Objective To determine the preventive effect of Celecoxib on postoperative adhesion formation and its mechanism. Methods We divided 80 SD rats into 5 groups: Groups A, B, C, H and S. Rats in Groups A, B, C and H received the operation of peritoneum rubbing to promote adhesion formation. Group S underwent sham operation. Rats in Group B were given Celecoxib of 40 mg/(kg·d), those in Group C were also given Celecoxib of 20mg/(kg·d), and those in Group H were given sodium hyaluronate (HA) during the operation. On the 8th and 15th postoperative day, half of the rats were sacrificed, the extent of adhesion formation was assessed and the adhesive peritoneum was subjected to immunohistochemistry with VEGF and CD_(34). Results The extent of postoperative adhesion differed significantly among the five groups (P<0.01). Groups B and C had significantly fewer adhesions than Groups H and A. VEGF was expressed most highly in Group A, followed by Groups H, C and B, and most weakly in Group S. CD34 was expressed most highly in Group A, followed by Groups H, C and B, and most weakly in Group S. Conclusion Celecoxib provides durable inhibition of intra-abdominal adhesions in a murine model compared with HA. The mechanism of preventing intra-abdominal adhesion via inhibiting COX-2 is possibly through down-regulated expression of VEGF and reduced microvascular density.

Humans ; Leiomyoma ; pathology ; Microtomy ; methods ; Microwaves ; Paraffin Embedding ; methods ; Specimen Handling ; methods ; Thyroid Neoplasms ; pathology

Objective To observe the effects of Bushen Yiqi recipe on aging rats′ exercise capacity, morphology and oxidation resis-tance.Methods Male sprague dawley rats were divided into normal group, model group, traditional Chinese medicine group, methandienone group.The rats in the latter three group were received a subcutaneous in-jection of 10%D-galactose with 0.1 mg? g -1? d-1 for 10 weeks.The rats in traditional Chinese medicine group and methandienone group were given medicine by gavage .The dosage is adults′7 times of per kilogram of body weight and equivalent dose respectively.The experiment were las-ted for 10 weeks.Then rats′exercise capacity were tested by treadmill. The Morphological structure of the skeletal muscle were observed by elec-tron microscope.Rats′advanced glycosylated end products( AGEs) were tested by Elisa method.Rats′superoxidedismutase ( SOD) and malondi-aldehyde ( MDA) content in blood serum were tested by spectrophotome-try.Results Compared with normal group, the rats′exercise capacity, the mitochondria number and volume of rats′skeletal muscle, the serum SOD activity, the thymus index and spleen index in model group dropped significantly.The serum AGEs and MDA content increased significant-ly.Compared with model group, the exercise capacity, the mitochondria number and volume of rats′skeletal muscle, the thymus index in traditional Chinese medicine group and methandienone group inceased obviously.The serum MDA content decreased obviously.Conclusion Bushen Yiqi recipe can slow the aging progress of skeletal muscle through improving the model rats′degenerative changes of the above-mentioned indexes.

In the current study, nine flavonoids were isolated and purified from 75% ethanol extract of Selaginella uncinata (Desv.) Spring by column chromatographic techniques over macroporous resin, polyamide, silica gel, Sephadex LH-20 and pre-HPLC. On the basis of their physico-chemical properties and spectroscopic data analyses, these compounds were elucidated as cirsimarin (1), nepitrin (2), apigenin-6-C-α-L-arabinopyranosyl-8-C-β-D-glucopyranoside (3), apigenin-6-C-β-D-glucopyranosyl-8-C-α-L-arabinopyranoside (4), apigenin-7-O-β-D-glucopyranoside (5), 2,3-dihydroamentoflavone (6), 4'-O-methylamentoflavone (7), 2,3-dihydro-4'-O-methyl-amentoflavone (8), and 2,3,2",3"-tetrahydron-4'-O-methyl-robustaflavone (9). Compounds 1-5 belong to flavonoid glycosides and were isolated from the genus Selaginella for the first time.
Flavonoids ; analysis ; Selaginellaceae ; chemistry

OBJECTIVE To map a comprehensive metabolic pathway of herbacetin in rats, specifically, to elucidate the biotransformation of herbacetin in vivo and to simultaneously monitor the pharmacokinetic process of both parent drug and its major metabolites. METHODS liquid chromatography/ion trap mass spectrometry (LC/MSn) and ultra-liquid chromatography coupled with mass spectrometry (UPLC/MS) were combined in the current study for qualitative and quantitative determinations of herbacetin and its metabolites in bile, urine and feces after both oral and intravenous administration of herbacetin to rats. Enzyme kinetic studies on the intestinal and hepatic metabolism of herbacetin were further conducted to elucidate metabolic profiles of herbacetin in rat tissues and organs. Additionally, plasma concentration profiles of herbacetin and its metabolites in rats were obtained to characterize the overall pharmacokinetic behavior of herbacetin. RESULTS It was found that herbacetin was excreted primarily from rat urine in the form of glucuronide-conjugations. Subsequent in vitro enzyme kinetic studies and in vivo pharmacokinetic investigations suggested an extensive hepatic metabolism of herbacetin and the high exposure of herbacetin- glucuronides in systemic circulation. The clearance, half- life and bioavailability of herbacetin in rats were determined as (16.4±1.92)mL·kg-1·min-1, (11.9±2.7)min, and 1.32%, respectively. On basis of these findings, a comprehensive metabolic pathway of herbacetin in rats was composed. In addition, a physiology based pharmacokinetic (PBPK) model was successfully developed with the aid of the GastroPlus to simulate the pharmacokinetic process of herbacetin in rats. Application of the PBPK modeling can provide a useful starting point to understand and extrapolate pharmacokinetic parameters among different species, populations, and disease states. CONCLUSION After oral administration, herbacetin was subjected to colonic degradation and extensive first pass metabolism, with glucuronidation as its dominating in vivo metabolic pathway.

OBJECTIVE To investigate the effect of hypoxia on the pharmacokinetic process of salidrosidein rats and to explore its underlying mechanisms. METHODS The Caco-2 cell monolayerwas exposed to 1% oxygen (O2) concentration for 24 h to build the hypoxiccell model. The transportation mode of salidroside was investigated with the aid of this hypoxia model by detecting the apparent permeability coefficient(Papp). Healthy Sprague Dawley (SD) rats were exposed to 9% O2 for 72 h for the construction of hypoxic rat model. Liver sample was subsequently collected from the hypoxic rats with an aim to identify enzymes responsible for salidroside metabolism. The expression levels of sali?droside-transporting and salidroside-metabolizing enzymes, including Sodium-dependent glucose cotrans?porters (SGLT1), β-glucosidase (GBA3)and sulfotransferase (SULT2A1), were thereafter detected by RT-PCR and Western blot. The metabolic activity of GBA3 and SULT2A1 was monitored by rat liver microsome incubation.In addition, the renal function of rats under hypoxia was assessed by detecting concentrations of blood urea nitrogen and creatinine. RESULTS The AUC and t1/2 values of salidroside in hypoxic rats were more than doubled, while the in vivo clearance was significantly reduced. Mechanistic study demonstrated that the PappA- B/PappB- A eualsto 10.3, indicating the potential active transport of salidrosile. The expression of SGLT1 and GBA3 was significantly decreased, which indicated a reduced metabolism of salidroside under hypoxia. Moreover, rat under hypoxia was found to suffer from renal dysfunction, with an abnormal value of blood urea nitrogen. CONCLUSION Due to the reduced metabolism and the abnormal renal function under hypoxia, the systemic exposure of salidroside in rats was signifi?cantly enhanced.

AIMTo study the active constituents of Swertia davidi Franch..

METHODSChromatography was used to isolate and purify the chemical components, their structures were identified by spectral analysis.

RESULTSThree compounds were identified as 1,7-dihydroxy-3,8-dimethoxyxanthone (gentiacaulein) (V), 1,8-dihydroxy-3,7-dimethoxyxanthone (methylswertianin) (VI) and 1,8-dihydroxy-3,4,7-trimethoxyxanthone (VII).

CONCLUSIONCompound VII is a novel xanthone, named daviditin A, the others were isolated from Swertia davidi Franch. for the first time.

Molecular Structure ; Plants, Medicinal ; chemistry ; Swertia ; chemistry ; Xanthones ; chemistry ; isolation & purification

Objective To study the effect of HCV receptors′sequence on virus entry based on the two-dimensional structure and via tandem expression of HCV receptors on mouse hepatocytes.Methods The construced recombinant expression vectors pCDH-hLDLR-hSR-BⅠ-hCD81-GFP, pCDH-hLDLR-hCD81-hSR-BⅠ and pCDH-hCLDN-1-hOCLN-DsRed were cotransfected into 293FT cells with package vectors.The collected recombinant lentivirus expressing hCLDN-1-hOCLN was concentrated and attacked mouse hepatocytes.The transgenic mouse hepatocytes with tandem overexpression of CLDN-1 and OCLN were established after G418-selection.The transduced cells LSCCO/Hepa1-6 and LCSCO/Hepa1-6 were sorted via flow cytometry and puro-G418-selection after recombinant lentivirus expressing hLDLR-hSR-BⅠ-hCD81 and hLDLR-hCD81-hSR-BⅠattacked Hepa1-6 respectively.The infectivity of transduced mouse hepatocytes LSCCO/Hepa1-6 and LCSCO/Hepa1-6 to HCV was analyzed via direct-infection of serum-derived virus.Furthermore, the effect of HCV receptors′sequence on virus entry was studied.Results Both LSCCO/Hepa1-6 and LCSCO/Hepa1-6 enhanced HCV-cell binding.The transduced mouse hepatocytes LSCCO/Hepa1-6 had more HCV endocytosis.Conclusion SR-BⅠhas priority over CD81 in HCV entry in the early stage.

Objective To investigate the molecular epidemiology of human immunodefieiency viruses (HIV)-1 infected individuals in Honghe district,Yunnan Province and provide the evidence of molecular biology features of HIV-1 infection.Methods HIV-1 pol gene was amplified by reverse transcription-polymerase chain reaction (RT-PCR).Then sequencing and phylogenetic tree analysis were employed tO determine HIV-I subgenotype.The sequence alignment was performed in the database of international drug resistance tO identify resistance-associated mutations.Results The samples from 60 HIV-1 infected individuals were investigated:39 were male,21 were female,with average age 35.5 years old.Thirty-four cases were infected with HIV-I through intravenous drug abuse,12 by sexual contacts,2 were contaminated blood/blood products transfusion and 12 with unknown transmission routes.Phylogenetic analysis revealed that 53 cases (88.3%) were subtype 08-BC,6 (10.0%) were subtype 07-BC and 1 (1.7%) was subtype 01_AE.The total rate of drug resistance associated mutations was 33.3%.The major mutations in protease (PR) and reverse transcriptase (RT) regions accounted for 5.0% and 3 1.7%,respectively.The major mutations in PR region were I541M,V82VFIL,M46MI,which were found in 1 case,respectively.The mutations in RT region were as follows:4 cases were T69D,6 were A62V,1 was D67DE,1 was E44D,3 were V179D,1 was V179E.1 was K238KN,1 was L234T+P236S and 1 was V106E.Conclusions The major transmission route of HIV-I infection in Honghe district,Yunnan Province is through drug injection.The major HIV-1 subtype of HIV-infeeted individuals is 08_BC.PR inhibitor and RT inhibitor drug resistance associated mutations in HlV-1 gene have already existed.

OBJECTIVETo explore the effect of Telbivudine (LDT) Tablet combined with Jianpi Bushen Recipe (JBR) on serum hepatitis B virus (HBV) specific cytotoxic T lymphocyte (CTL) and HBeAg seroconversion in chronic hepatitis B (CHB) patients.

METHODSTotally 90 HBeAg-positive and human leukocyte antigen (HLA)-A2 positive CHB patients were randomly assigned to the treatment group and the control group, 45 cases in each group. Patients in the treatment group took LDT Tablet (600 mg, once per day) combined with JBR granule (twice per day), while those in the control group took LDT Tablet alone. The therapeutic course for all was one year. HBV DNA negative conversion rate, HBeAg seroconversion rate, and level of HBV specific CTL were compared after 1 year treatment; liver function, drug resistance mutations, and adverse reactions were also compared between the two groups.

RESULTSAfter 1 year treatment, HBV DNA negative conversion rate and HBeAg seroconversion rate were 88.89% (40/45) and 40.00% (18/45) in the treatment group, higher than those of the control group [68.89% (31/45) and 20.00% (9/45)], with statistical difference (P < 0.05). Level of HBV specific CTL in the treatment group was 0.78% +/- 0.09% after treatment, higher than that of the control group after 1 year treatment (0.54% +/- 0.11%) and that before treatment (0.36% +/- 0.07%), with statistical difference (P < 0.01). Level of HBV specific CTL in 27 patients with HBeAg seroconversion was 0.81% 0.10%, higher than that of 63 patients without HBeAg seroconversion (0.60% +/- 0.09%), with statistical difference (P < 0.01). ALT returned to normal in 44 cases of the treatment group (97.78%), while it was 42 cases (93.33%) of the control group, with no statistical difference between the two groups (P > 0.05). Total bilirubin (TBil) in the two groups all turned to normal. rtM204I variation occurred in 1 case (2.22%) of the treatment group and 2 cases (4.44%) in the control group. No obvious adverse reaction occurred in the two groups.

CONCLUSIONLDT Tablet combined with JBR could elevate levels of HBV specific CTL and HBeAg seroconversion in CHB patients.

Drug Therapy, Combination ; Drugs, Chinese Herbal ; therapeutic use ; Hepatitis B e Antigens ; blood ; Hepatitis B virus ; Hepatitis B, Chronic ; drug therapy ; Humans ; Seroconversion ; T-Lymphocytes, Cytotoxic ; immunology ; Tablets ; Thymidine ; analogs & derivatives ; therapeutic use