Eleven compounds were isolated from the culture of Streptomyces sp. CPCC 202950 by a combination of various chromatographic techniques including column chromatography over macroporous resin HP-20, MCI, and reversed-phase HPLC. Their structures were identified as 1H-pyrrole-2-carboxamide(1),5'-deoxy-5'-methylthioinosine(2), vanillamide(3), trans-3-methylthioacrylamide(4), 1,2,3,4-Tetraydro-1H-pyrido[3,4-b]indole-3-carboxylic acid(5), cyclo(L-pro-L-tyr) (6), N-[2-(4-hydroxyphenyl)]ethylacetamide(7), benzamide (8), cyclo ('L-leucyl-trans-4-hydroxy-L-proline)(9), cyclo-(Phe-Gly) (10), and tryptophan (11). Among them, compounds 1 and 2 were new natural products. In the preliminary assays, none of the compounds exhibited obvious inhibition of HIV-1 protease activity (IC50 > 10 micromol x L(-1)).
Culture Media ; chemistry ; metabolism ; HIV Protease ; analysis ; HIV Protease Inhibitors ; chemistry ; isolation & purification ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization ; Streptomyces ; chemistry ; metabolism

OBJECTIVETo explore the situation of equity in health service delivery in the experimental region of new rural cooperative medical scheme (NRCMS).

METHODSA household questionnaire survey was conducted to 2112 residents in the experimental county of NRCMS in Yuexi county with a stratified-cluster sampling on the situation of health service delivery, from July 1-15,2005. Data was analyzed with Epi Info 6.04 and SPSS 11.0 software and indices as rate, ratio, Gini coefficient, concentration index (CI) and chi-square test etc.

RESULTSThere was no significante difference of the treatment-seeking rate during two weeks among five groups economic condition residents (chi2 = 5.52, P > 0.05) and the rates were 48.14 per thousand, 82.90 per thousand, 65.88 per thousand, 48.72 per thousand and 50.66 per thousand respectively with CI = -0.026. Similarly, the hospitalization rates were 59.08 per thousand, 67.36 per thousand, 51.76 per thousand, 58.97 per thousand and 52.86 per thousand respectively in the last year and the CI = - 0.017. But there was a significante difference of rates on chronic disease among the five groups of residents with different economic conditions in the last six months (chi2 = 18.42, P < 0.01) and the rates were 295.40 per thousand, 243.52 per thousand, 230.59 per thousand, 225.64 per thousand and 176.21 per thousand and the CI = -0.055. When income reduced, the prevalence had been increasing among residents. Meanwhile, the collection funds showed unfair in residents with various income and the compensating fund of new rural cooperative medical scheme had not reduced the gap between rich and poor.

CONCLUSIONThere was an unequity of medicine expenditure and compensating fund in residents with various income in the experimental region. The low income residents had a high health service need and the government should improve NRCMS greatly to change the situation.

China ; Data Collection ; Delivery of Health Care ; Health Expenditures ; Health Services Needs and Demand ; Healthcare Disparities ; Humans ; Income ; Rural Health Services ; economics ; utilization

By using a cell-based high throughput screening model for the CLA-1 up-regulator, Streptomyces 203909 was found to produce up-regulator of CLA-1. A novel trichostatin analogue was isolated from the rice fermentation of Streptomyces sp. CPCC 203909by a combination of various chromatographic techniques including column chromatography (CC) over silica gel, flash C18 CC, and reversed-phase HPLC. Its structure was identified as (-)-(R,2E,4Z)-7-[(4'-dimethylamino) phenyl]-4,6-dimethyl-7-oxohepta-2,4-dienoyl-L-glutamine (1) by the spectroscopic and chemical methods, and combination with the CD spectroscopy and Marfey's method. In the prelimi- nary assays, Compound 1 showed cytotoxicity against human embryonic kidney 293 cell line with IC50 value 35.3 [µmol · L(-1).
Cell Survival ; drug effects ; Fermentation ; Hep G2 Cells ; Humans ; Hydroxamic Acids ; chemistry ; isolation & purification ; metabolism ; pharmacology ; Molecular Structure ; Streptomyces ; chemistry ; metabolism

OBJECTIVETo compare the behavioral effects of psychoactive drugs between two strains of mice.

METHODSThe Kunming (KM) and ICR mice were injected intraperitoneally with caffeine (3, 10, 30, 100 mg/kg), ephedrine (3, 10, 30, 100 mg/kg), diazepam (1, 3,1 0 mg/kg) and chloral hydrate (10, 30, 100 mg/kg), respectively. Ten min after injection, the locomotor activity in the open field was recorded for 2 h. The total distance, the distance ratio to total distance and the time in central region were analyzed for each drugs. Thirty min after injection, the latent time in the passive avoidance test was measured in a shuttle box.

RESULTSCaffeine and diazepam prolonged the latent time, and ephedrine and chloral hydrate decreased the latent time, but there were no differences between the two strains. The two strains of mice exhibited significant differences in the total distance after injection of ephedrine 10 mg/kg, diazepam 3 mg/kg and chloral hydrate 100 mg/kg. Compared to KM mice, ICR mice exhibited an increase in the distance ratio and the time in central region after injection of ephedrine 10-100 mg/kg, but a decrease after diazepam 3-10 mg/kg.

CONCLUSIONKM and ICR mice show no differences in latent time, but significant differences in the total distance, the distance ratio and the time in central region in the locomotor activity. Therefore, selection of mouse strains is important in the study of psychoactive drugs.

Animals ; Caffeine ; pharmacology ; Central Nervous System Agents ; pharmacology ; Chloral Hydrate ; pharmacology ; Diazepam ; pharmacology ; Dose-Response Relationship, Drug ; Ephedrine ; pharmacology ; Mice ; Mice, Inbred ICR ; Motor Activity ; drug effects

OBJECTIVETo investigate the efficacy of pressure reduction by peritoneal catheterization in patients with malignant ascites-induced abdominal compartment syndrome (ACS).

METHODSClinical data of 29 patients with malignant ascites-induced ACS from October 2002 to October 2008 were analyzed retrospectively. Intra-abdominal pressure (IAP) was reduced by peritoneal catheterization. Changes of intra-abdominal pressure and ascites volume were observed during treatment. Clinical signs and urinary volume were monitored.

RESULTSIAP was less than 25 cm H(2)O in 2 cases, 25 to 35 cm H(2)O in 21 cases, more than 35 cm H(2)O in 6 cases. IAP decreased significantly after drainage of 1000 to 1500 ml of ascites, then IAP curve leveled off. With all the ascites drained, IAP maintained at 11 to 12 cm H(2)O and at 6 to 8 cm H(2)O after 24 hours. Blood pressure was stable without significant changes before and after IAP reduction (P>0.05). The breathing rate and heart rate were improved, and 24 h urinary volume increased significantly after IAP reduction (P<0.01).

CONCLUSIONEarly peritoneal catheterization can improve the cardiac, pulmonary, and renal function in malignant ascites-induced ACS.

Adult ; Aged ; Aged, 80 and over ; Ascites ; complications ; etiology ; Catheterization ; Compartment Syndromes ; etiology ; surgery ; Decompression, Surgical ; methods ; Female ; Humans ; Male ; Middle Aged ; Retrospective Studies ; Treatment Outcome

OBJECTIVETo review the current advances on the role of uncoupling protein (UCP) in the pathogenesis and progress of nonalcoholic fatty liver disease (NAFLD).

DATA SOURCESA comprehensive search of the PubMed literature without restriction on the publication date was carried out using keywords such as UCP and NAFLD.

STUDY SELECTIONArticles containing information related to NAFLD and UCP were selected and carefully analyzed.

RESULTSThe typical concepts, up-to-date findings, and existing controversies of UCP2 in NAFLD were summarized. Besides, the effect of a novel subtype of UCP (hepatocellular down regulated mitochondrial carrier protein, HDMCP) in NAFLD was also analyzed. Finally, the concept that any mitochondrial inner membrane carrier protein may have, more or less, the uncoupling ability was reinforced.

CONCLUSIONSConsidering the importance of NAFLD in clinics and UCP in energy metabolism, we believe that this review may raise research enthusiasm on the effect of UCP in NAFLD and provide a novel mechanism and therapeutic target for NAFLD.

Animals ; Fatty Acids, Nonesterified ; metabolism ; Fatty Liver ; etiology ; metabolism ; Humans ; Ion Channels ; physiology ; Mitochondrial Proteins ; analysis ; chemistry ; physiology ; Non-alcoholic Fatty Liver Disease ; Uncoupling Protein 2

Vincristine (VCR) is mainly used to treat acute lymphocytic leukemia, Hodgkin and non-Hodgkin lymphoma in clinic with definite therapeutic effect. But the obvious neurotoxicity and local stimulation of which limit its clinic use. In order to increase the lymph targeting to enhance the curative effect and to lower the adverse reaction of VCR, the VCR loaded transfersomes (VCR-T) were prepared with dry-film and ultrasonic dispersing methods, and the corresponding pharmaceutical properties, pharmacokinetical characteristics and the targeting ability were studied. The average particle size of VCR-T prepared was 63 nm with an entrapment ratio of 59%. The in vitro transdermal research with modified Franz cell showed that VCR-T permeated through the skin in accordance with polynomial equation, and with an accumulation permeation percentage of 67.4% up to 12 h. An HPLC method was utilized to determine the pharmacokinetics and tissue distribution of VCR. Compared with the iv injection of VCR solution, the retention time of VCR in blood was extended by 12 times with VCR-T, and the targeting index in rat lymph was increased by 2.75 times. As a result, transfersomes could penetrate the skin and enter into the systemic circulation carrying VCR with good lymph targeting ability, which makes it probably a new lymphtic targeting drug delivery system.
Administration, Cutaneous ; Animals ; Antineoplastic Agents, Phytogenic ; administration & dosage ; blood ; pharmacokinetics ; Area Under Curve ; Drug Delivery Systems ; Liposomes ; chemistry ; Lymph Nodes ; metabolism ; Male ; Particle Size ; Rats ; Rats, Sprague-Dawley ; Skin Absorption ; Spleen ; metabolism ; Surface-Active Agents ; chemistry ; Tissue Distribution ; Vincristine ; administration & dosage ; blood ; pharmacokinetics

OBJECTIVETo explore the quality of life and related social support among people living with HIV/AIDS with related factors.

METHODS331 people living with HIV/AIDS and 148 of their family members were selected using a typical sampling method. Questionnaires on general conditions, tables on history of infection, generic quality of life inventory-74 (GQOLI-74) and social support scale (SSS) were used.

RESULTSData from one-way analysis suggested that people living with HIV/AIDS and their family members with the different sexs, different villages and different cultural backgrounds had differences in GQOLI-74 scores (P < 0.05) while people living with HIV/AIDS with the different villages had differences in SSS scores (P < 0.05). Results from Multiple linear regression analysis revealed that being elderly and negative life events were negatively associated with social support (P < 0.05), while factors as more advanced educational background, harmonious neighborhood relationship and having bother pouring nature were the predictive factors (P < 0.05).

CONCLUSIONMany factors might affect dimensions of quality of life among people living with HIV/AIDS and their family members in rural areas of northern Anhui. Community care and social support of HIV/AIDS should still be greatly enhanced in the countryside of China. A community care mode based on family and neighborhood was expected to be developed.

Acquired Immunodeficiency Syndrome ; complications ; ethnology ; psychology ; China ; Cultural Characteristics ; Family Relations ; Female ; Humans ; Male ; Quality of Life ; Social Support

OBJECTIVETo compare the performance of full-field digital mammography (FFDM) and digital breast tomosynthesis (DBT) in the assessment of the lesions in dense breast, and to estimate the difference in diagnosis of breast disease by FFDM images alone and FFDM plus DBT images.

METHODSAccording to the breast imaging reporting and data system (BIRADS), 134 patients were selected. The morphology of the lesions shown on FFDM and DBT were evaluated and compared, and the maximum diameter of the lesions was measured. At first, doctors made the diagnosis of a patient by reading FFDM only. Then they made another diagnosis by combining with DBT images of the same patient. The two diagnoses were compared and analyzed according to the pathology results.

RESULTSOne hundred and thirty-four patients were included in this study, and all of them were confirmed by histology (65 benign cases, 69 malignant cases). DBT could show more details about the morphology of the lesions, including the border of the masses, spiculation and vessels. The numbers of those signs detected by DBT were 46, 30 and 3, respectively, while only 33 case with circumscribed masses and 14 cases with spiculation were detected by FFDM. Only the difference of spiculation in heterogeneously dense breast detected by DBT and FFDM was statistically significant (P < 0.05). Of the cases with calcifications, DBT images (reconstructed as a 1-mm-thick slice) showed calcifications superior to FFDM in 2 cases, equal to FFDM in 23 cases, and inferior to FFDM in 11 cases. The difference was statistically significant (P < 0.05). But when thickness was changed into 1 cm, the visibility of calcifications in those cases was equal between FFDM and DBT. The maximum diameter of lesions was 2.46 ± 1.64 cm in DBT image, and 2.58 ± 1.62 cm in FFDM image, with a significant difference (P < 0.05). Comparing with reading FFDM images only, the accuracy of FFDM combining with DBT was increased from 88.8% to 91.8%. For FFDM, the AUC of ROC was 0.887, while for DBT it was increased to 0.912, with a non-significant difference (P > 0.05).

CONCLUSIONSDBT is superior to FFDM in the morphological characterization and small calcification in the lesions in dense breast. Combining FFDM and DBT improves the accuracy of diagnosis, but the difference is not statistically significant.

Adolescent ; Adult ; Breast Diseases ; diagnostic imaging ; Breast Neoplasms ; diagnostic imaging ; Calcinosis ; diagnostic imaging ; Carcinoma in Situ ; diagnostic imaging ; Carcinoma, Ductal, Breast ; diagnostic imaging ; Female ; Fibroadenoma ; diagnostic imaging ; Humans ; Image Processing, Computer-Assisted ; Imaging, Three-Dimensional ; Mammography ; methods ; Middle Aged ; Radiographic Image Enhancement ; Tomography, X-Ray Computed ; Young Adult

OBJECTIVETo investigate the effect of oridonin on the human acute lymphocytic leukemia cell line Jurkat and its mechanism.

METHODSJurkat cells were cultured in vitro and treated with various concentrations (0, 1.25, 2.5, 5, and 10 μmol/L) of oridonin for different lengths of time (24, 48, and 72 hours). The proliferation of Jurkat cells was analyzed by MTT assay. The changes in nuclear morphology were evaluated by fluorescence microscopy at 12 hours after treatment with various concentrations of oridonin. The expression levels of Brg1, P53, and C-myc were determined by semi-quantitative Western blot in Jurkat cells treated with various concentrations of oridonin for 24 hours or 5 μmol/L oridonin for various lengths of time (0, 2, 6, 12, and 24 hours). The expression levels of P53 and C-myc and proliferation of Jurkat cells were evaluated after Brg1 expression was knocked down by Brg1-specific siRNA.

RESULTSCompared with the control group, the proliferation of oridonin-treated Jurkat cells was significantly inhibited in a concentration- and time-dependent manner (P<0.05). According to the florescence microscopic analysis, oridonin treatment led to nuclear pyknosis in Jurkat cells. Compared with the control group, Jurkat cells treated with 5 μmol/L oridonin had reduced expression of Brg1 and C-myc but elevated expression of P53. Brg1 knock-down led to a significant reduction in proliferation of Jurkat cells (P<0.05), up-regulated expression of P53, and down-regulated expression of C-myc.

CONCLUSIONSOridonin can inhibit the proliferation of Jurkat cells, probably via the Brg1 signaling pathway.

Antineoplastic Agents, Phytogenic ; pharmacology ; Cell Proliferation ; drug effects ; DNA Helicases ; analysis ; physiology ; Diterpenes, Kaurane ; pharmacology ; Dose-Response Relationship, Drug ; Down-Regulation ; Humans ; Jurkat Cells ; Nuclear Proteins ; analysis ; physiology ; Precursor Cell Lymphoblastic Leukemia-Lymphoma ; drug therapy ; Proto-Oncogene Proteins c-myc ; analysis ; Signal Transduction ; physiology ; Transcription Factors ; analysis ; physiology ; Tumor Suppressor Protein p53 ; analysis