AIMTo investigate the possibility of polymethacrylate nanoparticles (NP) for antisense oligodeoxynucleotides delivery system.

METHODSThe nanoparticles were prepared by evaporating ethenol solution containing Eudragit RL100 or RS100, and then mixtured with oligonucleotides. The morphology and size were investigated by a transmission electron microscope and Mastersizer particle characterization systems, and the cytotoxicity was evaluated by Trypan Blue staining and hemolysis test. The flow cytometer was used to determine the uptake of fluorescence-labelled oligodeoxynucleotides.

RESULTSThe morphology of nanoparticles showed spherical and orderly, the average diameter was about 127 nm, and almost the antisense oligodeoxynucleotides (ODN) were loaded when NP: ODN was 6.6. The uptake of ODN was significantly increased when loaded by nanoparticles, which well depended on the nanoparticles concentration. Meanwhile, slightly cytotoxicity was observed when high dose of nanoparticles was used.

CONCLUSIONThe polymethacrylate nanoparticles appeared to be a promising vehicle for gene delivery.

Acrylic Resins ; chemistry ; toxicity ; Animals ; Drug Carriers ; Drug Delivery Systems ; Hemolysis ; drug effects ; Nanotechnology ; Oligonucleotides, Antisense ; administration & dosage ; Particle Size ; Technology, Pharmaceutical ; methods

AIMTo survey the uptake behavior and subcellular distribution of antisense oligodeoxynucleotide polymethacrylate submicroparticles (AS-ODN-SMP) and infer its mechanism in MGC cell lines.

METHODSMGC cells were incubated at certain concentration of AS-ODN-SMP or AS-ODN for 8 h at 4 degrees C or 37 degrees C. Then the fluorescence oligodeoxynucleotide- labeled cells were counted by flow cytometer and the intracellular fluorescence intensity was determined after incubated with chloroquine for 2 h.

RESULTSCellular uptake of oligodeoxynucleotides was significantly increased following application of AS-ODN-SMP and total intracellular fluorescence intensity was enhanced by 683 folds with the vehicle concentration of 20 microg x mL(-1). AS-ODN-SMP entranced to cells profoundly with temperature-dependent manner. Rare cells took on fluorescence when incubated at 4 degrees C, while 37 degrees C they were significantly increased. But the intracellular fluorescence intensity appeared same level in present or absent of chloroquine.

CONCLUSIONWith the help of polyacrylate submicroparticles, oligonucleotides efficiently entranced the cells via endocytosis and could successfully escape the degradation in lysosome.

Animals ; Cell Line ; Drug Carriers ; Drug Delivery Systems ; Endocytosis ; drug effects ; Giant Cells ; cytology ; Lysosomes ; metabolism ; Nanoparticles ; Oligodeoxyribonucleotides, Antisense ; administration & dosage ; pharmacokinetics ; Particle Size ; Polymethacrylic Acids ; chemistry ; pharmacology ; Temperature

Panax ginseng is the king of herbs and plays important roles in the traditional Chinese medicine industry. In this paper, we summarized the development of ginseng cultivation in China and other main countries, analyzed the effects of ecological factors of soil and climate on ginseng distribution, and investigated the characteristic of main cultivation patterns (conversion of forest to cultivate ginseng soils, cultivated ginseng in the farmland and wild nursery). Aimed at the serious issues in the cultivation, research strategies have been provided to guarantee the sustainable development of the ginseng industry. The patterns of cultivated ginseng in the farmland should be strive to develop; pollution-free cultivation and studies of continuous cropping obstacles should be carried out; ginseng varieties suited to ecological environment of farmland should be bred using modern biotechnology.
Agriculture ; methods ; China ; Climate ; Ecosystem ; Panax ; chemistry ; growth & development ; Soil ; chemistry

Spinal biomechanics, especially the range of spine motion,has close connection with spinal surgery. The change of the range of motion (ROM) is an important indicator of diseases and injuries of spine, and the essential evaluating standards of effect of surgeries and therapies to spine. The analysis of ROM can be dated to the time of the invention of X-ray and even that before it. With the development of science and technology as well as the optimization of various types of calculation methods, diverse measuring methods have emerged, from imaging methods to non-imaging methods, from two-dimensional to three-dimensional, from measuring directly on the X-ray films to calculating automatically by computer. Analysis of ROM has made great progress, but there are some older methods cannot meet the needs of the times and disappear, some classical methods such as X-ray still have vitality. Combining different methods, three dimensions and more vivo spine research are the trend of analysis of ROM. And more and more researchers began to focus on vivo spine research. In this paper, the advantages and disadvantages of the methods utilized recently are presented through viewing recent literatures, providing reference and help for the movement analysis of spine.
Animals ; Humans ; Imaging, Three-Dimensional ; instrumentation ; methods ; trends ; Radiography ; Spine ; diagnostic imaging

Animals ; Cell Culture Techniques ; methods ; Cell Separation ; methods ; Culture Media ; Epithelial Cells ; cytology ; Respiratory System ; cytology ; Swine

CD38 is a multifunctional enzyme expressed in a variety of mammalian tissues, its catalytic activity was involved in a wide range of physiological processes. Based on the reported inhibitor of human CD38 NADase, 33 purine derivatives were designed and synthesized. The biological activity assay showed that compounds 20 and 38 exhibited almost the same extent of inhibitory activities on human CD38 NADase as the lead compound H2. The results also revealed that small substituents at C-6 of purine ring gave no obvious effect on inhibitory activity, but phenylpropionyl moiety at N-2 could affect the binding mode of the compound with CD38. This study provides a reliable basis for future rational design of inhibitors for CD38.
ADP-ribosyl Cyclase 1 ; antagonists & inhibitors ; Enzyme Inhibitors ; chemical synthesis ; chemistry ; Humans ; Purines ; chemical synthesis ; chemistry

The starting material L-tryptophan reacted with 4-chlorobenzaldehyde via Pictet-Spengler condensation and followed by oxidation and decarboxylation to afford the 1-(4-chlorophenyl)-beta-carboline. The intermediate was further reacted with alkyl halogenide by N(9)-alkylation and N2-quaternarization to obtain 12 novel 1-(4-chlorophenyl)-beta-carboline derivatives. The chemical structures of all target compounds were characterized by elemental analyses, MS and 1H NMR spectra. The antitumor activities of the target compounds were evaluated by MTT method. The results demonstrated that N2-quaternarized compounds enhanced the antitumor activity significantly. In particular, compound 15 was found to be the most potent compound with IC50 values lower than 5 micromol x L(-1) against 6 human tumor cells. These results confirmed that the N2-alkyl or aralkyl substituent on the beta-carboline ring played an important role in the modulation of the antitumor activities.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Carbolines ; chemical synthesis ; chemistry ; pharmacology ; Cell Line, Tumor ; Humans ; Inhibitory Concentration 50 ; Molecular Structure ; Structure-Activity Relationship

ObjectiveTounderstandthetrendsandepidemiologicalcharacteristicsofsexuallytransmitteddiseases(STDs)inChinaandprovidescientificbasisformakingcontrolstrategies.MethodsDuringtheperiodof1991～2001,thecase-reportingdataof8kindsofnotifiableandmonitoringSTDs,collectedfrom31provinces,autonomousregionsandmunicipalities,wereanalyzedwithepidemiologicalmethods.Results①Epidemictrends:Duringthisperiod,theincidenceof8kindsofSTDssteadilyincreasedfrom175528(15.48per100000population)in1991to859040(68.91per100000population)in2000.Theaverageannualgrowthofincidencewas19.30%,witharangeof2.59%～36.88%.However,thereportedcasesin2001were795612withadecreaseof7.38%comparedwiththosein2000,anditwasthefirstdecreasesinceSTDcaseswerereportedfrom1987.②Geographicaldistribution:Thehigh-incidenceareasweretheZhujiangRiverDelta,YangtzeRiverDelta,MinjiangRiverValley,NortheasternChina,andBeijing,Tianjin,andChongqingManicipalities,withtheincidencerateofover70～100casesper100000populationafter1997,andtherewereveryhighratesofincidenceover1000casesper100000populationinsomeareas.Thelow-incidenceareaswerenorthChina,partsofCentralChina,NorthwesternChinaandSouthwesternChina,withtheincidenceratesoflowerthan30～50per100000population.③Populationdistri-bution:Themaletofemaleratiodecreasedfrom1.60∶1～1.69∶1intheearly1990sto1.35∶1～1.40∶1inthelate1990s.STDincidencerateswerehighestinthe20～39agegroup,andthereportedSTDcasesofthisagegroupaccountedforover80%oftotalcases.ConclusionSexuallytransmitteddiseasesinChinahavebecomeaseriouspublichealthproblemandtheeffectiveinterventionprogrammesagainstSTDsmustbeimplementedacrossthecountry.

Objective To find out the cognition and participation of people in the disease areas of Shandong Province on prevention and treatment of iodine deficiency disorders (IDD), and to evaluate the effectiveness of a health education project on prevention and control of IDD. Methods From 2011 to 2015, a prospective research was used in study, 46 iodine-deficient counties (cities, districts) were selected as project counties in Shandong Province each year, and 3 townships (towns) were chosen in each project county. Health educational activities on IDD prevention and control knowledge were carried out in the central primary school, 3 villages were chosen in each selected township (town) where the health educational activities in the community were carried out. Before and after the healthy education activities, questionnaire surveys on IDD prevention and control knowledge were conducted among 30 students of grade 5 in the central primary school and 15 housewives lived near the schools in each selected township ( town ) . Results After the health education activities , the knowledge awareness rates of students and housewives on IDD prevention and control were 96.06％ ( 61232/63471 ) and 95.44％(32576/34131), respectively, which increased significantly compared with those before the intervention [ 79 . 00％ ( 50038/63342 ) and 81 . 25％( 27281/33576 ) ] , and the differences were statistically significant (χ2 = 8435.19, 3326.19, P < 0.05). Among the primary school students and housewives, the knowledge awareness rates of IDD prevention were increased by 17.06％ and 14.19％, respectively. Conclusion After implementing the intervention measures of IDD health education, the awareness rate of IDD prevention and control knowledge in iodine deficiency areas in Shandong Province is significantly increased, which has achieved the effectiveness of IDD health education behavioral intervention.

OBJECTIVETo analyze the pharmacokinetics of intraperitoneal chemotherapy with mitomycin C (MMC) bound to activated carbon particles.

METHODSA nude mouse model with transplanted human gastric cancer was established. The mice were given MMC by i.v. or intraperitoneal (i.p.) injections, or given i.p. MMC bound to activated carbon particles (MMC-CH). Pharmacokinetic assays were carried out at different time points (0.5, 1, 2, 3, 6, 12 and 24 h) in 7 mice per each time point, to compare the MMC concentrations revealed by the above mentioned methods.

RESULTSThe MMC concentration in peritoneal exudate, omentum and lymph nodes of MMC-CH group was significantly higher than that of MMC solution i.p. group and MMC i.v. group (P < 0.001). On the other hand, the MMC level in serum was significantly lower than that in two control groups (P < 0.001). High MMC level was maintained longer than 24 hours in the MMC-CH group. Intraperitoneal chemotherapy with MMC solution resulted in a low MMC concentration in serum, peritoneal exudates and lymph nodes, and only a transient high level of MMC in the omentum. After i.v. administration, a significantly higher level of MMC concentration occurred in the serum, but only a shortly increased concentration of MMC in the omentum, and lower concentration in peritoneal exudate and lymph nodes as compared with those in the other two groups (P < 0.001).

CONCLUSIONHigh concentration of MMC in peritoneal exudate, omentum and lymph nodes maintained longer than 24 hours and a significantly lower MMC serum concentration can be achieved by administration of intraperitoneal administration of MMC bound to activated carbon particles.

Animals ; Antibiotics, Antineoplastic ; administration & dosage ; pharmacokinetics ; Charcoal ; administration & dosage ; pharmacokinetics ; Female ; Humans ; Injections, Intraperitoneal ; Male ; Mice ; Mice, Inbred BALB C ; Mice, Nude ; Mitomycin ; administration & dosage ; pharmacokinetics ; Neoplasm Transplantation ; Stomach Neoplasms ; drug therapy ; metabolism ; pathology