Pharmacokinetic study of rhizoma Curcumae oil and rhizoma Curcumae oil-ß-cyclodextrin inclusion complex in pigs after oral administration.

Pharmacokinetics of rhizoma Curcumae oil-pure drug (RCO-PD) and its ß-cyclodextrin inclusion complex (RCO-ßCD) were studied in a randomized two-way crossover design following a single oral administration of the two formulations. Germacrone concentrations in plasma were determined by high-performance liquid chromatography with UV detector. The concentrations vs. time data were analyzed by a noncompartmental pharmacokinetic method. The result showed that germacrone in both groups was rapidly absorbed followed by a slow elimination. The main parameters in RCO-PD group were as follows: t(1/2λz) 6.63±1.08 h, C(max) 2.50±0.34 µg/mL, MRT 7.19±0.93 h, and AUC(0-∞) 13.92±2.75 mg/L·h, while in RCO-ßCD group, t(1/2λz) 6.77 ± 0.67 h, C(max) 2.98±0.24 µg/mL, MRT 8.87±0.76 h, and AUC(0-∞) 21.60 ± 1.95 mg/L·h, respectively. The above results indicated that C(max), T(max), AUC(0-t), AUC(0-∞), and MRT in RCO-ßCD group were significantly different from RCO-PD group, and the relative bioavailability of RCO-ßCD group is significantly higher while compared to RCO-PD group (F=156%, with its 90% confidence interval of 145-169%).

Tacrolimus for the treatment of systemic lupus erythematosus with pure class V nephritis.

OBJECTIVES: The treatment of pure membranous (class V) lupus nephropathy remains unsatisfactory. We studied the efficacy and safety of tacrolimus in the treatment of membranous nephritis secondary to SLE. METHODS: We recruited 18 consecutive SLE patients (tacrolimus group) with recently confirmed biopsy-proven class V lupus nephritis. They were treated with a tailing dose of oral prednisolone and tacrolimus 0.1-0.2 mg/kg/day for 6 months, followed by maintenance prednisolone and AZA. The rate of resolution of proteinuria and SLEDAI were compared with 19 historical controls treated with oral cyclophosphamide or AZA (control group). All patients were followed for 12 months. RESULTS: Baseline clinical characteristics were comparable between the groups. For the tacrolimus group, the complete and partial remission rates were 27.8 and 50.0%, respectively at 12 weeks; for the control group, they were 15.8 and 47.4%, respectively (overall chi-square test, P = 0.5). However, tacrolimus group had faster resolution of proteinuria than the control group by the general linear model with repeated measures (P = 0.032). At 12 weeks, proteinuria was reduced by 76.2 +/- 17.0% for the tacrolimus group and 47.1 +/- 51.1% for the control group (P = 0.028). Serial change in renal function and SLEDAI score did not differ between the groups. During the study period, four patients of the tacrolimus group, and 11 of the control group, developed lupus flare (P = 0.027). There was no serious adverse effect in the tacrolimus group. CONCLUSIONS: A 6-month course of tacrolimus is a safe and effective treatment of pure class V (membranous) lupus nephritis. As compared with conventional cytotoxic treatment, tacrolimus possibly results in a faster resolution of proteinuria, and a lower risk of lupus flare within 1 yr. The long-term effect and optimal regimen of tacrolimus require further study.

HIV-1 infected Germans have more variations on neck region of DC-specific intercellular adhesion molecule-3-grabbing nonintegrin than HIV-1 infected Chinese.

The C-type lectins DC-SIGN and DC-SIGNR bind and transmit HIV-1 depending on the tetramer formed by "neck" region and carbohydrate recognition domain (CRD). Recent studies indicated polymorphisms in neck region of DC-SIGNR were more frequent and associated with susceptibility to HIV-1 infection, whereas no similar trends were observed on DC-SIGN for rare variations of DC-SIGN among the researched subjects in those studies. In our present study, we found 9 genotype variations of DC-SIGN neck region among HIV infected Germans and 3 variations among HIV infected Chinese, respectively. Comparison of those variations between Chinese and Germans reveals strong ethnic discrepancies, and no significant evidence indicates those variations have resistance to susceptibility to HIV-1 infection.

Ultrasonic guided percutaneous ethanol injection with or without combined radiofrequency ablation for hepatocellular carcinomas.

OBJECTIVE: The aim of this retrospective study was to evaluate whether radiofrequency ablation (RFA) combined percutaneous ethanol injection (PEI) in the management of hepatocellular carcinoma (HCC) improves treatment outcomes. PATIENTS AND METHODS: We retrospectively included 66 HCC patients who received RFA or RFA plus PEI from February 2011 to January 2014 in Jingmen No. 1 People's Hospital. Moreover, 31 cases received RFA plus PEI as the experiment group and 35 subjects treated with RFA aloe as the control group. The overall survival and treatment related complications were compared between the two groups. RESULTS: For RFA group, the 1-year, 2-year, and 3-year survival rate were 82.0%, 69.3%, and 30.7%, respectively, with the median survival time of 27.1 months. For RFA plus PEI group, the 1-year, 2-year, and 3-year survival rate were 97.1%, 73.9%, and 37.5%, respectively, with the median survival time of 33.6 months. The overall survival of the two groups was not statistical different with the hazard ratio of 1.48 (P > 0.05); three cases of treatment associated complications were found in RFA group with 1 abscess, 1 pleural effusion, and 1 portal vein thrombosis. Moreover, 2 cases of complication were recorded in RFA plus PEI group with 1 pleural effusion and 1 portal vein thrombosis. The complicated incidence rate was not statistical different between the two groups (P < 0.05). CONCLUSION: The combination treatment of HCC was safe and had a slightly higher primary effectiveness rate than RFA alone.

A partial genome assay for quantitative trait loci in wheat (Triticum aestivum) using different analytical techniques.

F1 plants between two intervarietal chromosome substitution lines of European spring wheat varieties, 'Sicco' ('Chinese Spring 5B') and 'Highbury' ('Chinese Spring 5B'), were used to produce 114 doubled haploid lines, 45 by the Hordeum bulbosum technique and 69 by anther culture. These two sets of lines were characterized for variation at a range of morphological, isozyme and RFLP marker loci, and genetic maps were developed with emphasis on chromosomes 6B, 7A, 7B and 7D. A subset of lines, scored for production traits in field trials in 1986 and 1987, were analysed for quantitative trait loci (QTL). The performance of the lines for the quantitative traits studied showed no overall differences due to the method of production of the lines. QTL were located on the linkage map for ear emergence time, height, tiller weight, yield and 50-grain weight using four analytical methods. Many of these effects showed genotype x year interaction.

Attenuation of antigen-induced bronchoconstriction in guinea pigs by a new xanthine derivative (HWA448).

We examined the effect of a new xanthine derivative, HWA448, on antigen-induced bronchoconstriction in actively sensitized guinea pigs. Guinea pigs were sensitized by intraperitoneal injection of bovine serum albumin (BSA) on two occasions, separated by 10 days. Two weeks after the second injection, the animal was placed in a two-chambered whole body plethysmograph and specific airway resistance (SRaw) was monitored for 10 min after an aerosol inhalation of BSA. HWA448 prevented the increase in SRaw after challenge (at 5 and 20 mg/kg i.p.). Aminophylline also prevented the increase in SRaw at 20 mg/kg, but not at a 5-mg/kg dose. The concentration of HWA448, which produced 50% relaxation of the tracheal rings constricted with 0.1 mM of histamine, was 49.9 microM as compared with 18.2 microM in aminophylline. HWA448 has a protective effect on antigen-induced bronchoconstriction in guinea pigs and may be a useful agent in the therapy of bronchial asthma.

Phentolamine inhibits exocytosis of glucagon by Gi2 protein-dependent activation of calcineurin in rat pancreatic alpha -cells.

Capacitance measurements were used to investigate the molecular mechanisms by which imidazoline compounds inhibit glucagon release in rat pancreatic alpha-cells. The imidazoline compound phentolamine reversibly decreased depolarization-evoked exocytosis >80% without affecting the whole-cell Ca(2+) current. During intracellular application through the recording pipette, phentolamine produced a concentration-dependent decrease in the rate of exocytosis (IC(50) = 9.7 microm). Another imidazoline compound, RX871024, exhibited similar effects on exocytosis (IC(50) = 13 microm). These actions were dependent on activation of pertussis toxin-sensitive G(i2) proteins but were not associated with stimulation of ATP-sensitive K(+) channels or adenylate cyclase activity. The inhibitory effect of phentolamine on exocytosis resulted from activation of the protein phosphatase calcineurin and was abolished by cyclosporin A and deltamethrin. Exocytosis was not affected by intracellular application of specific alpha(2), I(1), and I(2) ligands. Phentolamine reduced glucagon release (IC(50) = 1.2 microm) from intact islets by 40%, an effect abolished by pertussis toxin, cyclosporin A, and deltamethrin. These data suggest that imidazoline compounds inhibit glucagon secretion via G(i2)-dependent activation of calcineurin in the pancreatic alpha-cell. The imidazoline binding site is likely to be localized intracellularly and probably closely associated with the secretory granules.