The effect of Fusarin C, a new mutagen extracted from Fusarium moniliforme,on murine peritoneal M? activation by measuring M?-mediated MTC ADCC and CS,Fusarin C could inhibit M? activation by both MAF and FDP. The inhibitory effect was dose-and time-dependent and the curves of dose-and time-response were similar in all three assays. There is, however, apparent difference in Fusarin C dose and time needed to induce significant in hibition among these assays. Significant inhibition occured at 0.4?g/ml and 0.5?g/ml for MTC and CS respectively, but 1.6?g/ml for ADCC. Similarly, the minimal period of time necessary to bring about significant inhibition was 2 hr for MTC, but 3 hr for ADCC. Finally, significance of the inhibitory effect of Fusarin C on M? anti-tumor activity in relation to carcinogenesis was discussed.

The inhibitory effect of Fusarin C,a new mutagen isolated from Fusarium moniliforme,on M? activation was investigated.The inhibitory effect of Fusarin C disappeared partially after 24 hr culture in the absence of the mycotoxin and completely after 72 hr.In addition,it could be overcome by high concentrations of M? activating factor or anti-serum to the target cells.

Objective To investigate the aberrant methylation and expression of growth arrest and DNA-damage-in-ducible 45 gamma (GADD45G) gene in gastric cardia adenocarcinoma (GCA). Methods Bisulfite conversion-methylation specific polymerase chain reaction method (BS-MSP) and immunohistochemistry method were used respectively to detect the methylation status and protein expression of GADD45G in 138 GCA tumor tissues and corresponding normal tissues. Re-sults The methylation status of GADD45G distal promoter (region 1) was not detected in GCA tumor tissues and corre-sponding normal tissues. For GADD45G region 2 and region 3, the BS-MSP results of region 3 were identical to that of re-gion 2. The methylation frequency of proximal promoter and exon 1 in GADD45G island 2 (region 2 and region 3) in GCA tu-mor tissues (49.3%, 68/138) was significantly increased compared to that in corresponding normal tissues (0, P＜0.01). The methylation status of this two sites in tumor tissues was associated with TNM stage of tumors (P＜0.05). The protein expres-sion of GADD45G in tumor tissues was significantly decreased than that in corresponding normal tissues (P ＜ 0.05),and threre was a significant negative correlation with methylation status of GADD45G proximal promoter and exon 1 (rs=-0.398). Conclusion The decreased expression of GADD45G by hypermethylation of proximal promoter exon 1 of the gene may play an important role in gastric cardia adenocarcinoma.

·AIM:To investigate the effect of β1-integrin overexpression on the adhesion and migration of rabbit corneal epithelial (RCE) cells.·METHODS:Eukaryotic expression vector encoding β1-integrin-GFP fusion DNA was transfected into RCE cells,and the β1-integrin-GFP fusion gene was examined by RT-PCR and Western blot.The adhesion to Matrigel and the migration of the transfected cells were determined by adhesion and mobility assays.The phosphorylation of focal adhesion kinase (FAK) was examined by Western blot.·RESULTS:The overexpression of β1-integrin-GFP fusion gene by RCE cells was successfully established.β1-integrin transfection significantly promoted the adhesion of RCE cells to Matrigel ( P < 0.05 ).β1-integrin overexpression also promoted the migration ability of RCE cells and induced FAK phosphorylation in them (P < 0.05).·CONCLUSION:These data suggest that overexpression of β1-integrin promotes the adhesion and migration of RCE cells and that the FAK pathway may play an important role in this process.

Objective: To investigate the absorption and transepithelial transport characteristics of scutellarin and scutellarein in the human colonic adenocarcinoma cell (Caco-2) monolayer model. The influence factors on these two compounds' absorption were investigated, such as buffer solution, duration of culture, and inhibitors of multidrug resistance-associated protein 2 (MRP(2)), breast cancer drug resistance protein (BCRP) and P-glycoprotein (P-gp). Methods: By using Caco-2 monolayer as an intestinal epithelial cell model, the transport process was studied from apical (AP) side to basolateral (BL) side or from BL to AP. The two compounds were determined by high-performance liquid chromatography coupled with diode-array-detector detection. Transport parameters and apparent permeability coeffients (P(app)) were calculated. Results: The P(app) values of scutellarin and scutellarein were different in two buffer solutions, respectively. In phosphate buffered saline, scutellarin had no absorption from AP to BL, while its P(app) value was 0.74×10(-6) to 1.58×10(-6) cm/s from BL to AP. The P(app) values of scutellarein were 4.33×10(-6) to 6.79×10(-6) cm/s and 1.32×10(-6) to 2.56×10(-6) cm/s from AP to BL and from BL to AP, respectively. The P(app) value gradually decreased with time. The absorption of scutellarein was better than that of scutellarin. The scutellarin absorption was improved by verapamil, MK-571 and reserpine. The scutellarein absorption was improved by verapamil whereas its excretion was improved by MK-571. Conclusion: Absorption of scutellarin is difficult in Caco-2 monolayer cells, which contributes to its low bioavailability. Scutellarein absorption is better than scutellarin absorption. Scutellarein transepithelial transport is passive diffusion. The inhibitor of P-gp can improve scutellarin and scutellarein transportation. The inhibitors of MRP(2) and BCRP can promote transportation of scutellarin. The inhibitor of MRP(2) can promote efflux of scutellarein. The multidrug resistance-associated protein may be the second reason for low bioavailability of scutellarin.

ObjectiveTo evaluate the anticancer activity of 5'-dexoxy-fluorouridine on colon cancer experimental models in BALB/C mice,compared with 5'-fluorouracil,an anticancer agent widely used in clinic,meanwhile,examined the conversion of 5'-Dexoxy-fluorouridine to 5' -fluorouracil in cancer tissues and serum of mouse models.MethodsThe xenografts of mouse colon cancer cell line CT 26 were transplantated to cecum in 60 male BALB/C mice.Three days lated,these mice were divided into 3 groups and intro- peritoneally injected:( 1 ) 5' - dexoxy- fluorouridine 0.1 mg/g,(2) 5' - Fluorouracil 0.02 mg/g,(3)0.9％ sodium chloride 0.4 mL (as a control),respectively.Two and three weeks later,6 mice were sacririced in every group respectively to measure the weight of tumors and bodies,to examine the Hb,RBC,WBC,PLT,AST,ALT,UREA,and CREA in blood.The rest 8 mice in each group were fed generally,and the survival time from operation to natural death was recorded.In addition,14 mice with xenografts of CT 26 about 2 weeks,were divided into 2 groups averagely,5' -dexoxy-fluorouridine 0.1 mg/g and 5' -fluorouracil 0.02 mg/g were intro-peritoneally injected respectively.Fifteen min later,the converted 5' -fluorouracil was detected from the blood and tumor tissues in sacrificed mice.ResultsThe lest tumor average weight was found in the mice injected 5 '-dexoxy-fluorouridine,being (0.07 ± 0.12) g and (0.24g ±0.29) g for the mice sacrificed at 2 and 3 weeks later,respectively.The average survival time for rest mice was ( 32.6 ± 8.9) d.The average tumor weight in 5' - fluorouracil group was (0.74 ± 0.43 ) g and ( 1.13 ±0.75) g at 2 and 3 weeks later,and the average survival time for the rest was (22.8 ±5.9)d,respectively.The average tumor weight in the control group was (0.70 ±0.47) g and ( 1.93 ±0.83) g at 2 and 3 weeks,and the average survival time for the rest was ( 17.5 ± 2.8 ) d.Either the average tumor weight or average survival time in the mice of 5 ' -dexoxy-fluorouridine group was significantly differen from either 5' -fluorouracil group or control (P ＜ 0.05 ).However,there was no significant difference for the numbers of WBC,PLC,Hb,and some function examination of liver and kidney among 3 group mice,besides the loss of weights in 5'-fluorouracil group mice after operation and medicine therapy which was significantly obvious than that in 5' -deoxy-fluorouridine and control groups ( P ＜ 0.05 ).In addition,( 54.71 ± 12.82) μg/g 5' -fluorouracil was detected in xenografts of mice injected 5' -dexoxy-fluorouridine 15 min later,which was the 6.20 folds of 5' -fluorouracil detected in serum from sthe ame group,P ＜0.05.However,( 133.35 ±20.69) μg/m 5'-fluorouracil were detected in serum of mice after 5' -fluorouracil were injected 15 min later,which was the 1.55 folds of 5' -fluorouracil detected in the xenografts from same group ( P ＜ 0.05 ).ConclusionsIn colon cancer tissues of mouse experimental models,5' - dexoxy- fluorouridine could be converted effectively to 5'-fluorouracil,an obvious high concentration being detected in serum of mice than in cancer tissues.The anticancer effect of 5'-dexoxy-fluorouridine on mouse colon cancer models was more effective than 5'-fluorouracil,resulting in a longer survival duration,less side effect and no significant injury on liver and kidney functions.However,the mechanism of 5' -dexoxy-fluorouridine converted to 5' -fluorouracil in cancer tissue is needed further investigation.

Objective To apply electrical impedance tnmography that is a new evaluation ap-proach to monitor the development of retroperitoneal injury. We used retroperitoneal inject blood model in pigs to study the feasibility on monitoring retroperitoneal bleeding and to provide premise in theory and practice for clinical application. Methods Five pigs were used on the experiment. We insert a vessel into the retroperitoneal and inject blood to simulate retroperitoneal bleeding. Sixteen electrodes were atta-ched on the abdominal region circumference of pigs and used for electrical current injection and surface voltage measurement. Then the monitoring images were performed by electrical impedance tomography. Results The images of electrical impedance tomography retroperitoneal inject blood model of five pigs were clear, the minimal impedance scale was decreasing significantly as the bleeding volume increasing and the images were changed significantly too. The computerized tomography and the dissecting results confirmed the blood was limited in retroperitoneal. Conclusions The establishments of pigs retroper-itoneal inject blood model was successful. The images of electrical impedance tomography retroperitoneal inject blood model were clear with significant contrast. It's feasible to use electrical impedance tomography system to monitor the retroperitoneal bleeding. This technique may become a useful tool for monitoring ret-roperitoneal injury in intensive care patients.

Actins ; metabolism ; Calcium-Binding Proteins ; metabolism ; Desmin ; metabolism ; Female ; Humans ; Leiomyoma ; metabolism ; pathology ; Microfilament Proteins ; metabolism ; Middle Aged ; Sex Cord-Gonadal Stromal Tumors ; metabolism ; pathology ; Uterine Neoplasms ; metabolism ; pathology

One unusual human G3P[3] group A rotavirus (RVA) strain M2-102 was identified in stool sample collected from a child with diarrhea in Guangxi Province, China in 2014. It is well known that G3P[3] is a genotype commonly identified in feline and canine RVAs. However, the preliminary phylogenetic analyses of the VP7 and VP4 genes of strain M2-102 indicated that these two genes were closely related to bat RVA strain MYAS33 and simian strain RRV, respectively, whereas both clustered distantly to feline/canine-like RVA strains. In this study, full genome sequencing and molecular analyses were conducted to obtain the true origin of strain M2-102. It was revealed that strain RVA/Human-wt/CHN/M2-102/2014/G3P[3] exhibited a G3-P[3]-I3-R3-C3-M3-A9-N3-T3-E3-H6 genotype constellation for VP7-VP4-VP6-VP1-VP2-VP3-NSP1-NSP2-NSP3-NSP4-NSP5 genes. Phylogenetic analyses revealed that 5 genes (VP7, VP1, VP2, NSP2 and NSP3) from strain M2-102 were closely related to those of bat strain MYAS33 from Yunnan Province which was thought a true bat RVA strain rather than a virus transmitted between species, while another 5 genes (VP4, VP3, NSP1, NSP4 and NSP5) clustered closely with those of simian strain RRV, yet the VP6 gene was closely related to that of human G3P[9] strain AU-1 and AU-1-like RVAs. The epidemiological data indicated that the child infected with M2-102 came from a countryside village, located in Dong Autonomous County of Sanjiang (subtropical hilly wooded area), Liuzhou city in Guangxi Province which might provide natural environment for reassortment events occurring among animal and human RVAs. Therefore, the data suggest that human strain M2-102 might originate from multiple reassortment events among bat, simian and human AU-1-like RVAs, yet it is not clear whether the genomic backbone based on bat MYAS33 (5 genes) and simian RRV (5 genes) like rotaviruses had been obtained through reassortment before being transmitted to the human. This is the first report on whole genome analysis of human G3P[3] RVA from China.
Child, Preschool ; China ; Genome, Viral ; Genomics ; Humans ; Male ; Molecular Sequence Data ; Phylogeny ; Reassortant Viruses ; classification ; genetics ; isolation & purification ; Rotavirus ; classification ; genetics ; isolation & purification ; Rotavirus Infections ; virology ; Viral Proteins ; genetics

Designing of natural product-like compounds using natural products as template structures is an important strategy for the discovery of new drugs. Gambogic acid (GA), which is a Garcinia natural product with a unique caged xanthone scaffold, inhibits potent antitumor activity both in vitro and in vivo. This review summarized the researches on the identification of the antitumor pharmacophore of GA, and the design, structural optimization and structure-activity relationship (SAR) of natural product-like caged xanthones based on it.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Biological Products ; chemical synthesis ; chemistry ; isolation & purification ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Drug Screening Assays, Antitumor ; Garcinia ; chemistry ; Humans ; Molecular Structure ; Structure-Activity Relationship ; Xanthones ; chemical synthesis ; chemistry ; isolation & purification ; pharmacology