Twenty-five compounds of novel quinoxaline-based scaffold with antiplatelet activity were designed and synthesized on the basis of previous quinoxaline analogues, and the structures were confirmed by ¹H NMR, ¹³C NMR, and MS. The antiplatelet activity was evaluated, structure-activity relationship (SAR) study was summarized and the selectivity of PAR4 was confirmed by calcium mobilization assays. It was indicated that compound 14a, 14g, 13i, 13p showed moderate activity against PAR4, especially, the activity of compound 14g (IC₅₀ = 0.26 μmol·L^-1) was 6.7 times than the lead compound A (IC₅₀ = 1.73 μmol·L^-1). Therefore, 2,3-dihydro-[1,4]dioxino[2,3-g]quinoxaline and [1,3]dioxolo[4,5-g]quinoxaline derivatives are promising compounds for the discovery of novel antiplatelet agents. It is worthy of further research to develop highly effective and selective PAR4 antagonists.

Objective: To observe the difference in clinical efficacy between acupuncture with point selection based on syndrome differentiation along the meridians and acupuncture at non-meridian and non-acupoint points for functional dyspepsia (FD). Methods: A total of 74 FD patients were randomized into an observation group and a control group, with 37 cases in each group. Both groups received acupuncture treatment. Zusanli (ST 36) and Neiguan (PC 6) were selected in the observation group, with Taichong (LR 3) and Neiting (ST 44) added for excess syndrome, and Gongsun (SP 4) and Yinlingquan (SP 9) added for deficiency syndrome. Four non-meridian and non-acupoint points were selected in the control group. The treatments in both groups were performed once a day with a 2-day break after 5 consecutive treatments, which constituted one treatment course. A total of 4 courses were performed. The scores of Nepean dyspepsia index (NDI) and Leeds dyspepsia questionnaire (LDQ) were recorded before and after treatment, and during follow-up (8, 12, 16, 20 and 24 weeks after recruitment) to assess the clinical efficacy. Results: The NDI scores in the two groups after treatment and at each time point during follow-up were higher than those before treatment (all P<0.05), and the LDQ scores were lower than those before treatment (all P<0.05). The NDI scores after treatment and at each time point during follow-up in the observation group were higher than those in the control group (all P<0.01); the total LDQ score and scores of upper abdominal pain, postprandial satiety and upper abdominal burning sensation after treatment and at each time point during follow-up in the observation group were significantly lower than those in the control group (P<0.01 or P<0.05).. Conclusion: Acupuncture with point selection based on syndrome differentiation along the meridians has a better curative effect than acupuncture at non meridian and non-acupoint points in the treatment of FD.

Abstract?AIM: To investigate the effect of epigallocatechin-3-gallate ( EGCG ) against oxidative stress induced by high glucose in human lens epithelium ( HLE) cells.? METHODS: The HLE cell oxidative damage model induced by high concentration glucose was established, and was intervented with different concentrations of EGCG. Cell viability was determined by MTT assay, cell morphology was investigated by convert microscope, cells apoptosis was assayed by flow cytometry with Hoechst-PI staining. Moreover, the levels of super oxide dismutase ( SOD) , glutathione peroxidase ( GSH-Px) and malondialdehyde ( MDA) in supernatant were also tested after different treatment either with high concentration glucose or with different concentrations of EGCG.?RESULTS: MTT results showed that HLE cells activity increased to 50. 33%± 3. 52% and 63. 33%± 4. 63% after treated with 10 μmol/L and 100 μmol/L EGCG respectively, the difference was statistically significant compared with oxidative injury group(32. 67%±3. 10%)(P<0. 05 ); HLE cells maintained better morphology intervented with EGCG under high glucose conditions, the number of apoptotic cells reduced, SOD and GSH-Px level within HLE cells increased and MDA levels decreased.?CONCLUSION:EGCG plays its strong antioxidant effect by increasing SOD, GSH-Px content and decreasing MDA content in cells, therefore provides a reliable experimental basis for the search for effective prevention and treatment of cataract drug.

OBJECTIVEIn order to get the method for improving the salt resistance of Lycium ruthenium seeds and seedlings under NaCl stress, the seed germination and physiological characteristics of L. ruthenium seedlings was studied.

METHODSeveral physiological indexes of L. ruthenium seeds under NaCl stress, such as the germination rate (Gr), germination vigor (Gv), germination index (Gi), vigor index (Vi), and relative salt damage rate were measured. Other indexes of the seedlings like relative water contents (RWC) , chlorophyll contents, soluble protein contents, electrolyte leakage, the contents of malondialdehyde (MDA), and peroxidase (POD) were also measured.

RESULTNaCl at lower concentration could promote the seed germination but inhibit the seed germination at higher concentration. After the treatment by CaCl2 at the different concentrations, all germination indexes were increased. With the increase of salt concentration, the relative water contents and the contents of chlorophyll were decreased, the content of MDA and electrolyte leakage were increased. The change trend of POD activity showed the first increase and then decrease with the increase of salt concentration, which was similar to that of the soluble protein. After the treatment by CaCl2, relative water contents, chlorophyll and POD activities were decreased more slowly, and also electrolyte leakage and MDA contents increased slowly.

CONCLUSIONThe CaCl2 could significantly alleviate the damages to the seeds and seedlings of L. ruthenium under NaCl stress, and promote the salt resistance to the seeds and seedlings of L. ruthenium.

Calcium ; pharmacology ; Germination ; drug effects ; Lycium ; drug effects ; metabolism ; physiology ; Seedlings ; drug effects ; metabolism ; physiology ; Seeds ; drug effects ; metabolism ; physiology ; Sodium Chloride ; metabolism

This study was aimed to select the best preparation form of Aurea Helianthus in order to provide a scientific basis for research and development of anti-myocardial ischemia drugs.The content of effective index components of preparation of Aurea Helianthus was detected using HPLC-PDA.Acute myocardial ischemia rat model introduced by injecting pituitrin was used to investigate the effect of anti-myocardial ischemia.The quality of preparation from Aurea Helianthus was characterized based on pharmacy and efficacy.And the characterized results were given correlation analysis.The results showed that the HPLC method for quantitative determination was verified by methodology.The average recoveries were in the range of 97.04％-102.44％.All three preparations of Aurea Helianthus had the efficacy of anti-myocardial ischemia in varying degrees.The enrichment had the highest effect with lowest extraction rate and the lowest dosage,which was the best form in medicinal-preparation application of Aurea Helianthus.It was concluded that the content of related drug components was higher with unique proportion in enrichment of Aurea Helianthus which was prepared based on drug system proved a high quality medicine.Therefore,the key to the improvement of efficacy was to explore the fittest proportion and improve the content of related pharmaceutical ingredients pertinently according to drug system.

OBJECTIVETo study the influence of cervical settling method on marginal accuracy of wax patters.

METHODS24 wax patterns were made on the standard cast specimens and round capsules of which twelve patters were made with the method of cervical settling (experiment group), twelve patters were made with the method of wax dripping (control group). Marginal accuracy of patterns were measured before sublation, sublation half an hour and twenty-four hours.

RESULTSThe results revealed that marginal accuracy had significant difference between the cervical settling methods and wax dripping methods (P < 0.05). There was significant difference between the cervical settling methods measured after half an hour and twenty-four hours (P < 0.01). There was also significant difference between the wax dripping methods measured after half an hour and twenty-four hours (P < 0.01).

CONCLUSIONWax patterns with the method of cervical settling can improve marginal accuracy of patterns. The marginal accuracy of wax patters are influenced by the existing time.

Dental Casting Technique ; Dental Marginal Adaptation

OBJECTIVETo investigate the effects and mechanisms of Shexiang Baoxin Pill (SBP) on myocardial fibrosis in spontaneous hypertensive rats (SHR).

METHODSSHR of 12 weeks old were divided into the SBP group, the control group (treated with benazepril) and the model control group. The effects on such indexes as systolic blood pressure (SBP), left ventricular mass (LVM), left ventricular mass index (LVMI), content of myocardial collagen (MC) in left ventricle, extracellular matrix fibronectin (FN), laminin (LN), cardiac fibroblast (cFb) and transforming growth factor-beta1 (TGF-beta1) were determined after 12 weeks of treatment.

RESULTSSBP had no marked pressure depressive effect, but had the effect similar to that of benazepril in reducing the level of LVM, LVMI and content of MC (P < 0.05), as well as the content of LN, FN in myocardium, cFb count and TGF-beta1 expression (P < 0.05).

CONCLUSIONSBP can prevent and treat myocardial fibrosis, whose action is independent of its hypotensive effect. The mechanism may be associated with such factors as the decrease of MC synthesis in left ventricle and the deposition of extracellular matrix.

Animals ; Collagen ; biosynthesis ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Fibrosis ; prevention & control ; Hypertension ; drug therapy ; pathology ; Hypertrophy, Left Ventricular ; prevention & control ; Male ; Myocardium ; pathology ; Phytotherapy ; Random Allocation ; Rats ; Rats, Inbred SHR ; Transforming Growth Factor beta ; biosynthesis ; genetics ; Transforming Growth Factor beta1

OBJECTIVETo explore and analyze the feasibility of Community Health Service Center(CHSC)-based HIV prevention and intervention in China.

METHODSData on case finding and case management indexes were collected from 42 CHSCs in 8 cities from November, 2011 to December, 2012, and complemented by questionnaires to investigate the willingness to accept community-based HIV services among health care providers and the service targets.

RESULTSDuring November, 2011 and December, 2012, 6 729 person-times HIV tests were carried out among MSM in the cooperation between CHSCs and CBOs, and 235 HIV positives were found. A total of 40 CHSCs among 42 have conducted HIV rapid tests. The sample sources were broad and the HIV screening positive detection rate from high-risk populations in key divisions of CHSCs 0.66% (38/5 769) was higher than that in outreach high-risk populations 0.41% (15/3 623) and people receiving physical check 0.31% (20/6 532). HIV positive detection rate in CHSCs was higher 0.4% (96/23 609) than that in conventional medical institutions 0.1% (11 870/9 644 944) and newly found positives among the confirmed positives was a little lower 73.7% (56/76) than conventional programs 80.1% (8 038/10 039). The case follow-up and CD4(+) T cell testing rates in CHSCs were 100.0% (1 046/1 046) and 99.1% (1 037/1 046), respectively. The testing cost was 6.1 RMB per person on average, and the cost of 1 case found positive was 2 727.3 RMB on average. Among 361 service providers, 68.1% (246)and 91.4% (330) service providers were willing to be involved in AIDS response and support HIV service in local CHSCs. Among 755 service targets including people who seek health care in key divisions of CHSCs, MSM, and high-risk populations in local communities, 77.3% (348), 73.9% (173) and 78.1% (57) were willing to accept free HIV tests in local CHSCs.

CONCLUSIONThe effect of case finding and case management in CHSCs was good and the cost of conducting HIV tests and finding new cases were relatively low, meanwhile, most of the service provides in CHSCs and service targets support HIV service in local CHSCs. The future CHSC-based HIV prevention and intervention was feasible.

China ; Community Health Centers ; Community Health Services ; HIV Infections ; prevention & control ; HIV Seropositivity ; Health Care Costs ; Humans ; Mass Screening ; Surveys and Questionnaires

OBJECTIVETo analyze the relationship between neonatal hypoxia and polycythemia and to study clinical characteristics of Tibetan neonates whose family lived in Tibetan plateau for generations and Han neonates whose family moved to the plateau.

METHODFrom Jan. 2005 to Oct. 2006, totally 739 patients were hospitalized in the ward of neonatology of the hospital. Of these patients, 40 (20 were Tibetan and the other 20 were Han) with neonatal polycythemia. The clinical features, transcutaneous oxygen saturation (TcSO₂), peripheral routine tests and myocardial enzyme profile were studied.

RESULTThe values of hemoglobin (Hb), hematocrit (HCT), and erythrocyte count (RBC) of the Han neonates were significantly higher than those of the Tibetan newborns. Han neonates with polycythemia had lower TcSPO₂ than Tibetan neonates (P < 0.01). Comparison of myocardial enzymes showed that Han neonates had higher CKMB than that of Tibetan groups before treatment (P < 0.01), troponin was not significantly different between the Han and Tibetan groups before treatment (P > 0.05). The major common clinical manifestations of the Han and Tibetan newborns were tachypnea, cyanosis, irritability, weak reflexes and hypoxemia. The Han neonates additionally had poor responses, apnea, lower muscle tone, confusion and asphyxia.

CONCLUSIONThe clinical characteristics, TcSO₂, peripheral blood routine tests and myocardial enzyme profile are helpful in diagnosis and treatment of neonatal polycythemia. Newborn infants born to mothers who moved to the plateau area may be more susceptible to neonatal polycythemia and are prone to impairments of other organs, esp. the functions of the heart and brain.

Altitude ; Altitude Sickness ; epidemiology ; ethnology ; Cardiomyopathies ; epidemiology ; ethnology ; Erythrocyte Count ; Ethnic Groups ; Female ; Hematocrit ; Hemoglobins ; analysis ; Humans ; Hypoxia ; epidemiology ; ethnology ; Infant, Newborn ; Male ; Polycythemia ; epidemiology ; ethnology

BACKGROUNDIn China, esophageal squamous cell carcinoma (ESCC) and gastric cardia adenocarcinoma (GCA) share susceptibility loci, but different rates of multiple primary cancer and male/female ratio suggest the proportion of familial cancer is not equal.

METHODSThe percent of cases with a positive family history, median onset age, rate of multiple primary cancer, and male/female ratio associated with upper, middle, lower third ESCC and GCA were compared to reveal the proportion of familial cancer. The 7267 subjects analyzed constituted all ESCC and GCA cases in whom the cancer was resected with cure intention between 1970 and 1994 at the 4th Hospital of Hebei Medical University.

RESULTSA positive family history for cancer was most often associated with the multiple primary ESCC and/or GCA cases, e.g. with 42% of the males and 59% of the females. For upper, middle, lower third ESCC and GCA, the percent of cases with a positive family history decreased by 38.5%, 26.3%, 26.5%, and 11.2% in males (P < 0.000) and 25.0%, 22.3%, 23.9%, and 9.8% in females (P < 0.0001). Median onset age increased from 49, 52, 55, to 56 years old in males and from 50, 53, 55, to 56 years old in females ( both P < 0.0001) for upper, middle, lower third ESCC and GCA. Male/female ratio increased from 2.2, 2.1, 2.2, to 6.2:1 for upper, middle, lower third ESCC and GCA (P < 0.0001). For upper, middle, lower third ESCC and GCA, the percent of multiple primary cancers decreased from 21.2%, 2.3%, 2.2%, to 1.5% in males and from 14.3%, 2.4%, 3.4%, to 3.1% in females. The preponderance of males, smoking, drinking, or onset-age ≥ 50 years was significantly higher in GCA than in ESCC, and the difference in the rates of multiple primary cancers between the preponderant and the non-preponderant cases was significant in GCA, but not in ESCC, suggesting non-equal requirement for genetic susceptibility when environmental hazards did not exist.

CONCLUSIONSThe proportion of familial cancer in upper gastrointestinal carcinomas decreases by the primary site of upper, middle, lower third esophagus and gastric cardia. Considering familial and sporadic cancers differ in preventability, screening strategy and recurrence, our findings have basic and clinical implications.

Adenocarcinoma ; genetics ; Age of Onset ; Carcinoma, Squamous Cell ; genetics ; Cardia ; China ; Esophageal Neoplasms ; genetics ; Female ; Genetic Loci ; Genetic Predisposition to Disease ; Humans ; Male ; Middle Aged ; Neoplasms, Multiple Primary ; epidemiology ; Risk Factors ; Stomach Neoplasms ; genetics