Objective: To investigate the activity of mono-tetrahydrofuran (THF) annonaceous acetogenins (ACGs) against mitochondrial complex I of rats. Methods: The inhibitory activity of mono-THF ACGs with six different chemical structures against mitochondrial complex I of rats was investigated to clarify the carbon number and substituted hydroxyl number between THF ring and lactone ring as well as the effect of the core configuration in THF ring on mitochondrial complex I of rats. Results: The results show that mono-THF ACGs can inhibit the mitochondrial complex I of rats. With analysis of the results from the structure-activity relationship between antitumoral activity and their chemical structure of mono-THF ACGs, the less the carbon number between the two rings is, the better their inhibitory activities are; The number of substituted hydroxyl groups is not the decisive factor for influencing its activity in mono-THF ACGs. Conclusion: The inhibitory activity of compound's configurations with th/t/er is better than that of the compound's configurations with th/t/th in mono-THF ACGs.

Objective:To explore the effects of omeprazole combined with somatostatin on intra-abdominal pressure and intestinal mucosal barrier function of elderly patients with severe acute pancreatitis.Methods:Selected 82 cases of elderly patients with severe acute pancreatitis from our hospital.They were divided into research group (48 cases) and control group (34 cases).The control group was treated with basic therapy,and the research group was treated with omeprazole combined with somatostatin on the basis of the control group.Analyzed and compared the clinical effects,intestinal mucosal barrier function and symptom indexes of patients in the two groups.Results:①The total effective rate of the research group was significantly better than that of the control group,and the difference was statistically significant (P=0.005).②After treatment,the D-lactose and diamine oxidase (DAO) levels of both groups were significantly lower than before treatment,and the difference was statistically significant (both P＜0.001).In addition,after treatment,the D-lactose and DAO levels were significantly lower in the research group than in the control group,and the differences were statistically significant (mean P ＜ 0.001).③After treatment,patients of the research group showed better results in abdominal pain and abdominal distension relief time,bowel recovery time,hospital stay and blood amylase index than those in the control group,and the difference was statistically significant (mean P ＜ 0.001).④After treatment,the intra-abdominal hypertension of two groups was significantly lower than before treatment,with statistical difference (P ＜ 0.001).Yet it was significantly lower in the research group than in the control group,with statistical difference (P ＜ 0.001).Conclusion:The combined treatment of omeprazole and somatostatin can effectively improve the clinical efficacy of severe acute pancreatitis in elderly patients,correct intra-abdominal hypertension and improve the intestinal mucosal barrier function of patients,so it is worthy of reference and promotion.

OBJECTIVE To develop a non-paper,interactive,multiplex medium way,and to obtain the information disinfection protection on second level of time.METHODS Using the computer,the touchscreen,the personal digital assistant(PDA),the general packet radio service(GPRS),the pronounciation(man-machine conversation),the video frequency and the other advanced technology methods,to study and develop an electronic version of intelligent search engine system for disinfection protection.RESULTS Touching namely attained the applied and guided information,such as to fulfil exactly the disinfection technology standard for the medical workers in medical establishments,to provide the post work instruction;to correctly guide the disinfection protection for common family;and to build the communication platfrom with the enterprisers in order to meet the demand for disinfection protection appliances from the society,hospital and family.CONCLUSIONS The intelligent search engine system is feasible applying to use.

Objective To evaluate the 80 mm volume shuttle cerebral CT perfusion(CTP) and 4D-CT angiography (CTA) in patients with stenosis or occlusion in Willis circle.Methods Conventional cerebral plain CT, 80 mm CTP and dynamic 4D-CTA were performed in 55 patients with unilateral MCA/ ICA stenosis or occlusion.The parameter maps of cerebral blood flow (CBF), cerebral blood volume (CBV), mean transit time (MTT) and time to peak (TTP) were analyzed.Meanwhile dynamic 4D-CTA images were also obtained.The significance of the differences of CBF, CBV, MTT and TTP between the affected side and the contralateral side was assessed using K Independent Samples analysis.Results In 40 patients with unilateral stenosis or occlusion of MCA/ICA, CTP was found abnormal in 36 patients.MTT and TTP of affected side [(7.18 ±1.34), (19.65 ±1.81) s] were significantly prolonged compared to contralateral side [(5.22±1.14) s, (17.62±1.65) s, X~2 =30.833,25.817, P<0.017].Centrum ovale or parietal lobe ischemic lesions were observed in 16 patients on CTP.In 15 patients with bilateral stenosis or occlusion of MCA/ICA, CTP was observed abnormal in 10 patients.CBF, CBV, MTT and TTP of affected side [(42.85 ±6.09) ml·100 g~(-1)·min~(-1), (2.63 ±0.42) ml·100 g~(-1), (11.27 ±1.43) s, (21.07 ±1.44) s)] were significantly different from those of contralateral side [(71.20 ±6.30) ml·100 g~(-1)·min~(-1), (2.29 ±0.15) ml·100 g~(-1), (3.38 ±0.61) s, (17.64 ±1.70) s (X~2 =17.314, 5.913,17.334,13.834,P<0.017)].On 4D-CTA covering 80 mm (0.625 mm×l28), unilateral stenosis of MCA were observed in 22 patients (13 right MCA and 9 left MCA), unilateral occlusion were observed in 5 patients (1 right MCA and 4 left MCA) and bilateral MCA stenosis/occlusion were observed in 9 patients.4D-CTA covering Willis cycle can display stenosis/occlsion of MCA as same as conventional CTA and DSA.Conclusion 80 mm volume shuttle CTP and 4D-CTA provide valuable information about the hemodynamic changes and the abnormalities of intracranial artery in patients with MCA/ICA stenosis or occlusion.

Objective To summarize clinical characteristics, prevention and treatment of postoperative chronic hyponatremia after liver transplantation(LT). Methods Clinical data of 26 patients presenting with chronic hyponatremia after LTwereretrospectivelyanalyzed.BaselinedataandmaincomplicationsofpatientswithhyponatremiaafterLTwererecorded. Thecorrelationbetweenpostoperativelengthofhospitalstayandthedurationofhyponatremiawasanalyzed.Clinicaltreatment and prognosis were summarized. Results Among 26 patients, the median blood sodium concentration was 131 mmol/L (range 125 to 133 mmol/L). Al patients were diagnosed with mild or moderate degree of hyponatremia. Main complications included pulmonary infection (n=13, 50%), acute rejection of liver graft (n=7, 27%) and digestive tract hemorrhage (n=7, 27%). Postoperative length of hospital stay was correlated with the duration of hyponatremia. After ful evaluation of patient's conditionandexcludingthepotentialinducers,aportionof3%ofhypertonicsalinewasadministeredviagastro-intestinaltract and/or vein. After positive treatment, 23 cases (88%) were healed and 3 (12%) died from infection complicated with multiple organ failure. Conclusions After LT, the incidence of chronic hyponatremia is low with mild severity. Postoperative length of hospitalstayiscorrelatedwiththedurationofhyponatremia.Thekeyoftreatmentistotimelyexcludetheinducers,correctthe low level of sodium based upon the individual principles and prevent the incidence of postoperative complications.

OBJECTIVETo explore the effect of KIR/HLA ligand matching which mediates activated or inhibitory signal pathways on acute rejection (AR) after kidney transplantation.

METHODSHLA and KIR genotype assortments were analyzed in 53 donor/recipient pairs of kidney transplantation. The recipients were divided into AR group (GI, n=19) and stable renal function group (GII, n=34) based on the early graft function. The impact of donor HLA, recipient KIR and distinct KIR/HLA class I ligand combinations on acute rejection after kidney transplantation was studied.

RESULTSNo significant differences were found in donor HLA-C1/2, HLA-A3, HLA-A11, or HLA-Bw4 between GI and GII groups. The frequency for KIR2DL2/2DS2 and KIR genotype assortment (AA) of the recipients in GI group were significantly lower than that in GII group (26.3% vs 55.9%, P=0.038; 31.6% vs 67.6%, P=0.011). The incidence of AR was significantly lower in donor HLA-C1/1 than in non-C1/1 (31.6% vs 46.7%, P>0.05), and lower in recipient KIR genotype assortment (AA) than in non-AA (20.7% vs 52.2%, P=0.011). A significant higher number of matches for the KIR2DL2/ HLA-C1 and KIR2DL3/HLA-C1 were observed in GII group (P=0.030, P=0.028).

CONCLUSIONDistinct KIR/HLA class I ligand combinations between the donor and recipient (such as KIR2DL2/ HLA-C1 and KIR2DL3/HLA-C1) may reduce the incidence of AR. A good KIR/HLA class I ligand matching will benefit the survival of the renal allograft.

Adolescent ; Adult ; Female ; Graft Rejection ; immunology ; Graft Survival ; immunology ; HLA Antigens ; immunology ; Humans ; Kidney Transplantation ; adverse effects ; immunology ; Ligands ; Male ; Middle Aged ; Receptors, KIR ; immunology ; Retrospective Studies ; Signal Transduction ; Young Adult

AIMA series of triazole antifungal agents were synthesized to search for novel triazole antifungal agents with more potent activity, less toxicity and broader spectrum.

METHODSTwenty-one 1-(1H-1, 2, 4-triazolyl)-2-(2, 4-diflurophenyl)-3-(4-substituted-1-piperazinyl)-2-propanols were synthesized, on the basis of the three dimensional structure of P450 cytochrome 14alpha-sterol demethylase (CYP51) and their antifungal activities were also evaluated.

RESULTSResults of preliminary biological tests showed that most of title compounds exhibited activity against the eight common pathogenic fungi to some extent and the activities against deep fungi were higher than that against shallow fungi. In general, phenyl and pyridinyl analogues showed higher antifungal activity than that of the phenylacyl analogues.

CONCLUSIONSeveral title compounds showed higher antifungal activities than fluconazole and terbinafine. Compound VIII-1, 4, 5 and IX-3 showed the best antifungal activity with broad antifungal spectrum and were chosen for further study.

Antifungal Agents ; chemical synthesis ; chemistry ; pharmacology ; Aspergillus fumigatus ; drug effects ; Candida albicans ; drug effects ; Cryptococcus neoformans ; drug effects ; Fluconazole ; pharmacology ; Microbial Sensitivity Tests ; Molecular Structure ; Naphthalenes ; pharmacology ; Structure-Activity Relationship ; Triazoles ; chemical synthesis ; chemistry ; pharmacology

This study was aimed to explore the prognostic significance of telomere length in patients with chronic lymphocytic leukemia (CLL) and to analyze relation of telomere length with Binet stage, IgVH mutation status, CD38, ZAP-70 expression as well as other clinical features. 35 CLL patients who contained 80% or more tumor cells in the peripheral blood or bone marrow samples were selected as objects studied, while 13 healthy donors were served as normal controls. The telomere relative length was detected by using a real-time fluorescent quantitative polymerase chain reaction method (qPCR); the expression of CD38 and ZAP-70 protein were detected by flow cytometry, the IgVH mutation was detected by multiplex PCR. The results showed that the mean telomere relative length in CLL patients and normal controls were 0.384 and 0.443 respectively, but the difference between them was not significant (p > 0.05). The telomere length was significantly correlated with Binet stages and IgVH mutation status. Patients in Binet stage B and C showed significantly shorter telomeres than those in Binet stage A (p = 0.001). Mean telomere relative lengths in patients without IgVH mutation were shorter than those in patients with IgVH mutation (p = 0.015). No relation of telomere length with sex, age, ZAP-70 protein and CD38 were found (p > 0.05). It is concluded that telomere length may have a prognostic significance for CLL patients. Combining telomere length and IgVH mutation status may achieve a better prognostic subclassification for CLL patients.
ADP-ribosyl Cyclase 1 ; metabolism ; Adult ; Aged ; Aged, 80 and over ; Case-Control Studies ; Female ; Humans ; Leukemia, Lymphocytic, Chronic, B-Cell ; genetics ; metabolism ; Male ; Middle Aged ; Mutation ; Prognosis ; Telomere ; chemistry ; genetics ; metabolism ; ZAP-70 Protein-Tyrosine Kinase ; metabolism

To simplify the traditional method for cryopreservation of peripheral blood stem cells(PBSCs) at -196 degrees C with rate-controlled freezing with 10% dimethyl sulfoxide(DMSO), the simplified method was carried out by freezing the cells to -80 degrees C in low-temperature freezer with the combination of 5% DMSO, 3% hydroxyethyl starch(HES) and 4% human serum albumin(HSA) as cryoprotectant. PBSCs were cryopreserved by different methods. Cell viability and recovery rate of mononuclear cells (MNC), CFU-GM and CD34(+) cells were compared. It was observed that the higher MNC and CFU-GM recovery rates were achieved and without agglutination with the simplified method. It was also found with this simplified method, satisfactory recovery rates of CFU-GM and CD34(+) cells could be obtained when PBSCs were preserved at -80 degrees C as long as 24 months. There was no difference observed in parameters of cryopreserved PBSCs thawed at 37 degrees C and 20 degrees C. After the cells being exposed to 5% DMSO at room temperature for 1 hour, the cell viability decreased from 93.2% to 84.5%, however, the CFU-GM recovery rate was not decreased. It is concluded that the simplified cryopreservation technique is better and simpler than the traditional crypreservation method, will be useful for institutions without rate-controlled freezing facility. Moreover, this method diminishes the amount of DMSO infused into patients, thus decreasing its toxicity.

Spontaneous transient outward currents (STOCs) play an important role in the myogenic regulation of small artery tone, such as coronary artery. In the present study, we investigated the electrophysiological properties and the regulation of STOCs in vascular smooth muscle cells (VSMCs) of porcine coronary artery by perforated patch-clamp technique. Our data showed that STOCs were dependent on voltage and extracellular calcium and they were highly variable in amplitudes and frequencies. STOCs superimposed stochastically onto whole-cell K(+) currents induced by step and ramp protocols. STOCs were completely abolished by ChTX [inhibitor of large-conductance Ca(2+)-activated potassium (BK(Ca)) channels], removal of extracellular Ca(2+), or addition of ryanodine (50 mumol/L) respectively. In contrast, CdCl2 and verapamil, inhibitors of voltage-dependent L-type Ca(2+) channels, had little effect on STOCs. Caffeine (5 mmol/L) transiently increased STOCs (hump), followed by a temporary inhibition. Ca(2+) ionophore A23187 increased both amplitude and frequency of STOCs. Na(+) ionophore monensin increased the frequency of STOCs. STOCs were strongly inhibited by KB-R7943, a selective inhibitor of the reverse mode of the Na(+)/Ca(2+) exchanger. Based on these observations, we conclude that STOCs are mediated by BK(Ca) channels. The generation and activation of STOCs depend upon Ca(2+) influx through Na(+)/Ca(2+) exchange and release of Ca(2+) from sarcoplasmic reticulum (SR) via ryanodine receptors. This suggests that Na(+)/Ca(2+) exchange determines calcium store refilling. Recycling of entering Ca(2+) from superficial SR may locally elevate Ca(2+) concentration at the plasma membrane, thereby activating BK(Ca) channels and then initiating STOCs.
Animals ; Coronary Vessels ; cytology ; physiology ; Electrophysiological Phenomena ; physiology ; Muscle, Smooth, Vascular ; cytology ; physiology ; Myocytes, Smooth Muscle ; cytology ; physiology ; Patch-Clamp Techniques ; Potassium Channels, Calcium-Activated ; physiology ; Sodium-Calcium Exchanger ; physiology ; Swine