To evaluate the regulating effect of Buyang Huanwu decoction and its simple prescription (Naojian tablet) on CDK4/Cyclin D1 expression in hippocampus tissues of rats with cerebral ischemia, SD rats were divided into the sham-operation group, the model group, the Buyang Huanwu decoction group (ig, 3.15 g · kg⁻¹) and the simple prescription group (ig, 2.41 g · kg⁻¹). Each group was further divided into five subgroups based on time points after the administration, i. e. 1 d, 3 d, 7 d, 14 d and 28 d, respectively. CDK4/Cyclin D1 expressions of the group at different time points were examined by using immunohistochemistry and real-time qPCR. According to the results, the cerebral ischemia model group showed higher CDK4/Cyclin D1 expression than the sham-operation groups (P < 0.05), suggesting that the cell cycle signal pathway would be activated by the cerebral ischemic injury. Both Buyang Huanwu decoction and simple prescription groups showed significantly lower cyclin expression than the model group at 3 d, 7 d, 14 d, 28 d (P < 0.05), indicating both Buyang Huanwu decoction and its simple prescription could play the neuroprotective effect through the cell cycle signal pathway.
Animals ; Brain Ischemia ; drug therapy ; genetics ; metabolism ; physiopathology ; Cell Cycle ; drug effects ; Cyclin D1 ; genetics ; metabolism ; Cyclin-Dependent Kinase 4 ; genetics ; metabolism ; Drugs, Chinese Herbal ; administration & dosage ; Humans ; Male ; Rats ; Rats, Sprague-Dawley

Adenoviridae ; genetics ; Calcium-Binding Proteins ; genetics ; metabolism ; Cells, Cultured ; Female ; Genetic Vectors ; Humans ; Microfilament Proteins ; genetics ; metabolism ; Myocytes, Smooth Muscle ; metabolism ; Myometrium ; cytology ; metabolism ; RNA, Small Interfering ; genetics ; Recombinant Fusion Proteins ; genetics ; metabolism ; Transfection

Ten novel compounds were designed and synthesized on the basis of compound 1, their insulin-sensitizing activities were evaluated in 3T3-L1 cells. Results showed that compound 10 exhibited strong differentiation-stimulating activity on 3T3-L1 cells model, which indicated that compound 10 may possess well insulin-sensitizing activity.
3T3-L1 Cells ; Animals ; Benzopyrans ; chemical synthesis ; pharmacology ; Drug Design ; Hypoglycemic Agents ; chemical synthesis ; pharmacology ; Insulin ; pharmacology ; Mice

OBJECTIVETo investigate the effects of methylprednisolone pretreatment on pulmonary lung permeability index and the content of the pulmonary surfactant dipalmitoylphosphatidylcholine (DPPC) in a rabbit model of reexpansion pulmonary edema.

METHODSTwenty-one male New Zealand white rabbits were randomly divided into control group, reexpansion, and reexpansion+methylprednisolone pretreatment groups. The rabbit model of reexpansion pulmonary edema was established using Sakaos method. A bolus dosage of methylprednisolone (3 mg/kg) in reexpansion+methylprednisolone group group or 2.0 ml/kg normal saline in the other two groups was administered intravenously 20 min before reexpansion pulmonary edema. Bronchoalveolar lavage fluid (BALF) and arterial blood samples were collected for measurement of the total protein (TP) and DPPC contents 4 h after reexpansion, and the pulmonary permeability index was calculated.

RESULTSThe pulmonary permeability index in methylprednisolone pretreatment group was significantly lower than that in the reexpansion group (0.007∓0.002 vs 0.177∓0.004, P<0.05). Methylprednisolone pretreatment significantly increased DPPC concentration in the BALF as compared with saline treatment in the reexpansion group (61.815∓28.307 vs 101.955∓24.544 µg/ml, P<0.05).

CONCLUSIONMethylprednisolone pretreatment can increase pulmonary surfactant content and improve pulmonary permeability in the rabbit model of reexpansion pulmonary edema.

1,2-Dipalmitoylphosphatidylcholine ; analysis ; Animals ; Bronchoalveolar Lavage Fluid ; Capillary Permeability ; drug effects ; Male ; Methylprednisolone ; pharmacology ; Permeability ; Pulmonary Edema ; metabolism ; physiopathology ; Pulmonary Surfactants ; metabolism ; Rabbits

AIMTo detect the hepatotoxic pyrrolizidine alkaloids (HPA) in the genus Ligularia Cass..

METHODSThe alkaloid extracts of Ligularia plant materials were detected and analyzed by the method of combination of TLC, and LC/MSn.

RESULTSAmong 22 species of Ligularia Cass., HPA were detected in 18 species with LC/MSn, and no HPA was detected in the remaining 4 species.

CONCLUSIONHPA was first detected with LC/MSn in L. tongelensis and other 15 species of Ligularia Cass.; HPA from these plants should be isolated, separated and identified and it is necessary to study the activities and toxicities of the HPA. The types and kinds of HPA from different species and sources are different, they should be detected separately.

Asteraceae ; chemistry ; classification ; Chromatography, Thin Layer ; Molecular Structure ; Plants, Medicinal ; chemistry ; Pyrrolizidine Alkaloids ; analysis ; chemistry ; Species Specificity ; Spectrometry, Mass, Electrospray Ionization

To design and synthesis a series of novel L-amino acid esters prodrugs of acyclic nucleoside phosphonates with more potent anti-HBV activity, adefovir dipivoxil was used as lead compound, according to the results of enhanced oral bioavailability and antiviral activities of nucleoside L-amino acid ester prodrugs. Eleven novel L-amino acid ester prodrugs of acyclic nucleoside phosphonates were designed and synthesized, their anti-HBV activities were evaluated in HepG2 2.2.15 cells. Eight compounds exhibited antiviral activity, and compound 11 showed the most potent anti-HBV activity and highest selective index in vitro (EC50 0.0952 micromol x L(-1), SI 69523). Moreover, by analyzing the primary structure and activity relationship of these compounds, it could be suggested that L-amino acid ester strategy has significant potential in the acyclic nucleoside phosphonates prodrug design.
Amino Acids ; chemistry ; Antiviral Agents ; chemical synthesis ; pharmacology ; Cell Line, Tumor ; Hepatitis B virus ; drug effects ; Humans ; Liver Neoplasms ; pathology ; virology ; Nucleosides ; chemical synthesis ; pharmacology ; Organophosphonates ; chemical synthesis ; pharmacology ; Prodrugs ; chemical synthesis ; pharmacology

Objective To systematically evaluate the effect of intranasal dexmedetomidine on agita-tion during emergence from general anesthesia with sevoflurane in pediatric patients. Methods Pubmed, Embase, The Cochrane Library, China National Knowledge Infrastructure, VIP, Wan-Fang databases were searched for randomized controlled trials involving the effect of intranasal dexmedetomidine on agitation during emergence from general anesthesia with sevoflurane in pediatric patients from the start of their data-base until June 2017, and the reference lists of all included studies were checked manually. Data were ex-tracted independently by two reviewers, and primary evaluation indexes included the incidence of emergence agitation and sedation score. Secondary evaluation indexes included emergence time, extubation time, du-ration of post-anesthesia care unit stay, postoperative consumption of analgesics, incidence of adverse reac-tions ( such as bradycardia, nausea and vomiting, pruritus, laryngeal spasm) during recovery from anes-thesia. The quality of methodology of included studies was assessed. Meta-analysis was conducted with Rev-Man 5. 3 software. Results Eight randomized controlled trials involving 520 pediatric patients were includ-ed in this meta-analysis. Compared with placebo group, the incidence of emergence agitation was signifi-cantly decreased, sedation score was increased, extubation time was prolonged ( P<0. 05) , no significant change was found in the duration of post-anesthesia care unit stay or incidence of postoperative nausea and vomiting in intranasal dexmedetomidine group ( P>0. 05) . The emergence time was prolonged in intranasal 0. 3-1. 0 μg∕kg dexmedetomidine group ( P<0. 05 ) , and no significant change was found in emergence time in intranasal dexmedetomidine 1. 0-2. 0μg∕kg group ( P>0. 05) . Conclusion Intranasal dexmedeto-midine can decrease the occurrence of agitation during emergence from general anesthesia with sevoflurane and raise the quality of emergence in pediatric patients.

Objective To find out the status of HIV infection,sexual behaviors with both men and women as well as condom use among currently married men who have sex with men (MSM) so as to document for HIV intervention targeting this sub-population,in Beijing,Chengdu,Harbin and Zhengzhou cities.Methods “Snowballing” sampling method was used to recruit subjects in four cities.Participants were investigated by anonymous questionnaire containing demographics,sexual orientation,both homosexual and heterosexual behaviors and condom use during the past 6 months.Blood samples from participants were used to test HIV antibodies.Results Of the 858 participants for four cities,the average age was 38.3 (SD=9.1) years.36.7％ of them had completed the junior high school or under.The percentage of participants who identified themselves as homosexual,bisexual,and heterosexual or undecided were 40.9％,54.3％ and 4.8％,respectively.The overall HIV prevalence was 8.0％,and among four cities the HIV prevalence in Chengdu was the highest ( 13.3％ ).Results from the Multiple logistic regression analysis showed that never used condoms when having anal sex with men during the past 6 months among participants who did not have a city residential card,identifying himself as having homosexual orientation,living in Harbin,having first anal sex experience before 18 years of age the range of OR value was 1.5-2.1.In addition,the faetors associated with never using condoms in vaginal sex with women during the past 6 months were as follows:being over 46 years old,not having a city residential card,living in Beijing,identifying himself as heterosexual orientated or with unknown sexual orientation,never using condoms in anal sex with men during the past 6 months,the range of OR value was 1.7-5.9.Conclusion The prevalence of HIV infection seemed to be quite high among those currently married MSM.High rates of unprotected homosexual and heterosexual behaviors might accelerate the spreading of HIV from currently married MSM to their wives.

Objective To evaluate the prevalence of depressive symptoms and influencing factors among adolescents. Methods A total of 635 students aged 13 to 18 years were selected in March 2017 and were investigated with general information questionnaire, CES-D and CTQ-SF. Results 630 questionnaires are effective and the positive rate of depression was 29.84％(188/630) . The average score of CTQ was 32.15±2.98; 38.73％ of the students were disregarded and only 2.22％ of that were abused during their childhood. 40.00％ of the students had no CTQ, 1 kinds of CTQ accounted for 31.43％ , 2 kinds of CTQ accounted for 18.25％, and more than 3 CTQ accounted for 10.32％. Multivariate logistic regression analysis show that gender (OR=1.034, 95％ CI: 1.012-1.056) , parents' marital status (OR=1.124, 95％ CI: 1.087-1.162) , family atmosphere (OR=1.025, 95％ CI: 1.024-1.158) , CTQ cumulative number (ORCTQ=1=1.528, 95％ CI: 1.214-1.923; ORCTQ=2=3.067, 95％ CI: 1.325-7.102; ORCTQ≥3=10.361, 95％ CI: 3.059-35.093) were the risk factors for depression. Conclusion Gender, parents' marital status, family atmosphere and CTQ cumulative number were risk factors for depression in adolescents.

OBJECTIVETo study the effects of calponin-1 expression inhibition on the proliferation , invasiveness, apoptosis and cytoskeleton of uterine smooth muscle cells, and explore the molecular mechanism of calponin-1 in the uterine smooth muscle cells for labor onset.

METHODSsiRNA-calponin-1 adenovirus plasmid was constructed and transfected into primarily cultured uterine smooth muscle cells. The proliferation, invasiveness and apoptosis of the cells were determined by MTT assay, matrigel invasion assays and flow cytometry, respectively. Rhodamine-Phalloidin was used for labeling filamentous actin (F-actin), and the morphology and the distribution of F-actin was observed under fluorescence microscopy and analyzed quantitatively.

RESULTSThe motor ability of uterine smooth muscle cells decreased significantly after transfection with siRNA-calponin-1 adenovirus plasmid (P<0.05). The transfected cells showed thinner, loosened and irregular F-actin microfibers, and the cells in the empty vector and blank control groups showed thicker and longer F-actin microfibers.

CONCLUSIONInhibition of calponin-1 expression can inhibit uterine smooth muscle cell migration and cause the morphological change and rearrangement of F-actin without affecting its proliferation and apoptosis in vitro, suggesting that the morphological change and rearrangement of F-actin of uterine smooth muscle cell may be one of the important mechanisms in the labor onset.

Apoptosis ; Calcium-Binding Proteins ; genetics ; Cell Movement ; Cell Proliferation ; Cells, Cultured ; Female ; Gene Silencing ; Humans ; Microfilament Proteins ; genetics ; Myocytes, Smooth Muscle ; cytology ; metabolism ; RNA Interference ; RNA, Small Interfering ; genetics ; Uterus ; cytology ; metabolism