2.New progress in the study of protein kinase C(PKC)inhibitors
Jing WU ; Rui YANG ; Shuye LIU
Tianjin Medical Journal 2016;44(1):114-117
Protein kinase C (PKC) is a group of phospholipid-dependent serine/threonine protein kinases, which togeth-er with protein kinase A (PKA) and protein kinase G (PKG) constitute a superfamily of serine/threonine protein kinase AGC. PKC includes classic PKC, novel PKC, atypical PKC and some members of kinase associated with PKC (PRK). PKC is wide-ly distributed in mammalian tissues and cells, which plays an important biological role in growth and metabolism, prolifera-tion and differentiation of cells. A series of studies have demonstrated that variations of multiple cells, occurrence and devel-opment of diseases are related to the abnormal expression of PKC. Therefore, designing and searching for efficient PKC inhib-itors have very important implications for synthesis of many kinds of effective drugs and treatment of a variety of clinical dis-eases including cancer, cardiovascular, and hypertension, et al. In recent years, the research on PKC inhibitors has become the focus of domestic and foreign research. A large number of literatures have reported many kinds of effective PKC inhibi-tors, and analyzed their function site, mechanism, clinical trial data and so on. The discovery of these PKC inhibitors has im-portant implications for structural analysis of PKC and the treatment of diseases. So in this paper, the efficient PKC inhibi-tors are summarized.
3.Mechanisms and reversal strategies of tumor multidrug resistance
Jing WU ; Rui YANG ; Shuye LIU
Journal of International Oncology 2013;40(12):889-892
Tumor multidrug resistance (MDR) is the leading cause of clinical chemotherapy failure and death.Researches show that the occurrence of MDR is related to P-glycoprotein,multidrug resistance-associated proteins,breast cancer resistance-associated proteins,lung resistance-related proteins and other factors.Now the reversal strategies of MDR include chemical drugs reversal,gene reversal,immune reversal,traditional Chinese medicine reversal and drug-loaded nano-system reversal,which make some progress and help to improve the effect of cancer chemotherapy.
4.Analytical performance of the electrochemiluminescence immunoassay system in detecting beta subunit human chorionic gonadotropin
Jing-Rui YANG ; Run-Ling ZHANG ;
Chinese Journal of Laboratory Medicine 2003;0(08):-
Objective To validate analytical performance of electrochemiluminescent immunoassay ?-HCG and explore a suitable validation mode on electrochemiluminescent immunoassay system of Elecsys 2010 under the guidance of evidence-based laboratory medicine.Methods The analytical performance of the electrochemiluminescence immunoassay(ECLIA)system of Elecsys 2010 including precision,analytical sensitivity,linear range,accuracy and reference range was validated by detecting the specimens of different concentrations.The results were analysed by statistical package for social science 10.0.Results Imprecision studies yielded with-run CV of 0.43%-2.12% and between-day CV of 1.07%-3.73%;CV for total imprecision were 1.81%-4.90%.Recovery after dilution of high-concentration samples in assay diluent were within the rang of 94%-110%.Analytical sensitivity was
5.Path Analysis of Related Factors to Quality of Life among Rural Elderly People in Shandong Province
Rui JING ; Xiangyun LI ; Xiaodong LIU ; Shuxiang YANG ; Liantang HAN
Chinese Mental Health Journal 2002;0(12):-
Objective: To explore the related factors of quality of life(QOL) among rural elderly population in Shandong Province and explore the relationship among these factors.Methods: In this cross-sectional study,a sample of 451 elderly peple(aged from 60 to 92,without hearing or mental problems) was selected by a stratified cluster random sampling method.The 36-item Short Form Health Survey(SF-36) was used to measure QOL,and the AMOS 5.0 was used to carry out path analysis.Results: The QOL average score of all subjects was(78.5?15.4);QOL scores of males was higher than that of females [(81.2?13.0) vs.(77.5?16.3),P=0.003].There was a significant decrease of the QOL score with increasing age [60-69 years,(82.2?13.3);70-79 years,(77.0?16.0);≥ 80 years,(71.4?16.4);P
6.Effect of auricular acupressure on stress reaction in conscious patients during emergency rescue in ICU
Yuanyuan CHEN ; Rui SHEN ; Jing CHEN ; Xuelian YANG
Modern Clinical Nursing 2013;(11):42-44,45
Objective To investigate the effect of auricular acupressure on the stress reaction of conscious patients during emergency rescue in the intensive care unit(ICU).Methods Fifty conscious patients admitted to ICU were randomly divided into experiment group and control group,25 cases in each group.The two groups received conventional interventions,all separated by curtains during the rescue for psychological nursing by full-time nurses.Besides,the experiment group received auricular acupressure. The two groups were compared in terms of heart rates,systolic blood pressure,blood glucose,plasma catecholamines(epinephrine and norepinephrine)and cortisol index.Results All the items of stress reaction at minutes 30 and 60 in the experiment group were significantly lower than those in the control group.The rescue times of 30min,1H in experiment group,the stress index of experiment group at 30 mins and 60 mins were lower than those in the control group,the differences were statistically significant(all P<0?05)Conclusions Auricular acupressure is of good effects on physiological stress reaction in conscious patients during emergency rescue in ICU?
7.EFFECTS OF 18α-GLYCYRRHIZIC ACID ON RAT LIVER CYTOCHROME P450 ISOENZYMES AND PHASE II TRANSFERASE
Jing YANG ; Renxiu PENG ; Rui KONG ; Jieping YU
Acta Pharmaceutica Sinica 2001;36(5):321-324
AIM To study the effect of 18α-glycyrrhizic acid (18α-GL) on hepatic microsomal drug metabolizing enzymes in rats. METHODS 18α-GL (12.5, 50.0 mg*kg-1*d-1) were given ip to male Wistar rats for 3, 6 or 12 consecutive days. The rats were sacrificed 24 h after the last dose and the liver microsomes were prepared for analysis of cytochrome P450 (CYP) isozymes and phase II transferase activites. RESULTS Aniline hydroxylase (CYP2E1) activities in the rats treated with 18α-GL (12.5, 50.0 mg*kg-1) for 6 days decreased dose-dependently by up to 53.2%; For 3, 6 or 12 days 7-ethoxyresorufin O-deethylase (CYP1A1) activities in the rats of 50 mg*kg-1 dose group decreased time-dependently by 17.6%, 38.3% and 47.3%, respectively; Erythromycin N-demethylase (CYP3A) activities was significantly inhibited from 23.1% to 34.3%. UDP-glucuronosyltransferase activities toward 7-hydroxy-4-methylcoumarin significantly increased ranging from 19.3% to 29.9%. UDP-glucuronosyltransferase activities toward 4-phenylphenol in the rats treated with 18α-GL (12.5, 50.0 mg*kg-1) for 6 days increased by 45.9% and 70.3%. Glutathione S-transferase (GST) activities in the rats treated with 18α-GL (12.5,50.0 mg*kg-1) for 6 days increased by 13.7% and 48.3% in dose-dependent manner. CONCLUSION 18α-GL inhibited rat liver microsomal cytochrome P450 while induced phase II transferase.
8.Analysis on the proportion of incidence of etiological agents in 133 cases with constitutional delayed puberty
Deyun LIU ; Liqi YANG ; Jing HU ; Rui DAI
Chinese Journal of Primary Medicine and Pharmacy 2011;18(7):877-878
Objective To analyze the proportion of incidence of etiological agents in 133 cases with constitutional delayed puberty.Methods Clinical data of etiological agents in 133 patients with constitutional delayed puberty were retrospectively analyzed.Results Etiological agents in 133 cases with constitutional delayed puberty were as follows:Hypo-gonadotrophic hormone group(56.39%,n=75):39 cases with unknown reason(idiopathy,3 cases were female),intrapartum asphyxia/hypoxia or hemorrhage(n=23),pituitary glands dysplasia(n=6),cephal trauma(n=3),postoperative craniopharyngioma(n=2),empty sella turciea(n=2),combined hormone deficiency(n=59).Hyper-gonadotrophic hormone group(17.29%,n=23):17 cases with chromosomal disorders(n=17,male:female=7:16),3 cases with unknown reason(idiopathy).31 cases with constitutional delayed puberty(23.31%),4 cases with functional delayed puberty(3.01%).Conclusion Many etiological agents could result in delayed puberty,different origins of delayed puberty had different therapies.Classification of etiological agents in patients with constitutional delayed puberty phyed an important role in guiding option of clnical treatment.
9.Reduction of bacterial colonization and catheter-related infection with antiseptic central venous catheter: a randomized controlled clinical trial
Jun YANG ; Rui CHENG ; Jing GONG ; Jingjing XI
Chinese Journal of Clinical Infectious Diseases 2011;4(3):139-143
Objective To investigate whether antiseptic central venous catheters (CVC) modified with chlorhexidine acetate and silver sulfadiazine can be beneficial in reducing bacterial colonization and catheter-related infection. Methods Prospective controlled non-blinded randomized clinical trial was conducted. Seventy adult inpatients with CVC from intensive care unit of General Hospital of Chinese People's Armed Police Force during June 2007-June 2009 were enrolled. Their baseline characteristics, APACHE Ⅱ score and therapeutic interventions were comparable. Patients were randomly received either an antiseptic CVC ( antiseptic group, n = 28) or a standard two-lumen CVC ( control group, n = 42 ). Microbiological evaluation was done after CVC removal. A catheter bacterial colonization ( CBC) was considered if bacterial growth of > 15 CFU was found by semi-quantitative roll-plate technique from a proximal or distal catheter segment. A catheter-related infection ( CRI) was defined as a colonized catheter with local signs of inflammation. A catheter-related bloodstream infection ( CR-BSI) was defined as a colonized catheter with isolation of the same organism from the patient' s blood with accompanying clinical signs of infection. SPSS 11.5 software was used for statistical analysis. Kaplan Meier curve was used to evaluate the association between CVC retention time and bacterial colonization or infection, and Log-rank test was performed to compare between the groups. Results CVC was removed from 3.6% (1/28) patients of antiseptic group and 21.4% (9/42) patients of control group because of infection (x2 = 5. 143, P <0. 05). Colonization of CVC was observed in 7. 1% (2/28) patients from antiseptic group and 35. 7% ( 15/42) from control group (x2 =7.458, P<0.01). CBC or CRI was not observed in antiseptic group until day 19, while CRI occurred at day 6 in the control group. CVC colonization and infection were developed in 31.4% and 14. 3% patients of antiseptic group during day 14-day 28 respectively, while the rates in the control group were 90% and 70% ( u = 27.5 and 14.31, P < 0.01). Conclusions Antiseptic CVC modified with chlorhexidine acetate and silver sulfadiazine can significantly lower the risks of CBC and CRI. But more than 50% patients would develop infection when colonization occured, no matter patients receive standard or antiseptic CVC. After CVCs have been inserted for > 2 weeks, the colonization and infection will increase significantly in both standard or antiseptic CVC, so to shorten the insertion time is an effective measure to decrease the CVC-related infection.
10.Effects of Hydrophilic Polymers on the Stability of Self-microemulsifying Drug Delivery Systems
Boyu JING ; Xia ZHENG ; Rui YANG ; Jia ZHAO ; Shaojun YU
China Pharmacy 2016;27(7):910-912
OBJECTIVE:To investigate the effects of hydrophilic polymers on the stability of self-microemulsifying drug deliv-ery systems (SMEDDS). METHODS:Taking felodipine (FDP) as model drug,the content of FDP was determined by HPLC method. The effects of pure water,0.5% Kollidon VA64,HPMC E5,HPMC K100LV,HPMC K4M,PVP K30 solution,while 0.1%,0.5% and 1.0% HPMC E5 and Kollidon VA64 on residual content of dissolved FDP were determined in SMEDDS. RE-SULTS:The residual contents of dissolved FDP in SMEDDS placed in Kollidon VA64,HPMC E5,HPMC K100LV,PVP K30, HPMC K4M and pure water for 1 h were 92.7%,63.6%,50.2%,46.2%,36.0%and 24.0%,respectively. The order of maintain-ing the supersaturation state was Kollidon VA64>HPMC E5>HPMC K100LV>PVP K30>HPMC K4M>pure water. The residu-al contents of dissolved FDP in SMEDDS placed in 0.1%,0.5%,1% Kollidon VA64 and HPMC E5 and pure water for 1 h were 93.2%,95.1%,96.0% and 48.4%,62.1%,75.1%. CONCLUSIONS:Kollidon VA64 and HPMC E5 can significantly inhibit drug release in SMEDDS and be used as stabilizer of SMEDDS,wherein Kollidon VA64 was better.