The chemical constituents from polarity part in the roots of Angelica dahurica var. formosana cv. Chuanbaizhi were studied in this paper. The compounds were separated and purified by repeated column chromatographic methods on silica gel and HPLC, and the chemical structures of compounds were determined by spectral data analyses. Fourteen compounds were obtained and identified as tert-O-β-D-glucopyranosyl-(R)-byakangelicin (1), (2"S) -3"-O-β-D-glucopyranosyl-oxypeucedanin hydrate (2), marmesinin (3), sec-O-β-D-glucopyranosyl-byakangelicin (4), isofraxidin-7-O-β-D-glucopyranoside (5), benzyl-O-β-D-glucopyranoside (6), 8-O-β-D-glycopyranosylxanthotoxol (7), prenyl-O-β-D-glucopyranoside (8), scopolin (9), (2' R) -5'-hydroxymarmesin-5'-O-β-D-glucopyranoside (10), (2'S,3'R) -3'-hydroxymarmesinin (11), skimmin (12), benzyl-O-β-D-apiofuranosyl-(1"--> 6')-β-D-glucopyranoside (13), and decuroside IV (14). Among them, compounds 2, 5, 6, 8, and 10-13 were obtained from the roots of title plant for the first time.
Angelica ; chemistry ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Mass Spectrometry ; Molecular Structure ; Plant Roots ; chemistry

Organic anion transporting polypeptide 1B1 (OATP1B1) is an important liver-specific uptake transporter, which mediates transport of numerous endogenous substances and drugs from blood into hepatocytes. To identify and investigate potential modulators of OATP1B1 from natural products, the effect of 21 frequently used natural compounds and extracts on OATP1B1-mediated fluorescein methotrexate transport was studied by using Chinese hamster ovary cells stably expressing OATP1B1 (CHO-OATP1B1) in 96-well plates. This method could be used for the screening of large compound libraries. Our studies showed that some flavonoids (e.g., quercetin, quercitrin, rutin, chrysanthemum flavonoids and mulberrin) and triterpenoids (e.g., glycyrrhetinic acid and glycyrrhizic acid) were inhibitors of OATP1B1 with IC50 values less than 16 µmol · L(-1). The IC50 value of glycyrrhetinic acid on OATP1B1 was comparable to its blood concentration in clinics, indicating an OATPlB1-mediated drug-drug interaction could occur. Structure-activity relationship analysis showed that flavonoids had much higher inhibitory activity than their glycosides. Furthermore, the type and length of saccharides had a significant effect on their activity. In addition, we used OATP1B1 substrates fluvastatin and rosuvastatin as probe drugs to investigate the substrate-dependent effect of several natural compounds on the function of OATP1B1 in vitro. Our results demonstrated that the effect of these natural products on the function of OATPlB1 was substrate-dependent. In summary, this study would be conducive to predicting and avoiding potential OATP1B1-mediated drug-drug and drug-food interactions and thus provide the experimental basis and guidance for rational drug use.
Animals ; Biological Products ; CHO Cells ; Cricetulus ; Drug Interactions ; Fatty Acids, Monounsaturated ; pharmacology ; Flavonoids ; pharmacology ; Indoles ; pharmacology ; Inhibitory Concentration 50 ; Organic Anion Transporters ; genetics ; metabolism ; Rosuvastatin Calcium ; pharmacology ; Structure-Activity Relationship

Objective To investigate the safty and accuracy ot estimating the living donor's graft volume with IQQA liver imaging evaluation system.Methods Between June 2007 and July 2010,123living liver donors were enrolled to undergo 16-slice CT scanning,then graft volume was estimated by both IQQA and manu-traced multi-slice spiral computed tomography (MSCT) approach.The graft volume and time consuming between IQQA and manu-traced MSCT were compared. Pearson Correlation test was uesd to verify the correlation between the estimated graft volume estimated each method and actual graft weight detected in operation.Linear correlation analysis was done.Results The mean graft volume by IQQA and manu-traced MSCT was (856.76 ± 162.18) and (870.64 ±172.54) cm3 respectively preoperation.Paired t-test showed there was no statistically significant difference between IQQA and MSCT methods (P＞0.05).It took mean ( 16.9 ± 1.4) min to calculatethe graft volume by IQQA and (39.3 ± 2.1 ) min by manu-traced MSCT,respectively (P＜0.05).The real graft volume was (632.59 ± 13 1.73) cm3.Pearson correlation test showed the graft volume calculated by either IQQA or MSCT method had a significantly positive correlation with the real graft weight (MSCT r =0.921,IQQA r =0.896,P＜0.01 ).Graft weight could be expressed in the equation:Actual graft weight =- 150.303 + 1.025 × IQQA value or =- 94.397 + 0.955 × MSCT value.Conclusion IQQA system has same accuracy with MSCT method in predicting the graft volume but consuming less time.IQQA system promotes the recognition of clinician on liver three dimensional anatomic structure.

OBJECTIVETo evaluate the effect of infrared radiation and magnetic field therapy on cartilage damage in rabbits with knee osteoarthritis.

METHODSKnee osteoarthritis was induced in 24 adult New Zealand rabbits by prolonged fixation of the knee joint in extension for 6 weeks. The rabbits were subsequently randomized into control group (without treatment), infrared therapy group, magnetic field therapy group and the combined infrared and magnetic field therapy group. At the end of the first, second and third weeks of the therapy, respectively, 2 rabbits from each group were sacrificed to observe the general changes and histopathology of the condylar cartilage of the femur, and the findings were assessed using Mankin scores.

RESULTSCompared with other groups, the rabbits in the combined therapy group showed significantly milder cartilage damage (including injury of the cartilage surface and chondrocyte's proliferation and disarrangement) with significantly lower Mankin scores (P<0.05). No significant differences were found in the findings between the two groups with exclusive infrared or magnetic field therapy (P>0.1).

CONCLUSIONCombined infrared and magnetic field therapy can effectively alleviate cartilage destruction, shortens the disease course and enhance the therapeutic effects in rabbits with knee osteoarthritis.

Animals ; Cartilage, Articular ; drug effects ; pathology ; Femur ; pathology ; Infrared Rays ; therapeutic use ; Knee Joint ; pathology ; Magnetic Field Therapy ; Osteoarthritis, Knee ; pathology ; therapy ; Rabbits

OBJECTIVESTo investigate the pathoanatomize histological and biochemical characteristics of benign prostatic hyperplasia (BPH) by use of old dogs with spontaneous BPH as animal models.

METHODSOld dogs aged 6 to 13 years were recruited after anus check, B-ultrasonic examination by recta spy and measurement under surgical exploration. Ten dogs with notable prostatic hyperplasia were used as models, and 6 with non-hyperplasia prostate as control. Serum testosterone (T), estrogen (E2), ACP and prostatic specific antigen (PSA) were analyzed, and prostates were checked histologically.

RESULTSProstate volume of the BPH group was significantly bigger than those of the control group, (14.7 +/- 2.3) and (13.8 +/- 1.9) cm3 vs (8.4 +/- 1.0) and (8.4 +/- 1.9) cm3, P < 0.01. Serum T [(14.3 +/- 2.9) vs (16.4 +/- 4.0) nmol/L] and E2 [(137.6 +/- 70.8) vs (164.4 +/- 82.0) pmol/L] were not different between the two groups (P > 0.05). ACP of the BPH group was higher than that of the control group [(6.63 +/- 2.76) vs (4.92 +/- 2.19) U/L], but the difference was not statistically significant (P > 0.05). There was significant difference between the BPH group and the control group in PSA level [(5.6 +/- 0.78) vs (3.1 +/- 0.54) microgram/L, P < 0.01]. The tissue slides of the BPH prostates showed hyperplasia with raised height of epithelium, and many long and offsetting mammillae in the gland cavity due to epithelium hyperplasia.

CONCLUSIONOld dogs with spontaneous BPH are useful animal models for the etiological and pharmacological researches of human BPH.

Animals ; Disease Models, Animal ; Dog Diseases ; pathology ; Dogs ; Male ; Prostate ; pathology ; Prostate-Specific Antigen ; blood ; Prostatic Hyperplasia ; pathology ; veterinary

OBJECTIVETo explore the expression of MICA/B in human esophageal cancer, and to analyze its correlation with clinicopathological features.

METHODSThe expression of MICA/B in 40 cases of esophagus carcinoma and corresponding normal esophageal mucosa tissues were examined by immunohistochemistry.

RESULTSThe positive rate of expression of MICA/B protein in the esophageal carcinoma was 75.0% (30/40), and that in the corresponding normal esophageal mucosa was 0 (0/40). Up-regulation of MICA/B expression was found in the esophageal carcinomas. The expression of MICA/B was related with histological grade of the esophageal carcinoma (P = 0.012).

CONCLUSIONMICA/B protein plays an important role in the esophageal carcinogenesis, and my become a useful molecular marker for the diagnosis of esophageal carcinoma.

Adult ; Aged ; Aged, 80 and over ; Biomarkers, Tumor ; metabolism ; Esophageal Neoplasms ; diagnosis ; metabolism ; pathology ; Female ; Histocompatibility Antigens Class I ; metabolism ; Humans ; Immunohistochemistry ; Male ; Middle Aged ; Neoplasm Grading ; Up-Regulation

AIM:To explore the effect of genistein on ammonia-induced nuclear factor-κB (NF-κB) activation and the underlying mechanism.METHODS:Primary astrocyte cultures were prepared and challenged with NH4Cl to establish a hyperammonemic model.The activation of ERK,Akt and NF-κB was examined by Western blot.RESULTS:AG1478 and genistein significantly inhibited ammonia-induced activation of ERK and Akt.Ammonia-induced NF-κB nuclear translocation was significantly inhibited by the pretreatment of LY294002,genistein and AG1478.CONCLUSION:Genistein significantly inhibited ammonia-induced ERK activation and Akt-mediated NF-κB activation,which might represent the important mechanism by which this naturally occurring substance exerts its swelling-inhibiting effect.

In order to explore the possibility of human adenovirus infection with tree shrews,the neutralizing antibody ti-ters of five kinds of human adenoviruses (HAdv)in the serum of tree shrews were analyzed.The levels of Ad3,Ad4,Ad7, Ad14 and Ad55 neutralizing antibody were detected by virus neutralization test.The results showed that the positive rate of four adenoviruses in group B were higher than Ad4 in group E,and the positive rates respectively were Ad14 (55.88%),Ad3 (47.06%),Ad55 (29.71%),Ad7 (14.71%)and Ad4 (8.82%).The antiserum mainly mixed with Ad3,Ad14 and Ad55 anti-body.Five species of human adenovirus can be naturally infected with tree shrews.Tree shrews are used as experimental ani-mals to establish human adenovirus infection model is alternative.

OBJECTIVETo evaluate the efficacy and investigate the influencing factors of the interferon (IFN) retreatment for patients with chronic hepatitis C relapsed after a previous IFN treatment.

METHODSA retrospective study was designed to analyze the retreatment with IFN of 60 relapsed chronic hepatitis C patients. All patients were from a randomized, opened and multi-center clinical trial about the efficacy and security of PEG-IFNalpha-2a compared to CIFNalpha-2a in the treatment of chronic hepatitis C in China. There were 35 patients treated with PEG-IFNalpha-2a and 25 with CIFNalpha-2a. The main parameter to evaluate the efficacy was sustained viral response (SVR) rate. The influence of viral concentration in serum, genotype and drug categories on the responses to IFN were analyzed.

RESULTSFor all the patients, the end of treatment virus response (ETVR) and SVR rates were 55.00% and 35.00% respectively. ETVR rate of PEG-IFNalpha-2a was significantly higher than that of CIFNalpha-2a (74.29% and 28.00% respectively, P < 0.01). SVR rate of PEG-IFNalpha-2a was also markedly higher than that of CIFNalpha-2a (45.71% and 20.00% respectively, P < 0.05). However, there was no significant difference between the high and low viral load groups. Among the patients with genotype 1, ETVR and SVR rates of PEG-IFNalpha-2a (75.00%, 45.83%) were significantly higher than those of CIFNalpha-2a (22.22%, 11.11%), (P < 0.01, P < 0.05 respectively), but in patients with genotype non-1, there were no such differences between the two groups.

CONCLUSIONSome relapsed patients were not responsive to the IFN retreatment. The efficacy of PEG-IFNalpha-2a was superior to CIFNalpha-2a. The conventional IFN was not suggested to be used in the relapsed cases with genotype 1. The viral load was not associated with the efficacy of IFN retreatment.

Adult ; Antiviral Agents ; therapeutic use ; Female ; Hepatitis C, Chronic ; therapy ; Humans ; Interferon-alpha ; therapeutic use ; Interferon-beta ; Interferons ; therapeutic use ; Male ; Middle Aged ; Polyethylene Glycols ; therapeutic use ; Recombinant Proteins ; Recurrence ; Retrospective Studies

OBJECTIVETo investigate the relationship between hepatitis C virus (HCV) genotype, serum viral load and ALT levels, and the factors associated with the viral relapse after IFN treatment in patients with chronic hepatitis C.

METHODSThe HCV RNA levels were determined with Cobas Amplicor Monitor Test, version 2.0, and HCV genotypes were examined by means of PCR products of 5' NTR digested with restriction endonucleases. The patients with chronic hepatitis C were treated with PEG-IFN alpha -2a and Roferon-A for 24 weeks. Those with a viral response after 24 week treatment were followed for an additional 24 weeks. The association of clinical characteristics, such as sex, age, the way of the HCV infection, IFN treatment history and platelet counts, and the HCV genotype, virus load and medicine used for the viral relapse after IFN treatment were analyzed.

RESULTSOf the 208 chronic hepatitis C patients, the ALT levels were not related to HCV RNA levels (r = 0.093, P > 0.05). No difference of ALT levels between HCV genotypes was found, and the HCV RNA load was also of no difference between HCV genotype 1 patients and non 1 patients. Of the 119 patients with viral response after 24 week treatment, 58 cases (48.7%) relapsed after another 24 week's follow-up. Relapse was not significantly related to the clinical characteristics, such as sex, age, mode of the infection, treatment history of IFN, AST/ALT ratio, platelet counts and the baseline viral load. Among patients with genotype 1 virus, the relapse rate was significantly higher than those patients with non-genotype 1 virus (54.5% vs 32.1%, P=0.039). The relapse rate after PEG-IFN alpha -2a treatment was lower than that of Roferon-A treatment (47.0% vs. 52.8%), but not significantly.

CONCLUSIONThe viral relapse of chronic hepatitis C patients after IFN treatment was significantly associated with the genotypes of the HCV.

Antiviral Agents ; therapeutic use ; Female ; Genotype ; Hepacivirus ; genetics ; Hepatitis C, Chronic ; drug therapy ; virology ; Humans ; Interferon-alpha ; therapeutic use ; Male ; Middle Aged ; RNA, Viral ; blood ; Recombinant Proteins ; Recurrence ; Treatment Outcome ; Viral Load