This study is to investigate the effects of aqueous extract of Schisandra chinensis Baill (WWZ), kadsurin, schisandrin A, schisandrin B and schisandrol B on rat hepatic CYP3A. Rats received a daily gavage of aqueous extract of WWZ for different times. The livers were harvested after gavage and subjected to microsome preparation. Microsomal CYP3A activity was determined by measuring the amount of the metabolite of testosterone (6 beta-hydroxytestosterone) with HPLC. Aqueous extract of WWZ, kadsurin and schisandrin A were incubated with microsomes obtained from rat. Microsomal CYP3A activity was determined by HPLC. Primary hepatocytes were separated and extracted from rat, then were treated with aqueous extract of WWZ, schisandrin A, schisandrin B and schisandrol B. Then, the expression of CYP3A1 mRNA was analyzed by RT-PCR. As for the in vivo assay, aqueous extract of WWZ significantly inhibited the enzyme activity of CYP3A after 12 h gavage. The inhibitory effect was converted to inductive effect after 3-day gavage. Aqueous extract of WWZ could induce the enzyme activity of CYP3A after 6-day gavage. Aqueous extract of WWZ and kadsurin showed a dose-dependent inhibition of CYP3A (IC50 of 487.8 microg mL(-1) and 6.2 micromol L(-1), separately). In rat primary hepatocytes, aqueous extract of WWZ (2.5 mg mL(-1)), schisandrin A (0.1 micromol L(-1)), schisandrin B (0.1 micromol L(-1)) and schisandrol B (10 micromol L(-1)) increased significantly the expression of CYP3A1 mRNA by 23%, 55%, 42% and 27%, respectively. Aqueous extract of WWZ could show dual effect on the enzyme activity of CYP3A in rat in vivo. Meanwhile, kadsurin showed a dose-dependent inhibition of the enzyme activity of hepatic CYP3A in vitro. And schisandrin A, schisandrin B and schisandrol B showed significant inductive effect on the expression of rat CYP3A1 mRNA.
Animals ; Cyclooctanes ; administration & dosage ; isolation & purification ; pharmacology ; Cytochrome P-450 CYP3A ; genetics ; metabolism ; Dioxoles ; administration & dosage ; isolation & purification ; pharmacology ; Dose-Response Relationship, Drug ; Drugs, Chinese Herbal ; administration & dosage ; isolation & purification ; pharmacology ; Hepatocytes ; drug effects ; enzymology ; Inhibitory Concentration 50 ; Lignans ; administration & dosage ; isolation & purification ; pharmacology ; Male ; Microsomes, Liver ; enzymology ; Plants, Medicinal ; chemistry ; Polycyclic Compounds ; administration & dosage ; isolation & purification ; pharmacology ; RNA, Messenger ; metabolism ; Rats ; Rats, Sprague-Dawley ; Schisandra ; chemistry

Abstract: Objective To analyze the occupational hazards of enterprises in Pingshan district of Shenzhen in 2017. Methods Occupational hazards were analyzed in 200 enterprises in Pingshan district of Shenzhen City selected using stratified Results random sampling method. A total of 24 industries were involved in the 200 enterprises. The declaration rate of ， occupational hazards was 91.5% and the exposure rate of occupational hazards among workers was 49.2%. The regular monitoring rate of occupational hazard factors in workplaces of the enterprises was 79.5%. There were 129 kinds of occupational ， ， hazard factors of which 19 factors exceeded the national occupational exposure limit accounting for 14.7%. The over standard ， ， ， ， ， ， ， ， rates of noise silica dust cotton dust methanol toluene and other dust were 28.7% 13.6% 11.8% 5.86% 0.5% and ， ， 0.4% respectively. There were 13 kinds of occupational hazard factors in the workplace of metal products industry all of which （ ） exceeded the occupational exposure limit. The exposure rate 56.7% of occupational hazard factors in workers was the highest. Conclusion ， ， The main occupational hazard factors were noise dust and chemical factor and the major occupational hazard industry was metal manufacturing in Pingshan district of Shenzhen City.

BACKGROUNDZhongfei Mixture (ZM), a traditional Chinese medicine, exploited from the clinical experience, has mainly been used for the treatment of advanced lung cancer since it was produced in 1983. However, little research has been conducted on its anti-tumor mechanism. In this study, we aimed to investigate the anti-tumor and apoptotic effects of ZM in vitro and in vivo.

METHODSThe growth inhibition effect of ZM on A549 cells was evaluated by MTT assay. Morphological observation and clone forming tests were performed to determine the effect of ZM on cell viability. Cell cycle distribution and apoptosis were analyzed by flow cytometry. In addition, the in vivo anti-proliferation activity of ZM was evaluated using mice bearing Lewis lung carcinoma. Further, the apoptosis of cells in tumor tissue was determined by the terminal deoxynucleotidyl transferase-mediated dUTP nick-end labeling (TUNEL) assay, and the expression of Ki-67 protein in tumor tissues was analyzed by En-Vision immuno-histochemistry staining.

RESULTSZM exerted an obvious inhibitory effect on proliferation of A549 cells. It arrested A549 cells in G(2)-M phase and induced apoptosis. Compared with 3.02% and 5.32% in control group, the percentages of cells arrested in G(2)-M phase were 19.20% and 19.58% in 7.94 mg/ml ZM treated A549 cells at 24 hours and 48 hours. Moreover, the apoptosis rate increased from 0.18% to 18.01% after ZM treatment for 48 hours. ZM also significantly inhibited tumor growth in the tumor-implanted mice. Compared with saline control group, the effects of ZM showed significant tumor growth inhibition (P < 0.05). Furthermore, ZM could down-regulate the expression of Ki-67 in tumor tissue in mice bearing Lewis lung carcinoma.

CONCLUSIONSOur results indicated that ZM has notable anti-tumor effect and the effects of ZM in moderate dose groups were superlative both in vitro and in vivo. The possible mechanism of ZM might be associated with arresting cell cycle in G(2)-M phase as well as down-regulating Ki-67 expression in tumor tissues.

Animals ; Antineoplastic Agents ; therapeutic use ; Apoptosis ; drug effects ; Cell Line, Tumor ; Drugs, Chinese Herbal ; therapeutic use ; Humans ; Medicine, Chinese Traditional ; methods ; Mice ; Xenograft Model Antitumor Assays

OBJECTIVETo investigate the chemical constituents from the aerial parts of Hyperricum monogynum.

METHODCompounds were isolated by various column chromatography and identified by spectral analysis.

RESULTTen compounds were isolated and identified as quercetin, quercitrin, hyperoside, rutin, (-)-epicatechin, 3,5-dihydroxy-1-methoxy-xanthone, 3,4-O-isopropylidenyl shikimic acid, shikimic acid, daucosterol, and oleanoic acid.

CONCLUSIONAll compounds were isolated from this plant for the first time.

Hypericum ; chemistry ; Plant Components, Aerial ; chemistry ; Plants, Medicinal ; chemistry ; Quercetin ; analogs & derivatives ; chemistry ; isolation & purification

The relationship of free amino groups on the surface and the characteristics of chitosan nanoparticles (CS-NPs) prepared by ionic gelation method was investigated. Free amino groups on the surface of CS-NPs were determined by colloidal titration, and the effects of the amount of free amino groups and its ionizable level on the particle size, zeta potential, appearance, drug entrapment efficiency and drug release profile in vitro of CS-NPs were investigated. The result showed that the surface free amino groups reduced, the average size, zeta potential, stability of nanoparticles, and the drug release rate and degree all decreased while the drug entrapment efficiency was not affected with the increase of tripolyphosphate (TPP) concentration. With the increase of pH, the free amino groups could be deprotonated and the ionizable level was stepped down, correspondingly the particle size and zeta potential of CS-NPs decreased. Additionally, the drug release rate and degree were elevated in acid medium while descended in neutral or base medium. The amount and ionizable level of free amino groups on the surface are affected by the gelation degree and pH, which further affected the volume phase transitions (swelling/shrinking processes) of CS-NPs. The properties of CS-NPs have correlation with the surface free amino groups.
Amines ; chemistry ; Chitosan ; chemistry ; Hydrogen-Ion Concentration ; Microscopy, Electron, Transmission ; Nanoparticles ; chemistry ; ultrastructure ; Particle Size ; Polyphosphates ; chemistry ; Surface Properties

OBJECTIVETo evaluate the effect of post-treatment PSA kinetics on the prognosis of prostate cancer (PCa).

METHODSWe retrospectively reviewed the clinical data of 114 cases of locally advanced PCa treated by maximal androgen blockade (MAB) combined with brachytherapy, and analyzed the association of the changes in PSA kinetics with the prognosis of the patients.

RESULTSThe median survival time of the patients was 81 (15 - 144) months, with 1-, 3- and 5-year survival rates of 91. 23%, 78.07% and 68.42% , respectively. Univariate analysis indicated that the baseline PSA level, PSA nadir, the time of PSA decreasing to nadir, PSA doubling time, and the extent of PSA declining were all predictive factors for the survival time of the PCa patients. Multivariate analysis demonstrated that PSA nadir, the time of PSA decreasing to nadir, and the extent of PSA declining were three independent prognostic factors, which prolonged the long-term survival of the patients by 1.7, 3.2 and 6.8 times, respectively.

CONCLUSIONFor locally advanced PCa treated by MAB combined with brachytherapy, PSA nadir <1 micro g/L, the time to nadir <3 months, and the extent of PSA declining >96% are independent prognostic factors.

Aged ; Aged, 80 and over ; Androgens ; administration & dosage ; therapeutic use ; Brachytherapy ; Humans ; Male ; Middle Aged ; Prognosis ; Prostate-Specific Antigen ; metabolism ; Prostatic Neoplasms ; metabolism ; therapy ; Retrospective Studies

OBJECTIVEIn order to evaluate the safety and immunogenicity of group A + C meningococcal polysaccharide vaccine, a controlled field trial was performed among children at 6-24 months and 5-13 years old in Longsheng county, Guangxi Zhuang Autonomous Region.

METHODSMore than 600 children were selected in this trial. 428 children, aged 6-24 month-old and 5-13 year-old were involved in two experimental groups and were inoculated 100 microg of group A + C meningococcal polysaccharide vaccine. 103 children in positive control group were inoculated 50 microg of group A meningococcal polysaccharide vaccine while 94 children in negative control group were inoculated 30 microg of Typhoid Vi polysaccharide vaccine. Both systemic and local reactions were observed in each group at 6 h,24 h,48 h and 72 h after inoculation. Blood samples were collected in all children before and at 1 month after inoculation. Additionally, at least 50 blood samples were taken in each experimental group at 6 and 12 months after inoculation. Serum bactericidal antibody was tested by micro bactericidal test.

RESULTSBoth systemic and local reactions were mild in two experimental groups with only 3 children (0.7%) had > or = 37. 6 degrees C fever, 4 children (0.9%) appeared mild areola but all adverse reaction disappeared within 48 hours. In 5-13 year-old experimental group, the rates for four-fold increase of bactericidal antibody were 96.59% and 92.15% to group A and group C meningococcus respectively at 1 month after inoculation, and remained 90.91% and 90.08% at 12 months after inoculation.

CONCLUSIONGroup A + C meningococal polysaccharide vaccine was safe and having good immunogenicity among Chinese children.

Adolescent ; Antibodies, Bacterial ; blood ; immunology ; Child ; Child, Preschool ; Female ; Humans ; Infant ; Male ; Meningococcal Vaccines ; adverse effects ; immunology ; Polysaccharides, Bacterial ; adverse effects ; immunology ; Typhoid-Paratyphoid Vaccines ; adverse effects ; immunology

OBJECTIVETo establish a rabbit model of intervertebral disc degeneration by puncturing the anulus fibrosus through an approach between the longissimus dorsi muscle and obliquus externus abdominis.

METHODSThe L(4/5) and L(5/6) intervetebral discs of 6 New Zealand white rabbits were punctured by an 18-gauge pin in the anterolateral annular fibrosus through an approach between the longissimus dorsi muscle and the obliquus externus abdominis with the right transverse processes of L(5) and L(6) resected; the L(2/3) discs were used as the control without exposure or needle stab, and the L(3/4) discs were subjected to sham operation with the discs exposed but not punctured after resecting the right transverse process of L(4). X-ray and magnetic resonance imaging (MRI) were performed preoperatively and at the 4th week after puncture. At 4 weeks after the operation, histological and immunohistochemical analyses of the discs were carried out.

RESULTSX-ray of the punctured discs at 4 weeks after the operation presented a significant decrease of disc height, osteophytosis formation, and end-plate stiffness; an obvious decrease of signal intensity on T(2)-weighted images was found in the puncture group but not in the control or sham-operated groups. Gross morphological inspection showed atrophy of the nucleus pulposus, which became loose, soft, and fragile with a light yellow color. Histological and immunohistochemical analyses showed a significant decrease of notochordal cells and type II collagen in the nucleus pulposus in the puncture group as compared to the control and sham-operated groups.

CONCLUSIONPuncture through the approach between the longissimus dorsi muscle and the obliquus externus abdominis allows the establishment of a reliable animal model for studying intervertebral disc degeneration.

Animals ; Disease Models, Animal ; Female ; Intervertebral Disc Degeneration ; Lumbar Vertebrae ; physiopathology ; Male ; Rabbits

BACKGROUNDTalaromyces (Penicillium) marneffei (TM) is an emerging dimorphic human pathogenic fungus that is endemic to Southeast Asia. TM mostly occurs as an opportunistic infection in patients with human immunodeficiency virus (HIV). The objective of this study was to compare the clinical and laboratory parameters of patients with TM infections who were HIV-positive and HIV-negative and to assess therapies and outcomes.

METHODSThis was a retrospective analysis of 26 patients diagnosed with disseminated TM infection from September 2005 to April 2014 at Fujian Provincial Hospital, China.

RESULTSPatients with TM infection tend to present with fever, weight loss, and anemia. The time from symptom onset to confirmed diagnosis was greater for HIV-negative patients (n = 7; median: 60 days, range: 14-365 days) than for HIV-positive patients (n = 19; median: 30 days, range: 3-90 days, Mann-Whitney U = 31.50, P= 0.041). HIV-negative patients were more likely to have dyspnea (57.1% vs. 5.3%, χ2 = 8.86, P= 0.010), low neutrophil count (Mann-Whitney U = 27.00, P= 0.029), high CD4 count (Mann-Whitney U = 0.00, P= 0.009), and high lymphocyte count (Mann-Whitney U = 21.00, P= 0.009). There were no significant differences in other demographic, clinical, or biochemical characteristics. Among all the patients, 12 HIV-positive patient and 1 HIV-negative patient received amphotericin and fluconazole treatment, 9 of whom improved, 1 died, 2 had kidney damage, 1 had hypokalemia due to exceeded doses.

CONCLUSIONSHIV-negative patients with TM infections tend to have a longer diagnostic interval, a higher percentage of dyspnea, higher levels of CD4 and lymphocytes, and lower neutrophil counts than TM infection in HIV-positive patients. Treatment programs with amphotericin and fluconazole are mostly effective.

Adult ; Aged ; CD4 Lymphocyte Count ; Female ; HIV Infections ; complications ; Humans ; Male ; Middle Aged ; Mycoses ; diagnosis ; drug therapy ; immunology ; Retrospective Studies ; Talaromyces ; drug effects

OBJECTIVETo assess the quality of whole spine images obtained by DR and magnetic resonance imaging (MRI) and analyze the whole spinal imaging sagittal parameters for standing DR and supine MRI.

METHODSSixty-one patients aged 49.9∓17.6 years with degenerative spinal disease underwent both standing DR and supine MRI of the whole spine from November, 2010 to March, 2016. The image quality was retrospectively reviewed, and the cervical lordosis (CL), thoracic kyphosis (TK), lumbar lordosis (LL), sacral slope (SS), and sagittal vertical axis (SVA) were measured on the whole spinal lateral DR and middle sagittal MR images.

RESULTSBoth the DR and MR whole spine images had a high quality (100%). The CL, TK, LL, SS, and SVA measured were 28.37mnplus;10.91 °, 29.98mnplus;8.96 °, 45.61mnplus;12.46 °, 34.38mnplus;9.05 °, and 17.20mnplus;26.39 mm on DR images and were 24.34mnplus;9.01 °, 21.22mnplus;8.13 °, 41.45mnplus;12.17 °, 37.45mnplus;8.19 °, and 36.51mnplus;12.44mm on MR images, respectively, showing significant differences in the measurements between the two modalities (P=0.000, 0.000, 0.000, 0.001, and 0.007, respectively). The correlation coefficient between DR and MR images for CL, TK, LL, SS, and SVA were 0.69, 0.68, 0.72, 0.51, and 0.27 (P=0.000, 0.000, 0.000, 0.000, and 0.034, respectively).

CONCLUSIONBoth standing DR and supine MR whole spine imaging can provide high-quality images. The CL, TK, LL, SS, and SVA measured on supine MR whole spine images are correlated with those on standing DR images but differ obviously. Supine MR imaging can not substitute standing DR examinations, and comprehensive assessment of degenerative spinal disease needs the combination of the two imaging techniques.