Objective: To explore the in vitro inhibition effect of Zuojin pills on 6 cytochrome P450 isoenzymes ( CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6 and CYP3A4) in human liver microsomes. Methods:The water extract of Zuojin pills, Cop-tidis Rhizoma and Euodiae Fructus was respectively incubated with human liver microsomes in the presence of seven probe substrates of CYP450 isoenzymes, and seven metabolites of cytochrome P450 probe substrate ( paracetamol/CYP1A2, 6α-hydroxypaclitaxel/CYP2C8, 4-hydroxydiclofenac/CYP2C9, 4-hydroxymephenytoin/CYP2C19, dextrorphan/CYP2D6, 6β-hydroxytestosterone/CYP3A4 and 1-hydroxymidazolam/CYP3A4) were simultaneously measured by LC-MS/MS, and the inhibitory effects were evaluated with IC50 value. Results:The IC50 value of Zuojin pills on CYP2D6, CYP1A2 and CYP3A4_T was 11. 6, 77. 4 and 97. 0 μg·ml-1 , respec-tively. The other IC50 values were from 334 to 690μg·ml-1 on CYP2C8, CYP2C9, CYP2C19 and CYP3A4_M isoenzymes. The IC50 value of Coptidis Rhizoma on CYP2D6, CYP1A2 and CYP3A4_T was 5. 8, 36. 8 and 59. 2 μg·ml-1 , respectively. The other IC50 values were from 163 to 476 μg·ml-1 on CYP2C8, CYP2C9, CYP2C19 and CYP3A4_M isoenzymes. The IC50 value of Euodiae Fructus on CYPs was over 107 μg·ml-1 . Conclusion:Zuojin pills shows notable inhibitory effect on CYP2D6, and weak inhibitory effects on CYP1A2 and CYP3A4_T. Coptidis Rhizoma has similar effects on CYPs and may be the main herbal medicine in the formu-la. Therefore, much attention should be paid to the combination of Zuojin pills and the drugs metabolized by human CYP2D6 in clin-ics.

Objective To understand the prevalence and distribution characteristics of symptoms of anorectal diseases in Chinese residents(older than 18) as to provide reference for prevention,care and treatment of anorectal diseases.Methods Stratified sampling was used according to the economic level in every province in the country,and each province selected two cities.Face-toface interviews were used to collect data in 68 906 interviewers and SPSS 17.0 was performed to analyze the data.Results Of 68 906 respondents,25 634 (37.20 ％) reported to suffer from at least one symptoms of anorectal diseases.The prevalence of the top 5 main symptoms of anorectal diseases were prolapse of anus neoplasms(14.55％),anal sore(16.53％),anal pendant expansion (14.98 ％),perianal abscess (5.88 ％),hematochezia (22.52 ％).Each symptom frequency difference was statistically significant (x2=7 727.6,P＜0.001).Populations which proned to suffer from symptoms of anorectal disease had the following characteristics:living in city,male,ageing 25-54 years old,having specialist qualifications,lacking of physical.Conclusion The prevalence of symptoms of anorectal diseases among Chinese residents was high,and each symptom had its distribution characteristics.More targeted interventions should be taken in anorectal disease prone people.

AIMTo study the effects of prophylene glycol mannate sulfate (PGMS) on monocyte chemoattractant protein-1 (MCP-1) mRNA expression in hyperlipidemic rat aorta and to clarify the molecular mechanism of PGMS for the prevention of atherosclerosis.

METHODSPGMS (37.8 and 75.6 mg.kg-1.d-1, ig) or PGMS (37.8 and 75.6 mg.kg-1.d-1, ig) combined with diethyldithiocarbamate (DDC, an inhibitor of SOD, 200 mg.kg-1 every three days, i.p.) were given to hyperlipidemic rats for three weeks. The MDA content and SOD activity were determined after 12 h of starvation, and MCP-1 mRNA expression in aorta was detected by reverse transcription-polymerase chain reaction (RT-PCR).

RESULTSThere was significant decrease (29.46% or 58.40)% of MCP-1 mRNA expression in aortic after the therapy. The SOD activity increased markedly and the MDA content decreased at the same time. After treatment with DDC, the SOD activity was inhibited and the MDA content increased, but with no significant effect on MCP-1 mRNA expression.

CONCLUSIONPGMS inhibited MCP-1 mRNA expression with no relation to its effect on decreasing MDA content.

Animals ; Aorta, Thoracic ; drug effects ; metabolism ; Chemokine CCL2 ; biosynthesis ; genetics ; Gene Expression ; drug effects ; Hyperlipidemias ; blood ; pathology ; Hypolipidemic Agents ; pharmacology ; Male ; Malondialdehyde ; blood ; metabolism ; Propylene Glycols ; pharmacology ; RNA, Messenger ; biosynthesis ; drug effects ; Random Allocation ; Rats ; Rats, Wistar ; Superoxide Dismutase ; blood ; metabolism

Dunhuang medicine is a branch of Dunhuang studies, including the characteristics of Dunhuang ancient medical prescriptions and treatment technique.Dunhuang Dabupi Decoction has good efficacy in nourishing vitality and yin and promoting the production of body fluid. Professor WANG Dao-kun used the prescription to treat gastric stuffiness, gaining significant curative effect. This article summaried cases of using this prescription, to show the advantages of Dunhuang ancient medical prescription Dabupi Decoction for present use.

OBJECTIVETo study the chemical constitutes of Acantophora spicifera.

METHODCompounds were isolated by normal phase silica gel and Sephadex LH-20 gel column chromatography, and reverse-phase HPLC, as well as recrystallization. Their structures were elucidated by spectroscopic methods.

RESULTSeven compounds were isolated from A. spicifera and their structures were identified as aplysin (1), loloilide (2), (R)-(-)-dehydrovomifoliol (3), uracil (4), thymine (5), 1-methoxy-4-(1-propenyl) benzene (6).

CONCLUSIONThe compounds were obtained from this genus for the first time. Compound 6 was firstly obtained from marine organisms.

Chromatography ; methods ; Chromatography, High Pressure Liquid ; methods ; Rhodophyta ; chemistry ; isolation & purification ; Sesquiterpenes ; chemistry ; isolation & purification ; Styrenes ; chemistry ; isolation & purification ; Thymine ; chemistry ; isolation & purification ; Uracil ; chemistry ; isolation & purification

OBJECTIVETo investigate the chemical constituents of marine alga Chaetomorpha basiretorsa.

METHODCompounds were isolated by normal phase silica gel and Sephadex LH-20 gel colum chromatography, reverse phase MPLC, reverse phase HPLC and recrystallization. Their structures were elucidated by spectroscopic methods including MS, IR, NMR, and X-ray crystalography. Cytotoxicity of the compounds were screened by using standard MTT method.

RESULTNine compounds were isolated from C. basiretorsa and their structures were identified as N-phenyl-2-naphthalenamine( I ), dibutyl phthalate( II ), diisobutyl phthalate( III ), 1-phenyl-ethane-1, 2-diol( IV ), 2-hydrox-gamma-benzaldehyde( V ), diethyleneglycol monobenzoate( VI ), uracil( VII ), thymine( VIII ) and thymidine( IX ).

CONCLUSIONAll these compounds were obtained from this genus for the first time, N-phenyl-2-naphthalenamine and diethyleneglycol monobenzoate were first reported from the marine organisms. Compound I and VII showed moderate activity against KB cell(IC50 10.15 microg x mL(-1) for I and 3.79 microg x mL(-1) for VII ) and MCF-7 cell(IC50 3.24 microg x mL(-1) for VII).

1-Naphthylamine ; analogs & derivatives ; chemistry ; isolation & purification ; Chlorophyta ; chemistry ; Crystallization ; Humans ; KB Cells ; drug effects ; Uracil ; chemistry ; isolation & purification ; pharmacology

OBJECTIVETo search for chemical constituents with structural diversity from Laurencia tristicha to supply for biological assay.

METHODCompounds were isolated by means of column chromatography over normal phase silica gel and Sephadex LH-20, recrystallization and HPLC. Structures were identified by spectroscopic methods including 1D NMR, IR and MS. Cytotoxicities of the purified compounds were evaluated by MTT method.

RESULTSeven compounds were isolated from L. tristicha. Their structures were elucidated as cholesterol (1), cholesta- 5-en-3beta, 7alpha-diol (2), beta-stigmasterol (3), phytol (4), zeaxanthin (5), 4 -hydroxybenzaldehyde (6), indolyl-3-carbaldehyde (7). In the cytotoxic assay compound 2 was active against human cancer cell lines HCT-8, Bel-7402, BGc-823, A549 and HELA with IC50 values of 1.90, 2.02, 1.99, 6.52 and 1.20 microg x mL(-1), respectively. Compound 4 showed cytotoxicity against HCT-8 and HELA with IC50 value of 3.51 and 2.04 microg x mL(-1), and other compounds were inactive ( IC50 > 10 microg x mL(-1)).

CONCLUSIONCompounds 1-7 were isolated from L. tristicha for the first time. In additon, compounds 2 and 4 were cytotoxic against several human cancer cell lines.

Antineoplastic Agents ; chemistry ; isolation & purification ; pharmacology ; Cell Line, Tumor ; drug effects ; Cholestenes ; chemistry ; isolation & purification ; pharmacology ; Cholesterol ; chemistry ; isolation & purification ; pharmacology ; Humans ; Inhibitory Concentration 50 ; Laurencia ; chemistry ; Phytol ; chemistry ; isolation & purification ; pharmacology

Objective To evaluate the effectiveness of minimally invasive therapy on treating hypertensive cerebral hemorrhage.Methods 40 cases hypertensive cerebral hemorrhage were randomly divided into two groups, 20 cases were received the minimally invasive drainage therapy and 20 cases medicine therapy.Results Effective rate was high(P

OBJECTIVETo observe the expression of the matrix metalloproteinase 2 (MMP-2) and membrane-type 1 metalloproteinase (MT1-MMP) in lung of rats exposed to paraquat (PQ) and the effects of Salvia miltiorrhiza monomer IH764-3 on above expression.

METHODSNinety adult healthy Sprague-Dawley (SD) rats were randomly divided into the control group (group A, 6 rats), the exposure group (group B, 42 rats) and the group treated by Salvia miltiorrhiza monomer IH764-3 (group C, 42 rats). The group B and C were treated intragastrically with 1ml of PQ (50 mg/kg), and the group A was treated intragastrically with normal saline. The group C was treated intraperitoneally with 1 ml Salvia miltiorrhiza monomer IH764-3 at the dose of 40 mg/kg a day. The group A and B were treated intraperitoneally with 1 ml normal saline day. The expression of MMP-2 and MT1-MMP was detected on the 1st, 3rd, 7th, 14th, 21st, 28th and 35th days after exposure for all groups.

RESULTSAs compared with the expression level (0.305 ± 0.045) of MMP-2 mRNA in group A, the expression levels of MMP-2 mRNA in Group B significantly increased, which were 0.654 ± 0.077, 0.623 ± 0.051, 0.637 ± 0.024, 0.533 ± 0.043 and 0.552 ± 0.050 on the 1st, 3rd, 7th, 14th, 21st days after exposure, respectively (P < 0.01). As compared with group A, the the expression levels of MMP-2 mRNA on the 1st, 3rd, 7th days in Group C slightly increased, but the expression levels of MMP-2 mRNA on the 1st, 3rd, 7th, 14th, 21st days in Group C were 0.523 ± 0.074, 0.567 ± 0.097, 0.514 ± 0.058, 0.359 ± 0.018 and 0.374 ± 0.020, respectively, which were significantly lower than those in group B (P < 0.01). As compared with the expression level (0.391 ± 0.058) of MT1-MMP mRNA in group A, the expression levels of MT1-MMP mRNA in Group B significantly increased, which were 0.796 ± 0.021, 0.762 ± 0.043, 0.590 ± 0.010, 0.803 ± 0.076 and 0.680 ± 0.034 on the 1st, 3rd, 7th, 14th and 21st days after exposure, respectively (P < 0.01). As compared with group A, the expression levels of MT1-MMP mRNA in Group C significantly increased, which were 0.594 ± 0.010, 0.653 ± 0.044 and 0.564 ± 0.009 on the 1st, 3rd and 21st days after exposure, respectively (P < 0.01). The expression levels of MT1-MMP mRNA in Group C were significantly lower than those in group B (P < 0.05 or P < 0.01).

CONCLUSIONThe expression changes of MMP-2 and MT1-MMP genes of lungs in rats intragastrically exposed to PQ could result in the unbalance the synthesis and degradation of ECM, which may be a cause of lung fibrosis. The Salvia miltiorrhiza monomer IH764-3 could affect the expression of MMP-2 and MT1-MMP genes to a certain extent, resulting in the reduction of lung fibrosis.

Animals ; Drugs, Chinese Herbal ; pharmacology ; Female ; Lung ; drug effects ; metabolism ; Male ; Matrix Metalloproteinase 14 ; metabolism ; Matrix Metalloproteinase 2 ; metabolism ; Paraquat ; toxicity ; RNA, Messenger ; genetics ; Rats ; Rats, Sprague-Dawley ; Salvia miltiorrhiza

AIMTo study the effect of propylene glycol mannate sulfate (PGMS) on blood lipids and lipoprotein lipase in hyperlipidemic rat, and its anti-hyperlipidemic mechanism.

METHODSPGMS was administered ig at different doses (37.8 mg.kg-1.d-1 and 75.6 mg.kg-1.d-1) to hyperlipidemic rats for three weeks and blood serum was obtained after starved 12 h. Total cholesterol (TC), triglyceride (TG), low density lipoprotein cholesterol (LDL-C) and high density lipoprotein cholesterol (HDL-C) were examined. The mRNA expression of lipoprotein lipase (LPL) in liver, spleen and artery was detected by reverse transcription polymerase chain reaction (RT-PCR).

RESULTSPGMS significantly decreased the levels of TC, TG and LDL-C and increased that of HDL-C in hyperlipidemic serum dose-dependently. PGMS was shown to increase the level of LPL mRNA expression, which is related directly to the controlling effects of PGMS on blood lipids.

CONCLUSIONPGMS modulated blood lipids by promoting mRNA expression of LPL. This may be one important mechanism of PGMS to modulate blood lipids.

Animals ; Cholesterol, HDL ; blood ; Disease Models, Animal ; Hyperlipidemias ; blood ; drug therapy ; enzymology ; Lipoprotein Lipase ; biosynthesis ; genetics ; Male ; Propylene Glycols ; therapeutic use ; RNA, Messenger ; biosynthesis ; Random Allocation ; Rats ; Rats, Wistar ; Triglycerides ; blood