(1)H-NMR and (13)C-NMR assignments of 12-oleanene-3,11-dione (compound 1) were completely described for the first time through conventional 1D NMR and 2D shift-correlated NMR experiments using (1)H-(1)HCOSY, HMQC, HMBC techniques. Based on its NMR data, the assignments of 28-hydroxyolean-12-ene-3,11-dione (compound 2) were partially revised.
Euonymus ; metabolism ; Magnetic Resonance Spectroscopy ; Molecular Conformation ; Oleanolic Acid ; analogs & derivatives ; analysis ; chemistry ; Triterpenes ; analysis ; chemistry

OBJECTIVETo investigate the association between pulmonary vascular remodeling and expression of hypoxia-inducible factor-1α (HIF-1α), endothelin-1 (ET-1) and inducible nitric oxide synthase (iNOS) in pulmonary vessels in neonatal rats with hypoxic pulmonary hypertension (HPH).

METHODSA neonatal rat model of HPH was established as an HPH group, and normal neonatal rats were enrolled as a control group. The mean pulmonary arterial pressure (mPAP) was measured. The percentage of medial thickness to outer diameter of the small pulmonary arteries (MT%) and the percentage of medial cross-section area to total cross-section area of the pulmonary small arteries (MA%) were measured as the indicators for pulmonary vascular remodeling. The immunohistochemical reaction intensities for HIF-1α, ET-1 and iNOS and their mRNA expression in lung tissues of neonatal rats were measured. Correlation analysis was performed to determine the relationship between pulmonary vascular remodeling and mRNA expression of HIF-1α, ET-1 and iNOS.

RESULTSThe mPAP of the HPH group kept increasing on days 3, 5, 7, 10, 14, and 21 of hypoxia, with a significant difference compared with the control group (P<0.05). The HPH group had significantly higher MT% and MA% than the control group from day 7 of hypoxia (P<0.05). HIF-1α protein expression increased significantly on days 3, 5, 7 and 10 days of hypoxia, and HIF-1α mRNA expression increased significantly on days 3, 5 and 7 days of hypoxia in the HPH group compared with the control group (P<0.05). ET-1 protein expression increased significantly on days 3, 5 and 7 days of hypoxia and ET-1 mRNA expression increased significantly on day 3 of hypoxia in the HPH group compared with the control group (P<0.05). Both iNOS protein and mRNA expression were significantly higher on days 3, 5 and 7 days of hypoxia than the control group (P<0.05). Both MT% and MA% were positively correlated with HIF-1α mRNA expression (r=0.835 and 0.850 respectively; P<0.05).

CONCLUSIONSPulmonary vascular remodeling is developed on day 7 of hypoxia in neonatal rats. HIF-1α, ET-1 and iNOS are all involved in the occurrence and development of HPH in neonatal rats.

Animals ; Animals, Newborn ; Endothelin-1 ; analysis ; physiology ; Hypertension, Pulmonary ; etiology ; metabolism ; pathology ; Hypoxia ; complications ; Hypoxia-Inducible Factor 1, alpha Subunit ; analysis ; physiology ; Immunohistochemistry ; Nitric Oxide Synthase Type II ; analysis ; physiology ; Pulmonary Artery ; chemistry ; pathology ; Rats ; Rats, Wistar

OBJECTIVETo study the action mechanism of Yiqi Yangyin Recipe (YYR) in treating leukemia by observing the effects of YYR and its different assembling, energy supporting part (P1) and evil dispelling part (P2) on expressions of Flt3 and N-ras gene in acute myeloid leukemic (AML) cells.

METHODSThe mononuclear cells collected from bone marrow of 60 AML patients were assigned to four groups: the blank was untreated for control and the three tested groups were treated with YYR, P1 and P2, respectively. The effects on Flt3 and N-ras gene expressions and FLT3 protein expression were observed by RT-PCR and Western bloting.

RESULTSRT-PCR test showed the expression of Flt3 in the control, YYR, P1 and P2, group was 90.78% +/- 6.92%, 38.18% +/- 4.50%, 65.57% +/- 5.55% and 61.35% +/- 6.39%, respectively; and that of N-ras in them 93.28% +/- 5.54%, 34.38% +/- 6.69%, 59.42% +/- 7.35% and 65.28% +/- 7.64%, respectively, both showed significant difference as compared the data in the tested groups with those in the control group (P < 0.05). Western bloting test showed the FLT3 protein gray value in the four groups was 0.8127 +/- 0.0284, 0.4265 +/- 0.0353, 0.5396 +/- 0.0274 and 0.5473 +/- 0.0282, respectively, also showed significant difference between the control and the tested groups (P < 0.01).

CONCLUSIONYYR can inhibit the colonic proliferation of AML cells, decrease the expressions of FLT3 and N-ras in cells, therefore shows a therapeutic effect on AML.

Adolescent ; Adult ; Bone Marrow Cells ; pathology ; Child ; Drugs, Chinese Herbal ; pharmacology ; Female ; Genes, ras ; Humans ; Leukemia, Myeloid, Acute ; genetics ; pathology ; Leukocytes, Mononuclear ; metabolism ; pathology ; Male ; Middle Aged ; Tumor Cells, Cultured ; Young Adult ; fms-Like Tyrosine Kinase 3 ; genetics ; metabolism ; ras Proteins ; genetics ; metabolism

Objective To compare the coherence of serum creatinine,creatinine clearance(Ccr), Cystatin C,and estimated glomerular filtration rate(eGFR)in each stage of chronic kidney disease(CKD) patients.Methods Creatinine in serum and urine were determined by Jaffe method;serum Cystatin C was measured by particle enhanced turbidimetric method,while eGFR was calculated using the abbreviated Modification of Diet in Renal Disease(MDRD)equation which was mainly based on the serum creatinine concentration.According to the American national kidney foundation-Kidney Disease Outcome Quality Initiative(NKF-K/DOQI)guideline,all cases were grouped by eGFR into 5 stages.Results In these 228 cases,as eGFR decreased gradually,the average levels of creatinine and Cystatin C increased,while Ccr decreased.The level of each items showed a statistic difference among each stage(P0.05);in eGFR 60-89 ml/min group,the average level of creatinine was 83.3 ?mol/L,the abnormal rate was only 6.8%,it was not a sensitive marker to detect the slightly damaged GFR,the levels of Ccr and Cystatin C showed a marginal decrease and increase,with an abnormal rates of 70% and 86%,there was a statistic difference among the three abnormal rates(P

Background Qiang minority is minority groups of China with the special habits and customs and living condition. So whether the spectrum of disease and bacteria spectrum in conjunctiva are similar with Han nationality is worth paying attention. Objective Present survey was to obtain the data about bacterial species in conjunctival sac in Qiang minority population with the age 40 years old and more and the compare with matched Han nationality population. Methods This survey study was performed as the standardized training and protocol. A total of 212 eyes of 106 individuals from Qiang minority in Beichuan county and 640 eyes of 320 subjects from Han nationality in Mianyang city received questionnaire survey and ophthalmological examination. The secretion of the inferior palpebral conjunctival sac was embrocated and inoculated on blood plate for 48-72 hours. The bacteria was separated and identified. This study was approved by the Ethic Committee of Sichuan Provicial People' s Hospital. Orally informed consent was obtained before the medical procedure. Results All the examinee finished the survey and examination with a good compliance. No significant difference was found in the demography between these two groups of population. The multiple bacterial positive rate in conjunctival sac was 59. 4% in Qiang minority and that of Han people was 66. 3% with a considerably difference between them (χ2 = 2. 27,P = 0. 13). The multiple bacterial species were simultaneously detected in 26.2% in Qiang minority population and 11.88% Han people, showing evidently difference (χ2 = 106. 40, P = 0. 00 ) . The positive rate of corynbaccterium in conjunctival sac of Qiang minority was statistically lower than that of Han people (20. 7% versus 45. 0% ,χ2 =31. 75 ,P = 0. 00) ,but there was no statistical difference in the positive rate of staphylococcus epidemics between two groups (χ2 = 1. 89 ,P = 0. 17). Conclusion The bacteria positive rate in conjunctiva sac is resemble in the population over 40 years in both the Qiang minority and Han nationality. The simple bacterial species is found in majority people in two groups of subjects. The positive rate of multiple bacterial strains coexistence is more in the Qiang minority. The bacterial strains is different between Qiang minority and Han nationality.

OBJECTIVETo compare the ventricular-dynamic parameters and thoracic aorta tension induced by two septic shock models in rats.

METHODSSeptic shock models were induced by cecal ligation or puncture (CLP) and intraperitoneal injection of lipopolysaccharide (LPS) in rats. The carotid artery was cannulated and connected to a pressure transducer to determine mean arterial blood pressure (MABP). Ventricular dynamic parameters, including heart rate (HR), left ventricular developed pressure (LVDP) and maximal rise/fall velocity of ventricular pressure (± dP/dtmax) were determined. Isolated thoracic rings were mounted on an organ bath and the tension of the vessel was recorded.

RESULTThe mortality was 65.2% in CLP shock rats, but no death in LPS shock rats. The MABP and HR of CLP rats were decreased more prominently than those of LPS rats (P < 0.01). Contraction induced by high K(+) (60 mmol/L) or 10⁻⁶ mol/L phenylephrine (PE) in endothelium-intact and endothelium-denuded aortic rings was all attenuated, but in LPS rats it was more prominent (P < 0.01).

CONCLUSIONTwo rat septic shock models can decrease ventricular-dynamic parameters and vasoconstriction responsiveness of aorta. The ventricular-dynamic parameters decrease more prominently in CLP model, while vasoconstriction responsiveness of aorta changes more in LPS model.

Animals ; Cecum ; surgery ; Disease Models, Animal ; Hemodynamics ; Ligation ; adverse effects ; Lipopolysaccharides ; toxicity ; Male ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Shock, Septic ; etiology ; physiopathology ; Vasoconstriction ; Ventricular Pressure ; physiology

OBJECTIVETo study the effects of long-term exposure to carbon disulfide (SC(2)) on cardiovascular system of workers.

METHODSThe concentrations of CS(2) were detected in the representative workshops with different exposure levels. The indicators related to cardiovascular system were tested in 633 workers occupationally exposed to CS(2), which included blood pressure, electrocardiogram, blood routine (blood RT), cholesterol (TCHO), triglyceride (TG) and so on. The data were analyzed by chi-square test and multiple logistic regression analysis.

RESULTSThe exposure concentration of CS(2) for 389 workers was less than or equal to 5 mg/m(3), which for other 244 workers was higher than 5 mg/m(3). The maximum exposure concentration of CS(2) was 15.73 mg/m(3). There were no significant effects of CS(2) on the electrocardiogram, red blood cells, white blood cells, blood platelet, TCHO and TG of workers. However, the positive effects of CS(2) on blood pressure and negative effects of CS(2) on hemoglobin were found. The rates of high TCHO, TG and hypertension in male workers were significantly higher than those in female workers (P < 0.05). The rates of high TCHO, hypertension and sinus arrhythmia in older workers (≤ 30 years old) were significantly higher than those in young workers (> 30 years old) (P < 0.05). The rate of sinus arrhythmia in workers with 1 - 10 working years was significantly higher than that in workers with more than 10 working years (P < 0.05). The rate of hypertension in workers with 1 - 10 working years was significantly lower than that in workers with more than 10 working years (P < 0.05).

CONCLUSIONThere were no significant effects of CS(2) exposure on the indexes of cardiovascular system of workers.

Adult ; Blood Pressure ; Carbon Disulfide ; adverse effects ; Cardiovascular System ; drug effects ; physiopathology ; Erythrocyte Count ; Female ; Humans ; Male ; Middle Aged ; Occupational Exposure ; analysis ; Risk Factors ; Young Adult

OBJECTIVETo explore the changes on the content of substrate, the activity of correlative enzyme and the mRNA and protein expressions of beta(3)-adrenoceptor and peroxisome proliferator-activated receptor alpha (PPARalpha) in human failing heart.

METHODPapillary muscles from 20 patients with heart failure during mitral valves replacement and 6 control subjects died of non-cardiac accidents were obtained and free fat acid (FFA), lactic acid (LD) and the activity of Na(+)K(+)-ATPase and Ca(2+)Mg(2+)-ATPase, protein and mRNA expressions of beta(3)-adrenergic receptor and PPARalpha were measured.

RESULTIn the failing heart, the contents of fat acid, LD and expression of beta(3)-adrenoceptor mRNA and protein were significantly higher while the activity of Na(+)K(+)-ATPase and Ca(2+)Mg(2+)-ATPase, expressions of PPARalpha at mRNA and protein levels were significantly lower than those in control myocardium.

CONCLUSIONMetabolic remodeling (upregulation of beta(3)-adrenoceptor and downregulation of PPARalpha) might contribute to the pathophysiology of heart failure.

Adult ; Female ; Heart Failure ; metabolism ; Humans ; Male ; Middle Aged ; Myocardium ; metabolism ; PPAR alpha ; metabolism ; Receptors, Adrenergic, beta-3 ; metabolism

OBJECTIVETo evaluate the effects of tramadol on the proinflammatory responses in a rat model of incisional pain by investigating its effects on nociceptive thresholds and serum interleukin-6 (IL-6) and IL-2 levels.

METHODSForty-two male Sprague-Dawley (SD) rats scheduled for plantar incision were randomly divided into 7 groups (n=6 in each group). Rats in Group 1 receiving general anesthesia with no incision were served as control; At 30 min before skin incision, Groups 2 to approximately 5 were given 5 ml normal saline or 1, 10, and 20 mg/kg tramadol, respectively, intraperitoneally (i.p.); Group 6 received 10 mg/kg tramadol after operation; Group 7 received 10 mg/kg tramadol before incision, followed by 200 microg/kg naloxone after operation. Mechanical allodynia was measured by electronic von Frey filament to evaluate the nociceptive thresholds 1 h before incision, and 1 h and 2 h after operation. Serum IL-6 and IL-2 levels were measured by enzyme-linked immunosorbent assay (ELISA) 2 h after operation.

RESULTSMechanical thresholds decreased significantly and serum IL-6 level increased significantly after operation in Group 2 compared with control (P<0.01), and these changes were reversed respectively by tramadol in a dose-dependent manner (P<0.05 and P<0.01, respectively). IL-2 level remained unchanged after operation in Group 2, but decreased in Group 3 (P<0.05), then gradually returned to the normal level in Groups 4 and 5. The intraperitoneally injected tramadol (10 and 20 mg/kg) produced a potent and dose-dependent antinocicptive effect on the lesioned paw. The antinocicptive effects of tramadol were partially antagonized by naloxone (200 microg/kg), suggesting an additional non-opioid mechanism.

CONCLUSIONThe results suggest that tramadol could be a good choice for the treatment of pain under the conditions that immunosuppression may be particularly contraindicated.

Analgesics, Opioid ; pharmacology ; Animals ; Dose-Response Relationship, Drug ; Interleukin-2 ; biosynthesis ; blood ; Interleukin-6 ; biosynthesis ; blood ; Male ; Pain Measurement ; methods ; Pain Threshold ; drug effects ; Pain, Postoperative ; blood ; drug therapy ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Tramadol ; pharmacology

OBJECTIVETo investigate effect of tramadol on c-fos expression in spinal cord dorsal horn and serum IL-6 levels induced by plantar incision in rats.

METHODSThe Brennan pain model was induced by incision on the planter surface of left hind paw in rats. Forty-eight rats were randomly divided into six groups: Sham group (Group C), control group (Group I,pretreatment with saline 5 ml), three tramadol pretreatment groups (Group T1, T10 and T20,pretreated with 1 mg/kg, 10 mg/kg and 20 mg/kg tramadol, respectively) and one tramadol treatment group (Group PT10, treated with tramadol 10 mg/kg immediately after operation). Pain behavior was assessed by withdrawal threshold to von Frey filament stimulation intensity, response latency of the hind paw to radiant thermal and a cumulative pain score 2 h after incision. Fos-positive neurons in spinal cord were identified by the immunohistochemical technique. Serum IL-6 levels were measured by enzyme-linked immunosorbent assay (ELISA).

RESULTSWithdrawIal threshold to von Frey filament stimulation intensity and response latency of the hind paw to radiant thermal in Group I were significantly lower than those in Group C (P<0.01). Cumulative pain score in Group I was significantly higher than that in Group C (P<0.01). In Groups of T10 and T20, withdrawal threshold to von Frey filament stimulation intensity and response latency of the hind paw to radiant thermal were significantly higher than those in Group I (P<0.01), cumulative pain score was significantly lower than that in Group I in a dose-dependent manner (P<0.01), and were also those in Group PT10. The greatest density of Fos-positive neurons was located in lamine I-II in Group I. Serum IL-6 levels were significantly elevated in Group I. Pretreatment with tramadol showed a dose-depended inhibitory effect on c-fos expression and serum IL-6 production,but not in Group T1. Administration of tramadol postoperatively also suppressed the c-fos expression and serum IL-6 production as showed in PT10 but were weaker than those in Group T10.

CONCLUSIONPretreatment with tramadol can produce dose-dependent inhibitory effect on c-fos expression in spinal cord dorsal horn and then suppress the inflammatory response to the trauma.

Analgesics, Opioid ; pharmacology ; therapeutic use ; Animals ; Interleukin-6 ; blood ; Male ; Pain Threshold ; drug effects ; Pain, Postoperative ; drug therapy ; metabolism ; Posterior Horn Cells ; drug effects ; metabolism ; Proto-Oncogene Proteins c-fos ; metabolism ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Tramadol ; pharmacology ; therapeutic use