysticercosis in immunological assays. The aim of the present study was to investigate genetic variations and phylogenetic relationships of the 8-kDa proteins for evaluating the possibility of utilizing these proteins as diagnostic antigens for other metacestode infections., Methods: The genes and complementary DNAs (cDNAs) encoding the 8-kDa proteins from Echinococcus (E.) granulosus, Taenia (T.) multiceps and T. hydatigena were amplified using PCR method. Their amplicons were cloned into the vector pMD18 and the positive clones were sequenced. Sequence data were analyzed with the SeqMan program, and sequence homology searches were performed using the BLAST program. Alignments were conducted using the ClustalX program, and the phylogenetic analyses were performed with the Protein Sequences Program and the Puzzle Program using the Neighbor-joining method., Results: Fifteen, 18 and 22 different genomic DNA sequences were identified as members of the 8-kDa protein gene family from E. granulosus, T. multiceps and T. hydatigena, respectively. Eight, four and six different cDNA clones respectively from E. granulosus, T. multiceps and T. hydatigena were characterized. Analysis of these sequences revealed 54 unique 8-kDa protein sequences. Phylogenetic trees demonstrated that the taeniid 8-kDa proteins are clustered into eight clades at least: Ts18, Ts14, TsRS1, TsRS2, T8kDa-1, T8kDa-2, T8kDa-3 and T8kDa-4., Conclusion: We found that the gene family encoding for the taeniid 8-kDa antigens is comprised of many members with high diversity, which will provide molecular evidence for cross-reaction or specific reaction among metacestode infections and may contribute to the development of promising immunological methods for diagnosis of metacestodosis.

Objective: To define the normative data of gastroesophageal reflux (GER) and laryngopharyngeal reflux (LPR) in healthy Chinese volunteers., Methods: Healthy volunteers without gastrointestinal and throat disease and symptoms were enrolled and underwent 24-hour impedance-pH monitoring., Results: A total of 37 healthy volunteers completed all the tests (female 54.1%; age 38.0±15.2 years). Of 1862 GER, 49.6% were mixed, 40.9% were liquid and 9.5% were gas. More than half (54.9%) were acid. The median and 95th percentile numbers of GER were 52 and 71, respectively. The number of LPR was eight, of which two were mixed and the others were liquid. Only one episode of reflux was classified as acid LPR. The median and 95th percentile numbers of LPR were 0 and 2, respectively. More liquid reflux were associated with LPR (P=0.02). Age had no influence on GER and LPR reflux profiles., Conclusions: Few LPR occurred in healthy Chinese volunteers and they were rarely acid when they reached the larynx. LPR was mostly associated with liquid reflux., (© 2011 The Authors. Journal of Digestive Diseases © 2011 Chinese Medical Association Shanghai Branch, Chinese Society of Gastroenterology, Renji Hospital Affiliated to Shanghai Jiaotong University School of Medicine and Blackwell Publishing Asia Pty Ltd.)

In the title compound, C(30)H(38)O(4)S(2), the centroid of the benzene ring lies on a center of inversion. The thio-phene ring is aligned at 49.8 (1)° with respect to the benzene ring. The alkyl chain adopts an extended zigzag conformation.

A fluorescent and colorimetric receptor (L) for specific recognition of TNP was described. The origins of this remarkable affinity was disclosed by the crystal structure of corresponding host-guest complex L·TNP., (© The Royal Society of Chemistry 2011)

Six new homodinuclear lanthanide(III) complexes with a flexible tripodal carboxylate ligand (H(3)L), of formulae [Ln(2)L(2)(DMF)(4)]·4DMF (Ln = La (1), Nd (2), Eu (3), Gd (4), Tb (5), Dy (6), DMF = N, N-Dimethylformamide) have been synthesized. Among them, 1, 2, 3, 4, 6 were characterized by single-crystal X-ray diffraction, which crystallized in the monoclinic space group P2(1)/n with a = 13.309(2) Å, b = 27.404(4) Å, c = 16.686(3) Å, β = 105.115(2) and V = 5875.2(17) Å(3) for 1, a = 13.3016(5) Å, b = 27.1952(12) Å, c = 16.6339(7) Å, β = 105.030(2) and V = 5811.3(4) Å(3) for 2, a = 13.2797(10) Å, b = 27.072(2) Å, c = 16.6564(13) Å, β = 104.9390(10) and V = 5785.7(8) Å(3) for 3, a = 13.2855(3) Å, b = 27.0074(6) Å, c = 16.6357(3) Å, β = 104.9790(10) and V = 5766.2(2) Å(3) for 4, a = 13.2837(5) Å, b = 26.9105(10) Å, c = 16.6066(6) Å, β = 104.917(2) and V = 5736.3(4) Å(3) for 6. The crystal structures reveal that these complexes are isostructural, and molecules are connected from 0D to 3D supramolecular structures by hydrogen bonds. All of them were characterized by elemental analysis, IR spectroscopy, XRD and TGA. Unusually, non-luminescent Tb(III) complex was obtained. The photophysical property of the Eu(III) complex and the magnetic property of Gd(III) complex are investigated and discussed in detail.

Conflicting data exist as to whether meclizine is an activator of human pregnane X receptor (hPXR). Therefore, we conducted a detailed, systematic investigation to determine whether meclizine affects hPXR activity by performing a cell-based reporter gene assay, a time-resolved fluorescence resonance energy transfer competitive ligand-binding assay, a mammalian two-hybrid assay to assess coactivator recruitment, and a hPXR target gene expression assay. In pregnane X receptor (PXR)-transfected HepG2 cells, meclizine activated hPXR to a greater extent than rat PXR. It bound to hPXR ligand-binding domain and recruited steroid receptor coactivator-1 to the receptor. Consistent with its hPXR agonism, meclizine increased hPXR target gene expression (CYP3A4) in human hepatocytes. However, it did not increase but decreased testosterone 6β-hydroxylation, suggesting inhibition of CYP3A catalytic activity. Meclizine has also been reported to be an inverse agonist and antagonist of human constitutive androstane receptor (hCAR). Therefore, given that certain tissues (e.g., liver) express both hPXR and hCAR and that various genes are cross-regulated by them, we quantified the expression of a hCAR- and hPXR-regulated gene (CYP2B6) in cultured human hepatocytes treated with meclizine. This drug did not decrease constitutive CYP2B6 mRNA expression or attenuate hCAR agonist-mediated increase in CYP2B6 mRNA and CYP2B6-catalyzed bupropion hydroxylation levels. These observations reflect hPXR agonism and the lack of hCAR inverse agonism and antagonism by meclizine, which were assessed by a hCAR reporter gene assay and mammalian two-hybrid assay. In conclusion, meclizine is a hPXR agonist, and it does not act as a hCAR inverse agonist or antagonist in cultured human hepatocytes.

Objectives: To determine the prevalence and symptom pattern of pathologic esophageal acid reflux (PEAR) in patients with functional dyspepsia (FD) using the Rome III criteria, and to explore the value of a proton pump inhibitor (PPI) test in distinguishing the patients with and those without PEAR among FD patients., Methods: Consecutive FD patients who fulfilled the Rome III criteria without predominant typical reflux symptoms (i.e., heartburn or regurgitation) were enrolled. All patients underwent upper endoscopy and an ambulatory 24-h pH monitoring. PEAR was defined as the percentage total time for which a pH value <4 was >4.2% in the distal esophagus. Then, patients were treated with rabeprazole 10 mg twice daily for 28 days. The symptom scores were measured by the frequency score multiplied by the severity scores of the predominant symptom before and at the end of the treatment, and the "PPI test" was defined as positive if the overall scores of the predominant dyspeptic symptom in the fourth week decreased by >50% compared with those of the baseline., Results: One hundred eighty-six FD patients were enrolled, with predominant symptoms of epigastric pain (n=68), epigastric burning (n=47), bothersome postprandial fullness (n=54), and early satiation (n=17). The prevalence of PEAR was 31.7%, with the highest percentage (48.9%) in patients with epigastric burning as their predominant symptom. The prevalence of PEAR in patients with postprandial distress syndrome (PDS) and epigastric pain syndrome (EPS) were 36.6% (26/71) and 28.7% (33/115), respectively. Overall, 63.4% were positive for the "PPI test"; the rates were 51.5, 85.0, 66.7, and 41.1% in patients with epigastric pain, epigastric burning, bothersome postprandial fullness, and early satiation as their predominant symptoms, respectively (χ(2)=17.59, P=0.001). The positive rates were 65.5 and 60.6% in patients with PDS and EPS, respectively (χ(2)=0.41, P=0.522). The sensitivity and specificity of the "PPI test" in distinguishing FD patients with PEAR was 83.1 and 45.7%, respectively., Conclusions: PEAR is present in almost one third of FD patients; the prevalence is ∼50% in those with epigastric burning. The "PPI test" has a limited value in distinguishing the FD patients with and those without PEAR.

Ginkgo biloba extract activates pregnane X receptor (PXR), but how this occurs is not known. Therefore, we investigated the mechanism of PXR activation by the extract and the role of five individual terpene trilactones in the activation. In a cell-based reporter gene assay, G. biloba extract activated human PXR (hPXR), and at a concentration present in the extract, ginkgolide A, but not ginkgolide B, ginkgolide C, ginkgolide J, or bilobalide was partially responsible for the increase in hPXR activity of the extract. Likewise, in cultured human hepatocytes, only ginkgolide A contributed to the increase in hPXR target gene expression (CYP3A4 mRNA and CYP3A-mediated testosterone 6β-hydroxylation). The extract, but none of the terpene trilactones, bound to hPXR ligand-binding domain, as analyzed by a time-resolved fluorescence resonance energy transfer competitive binding assay. Only the extract and ginkgolide A recruited steroid receptor coactivator-1, as determined by a mammalian two-hybrid assay. Compared with hPXR, rat PXR (rPXR) was activated to a lesser extent by G. biloba extract. Similar to hPXR, only ginkgolide A contributed to rPXR activation by the extract. In contrast to the effect of G. biloba extract on PXR function, it did not affect hPXR expression. Overall, the main conclusions are that G. biloba extract is an hPXR agonist, and among the five terpene trilactones investigated, only ginkgolide A contributes to the actions of the extract. Our findings provide insights into the biological and chemical mechanisms of hPXR activation by G. biloba extract.

Five new rare earth complexes with a new flexible tripodal salicylic ligand (H(3)L), 2,2'-(2-((2-carboxyphenoxy)methyl)-2-(4-methylphenylsulfonamido)propane-1,3-diyl)bis(oxy)dibenzoic acid, of formulae [La(2)L(2)(DMF)(4)]·4DMF·4EtOH·2H(2)O (1), [Eu(2)L(2)(DMF)(4)]·2DMF (2), {[GdL(DMF)(H(2)O)(2)]·DMF}(∞) (3), {[TbL(DMF)(H(2)O)(2)]·DMF}(∞) (4) and {[YL(DMF)(H(2)O)(2)]·DMF}(∞) (5) (DMF = N,N-dimethylformamide) have been prepared. The single-crystal X-ray diffraction analysis revealed that complexes 1 and 2 present a cage-like homodinuclear species, while 3-5 show a helical one-dimensional coordination polymer. All these complexes are further connected by hydrogen bonds or π-π interactions, resulting in 3D supramolecular structures. The photophysical properties of the Eu and Tb complexes are investigated in the solid state at room temperature.

Objectives: We sought to investigate the prevalence of clinically significant endoscopic findings (CSEFs) in Chinese patients presenting with uninvestigated typical reflux symptoms in the absence of alarm symptoms, and to evaluate whether prompt endoscopy is an appropriate initial management in these patients., Methods: Consecutive patients presenting with uninvestigated typical reflux symptoms (i.e., heartburn or acid regurgitation) as chief complaints were recruited for symptom evaluation and upper endoscopy, followed by a 2-week proton pump inhibitor (PPI) therapy., Results: Of 469 patients recruited, CSEFs were observed in 180 (38.4%): 154 (32.8%) with erosive esophagitis (EE), 18 (3.8%) with Barrett's esophagus (BE), 24 (5.1%) with peptic ulcer disease (PUD), and 4 (0.9%) with carcinomas (1 esophageal carcinoma and 3 gastric adenocarcinomas). Multivariate analysis identified that an age >50 years (odds ratio (OR)=1.94, P=0.008), male gender (OR=4.11, P<0.001), being overweight or obese (OR=2.99, P<0.001), and alcohol use (OR=9.96, P<0.001) were independent risk factors for EE; an age >50 years (OR=4.61, P=0.003) and alcohol use (OR=5.50, P=0.003) were independent risk factors for BE; and Helicobacter pylori infection (OR=8.52, P<0.001) and alcohol use (OR=4.08, P=0.004) were independent risk factors for PUD. Symptom evaluation and response to PPI treatment were not correlated with EE, BE, and PUD in these patients., Conclusions: CSEFs other than gastroesophageal reflux disease are present in a considerable proportion of Chinese patients with uninvestigated typical reflux symptoms but without alarm features. Symptom evaluation is of limited practical value, and thus prompt endoscopy seems to be an appropriate initial management option in these patients.

The mol-ecule of the title compound, C(30)H(24)N(2)O(2)S(4), adopts a Z-shaped conformation. The terminal benzothia-zole ring systems are oriented at a dihedral angle of 60.81 (8)°, while the central benzene rings are twisted to each other by a dihedral angle of 13.56 (14)°. Weak inter-molecular C-H⋯π inter-actions are present in the crystal structure.

Background: The relationship between symptom elimination and normalization of esophageal acid level of gastroesophageal reflux disease (GERD) on proton-pump inhibitor (PPI) therapy has been questioned. This study aimed to evaluate the relationship between symptom response and gastro-esophageal acidity control in Chinese patients with GERD on esomeprazole therapy, and to assess the role of 24-hour esophageal pH-metry after therapy in GERD patients., Methods: GERD patients with typical reflux symptoms were enrolled and received esomeprazole 40 mg once daily for 4 weeks. Patients with positive baseline 24-hour esophageal pH-metry were divided into two groups depending on an additional dual-channel 24-hour pH-metry after treatment. The pH- group achieved normalization of esophageal pH level whereas the pH+ group did not., Results: Of the 80 patients studied, 76 had abnormal baseline esophageal pH levels. Of these, 90% (52/58) of symptom-free patients and 67% (12/18) of symptom-persistent patients achieved esophageal pH normalization after therapy (P = 0.030). The mean post-therapy gastric nocturnal percent time of pH < 4.0 was significantly higher in pH+ group than that in pH- group (P < 0.001) after therapy. The multivariate regression analysis identified hiatus hernia (P < 0.001) and persistent reflux symptom (P = 0.004) were two independent factors predicting the low post-therapy esophageal pH level., Conclusions: Symptom elimination is not always accompanied by esophageal pH normalization, and vice verse. Esophageal pH-metry is recommended for GERD patients with hiatus hernia or with persistent reflux symptoms after PPI therapy.

Background: Mitochondrial genomes provide a rich source of molecular variation of proven and widespread utility in molecular ecology, population genetics and evolutionary biology. The tapeworm genus Taenia includes a diversity of tapeworm parasites of significant human and veterinary importance. Here we add complete sequences of the mt genomes of T. multiceps, T. hydatigena and T. pisiformis, to a data set of 4 published mtDNAs in the same genus. Seven complete mt genomes of Taenia species are used to compare and contrast variation within and between genomes in the genus, to estimate a phylogeny for the genus, and to develop novel molecular markers as part of an extended mitochondrial toolkit., Results: The complete circular mtDNAs of T. multiceps, T. hydatigena and T. pisiformis were 13,693, 13,492 and 13,387 bp in size respectively, comprising the usual complement of flatworm genes. Start and stop codons of protein coding genes included those found commonly amongst other platyhelminth mt genomes, but the much rarer initiation codon GTT was inferred for the gene atp6 in T. pisiformis. Phylogenetic analysis of mtDNAs offered novel estimates of the interrelationships of Taenia. Sliding window analyses showed nad6, nad5, atp6, nad3 and nad2 are amongst the most variable of genes per unit length, with the highest peaks in nucleotide diversity found in nad5. New primer pairs capable of amplifying fragments of variable DNA in nad1, rrnS and nad5 genes were designed in silico and tested as possible alternatives to existing mitochondrial markers for Taenia., Conclusions: With the availability of complete mtDNAs of 7 Taenia species, we have shown that analysis of amino acids provides a robust estimate of phylogeny for the genus that differs markedly from morphological estimates or those using partial genes; with implications for understanding the evolutionary radiation of important Taenia. Full alignment of the nucleotides of Taenia mtDNAs and sliding window analysis suggests numerous alternative gene regions are likely to capture greater nucleotide variation than those currently pursued as molecular markers. New PCR primers developed from a comparative mitogenomic analysis of Taenia species, extend the use of mitochondrial markers for molecular ecology, population genetics and diagnostics.

Ardisia elliptica Thunberg (Myrsinaceae) is a medicinal plant traditionally used for alleviating chest pains, treatment of fever, diarrhoea, liver poisoning and parturition complications. The objectives of the study were to investigate the effect of A. elliptica on collagen induced platelet aggregation and to isolate and purify potential antiplatelet components. Fresh A. elliptica leaves were extracted using methanol (70% v/v) by Soxhlet extraction and the extract was analysed for its inhibition of collagen-induced platelet aggregation. Inhibition of platelet aggregation was assessed by incubating the extracts with rabbit blood and collagen in a whole blood aggregometer and measuring the impedance. The leaf extract was found to inhibit platelet aggregation with an IC50 value of 167 microg/ml. Using bioassay guided fractionation, beta-amyrin was isolated and purified. The IC50 value of beta-amyrin was found to be 4.5 microg/ml (10.5 microM) while that of aspirin was found to be 11 microg/ml (62.7 microM), indicating that beta-amyrin was six times as active as aspirin in inhibiting platelet aggregation. This paper is the first report that beta-amyrin isolated from A. elliptica is more potent than aspirin in inhibiting collagen-induced platelet aggregation. In conclusion, A. elliptica leaves were found to inhibit collagen-induced platelet aggregation and one of the bioactive components responsible for the observed effect was determined to be beta-amyrin.

Danggui Buxue Tang (DBT), a herbal decoction composed of Radix Astragali (RA) and Radix Angelica sinensis (RAS), has been used for treating menopausal irregularity in women for more than 800 years in China. According to the old tradition, RAS had to be processed with yellow wine before DBT preparation, which markedly reduced the amount of ligustilide in RAS and DBT, as well as enhanced the bioactivities of DBT. Here, we hypothesized that ligustilide would be an ingredient that possessed suppressive effects on DBT's functions. In the presence of ligustilide, the amount of astragaloside IV, calycosin, formononetin, and total polysaccharides extracted from RA were decreased. An increase of ligustilide caused a decrease of DBT's osteogenic activity in stimulating proliferation and differentiation of cultured bone cells. In addition, in the presence of a high level of ligustilide, DBT caused a side effect inducing the proliferation of breast MCF-7 cells. The current results strongly suggest that ligustilide is a negative regulator that hinders DBT to achieve its biological efficacy, which supports the traditional practice of preparing DBT using the ethanol-treated RAS., ((c) Georg Thieme Verlag KG Stuttgart . New York.)

In the binuclear title complex, [Ag(2)(C(31)H(22)N(4)O)(2)](ClO(4))(2)·2C(3)H(7)NO, the Ag(I) atom is penta-coordinated by three N atoms from the tridentate chelating terpyridyl group and by one N atom and one O atom from the quinolin-8-yl-oxy group in a distorted square-pyramidal geometry with the O atom at the apical position. The centrosymmetric complex cation involves intra-molecular π-π stacking inter-actions [centroid-centroid distance = 3.862 (4) Å] between the central pyridine and benzene rings. In the crystal structure, inter-molecular C-H⋯O hydrogen bonds result in the formation of a supra-molecular network.

Mo and W MonoAryloxide-Pyrrolide (MAP) olefin metathesis catalysts can couple terminal olefins to give as high as >98% Z-products in moderate to high yields with as little as 0.2% catalyst. Results are reported for 1-hexene, 1-octene, allylbenzene, allyltrimethylsilane, methyl-10-undecenoate, methyl-9-decenoate, allylB(pinacolate), allylOBenzyl, allylNHTosyl, and allylNHPh. It is proposed that high Z-selectivity is achieved because a large aryloxide only allows metallacyclobutanes to form that contain adjacent cis substituents and because isomerization of Z-product to E-product can be slow in that same steric environment.

Ethnopharmacological Significance: Panax notoginseng (Burk.) F. H. Chen (Araliacea) is traditionally used for its hemostatic and cardiovascular effects when raw and as a tonic when steamed., Aim of the Study: This study aims to compare the effects of raw and steamed Panax notoginseng, Panax ginseng C. A. Meyer and Panax quinquefolium Linn. on platelet aggregation and plasma coagulation., Materials and Methods: Effects on collagen-induced platelet aggregation were investigated using a platelet aggregometer, while the plasma coagulation times (prothrombin time, activated partial thromboplastin time and thrombin time) were determined using a blood coagulation analyzer. The data was corroborated with ex vivo platelet aggregation and in vivo rat bleeding time., Results: Raw and steamed Panax notoginseng significantly inhibit platelet aggregation and plasma coagulation. Steamed Panax notoginseng has significantly more potent antiplatelet and anticoagulant effects than the raw extract, and the antiplatelet and anticoagulant effects increase with increasing steaming durations. Comparing the three common Panax species, Panax notoginseng has higher antiplatelet effect than Panax ginseng and Panax quinquefolium. The in vitro antiplatelet and anticoagulant effects are positively translated into a prolongation of in vivo rat bleeding time after oral administration of the raw and steamed extracts., Conclusion: The results indicate that the three common Panax species affect platelet aggregation and plasma coagulation differently, with steamed Panax notoginseng showing the greatest antiplatelet and anticoagulant effects. Panax notoginseng may be a good source of lead compounds for novel antiplatelet and anticoagulant therapeutics.

A highly efficient Friedel-Crafts reaction of pyrroles with nitroolefins by a chiral phosphoric acid was realized. With 5 mol % of catalyst, reactions conducted at rt afforded the 2-substituted or 2,5-disubstituted pyrroles in up to 94% ee for a wide range of substrates.

Cytochrome P450 2B6 (CYP2B6) is expressed predominantly in human liver. It catalyzes the oxidative biotransformation of various drugs, including bupropion, which is an antidepressant and a tobacco use cessation agent. Serious adverse effects of high dosages of bupropion have been reported, including the onset of seizure. As Ginkgo biloba extract may be consumed with bupropion or another CYP2B6 drug substrate, potential exists for an herb-drug interaction. Therefore, we investigated the effect of G. biloba extract and some of its chemical constituents (terpene trilactones and flavonols) on the in vitro catalytic activity of CYP2B6 as assessed by the bupropion hydroxylation assay with recombinant enzyme and hepatic microsomes. The amount of hydroxybupropion was quantified by a novel and validated ultraperformance liquid chromatography/mass spectrometry method. Enzyme kinetic analysis indicated that G. biloba extract competitively inhibited hepatic microsomal CYP2B6-catalyzed bupropion hydroxylation (apparent K(i) was 162 +/- 14 microg/ml). Bilobalide and ginkgolides A, B, C, and J were not responsible for the inhibition of CYP2B6 catalytic activity by the extract. Whereas the 3-O-glucoside and 3-O-rutinoside of quercetin, kaempferol, and isorhamnetin had no effect, the corresponding aglycones (10 and 50 microg/ml) decreased hepatic microsomal bupropion hydroxylation. The inhibition of CYP2B6 by kaempferol was competitive (apparent K(i) was 10 +/- 1 microg/ml). In summary, G. biloba extract and its flavonol aglycones are naturally occurring inhibitors of in vitro CYP2B6 catalytic activity and bupropion hydroxylation. Future studies are needed to investigate whether G. biloba extract interacts in vivo with bupropion or other clinically important CYP2B6 drug substrates.

The molybdenum-based monoaryloxide monopyrrolide (MAP) species, Mo(NAd)(CHCMe(2)Ph)(C(4)H(4)N)(HIPTO) (2a), which contains "small" imido (Ad = 1-adamantyl) and "large" aryloxide (HIPTO = O-2,6(2,4,6-i-Pr(3)C(6)H(2))C(6)H(3)) ligands, catalyzes Z-selective metathesis reactions as a consequence of intermediate metallacyclobutane species not being able to have an (anti) substituent pointing toward the HIPTO group. Ring-opening metathesis polymerization (ROMP) of dicarbomethoxynorbornadiene (DCMNBD) with 2% 2a in toluene leads to >99% cis and >99% syndiotactic poly(DCMNBD), while ROMP of cyclooctene and 1,5-cyclooctadiene (300 equiv) with initiator 2a leads to poly(cyclooctene) and poly(cyclooctadiene) that have cis contents of >99%; all are previously unknown microstructures. Z-Selectivity is also observed in the metathesis of cis-4-octene and cis-3-hexene by initiator 2a to give cis-3-heptene.

Two diastereomers of the monoalkoxidepyrrolide (MAP) species, W(NAr)(CH(2))(Me(2)Pyr)(OR*) (1; Ar = 2,6-diisopropylphenyl, Me(2)Pyr = 2,5-dimethylpyrrolide, OR* = (R)-3,3'-dibromo-2'-(tert-butyldimethylsilyloxy)-5,5',6,6',7,7',8,8'-octahydro-1,1'-binaphthyl-2-olate), were generated through addition of R*OH to W(NAr)(CH(2))(Me(2)Pyr)(2). The unsubstituted tungstacyclobutane species, W(NAr)(C(3)H(6))(Me(2)Pyr)(OR*) (2), was isolated by treating the mixture of diastereomers of 1 with ethylene. An X-ray study revealed 2 to have a trigonal bipyramidal structure in which the imido and phenoxide ligands are in axial positions. A variety of NMR experiments were carried out on 1 and 2. The major findings are the following: (i) the methylidene ligands in the two diastereomers of 1 rotate readily about the W horizontal lineC bond (k = 2-7 s(-1) at 22 degrees C); (ii) NMR studies are consistent with 2 breaking up to give an intermediate alkylidene/ethylene complex, (R)- and (S)-W(CH(2))(C(2)H(4)); and (iii) the ethylene in the (R)-W(CH(2))(C(2)H(4)) intermediate can rotate about the W-ethylene bond axis at approximately the same rate as 2 re-forms or ethylene is lost to give 1. Compound 1 reacts with trimethylphosphine to yield (R)-1(PMe(3)). Two intermediate PMe(3) adducts were observed and found to convert to (R)-1(PMe(3)) in an intramolecular fashion with an average rate constant at 5 degrees C of approximately 1.4 x 10(-4) s(-1). Both neophylidene (4) and methylidene (5) MAP species containing 2,3,5,6-tetraphenylphenoxide ligand also were prepared. Compound 5 can be heated to 80 degrees C, where methylidene rotation about the W=C bond is facile and observable in a variable-temperature (1)H NMR spectrum. A (1)H-(1)H EXSY spectrum of 5 in benzene-d(6) at 20 degrees C showed that the methylidene protons are exchanging with k = 90 s(-1). A structure of 5(THF) showed it to be a square pyramid with the methylidene ligand in the apical position and THF coordinated trans to the imido ligand. Exposure of 5 to ethylene generated the tungstacyclobutane complex, W(NAr)(C(3)H(6))(Me(2)Pyr)(OR) (6), whose structure is analogous to that of 2. Treatment of 5 with PMe(3) yielded yellow 5(PMe(3)), an X-ray study of which revealed it to be a square pyramid with the methylidene ligand in the apical position and the phosphine trans to the pyrrolide. These studies suggest that metallacyclobutane intermediates in metathesis reactions with MAP species are likely to contain axial imido and phenoxide ligands, that metallacycles are formed when an olefin approaches the metal in a MAP species trans to the pyrrolide, and that the configuration at the metal inverts as a consequence of each forward metathesis step.

Two novel binaphthyl compounds have been synthesized for the selective fluorescent recognition of Ca(2+) or Pb(2+). By introducing different terminal groups to the receptor unit, the fluorescence signals of the receptors are significantly changed: 1 is fluorescence enhancement for Ca(2+), 2 is fluorescence quenching for Pb(2+). The binding properties for metal ions were examined by the absorption and fluorescence spectra. The fluorescence intensity enhancement was ascribed to the complex formation between Ca(2+) and 1 which blocked the photo-induced electron transfer process.

Slowly does it! By adding the substrate by a syringe pump, a highly efficient Friedel-Crafts reaction of 4,7-dihydroindoles with nitroolefins was realized with 0.5 mol % of a chiral phosphoric acid. The Friedel-Crafts alkylation, together with a subsequent oxidation of the product, led to 2-substituted indoles in excellent enantiomeric excesses, which can be easily transformed to enantioenriched tetrahydro-gamma-carbolines.

Objective: To determine the degree of agreement of Rome III and Rome II criteria in diagnosing irritable bowel syndrome (IBS) and to compare the clinical difference between the patients diagnosed with these two criteria., Methods: 3014 patients in the gastrointestinal outpatient department were enrolled consecutively and interviewed face to face with a standard questionnaire., Results: (1) 480 patients were diagnosed as IBS with Rome III criteria. The overall detection rate was 15.9% (480/3014). The proportion of IBS subtypes was as follows: IBS with constipation 27.9% (134/480), IBS with diarrhea 32.7% (157/480), Mixed IBS 6.7% (32/480), Unsubtyped IBS 32.7% (157/480). No difference was observed between different sex and age groups; with Rome II criteria, 558 patients were diagnosed with a detection rate of 18.5% (558/3014). The proportion of IBS subtypes was as follows: constipation predominant IBS 33.2% (185/558), diarrhea predominant IBS 38.2% (213/558), others 28.7% (160/558). The detection rate was higher in female patients (P = 0.002), but there was no difference between different age groups. The detection rate of Rome III criteria was lower than that of Rome II criteria (P = 0.008). There was a good accordance between these two criteria in the diagnosis of IBS (P < 0.01). (2) Patients classified according to Rome III criteria complained more severe abdominal symptoms (P = 0.04) and abnormal bowel habit (P < 0.001) as well as a higher healthcare seeking rate in the last 3 months (35.6% vs 26.5%, P = 0.02) as compared with those classified according to Rome II criteria. (3) According to Rome III criteria, the severity of bowel habit was different among the four subtypes (C-IBS, M-IBS > D-IBS > U-IBS, P < 0.005) while no difference was observed on the abdominal symptoms and the healthcare seeking rates in the last 3 months., Conclusions: There is a good accordance between Rome II and Rome III criteria in diagnosing IBS. Compared to Rome II criteria, Rome III criteria has a lower detection rate. It is more practical in the clinical practice with clear definition of symptom frequency and easy way of subtyping IBS. The patients diagnosed with Rome III criteria had more severe symptoms and higher healthcare seeking rate, they are more suitable for clinical trial.

To discover new 1,2,4-triazole derivatives which may possess significant biological activities, we synthesized a series of novel 6-aryl-3-(D-galactopentitol-1-yl)-7H-1,2,4-triazolo[3,4-b][1,3,4]thiadiazines and 4-(arylmethylidene)amino-5-(D-galactopentitol-1-yl)-3-mercapto-4H-1,2,4-triazoles from 4-amino-3-(D-galactopentitol-1-yl)-5-mercapto-1,2,4-triazole. All the title compounds were characterized by elemental analysis, IR, 1H- and 13C-NMR. Plant growth-regulating activity tests showed that these compounds have remarkable effects on the growth of radish and wheat.

We have synthesized a number of novel Schiff's bases from 4-amino-3-(D-glucoheptonic-hexitol-1-yl)-1H-1,2,4-triazole-5-thione. By attaching D-glucoheptonic-hexitol-1-yl residues to 1,2,4-triazole at the 3-position, the solubility of the title compounds has been improved greatly. All the products have been characterized by elemental analysis, IR, 1H-NMR, 13C-NMR and MS. The plant-growth regulating effects of the title compounds were examined. From the biological activity results, we found that most compounds showed weak to moderate activities.

A series of 6-aryl-3-(3-hydroxypropyl)-7H-1,2,4-triazolo[3,4-b][1,3,4]-thiadiazines were synthesized by the reaction of 4-amino-3-(3-hydroxypropyl)-5-mercapto-1,2,4-triazole (1) with substituted omega-haloacetophenones. Their structures were confirmed by elemental analysis, IR, 1H-NMR, and 13C-NMR. Tests of plant growth regulating effects showed that the title compounds display remarkable inhibitory activities on the growth of radish and wheat.

At present, metabolite profiling is of growing importance in herbal medicine fields such as breeding, formulation, quality control and clinical trials. This preliminary study indicated that ultra-performance liquid chromatography/time-of-flight mass spectrometry (UPLC/TOFMS)-based metabolomics allows direct detection of down-stream derivatives of metabolites, arising from the herbal formulation process. This analytical approach allows the discrimination and tentative authentication of unique biomarkers related to different herbal extracts using unsupervised multivariate principal component analysis (PCA). The tentative identification of biomarkers is complemented significantly by the accurate mass measurement of TOFMS and the high resolution and high retention time reproducibility rendered by UPLC. The application of this approach in herbal extract discrimination and ginsenoside biomarker discovery of raw and steamed Panax notoginseng (Burk.) F.H. Chen is demonstrated and discussed., (Copyright (c) 2007 John Wiley & Sons, Ltd.)

This review focuses on the application of phage display technology in the prevention, diagnosis and treatment of parasitic diseases. It covers: (1) an introduction of phage display technology, filamentous phage and the advantage of carrier. (2) Construction of phage antibody libraries of parasites, epitope mapping and mimotope, and their potential application in the development of novel diagnostic reagents and vaccines.

Dencichine (beta-N-oxalyl-L-alpha,beta-diaminopropionic acid) is a haemostatic agent present in important Chinese medicinal herbs such as Panax notoginseng, as well as other Panax species. It is also a reported neurotoxic agent found in Lathyrus sativus (grass pea seed). A selective analytical method incorporating hydrophilic interaction chromatography with positive electrospray ionization tandem mass spectrometry (HILIC/ESI-MS/MS), for the analysis of dencichine in Panax plant species, was developed. Using multiple reaction monitoring (MRM) mode, underivatized dencichine, a small and highly polar compound, was selectively detected and quantified. The contents of dencichine in raw and steamed Panax notoginseng roots, 11 pairs of raw and steamed P. notoginseng herbal products, Panax ginseng roots, and Panax quinquefolium roots, were analyzed and compared. Optimal sensitivity of 0.3 ppm (detection limit) and 1.5 ppm (quantification limit) was achieved. The method was rapid (< or =5 min), with the HILIC peak eluting at about 1 min. Steamed P. notoginseng samples were found to contain less dencichine than the corresponding raw samples, and there were also differences among the three Panax species; raw P. ginseng and P. quinquefolium contained less dencichine than the raw P. notoginseng species. This rapid and specific method may be applied to the quantification of dencichine in complex medicinal plants and their products., (Copyright 2005 John Wiley & Sons, Ltd.)

A high-performance liquid chromatographic (HPLC) method coupled with chromatographic pattern matching was developed to differentiate whole chromatograms of raw and steamed Panax notoginseng objectively and quantitatively. The major peaks differentiating chromatograms of raw and steamed samples were also identified for the first time in this herb. The raw and steamed P. notoginseng roots and its products were successfully differentiated. The quantitative differences between the chromatograms were correlated to the duration of steaming. Chromatographic pattern matching allows rapid, simple, automated, and quantitative comparisons of complex chromatograms. It is a useful tool in ensuring safety and quality of herbal products.

A reversed-phase high-performance liquid chromatography-diode array detection method was developed and validated for the simultaneous determination of six saponins (notoginsenoside R1, ginsenosides Rg1, Re, Rb1, Rc, Rd) in raw and steamed Panax notoginseng. Linearity (r2 > 0.9988), intra- and inter-day precision (RSD < 4%), limit of detection (0.008-0.013 mg/ml), limit of quantification (0.027-0.042 mg/ml) of the saponins were determined. The method was successfully applied to 11 pairs of raw and steamed P. notoginseng products. Three products showed discrepancies between theirlabelled claims (raw or steamed) and the results of analysis. This new, simple and reliable method could be used in the quality control of raw and steamed P. notoginseng.

Adulterations with synthetic drugs are common problems with herbal medicine and this can potentially cause serious adverse effects. It is therefore important to determine the presence of synthetic drugs in herbal medicine to ensure patients' safety. The objective of this study was to develop sensitive and specific methods to analyse phenylbutazone, caffeine and oxyphenbutazone present in a traditional Indonesian herbal product. Liquid chromatography-mass spectrometry-mass spectrometry (LC-MS-MS) methods in the selected reaction-monitoring (SRM) mode were developed. It was found that the sample contained 0.53% w/w (n=3, RSD=7.56%) phenylbutazone and 0.04% w/w (n=3, RSD=8.39%) caffeine. This corresponded to 43.17 mg phenylbutazone and 3.23 mg caffeine in each sachet of powder. The methods were validated for linearity, precision, accuracy, LOD and LOQ. LOD and LOQ were found to be 3.69 and 12.29 ng/ml, respectively for phenylbutazone. For caffeine, the LOD and LOQ were 0.84 and 2.80 ng/ml, respectively. Oxyphenbutazone in the sample was found to be present at a level below the quantification level of 10.2 ng/ml. With better methods developed for analysis of adulterants in herbal medicine, the quality and safety of these medicines can be better controlled and regulated to ensure patients' safety.

Background: High levels of hyperoxemia may have utility in the treatment of regional tissue ischemia, but current methods for its implementation are impractical. A catheter-based method for infusion of O2, dissolved in a crystalloid solution at extremely high concentrations, ie, 1 to 3 mL O2/g (aqueous oxygen [AO]), into blood without bubble nucleation was recently developed for the potential hyperoxemic treatment of regional tissue ischemia., Methods and Results: To test the hypotheses that hypoxemia is correctable and that hyperoxemia can be produced locally by AO infusion, normal saline equilibrated with O2 at 3 MPa (30 bar; 1 mL O2/g) was delivered into arterial blood in two different animal models. In 15 New Zealand White rabbits with systemic hypoxemia, AO was infused into the midabdominal aorta at 1 g/min. Mean distal arterial PO2 increased to 236+/-113 and 593+/-114 mm Hg on 1-hour periods of air and O2 breathing, respectively, from a baseline of 70+/-10 mm Hg (P<.01). In contrast, infusion of ordinary normal saline in a control group (n=7) had no effect on arterial PO2. No differences between groups (P>.05) in temporal changes in blood counts and chemistries were identified. In 10 dogs, low coronary blood flow in the circumflex artery was delivered with a roller pump through the central channel of an occluding balloon catheter. Hypoxemic, normoxemic, and AO-induced hyperoxemic blood perfusates (mean PO2, 52+/-4, 111+/-22, and 504+/-72 mm Hg, respectively) were infused for 3-minute periods in a randomized sequence. Short-axis two-dimensional echocardiography demonstrated a significant decrease (P<.05) in left ventricular ejection fraction compared with baseline physiological values with low-flow hypoxemic and normoxemic perfusion but not with low-flow hyperoxemic perfusion., Conclusions: Intra-arterial AO infusion was effective in these models for regional correction of hypoxemia and production of hyperoxemia.

Laser balloon angioplasty (LBA) has been shown to acutely increase angiographic luminal dimensions after conventional balloon angioplasty (PTCA) without a favorable impact on chronic restenosis. Experimentally, laser and thermal energy enhance binding of heparin to the injured arterial wall and to the thrombus. In view of the anticoagulant, antiproliferative, and antifibrotic activities of the drug, a pilot study was performed to evaluate the potential safety and efficacy of LBA combined with local heparin therapy. Ten patients scheduled for elective PTCA were entered in the study. In each patient, a single lesion was treated with a laser balloon and coated with a heparin film (3000 I.U. at a concentration > 100,000 I.U./gm) immediately after optimal PTCA. The mean minimum luminal diameter and mean percent stenosis of the 10 treated lesions after PTCA were 1.62 +/- 0.39 mm and 37% +/- 9%, respectively. After LBA and local heparin therapy, the mean minimal lumen diameter increased to 2.01 +/- 0.34 mm (p < 0.01) and the mean percent stenosis decreased to 20% +/- 10% (p < 0.01). Systemic heparin was discontinued immediately after the procedure in all patients. Acute or inhospital complications, either major or minor, occurred in none (0%) of the 10 patients (95% confidence interval 0% to 31%); all were discharged home on the day after the procedure. All patients remained well and free of cardiac symptoms for at least 2 months after the procedure. However, restenosis developed in six (60%) of the 10 patients (95% confidence interval 26% to 88%) 2 to 6 months after the procedure. The results suggest that LBA and local heparin therapy, with discontinuation of systemic heparin immediately after angioplasty, is a safe treatment modality that yields favorable acute angiographic results.