Inhibitory Effect of Sophora alopecuroides Total Alkaloids and Two Monomer Alkaloids on PC12 Cell Activity / 中国实验方剂学杂志

ObjectiveTo compare the effects of total alkaloids， matrine， and sophoridine extracted from Sophora alopecuroides on the activity of pheochromocytoma cells （PC12 cells）. MethodThe effect of S. alopecuroides total alkaloids， matrine， and sophoridine at concentrations of 2， 1， 0.5， 0.25， 0.125， and 0.062 5 g·L-1 on the proliferation of PC12 cells was evaluated using the 3-（4，5-dimethylthiazol-2-yl）-2，5-diphenyl tetrazolium bromide （MTT） assay. The lactate dehydrogenase （LDH） leakage rate was measured by enzyme-linked immunosorbent assay （ELISA）. Flow cytometry was used to assess cell apoptosis rate， cell cycle distribution， and intracellular Ca2+ levels. Real-time quantitative polymerase chain reaction （Real-time PCR） was performed to determine the mRNA transcription levels of B-cell lymphoma-2 （Bcl-2） and Bcl-2-associated X protein （Bax）. Protein expression levels of apoptosis-related proteins Caspase-3， Caspase-8， Bcl-2， and Bax were detected by Western blot. ResultCompared to the control group， S. alopecuroides total alkaloids， matrine， and sophoridine inhibited the proliferation of PC12 cells， increased LDH leakage rate， enhanced intracellular Ca2+ fluorescence intensity， and induced cell apoptosis in concentration-dependent manner （P<0.05， P<0.01）. Among them， S. alopecuroides total alkaloids had the strongest inhibitory effect on cell proliferation and induction of apoptosis in PC12 cells （P<0.01）. After treatment with S. alopecuroides total alkaloids， matrine， and sophoridine， the cell cycle progression of PC12 cells was arrested at G1/G0 in the S. alopecuroides total alkaloids group， and at G1/S in the matrine and sophoridine groups. The expression levels of Bax mRNA were significantly increased （P<0.05， P<0.01）， while the expression levels of Bcl-2 mRNA were significantly decreased （P<0.05， P<0.01）. All treatments significantly downregulated the expression of the anti-apoptotic protein Bcl-2 （P<0.05， P<0.01） and upregulated the expression of the pro-apoptotic proteins Bax， Caspase-3， and Caspase-8 （P<0.05， P<0.01）， with the most significant protein expression changes observed in the S. alopecuroides total alkaloids group. ConclusionAmong the S. alopecuroides total alkaloids， matrine， and sophoridine， S. alopecuroides total alkaloids exhibit the strongest inhibitory effect on the activity of PC12 cells， and its mechanism of action may be related to the inhibition of anti-apoptotic protein expression， upregulation of pro-apoptotic protein expression， and activation of the mitochondrial Caspase-8 apoptotic pathway.

In vitro study of the effects of honeysuckle on Streptococcus mutans UA159 / 口腔疾病防治

Objective@# To investigate the inhibitory effect of honeysuckle on Streptococcus mutans UA159 in vitro.@*Methods@# We used a double-dilution method to measure the minimum inhibitory concentration (MIC) of honeysuckle against Streptococcus mutans UA159. Lonicerae lonicerae powder was dissolved in the solvent DMSO, different concentrations of liquid medicine were prepared, and bacterial liquid was added. The solution control group and bacterial liquid control group were set at the same time. The growth and acid production of UA159 were determined using antibacterial experiments. A growth curve and acid production curves were drawn, and the adhesion rate and adhesion inhibition rate were calculated. The effect of honeysuckle on the formation of Streptococcus mutans UA159 was determined by crystal violet quantification, and a microscope and a scanning electron microscope were used to observe biofilm formation and structural changes.@* Results @# The MIC of honeysuckle against Streptococcus mutans UA159 was 12.5 mg/mL. The bacteriostatic experiments showed a difference in the growth, acid production and adhesion of UA159 after honeysuckle treatment (P<0.05) compared with the controls, and the inhibitory effect increased as the drug liquid concentration increased. Crystal violet quantification showed a significant difference in biofilm formation between the pharmaceutical liquid group and the control group (P<0.05). Meanwhile, the forward microscope showed a significant decrease in biofilm formation. Under SEM, the number of bacteria decreased significantly at 0, 6 and 12 h after honeysuckle addition. @*Conclusion @# Honeysuckle inhibits the growth and acid production of UA159 and inhibits adhesion and the formation of biofilms.

Inhibitory effect of baicalin on Streptococcus mutans UA159 in vitro / 口腔疾病防治

Objective @# To investigate the inhibitory effect of baicalin on Streptococcus mutans UA159 in vitro.@*Methods @#The minimum inhibitory concentration (MIC) of baicalin on Streptococcus mutans UA159 was determined by the liquid multiple dilution method combined with the OD600 value measured by microplate. The OD600 value of Streptococcus mutans UA159 in different concentrations of baicalin was measured by an enzyme mapping instrument. A growth curve was drawn, and the adhesion rate and adhesion inhibition rate were calculated. The effect of baicalin on the formation of Streptococcus mutans UA159 biofilms was observed by the crystal violet quantitative method and scanning electron microscopy. The effect of baicalin on the total number of Streptococcus mutans UA159 bacteria was observed by scanning electron microscopy.@*Results@#The MIC of baicalin on Streptococcus mutans UA159 was 12 mg/mL. With increasing baicalin concentration, the growth rate of Streptococcus mutans UA159 was slowed, the adhesion rate of Streptococcus mutans UA159 decreased and the adhesion inhibition rate increased（P < 0.05）. The results of crystal violet quantitative method showed that compared with the bacterial control group, the biofilm formation of Streptococcus mutans UA159 was significantly reduced after adding baicalin at 0 h, 6 h and 12 h (P < 0.001). Under a scanning electron microscope, the total number of bacteria decreased significantly after adding baicalin at 0 h, 6 h and 12 h.@*Conclusion@# baicalin ; natural medicine ; Streptococcus mutans UA159 ; caries ; minimum inhibitory concentration ; growth curve ; adhesion rate ; adhesion inhibition rate ; biofilm formation ; in vitro study

Correlation study between cytochrome P4502C19 gene polymorphism or metabolic type and ADP induced-platelet aggregation inhibition and clopidogrel resistance / 中国临床药理学与治疗学

AIM: To investigate the effect of the polymorphism and metabolic type of cytochrome P450 (CYP) 2C19 gene on the inhibitory rate of platelet aggregation induced by ADP and relationship with resistance of clopidogrel. METHODS: A total of 163 patients that are administrated with aspirin and clopidogrel were collected from the Yijishan Hospital of Wannan Medical College from June 2016 to July 2017. The CYP2C19*2, *3 and *17 genotypes of patients were detected with fluorescence staining in situ hybridization, according to the genotype, CYP2C19 enzyme activity was divided into fast metabolic (RM), intermediate metabolic (IM), slow metabolic (PM) and ultrafast metabolic type (UM). After 5 days of drug delivery, the platelet aggregation inhibition rate (IPAADP) induced by ADP was detected by thrombus elasto graph. IPAADP differences between CYP2C19*2, *3 and *17 genotype and CYP2C19 enzyme metabolic type were evaluated. CYP2C19 genotype and metabolic type as well as their distribution in clopidogrel resistance group (CR) and non clopidogrel resistance group (NCR) were observed. RESULTS: The mutation rates of CYP2C19*2, *3 and *17 were 30.98%, 6.75% and 1.23%, respectively. The average IPAADP was (67.03±26.79)% and the incidence of CR was 26.99%, and the IPAADP was (31.29±12.60)%. The IPAADP of CYP2C19*2 and *3 gene carriers were decreased significantly (P0.05). There was no statistical difference in the distribution of CYP2C19 genotypes and metabolic types in NCR and CR (P>0.05). CONCLUSION: CYP2C19 genotypes have significant effect on IPAADP, but there is no association with the occurrence of CR, and the related study needs to be further verified.

Study on the Correlation between CYP2C19 Gene Polymorphisms and Antiplatelet Reactivity of Clopidogrel in Xinjiang Uygur Patients with Acute Coronary Syndrome / 中国药房

OBJECTIVE：To investigate the correlation between CYP2C19 gene polymorphisms and antiplatelet reactivity of clopidogrel in Xinjiang Uygur patients with acute coronary syndrome （ACS）. METHODS ：Totally 90 Uygur patients with ACS who were admitted to the cardiovascular department of Xinjiang Kashi Second People ’s Hospital from Jan. 2018 to Jan. 2019 were selected as the study subjects. They were given anti-platelet therapy of asprin+clopidogrel ，and received the treatment continuously for one year after discharge. The platelet aggregation inhibition （DPAI）rate of the patients were determined ，and the response to clopidogrel was evaluated. PCR-fluorescence probe method was used to detect genotype of CYP2C19*2 and * 3，and PCR-direct sequencing method was used to detect genotype of * 17. Multivariate Logistic regression analysis was adopted to investigate the correlation of gene and non-gene factors with DPAI of patients. RESULTS ：Among 90 patients，there were 10 patients with clopidogrel resistance （CR）and 80 patients with non-CR. There were 58，28 and 4 patients with CYP2C19*2 G/G，G/A，A/A genotype，respectively；there were 88 and 2 patients with CYP2C19*3 G/G，G/A genotype ，respectively；there were 64 and 26 patients with CYP2C19*17 C/C，C/T genotype ，respectively；the genotype frequency of each genotype was consistent with Hardy-Weinberg equilibrium （P＞0.05）. After treatment ，DAPIs of patients with CYP2C19*2 G/A，A/A genotype were decreased significantly，while those of the patients with A/A genotype were significantly lower than patients with G/A genotype patients （P＜ 0.05）. DAPIs of patients with CYP2C19*17 C/T genotype were increased significantly ，compared with C/C genotype 2016D01C087） patients （P＜0.05）. There was no statistical significance in @fudan.edu.cn DAPIs between CYP2C19*3 G/A and A/A genotype patients （P＞0.05）. Multivariate Logistic regression analysis showed 85775264@qq.com that CYP2C19 gene pol ymorphism was independently related to DPAI in Xinjiang Uygur patients with ACS [OR ＝2.314，95％CI（1.569，3.144），P＝0.009]，while age ，gender，smoking and other non-gene factors were not related to DPAI （P＞0.05）. CONCLUSIONS ：CYP2C19 gene polymorphism is associated with antiplatelet reactivity of clopidogrel in Xinjiang Uygur patients with ACS. * 2 wild type patients may have higher DPAI ，while * 17 wild type patients may have lower DPAI.

Screening combination ratio and exploring mechanism of Momordicae Semen and Epimedii Folium / 中国中药杂志

The aim of this paper was to obtain low toxicity and high efficiency anti-tumor Chinese medicine through screening the combination ratios of Momordicae Semen and Epimedii Folium, and to explore the anti-tumor mechanism of the combination of two drugs by observing their effect on apoptosis-related proteins in cancer cells. Methyl thiazolyl tetrazolium(MTT) assay was used to observe the effect of drug combination on the proliferation of tumor cells from different tissue sources. The effects of the combination of the two drugs on tumor cells were analyzed by Compusyn software. Plate cloning assay was used to observe the effect of combination of these two drugs on the proliferation of A549 cells in vitro. The expression of reactive oxygen species(ROS) and apoptotic proteins p53, Bcl-2 and Bax were compared by using ROS kit and Western blot. Lewis lung cancer model was used to observe the anti-tumor effect of drugs in vivo. The results showed that the anti-tumor effect of their ethanol extract was more significant than that of water extract, and the anti-proliferation effect was strongest when the ratio was 1∶1(P<0.05). Compusyn analysis showed that the combination of the two drugs had synergistic effect. Further studies showed that after combined use, the number of clonogen formation in A549 cells was significantly reduced(P<0.01); ROS production was increased; the expression of apoptosis-related protein p53 was up-regulated, and the ratio of Bcl-2/Bax was decreased. In vivo animal study showed that the tumor inhibition rate was 53.06%(P<0.05) in the high dose group. As compared with the single use of the two drugs, the combination of the two drugs had more significant anti-proliferative effect on tumors, and the optimum ratio was 1∶1. The combination of the two drugs at a ratio of 1∶1 inhibited the proliferation of various tumor cells, and had no significant effect on normal liver cells LO2 when compared with other ratios. Therefore, it can be preliminarily inferred that the combination of the two drugs may have the effect of synergism and detoxification. Further studies showed that the combination of the two drugs can significantly inhibit the proliferation of A549 cells, and its mechanism may be related to the activation of endogenous apoptotic pathway. In vivo experiments also showed that the tumor inhibition rate increased with the increase of drug concentration.

Comparative study on the suitability of chemical fingerprint and anti-platelet aggregation/anti-inflammatory biopotency in the overall quality evaluation of Xiaojin pills / 药学学报

Xiaojin pills, the first choice for clinical treatment of breast hyperplasia, were selected to explore the suitability of a bioactivity assay with chemical fingerprinting for the development of an overall quality evaluation assay. The liposoluble and water-soluble fraction fingerprints of Xiaojin pills were established. The ability to inhibit platelet aggregation and the rate of inhibition of cyclooxygenase-2 (COX-2) for 16 batches of Xiaojin pills from several manufacturers was analyzed; the chemical fingerprints of these samples were correlated with the bioactivity and chemical analysis. The animal protocol was approved by the Committee on the Ethics of Animal Experiments of Affiliated Hospital of Chengdu University of Traditional Chinese Medicine Approval, ID: 2018BL-002. Results showed that the antiplatelet aggregation activity of 16 batches was 0.712-1.278 U∙mg-1, with a relative standard deviation (RSD) of 15.4%. COX-2 inhibition was 52.07%-68.95% and the RSD was 8.91%. The results showed that there was little difference in the biological effects of these samples. However, the chemical fingerprint consistency of these 16 batches of Xiaojin pills was poor, and the similarity of nearly half of the samples was less than 0.9. The total peak area of Xiaojin pills was 32.74%-165.37% across samples, showing very poor chemical consistency. In order to explore the reasons for the poor chemical consistency despite good consistency in the biological assays, the fingerprint chromatogram was analyzed by multivariate statistical analysis. The main chromatographic peaks were identified. The results showed that the similarity of Xiaojin pills was mainly determined by the prominent chromatographic peaks 17, 18, 20, 23 and 27 in the liposoluble fingerprints, which were identified from Liquidambaris resina and Angelica sinensis Radix. However, Liquidambaris resina and Angelicae sinensis Radix had almost no anti-platelet aggregation activity or COX-2 inhibitory effect at the normal prescription ratio. As a result, the ability to utilize chemical fingerprints to evaluate the quality consistency of Xiaojin pills is limited. The selection of biological evaluation methods that reflect clinical efficacy could make up for the shortcomings of chemical evaluation methods for quality assessment, and provide new ideas and methods for the overall quality evaluation of complex Chinese patent medicines.

Correlations of CYP2C19 gene polymorphism with platelet inhibitionrate and clopidogrel low responsiveness / 实用医学杂志

Objeetive To investigate the relationships of CYP2C19 genotype polymorphism with platelet inhibition rate and clopidogrel low responsiveness in patients taking percutaneous coronary intervention (PCI) during perioperative administration of clopidogrel.Methods 404 patients taking clopidogrel after PCI were included from February 2016 to February 2017.They were divided into three groups:fast metaboliszer,moderate metaboliszer and slow metabolizer,according to the CYP2C19 genotype.Platelet inhibition rate induced by adenosine diphosphate (ADP) was detected by thrombelastogram,platelet inhibition rate ＜ 30％ was defined as clopidogrel low responsiveness (CLR) group and the relationships between the three groups were analyzed in view of CYP2C19 genotype and the platelet inhibition rate and the clopidogrel low responsiveness.Results (1) The proportions of the three groups was 45.5％,45.3％ and 9.2％ in the 404 patients,no statistically significant difference among the three groups in general data (age,sex,platelet,hypertension,diabetes mellitus,hyperlipidemia) (P ＞ 0.05).(2) There was no statistically significant difference in the platelet inhibition rate between the three groups (P =0.312).(3) There was no significant difference in the clopidogrel low responsiveness between the three groups (P =0.295),with the fast metabolizer group vs.intermediate metabolizer (P =0.522),the fast metabolizer group vs.the slow metabolizer (P =0.117) and the intermediate metabolizer group vs.slow metabolizer (P =0.255).Conclusion There is no correlation of CYP2C19 genotype with platelet inhibition rate and clopidogrel low responsiveness in patients taking clopidogrel after PCI.Only the detection of CYP2C19 genotype may not accurately predict the antiplatelet aggregative activity of clopidogrel.

Preparation and Antitumor Activity of Etoposide-loaded Solid Lipid Nanoparticles / 中国药师

Objective:To prepare solid lipid nanoparticles of etoposide and evaluate the inhibitory rate against Lewis lung cancer cells in mice. Methods:Etoposide-loaded solid lipid nanoparticles were prepared by a hot melting emulsification and high pressure homogenization method. The physicochemical properties such as the appearance, microstructure, particle size distribution and zeta potential of the solid lipid nanoparticles were studied. The in vitro release behavior of the solid lipid nanoparticles were evaluated. The inhibitory effect of etoposide-loaded solid lipid nanoparticles and etoposide injection on Lewis lung cancer cells was compared. Results:Etoposide-loaded solid lipid nanoparticles showed a light blue transparent liquid,which was uniformly spherical under the transmission electron microscope. The average particle size was (153.2 ± 32.8) nm, PdI was (0.185 ± 0.031),and the zeta potential was(-17.4 ± 1.1) mV. The solid lipid nanoparticles could delay the drug release and 52.4% of the drug was released in 24 h. Etoposide-loaded solid lipid nanoparticles could significantly inhibit the growth of Lewis lung cancer cells in mice. And the inhibitory rate of the solid lipid nanoparticles was significantly higher than that of etoposide injection (P < 0.05). Conclusion:The solid lipid nanoparticles prepared by hot melting emulsification and high pressure homogenization method have good antitumor effect on Lewis lung cancer cells,which can be used as a new drug delivery system for etoposide with certain application prospect in lung cancer treatment.

Interaction between gomizine D and α-glucosidase / 中国中药杂志

This paper describes a study exploring the interaction between gomizine D and α-glucosidase. The inhibitory activity of α-glucosidase by gomizine D was determined using PNPG as substrates Gomizine D gave the IC₅₀ value of 0.59 mmol•L⁻¹, which was higher than that of acarbose (1.95 mmol•L⁻¹). Gomizine D was a reversible and non-competitiveα-glucosidase inhibitor with an inhibition constant Ki=4.026 g•L⁻¹. The binding mode between gomizine D and α-glucosidase was analyzed by AutoDock Vina molecular docking software. The lowest energy of Gomizine D binding to α-glucosidase was -7.7 kcal•mol⁻¹, which was lower than that of acarbose (-6.6 kcal•mol⁻¹). After binding with gomizine D, UV spectroscopy analysis displayed that the microenvironment of aromatic residue in the secondary structure of α-glucosidase was changed, and the polarity of protein was reduced.

The Therapeutic Effect of Quercetin-loaded PLGA-TPGS Nanoparticles on the Hepatocarcinoma Ectopic Solid Tumor-bearing Mice / 中国医科大学学报

Objective To investigate the therapeutic effects of Quercetin (QT)-loaded PLGA-TPGS nanoparticles (QPTN) on solid tumor-bearing mice with HCa-F hepatocarcinoma in vivo.Methods The model of HCa-F hepatocarcinoma solid tumor-bearing mice was established by implanting HCa-F cells into 48 mice.The mice were divided into 6 groups randomly:the negative control,empty PLGA-TPGS nanoparticles,5-Fluorouracil solutions (FS),Quercetin solutions (QTS),QT-loaded PLGA nanoparticles (QPN),and QPTN groups.Each group was treated using tail vein twice a day for 20 days;then,all mice were sacrificed.The increment tumor volumes and tumor growth inhibition rate were counted.Then,tumor specimens were prepared for hematoxylin & eosin (HE) staining and observed under a microscope.Results The results showed that the increment tumor volumes of mice in the QPTN,QPN,and FS groups were significantly smaller than that in the negative control group (P ＜ 0.05 or P ＜ 0.01).The tumor growth inhibition rate of the QPTN group was 59.07％,which was much higher than that of the QTS group (23.94％),the FS group (35.14％),and the QPN group (46.14％).The results of the HE staining on the tumor sections also indicated that the QPTN group showed a better therapeutic outcome compared to the other groups.Conclusion The QPTN has a better therapeutic effect on the model of solid tumor using HCa-F cells-bearing mice than the QPN,QTS,and FS.

Inhibitory effect of SM-1 on human liver microsomal cytochrome P450 enzyme / 中国药理学通报

Aim To investigate the effect of SM-1 on seven main cytochrome P450(CYP450)in human liver microsomes.Methods Substrate or SM-1 was incubated with human liver microsomes for 30 min in vitro,and divided into control group and experimental group.The effects of SM-1 on the main phase I metabolic enzymes in human liver microsomes was detected by HPLC.Phenacetin,bupropion,paclitaxel,tolbutamide,omeprazole,dextromethorphan,testosterone were investigated as probe drugs.Results Inhibition rate of SM-1 on the classical substrate of human liver microsomal CYP was 0.05％,3.37％,0.08％,2.07％,4.20％,-0.15％and 10.84％,respectively.Conclusions SM-1 may have inhibitory effect on CYP3A4.Attention should be paid to the interaction of clinical drug induced by CYP enzyme inhibition.

Effects of Sinomenine on Tumor Suppressor Gene P16 And P53 in Rats with Lung Cancer / 世界科学技术-中医药现代化

This study was aimed to investigate the effect of sinomenine on the expression of tumor suppressor gene P 16 and P53 in rats with lung cancer.A total of 40 male SD rats were treated by left-lung vein injection of WALKER-256 cell suspension to establish transplanted lung cancer model.After 3 weeks,30 rats screened of tumor were randomly divided into the model group,cyclophosphamide (CP) group and the sinomenine treatment group.Another 10 healthy SD rats were set as the normal control group.Sinomenine treatment group was treated with the subcutaneous injection of 10％ sinomenine hydrochloride for 10 weeks.CP was injected in the CP group as positive control.The same amount of normal saline was injected in the normal control group and the model control group.After 10 weeks of treatments,lung tumors of each group were removed to measure the tumor volume and weight.And the tumor inhibition rate was calculated.Then,flow cytometry was used to detect the proportion of WALKER-256 cells in tumor tissues in G1,G2,M and S around four cycles.Immunohistochemistry was adopted to detect positive expression rates of P16 and P53 protein.Reverse transcription polymerase chain reaction (RT-PCR) were used to detect expression of P16mRNA and P53mRNA.The results showed that compared with the model control group,the inhibition rate of sinomenine group was 30.15％;the positive expression rate of P16mRNA and P53mRNA protein were significantly decreased;expressions of P 16mRNA and P53mRNA were lower;tumor volume and tumor weight in S period got down significantly.The rates of cells in G1 and G2 periods got higher (P＜0.05).It was concluded that sinomenine may inhibit the differentiation and proliferation of WALKER-256 transplanted lung cancer cells in rats by regulating the expression of tumor suppressor gene P 16 and P53,regulating the ratio of cells in G1,G2 and S periods.

Effects of Salvianolate on the Expression of VEGF and MMP-9 in Lung Tissue of Mice with Lung Cancer / 中国药房

OBJECTIVE:To study the effects of salvianolate on the expression of vascular endothelial growth factor (VEGF) and matrix metalloproteinase-9(MMP-9)in lung tissue of mice with lung cancer. METHODS:C57BL/6 mice were randomly divid-ed into model group (normal saline),positive control group (cyclophosphamide 50 mg/kg) and salvianolate low-dose,medi-um-dose and high-dose groups(20,40,80 g/kg)with 10 mice in each group. They were ig 1 000 mg/kg urethane,twice a day, for consecutive 4 weeks to establish lung cancer model. After modeling,they were given relevant medicine intragastrically once a day for consecutive 14 d. Mice behaviors,symptoms,body weight,tumor inhibition rate,spleen index,thymus index,and the ex-pressions of VEGF and MMP-9 in lung tissue among groups were compared. RESULTS:The activity of mice in model group disap-peared,dull coat color,preferred crowding together;the above-mentioned phenomenon improved in positive control group and sal-vianolate different dose groups. The body weight of mice in positive control group,salvianolate low-dose group,medium-dose group and high-dose group were(21.01±2.95)g,(20.89±3.14)g,(21.03±3.02)g,(21.24±3.17)g;and the tumor inhibition rates were(41.12±15.42)%,(36.92±10.42)%,(39.41±12.39)% and(37.19±10.39)%;compared with model group,spleen index,thymus index,and the expressions of VEGF (except for positive control group) and MMP-9 in other 4 groups decreased (P<0.05). CONCLUSIONS:Salvianolate shows obvious inhibitory effects on mice with lung cancer,which may be related to in-hibiting expressions of VEGF and MMP-9 in lung tissue.

Effect of temozolomide combined with curcumin on the apoptosis of the C6 glioma cells / 实用医学杂志

Objective To study the temozolomide combined with curcumin on the inhibitory effect and apoptosis of the C6 glioma cells. Methods The C6 glioma cells were treated with temozomide in combination with curcumin. The anti proliferation effect of liposomes on the C6 glioma cells was investigated by using the method of sulforhodamine B (SRB). Flow cytometry was used to detect apoptosis of the C6 glioma cells. Confocal laser scan-ning microscope was used to observe apoptosis and location in the C6 glioma cells. Results The results of SRB as-say showed that temozolomide in combination with curcumin inhibition rate were (91.22 ± 0.51)%in 48 h of the C6 glioma cells; Flow cytometry showed that the apoptosis rate were (33.15 ± 0.79)% with temozolomide (5 μmol/L) in combination with curcumin (10 μmol/L). Laser scanning confocal scanning microscope indicated that the apop-tosis of in the C6 glioma cells treated with temozolomide in combination with curcumin was more than that of free drug. Conclusion The temozolomide in combination of curcumin can inhibit the growth and induce apoptosis of the C6 glioma cells.

Effects of Lactobacillus fermentum on the Inhibition of Cytoxan on Human Colorectal Cancer HCT116 Cells / 中国药房

OBJECTIVE:To study the effects of Lactobacillus fermentum(Lb-f)on inhibition of cytoxan(CTX) on HCT116 cells of human colorectal cancer in vitro and in vivo. METHODS:HCT116 cells were cultured in vitro. MTT assay was used to in-vestigate the effects of 4,2,1μg/ml CTX and combined with 10μg/ml Lb-f on the survival rate of HCT116 cells. HCT116 cell xe-nograft tumor nude mice model was induced to investigate the effects of 100,50,25 mg/kg CTX and combined with 180 mg/kg Lb-f on tumor volume,tumor weight,relative tumor inhibition rate,the sensitization effect of chemotherapy (by q value),the number of peripheral blood leucocyte and platelet. RESULTS:Compared with CTX alone,CTX combined with Lb-f had no signifi-cant effect on survival rate of HCT116,relative inhibition rate of tumor volume in nude mice, relative inhibition rate of tumor weight and q value (P>0.05),but increased the number of peripheral blood leucocyte and platelet (P<0.05). CONCLUSIONS:No synergistic effects of Lb-f is found on the inhibition of CTX on the growth of HCT116 in vitro and in vivo;Lb-f can inhibit the decrease of peripheral blood leucocyte and platelet of HCT116 cell xenograft tumor nude mice induced by CTX.

Preparation and Tumor Inhibition Effect of Transferrin Modified Paclitaxel-loaded Liposome / 中国药房

OBJECTIVE:To prepare transferrin modified paclitaxel-loaded liposome(TF-PTX-LP),and to study the tumor in-hibition effect. METHODS:TF-PTX-LP was prepared by thin-film method,and morphology of TF-PTX-LP was observed. Qualita-tive and quantitative investigation were used to value the uptake efficiency of TF-LP and LP by HepG2 cells. The proliferation inhi-bition rate of HepG2 cells was investigated after treated with PTX,PTX-LP and TF-PTX-LP for 24,48 and 72 h. Tumor spheres were prepared by using HepG2 cells. Effects of normal saline,PTX,PTX-LP and TF-PTX-LP on the volume of tumor spheres were investigated after 0,1,2,4,5,6 and 7 d treatment. HepG2 tumor-bearing nude mice model was induced. Inhibitory effects of normal saline,PTX,PTX-LP and TF-PTX-LP(8.5 mg/kg by PTX)on transplantable tumor of tumor-bearing nude mice were in-vestigated. RESULTS:TF-PTX-LP showed uniform spherical shape,with particle size of 100-120 nm. The fluorescence intensity of HepG2 cells treated with TF-LP was stronger than that treated with LP(P<0.01). Compared with PTX and PTX-LP,TF-PTX-LP showed higher proliferation inhibition rate(P<0.01). Compared with normal saline,PTX and PTX-LP,tumor spheres were small-er in volume after treated with TF-PTX-LP,and inhibition rate of tumor was higher in tumor-bearing nude mice;there were statisti-cal significance after treated for 6,7 d(P<0.01). The proliferation inhibition rate and tumor spheres volume changed in time-de-pendent manner. CONCLUSIONS:TF-PTX-LP which owns good tumor inhibition effect is prepared successfully.

Bleeding risk of short-term intensive statin therapy after coronary artery bypass grafting / 临床外科杂志

Objective To observe the bleeding risk of short-term intensive statin therapy after coronary artery bypass grafting. Methods A total of 240 patients treated with coronary artery bypass grafting were randomly divided into group A(experimental group)and group B(control group). All pa-tients were normalized to conventional treatment and they were given low molecular weight heparin for an-ticoagulant therapy during the perioperative period. Patients in group A were given 40 mg of atorvastatin before surgery,and 40 mg of atorvastatin every night for one month after the surgery. Patients in group B were given 10 mg of atorvastatin every night during the treatment. One month after the operation,platelet aggregation rate and bleeding events of patients were compared. Results There were significant differ-ences in maximum platelet aggregation rate[(14. 5 ± 3. 7)% vs(38. 1 ± 7. 4)% ,P < 0. 05],inhibition rate of platelet aggregation[(79. 5 ± 4. 3)% vs(50. 8 ± 10. 2)% ,P < 0. 05],and incidence of postopera-tive bleeding[27. 5% vs 12. 5% ,P < 0. 05]between group A and B,respectively. Conclusion Short-term intensive statin therapy can increase the bleeding risk after coronary artery bypass grafting.

Synergism and attenuation effects of Scapharca Subcrenata Extraction on NP chemotherapy / 中国比较医学杂志

Objective To investigate the synergism and attenuation effects of Scapharca Subcrenata Extraction on NP chemotherapy in model mice.Methods The models of nude mice were induced with A549 cell line xenograft.The tumor inhibiting rates, body weight, food intake, hematology and blood biochemistry index were determined to evaluate the synergism and attenuation effects of Scapharca Subcrenata Extraction (125、250、500 mg/kg, i.g) on NP chemotherapy. Results Compared with NP chemotherapy group, the tumor inhibiting rates, body weight, food intake, white blood cell number were increased and glutamate pyruvate transaminase, glutamic oxalacetic transaminase and urea nitrogen were decreased markedly in NP chemotherapy plus Scapharca Subcrenata Extraction groups. Conclusion Scapharca Subcrenata Extraction has a remarkable synergism and attenuation effects on NP chemotherapy.

Effect of Clopidogrel on Antiplatelet Therapy in Patients With Coronary Artery Disease Combining Chronic Kidney Disease / 中国循环杂志

Objective: To investigate the effect of clopidogrel on antiplatelet therapy in patients with coronary artery disease (CAD) combining chronic kidney disease (CKD) in order to provide a medication reference in clinical practice. Methods: We retrospectively investigated 423 CAD patients with coronary angiography (CAG) conifrmed diagnosis in our hospital from 2014-01 to 2014-09. According to the value of eGFR, the patients were classiifed into 2 groups:CAD+ CKD- group,n=257 patients with eGFR ≥ 90 ml/(min?1.73 m2), including 182 male and 75 female at the mean age of (60.39 ± 11.09) years, and CAD+CKD+ group,n=166 patients with eGFR < 90 ml/(min?1.73 m2), including 107 male and 59 female at the mean age of (65.80 ± 10.84) years. The patients were treated either by aspirin 0.1 g/d with clopidogrel 75 mg/d for at least 7 days, or by PCI operation with the load of aspirin 0.3g and clopidogrel 300 mg. The thrombelastography was conducted to examine and compare the inhibitory rates of ADP receptor and arachidonic acid (AA) pathway in platelet between 2 groups. Results: The inhibitory rate of platelet ADP receptor in CAD+CKD- group (64.9 ± 27.2) % was higher than that in CAD+CKD+ group (56.6 ± 27.4) %,P=0.039. Based on clinical standard of platelet’s ADP and AA inhibitory rates, in CAD+CKD- group, there were 24/257 (9.4%) of patients only insensitive to clopidogrel, in comparison with 25 (9.7%) of patients only insensitive to aspirin,P=0.99. While in CAD+CKD+ group, there were 21/166 (12.7%) of patients only insensitive to clopidogrel, in comparison with 11 (6.6%) of patients only insensitive to aspirin,P= 0.045. Conclusion: Clopidogrel has decreased effect on anti-platelet therapy in CAD patients combining with CKD, such patients have reduced sensitivity to relevant medication.