Objective To establish the disease-syndrome integrated animal models suitable for the studies of TCM through differen- tiating the property of TCM syndromes of spontaneous diseased animal models.Methods With the observation on general behaviors, irritable degree,turning endurance time,pain threshold,urine and stools,luster of hair,growing speed of hair,body weight,tongue condition,degree of eyeball protruding,conjunctiva chroma,blood pressure,heart rate,etc.of spontaneous hypertension rats(SHR) and the comparison with normal rats,the study was carried out on the macroscopic description of property of TCM syndrome of SHR (14～18 weeks of age)and their ethology.Results The blood pressure of SHR at the early stage tended to raise with age growing. Compared with the normal group,the heart rate of SHR rats was obviously quicker(P

Objective: To investigate the antihypertensive time-effect and dose-effect features of Sancao jiangya decoction(SCD).Methods: The blood pressure of spontaneously hypertensive rats at different time points were measured after treatment with Sancao jiangya decoction of low,middle,high concentration by tailartery blood pressure measurement for conscious rats.Results: The blood pressure was decreased at 2 hours after drug taken,there were significant dose-effect relationship between the antihypertensive effect and the low,middle,high dose.At 4h after drug taken,the high,middle dose had dose-effect correlation,but the low-dose had no antihypertensive effect.Further research on the middledose shows that the blood pressure reduced at 1h after drug taken,and the stable antihypertensive effect was keeping during 1-4h,the blood pressure began to rise at 6h,and got back to the level before drug taken at 8h.Conclusion: To choose the Middle-dose(10.4g crude drug/kg body weight) and 2h after drug taken is appropriate for SCD's use.This result laid a substantial foundation for further research on effects evaluation and mechanism of antihypertensive medicine.

Objective To evaluate diagnostic value of the novel virtual touch tissue imaging quantification (VTIQ) technique of acoustic radiation force impulse (ARFI) shear wave elastography in the differential diagnosis between benign and malignant thyroid lesions. Methods From June to July 2014, the imaging data of 82 thyroid lesions in 75 patients proven by fine needle aspiration cytology (FNAC) biopsy on conventional ultrasound and VTIQ were retrospectively analyzed. The thyroid nodules were examined by conventional ultrasound firstly and then the lesions were classified by thyroid imaging report and data system (TI-RADS). The maximum, minimum, median and average of shear wave velocity (SWV) values were obtained from multiple SWV measurement under the VTIQ speed mode. The region of interest (ROI) was determined according to the VTIQ quality mode after the patients holding the breath. According to the FNAC cytology results, ROC curve were plotted to determine the most accurate SWV value and the cut-off value for differential diagnosis. Results According to the FNAC results, grading≥5 level was set as the positive results and FNAC<5 level as the negative results. There were 28 positive nodules and 54 negative nodules in 82 thyroid nodules. The positive rates of TI-RADS classification were consistent with the theoretical results. The SWVmax, SWVmin, SWVmedian, and SWVmean on VTIQ of negative and positive thyroid nodules were (3.2±0.6), (2.2±0.4), (2.7±0.4), (2.6±0.4) m/s, and (4.6±1.7), (3.1±0.8), (3.5±1.0), (3.6±1.1) m/s. There were significant differences between positive and negative thyroid nodules in SWVmax, SWVmin, SWVmedian, and SWVmean on VTIQ (t=3.53, 3.68, 3.32, 3.81, all P<0.01). Based on the area under curve of ROC, the SWVmean value in the nodule was the best value in comparison with other SWV values. The cut-off value of VTIQ mean was 2.9 m/s. According to ROC curve analysis, the sensitivity, specificity and Youden index for VTIQ were 70.6%, 88.5%, 0.59, respectively. Conclusion The study proved that VTIQ elastography technique plays an important role in differential diagnosis of thyroid nodules and the VTIQ SWVmean is the best parameter for differential diagnosis.

Objective To evaluate the influence of thermal damage on the cell proliferation,invasive metastasis and epithelial-mesenchymal transition of hepatocellular carcinoma (HCC) through experiments in vitro,and to explore the relationship between thermal ablation and the recurrence,metastasis of HCC.Methods The McA-RH7777 HCC cell thermal damage model was established by using external heating method.The effect of thermal damage on the proliferation of HCC cells was detected by Kit-8 assay (CCK-8),and the cell cycle changes were studied by flow cytometry.The effect of thermal damage on the invasion potential of HCC cells was assessed by using Transwell assay.Fluorescence quantitative polymerase chain reaction (RT-PCR) and Western blot were used to evaluate the influence of thermal damage on HCC cell invasion potential,and on the mRNA and protein expression levels of EMT-related molecular markers,including VEGF,MMP-9,Nm23,E-cadherinand vimentin.Results Heating treatment of McA-RH7777HCC cells was performed by putting the cells in 43.5℃ water basin for 30 min.Two to five days after heating treatment the cell proliferative ability was significantly higher than that of control group (P＜0.05).At 48-72hours after heating treatment the proportion of HCC cells in G1 phase was obviously reduced and the proportion of HCC cells in S+G2 phase was significantly increased,the differences were statistically significant (P＜0.05).Compared with the control group,the difference in HCC cell invasion potential determined at 24 h after heating treatment was not significant,while the HCC cell invasion potential determined at 72 h after heating treatment was strikingly increased (22.3±2.46 vs.14.2±l.82,P＜0.001).Real-time PCR and Western blotting results indicated that at 72 h after heating treatment the expression levels of VEGF,MMP-9 and vimentin were significantly increased,while the expression level of E-cadherin was remarkably decreased,the differences were statistically significant (P＜0.05).Conclusion Thermal damage with sub-lethal heating dose can induce McA-RH7777 HCC cell to develop epithelial-mesenchymal transition and to enhance its proliferation and invasive metastasis potential,and HCC cells show higher malignant potential.

AIMTo synthesize new fluoroquinolone analogues as antibacterial compounds.

METHODS AND RESULTSBy reaction of acryl chloride(chloro-carbonic ester) with sodium sulfocyanate, acyl isosulfocyanic ester were easily obtained. Twelve 7-(4-acylamino-thiocarbamoyl-1-piperazinyl) fluoroquinolone analogues (1-12) were synthesized through modifying the 7-piperazine of norflorxacin and ciprofloxacin with isosulfocyanic ester synthesized above. The structures of synthesized compounds were characterized by 1HNMR, IR and elemental analysis.

CONCLUSIONAntibacterial activities of the new compounds were evaluated in vitro compared with norflorxacin. Compounds 5, 7, 10 and 12 showed antibacterial activities.

Anti-Infective Agents ; chemical synthesis ; chemistry ; pharmacology ; Bacillus subtilis ; drug effects ; Ciprofloxacin ; chemistry ; pharmacology ; Combinatorial Chemistry Techniques ; methods ; Escherichia coli ; drug effects ; Fluoroquinolones ; chemical synthesis ; chemistry ; pharmacology ; Microbial Sensitivity Tests ; Molecular Structure ; Norfloxacin ; chemistry ; pharmacology

Lignin peroxidase (LiP) hosted in Brij 30/cyclohexane/water nonionic reversed micelle could express its catalytic activity, but in Triton X-100/n-pentanol/cyclohexane/water nonionic reversed micelle LiP didn't show any catalytic activity. Some key factors that affected the catalytic activity of LiP in Brij 30 reversed micelle were studied at 20 degrees C. The optimum conditions were:omega0 = 8.5, pH = 2.2, [Brij30] = 600 mmol/L; under these conditions the half time of LiP was ca. 50 hours. As compared with the properties of LiP in aqueous solution, the activity of LiP hosted in Brij 30 reversed micelle dropped, but its stability improved greatly. To reveal the role of normal alcohol, which was a necessary component for forming Triton X-100 reversed micelles, the effect of n-pentanol on the catalytic activity of LiP in Brij 30 reversed micelle was investigated. Results indicated that high concentration of the alcohol deactivated LiP. So it was deduced that the phenomenon that LiP hosted in the Triton X-100 reversed micelles could not express its activity was mainly due to the alcohol co-surfactant.
Catalysis ; Cyclohexanes ; chemistry ; Enzyme Activation ; drug effects ; Micelles ; Octoxynol ; chemistry ; Pentanols ; chemistry ; Peroxidases ; metabolism ; Surface-Active Agents ; chemistry

To exert pharmacological effects, no matter therapeutic effect or toxic/side effect, it's necessary to achieve enough plasma concentration. Chinese medical compounds, which contain various ingredients, influence the metabolism of some active ingredients through the interaction of ingredients to improve curative effects or reduce toxic/side effects. Pharmacokinetics can be used to explore how Chinese medical compounds influence the in vivo metabolism of some active ingredients to achieve better curative effects.
Drugs, Chinese Herbal ; pharmacokinetics ; pharmacology ; Humans

AIMTo study the effect of Nociceptin/orphanin FQ (N/OFQ) on transient outward potassium (I(A)) in rat cerebral cortical neurons and its kinetic mechanism.

METHODSThe effects of N/OFQ on I(A) were investigated by using the whole cell patch clamp technique in acutely dissociated rat cerebral cortical neurons.

RESULTS(1) At the voltage of + 60 mV, 0.1 micromol/L N/OFQ made I(A) decreased from (5356.1 +/- 361.6) pA to (4113.3 +/- 312.7) pA (P < 0.01, n = 10) and the percent inhibition was 23.2% +/- 2.2%. (2) (N/OFQ made I-V curve of I(A) decreased significantly (P < 0.01, n = 10).(3) 0.1 micromol/L N/OFQ shifted the activation curve of I(A) to positive potential from (-9.2 +/- 2.5)mV to (30.6 +/- 3.7) mV (P < 0.01, n = 8) and changed the slope factor(kappa) of the activation curve from (20.4 +/- 2.3) mV to (22.6 +/- 2.1) mV (P > 0.05, n = 8). (4) 0.1 micromol/L N/OFQ caused a significant hyperpolarizing shift of the inactivation curve from (-64.1 +/- 3.2) mV to (-55.9 +/- 1.9) mV (P < 0.05, n = 5), without significant effect on kappa of the inactivation curve.

CONCLUSION0.1 micromol/L N/OFQ has a significant inhibition on I(A) and shift the activation and inactivation curve to depolarization in cerebral parietal cortical neurons of rats.

Animals ; Cerebral Cortex ; physiology ; Female ; Male ; Neurons ; physiology ; Opioid Peptides ; physiology ; Parietal Lobe ; physiology ; Potassium Channel Blockers ; Potassium Channels ; physiology ; Rats ; Rats, Wistar

The modulation of ACh on delayed rectifier-like potassium currents (I(K)) was studied in freshly dissociated cerebral cortical neurons using the whole-cell patch-clamp technique. Wistar rats between 10- and 14-day old of both sexes were used. After rats were decapitated, their brains were quickly removed, iced, and then manually cut into 400 mum slices. Slices were then incubated for 0.5 h at 32 degrees C in a buffered artificial cerebrospinal fluid (ACSF) bubbled with 95% O2, 5% CO2. Slices were then removed into buffered ACSF containing protease (0.5 mg/ml) at 32 degrees C. After 30 min of enzyme digestion, tissue was rinsed three times in the buffered saline. Then the enzyme-treated slices were mechanically dissociated with a graded series of fire-polished Pasteur pipettes. The cell suspension was then plated into a 35 mm dish and placed on the stage of a Olympus inverted microscope. For whole-cell recordings of currents, standard voltage-clamp techniques were used. Neurons were held at -80 mV, and the I(K) was evoked by 2 000 ms depolarizing voltage commands to potential between -40 mV and +60 mV in 10 mV steps applied at a frequency of 0.5 Hz. It was found that the inhibitory effect of ACh (0.1, 1, 10, 100 mumol/L) on I(K) was dose-dependent. It was also found that ACh affected the activation process of I(K) significantly, i.e., the activation curve of I(K) was characterized by half-activation potential of (-41.8+/-9.7) mV and a slope factor of (30.7+/-7.2) mV in the cortical neurons and they were changed to (-122.4+/-38.6) mV and (42.4+/-7.0) mV, respectively, after giving ACh (10 mumol/L). Tubocurarine (100 mumol/L) antagonized the inhibitory effect of ACh on I(K), and the drop of currents varied from the control value of (36.5+/-7..8)% to (16.9+/-13.8)% (n=8, P<0.01). 4-DAMP (10 mumol/L) blocked the inhibitory effect of ACh on I(K), and the currents reduced from the control value of (36.5+/-7.8)% to (26.8+/-4.7) % (n=6, P<0.05). Pirenzepin did not antagonize the inhibition of ACh on I(K) (n=7, P>0.05). Chelerythrine (20 mumol/L) blocked the inhibitory effect of ACh on I(K) and the currents reduced from the control value of (36.5+/-7.8)% to (11.7+/-17.3)% (n=6, P<0.05). On the contrary, PDBu (10 mumol/L) strengthened the inhibition of ACh on I(K) and the drop of currents changed from the control value of (36.5+/-7.8)% to (59.2+/-14.0)% (n=5, P<0.05). PDBu abolished the antagonism of chelerythrine on ACh in cortical neurons. It is suggested that the ACh-induced depolarization of neurons in the cortex is attributed to the inhibition of I(K) that is most likely evoked by the activation of nicotinic ACh receptors and muscarinic M3 receptor via protein kinase C (PKC) signal transduction pathway.
Acetylcholine ; physiology ; Animals ; Cell Separation ; Delayed Rectifier Potassium Channels ; antagonists & inhibitors ; Female ; Male ; Neurons ; metabolism ; physiology ; Patch-Clamp Techniques ; Protein Kinase C ; metabolism ; physiology ; Rats ; Rats, Wistar ; Receptor, Muscarinic M3 ; metabolism ; Receptors, Nicotinic ; metabolism ; Signal Transduction ; physiology ; Somatosensory Cortex ; cytology ; physiology

Adolescent ; Adult ; China ; HIV Infections ; prevention & control ; Humans ; Male ; Rural Population ; Sexual Behavior ; Single Person ; Young Adult