Objective To synthesize soybean isoflavones, and their 7-alkaline analogues and to evaluate their uterotrophic activities and anti-uterotrophic activities preliminarily. Methods The target molecules were synthesized by multi-step from resorcinol and p-substituted phenylacetic acid as the starting material. Their uterotrophic activities and anti-uterotrophic activities were evaluated by female mouse at the concentration of 1.1?10 -2 ?mol/ml and 1.85?10 -3 ?mol/ml. Results Twenty-two compounds were synthesized, among which 4 intermediates and 12 isoflavones are new compounds. Conclusion All the target molecules except for 6a show weak uterotrophic activities and high anti-uterotrophic activities.

Aim To investigate the effect of piperazinyl estrone(PE) on estrogen receptor expression and the transcriptional regulation of target genes.Methods Ovariectomized mice were given with PE in different doses (0.5 mg·kg~(-1),1 mg·kg~(-1),2 mg·kg~(-1))and estrone(0.71 mg·kg~(-1)) for 42 days,the protein expressions of Ers(Erαand Erβ)were shown by immunohistochemical method; To study transcriptional regulation of PE, PACT2-hERα and ERE2-TATA-LUC were co-transfected into MCF-7 cells by using Tfx 50 cationic liposome.Results Compared with ovx group, the groups with PE could up-regulate Ers of uteri in a dose-dependent manner,but its effect on Erα subtype was obvious.The classical ER signaling pathways could be activated by PE in co-transfected MCF-7 cells,but activation of PE was feebler than estrone with the same dose.Conclusion PE can up-regulate estrogen receptors in uteri. PE can transactivate ERE reportor gene through Erα and Erβ in MCF-7 cells, but its effect is feeble.

Aim To investigate the effect of intracerebroventricular morphine postconditioning against ischemia-reperfusion injury in rat heart and the mechanism of the central nervous system opioid receptor.Methods Forty-two Sprague-Dawley Rats were established intracerebroventricular catheter placement and myocardial ischemia/reperfusion models and randomly assigned to 7 groups:Sham group(Sham),control group(CON),intravenous control group(VCON),morphine postconditioning group(POC),intracereborventricular morphine postconditioning group(MOC).According to the dosage of intracerebroventricular morphine(3 ?g?kg-1,0.3 ?g?kg-1,0.03 ?g?kg-1),MOC group was assigned to three groups :MOC 1,MOC 2,MOC 3.Infarct size(IS),a percentage of the area at risk(AAR) was determined by triphenyltetrazolium(TTC) staining.c-fos expression in nucleus of tractus solitarius was determined by immunohistochemical method and Cardiac TroponinI(cTnI) of serum was observed at 120 min of reperfusion.Results Compared with control group,IS,IS/AAR and cTnI were significantly reduced in POC and MOC groups(P0.05).c-fos expression in nucleus of tractus solitarius were significantly reduced in MOC 2,POC(P

A novel derivative of oxytocin containing nonprotein amino acid L-alpha, beta-diaminopropionic acid (L-Dap) was synthesized by 7+2 fragment combination in solution. N beta of all the amino acid necessary was protected by carbobenzoxy (Z) and N beta of L-Dap was protected by tert. -butoxycarbonyl (Boc) . The important intermediate, heptapeptide, was synthesized by the stepwise elongation method using carbobenzoxy amino acid p-nitrophenyl esters in solution. Azide synthesis was used to get the nonapeptide. Z group was removed by treatment with 5% Pd/C and Boc with CF3COOH. Eight new compounds incorporating L-Dap were obtained and confirmed by the amino acid analysis and mass spectral detection.
Chromatography, High Pressure Liquid ; Oxytocin ; analogs & derivatives ; chemical synthesis

Objective To compare the effects of different doses of dexmedetomidine in inhibition of cardiovascular response to endotracheal intubation. Methods One hundred and twenty ASA Ⅰ or Ⅱ patients, aged 18-60 yr, weighing 45-80 kg, scheduled for upper abdominal surgery, were randomly assigned to one of 4 groups (n = 30 each): control group (group C); low, median and high doses of dexmedetomidine groups (group M1-3) .In group M1-3, 15 min before anesthesia induction, dexmedetomidine 0.25, 0.5 and 1.0 μg/kg were infused over 15 min respectively, while normal saline 15 ml was given instead of dexmedetomidine in group C. After anesthesia induction, tracheal intubation was performed when the BIS value ≤ 60 and it was maintained for 5 s. The patients were mechanically ventilated. BP and HR were recorded before infusion of dexmedetomidine (T0), before intubation (T1), immediately after intubation (T2) and at 1, 3, 5 and 10 min after intubation (T3-6). Venous blood samples were also taken at the same time to measure the plasma concentrations of epinephrine (E) and norepinephrine (NE). Results Compared with T0, HR was significantly decreased at T1 in group M1-3, BP was significantly increased at T1 in group M3, and the plasma concentrations of E and NE were significantly increased at T4-6 in group C and M1(P ＜0.05). BP and HR were significantly lower at T2, while higher at T3-5 in group C and M1than at T1 (P ＜ 0.05). BP at T1-6 was significantly higher in group M3 than in group M2 (P ＜ 0.05). Conclusion When the dose of dexmedetomidine reaches 0.5 μg/kg, it may effectively inhibit the stress reaction to noxious stimulation.

The purpose of this study was to determine the effects of piperazinyl estrone, a new estrogen derivative, on bone turnover, bone mass and uterine weight in female aged rats. Thirty-two Sprague-Dawley female rats at the age of 22 months were treated with vehicle or with piperazinyl estrone (P-E) at 0.5, 1 and 2 mg/kg/day, subcutaneous injection for 1 month. At the time of death, the uterine weight was measured and bone histomorphometric analysis of proximal tibial metaphyses (PTM) was performed in undecalcified sections. Compared with control, bone mass was increased in P-E groups. Dynamic data showed that bone resorption were decreased, but bone formation was not declined and bone mass was increased significantly in P-E (1 mg/kg day) group. There was no significant change in uterine weight. The findings of this study show that piperazinyl estrone at dosage of 1 mg/kg/d is most efficacious in preventing the bone losses in aged rats and has no side effect on uterus.
Aging ; Animals ; Estrone ; adverse effects ; analogs & derivatives ; pharmacology ; Female ; Osteogenesis ; drug effects ; Osteoporosis ; prevention & control ; Rats ; Rats, Sprague-Dawley ; Uterus ; drug effects

Objective: To examine the effects of bisphenol A (BPA), bisphenol S ( BPS ), bisphenol F ( BPF ) and bisphenol AF ( BPAF ) on the proliferation and oxidative stress of BRL 3A rat liver cells, and to preliminarily evaluate their mutagenicities. Methods: In vitro cultured BRL 3A rat liver cells were treated with BPA, BPS, BPF and BPAF at concentrations of 0, 5, 10, 25, 50, 100, 150 and 200 μmol/L for 48 h, respectively. Then, the cell viability was determined using the CCK-8 assay, and the half maximal inhibitory concentration ( IC50 ) was calculated. The minimum inhibitory concentration for BRL 3A cell proliferation was screened, and the intracellular reactive oxygen species ( ROS ) was measured in BRL 3A cells using the 2',7'-dichlorodihydrofluorescein diacetate ( DCFH-DA ) assay. In addition, the effects of BPA, BPS, BPF and BPAF at concentrations of 1 000, 200, 40, 8 and 1.6 μg/plate on the mutant colonies of histidine-deficient Salmonella typhimurium ( TA1535, TA97a, TA98, TA100 and TA102 ) were tested using the Ames test. Results: Treatment with BPA and BPF at concentrations of 100 to 200 μmol/L and with BPAF at concentrations of 25 to 200 μmol/L inhibited BRL 3A cell survival at a concentration-dependent manner, while exposure to BPS at concentrations of 5 to 200 μmol/L resulted in no changes in BRL 3A cell survival. The IC50 values of BPA, BPS, BPF and BPAF were 131.7, >200, 187.5 and 21.6 μmol/L against BRL 3A cells, respectively. Treatment with BPS at 100 μmol/L or BPAF at 25 μmol/L caused no significant changes in the ROS level; however, exposure to BPA at 100 μmol/L and BPF at 100 μmol/L significantly increased the ROS level. Ames test showed that BPA, BPS, BPF and BPAF did not induce mutagenicity in TA1535, TA97a, TA98, TA100 or TA102 strains. Conclusions BPAF shows the highest cytotoxicity to BRL 3A cells, and low-concentration exposure to BPS has few effects on BRL 3A cells. The cytotoxicity of bisphenols against BRL 3A cells may be associated with the induction of oxidative stress. None of the four bisphenols show mutagenic effects under the present experimental conditions.

This study was performed to investigate the mechanism of an anti-osteoporosis new drug XW630 for promoting the osteogenic action. Osteoblast clone was cultivated from SD adult rat calvaria in vitro, the estrogen receptor messenger RNA(ERmRNA) expression in the osteoblasts of rats was detected directly with high-sensitive RT-PCR firstly. The results indicated that XW630 can significantly promote ERmRNA expression in osteoblasts in the time-dependent manner. Being superior to other two kinds of estrogen in the same concentration (10(-6) mol/L), XW630 probably plays an important role in the bone pathogenesis by means of ER gene regulatory functions.
Animals ; Cells, Cultured ; Female ; Gene Expression ; Osteoblasts ; drug effects ; metabolism ; Piperazines ; pharmacology ; RNA, Messenger ; genetics ; metabolism ; Rats ; Rats, Sprague-Dawley ; Receptors, Estrogen ; genetics ; metabolism ; Reverse Transcriptase Polymerase Chain Reaction ; Tetracycline ; pharmacology ; Tetracyclines

We adopted firstly the dextran-coated charcoal(DCC) and SP methods to detect estrogen receptor (ER) expression of bone tissue in ovariectomized(OVX) rats. The results demonstrate that in OVX rats, XW630 can significantly promote ER expression in bone tissue and increase the ER content. XW630 is superior to estrone in effectiveness. The results also reveal that the ER expression in OVX rat bone tissue decreases with the lapse of time, indicating that the expression of ER depends on the existence of estrogen.
Animals ; Bone and Bones ; metabolism ; Estrogens, Conjugated (USP) ; pharmacology ; Female ; Ovariectomy ; Piperazines ; pharmacology ; Rats ; Rats, Sprague-Dawley ; Receptors, Estrogen ; biosynthesis ; Tetracycline ; pharmacology ; Tetracyclines

Objective: To understand the epidemiological characteristics and relevant factors on the comorbidity of hyperactivity behavior and allergic disease among preschool children in urban areas of Ma'anshan city. Methods: During April 2014 to April 2015, 91 kindergartens over 3 years old were investigated. In the investigation, 16 439 questionnaires were distributed to parents, and 15 291 valid questionnaires were collected. Conners abbreviated symptom questionnaire (brief symptom questionnaire) was filled out by parents to assess the children's hyperactive behaviors. Information of allergic disease history was reported by parents, including allergic dermatitis/eczema, food/drug allergy, allergic rhinitis and asthma. Multivariate unconditional logistic regression was used to analyze the relevant factors of comorbidity of hyperactivity behavior and allergy diseases. Results: The average age of the 15 291 children were (4.5±1.0) years old, among which 53.7% (8 218/15 291) were boys. The prevalence of hyperactive behaviors was 8.6%(1 317/15 291), and the comorbidity rate of hyperactivity and allergic deseases was 1.7% (258/15 291). After confounding factors including gender, age, delivery mode, father's age and pregnancy complications adjusted, poor sleep quality (OR=4.45, 95%CI: 2.85-6.94), long duration of watching TV at weekend (OR=1.39, 95%CI: 1.00-1.94) and poor eating behavior (OR=1.78, 95%CI: 1.07-2.98) were relevant factors of the comorbidity of hyperactivity and allergic diseases. Conclusion The prevalence of comorbidity of hyperactivity behavior and allergic disease among preschool children in urban areas of Ma'anshan city was not high. Poor night sleep quality, long duration of watching TV and frequently picky eating were relevant factors of the comorbidity of hyperactive behaviors and allergic diseases.