Aim To establish a cell model for high throughput screening and search for novel inhibitors of P-gp.Methods A fluorescent cell-based assay was developed for application in high throughput screening.A library of 480 traditional Chinese medicine samples was screened. Results The value of Z′ was 0.72. Screening of a library of 480 traditional Chinese medicine identified 2 positive samples.Conclusions This HTS model for screening P-gp inhibitors was stable and sensitive.The 2 positive samples had good P-gp inhibitory activities.

Objective: To investigate the health literacy and its influencing factors among residents in areas out of poverty in Kunming City, so as to provide insights into formulating health education strategies. Methods: A total of 1 916 permanent residents at ages of 15 to 69 years were sampled in three areas out of poverty in Kunming City using the multi-stage stratified random sampling method and probability proportionate to size sampling method from August to October, 2020. Health literacy was investigated using the Questionnaire on the Health Literacy among Chinese Residents, the level of health literacy was analyzed and weighted by the population of the China's Seventh National Population Census. Factors affecting health literacy among residents in areas out of poverty were identified using a multivariable logistic regression model. Results: A total of 1 916 questionnaires were allocated, and 1 908 valid questionnaires were recovered, with an effective recovery rate of 99.58%. The respondents included 997 men (52.25%) and 911 women (47.75%), and had a mean age of (45.58±14.28) years. The level of health literacy was 21.38%. Multivariable logistic regression analysis identified age (15 to 24 years, OR=5.087, 95%CI: 1.573-16.450; 25 to 34 years, OR=6.016, 95%CI: 1.991-18.183; 35 to 44 years, OR=7.526, 95%CI: 2.541-22.289; 45 to 54 years, OR=4.800, 95%CI: 1.640-14.050), educational level (junior high school, OR=5.333, 95%CI: 3.100-9.175; high school/vocational high school/technical secondary school, OR=19.895, 95%CI: 10.418-37.966; college or above, OR=27.580, 95%CI: 12.349-61.597) as factors affecting health literacy among residents in areas out of poverty in Kunming City. Conclusion The level of health literacy is 21.38% among residents in areas out of poverty in Kunming City, and age and educational level are associated factors.

The discovery of high performance leading antidiabetic compounds containing sulfonamide and 4-aminophenylacetic acid moieties is reported. This was achieved by the synthesis of 6 intermediates and subsequently 20 target molecules using 4-aminophenylacetic acid as the starting materials, and through a few synthetic routes aided by multi-step reactions including sulfonylation of amino group, deacylation of amides and esterification of carboxyl group, as well as acylation of amino group. The chemical structures of the twenty-four new compounds were determined using 1H NMR, 13C NMR and HR-MS techniques. Screening in vitro of their peroxisome proliferator-activated receptor (PPAR) activation activities showed weak relative PPAR activation activities to most of the target molecules. However, 4 target molecules exhibit PPAR over 58%, and as high as 81.79% for TM2-i, presenting itself as potent leading compound for antidiabetic drugs. This research also confirms that it is probable to achieve esterification of carboxyl group and deacylation of fatty acid N-phenyl amides concurrently in SOCl2/alcohol solvent system. This provides new synthetic method for the selective reaction within molecules containing both carboxyl and N-aryl amido groups of fatty acids.

The design, synthesis and bioevaluation of a series of novel L-tyrosine derivatives as peroxisome proliferator-activated receptor (PPAR) agonists are reported. Four intermediates and twenty L-tyrosine derivatives containing phenoxyacetyl moiety TM1 were synthesized starting from L-tyrosine via four step reactions including the esterification of carboxyl group, phenoxyacetylation of a-amino group, bromoalkylation of phenolic hydroxyl group and then nucleophilic substitution reaction with various heterocyclic amines in 21%-75% overall yield. Subsequently TM1 were hydrolyzed to give sixteen corresponding target compounds TM2 in 77%-99% yield. The chemical structures of the thirty-nine new compounds were identified using 1H NMR, 13C NMR techniques and thirty-five were confirmed by HR-MS techniques. Screening results in vitro showed that the PPAR relative activation activities of the target molecules are weak overall, while compound TM2i reaches 50.01%, which hints that the molecular structures of these obtained compounds need to be modified further.

AIM: Construction of an eukaryote- E. coli shuttle expressing recombinant plasmid which expresses OmpL1 envelope protein of pathogenic Leptospira, serovar Lai strain 017. METHODS: The OmpL 1 gene was amplified by PCR from the leptospiral genome. Then it was cut with restriction enzymes and ligated to the plasmid pBK-CMV. The correct recombinant plasmid was screened out with analysis of restriction enzymes and PCR. After inducing the E. coli baring recombinant plasmid with IPTG,the complete protein of the bacteria was extracted for SDS-PAGE. At the same time, OD600 of the host bacteria was examined at different time after inducing or uninducing with IPTG. RESULTS: Five strains E. coli containing proper recombinant plasmids were screened out. Four strains E. coli expressed a new protein with a weight of 37 kD among them. With the expression of the heterogenous protein,the OD600 of the host bacteria decreased. CONCLUSION: The shuttle expressing plasmid of the OmpL 1 gene of strong virulent Leptospira strain 017 was successfully constructed. Furthermore,the recombinant plasmid expressed the expected OmpL 1 fusion protein in E. coli and the expression of the heterogenous protein had toxic effect on the host bacteria. This work was important for the future research of OmpL1 protein which relates to the diagnosis,new vaccine preparing and the pathogenic mechanism of leptospirosis.

Objective To investigate the dynamic changes of MDA, NO, SOD and pathologic changes of the lung and kidneyduring repefusion after haemorrhagic shock in rabbits, and to study the protective effects of edaravone during thecourse.Method Totally 29 beparinized (3 mg/kg) rabbits were randomly divided into three groups:tho sham-operatedcontrol group (group C, n = 7), the haemorrhagic shock group (group I/R, n = 10), and the haemorrhagicshock group with edaravone infusion (group I/R-edaravone, n = 12). Rabbits in the latter two groups were bledfrom left arteria cmralis in 10 minutes with MAP maintained at 40 mmHg for 60 minutes, and then group I/R-edar-avone was given edaravone intravenously. After that, resuscitation began:all blood loss was replaced with normalsaline within 60 minutes with MAP at the end ≥ 70% MAP before haemorrhagic shock. Edaravone was reinjectedat 10 hours after shock.All rabbits were killed at 20 h after reperfusion.Plasma nitric oxide(NO), malonyldialde-hyde (MDA) and superoxide dismutase(SOD) in every group were measured before shock,60 minutes after shockaad 1 h, 5 h and 20 h after reperfusien. Part of the right lung and the right kidney tissues were taken from everyrabbit for pathologic examnation after sacrifice.Results There was no significant difference in MDA,NO aad SOD among three groups before shock. A higherlevel of MDA (5.35±0.29 μmol/L), NO(27.75 ±2.88 μmol/L)and lower serum concentration of SOD(194.58±14.42U/ml)could be found in group I/R during haemorrhagic shock,as compared to group C(4.44±0.59 μmol/L,25.01±4.95μmol/L,210.86±24.54U/ml,respectively,P<0.01).At 20 hours after resuscitation,MDA and NO contents continued to increase(5.69±0.24 μmol/L and 28.01±3.10 μmol/L respectively,P<0.05)while SOD contents kept decreasing(151.83±9.36 U/ml,P<0.05)in group I/R.Comparing to group I/R,group I/R-edaravone had significant lower level of MDA(3.48±0.23 μmol/L,P<0.01)and higher concentration of SOD(195.10±11.87U/ml,P<0.01).Edaravone attenuated the pathologic changes in the lung and kidney.Conclusions Edaravone could effectively protect vital organs from reperfusion injury caused by free radicals following haemorrhagic shock by reducing plasma levels of MDA,NO and increasing levels of SOD.

Twenty five new beta-aminoalcohols containing nabumetone moiety were prepared via the reduction of potassium borohydride with a convenient and efficient procedure, starting from beta-aminoketones that have been synthesized by our group. Their chemical structures were determined by IR, MS, 1H NMR, 13C NMR, HR-MS and antidiabetic activities were screened in vitro. Preliminary results revealed that the antidiabetic activity of most beta-aminoalcohols were better than that of the corresponding beta-aminoketones. Although most compounds showed weak antidiabetic activity, the alpha-glucosidase inhibitory activity of compounds 5hd(1) and 5id(2) reached 74.37% and 90.15%, respectively, which were superior to the positive control. The relative peroxisome proliferator-activated receptor response element (PPRE) activity of five compounds were more than 60%, among them compound 5ca possessed the highest activity (112.59%). As lead molecules of antidiabetic agents, compounds 5hd(1), 5id(2) and 5ca deserve further study.

Objective To observe the effect of medication compliance and self-efficacy of schizophrenia patients with diabetes by continuing self-management education. Methods A total of 60 patients with schizophrenia with diabetes diagnostic criteria were divided into experimental group (30 cases) and control group (30 cases) by the admission number, 2 groups received conventional drug treatment, the control group received general preaching health education pattern, were each issued a health education manual, with schizophrenia and diabetes health knowledge division, the test group on the basis of the continuation of the implementation of self-management education, followed up 12 months after discharge, compared 2 groups of patients with medication compliance and recurrence rate, with General Perceived Self-Efficacy Scale (GSES) assessment level of 2 groups of patients with self-efficacy, fasting blood glucose (FPG) was determined by automatic biochemical analyzer, 2 hours postprandial blood glucose (2 hPBG). Results Six months after discharge, 82.1%(23/28) cases were complete compliance, 14.3%(4/28) cases of partial compliance, 3.6%(1/28) cases of non-compliance, 55.2%(16/29)cases of the control group complete compliance, 27.6%(8/29) cases of partial compliance, 17.2%(5/29) cases of non-compliance, the differences between two groups were statistically significant (χ2=37.41, P<0.05). The 12 month test group of full compliance discharged 75.0%(21/28) cases, 14.3%(4/28) cases of partial compliance, 10.7%(3/28) cases of non-compliance, 31.0%(9/29) cases of the control group complete compliance, 31.0%(9/29) cases of partial compliance, 37.9%(11/29) cases of non-compliance, the test group compliance was higher than the control group (χ2=11.27, P<0.05). The score after 6 months and 12 months respectively for the test group general self-efficacy scored 35.32 ± 2.02, 34.18 ± 1.77, control group scored 24.03 ± 3.04, 22.48 ± 2.01, the differences between two groups were statistically significant (t=16.445, 23.304, P<0.01). After 6 months in test group FPG and 2 hPBG were (5.71 ± 1.05), (9.46 ± 1.37) mmol/L, control group were (7.79 ± 1.05),(12.28 ± 2.07) mmol/L, the differences between two groups were statistically significant (t=7.483, 6.023, P<0.01). 12 months after discharge in test group FPG and 2 hPBG respectively (5.89±1.13), (9.68±1.09) mmol/L, control group (9.14±1.19), (13.17±1.42) mmol/L, test group FPG and 2 hPBG were lower than the control group (t=10.550, 7.431, P<0.01). After 6 months and 12 months, the recurrence rate of experimental group were 7.1% (2/28) and 24.1% (7/29) respectively, and control group were 14.3%(4/28) and 44.8%(13/29), the recurrence rate of experimental group was lower than the control group, there was significant difference between 2 groups (χ2=4.326, 6.225, P< 0.05 or 0.01). Conclusions Self-management education can improve the medication compliance and self-efficacy, improve mental symptoms and sugar metabolism, and reduce the recurrence rate.

Searching for new antidiabetic lead compound, 4-(1-aryl-3-oxo-5-phenylpentylamino) benzenesulfonamides were designed and synthesized directly by three component one-pot condensation of 4-phenyl-2-butanone and sulfanilamide with some aromatic aldehydes at an yield of 23%-97%. The chemical structures of the twelve new Mannich bases were confirmed by 1H NMR, 13C NMR, FTIR, ESI-MS and HR-MS. The screening results of antidiabetic activity indicated that most of these title compounds possess alpha-glucosidase inhibitory activity, among which compound le is the strongest one. And compound 11 possesses good peroxisome proliferator-activated receptor response element (PPRE) agonist activity. The structure-activity relationship of these new beta-amino ketones containing benzenesulfonamide unit was also discussed preliminarily.

Objective To evaluate the efficacy of follicular unit extraction (FUE) in the repair of scarring eyebrow loss.Methods A total of 30 patients with scarring eyebrow loss were treated with FUE technique in the Department of Plastic Surgery of Zhengzhou First People's Hospital,including 18 females and 12 males with 41 eyebrow defects.Fine soft hairs with a length of 5-10 mm were extracted from the back of the ear and temporal region of the patients,and then were split into individual follicular units under a microscope at 6 × magnification.The transplant density ranged from 20 to 30 FU/cm2.Results During the 3-18 months of follow-up after the surgery,eyebrows in the recipient areas grew in a natural direction and showed good appearance.The survival rate of hair grafts was up to 90％,and the patients were satisfied with the results.Conclusion FUE may be an ideal method for the treatment of scarring eyebrow loss with less injury and high survival rate of hair grafts.