Aim To investigate interaction of CJX1,an amlodipine derivative,with ATPase activity of human P-glycoprotein.Methods Plasma membranes were prepared from K562/DOX cells,the P-gp adenosine triphosphatase activity of K562/DOX cell membranes was estimated by measuring inorganic phosphate liberation.Results The basal P-gp ATPase activity was increased by CJX1 with half-maximal activity concentration (Km) of (8.6?1.4) ?mol?L-1,CJX1 might interact with P-gp with a higher affinity and exhibit more potent effect than Verapamil (Ver).Kinetic analysis indicated a non-competitive inhibition of Ver-stimulated P-gp ATPase activity by CJX1 and a competitive inhibition of CJX1-stimulated P-gp ATPase activity by tetrandrine (Tet),moreover,the effect of CsA on CJX1-stimulated and Ver-stimulated P-gp ATPase activity showed a non-competitive and a competitive inhibition respectively.Conclusion CJX1 and Tet can bind P-gp on overlapping sites,while CJX1 and Ver as well as CsA can bind P-gp on separated sites in K562/DOX cells.

AIM To observe protective effects of doxepin on focal cerebral ischemia-reperfusion(I-R)injured rats. METHODS 120 rats were randomly divided into ischemia-reperfusion group,doxepin, nimodipine group and sham-operated group respectively, ischemia-reperfusion model was made by using the suture emboli method, the content of NO and MDA, activities of NOS and SOD in the cerebral tissues and the intracellular [Ca 2+ ] i in the cerebral cortex were determined respectively. RESULTS The content of NO, MDA and [Ca 2+ ] i and the activities of NOS decreased and the activities of SOD increased significantly in the doxepin and nimodipine group compared with ischemia-reperfusion group respectively(P

Aim To investigate the reversal of resistance to doxorubicin by CJZ3,a lomerizine derivative,in doxorubicin-resistant human myelogenous leukemia(K562/DOX)cells.Methods The effect of CJZ3 on P-glycoprotein(P-gp)function and resistance to doxorubicin in K562/DOX cells were observed by using flow cytometry and MTT assay.Results CJZ3 increased intracellular uptake and accumulation of rhodamine123(Rh123)in K562/DOX cells in a concentration-related manner,significantly inhibited the efflux of Rh123 from the cells,and increased the doxorubicin-induced cytotoxicity,apoptosis rate,Caspase-3 activity in doxorubicin-treated cells and the intracellular accumulation of doxorubicin.Conclusions The reversed effect of CJZ3 on resistance to doxorubicin in K562/DOX cells was associated with its inhibitory effect on P-gp function in vitro.

Aim To evaluate the mechanism of HG251-induced apoptosis in K562/DOX cells.Methods Cell viability was assessed by MTT assay;cell cycle distribution,apoptosis and mitochondrial membrane potential were measured by flow cytometry;the protein expressions of P-gp,caspase-3,caspase-8,caspase-9,p53,Bcl-xL and cytochrome c in the K562/DOX cells were evaluated by Western blot.Results HG251 was able to inhibit cells proliferation,induce apoptosis,lose mitochondrial membrane potential,activate caspase-3,caspase-8,caspase-9,up-regulate p53 protein and down-regulate Bcl-xL protein in a dose-dependent manner but it had no effect on P-gp protein expression.Conclusion HG251 could overcome apoptotic resistance via up-regulating p53 protein and down-regulating Bcl-xL protein.In addition,HG251 also induced K562/DOX cells apoptosis via mitochondrial pathway and membrane death receptor pathway.

AIM: To study the protective effects of Imipramine (Imi) on ischemic injury in cultured rat cerebral cortical neurons. METHODS: Cortical neurons of fetal rat were cultured in vitro. The protective effects of Imi on ischemic injury in cultured rat cerebral neurons were observed. RESULTS: Imi ( 10 -5, 10 -6, and 10 -7 mol?L -1) reduced the number of cell death, lowered LDH,NO,and MDA content, and increased of activity of SOD. CONCLUSION: Imi can protect rat cerebral cortical neurons from ischemic injury and toxicity of Glu. And it maybe attribute its to antioxidation and calcium antagonism.

Objective: To examine the retention rate and caries prevention effect of fit-and-fissure sealants after 3 years of children oral disease comprehensive intervention program in Henan province. Methods: For each of the five provincial regions attending the program in 2015, two classes from grade 2 in four primary schools were selected. Children in two schools were assigned into intervention group and the first permanent molars which were appriopriate for sealing were sealed with pit-and-fissure sealants. Children in other two schools were included in the control group and the first permanent molars were only examined for caries conditions. Three years later, retention rate of pit-and-fissure sealants and the dental caries prevalence was compared. Results: Complete retention rate of sealants in the first permanent molars was 65.55% and the whole retention rate was 94.78%. The caries incidence and mean value of the first permanent molars in the intervention group children was 9.71%, (0.12±0.40) respectively whereas those in control group was 21.90%, (0.39±0.78) respectively. The differences between two groups were statistically significant(χ2/t=27.76, 6.91, P<0.01). The relatively effective rate of sealing for caries reduction was 63.43% and the actural effective rate was 6.51% and the pure yield rate of sealing was 12.19%. Higher sealant retention rate was associated caries prevalence(χ2=153.28, P<0.01). Conclusion Childhood oral disease intervention project in Henan Province shows positive effects. Sealing of the first permanent molars effectively prevent dental pit and fissure caries.

Objective: To investigate the epidemiology and associated factors of deciduous dental caries in 3-5 years old children in Henan Province, and to provide a epidemiological reference for prevention work of deciduous dental caries among children. Methods: According to the basic methods of the Fourth National Oral Health Survey, 12 kindergartens were randomly selected from 2 counties and 2 districts in Henan Province and a total of 1 296 children aged 3-5 years old were randomly selected with stratified multi-stage random sampling method. The deciduous teeth of these children were examined for caries and their guardians were surveyed with questionnaires regarding oral health behavior, knowledge and attitude. Results: Deciduous dental caries occurred in 755 children, accounting for 58.3% and the average decay-missing-filled teeth (dmft) was 2.83. The differences of prevalence of dental caries of boys and girls (60.5%, 56.0%) and mean dmft index (2.88, 2.78) were of no statistical significance(χ2/F=2.64, 0.22, P>0.05). The prevalence of dental caries and mean dmft index for 3, 4 and 5-year-old group was 46.7%, 2.02 and 60.9%, 2.85 and 67.5%, 3.64, respectively. There was statistical significance among three age groups(χ2/F=40.00, 21.68, P<0.01). No significant difference was found in the dental caries prevalence and mean dmft index between urban (58.9%, 2.87) and rural area (57.7%, 2.79)(χ2/F=0.20, 0.16, P>0.05). Multivariate logistic regression showed that age, feeding pattern within the first six months after birth, dental care experience and self-perceived oral health status associated with deciduous caries in 3-5 year-old children in Henan Province(P<0.05). Conclusion Dental caries prevalence is highly prevalent among preschool children in Henan Province. Effective caries precaution measures should be taken to improve oral health level of these children.

Objective: To explore periodontal health knowledge and behavior among adolescents aged 12-15 years in Henan Province so as to provide scientific basis for oral health care. Methods: According to the basic methods of the Fourth National Oral Health Survey, 3 786 school adolescents, aged 12-15 years, were selected from 12 middle schools in two district and two country in Henan by multi-stage stratified equal capacity random sampling. Oral examination and a questionnaire survey were performed among these students. Results: The rate of periodontal health was 6.08%, the prevalence of gingival bleeding in these adolescents was 93.92%, its calculus existence was 90.99%. The rate of brushing teeth was 77.79%. However, the rate of brushing teeth twice or more per day was 17.56%, the rate of using fluoride toothpaste was 4.57%. The rate of periodontal health of adolescents who brushing teeth, using fluoride toothpaste were higher than adolescents who did not brush teeth, did not use fluoride toothpaste (χ2=10.81, 5.96, P<0.05). The recognition of oral care knowledge was 62.31%; except for "bacteria can cause dental caries", the awareness rate of other related periodontal diseases is more than 50.00%. Conclusion The status of periodontal health among adolescents aged 12-15 in Henan Province was not optimistic. Adolescents are lake of knowledge and health behavior towards periodontal health, The promotion of adolescents’s oral health education should be strengthened.