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The p21 activated kinase 4 (PAK4) is serine/threonine protein kinase that is critical for cancer progression. Guided by X-ray crystallography and structure-based optimization, we report a novel subseries of C-3-substituted 6-ethynyl-1H-indole derivatives that display high potential and specificity towards group II PAKs. Among these inhibitors, compound 55 exhibited excellent inhibitory activity and kinase selectivity, displayed superior anti-migratory and anti-invasive properties against the lung cancer cell line A549 and the melanoma cell line B16. Compound 55 exhibited potent in vivo antitumor metastatic efficacy, with over 80% and 90% inhibition of lung metastasis in A549 or B16-BL6 lung metastasis models, respectively. Further mechanistic studies demonstrated that compound 55 mitigated TGF-β1-induced epithelial-mesenchymal transition (EMT).
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Objective:To evaluate the effects of transcutaneous electrical acupoint stimulation (TEAS) on sedation in healthy volunteers.Methods:Forty-six healthy volunteers of both sexes, with the Sleep Self-Rating Scale score 10-30, aged 22-28 yr, with the body mass index 18.5-23.0 kg/m 2, were selected and divided into 2 groups ( n=23 each) using a random number table method: TEAS group (E group) and control group (C group). Bilateral Neiguan and Shenmen acupoints were stimulated for 30 min in group E, while the stimulator was only connected, and no current was given in group C. The bispectral index (BIS)value, heart rate, oxygen saturation and mean arterial pressure were recorded at 10 min in the supine position (T 0) during the quiet period, at 10 min intervals during stimulation (T 1, 2) and at 5 min intervals within 15 min after the end of electrical stimulation (T 3-5). Then the condition whether the patient had fallen asleep was observed, and the patients were followed up on the second day for sleep status and related complications. Results:Compared with the baseline at T 0, the BIS value was significantly decreased at T 2-5 in group E ( P<0.05). The BIS value was significantly lower at T 3, 4 in group E than in group C ( P<0.05). There was no significant difference in sleep status during stimulation and at the night of the trial between the two groups ( P>0.05). Heart rate, oxygen saturation and mean arterial pressure were in the normal range at each time point, and no trial-related complications occurred in the two groups ( P>0.05). Conclusion:TEAS can produce certain sedative effect on healthy volunteers.
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Objective:To explore the cognition of nursing undergraduates and teachers on the integration of clinical curriculums under the background of nursing professional certification.Methods:With the Dundee Ready Education Environment Measure (DREEM) translated by the center for education and research of China Medical University as reference, two self-made questionnaires were used for evaluating the integrated nursing clinical curriculum (student and teacher Editions), which included self-evaluation of teachers or students, assessment of practice teaching environment, classroom harvest and self-learning, learning attitude and emotions etc. From May to July 2017, 300 questionnaires were given to300 nursing undergraduates from grades 2013, 2014, 2015 of, and 295 copies were returned. 60 questionnaires were given to 30 nursing teachers who gave clinical practice teaching and 30 medical nursing teachers wwo teach only, and 58 copies were collected. SPSS 21.0 software was used for t-test, difference analysis and linear correlation description. Results:The results of the survey showed that ①the scores of the items of "save time and energy", "the satisfaction with curriculum integration" and "reduce learning burden" in the survey were higher than those of other items. ②The scores of "the students' adaptation degree", "interns' adaptation degree" and "the mastery of the content of experiment course" were higher than those of other items in the investigation of the clinical teaching teachers. The three items with top scores evaluated by professional nursing teachers who teach only in medical college and universities were "interns' adaptation degree", "the mastery of the teaching content" and "the amount of information of the teaching content". ③There were significant differences in the average scores of the items of students from different grade ( F=6.648, P=0.002), with the increase of grade, the average score was higher with higher linear correlation ( r=0.202, P=0.005). ④There was statistically significant difference in the cognition of clinical course integration of nursing teachers who gave clinical practice teaching and medical nursing teachers who teach only ( P<0.05). Conclusion:Based on the background of nursing professional certification, nursing undergraduates care about the reduction of time, energy and other learning-related factors brought by curriculum integration, while nursing teachers pay more attention to the application of clinical curriculum integration.
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Objective To observe the therapeutic effect of beehive extract for the treatment of allergic rhinitis. Methods Sixty qualified subjects were evenly randomized into large dose group and small dose group, 30 in each group. The large dose group was given oral use of beehive extract 15 g per time, and the small dose group was given 5 g per time, three times per day. One week constituted a treatment period, and the treatment lasted 4 courses. After treatment, the therapeutic effect was evaluated in both groups. Follow-up was carried out one month after suspension of medicine. Results ( 1) The total effective rate was 90.00% in the large dose group, and was 93.00% in the small dose group, and the rank sum test results showed the difference was insignificant between the two groups (P>0.05) . (2) After treatment and during follow-up, the scores of general symptom Visual Analog Scale ( Uni-VAS) and the scores of Rhinoconjunctivitis Quality of Life Questionnaire ( RQLQ) were decreased in both groups ( P0.05) . Conclusion Oral use of large or small dose of beehive extract shows certain therapeutic effect for allergic rhinitis by obviously relieving the symptoms of patients. The effect of large dose is similar to small dose, but the long-term effect of large dose is better.