OBJECTIVETo observe the effect of Wenyang Huoxue Lishui Recipe (WHLR) containing serum on the expression of cathepsin L (CatL) in puromycin aminonucleoside-induced injury of mouse glomerular podocytes.

METHODSMouse podocyte cells (MPCs) in vitro cultured were divided into the normal control group, the model group, the dexamethasone (DEX) group, 10% WHLR containing serum group, 20% WHLR containing serum group, the vehicle serum control group. MPCs in the normal control group were cultured at 37 degrees C culture solution for 24 h. 45 mg/L puromycin was acted on MPCs in the model group for 24 h. On the basis of puromycin intervention, 1 limol/L DEX was co-incubated in MPCs of the DEX group for 24 h; 10% or 20% WHLR containing serum was co-incubated in MPCs of the 10% WHLR containing serum group and 20% WHLR containing serum group for 24 h. The vehicle serum control group was also set up by incubating with WHLR containing serum alone for 24 h. The expression of CatL and its substrate Synaptopodin in podocytes were detected by cell immunofluorescence staining. FITC-conjugated phalloidin was used to stain F-actin. A cortical F-actin score index (CFS index) was designed to quantify the degree of cytoskeletal reorganization in cultured podocytes.

RESULTSCompared with the normal control group, the expression of synaptopodin significantly decreased and the expression of CatL significantly-increased in the model group. F-actin arranged in disorder, gradually forming pericellular F-actin ring. CFS index was obviously elevated (P < 0.01). Compared with the model group, the epression of synaptopodin increased, the expression of CatL decreased, and CFS index also decreased in the DEX group, 10% WHLR containing serum group, and 20% WHLR containing serum group (P < 0.05, P < 0.01). Compared with the DEX group, the expression of synaptopodin decreased in 10% WHLR containing serum group, CFS index also decreased in 20% WHLR containing serum group (P < 0.05).

CONCLUSIONSWHLR could up-regulate the expression of synaptopodin, down-regulate the expression of CatL, and alleviate cytoskeletal reorganization of F-actin. It was helpful to stabilize the cytoskeleton of F-actin and improve the merging of podocytes.

Actins ; metabolism ; Animals ; Cathepsin L ; metabolism ; Cells, Cultured ; Down-Regulation ; Drugs, Chinese Herbal ; pharmacology ; Kidney Glomerulus ; cytology ; Mice ; Microfilament Proteins ; metabolism ; Podocytes ; drug effects ; pathology ; Puromycin Aminonucleoside ; adverse effects ; Up-Regulation

Animals ; Cells ; metabolism ; radiation effects ; Electromagnetic Fields ; Humans ; Reactive Oxygen Species ; metabolism

A series of isoindoline derivatives were designed, synthesized, and evaluated for their double inhibitory activities. All of them were new compounds, and their structures were confirmed by 1H NMR and HR-MS. Preliminary in vitro pharmacological tests showed that all compounds exhibited 5-HT or NE reuptake inhibition activity. Among the tested compounds, compound I-3 exhibited potent inhibitory activity against 5-HT and NE reuptake in vitro, and exhibited potent antidepressant activity in vivo. These compounds designed can be further optimized for finding more potent 5-HT/NE dual reuptake inhibitors and antidepressant candidates as well.
Antidepressive Agents ; chemical synthesis ; chemistry ; Biological Transport ; Drug Design ; Isoindoles ; chemical synthesis ; chemistry ; Serotonin Uptake Inhibitors ; chemical synthesis ; chemistry ; Structure-Activity Relationship

On account of the dense cuticles of the fresh stem and the light, hard and pliable texture of the dried stem, Dendrobii Caulis is difficult to dry or pulverize. So, it is very important to the ancient doctors that Dendrobii Caulis should be properly treated and applied to keep or evoke its medicinal effects. The current textual research results about the preliminary processing, processing and usage methods of Dendrobii Caulis showed that: (1) In history the clinical use of fresh or processed Dendrobii Caulis as teas and tinctures were very common. (2) Its roots and rhizomes would be removed before using. (3) Some ancillary approaches were applied to shorten drying times, such as rinsing with boiling mulberry-ash soup, washing or soaking with liquor, mixing with rice pulp and then basking, etc. (4) According to the ancients knowledge, the sufficient pulverization, by means of slicing, rasping, hitting or pestling techniques, was necessary for Dendrobii Caulis to take its effects. (5) The heat processing methods for Dendrobii Caulis included stir-baking, stir-frying, steaming, decocting and stewing techniques, usually with liquor as an auxiliary material. Among above mentioned, steaming by pretreating with liquor was most commonly used, and this scheme was colorfully drawn in Bu Yi Lei Gong Pao Zhi Bian Lan (Ming Dynasty, 1591 CE) ; moreover, decocting in advance or long-time simmering so as to prepare paste products were recommended in the Qing Dynasty. (6) Some different processing programs involving stir-baking with grit, air-tightly baking with ondol (Kangs), fumigating with sulfur, which appeared in modern times and brought attractive outward appearance of the drug, went against ancients original intentions of ensuring drug efficacy.
Dendrobium ; History, Ancient ; Medicine, Chinese Traditional ; history ; Technology, Pharmaceutical ; history

Objective To investigate the clinical outcomes of minimally invasive percutaneous nephrolithotomy(MPCNL)in the treatment of lower caliceal calculi.Methods We retrospectively re- viewed the clinical outcomes and complications of 33 patients who underwent MPCNL for lower caliceal cal- culi from March 2001 to April 2005.The average diameter of the calculi was 2.8 cm.Single tract nephrosto- my was performed in all 33 cases;among them renal access was obtained through a middle calyx in 10 cases and a lower calyx in 23.Nine cases had F14 renal access;and 24 cases,F16.Results Of 33 cases,28 (85%)achieved stone-free at 1 session.A second-look was needed in 3 cases due to intraoperative bleed- ing;ESWL,in 1 case with residual,calculi;no treatment,in 1 case with residual calculi＜4 ram.The mean operative time was 93 min;mean blood loss was 113 ml;mean hospital stay was 11 d.Blood transfusion was needed in 1 patient who suffered from hepatic cirrhosis preoperatively;another experienced severe bleeding 7 d after operation and was cured with hyperselective spongia gelatinosa embolization of the renal artery.Fol- low-up was available in 19 cases for 2-48 months,and no recurrence of renal calculi was noted.Conclu- sions Minimally invasive percutaneous nepbrolithotomy has advantages of safety,less invasion,and easy re- covery for the treatment of lower caliceal calculi.

Objective To compare the efficacy of 18F-FDG PET/CT, 99Tcm-MDP bone scintigraphy (BS), and combination of the two techniques (PET/CT + BS) for detecting bone metastasis by ROC curve analysis. Methods All 296 patients with various cancers, who underwent both 99Tcm-MDP BS and 18F-FDG PET/CT within two months, were retrospectively analyzed. These images were interpreted according to 5-point scale (0: definitely negative, 1: probably negative, 2: equivocal, 3: probably positive, 4:definitely positive for bone metastasis), and the scale of PET/CT + BS was the sum of PET/CT and BS. In light of the confirmed diagnosis derived from pathology or follow-up, ROC curve analysis was performed.The area under the ROC curve (AUC) was compared by z-test. Results Of 296 cases, 61 (20.6%) were confirmed as bone metastases and 235 (79.4%) were negative. The AUC were 0. 919 (95% confidence interval (95% CI) :0. 867 - 0. 971) for BS, 0. 949 (95% CI: 0. 906 - 0. 991) for PET/CT, and 0. 994 (95% CI: 0.988-0.999) for PET/CT + BS, rctrospectively. The AUC of PET/CT + BS was statistically significantly larger than that of BS (z=2. 866, P=0.004) or PET/CT (z =2.027, P=0.043), while the AUC of PET/CT was larger than that of BS, but no statistically significance (z = 0. 881, P = 0. 378) was showed. The optimal sensitivity, specificity, accuracy, positive predictive value (PPV), negative predictive value(NPV) were 90. 2% (55/61), 85. 1% (200/235), 86. 1% (255/296), 61. 1% (55/90), 97. 1%(200/206) for BS, 88.5% (54/61), 97.0% (228/235), 95.3% (282/296), 88.5% (54/61), 97.0% for PET/CT, and 98.4% (60/61), 95.7% (225/235), 96.3% (285/296), 85.7% (60/70) for PET/CT + BS,respectively. The specificity (χ2 = 19.862, P<0. 001), accuracy (χ2 = 23. 361, P<0.001) and PPV (χ2 =11. 791, P =0.001) of PET/CT + BS were significantly higher than those of BS, the sensitivity of PET/CT +BS was significantly higher than that of PET/CT (χ2 =4.167, P=0.031). Compared with BS, PET/CT had a higher specificity (χ2 = 19.600, P<0. 001), accuracy (χ2 = 13. 755, P <0. 001), PPV (χ2 = 13. 608, P <0. 001), but their sensitivity showed no statistically significant difference (χ2 = 0, P = 1. 000). Conclusions The efficacy of 18F-FDG PET/CT for detecting malignant bone metastasis was superior to that of 99Tcm-MDP BS alone. The detection ability can be obviously improved by combination of the two techniques.

This study is to investigate the sedative and hypnotic effects of a novel compound H1208. The sedative activity of H1208 was investigated by recording the spontaneous locomotor activity of mice. The hypnotic property was evaluated by the latency and duration of sleep (loss of righting reflex) in mice and the effect of hypnotics on sleep pattern of electroencephalogram were studied in conscious, freely moving mice with chronically implanted electrodes. The brain monoamine neurotransmitters levels in mice were measured by high performance liquid chromatography-electrochemical detection. The spontaneous locomotor activity was decreased by 56.7% and 80.2% in H1208 (5 and 25 mg x kg(-1), ip) treated mice, respectively. The loss of righting reflex was directly induced in mice after H1208 (60 mg x kg(-1), ip) administration. The non-rapid eye movement sleep increased significantly by 131% and 259%, respectively, within 3 hours after H1208 (30 and 60 mg x kg(-1), ip) administration. However, the rapid eye movement sleep decreased significantly. The contents of DA in the striatum and cortex and 5-HT in the cortex decreased significantly. These results demonstrated that H1208 has potent sedative and hypnotic effects, which may be closely related to the decreased contents of DA and 5-HT in mouse brain.
Animals ; Brain ; drug effects ; physiology ; Dopamine ; metabolism ; Electroencephalography ; Hypnotics and Sedatives ; pharmacology ; Mice ; Motor Activity ; drug effects ; Serotonin ; metabolism ; Sleep ; drug effects

To improve the efficiency of halophilic actinobacteria screening and carry out the rapid selection of targeted strains, we tested 34 strains of Streptomonospora by PCR-single strand conformation polymorphism analysis (PCR-SSCP) based on genus-specific primers for the PCR identification. This approach employs PCR with two pairs of primers located in the 16S rRNA sequence flanking two variable region, then build clustering tree according as SSCP data. Synchronously, we sequenced all the 16S rRNA partial sequences for these strains to verify them. The results showed that the PCR-SSCP analysis was an efficient, easy-to-handle and economic method for rapid selection of halophilic actinobacteria resources.

Aim To study inhibitory effect of 5-fluorouracil encapsulated by galactosylceramide liposomes (5-Fu-GCL)on 5-Fu-resistent HepG_2 cells and its mechanisms. Methods Inhibitory effect of 5-Fu-GCL on established model of 5-Fu-resistant HepG_2 cells was assessed with MTT assay in vitro. The concentration-time course of 5-Fu-GCL in intracellular fluid was detected with high performance liquid chromatography (HPLC). Thymidylic acid synthase (TS) expression was observed with immunohistochemical method,and NO content was determined with chemical method. Results Obvious inhibitory effects of 5-Fu-GCL (75,150,300,600,1200?mol?L-1) on 5-Fu-resistant HepG_2 cells were observed with IC_ 50 of 158.6 ?mol?L-1,far lower than that of free 5-Fu (400.9 ?mol?L-1). 5-Fu-GCL (300 ?mol?L-1) inhibited 5-Fu-resistant HepG_2 cells in a time-dependent manner,and the inhibitory effect of 5-Fu-GCL was stronger than that of free 5-Fu during 12～48 h. Compared with free 5-Fu,5-Fu-GCL (300 ?mol?L-1) increased the content of intracellular fluid in 5-Fu-resistant HepG_2 cells. 5-Fu-GCL(62.5,300,1200 ?mol?L-1) not only inhibited the expression of TS,but also increased the production of NO in 5-Fu-resistant HepG_2 cells,and these effects of 5-Fu-GCL(300,1200 ?mol?L-1) were stronger than those of free 5-Fu. Conclusion 5-Fu-GCL has inhibitory effect on 5-Fu-resistant HepG_2 cells. The effect may be related to the increased concentration of 5-Fu-GCL in intracellular fluid,inhibited expression of TS and increased production of NO.