Cassiae Semen is a common traditional Chinese medicine, and contents of anthraquinones of Cassiae Semen different significantly from area to area. According to Chinese Pharmacopoeia (2010 edition), only contents of aurantio obtusin and chrysophanol were used to evaluate the quality of Cassiae Semen, another data could be added later. Ten batches of Cassiae Semen from different areas were determined, and total anthraquinones, total free anthraquinones and total combined anthraquinones contents were assessed by ultraviolet visible spectrophotometer, contents of aurantio obtusin, rhein, aloe emodin, emodin, chrysophanol and physcion were determined by HPLC. After that, principal components analysis was used to evaluate these data determined previous by dimension reduction analysis. At last, the result suggests that three main components were found out, it shows that content of aloe emodin could be used to evaluate the quality of Cassiae Semen as well as contents of aurantio obtusin and chrysophanol. And Cassiae Semen from Hebei province posseses higher quality than Cassiae Semen from other different areas. All these results can provide a good reference for quality evaluating of Cassiae Semen medicinal materials at a certain extent.
Anthraquinones ; analysis ; Cassia ; chemistry ; Chromatography, High Pressure Liquid ; Principal Component Analysis

Objective To investigate clinical feature,therapy and prognosis of 63 (rhabdomyolysis,RM) patients.Methods Retrospective analysis was used for the 63 patients who were from Nanjing from Janurary 2010 to August of 2016.Results Clinical history:the pathogenic factors mainly contained eating lobster,excessive exercise,lipid-lowering drugs,and minority patients were induced by infection,cardiac defibrillation,alcohol,and unexplained factors.Clinical features:most patients presented different degree of muscle soreness and weakness,and urine color of soy sauce;and few patients manifested a fever,respiratory distress and sound hoarse.Of which 11 RM patients concurrent acute kidney injury (AKI),there was no obvious bias of pathogenic factors among 11 patients.Clinical examination:the data was described by median,including creatine kinase 6 400 U/L,aspartate aminotransferase 399 U/L,lactate dehydrogenase 816 U/L,α-hydroxybutyric acid 445 U/L,and myoglobin 1 200 ng/ml.Creatine kinase and myoglobin were selected to measure muscle injure,there was no significant difference among the groups (P ＞ 0.05).Renal tubular injury index such as urincosmotic pressure,urine retinol-binding protein and N-acetyl-beta-D-glucosaminidase (NAG) enzyme,the abnormal percentage were 62.5％,50％,and 47.6％.Treatment:patients without complications through resting,water infusion,urine alkalization,were cured;and 11 cases of patients with AKI,1 case gave up,5 cases underwent hemodialysis,and 5 cases underwent conservative treatment,creatinine decreased to the basic level.Conclusions Among different pathogenic factors of RM,there were no obvious differences in clinlcal symptom,muscle damage degree,and whether the coexistence of AKI and prognosis.The understanding of RM,early diagnosis and treatment would prevent AKI and improve the prognosis.

To figure out the stability and intestinal bacteria metabolites of rats in vitro of astragaloside IV ( AST), this research was done to explore the stability of AST in the artificial gastric juice. artificial intestinal juice and rat liver homogenate and the metabolism in rat intestinal in vitro. HPLC was used to calculate the remaining rate of AST in biological samples by measuring the content of AST, while metabolites were determined by combining the methods of TLC, HPLC and LC-MS/MS. It turned out that AST was difficult to metabolize in the artificial gastric juice, artificial intestinal juice and rat liver. Also, the metabolic pathway of AST was stepped by deglycosylation. Firstly, AST was converted to its secondary etabolites (6-O-β-D-glucopyranosyl- cycloastragenol, CMG) by removal of xylose moiety at C-3, then transformed into cycloastragenol (CAG) after hydrolytic removal of the glucose moiety at C-6. All the results suggested that the metabolism of AST in vivo occurs mainly in the intestinal by hydrolysis of glycosyl. In conclusion, hydrolysis of intestinal flora is the main reason that AST metabolizes.
Animals ; Bacteria ; metabolism ; Chromatography, High Pressure Liquid ; Drug Stability ; Intestines ; microbiology ; Liver ; metabolism ; Rats ; Rats, Sprague-Dawley ; Saponins ; chemistry ; metabolism ; Tandem Mass Spectrometry ; Triterpenes ; chemistry ; metabolism

OBJECTIVETo prepare a novel floating micropellets containing hydroxy propyl-beta-oyclodextrin(puerarin-HP-beta-CD) for gastroretentive dosage form and evaluate its pharmaceutical characteristics in vitro.

METHODThe puerarin HP-beta-cyclodextrin inclusion complex was prepared by freeze-drying method. Puerarin and its HP-beta-CD inclusion complex were incorporated into alginate beads, respectively. The effect of methyl cellulose (MC), Mg-Stearate and chitosan on buoyancy and cumulative release rate of puerarin were investigated in simulated gastric fluid.

RESULTThe spectrums of FTIR and profiles of X-ray powder diffraction of samples proved the formation of inclusion complex between puerarin and HP-beta-CD. Magnesium stearate had a significant effect on the buoyancy of micropellets, and satisfied results were gained by the content with 2%. The solubility of puerarin was increased 65.6-fold by the formation of inclusion complex, the dissolution rate and cumulative release percentage also improved significantly although with the burst release phenomena. The micropellets showed sustained release properties by using puerarin-HP-beta-CD inclusion complex mixed with puerarin (1:1) and treated thoroughly under homogenizer.

CONCLUSIONThe solubility and release rate of puerarin are increased by the formation of inclusion complex with HP-beta-CD and its gastroretentive dosage forms displayed satisfied floating and sustained release characteristics.

2-Hydroxypropyl-beta-cyclodextrin ; Dosage Forms ; Freeze Drying ; Isoflavones ; chemistry ; Solubility ; Spectroscopy, Fourier Transform Infrared ; X-Ray Diffraction ; beta-Cyclodextrins ; chemistry

OBJECTIVETo observe the killing effect of Herceptin and adriamycin sequentially applied on breast cancer cell line in vitro.

METHODSBT-474 human breast cancer cells in exponential growth phase were treated with Herceptin alone, adriamycin alone and their sequential administration (Herceptin before adriamycin and vice versa), respectively. Under optical microscope, the morphological changes of the cells were observed before and after drug administration. The expression rate and mean fluorescence intensity (MFI) of HER-2/neu and cell death rate were detected by flow cytometry.

RESULTSMicroscopically, the cells treated with different protocols all exhibited such changes as darkening and increase of cellular debris with irregular cell morphology. Flow cytometry revealed no significant difference in the expression rate of HER-2/neu in each group before and after treatment, but the MFI of HER-2/neu and death rate of the treated cells were significant different from those of the control group (P<0.05). The cell death rate of Herceptin-pretreated cells was significantly higher than that of adriamycin-pretreated ones (P<0.05).

CONCLUSIONHerceptin pretreatment enhances the killing effect of adriamycin on breast cancer cell line BT-474, which provides experimental evidence for designing clinical sequential biochemotherapy of breast cancer.

Antibiotics, Antineoplastic ; pharmacology ; Antibodies, Monoclonal ; pharmacology ; Antibodies, Monoclonal, Humanized ; Antineoplastic Agents ; pharmacology ; Breast Neoplasms ; metabolism ; pathology ; Cell Death ; drug effects ; Cell Line, Tumor ; Doxorubicin ; pharmacology ; Drug Synergism ; Female ; Flow Cytometry ; Humans ; Receptor, ErbB-2 ; biosynthesis ; Trastuzumab

Epiberberine, one of the most important isoquinoline alkaloid in Coptidis Rhizoma, possesses extensive pharmacological activities. In this paper, the liquid chromatography-tandem mass spectrometry (LC-MS/MS) was used to study phase I and phase II metabolites. A Thermo HPLC system (including Surveyor AS, Surveyor LC Pump, Surveyor PDA. USA) was used. The cocktail probe drugs method was imposed to determine the content change of metoprolol, dapsone, phenacetin, chlorzoxazone and tolbutamide simultaneously for evaluating the activity of CYP2D6, CYP3A4, CYP1A2, CYP2E1 and CYP2C9 under different concentrations of epiberberine in rat liver microsomes. The result showed that epiberberine may have phase I and phase II metabolism in the rat liver and two metabolites in phase I and three metabolites in phase II are identified in the temperature incubation system of in vitro liver microsomes. Epiberberine showed significant inhibition on CYP2D6 with IC50 value of 35.22 μmol L(-1), but had no obvious inhibiting effect on the activities of CYP3A4, CYP1A2, CYP2E1 and CYP2C9. The results indicated that epiberberine may be caused drug interactions based on CYP2D6 enzyme. This study aims to provide a reliable experimental basis for its further research and development of epiberberine.
Animals ; Berberine ; analogs & derivatives ; chemistry ; metabolism ; Chromatography, High Pressure Liquid ; Cytochrome P-450 CYP2D6 ; metabolism ; Cytochrome P-450 CYP2D6 Inhibitors ; chemistry ; metabolism ; Drugs, Chinese Herbal ; chemistry ; metabolism ; Male ; Microsomes, Liver ; drug effects ; enzymology ; metabolism ; Molecular Structure ; Rats ; Rats, Sprague-Dawley ; Tandem Mass Spectrometry

OBJECTIVETo investigate the killing effect of ZD6474 combined with adriamycin (ADM) on MCF-7 human breast cancer cells.

METHODSThe inhibitory effects of ZD6474 and ADM alone and in combination on the proliferation of MCF-7 cells were assessed by MTT assay. The cell cycle and cell apoptosis were detected by flow cytometry.

RESULTSZD6474 and ADM both significantly inhibited the proliferation of MCF-7 cells, showing a synergistic effect of their reactions in combined use (P<0.05). ZD6474 or ADM alone caused cell cycle arrest at G0/G1 and S phases, respectively. Combined use of the two drugs resulted in significant reduction of the M-phase cell percentage and cell cycle arrest at G0/G1 and S phases. The coadministration of the drugs significantly increased the apoptosis rate of the cells as compared with ZD6474 or ADM treatment alone (P<0.05).

CONCLUSIONSZD6474 and ADM show a synergistic effect in inhibiting the proliferation and inducing apoptosis of MCF-7 cells.

Antibiotics, Antineoplastic ; pharmacology ; Antineoplastic Agents ; pharmacology ; Apoptosis ; drug effects ; Breast Neoplasms ; pathology ; Cell Cycle ; drug effects ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Doxorubicin ; pharmacology ; Drug Synergism ; Female ; Humans ; Piperidines ; pharmacology ; Quinazolines ; pharmacology

BACKGROUNDThe elevated matrix metalloproteinase (MMP) activity is an important cause of chronic wound healing failure. Arsenolite, whose main component is arsenic trioxide (As2O3), is a common traditional Chinese medicine wildly used in treating chronic wounds; it can remove necrotic tissue and promote tissue regeneration. This research was designed to evaluate the effects of As2O3 on production and activities of MMP-1, MMP-2 and MMP-9, and on regulation of its signal transduction pathway in human skin fibroblasts (HSFb) and human monocyte line (THP-1 cells) that were in an inflammatory state.

METHODSWe established three cell models; HSFb activated by TNF-α, THP-1 cells activated by phorbol 12-myristate 13-acetate (PMA) and an HSFb-THP-1 co-culture system. Three cell models was cultured with As2O3 for 24 hours. The levels of MMP-1, MMP-2, MMP-9, TNF-α and IL-1β in the cell culture supernatants were assayed by ELISA. The mRNA expressions of MMP-1, MMP-2 and MMP-9 were determined by RT-PCR. The activities of MMP-2 and MMP-9 were tested by Gelatin zymography assays. The phosphorylation levels of ERK1/2 and p38MAPK were assayed by Western blotting.

RESULTSAs2O3 inhibited the expression of MMP-1, MMP-2 and MMP-9 mRNA, the secretion and activity of MMP-1, MMP-2 and MMP-9 in HSFb and THP-1 cells in the inflammatory state (P < 0.05 and P < 0.01 respectively). It also inhibited the secretion of TNF-α and IL-1β in THP-1 cells and in the co-culture system (P < 0.05 and P < 0.01, respectively). It also decreased the phosphorylation of ERK1/2 and p38 MAPK in HSFb and THP-1 cells (P < 0.05 and P < 0.01, respectively).

CONCLUSIONSAs2O3, as a main component of arsenolite, can inhibit the production of MMPs by HSFb and THP-1 cells in an inflammatory state through inhibiting the release of inflammatory factors and the activation of the MAPK cascade pathway. This may be a possible mechanism for arsenolite healing chronic wounds.

Arsenicals ; pharmacology ; Cell Line ; Cells, Cultured ; Electrophoresis, Polyacrylamide Gel ; Fibroblasts ; drug effects ; enzymology ; Humans ; Interleukin-1 ; metabolism ; Matrix Metalloproteinase 1 ; metabolism ; Matrix Metalloproteinase 2 ; metabolism ; Matrix Metalloproteinase 9 ; metabolism ; Monocytes ; drug effects ; enzymology ; Oxides ; pharmacology ; Tumor Necrosis Factor-alpha ; metabolism

Objective To investigate the related risk factors for dyed cornea of orthokeratology, and to analyze the related risk factors, and to determine the independent risk factors, Provide evidence for intervention measures. Methods The clinical date were investigated for 990 patients with fitting orthokeratology lens between may.2014 and may.2016 in our hospital,through access to medical records, follow-up visit,questionnaire investigation to find out the cause of orthokeratology adverse reactions, the related risk factors were analyzed by univariate and multivariate Logistic regression analysis, using SPSS17.0 statistical processing. Results The incidence rate of dyed cornea of orthokeratology lens fitting in was 14.55%(144 in 990 patients); the single factor analysis found gender, age, region, refraction, lens position, family members, no significant difference . Eye disease combined (χ2= 28.73, P＜0.01), Schirmer I test (χ2=17.68, P＜0.01), lens activity (χ2=67.1, P＜0.01), Lens deposit(χ2=64.29, P＜0.01), lens wearing time (χ2=43.25, P＜0.01), health habits (χ2=38.01, P＜0.01) and water resources (χ2=3.81, P＜0.05), the difference was statistically significant; Logistic Logistic regression analysis found that Schirmer I test ( OR=4.126, P=0.003), lens activity ( OR=1.733, P=0.104), Lens deposit( OR=3.723, P=0.038), lens wearing time ( OR=5.034, P=0.002), health habits ( OR=6.544, P=0.002) and water resources ( OR=7.501, P=0.002) were independent risk factors for adverse reactions of orthokeratology. Conclusions Intervention measures that improve the fitting technology, complete removal of lens depositthe, Control wearing time, improve the health behaviors of the patients with the habit, use saline and professional cleaning are of great significance to reduce the incidence of adverse reactions of orthokeratology.

OBJECTIVE: To analyze the echocardiographic abnormalities and the prevalence of anticardiolipin antibodies (aCL) in systemic lupus erythematosus (SLE) patients and to evaluate the relationship between aCL and cardiac valvular abnormalities in SLE patients. METHODS: Ninety SLE patients were performed M-mode, 2-dimensional and Doppler echocardiography and aCL IgG and IgM were measured by an enzyme-linked immunosorbent assay (ELISA). According to the abnormalities in the echocardiography, the patients were assigned into valvular abnormality group and non-valvular abnormality group. Chi-square method was used to compare the difference of aCL prevalence between the two groups. RESULTS: The prevalence of echocardiographic abnormalities was 53.33%, and valvular abnormality (38.89%) and pericardial effusion (34.44%) presented most frequently. The aCL prevalence was 32.56% in the 43 SLE patients. The prevalence of aCL in the valvular abnormality group was significantly higher than that in non-valvular abnormality group (52.94% vs 19.23%, P<0.05). CONCLUSION The incidence of echocardiographic abnormalities is high in SLE patients, most often in valves and pericardium. The aCL is probably related to valvular damage in SLE patients.
Adolescent ; Adult ; Antibodies, Anticardiolipin ; blood ; Echocardiography, Doppler ; Female ; Heart Valve Diseases ; etiology ; immunology ; physiopathology ; Humans ; Lupus Erythematosus, Systemic ; complications ; immunology ; physiopathology ; Male