OBJECTIVE:To investigate the permeability of lomefloxacin through blood-pancreatic barrier in rats.METHO-DS:Lomefloxacin(20mg/kg body weight) was injected through caudal vein.At the given time points,the samples were collected.The concentrations of lomefloxacin in the serum,pancreatic tissue and liver tissue were measured by HPLC.RESULTS:The concentration-time profiles of lomefloxacin could be described as two-compartment model in rats.The peak concentrations in serum,pancreatic tissue and liver tissue were 65.550?g/ml,48.801?g/g and 84.121?g/g at 5 min post-injection respectively.Then the concentrations decreased quickly in all of them.Concentrations in pancreatic tissue were higher than those in serum at 10 min and even at 480 min post-injection.The permeation ratio (PR) through blood-pancreatic barrier was 0.744 at 5 min and rose to 3.817 at 480min.CONCLUSION:After intravenous injection,lomefloxacin can permeate blood-pancreatic barrier satisfactory,therefore it is worthy of being recommended for prevention and treatment of pancreatic infections.

Objective:To compare the efficacy and safety between direct anterior approach (DAA) and posterior approach (PA) in total hip arthroplasty.Methods: This study evaluated postoperative results of 92 consecutive total hip arthroplasties performed by a single surgeon;44 from the DAA,and 48 from PA.The age,body mass index,operation time,blood loss,hospital stay,positioning of the artificial hip,postoperative Harris score and postoperative complications were recorded and analyzed.Results: Both the average age of the patients separately (58.0±11.9) years in DAA group and (61.0±10.4) years in PA group and the body mass index (25.1±3.7) in DAA group and (24.7±3.3) in PA group,showed no significant difference between the two groups.The DAA group had significantly reduced the hospital stay (3.8±1.7) days vs.(4.9±2.3) days for the PA group (P<0.05) and operation time was (76.0±17.4) min in DAA group,and (71.0±14.3) min in PA group (P>0.05).The amount of blood loss: in group DAA (238.0±55.3) mL,and in group PA (387.0±61.2) mL (P<0.05).There was no statistical difference in the positioning of the artificial hip: the cup anteversion in DAA group and PA group was 17.3°±5.3° vs.18.6°±5.1°,the cup inclination was 38.5°±5.7° vs.37.7°±5.2°.In DAA group,there was significantly less use of assistive devices [(24.6±7.8) d vs.(31.7±10.2) d,P<0.05],and the pain was significantly lower.Harris score at the end of 6 weeks of the follow-up: in DAA group 85.7±5.4,and in PA group 81.3±6.1 (P<0.05);at the end of the last follow-up: in DAA group 93.4±4.7,and in PA group 92.3±5.3 (P>0.05).Complications were encountered in the two groups.There were two intraoperative complications (4.4％),1 great trochanter fracture and 1 lateral cutaneous nerve injury in DAA group.No dislocation was observed in DAA group.One dislocations and 1 groin pain were recorded in PA group.No prosthesis loosening,deep vein thrombosis,sciatic nerve injury and other complications occurred in the two groups.Conclusion: Total hip arthroplasty using the anterior approach allows for superior recovery and better stability.

OBJECTIVETo investigate the influence of total flavonoids of epimedium (TFE) on the streptozocin (STZ)-induced kidney injury in diabetic rats and discuss the possible mechanism.

METHODSDiabetes was produced by a single injection of streptozocin (40 mg/kg, iv) in male SD rats. The rats were randomly divided into three groups (n = 10): control group, model group and TFE group (100 mg/kg, ig). Animals were sacrificed 12 weeks later. The level of blood glucose, blood urea nitrogen (BUN) and creatinine (Cr) as well as the renal index were determined. Detect the specific biochemical of renal tissue: superoxide dismutase (SOD), malondialdehyde (MDA). Use masson staining to observe the morphology of the renal tissue. Immunohistochemistry was employed to determine the protein levels of transforming growth factor-beta1 (TGF-beta1).

RESULTSCompared to control group, the enhancement of blood glucose, renal index, BUN and Cr was found in model group, which was significantly attenuated by treatment with TFE. Meanwhile, elevated MDA level in renal tissue as well as decreased SOD activities in renal tissue were significantly remitted by TFE. Furthermore, TFE decreased the expression of TGF-beta1.

CONCLUSIONTFE can evidently relieve renal damage in rats with diabetic nephropathy induced by STZ, which might be related to antioxidation and modulating the expression of TGF-beta1 protein.

Animals ; Diabetes Mellitus, Experimental ; metabolism ; Diabetic Nephropathies ; metabolism ; prevention & control ; Epimedium ; chemistry ; Flavonoids ; pharmacology ; Kidney ; drug effects ; metabolism ; Male ; Rats ; Rats, Sprague-Dawley

HIV-1 fusion inhibitors are a new class of anti-HIV compounds, which block the entry of HIV into target cells through preventing the fusion between viral and cell plasma membrane and thus interrupt the initial steps of viral replication. T-20 (enfuvirtide), which has been clinically approved as the first fusion inhibitor of HIV-1 by U.S. FDA in 2003, can suppress replication of HIV variants with multi-drug resistance to reverse transcriptase and protease inhibitors. Peptides and small molecules display potent anti-HIV fusion activities by targeting gp41 thus inhibit its fusogenic function. In recent years, with the development of studies on the molecular mechanism of HIV membrane fusion process and the function of gp41, many new fusion inhibitors are found and some have been in advanced clinical trials. This review discusses recent progress in the development of HIV-1 fusion inhibitors targeting the gp41.
Anti-HIV Agents ; chemical synthesis ; chemistry ; pharmacology ; Drug Resistance, Multiple ; HIV Envelope Protein gp41 ; chemical synthesis ; chemistry ; pharmacology ; HIV Fusion Inhibitors ; chemical synthesis ; chemistry ; pharmacology ; HIV Infections ; drug therapy ; HIV-1 ; drug effects ; physiology ; Humans ; Peptide Fragments ; chemical synthesis ; chemistry ; pharmacology ; Peptides ; chemical synthesis ; chemistry ; pharmacology ; Recombinant Fusion Proteins ; chemical synthesis ; chemistry ; pharmacology ; Virus Replication ; drug effects ; alpha 1-Antitrypsin ; chemical synthesis ; chemistry ; pharmacology

OBJECTIVETo evaluate the effect of exteral use of papaverine cream on enhancement of skin graft.

METHODSFive mini-pigs were used for the study. 20 full-thickness wounds were created on the back of each animal. Along the midline of the abdomen, a 40 cm x 2 cm full-thickness skin graft was harvested and the wound sutured.The full-thickness graft was prepared and trimmed to 2 cm x 2 cm of 0.6 mm thickness split-skin grafts, which were transplanted to each wound with tie-over bolsters. The sutures were removed 2 weeks after the operation. Twelve pairs of 100%-survived skin grafts were selected and divided into group A (the left side) and group B (the right side), with each pair locating on the same and opposite position. From the day of suture removal, 2% papaverine cream was used to group A while plain cream was used to group B. The grafts were measured and observed for healing condition at the time of suture removal and the first, second, third, fourth, fifth, and sixth month. The surface area of the graft was measured and the shrinking ratio was calculated. After the animals were killed at the sixth month, samples of the skin grafts were taken and processed with 10% formalin, routine paraffin wax and Hematoxylin-eosin staining. The tissue structure was observed and the results were analyzed statistically.

RESULTSThe grafts in two groups did not have significant differences at the time of suture removal. Observations from the first to the sixth month showed that the two groups had significant differences in skin graft contracture and histological changes. HE stains demonstrated that the skin grafts in group A had less fibroblasts, more microvessels and orderly-arranged collagenous fibers.

CONCLUSIONSExternal use of papaverine cream can inhabit the contraction of skin grafts. It is a safe, effective, simple, and reliable method,which has the advantages of easy delivery,cheapness, less injury and infection,and no side effects.

Animals ; Contracture ; prevention & control ; Male ; Papaverine ; pharmacology ; Skin Transplantation ; adverse effects ; Swine ; Swine, Miniature ; Wound Healing ; drug effects

Objective The aim is to describe the epidemiological characteristics of Japanese encephalitis(JE) in Sichuan Province from 2008 to 2018, to build time series autoregressive integrated moving average(ARIMA) model, and to discuss the model application in the prediction of JE incidence trends. Methods Descriptive epidemiological analysis was used to analyze the epidemic situation of JE in Sichuan Province from 2008 to 2018. Monthly surveillance data of JE in Sichuan Province from January 2008 to December 2017 were used to fit ARIMA model. The number of reported cases from January to December in 2018 was used to test the model. Results The epidemic situation of JE in Sichuan Province from 2008 to 2018 showed a downward trend, and eastern and southern areas were the highly prevalent areas. The incidence peak was from July to September every year. Children were the high-risk group, but the incidence of adolescent and adult was on the rise in recent years. ARIMA(1,0,0)(2,1,0)12 could appropriately fit the time series. Conclusion ARIMA model can be used for short-term prediction of the reported incidence of JE in Sichuan Province.

A rapid UPLC method for simultaneous determination of protocatechuic acid, coumarin, cinnamic alcohol, cinnamic acid and cinnamaldehyde in Cinnamomi Ramulus was established. The optimal conditions of separation and detection were achieved on an HSS T3 Column (2.1 mm x 100 mm, 1.8 microm) eluted with a gradient of acetonitrile and 0.05% aqueous phosphoric acid, at a flow rate of 0.5 mL x min(-1), detected at 254 nm. The linear response ranges of protocatechuic acid, coumarin, cinnamic alcohol, cinnamic acid and cinnamaldehyde were 0.359-3.59 mg x L(-1) (r = 0. 999 3), 2. 834-28.34 mg x L(-1) (r = 0.999 8), 0.574-5.74 mg x L(-1) (r = 0.999 8), 2.400-24.00 mg x L(-1) (r = 0.999 9), 32.57-325.7 mg x L(-1) (r = 0.999 8), respectively (n = 6). The mean recoveries (n = 9) of the five components were 96.7%-101.0%, RSD < 2.3%. The assay demonstrates that the method has adequate accuracy and selectivity to measure the concentration of protocatechuic acid, coumarin, cinnamic alcohol, cinnamic acid and cinnamaldehyde in Cinnamomi Ramulus.
Acrolein ; analogs & derivatives ; analysis ; Chromatography, Liquid ; methods ; Cinnamates ; analysis ; Cinnamomum ; chemistry ; Coumarins ; analysis ; Drugs, Chinese Herbal ; chemistry ; Hydroxybenzoates ; analysis ; Propanols ; analysis

OBJECTIVETo investigate the effects of static magnetic fields (SMFs) with different exposure time on the maturation of rat osteoblasts in vitro and the expression of the estrogen receptor (ER) gene.

METHODSThe calvarial osteoblasts were isolated from newborn rats by enzyme digestion and randomly divided into 9 groups after one passage based on the exposure time of the SMFs[0 (control), 0.5 h, 1.0 h, 1.5 h, 2.0 h, 2.5 h, 3.0 h, 3.5 h, and 4.0 h]. The intensity was 3.9 mT in all SMFs. Those without SMFs exposure were used as the controls. The oeteoblasts were observed under the contrast phase microscope on a daily basis. After 48 h, cell proliferation was assayed by MTT method. The osteocalcin contents were measured after exposure to SMFs for 3 d, 6 d, 9 d, and 12 d. ERΑ and ERΒ mRNA expressions were measured by real-time PCR after SMFs treatment for 0 h, 24 h, 48 h, and 72 h.

RESULTSCompared with the controls, the cell proliferation was significantly enhanced in the 2.0-h, 2.5-h, and 3.0-h groups (P<0.05). After SMFs treatment for 6 d, 9 d and 12 d, the 2.5-h group had significantly higher osteocalcin content than the control group did (P<0.05). After SMFs treatment for 0 h and 72 h, elevated ERΑ mRNA expression and reduced ERΒ mRNA expression were observed.

CONCLUSIONExposure to SMFs, regardless of exposure time, is associated with enhanced cell proliferation, increased osteocalcin contents, and altered ERΑ and ERΒ mRNA expressions in opposite directions.

Animals ; Cell Differentiation ; Cell Proliferation ; Cells, Cultured ; Magnetic Fields ; Osteoblasts ; cytology ; metabolism ; Rats ; Receptors, Estrogen ; genetics ; metabolism

In order to improve the laboratory identification ability of Lodderomyces elongisporus, we analyzed the main biological characteristics of Lodderomyces elongisporus isolated from peripheral venous blood and catheter blood of a brain stem infarction patient with a body temperature of 38.4 ℃, observed the colony color of the strain on CHROMagar Candida medium and the ascospores on Mcclary agar, identified the isolates with Vitek 2 compact, MALDI-TOF MS and sequence analysis, and tested the MICs with borth microdilution. The MICs of antifungal agents against Lodderomyces elongisporus are well below the normal values of these drugs. The central venous catheter was removed and antifungal drugs were used until two weeks after the last positive blood culture. During the medication perios, the blood culture was repeatedly negative, the patient had no fever and the infection index decreased to normal, which can be used for clinical reference.

Objective:To study the efficacy of direct intrahepatic portosystemic shunt (DIPS) in treatment of Budd-Chiari syndrome (BCS).Methods:From January 1, 2015 to June 31, 2017, consecutive patients with BCS who were treated with DIPS at the Department of Interventional Therapy of Beijing Shijitan Hospital, the Liver Disease Research Center of Beijing Friendship Hospital and the General Surgery Department of Beijing Ditan Hospital were retrospectively analyzed. The symptoms, physical signs (including abdominal distension, ascites, pleural effusion, splenomegaly, hepatic encephalopathy) and perioperative laboratory results of these patients were collected and analyzed. Biochemical indicators including alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin (TBil), direct bilirubin (DBil), and portal pressure gradient were compared before and 2 weeks after treatment. The patients were followed up for at least 3 years to assess their clinical symptoms, patency of shunt, oncological status and survival.Results:Of 67 patients with BCS who were included in the study, there were 45 males and 22 females, aged (38.12±23.22) years. The BCS classification of these patients were hepatic vein type ( n=65), including 62 patients with complete hepatic vein obstruction, 3 patients with hepatic vein occlusion due to thrombosis, and 2 patients with mixed hepatic vein and inferior vena cava occlusion. All 67 patients underwent DIPS with 93 stents being implanted. In addition, 43 patients underwent gastric coronary vein embolization, and 2 patients with mixed type of BCS underwent inferior vena cava stenting. The portal pressure gradient decreased from (22.17±9.16) mmHg (1 mmHg=0.133 kPa) to (9.87±4.75) mmHg, the difference was statistically significant ( P<0.05). Abdominal distension was relieved, at one month and ascites completely subsided in 3 months after operation. The liver congestion and swelling were obviously relieved. Comparison of patients 2 weeks after operation and before operation, ALT decreased from (65.28±27.75) U/L to (28.43±13.46)U/L, AST from (68.75±29.23) U/L to (26.92±13.33)U/L, TBil from (175.31±80.48)μmol/L to (45.08±26.54)μmol/L, DBil from (127.55±44.65)μmol/L to (35.12±10.77)μmol/L, and albumin increased from (31.56±7.22) g/L to (44.18±11.36)g/L, the difference was statistically significant (all P<0.05). All patients were followed up for at least 3 years. Shunt stenosis was detected in 5 patients (7.46%) with shunt expansion being performed, variceal bleeding in 2 patients (2.99%), ascites recurrence in 4 patients (5.97%) and hepatic encephalopathy in 2 patients (2.99%). No patients were diagnosed with hepatic cancer, and no patients died. Conclusion:DIPS was efficacious, safe and reliable to that BCS patients. It rapidly reduced portal venous pressure, relieved liver congestion, and restored liver morphology and liver function in these patients.