To investigate the effect of compound Chinese traditional medicine PC-SPES II I in inhibiting proliferation of human prostate cancer cell LNCaP based on the androgen receptor (AR) signaling pathway. The effect of PC-SPES II on LNCaP cell proliferation was detected by MTT assay. According to the findings, at the mass concentration of 180-1 440 mg x L(-1), PC-SPES II significantly inhibited the proliferation of LNCaP cells; the IC50 of PC-SPES II at 24 h and 48 h were 311.48, 199.01 mg x L(-1), respectively. The flow Cytometry detection showed 240 mg x L(-1) PC-SPES II arrested cells in G2/M phase, and an obvious apoptotic peak appeared before G0/G1 peak and rose over time. Meanwhile, Hoechst 33258 staining revealed apoptotic cellular morphology. Annexin V-FITC/PI staining manifested an increase in apoptotic cell ratio at the PC-SPES II concentration of 480 mg x L(-1) in a dose dependent manner. The prostate specific antigen (PSA) secretion of LNCaP cells was tested by PSA ELISA kit. Besides, compared with 25 mg x L(-1) Bic, 480 mg x L(-1) PC-SPES II significantly reduced the cell secretion of PSA. The AR and PSA mRNA and protein expressions were detected by qRT-PCR and Western blot. According to the results, after the induction of LNCaP cells with synthetic androgen 25 μg x L(-1) R1881, 240-480 mg x L(-1) PC-SPES II notably down-regulated the AR and PSA mRNA and protein expressions and inhibited the translocation of AR from cytoplasm to nucleus. In summary, PC-SPES II significantly can inhibit the in vitro proliferation of LNCaP cells and arrest cell cycle arrest in G2/M phase. Its mechanism may be associated with the down-regulation of the AR and PSA expressions and the inhibition of AR nuclear translocation.
Antineoplastic Agents, Phytogenic ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Drugs, Chinese Herbal ; pharmacology ; Humans ; Male ; Prostate-Specific Antigen ; genetics ; metabolism ; Prostatic Neoplasms ; drug therapy ; genetics ; metabolism ; physiopathology ; Receptors, Androgen ; genetics ; metabolism ; Signal Transduction ; drug effects

[Objective]To explore the intracellular antimicrobial activities of erythromycin,ciprofloxacin,levofloxacin,moxifloxacin against Legionella pneumophila.[Methods]The minimum inhibition concentration(MIC)of each antibiotic was evaluated by E-test method and microdilution method respectively.The minimal extracellular concentration inhibiting intracellular multiplication(MIEC)of each antibiotic was evaluated by the MTT colorimetric assay system.[Results]The MIC concentration for each drug by E-test method were:erythromycin,0.047 μg/mL;ciprofloxacin,0.38 μg/mL;levofloxacin,0.125 μg/mL;moxifloxacin,0.125 μg/mL,the MIC concentrations for each drug by microdilution method were:erythromycin,0.125 μg/mL;ciprofloxacin,0.03 μg/mL;levofloxacin,0.016 μg/mL;moxifloxacin,0.016 μg/mL.The MIEC concentration for each drug were:erythromycin,0.25 μg/mL;ciprofloxacin,0.016 μg/mL;levofloxacin,0.016 μg/mL;moxifloxacin,0.004 μg/mL.[Conclusions]Fluoroquinolones have superior activity than erythromycin in U937 cells infected with L.pneumophila.Moxifloxacin is the most potent drug among the four tested antimicrobials.Our results indicated that the MTT assay system allows comparative and quantitative evaluations of the intracellular activities of antibiotics against L,pneumophila and efficient processing of a large number of samples.

Objective To explore the risk factors in elderly type 2 diabetes mellitus with cerebral infarction. Methods Retrospective investigarion was performed on 148 elderly hospitalized patients with type 2 diabetes.The patients were classified based on the presence or absence of cerebral infarction and compared with 60 controls.Logis- tic regression analysis was used to reveal the risk factors for cerebral infarction.Results The levels of systolic blood pressure(SBP),body mass index (BMI),fasting blood glucose (FBG),total cholesterol (TC),triglyceride (TG) and plasma fibrinogen(Fg) were higher in the patients with cerebral infarction[141.15?17.46)mmHg,(23.81?3.53)kg/m~2,(8.82?2.81)mmol/L,(5.69?1.15)mmol/L,(2.08?0.75)mmol/L and (4.08?0.65)g/L] than those without cerebral infarction[(129.78?14.65) mmHg,(22.18?3.22)kg/m~2,(7.06?1.72 )mmol/L,(5.09?1.12)mmol/L,(1.62?0.43)mmol/L and (3.48?0.58)g/L].The logistic analysis showed COUR,SBP,FBG, TC,TG and Fg were the independent risk factors for cerebral infarction.Conclusion Early intervention of the inde- pendent risk factors including SBP,FBG,TC,TG and Fg in elderly patients with type 2 diabetes was important for reduction and postponement of cerebral infarction.

Objective To study the relationship between the levels of uric acid in type 2 diabetic patients aged over forty years and lower extremity arterial disease(LEAD).Methods Lower extremities of 212 patients with type 2 diabetes were detected by high resolution color Doppler ultrasonography,and the levels of uric acid,fasting blood glucose and serum lipid were examined,which were applied to anylaze the relationship with diversity process of lower extremity arterial disease.Results The uric acid,low-density lipoproteins cholesterol(LDL-C),body mass in- dex(BMI),age and course in lower extremity arterial disease group was significantly higher than those without LEAD group(P

Objective: To observe the clinical efficacy of moxibustion therapy plus Liu's pediatric massage (tuina) for children with recurrent respiratory tract infections due to qi deficiency of spleen and lung. Methods: A total of 60 children who met the inclusion criteria were divided into an observation group and a control group according to the visiting sequence, with 30 cases in each group. Children in the observation group were treated with moxibustion therapy plus Liu's pediatric massage, and those in the control group were treated with Liu's pediatric massage alone. The incidence of respiratory tract infections and traditional Chinese medicine (TCM) symptoms score were observed and recorded in both groups before and after treatment. And the clinical efficacy was compared between the two groups. Results: The total effective rate of the observation group was 93.3％, and that of the control group was 83.3％. The difference between the two groups was statistically significant (P<0.05). After treatment, the TCM symptoms score and total times of infections in both groups were all statistically different from those before treatment (all P<0.05). The differences in TCM symptoms score and infection frequency before and after treatment in the observation group were statistically different from those in the control group (both P<0.05). Conclusion: Moxibustion therapy plus Liu's pediatric massage has a better effect in improving the clinical symptoms and reducing the frequency of respiratory tract infections for children with recurrent respiratory tract infections due to qi deficiency of spleen and lung than the pediatric massage alone.

Mesaconitine was incubated with rat liver microsomes in vitro. The metabolites of mesaconitine in rat liver microsomes were identified by ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method with high resolution power. A typical reaction mixture of 100 mol L-1 Tris-HCI buffer (pH 7.4) containing 0.5 gL-1 microsomal protein and 50 micro molL-1 mesaconitine was prepared. The above reaction mixture was divided into six groups, and the volume of each group was 200 micro L. The incubation mixture was pre-incubated at 37 degrees C for 2 min and the reactions were initiated by adding NADPH generating system. After 90 min incubation at 37 degrees C, 200 micro L of acetonitrile was added to each group to stop the reaction. The metabolites of mesaconitine were investigated by UPLC-MS/MS method. Mesaconitine and 6 metabolites M1-M6 were found in the incubation system. The structures were characterized according to the data from MS/MS spectra and literatures. The metabolic reactions of mesaconitine in rat liver microsomes included the demethylation, deacetylation, dehydrogenation and hydroxylation. The major metabolic pathways of mesaconitine in rat liver microsomes were determined by UPLC-MS/MS on multiple reaction monitoring (MRM) mode combined with specific inhibitors of cytochrome P450 (CYP) isoforms, including alpha-naphthoflavone (CYP1A2), quinine (CYP2D), diethyldithiocarbamate (CYP2E1), ketoconazole (CYP3A) and sulfaphenazole (CYP2C), separately. Mesaconitine was mainly metabolized by CYP3A. CYP2C and CYP2D were also more important CYP isoforms for the metabolism reactions of mesaconitine, but CYP1A2 and CYP2E1 haven't any contribution to MA metabolism in rat liver microsomes.
Aconitine ; analogs & derivatives ; metabolism ; Animals ; Chromatography, High Pressure Liquid ; Cytochrome P-450 CYP3A ; metabolism ; Cytochrome P-450 CYP3A Inhibitors ; Cytochrome P-450 Enzyme Inhibitors ; Cytochrome P-450 Enzyme System ; metabolism ; Enzyme Inhibitors ; pharmacology ; Ketoconazole ; pharmacology ; Male ; Metabolic Networks and Pathways ; Microsomes, Liver ; enzymology ; metabolism ; Quinine ; pharmacology ; Rats ; Rats, Sprague-Dawley ; Sulfaphenazole ; pharmacology ; Tandem Mass Spectrometry

Objective To evaluate the relationship between carotid atherosclerotic plaques stability and the clinical symptoms of carotid atherosclerosis by contrast-enhanced ultrasonography. Methods Fifty patients with carotid atherosclerotic plaques were examed with contrast-enhanced ultrasonography,the contrast agent visualization of the carotid atherosclerotic plques were analyzed and compared with their clinical symptoms. Results Twenty-three patients who suffered from obvious clinical symptom were entirely visualized. Twenty-weven patients had not apparent clinical symptom,of these patients,15 were sparse visualized,there was no visualization in other 12 patients. Conclusions Conlrast enhanced ultrasonography can real-time observe microcirculation in carotid atherosclerotic piques,and assess the stability of carotid atherosclerotic plaques.

Objective: To explore the points selection pattern of acupuncture for sleep apnea syndromes by data mining technique. Methods: Clinical literature about acupuncture therapy for sleep apnea syndromes was derived from China National Knowledge Infrastructure (CNKI), Wanfang Academic Journal Full-text Database (Wanfang), Chongqing VIP Database (CQVIP), PubMed and Science Direct between the time that databases were created and March 25th,2017. Relevant excel database was established and descriptive studies and association rules were analyzed. Results: The most frequently used point was Lianquan (CV 23) and the most frequently used meridian was the Stomach Meridian. The analysis of association rules showed that the clinical choice of acupuncture points was highly correlated, among which the combination of the highest degree of confidence and the highest degree of support was Shenmen (HT 7) and Sishencong (EX-HN 1); Lieque (LU 7), lianquan (CV 23) and Zhaohai (KI 6). Conclusion: Acupuncture treatment of sleep apnea syndromes has specific selection rules of points, providing certain references for clinical and scientific research.

Objective To study the pathological characteristics of skeletal muscle in patients with polymyalgia rheumatica(PMR).Methods Thirteen patients were diagnosed PMR according to the diagnostic criteria described by Bird in 1979.The onset of disease was between 49-78 years of age (median 60.3 years).All of them showed continuous symmetric myalgia with markedly elevated erythrocyte sedimentation rate(ESR).Five patients had mild fever and 8 patients had elevated C-reactive protein(CRP).Electromyogram(EMG)showed myogenic pattern in 2 patients.Only 1 patient showed anemia and 2 patients had mild elevated creatinine phosphokinase.None of them showed evidence of temporal arteritis.Biceps brachii muscle biopsies were performed in all patients before corticosteroid therapy.Results The typeⅡmuscle fiber atrophy was observed in all patients.Moth-eaten changes appeared in 8 cases,increased intramuscular lipid drops in 8 cases and ragged red fibers(RRF)in 3 cases of them.After steroid therapy,all patients showed improvement of myalgia and normal ESR as well as CRP.Conclusions The main symptoms of the patients are myalgia and abnormal ESR.Some patients have high level of CRP and abnormal EMG.Anemia and temporal arteritis are less frequent.The main myopathological changes were typeⅡmuscle fiber atrophy.Some patients have moth-eaten changes.More lipid drops and RRF indicate abnormal metabolism of skeletal muscle.

Objective:To analyze the clinical characteristics that affect the early outcomes of the elderly patients with transient ischemic attack(TIA) and provide the guidance for the prediction of disease recurrence.Methods:From January 2016 to December 2019, 315 TIA patients over 60 years old based on the time-clinical definition who were admitted to the department of neurology in Beijing Shijitan Hospital were divided into recurrence cerebrovascular events group(RCVEs group) and non-recurrence cerebrovascular events group(non-RCVEs group) according to the recurrence at 1 month after onset. The clinical characteristics of the two groups were compared by Logsitic regression analysis.Results:There were 29 cases in the RCVEs group and 286 cases in the non-RCVEs group. Compared to the non-RCVEs group, patients in RCVEs group were more likely have higher prevalence of hypertension history(14/15, 83/203), moderate or severe intracranial artery stenosis(21/8, 132/154), carotid stenosis(22/7, 107/179), DWI positive, motor symptoms, carotid artery stenting and higher times of TIA episodes(2(2, 3), 2(1, 2)), fasting blood glucose and glycosylated hemoglobin levels(8.86(8.17, 9.56)mmol/L, 5.82(5.27, 6.33)mmol/L). Logistic regression analysis showed that patients in RCVEs group had a DWI positive( B=1.634, OR=5.124, 95% CI: 2.898-9.059, P=0.000) and higher prevalence of moderate to severe stenosis of carotid artery( B=0.572, OR=1.773, 95% CI: 1.050-2.993, P=0.032). Conclusion:DWI positive and moderate to severe carotid stenosis may influence the early poor prognosis in patients with TIA.