AIM: To study the absorption and distribution characteristics of oxybutynin (OXY) oral tablet and transdermal gel. METHODS: A single dose of 0.1 g OXY transdermal gel (2 mg OXY) was applied to abdominal area about 4 cm2 and 0.5 mg immediate-release tablet was orally given to 48 rats in a randomized, open-label, control design test. The plasma, bladder and liver tissue were collected, disposed and analyzed and OXY pharmacokinetic parameters were calculated and evaluated. RESULTS: The Cmax of OXY transdermal gel and oral tablets in bladder are approximately 800 and 70 times higher than those in plasma. The plasma half life of OXY gel delayed 5.99 h, tablets 2.18 h. CONCLUSION: OXY gel show better pharmacokinetic properties, characterized with long half life and high target organ concentrations than those of tablets.

Objective To explore the community elderly depression effect on quality of life and provide the basis for the elderly mental health intervention. Methods Adopting stratified random sampling method, using the SF-12,CES-D and psychological capital questiennaire of elder to survey among 500 community elderly people and established the structural equation model. Results The age, degree of education, income situation, depression and the old psychological capital of the community elderly can be used to predict the quality of life, can explain 88.6%variance of life quality(P<0.05);depression on quality of life has a direct effect of-0.21(P < 0.05); depression through psychological capital indirect effect on quality of life for-0.64(P<0.05). Conclusions The elderly depression through psychological capital intermediary effect on the quality of life.

Objective To summarize the clinical features,neuroimaging findings and pathological characteristics of demyelinating pseudotumors(DPT)of the brain,and to differentiate it from glioma. Methods The clinical features,neuroimaging findings and pathological characteristics of 35 patients with demyelinating pseudotumors of the brain were summarized,and the diagnosis for 18 of them was confirmed by bioscopy.Results Demyelinating pseudotumors affected adults of both sexes.The onset age of patients ranged from 9 to 69 years old.There was no definite antecedent,and the clinical syndromes were atypical. Neuroimaging scans showed multiple lesions in cerebral hemisphere,while the lesion in brain stem and spinal cord was single.The symptom and neuroimaging were not parallel.While with many or large lesions, the symptoms and signs were less.The lesions were not enhanced on CT scan,but appeared round or patch enhancement on MRI scan.Nine patients with DWI all appeared high density.The myelin basic protein was useful for diagnosis.The typical pathological changes were demyelination,perivascular inflammatory infiltration and reactive gliosis.The Creutzfeuldt cells were also found in these patients.The lesions might become small or disappear after treatment,but could not serve as the criterion to exclude brain neoplasm. Conclusions DPT is a distinct demyelination disease entity,which is confusable with brain neoplasm.It is difficult to distinguish DPT from brain neoplasm with the clinical features and conventional neuroimaging scan.But DWI scan is useful.The pathological changes accord with demyelination,and Creutzfeuldt cells are also found.It is important to apply corticosteroid treatment or biopsy rather than being anxious to excise the lesions.

Objective To evaluate the structure and stiffness of the common carotid artery (CCA) in patients with obstructive sleep apnea syndrome (OSAS) by RFQIMT and RFQAS technology and analyze the relationships between the parameters of CCA and cardiovascular risk factors.Methods 113 participants with habitual snoring suspected OSAS were divided into control group,mild,moderate and severe OSAS groups according to apnea hypopnea index(AHI)＜5,5-20,20-40,＞40 event/hour respectively.Carotid parameters included intima-media thickness (IMT),diameter (D),distension (Dis),distensibility coefficient (DC),compliance coefficient (CC),pulse wave velocity (PWV),stiffness index α and β were collected by RFQIMT and RFQAS.Multivariate linear regression analysis was applied to analyze the relationships between CCA parameters and cardiovascular risk factors.Results ①The clinical characteristics:blood pressure had significant difference among the four groups (P ＜0.05).SO2,SO2 min decreased and T90,ODI increased significantly in mild,moderate and severe group (P ＜0.05).②The structure parameters of CCA:IMT,D and plaques had no significant difference among the four groups (P ＞0.05).③The elasticity parameters of CCA:Compared with control group,Dis increased significantly in mild group (P ＜0.05).PWV,α,β increased significantly in moderate group (P ＜ 0.05).Compared with mild group,PWV,α,β increased significantly in moderate group (P ＜0.05).Compared with moderate group,α,β increased significantly in severe group (P ＜0.05).④By multivariate linear regression analysis,age was an independent predictor of IMT,Dis,D,CC,PWV,α,β(P ＜0.05).A blunted nocturnal fall was an independent predictor of D,DC,CC,PWV (P ＜0.05),SBP,DBP and PP of daytime had an important effect on D (P ＜0.05).SO2 was independently correlated with PWV (P ＜0.05).PP was an independent predictor of PWV,α,β (P ＜0.05).Smoking was an independent predictor of plaque (P ＜0.05).Conclusions ①Stiffness is damaged earlier than morphology of CCA in patient with OSAS.②PP,a blunted nocturnal fall and SO2 are correlated with stiffness of CCA significantly.It indicates that abnormal circadian blood pressure rhythm and hypoxia are associated significantly with stiffness of CCA in patient with OSAS.

Objective:To investigate the expression levels of PPARα/γin RAW264. 7 cells in the early stages of co-cultivation with Echinococcus granulosus in vitro. Methods:RAW264. 7 cells were co-cultured with E. granulosus and collected at 12,24,36,48, 72 h. The mRNA levels of PPAR-γ,PPAR-α,M1 macrophages-associated cytokines including TNF-α,MCP-1 and IL-1β,and M2 mac-rophages-associated cytokines including Arg-1,TGF-β and Fizz-1 were detected by qRT-PCR. The protein levels of Arg-1 and MR were analyzed by ELISA. Results:The expression levels of PPAR-γ, PPAR-αand the M2 macrophages-associated cytokines including Arg-1,TGF-β,Fizz-1 and MR were significantly increased,especially at 72 h (P<0. 05). M1 macrophages-associated cytokines including TNF-α,MCP-1 and IL-1β were decreased at 72h although increased at first. Conclusion:During the early stages of co-cultivation with Echinococcus granulosus in vitro, the levels of PPAR-γ/α are up-regulated in RAW264. 7 cells, which may drive macrophage polarization and play a role in the immune escape.

Molecular glues are a class of small molecules that induce the formation of protein-protein interactions to confer new biological function or therapeutic effects. As a unique pharmacological modality, molecular glues could target proteins without druggable binding pockets. It exhibits a variety of functions, including regulating signal transduction, stabilization or degradation of targeted proteins, through sticking different proteins together. This review will summarize the development and current status of molecular glues derived from natural products and analogs by illustrating the discovery and interaction mechanism. We hope to present a systematic view, provide valuable clues for researchers and encourage them to explore more efficient and rational molecular glue discovery strategies.

OBJECTIVETo observe the efficacy on primary osteoporosis treated with spreading moxibustion for warming yang and activating blood circulation so as to provide the effective clinical therapeutic methods for osteoporosis.

METHODSSixty cases of primary osteoporosis were randomized into a spreading moxibustion group (30 cases) and a calcium tablet group (30 cases). In the calcium tablet group, caltrate was prescribed for oral administration, 600 mg per day. In the spreading moxibustion group, on the basis of the treatment as the calcium tablet group, the spreading moxibustion was applied at Dazhui (GV 14) to Yaoshu (GV 2) for warming yang and activating blood circulation. The duration of treatment was 12 weeks. Visual analogue scale (VAS) score, TCM clinical symptom score and bone mineral density (BMD) were observed and compared before and after treatment in the patients between the two groups.

RESULTSVAS scores were reduced apparently after treatment in the two groups (both P < 0.01) and the results in the spreading moxibustion group were obviously superior to that in the calcium tablet group (2.36 +/- 0.43 vs 4.52 +/- 0.35, P < 0.01). BMD were all increased in the two groups (P < 0.05, P < 0.01) and the results in the spreading moxibustion group were superior to those in the calcium tablet group (both P < 0.05). The total clinical effective rate was 86.67% (26/30) in the spreading moxibustion group, apparently better than 63.33% (19/30) in the calcium tablet group (P < 0.05). TCM clinical symptom scores after treatment were all reduced apparently in the two groups (both P < 0.01), and the result in the spreading moxibustion group was obviously superior to that in the calcium tablet group (4.72 +/- 1.90 vs 6.82 +/- 2.30, P < 0.01). The total effective rate of TCM symptoms was 93.33% (28/30) in the spreading moxibustion group, apparently better than 70.00% (21/30) in the calcium tablet group (P < 0.05).

CONCLUSIONThe combined therapy of spreading moxibustion for warming yang and activating blood circulation and the oral administration of caltrate apparently relieves pain and TCM clinical symptoms, improves BMD in the patients of osteoporosis and achieves definite clinical efficacy in the patients of osteoporosis.

Aged ; Blood Circulation ; Bone Density ; Female ; Humans ; Male ; Middle Aged ; Moxibustion ; Osteoporosis ; physiopathology ; therapy ; Yang Deficiency ; physiopathology ; therapy

OBJECTIVETo observe the clinical effect of electric stimulation of long-term retaining needle on analgesia after laparoscopic cholecystectomy (LC) and the impacts on the post-surgical flatus time.

METHODSUnder static absorptive composite general anesthesia, 90 cases of LC were randomized into three groups, 30 cases in each one. In the control group, the analgesia was not applied after LC. In the analgesia-pumper group, the patient controlled intravenous analgesia (PCIA) was used. In the needle-retaining group, the electric acupuncture stimulator was used. The needles were inserted transversely at Riyue (GB 24), Qichong (ST 30) and Yanglingquan (GB 34) and fixed with sterile sticker. Separately, in 8 h and 24 h after surgery, the electric acupuncture stimulation with disperse-dense wave, 2 Hz/100 Hz frequency was applied continuously for 30 min. Visual analogue scale (VAS), adverse reactions such as vomiting and nausea and the postoperative flatus time in 2, 4, 8, 12, 24 and 36 h after surgery were observed and recorded in the three groups.

RESULTSIn 2, 4, 8, 12 and 24 h after surgery, VAS scores in the needle-retaining group and the analgesia-pumper group were all lower than those in the control group (P < 0.05, P < 0.01). The analgesia effect at the above time points in the needle-retaining group was better than that in the analgesia-pumper group (all P < 0.05). There was not adverse reaction in the needle-retaining group. But there were 3 cases of somnolence, 6 cases of nausea and 3 cases of vomiting in the analgesia-pumper group, and 2 cases of nausea and 1 case of vomiting in the control group. The flatus time was quite earlier in the needle-retaining group as compared with the other two groups [(14.77 +/- 4.99) h vs (18.50 +/- 4.22) h, P < 0.01; (14.77 +/- 4.99) h vs (18.17 +/- 4.69) h, P < 0.05].

CONCLUSIONThe electric stimulation of long-term retaining needle is safe and effective in analgesia after LC. It avoids the adverse reactions of analgesics and promotes postoperative flatus.

Acupuncture Analgesia ; instrumentation ; Adult ; Aged ; Cholecystectomy, Laparoscopic ; adverse effects ; Electroacupuncture ; instrumentation ; Female ; Humans ; Male ; Middle Aged ; Pain Management ; Pain, Postoperative ; etiology ; therapy

Carcinoma, Adenosquamous ; diagnosis ; Carcinosarcoma ; diagnosis ; Female ; Humans ; Middle Aged ; Thymus Neoplasms ; diagnosis

OBJECTIVETo investigate the role of lymphatics in bacterial translocation from intestine of rats with burn.

METHODSEscherichia coli (E. coli) labeled with chloromethylbenzamidodialkylcarbocyanine (CM-DIL) were prepared. Sixty adult male Wistar rats were randomly divided into scald group and sham injury group according to the envelope method, with 30 rats in each group. Rats in both groups were gavaged with 0.5 mL fluid containing CM-DIL-labeled E. coli. Rats in scald group were inflicted with 30% TBSA deep partial-thickness scald (verified by pathological section) and resuscitated with fluid. Rats in sham injury group were sham injured by bathing in 25 degrees C water for 10 s (verified by pathological section) and also received with fluid infusion. Mesenteric lymph node (MLN), liver, mesenteric lymph fluid (MLF), and liver vein blood (LVB) were harvested at post injury hour (PIH) 2, 24, and 72. Bacteria translocation was detected with fluorescent tracing technique and bacteria culture. The endotoxin content in above-mentioned four kinds of specimens was quantitatively determined with chromogenic substrate limulus amebocyte lysate. The carrying capacity of endotoxin in MLF and LVB was calculated. Data were processed with t test or one-way analysis of variance.

RESULTS(1) Living bacteria were in short-stick form, and they were seen moving in single or in doubles or triples in sample fluid. Dead bacteria were in irregular aggregates. Labeled bacteria in small amount were detected in sham injury group, their number peaked at PIH 24. A large amount of labeled bacteria were detected in scald group at PIH 2, which peaked at PIH 24 and decreased at PIH 72. The largest amount of labeled bacteria were found in MLN in scald group as compared to those in the other samples, and the number peaked at PIH 24 [(5872 +/- 1976) x 10(3) CFU/g], which was obviously higher than that [(216 +/- 110) x 10(3) CFU/g, t = 30.129, P = 0.000] in sham injury group. The number of bacteria decreased at PIH 72, but it was still significantly different from that in sham injury group ( t = 4.323, P = 0.000). The number of bacteria in LVB was the smallest. (2) 29 (24.2%) samples out of the 120 samples in sham injury group were positive for bacteria. 72 (60.0%) samples out of the 120 samples in scald group were positive for bacteria. No alive bacterium was detected at any time point in LVB sample in both group; the other three samples were detected with alive bacteria since PIH 2. There were more alive bacteria detected in MLN and liver as compared with the other two kinds of samples in scald group. The amount of bacteria in MLN, liver, and MLF in scald group were higher than those in sham injury group (with t value respectively 4.353, 4.354, 4.965, P values all equal to 0.000). (3) The endotoxin level in each kind of sample at each time point was obviously higher in scald group than that in sham injury group, and it peaked at PIH 2 in liver and MLF. The difference of endotoxin level among 4 kinds of samples in scald group at PIH 2 was statistically significant ( F = 258.47, P = 0.000), and the endotoxin level was higher in liver, MLN, and MLF. They were obviously higher than those in sham injury group (with t value respectively 43.378, 43.123, 22.423, P values all equal to 0.000). The endotoxin level in MLF was 9 times of that in LVB. (4) The carrying capacity of endotoxin in LVB and MLF at each time point in scald group was higher than that in sham injury group.

CONCLUSIONSCM-DIL marked bacteria can reflect the microbial translocation condition. The lymphatic route is an important pathway for bacteria translocation.

Animals ; Bacterial Translocation ; Burns ; microbiology ; Intestinal Mucosa ; microbiology ; Lymph Nodes ; microbiology ; Lymphatic System ; microbiology ; Lymphatic Vessels ; Male ; Rats ; Rats, Wistar