Cardiac Pacing, Artificial ; adverse effects ; Diaphragm ; Female ; Humans ; Muscular Diseases ; etiology ; Pacemaker, Artificial ; Young Adult

OBJECTIVETo establish an HPLC-DAD/ESI-MS method for quickly identifying chemical constituents in diterpene lactone effective fraction of Andrographis panniculata and to study its pharmacodynamics.

METHODThe separation was performed on an Agilent SB-C18 column (2.1 mm x 150 mm, 5 μm) with a mobile phase of acetonitrile (A) and water (B). The flow rate was maintained at 0.4 mL x min(-1) and detection wavelength was set at 205 nm. The samples were analyzed in positive ion mode, and mass scan range was m/z 50-1 000. Using two kinds of tumor cell lines made living animal models, and studied preliminary pharmacodynamics on anti-tumor aspect.

RESULTFive diterpene lactones in the diterpene lactone effective fraction of A. panniculata could be separated in one run. Pharmacodynamic experiments showed that the effectve fraction had an inhibitory effect on the growth of tumor.

CONCLUSIONA rapid and efficient HPLC-ESI-MS method to determine the chemical constituents in diterpene lactone effective fraction of A. panniculata has been established, and the preliminary pharmacodynamics research has been done, which could be used for the quality control and further studies of diterpene lactone effective fraction of A. panniculata in vivo.

Andrographis ; chemistry ; Animals ; Antineoplastic Agents, Phytogenic ; administration & dosage ; chemistry ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; Female ; Humans ; Lung Neoplasms ; drug therapy ; physiopathology ; Mice ; Mice, Inbred C57BL ; Spectrometry, Mass, Electrospray Ionization

Objective To investigate the relapse risk assessment for patients with acute promyelocytic leukemia(APL)through testing PML-RAR? fusion gene by real-time quantitative polymerase chain reaction(RQ-PCR).Methods Relative copies of PML-RAR? fusion gene were measured in 25 patients with APL in phases of first diagnosis,complete remission(CR)and relapse.The minimal residual disease(MRD)situations were also monitored in 6 of the 25 patients.Results Different PML-RAR? fusion gene expression levels were observed in patient groups of different phases of the disease.(P

Syl948 is a synthesized selective S1P1 agonist with novel structure. HTRF-IP1 test indicated that Syl948-P, the active form of Syl948 in vitro, has strong activity against S1P1 (EC50: 83 +/- 16 nmol x L(-1)), but its effect on S1P3 was very weak (EC50: 1 026 +/- 90 nmol x L(-1)). In SD rats, oral administration of Syl948 10 mg x kg(-1) significantly decreased the peripheral blood lymphocytes (PBL), with the maximal PBL inhibition rate of 63%, which was as similar as equal dose of fingolimod (FTY720). Oral administration of Syl948 10 mg x kg(-1) had no effect on heart rate of SD rats, which was better than FTY720. Daily oral administration with Syl948 (2 or 4 mg x kg(-1)) significantly prolonged the survival time of the allografts of skin slice on mice. In summary, the above results demonstrated that Syl948 has great selectivity in vitro and good activity in vivo, which indicated its potential use as an anti-rejection drug in skin transplantation.
Animals ; Fingolimod Hydrochloride ; Graft Survival ; drug effects ; Immunosuppressive Agents ; pharmacology ; Lymphocytes ; drug effects ; Mice ; Propylene Glycols ; pharmacology ; Rats ; Receptors, Lysosphingolipid ; agonists ; Skin Transplantation ; Sphingosine ; analogs & derivatives ; pharmacology ; Transplantation, Homologous

Tumorous cells are characterized by distinctive metabolic reprogramming and living conditions. Understanding drug metabolizing features in tumor cells will not only favor the estimation of metabolic rate, elimination half life and the assessment of potency, but also facilitate the optimal design of anti-tumor drugs/prodrugs. This article reviewed the expression and activity features of major drug metabolizing enzymes (DMEs) in solid tumorous tissues, such as liver, intestine, breast and lung, and the difference from the correspondingly normal tissues, exemplified by the metabolic properties of some classic antitumor-agents in tumorous tissues. In combination with the data retrieved in vitro tumor cell lines, we discussed the similarities and differences of DMEs expression and function between tumor tissues (in vivo) and tumor cells (in vitro), and proposed the possible factors that cause the differences.
Antineoplastic Agents ; pharmacokinetics ; Cell Line, Tumor ; Humans ; Inactivation, Metabolic ; Liver ; metabolism ; Neoplasms ; enzymology ; Prodrugs ; pharmacokinetics

Fourteen compounds were isolated by column chromatography from the ethyl acetate extract of the seeds of Brassica campestris. Their structures were elucidated by physicochemical properties and spectroscopic data analysis. The isolated compounds were respectively identified as (5Z,7E)-4, 4-dimethyl-5-acetyl-5, 7-nonadienoic acid (1), indole-3-carboxaldehyde (2), blumenol A (3), vinylsyringol (4), sinapinic acid (5), sinapic acid ethyl ester (6), protocatechuic acid (7), crinosterol (8), campesterol (9), 7-oxo-stigmasterol (10), kaempferol (11), 2,5-dihydroxybenzoic acid (12), syringic acid (13) and daucosterol (14). Compound 1 was a new compound and the other compounds were isolated from this plant for the first time except for compounds 4, 5 and 13.
Brassica ; chemistry ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Molecular Structure ; Seeds ; chemistry ; Spectrometry, Mass, Electrospray Ionization

A series of novel sorafenib analogues were designed and synthesized. The cytotoxic activities of these compounds were tested in four tumor cell lines. Some of the compounds showed potent antiproliferative activity against the tested cell lines with IC50 = 4-20 micromol x L(-1). Some compounds demonstrated competitive antiproliferative activities to sorafenib against tested cancer cell lines. Among them, compound 7c demonstrated significant inhibitory activities on ACHN, HCT116 and MDA-MB-231 cell lines with IC50 values of 9.01, 4.97, 6.61 micromol x L(-1), respectively.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Humans ; Inhibitory Concentration 50 ; Molecular Structure ; Niacinamide ; analogs & derivatives ; chemical synthesis ; chemistry ; pharmacology ; Phenylurea Compounds ; chemical synthesis ; chemistry ; pharmacology ; Structure-Activity Relationship

OBJECTIVETo observe the expression of Ginkgo biloba Tablet (GbT) on scavenger receptor A (SRA) of the aortic wall and changes of serum inflammatory factors in atherosclerotic rats, and to explore its new mechanism for fighting against atherosclerosis (AS).

METHODSTotally 45 male Wistar rats were randomly divided into the control group, the model group, the GbT group, 15 rats in each group. Levels of blood glucose, blood lipids, blood calcium, serum C-reactive protein (CRP), soluble intercellular adhesion molecule-1 (slCAM-1), and soluble vascular cell adhesion molecule-1 (sVCAM-1) were measured in all rats. The expression of SRA in the aortic wall of atherosclerotic rats was observed by immunohistochemical assay. The correlation between the expression of SRA and levels of in-flammatory factors was also observed.

RESULTSCompared with the control group, blood glucose and blood calcium obviously increased (P < 0.05); levels of TG, TC, and LDL-C were significantly elevated (P < 0.01); neointimal areas were significantly thickened, increased intima percentage was significantly enlarged, narrowed lumen index was significantly reduced; levels of CRP, sICAM-1, and sVCAM-1 were significantly elevated in the model group (all P < 0.01). Compared with the model group, blood glucose and blood calcium obviously decreased (P < 0.05); levels of TG, TC, and LDL-C significantly decreased (P < 0.01) in the GbT group. Aortic lumens were obviously narrower in the model group than in the GbT group (P < 0.05). SRA expressed at the aortic wall. The aforesaid 3 indices were significantly improved in the GbT group than in the model group (P < 0.01). Serum levels of CRP, sICAM-1, and sVCAM-1 were significantly decreased in the GbT group than in the model group (P < 0.01). Serum levels of CRP, sICAM-1, and sVCAM-1 were positively correlated with the percentage of SRA positive expression area (r = 0.701, 0.604, 0.581, all P < 0.01).

CONCLUSIONSSerum levels of inflammatory factors in atherosclerotic rats were elevated, and the expression of SRA in the aortic wall was enhanced. The expression of SRA was closely correlated with serum levels of inflammatory factors. GbT could decrease serum levels of inflammatory factors and inhibit the expression of SRA.

Animals ; Aorta ; drug effects ; metabolism ; Atherosclerosis ; drug therapy ; Blood Glucose ; analysis ; C-Reactive Protein ; analysis ; Calcium ; blood ; Drugs, Chinese Herbal ; pharmacology ; Ginkgo biloba ; chemistry ; Intercellular Adhesion Molecule-1 ; blood ; Lipids ; blood ; Male ; Random Allocation ; Rats ; Rats, Wistar ; Scavenger Receptors, Class A ; metabolism ; Tablets ; Vascular Cell Adhesion Molecule-1 ; blood

Humans ; Lung Neoplasms ; metabolism ; pathology ; surgery ; Lymph Node Excision ; Male ; Middle Aged ; Pneumonectomy ; methods ; Pulmonary Blastoma ; metabolism ; pathology ; surgery ; Vimentin ; metabolism

Objective:To observe the effect of Shuxuetong Injection on unstable angina pectoris in diabetic pa- tients after coronary stent implantation.Method:40 diabetic patients after coronary stent implantation were randomly divid- ed into two groups.The patients in the two groups were treated with basic drugs.17 patients in the controlled group were venously treated with Danshen injection 6 milliliters dissolved in 250 milliliters 0.9% sodium chloride injection once daily. 23 patients in the treatment group were venously treated with Shuxuetong injection 6 milliliters dissolved in 250 milliliters 0.9% sodium chloride injection once a day.The treatment course was fifteen days in both groups.The clinical effect and the frequency of angina attack were observed in both groups.The concentrations of plasma fibrinogen(FBG)and serum C- reactive protein(CRP)were measured before and after the treatment.Result:Compared with those of the controlled group, the frequency of angina attack and the indication of myocardial ischema in electrocardiogram greatly improved(P