A series of novel tetrahydrocarboline derivatives was designed and synthesized in order to discover more potent peroxisome proliferator-activated receptor (PPAR) alpha/gamma dual regulators. The structures of these compounds were confirmed by 1H NMR and HR-MS; their PPAR-regulating activities were evaluated in vitro. Compounds 6h, 6n, 6p and 6q exhibited more potent PPARalpha agonistic activities than the control drug WY14643, while compounds 60, 6g, 6i and 6q exhibited more potent PPARgamma agonistic activities than the control drug rosiglitazone. Compound 6q was discovered as a potent PPARalpha/gamma dual agonist and deserves further investigation.

Objective:To investigate whether the mindfulness training can reduce the aggression level and im-prove the sleeping quality among incarcerated people.Methods:Fifty-four male criminals were recruited into the study.They were divided into mindfulness training group (n =25)and control group (n =29).The training group took mindfulness exercise once a week for 6 weeks.While the participants in waiting list control group waited for 6 weeks without intervention.After 6-week mindfulness training for training group and post-assessment for all partici-pants,the waiting list control group went into 6-week mindfulness training.The Five Facet Mindfulness Question-naire (FFMQ),Aggression Questionnaire (AQ)and Pittsburgh Sleep Quality Index (PSQI)were assessed before and after the intervention.Results:There were 19 valid data in training group,and 21 in control group.After 6-week training,the score difference between pre-and post-assessment of FFMQ (P <0.01 )was higher in the training group than in the control group,and the difference of AQ (P <0.01)and PSQI (P <0.01)was lower in training group than in the control group.Conclusion:The results suggest that 6-week mindfulness training could effectively reduce the aggression level and improve the sleep quality in the long-term incarcerated males.

Objective To explore the effect of applying problem-based learning(PBL)in clin-ical anesthesiology demonstration for clinical undergraduates. Methods Eighty-nine 2009 clinical undergraduates were divided into two groups:experimental group and control group. Students in ex-perimental group received PBL while those in control group received traditional teaching. The effect was evaluated according to the results of case examination and investigation table. The results were analyzed by X2 test. Results Most students (42/45) answered questions correctly in experimental group while only 30 of 44 students(30/44)did in control group(P<0.05). Concerning the results of investigation,PBL had more advantages than traditional teaching method in the following 5 aspects:self-studying ability(86.7%,39/45),clinical thinking ability(73.3%,33/45),information seeking ability (75.6%,34/45),expressing ability (82.2%,37/45),communicating between students (75.6%, 34/45)(P<0.05). Conclusions PBL has evident advantages in anesthesiology clinical demonstration. It can inspire students,cultivate abilities,enhance critical thinking and finally improve teaching effect.

A series of novel tetrahydrocarboline derivatives was designed and synthesized in order to discover more potent peroxisome proliferator-activated receptor (PPAR) alpha/gamma dual regulators. The structures of these compounds were confirmed by 1H NMR and HR-MS; their PPAR-regulating activities were evaluated in vitro. Compounds 6h, 6n, 6p and 6q exhibited more potent PPARalpha agonistic activities than the control drug WY14643, while compounds 60, 6g, 6i and 6q exhibited more potent PPARgamma agonistic activities than the control drug rosiglitazone. Compound 6q was discovered as a potent PPARalpha/gamma dual agonist and deserves further investigation.
Animals ; Carbolines ; chemical synthesis ; chemistry ; pharmacology ; Cells, Cultured ; Drug Design ; Hypoglycemic Agents ; chemical synthesis ; chemistry ; pharmacology ; Molecular Structure ; PPAR alpha ; agonists ; PPAR gamma ; agonists ; Peroxisome Proliferator-Activated Receptors ; agonists ; Pyrimidines ; metabolism ; Structure-Activity Relationship ; Thiazolidinediones ; metabolism ; Transfection

Abstract? AIM: To evaluate the efficiency of two different operation ways, vitrectomy and vitrectomy combined with inferior scleral buckling, for a complex kind of retinal detachment.?METHODS:The complex kind of retinal detachment were diagnosed in 100 cases ( 100 eyes ) , with the common features:1)the course of more than 1mo;2) at least one retinal hole located in the inferior marginal retina;3) the detachment of retina was found proliferated, there was at least 1 retinal fold in retinal detachment area. The patients were randomly divided into two groups: the treatment group ( 50 eyes ) who received vitrectomy combined with inferior scleral buckling;the control group ( 50 eyes ) who received vitrectomy without scleral buckling. The retinal anatomic reattachment, visual function recovery, macular central fovea thickness and complications in two groups were observed.? RESULTS: There were 49 eyes ( 98%) with retinal anatomic reattachment in the treatment group while 42 eyes(84%)in control group(χ2=4.2605, P<0.05);the best corrected visual acuity ( BCVA) was 0.254 ±0.238 in the treatment group while it was 0.219±0.229 in control group (t=1.8879,P>0.05);the macular central fovea thickness was 272 ±32.21μm in the treat group while it was 316 ± 33.46μm(t=12.597,P<0.01).Intraocular pressure in 12 eyes ( 24%) was more than 30mmHg in the treatment group while 4 eyes ( 8%) in control group within 1wk postoperation (χ2=4.7619,P<0.05); intraocular pressure in 100 eyes were controlled below 21mmHg 1mo postoperatively.? CONCLUSION: It is a more effective method to vitrectomy combined with inferior scleral buckling than the single vitrectomy for the special kind of retinal detachment.It can increase the rate of retinal anatomic reattachment and reduce macular edema.

Objective To report the microsurgical outeome of the meningiomas located in the eranio- cervical junction.Methods Seven eases of meningiomas arising from the craniocervical junction operated with microsurgical technique by use of the posterior approaehes including the suboccipital approach,the lower lateral suhoecipital approach and for lateral approach.Reviewed the related ariieales and were analysed relative to their approach selection and outcomes were analysed.Results The tumors ranged in size from 0.8 to 4.8 cm and the tumors location with 2 cases posterior,3 cases anterior and 2 cases lateral to the brain stem.3 in 7 cases were operated by use of the suboccipital approach,2 in 7 cases with the lower lateral suboccipital ap- proach and 2 in 7 cases with farlateral approach.Total excisions were got in 6 of 7 cases,4 in 6 cases with Simpson gradeⅠand 2 in 6 cases withⅡ.The subtotal excision was got in 1 of 7 cass.Follow-up with 6 ca- ses between 6 to 36 months,the occupied symptoms in 6 cases improved good.No remnant tumor and recur- rent were found in the MRI follow-up.Conclusion By using of the proper posterior approaches,the micro- surgical outonmes of the meningiomas arising from craniocervical junction are good.

To investigate cytotoxic secondary metabolites of Micrococcus sp. R21, an actinomycete isolated from a deep-sea sediment (-6 310 m; 142 degrees 19. 9' E, 10 degrees 54. 6' N) of the Western Pacific Ocean, column chromatography was introduced over silica gel, ODS, and Sephadex LH-20. As a result, eight compounds were obtained. By mainly detailed analysis of the NMR data, their structures were elucidated as cyclo(4-hydroxy-L-Pro-L-leu) (1), cyclo(L-Pro-L-Gly) (2), cyclo( L-Pro-L-Ala) (3), cyclo( D-Pro-L-Leu) (4), N-β-acetyltryptamine (5), 2-hydroxybenzoic acid (6), and phenylacetic acid (7). Compound 1 exhibited weak cytotoxic activity against RAW264. 7 cells with IC50 value of 9.1 μmol x L(-1).
Animals ; Biological Factors ; chemistry ; isolation & purification ; metabolism ; pharmacology ; Cell Survival ; drug effects ; Macrophages ; cytology ; drug effects ; Magnetic Resonance Spectroscopy ; Mass Spectrometry ; Mice ; Micrococcus ; chemistry ; genetics ; isolation & purification ; metabolism ; Molecular Structure ; Phylogeny ; RAW 264.7 Cells ; Seawater ; microbiology ; Secondary Metabolism

Objective:To compare the safety and long-term survival of patients with synchronous rectal cancer liver metastasis, who received either simultaneous or staged resection to treat primary tumor and liver metastases. Methods:Clinicopathologic and peri-operative data were collected retrospectively from 54 patients with synchronous rectal cancer liver metastasis, who received both prima-ry and liver resections between January 2000 and April 2015 at Peking University Cancer Hospital. Routine follow-up was conducted. The safety and long-term survival of 19 patients who underwent simultaneous resection were compared with those of 35 patients who received staged resection. Results:The clinicopathologic data between the two groups were comparable. Postoperative Clavien-Dindo grades 1, 2, 3, and 4 complications were 10.5%(2/19), 31.6%(6/19), 5.3%(1/19), and 10.5%(2/19) for the simultaneous group, respec-tively, and 8.6%(3/35), 17.1%(6/35), 25.7%(9/35), and 0%(0/35) for the staged group correspondingly, which were not significantly different (P=0.093). However, the median postoperative hospital stay of the simultaneous group was significantly shorter than that of the staged group (14 days versus 25 days, P<0.001). The median postoperative overall survival (OS) and disease-free survival (DFS) be-tween these groups were not significantly different [not reached versus 39 months for OS, respectively (P=0.649);10 months versus 10 months for DFS, respectively (P=0.827)]. Conclusion:The postoperative complications in simultaneous resection group were not sig-nificantly increased compared with those in staged resection group for synchronous rectal cancer liver metastasis. The long-term results among the groups were similar.

Objective:To observe the effect of An-pressing manipulation on biceps brachii with delayed onset muscle soreness (DOMS) in healthy male volunteers.Methods:A total of 30 male college student volunteers were randomly divided into a blank group,a model group and a treatment group,10 cases in each group.Subjects in the blank group did not receive any intervention;subjects in the model group received active weight-bearing eccentric exercise on the non-favored side of the upper limb to establish the models,while not receiving any treatment;subjects in the treatment group received both the same modeling and An-pressing manipulation treatment.The subjective rating of perceived exertion (RPE),subjective soreness sensation threshold and soreness grade were evaluated before modeling,immediately after modeling,and 24,48,72,96 and 120 h after modeling.Serum total antioxidant capacity (T-AOC) was measured before modeling,immediately after modeling,and 24,48 and 72 h after modeling.Serum creatine kinase MM isoenzyme (CK-MM) was measured before modeling and 24,48 and 72 h after modeling.Results:At 24,48,72 and 120 h after treatment,the soreness grades of the treatment group were lower than those of the model group (all P＜0.05).The RPE scores of the treatment group were lower than those of the model group (all P＜0.05) immediately after modeling,at 24,48,72,96 and 120 h after modeling.The subjective soreness sensation threshold of the treatment group was higher than that of the model group immediately after modeling,at 24,48,72 and 96 h after modeling (all P＜0.05).Immediately after modeling,T-AOC value in the treatment group was higher than that in the model group and blank group (both P＜0.05).CK-MM of the treatment group was lower than that of the model group at 48 h and 72 h after modeling (P＜0.05).Conclusion:An-pressing manipulation shows a certain therapeutic effect on biceps brachii with DOMS by strengthening the body's antioxidant and anti-damage abilities,which can effectively reduce the pain and accelerate the recovery from fatigue damage.

Objective:To observe the influence of pressing force and time on the thermal effect of An-pressing manipulation.Methods:Eight healthy volunteers were recruited to receive An-pressing manipulation at Xinshu (BL 15) on the right side.The pressing force and time were both divided into five levels:the force described as extremely mild,mild,moderate,strong and extremely strong and time given by 2.5 min,5.0 min,7.5 min,10.0 min and 15.0 min.The real-time change in local acupoint temperature as well as the change during 1.0-15.0 min after the manipulation were observed.Results:Compared with the baseline data,the real-time changes in the temperature after An-pressing Xinshu (BL 15) on the right side with different levels of force (from mild to strong) were respectively (1.88t0.64) ℃,(2.05±0.68) ℃,(2.25±0.59) ℃,(2.35±0.61) ℃ and (2.32±0.69) ℃;the changes in 15.0 min after the manipulation were respectively (-0.11±0.11) ℃,(0.03±0.14) ℃,(0.59±0.58) ℃,(1.38±0.70) ℃ and (2.09±0.98) ℃.The real-time temperature changes after the manipulation for different durations (from short to long) were respectively (1.94±0.37) ℃,(2.33±0.29) ℃,(2.49±0.31) ℃,(2.51±0.39) ℃ and (2.41±0.55) ℃;the changes in 15.0 min after the manipulation were respectively (0.53±0.49) ℃,(0.33±0.30) ℃,(0.52±0.33) ℃,(0.55±0.38) ℃ and (0.76±0.36) ℃.Conclusion:The thermal effect presented an increasing tendency with the extension of pressing time,and the temperature reached the top at 7.5 min;the thermal effect showed an increasing tendency with the rise of pressing force,and the temperature reached the top upon a moderate level of force.The pressing time can produce a greater influence on the real-time temperature than the pressing force;the pressing force can produce a greater influence on maintaining the temperature than the pressing time.