Objective: To prepare ibuprofen dispersible tablet and compare its pharmacokinetics and bioavailability with market tablets in rabbits. Methods: According to inspection of factors and orthogonal design, optimal formulation was decided. A randomized crossover and self control design was used. Eight healthy rabbits were single oral dosed with 100 mg ibuprofen dispersible tablet or market tablet, respectively. The plasma drug concentration was determined by HPLC method. The pharmacokinetic parameters were calculated by 3P87 program and the bioequivalence was assessed by NDST5.0 program. Results: A one compartment open model was adopted and the pharmacokinetic parameters of dispersible tablet and market tablet were as follows: c max were (9.79?2.25) and (4.54?1.50) ?g/ml; t max were (0.27?0.07) and (2.03?0.53) h; t 1/2 were (6.65? 2.14) and (9.17?4.38) h; AUC 0~∞ were (94.11?28.38) and (65.20?18.38) ?g?h?ml -1 , respectively. Ralative bioavailability of the dispersible tablet was 164.11% compared to market tablet. Conclusion: Ibuprofen dispersible tablet is administrated easily and absorbed quickly, and its bioavailability is far more better than the market one. [

ATP (Adenosine triphosphate) is an important endogenous damage-associated molecular pattern (DAMP). P2X7R is an ATP-gated cation channel. ATP-P2X7R plays a vital role in the pathophysiology of many diseases because P2X7R is distributed on various immune cells. ATP-P2X7R signal transduction pathway has been implicated to participate in the body's im-mune defense against pathogens. This paper reviews the recent progress regarding ATP-P2X7R and its effects on parasitic diseas-es.

Objective To investigate the protective effect of hypoxia-inducible factor-1α(HIF-1 α) on the neurovascular unit in rats with traumatic brain injury (TBI).Methods The fluid percussion model was applied to induce TBI in rats.A total of 600 rats were divided into sham operation group,TBI group,TBI + HIF-1 α silence group and TBI + control virus group according to the random number table,with 150 rats in each.Virus-mediated HIF-1 α silence gene and control virus were delivered 24 h before the fluid percussion injury.After 3,7 and 14 d,brain injury area and morphological changes in injured region were detected by HE staining,expressions of vascular endothelial cell markers (vWF) and HIF-1 α were detected by Western blot method,and expressions of vascular endothelial growth factor (VEGF),matrix metalloproteinase-9 (MMP-9),tumor necrosis factor-α (TNF-α),interleukin 6 (IL-6) and nuclear factor-κB (NF-κB) in peripheral blood and brain tissue were detected by ELISA method.Rat neural function was dynamically assessed using the modified neurological severity score (mNSS).Results (1) Brain injury area and edema area in TBI + HIF-1 α silence group were higher than those in TBI group at all time points (P ＜ 0.05).(2) Compared with sham operation group and TBI + control virus group,expression of HIF-1α in TBI group gradually increased and remained high at 7 and 14 d postinjury (P ＜ 0.05).Compared with TBI group,expression of vWF in TBI + HIF-1αsilence group decreased at all time points (P ＜ 0.05) and inhibited angiogenesis.(3) TBI + HIF-lα silence group versus TBI group showed remarkably decreased VEGF at all time points,increased expressions of TNF-α,IL-6 and NF-κB at all time point,and increased expression of MMP-9 at 7 and 14 d postinjury (all P ＜0.05).(4) TBI + HIF-1α silence group versus TBI group showed significant difference in mNSS at 7 and 14 d postinjury (all P ＜ 0.05).Conclusions After TBI,high expression of HIF-1αcan facilitate vascular formation and inhibit inflammatory reaction related factor expression,inducing the mitigation of brain edema and brain injury.Therefore,promoting HIF-1α expression may become a new means to improvement of neurovascular function after TBI.

Objective To explore the effect of 1-alpha,25-dihydroxy-cholecalcifero(1,25(OH)2D3)on liver fibrosis and its mechanism. Methods Degree of liver fibrosis was assessed through pathological detection and blood biochemical examination of liver function. Immunohistochemical assay was used to detect expressions of α-SMA,TGF-βand collagen I to observe activation level of hepatic stellate cells. Impact of 1,25(OH)2D3 on CD4+T cell differentiation was analyzed by flow cytometry,ELISA,and RT-PCR. Results 1,25(OH)2D3 improved the structure of the liver tissue and liver fibrosis. Expressions of collagen I ,TGF-βandα-SMA were significantly ele-vated in the liver tissue in rats with fibrosis(P < 0.05)but were markedly decreased after treatment with 1,25 (OH)2D3(P < 0.05). After 1,25(OH)2D3 treatment,the proportion of Th17 cells reduced while that of Th2 in-creased;concentration levels of IFNγ,IL-17A,and IL-22 markedly declined but IL-4 elevated(P>0.01);and ex-pressions of RORγt and T-bet decreased whereas GATA3 expression increased(P>0.01);as compared with those in the control group. Conclusions 1,25(OH)2D3 can alleviate the degree of liver tissue by lowering HSC activation and regulating Th cell differentiation.

Objective To observe the clinical features and prognosis of endogenous bacterial endophthalmitis (EBE).Methods Ten eyes of 10 patients diagnosed with unilateral EBE were retrospectively reviewed,including 7 males and 3 females.The mean age was 57.6± 10.8 years old.Eight patients were with diabetes and 7 of them were diagnosed over 5 years.There were 3 patients with hepatocirrhosis,1 patient with hypertension,and 1 patient with coronary disease.Nine cases had infectious diseases,including liver abscess (7 cases),pulmonary infection (3 cases),erysipelas (1 case) and perianal abscess (1 case).Seven cases had fever history.Culture and drug sensitive tests for aerobic bacteria,anaerobic bacteria and fungal were performed for 9 eyes using vitreous samples from the procedures of vitrectomy and/or intravitreal injection.All patients were treated with broad-spectrum antibiotics and adjusted for drug use according to microbiological culture and drug sensitivity test results.After the diagnosis was established,vitrectomy combined with lens removal was performed in 5 hours (3 eyes) and 24 hours (5 eyes);Vitreous tamponade of C3F8 (1 eye) and silicone oil (7 eyes) was used;At the end of the operation,0.1 ml vancomycin (1 mg) and 0.1 ml ceftazidime (1 mg) were injected into the vitreous cavity.One eye received intravitreal injection of 0.1 ml vancomycin (1 mg) and 0.1 ml ceftazidime (mg),one eye received evisceration.During the follow up period from 6 to 24 months,visual function,slit lamp and fundus examinations were performed at each office visit.Results All patients complained of blurred vision and 5 patients had ocular pain.The visual acuity was no light perception (3 eyes),light perception (5 eyes);hand motion (1 eye) and 0.1 (1 eye).Corneal edema was found in all 10 eyes;hypopyon in 8 eyes;diffuse vitreous opacity in 10 eyes,including 3 eyes with retinal detachment.For 8 eyes treated by vitrectomy and intravitreal injection,1 eye was eviscerated due to uncontrolled inflammation.The eye treated with intravitreal injection was enucleated for its uncontrolled inflammation.For 9 eyes received vitreous culture and drug testing,8 eyes (88.9％) had positive results,including 5 eyes with Klebsiellar pneumonia,and 1 eye with Staphylococcus aureus,or Streptococcus agalactiae or Enterococcus faecalis respectively.At last office visit,2 eyes were with no light perception;4 eyes were with hand motion;and 1 eye with visual acuity of 0.1.Conclusions Most of the patients with endogenous bacterial endophthalmitis have systemic predisposing factors.Klebsiella pneumoniae is the leading cause of ocular EBE.Vitrectomy combined with intravitreal injection of antibiotics showed efficacy in treating EBE.

Objective To study the effect of simvastatin (SIM) on the expression of neuron specific enoalse (NSE) in rat brain and serum after traumatic brain injury (TBI), and therapeutic effects of SIM on TBI thereof. Methods A total of 90 Sprague-Dwalye (SD) rats aged 8 weeks were randomly divided into sham TBI group, control group and treatment group (n=30). The TBI model was established in control group and treatment group by using Feeney method. Rats in treatment group were fed SIM 10 mg/kg in the evening pre-injury and in every evening post-injury while those in control group were fed the same dose of starch at the same time. Blood samples (3 mL) were collected from carotid atrery in three groups, then rats were sacrificed and brains were collected at different time points (3 h, 12 h, 24 h, 3 d, 7 d and 14 d post-injury). The serum ex-pressions of NSE were detected by ELISA method. The NSE expressions in hippocampal area CA3 were detected with immu-nohistochemistry. Results (1) In control group, the serum NSE level was significantly increased at 3 h after injury, reached the peak at 3 d, and was still higher than that of sham injury group at 14 d. In treatment group, the serum NSE level was in-creased 3 h after injury, reached the peak at 24 h, decreased after 3 d, and was near the sham injury group at 14 d after inju-ry, but was significantly lower than that of control group. (2) Immunohistochemical detection showed that the NSE optical density values in hippocampal area CA3 area were decreased at 3 h after injury in control group. The optical density values reached the lowest level between 3 d to 7 d and were still significantly lower than those of sham injury group at 14 d. In treat-ment group the optical density value was decreased at 3 h after injury, reached the lowest level between 12 h to 24 h and re-bounded significantly at 7 d, then at 14 d up to the level of sham injury group. Conclusion SIM can promote the decrease of serum NSE level in TBI rats and increase the NSE expression of hippocampal neurons of injured side, showing protective effects on neuronal damage after traumatic brain injury.

This study was aimed to establish a rapid discrimination method of Pinellia ternataand its adulterants based on the odour fingerprints analysis.Typhonium flagelliforme and Arisaema Rhizome,which were the common adulterants of Pinellia ternata,were collected.The adulterants were mixed with Pinellia ternatain different proportions.E-nose technology was used to obtain the odour fingerprints of Pinellia ternataand its adulterants of different types and proportions.Chemometrics methods,such as the analysis of variance (ANOVA),principal component analysis (PCA) and discriminant factor analysis (DFA) were used in the analysis and discrimination on sensors response data collected by sensors.The results showed that there were obvious differences on the odour characteristics between Pinellia ternateand its adulterants.PCA can obviously discriminate Pinellia ternateand its adulterants.And the odour difference became obvious along with the increasing of the adulteration proportion.There was a linear relationship between e-nose signal and the proportion of Typhonium flagelliforme.The cumulative proportion in ANOVA of the DFA model was 100%.The correct recognition rate was not less than 97%.It was concluded that e-nose can be used for rapid discrimination of Pinellia ternataand its adulterants.This study provided new technology and method for the discrimination of adulterants of Chinese materia medica.

Rhizoma Pinelliae Fermentata(RPF)wasoneofthecommonlyusedChinesemateriamedica(CMM). According to the ancient and modern literatures on RPF, the historical evolution, fermentation methods, chemical compositions, efficacy and microbes of RPF were systematically summarized in this paper. Through the analysis on existing problems of fermentation strains, effective components, quality standard and fermentation process, the corresponding solutions were proposed. This work may provide an idea and reference for the further study of RPF.

Radiotherapy is a treatment for cancer with undesired by-effects. In order to develop a new radiation protective agent that could reduce the by-effects, we tried to express and purify human cryptochrome 1 (hCRY1). The coding sequence of hCRY1 was inserted into prokaryotic expression plasmid pET28a(+), and this protein was purified from Escherichia coli BL21(DE3) after IPTG induction, ultrasonication, inclusion body dissolution, gradient dialysis, nickel column purification and ultrafiltration. The yield of hCRY1 in 1 L E. coli culture (LB medium) was about 10-15 mg. The radiation protective efficiency of hCRY1 was monitored by detecting X-ray-induced H2A.X foci in HaCaT cells. The results of immunofluorescence show that hCRY1 significantly reduces X-ray stimulated DNA damage response. The apoptosis of HaCaT cell was also detected, and the repression of H2A.X foci formation was not due to hCRY1's cytotoxity. All these data suggest a potential application of recombinant hCRY1 as a protective agent for radiotherapy.
Cryptochromes ; biosynthesis ; Escherichia coli ; Humans ; Plasmids ; Radiation-Protective Agents ; Recombinant Proteins ; biosynthesis

Estrogen receptors are steroid receptors, widely distributed in skeletal muscle, liver and other tissues.Currently, there are 5 known estrogen receptors.Different estrogen receptors are distributed in different places and have different functions.By mediating different estrogen receptors, estrogen plays an important role in anti-inflammation, promoting proliferation and inhibiting muscle atrophy.Skeletal muscle is the main tissue in the human body, accounting for about 40% of body weight.Skeletal muscle not only plays the role of exercise and support, but also plays an important role in maintaining the body′s metabolism.In recent years, estrogen receptors have received extensive attention in skeletal muscle diseases.Estrogen receptors are considered as potential targets for the treatment of skeletal muscle diseases such as Duchenne muscular dystrophy(DMD)and myotubular myopathy(MTM). This article reviews the research progress of estrogen receptors in skeletal muscle diseases.