China ; Developed Countries ; Insurance, Health ; Occupational Health

Chemical constituents of Inula japonica were isolated and purified by repeated column chromatographies, over silica gel, and Toyopearl HW-40, and preparative HPLC. On the basis of spectral data analysis, including NMR and MS data, the structures of the isolates were elucidated and their anti-inflammatory activities were assayed. Fifteen compounds were isolated from the ethyl acetate extract of I. japonica, and their structures were elucidated as dihydrosyringenin (1), (3S, 5R, 6S, 7E)-5,6-epoxy-3-hydroxy-7-megastigmen-9-one (2), (6R, 7E) -9-hydroxy-4,7-megastigmadien-3-one (3), arnidiol (4), taraxasterol acetate (5), 8,9,10-trihydroxythymol (6), taxifolin (7), luteolin (8), napetin (9), eupatin (10), spinacetin (11), quercetin (12), p-hydroxycinnamic acid (13), caffeic acid (14), and caffeoyl acetate (15). Compounds 1, 2, 7, 13 and 15 were isolated from the genus Inula for the first time, and compounds 3, 4, 9-11 and 14 were isolated from this plant for the first time. The anti-inflammatory activity result showed that compounds 3, 6-12 and 14 exhibited inhibition effect against leukotriene C4 (LTC4) synthesis and degranulation definitely in c-Kit Ligand (KL) induced mast cells, and compound 8 and 12 also had the suppression effect against lipopolysacharide(LPS) induced nitric oxide (NO) activity in RAW264.7 macrophages. It is firstly reported that compounds 7 and 9-11 possessed potent inhibition activities against LTC4 generation and degranulation in mast cells.
Animals ; Anti-Inflammatory Agents ; chemistry ; pharmacology ; Cell Line ; Inula ; chemistry ; Macrophages ; drug effects ; Mast Cells ; drug effects ; Mice ; Mice, Inbred BALB C ; Plant Extracts ; chemistry ; pharmacology

The objects of research on the resources chemistry of Chinese medicinal materials (RCCMM) are promotion of efficient production, rational utilization and improving quality of CMM and natural products. The development of TCM cause depends on the efficient utilization and sustainable development of CMM, hinges on the technologies and methods for using and discovering medicinal biological resources, stand or fall on the extension of industy chains, detailed utilizaion of resource chemical components by multi-way, multi-level. All of these may help to the recycling utilization and sound development of RCMM. In this article, five respects were discussed to the RCCMM researches and resources recycling utilization ways and goals and tasks. First, based on the principle of resource scarcity, discovering or replacing CMM resources, protecting the rare or endangered species or resources. Second, based on the multifunctionality of CMM, realizing the value-added and value compensation, and promoting the utilization efficiency through systermatic and detailed exploitation and utilization. Third, based on the resource conservation and environment-friendly, reducing raw material consumption, lowering cost, promoting recycling utilization and elevating utilization efficiency. Fourth, based on the stratege of turning harm into good, using the invasive alien biological resources by multi-ways and enriching the medicial resources. Fifth, based on the method of structure modification of chemical components, exploring and enhancing the utility value of resouces chemical substances. These data should provide references and attention for improving the utilization efficiency, promoting the development of recycling economy, and changing the mode of economic growth of agriculture and industry of CMM fundamentally.
Agriculture ; economics ; trends ; China ; Conservation of Natural Resources ; economics ; trends ; Drugs, Chinese Herbal ; chemistry ; economics ; Materia Medica ; chemistry ; economics ; Medicine, Chinese Traditional ; economics ; trends ; Plants, Medicinal ; chemistry ; growth & development

The industrialization chains and their products, which were formed from the process of the production of medicinal materials-prepared drug in pieces and deep processed product of Chinese material medica (CMM) resources, have generated large benefits of social and economic. However, The large of herb-medicine castoff of "non-medicinal parts" and "rejected materials" produced inevitably during the process of Chinese medicinal resources produce and process, and the residues, waste water and waste gas were produced during the manufactured and deep processed product of CMM. These lead to the waste of resources and environmental pollution. Our previous researches had proposed the "three utilization strategies" and "three types of resources models" of herb-medicine castoff according to the different physicochemical property of resources constitutes, resources potential and utility value of herb-medicine castoff. This article focus on the conversion efficiency of resources model and analysis the ways, technologies, practices, and application in herb-medicine cast off of the conversion efficiency of resources model based on the recycling economy theory of resources and thoughts of resources chemistry of CMM. These data may be promote and resolve the key problems limited the industrialization of Chinese material medica for long time and promote the realization of herb-medicine castoff resources utilization.
Biotransformation ; Conservation of Natural Resources ; methods ; Drug Industry ; Drugs, Chinese Herbal ; chemistry ; metabolism ; Materia Medica ; chemistry ; metabolism ; Research Design

By repeated column chromatography, including silica gel, macroporous resin, and preparative HPLC, a new compound (1) was isolated and purified. On the basis of spectroscopic methods, the structure of 1 was elucidated as ( - ) -epiafzelechin-3, 5-di-O-beta-D-apiofuranoside (1). In the bioassay screening experiments, glucose consumption assays in IR HepG2 cells and colorimetric assay of surface GLUT4myc translocation were used to assess the effects on glucose metabolism of compound 1. Both compound 1 and its derivatives--naringin could improve glucose consumption in IR HepG2 cells and enhance GLUT4 translocation in skeletal muscle cell L6myc in a dose-dependent manner, indicating that these two compouds showed potential anti-diabetic activities in vitro.
Catechin ; analogs & derivatives ; pharmacology ; Dose-Response Relationship, Drug ; Glucose ; metabolism ; Glucose Transporter Type 4 ; metabolism ; Glycosides ; pharmacology ; Hep G2 Cells ; Humans ; Hypoglycemic Agents ; pharmacology ; Polypodiaceae ; chemistry ; Protein Transport ; drug effects

An efficient modified route based on the targeting mechanism of antibacterial fluoroquinolones for the shift from the antibacterial activity to the antitumor one was further developed. Using a fused heterocyclic ring, s-triazolothiadiazine as a carboxyl bioisostere of ciprofloxacin, the title compounds, 1-cyclopropyl-6-fluoro-7-piperazin-1-yl-3-(6-substituted-phenyl-7H-[1, 2, 4]triazolo[3, 4-b][1, 3, 4]thiadiazin-3-yl)-quinolin-4(1H)-ones (5a-5e) and their corresponding N-acetyl products (6a-6e), were designed and synthesized, separately. Meaningfully, a ring-contraction of fused six-membered thiadiazine occurred by a sulfur extrusion reaction gave new tri-acetylated fused heterocycles related to pyrazolo[5, 1-c][1, 2, 4] triazoles (7a-7e). The in vitro antitumor activity against L1210, CHO and HL60 cell lines was also evaluated for the synthesized fifteen heterocycles compared to parent ciprofloxacin by methylthiazole trazolium (MTT) assay. Interestingly, the results displayed that fifteen fused heterocyclic compounds showed more significant growth inhibitory activity (IC50 < 25.0 micromo x L(-1)) than that of parent ciprofloxacin (IC50 > 150.0 micromol x L(-1)), and the active order decreased from 7a-7e to 5a-5e to 6a-6e, respective.
Animals ; Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; CHO Cells ; Cell Line, Tumor ; Ciprofloxacin ; pharmacology ; Cricetinae ; Cricetulus ; Fluoroquinolones ; chemical synthesis ; chemistry ; pharmacology ; HL-60 Cells ; Humans ; Inhibitory Concentration 50 ; Leukemia L1210 ; pathology ; Mice ; Structure-Activity Relationship ; Thiadiazines ; chemical synthesis ; chemistry ; pharmacology ; Triazoles ; chemical synthesis ; chemistry ; pharmacology

To study chemical constituents from Pachysandra terminalis. By repeated column chromatography, including silica gel, Toyopearl HW-40, and preparative HPLC, four new (14) and one known (5) compounds were isolated and purified. On the basis of spectral data analysis, the structure of isolated compounds were elucidated as follow: 2-methyl-3-methylenepentane-1, 2, 5-triol (1), 4-methyl-3-methylenepentane-1, 2, 5-triol (2), 4-methyl-3-methylenepentane-1, 2, 5-triol-5-O-beta-D-glucopyranoside (3), 4-methyl-3-methylenep- entane-1, 2, 5-triol-1-O-beta-D-glucopyranoside (4), (7S, 8R, 8' R)-(+)-lariciresinol-9-O-beta-D-glucopyrano-side (5). Compound 5 was isolated from this genus for the first time.
Chromatography, Gel ; Chromatography, High Pressure Liquid ; Glucosides ; chemistry ; isolation & purification ; Molecular Structure ; Pachysandra ; chemistry ; Plant Extracts ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry

BACKGROUNDWilms' tumor (nephroblastoma) is a cancer of the kidneys that occurs typically in children and rarely in adults. Early diagnosis is very important for the treatment and prognosis of the disease. The aim of our study was to discover and identify potential non-invasive and convenient biomarkers for the diagnosis of Wilms' tumor.

METHODSNude mice were used to construct a Wilms' tumor model by injecting nephroblastoma cells into their bilateral abdomen. We collected 94 serum samples from mice consisting of 45 samples with Wilms' tumor and 49 controls. The serum proteomic profiles of the samples were analyzed via surface-enhanced laser desorption/ionization time-of-flight mass spectrometry. The candidate biomarkers were purified by high-performance liquid chromatography, identified by liquid chromatography-mass spectrometry, and validated using ProteinChip immunoassays.

RESULTSWe finally retrieved two differential proteins (m/z 4509.2; 6207.9), which were identified as apolipoprotein A-II and polyubiquitin, respectively. The expression of apolipoprotein A-II was higher in the Wilms' tumor group than in the control group (P < 0.01). By contrast, the expression of polyubiquitin was lower in the Wilms' tumor group than in the control group.

CONCLUSIONApolipoprotein A-II and polyubiquitin may be used as potential biomarkers for nephroblastoma in children, and the analysis of apolipoprotein A-II may help diagnose and treat Wilms' tumor.

Animals ; Apolipoprotein A-II ; blood ; Biomarkers ; blood ; Cell Line, Tumor ; Mice ; Mice, Nude ; Polyubiquitin ; blood ; Proteomics ; methods ; Wilms Tumor ; blood ; metabolism ; pathology

OBJECTIVETo investigate the relation between the alleles of HLA-DRB1*04 and outcome of HBV infection.

METHODSThe alleles of HLA-DRB1*04 were detected by polymerase chain reaction-sequence specific primer (PCR-SSP). The frequency of allele of HLA-DRB1*04 in four groups[106 asymptomatic HBsAg carriers (group ASC), 93 chronic hepatitis B patients (group CHB), 77 patients with hepatitis B cirrhosis and 102 cases of spontaneous recovery after HBV infection (control group)] were studied, and the frequency of that in different replication of HBV was also studied.

RESULTSThe frequency of allele of HLA-RB1*04 in groups ASC, CHB and hepatitis B cirrhosis was markedly higher than that of control group (25.94%, 26.34%, 27.92% respectively versus 14.22%, P< 0.01); the frequency of HLA-DRB1*0401 in groups ASC, CHB and hepatitis B cirrhosis was also higher than that of control group (20.91%, 24.49%, 22.09% respectively versus 8.62%, P< 0.05, P< 0.01,P< 0.05 respectively); the frequency of HLA-DRB1*0405 in groups ASC, CHB and hepatitis B cirrhosis was lower than that of control group (3.64%, 2.04%, 3.49% respectively versus 15.52%, P< 0.01, P< 0.01, P< 0.05 respectively ). There was no statistical significance in the allele frequency of HLA-DRB1*04 among groups ASC, CHB and hepatitis B cirrhosis (P> 0.05), and the same result was observed in different replication of HBV (P> 0.05).

CONCLUSIONHLA-DRB1*04 gene is one of the factors which determine the outcomes of HBV infection, while it has no influence on HBV replication.

Adolescent ; Adult ; Alleles ; Female ; Gene Frequency ; Genetic Predisposition to Disease ; genetics ; HLA-DR Antigens ; genetics ; HLA-DRB1 Chains ; Hepatitis B ; genetics ; pathology ; Humans ; Male ; Middle Aged ; Polymerase Chain Reaction ; Polymorphism, Genetic ; genetics ; Prognosis ; Young Adult

OBJECTIVETo investigate changes in apoptosis-related ligands in serum in rats with severe scald and the effect of intensive insulin therapy on the changes.

METHODSOne hundred and fifty Wistar rats were randomly divided into 3 groups: sham burn (SB), scald (S) and treatment (T) groups. Rats in S and T groups were inflicted with 40% TBSA full-thickness burn, followed by intraperitoneal injection with 40 mL/kg of isotonic saline for resuscitation. Rats in T group were subcutaneously injected insulin in a dose of 0.25 U/100 g 24 hours after burn injury, and every 12 hours for 5 days (0.25, 0.50, 0.75, 1.00, 1.25 U/100 g each day, respectively) to control the level of blood glucose between 3 and 6 mmol/L. Rats in SB group were sham scalded at 37 degrees C without resuscitation. Blood was drawn from abdominal aorta on 1, 4, 7, 10, 14 post burn day (PBD) for determination of serum levels of TNF-alpha, soluble Fas ligand (sFasL) and soluble Fas receptor (sFas) by enzyme-linked immunosorbent assay (ELISA), and insulin by radioimmunity assay (RIA).

RESULTSThe serum level of TNF-alpha in S group peaked on 1 PBD (30.9 +/- 8.7) ng/L, which showed statistically significant difference when compared with that of SB and T groups (12.7 +/- 2.8) ng/L, (16.8 +/- 4.7) ng/L, respectively, P < 0.01), then lowered gradually to become similar to that of SB group on 7 PBD. The level of TNF-alpha in T group increased gradually, but was obviously lower than that of S group on 1, 4, 7 PBD (P < 0.01). The level of sFasL in S (on 7-14 PBD) and T (4-10 PBD) groups was significantly higher than that in SB group (P < 0.05), then lowered to normal level. The levels of sFas on 4-10 PBD in T group were obviously higher than that in S and SB group (P < 0.05). Ratio of sFasL to sFas in serum of S group was higher than that in SB group on 7, 10 PBD, which was higher than that in T group on 7 PBD (P < 0.05). There was significant decrease in serum level of insulin in S group compared with that of SB group on 4-10 PBD (P < 0.05). The level of insulin in T group increased on 1 PBD, peaked on 4 PBD (327 +/- 15 microU/mL), which was significantly higher than that in SB and S groups (42 +/- 15, 28 +/- 10 microU/mL, respectively, P < 0.01), then decreased gradually to normal level.

CONCLUSIONSInsulin may inhibit apoptosis after burn by down-regulating secretion of apoptotic ligands.

Animals ; Apoptosis ; Blood Glucose ; analysis ; Burns ; blood ; drug therapy ; Fas Ligand Protein ; blood ; Insulin ; therapeutic use ; Male ; Rats ; Rats, Wistar ; Tumor Necrosis Factor-alpha ; blood ; fas Receptor ; blood