Azacitidine ; analogs & derivatives ; therapeutic use ; Clinical Trials, Phase III as Topic ; Humans ; Leukemia, Myeloid, Acute ; drug therapy ; Multicenter Studies as Topic

A strain no.H5 isolated from Rhizophora stylosa Griff in Zhanjiang had a good antagonistic activity against Aspergillus niger,pathogen of Dracaena Sanderiana black-rot disease.It was identified as Bacillus licheniformis.Dual culture,mycelium growth rate and inhibitory zones were used to test the effect. Strong inhibition was shown against A.niger.Inhibitory ratios of H5 germ-free fermented filtrate on mycelium growth and conidial germination were 91.9%and 100%respectively.In addition,mycelia on the edge of antagonistic band became abnormal and over-branching.Meanwhile,a lot of vesicles appeared on the surface.When treated with heat,acid and alkali,the filtration of H5 was always with stable activity.Precipitate in 55%saturated ammonium sulfate dissolved in phosphate buffer solution maintained most of the activity after high pressure steam sterilization for 25 minutes.It was preliminarily considered as a kind of heat resistant protein.

OBJECTIVETo observe the effect of Fengshi No. 1 (FS1) in treating patients with active stage of rheumatoid arthritis (RA).

METHODSPatients with RA were randomly divided into two groups, the 40 patients in the treated group were treated with combined therapy of methotrexate (MTX), sulfasalazine (SSZ) and FS1, and the 20 in the control groups were treated with MTX and SSZ alone.

RESULTSIn the treated group, the total effective rate was 97.5%, the clinical controlled and markedly effective rate 95.0% and the occurrence rate of side-toxic reaction 10.0%, as compared with those in the control group, 60.0%, 20.0% and 45.0% respectively, the difference was significant (chi 2 = 11.91, 32.23 and 7.67 respectively, all P < 0.01). The effect in the treated group was superior to that in the control group in abating joint swelling and pain, improving function of joint, reducing immune indices and ameliorating iconographic features (P < 0.01 or P < 0.05).

CONCLUSIONFS1 not only has the effects of anti-inflammation, analgesis, regulating immune reaction, but also could retard the occurring of bone destruction, reduce the toxic-side effects of MTX and SSZ.

Adult ; Aged ; Anti-Inflammatory Agents, Non-Steroidal ; therapeutic use ; Arthritis, Rheumatoid ; drug therapy ; Drug Therapy, Combination ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Humans ; Male ; Methotrexate ; therapeutic use ; Middle Aged ; Phytotherapy ; Sulfasalazine ; therapeutic use

Pancreatic ductal adenocarcinoma (PDAC) is one of the five most malignant cancer. ZX-1201 is one of the active constituents in Alismatis Rhizoma,a well-known traditional Chinese medi-cine with a wide variety of pharmacological properties including diuretic,anti-hyperlipidemic,anti-atheroscle-rotic,anti-cancer,anti-inflammatory and anti-oxidative activities.We investigated the inhibitory effect of ZX-1201 on pancreatic cancer and the relevant molecular mechanism in vitro and in vivo. ZX-1201 inhibited the growth and metastasis of PANC-1 cells in BALB/c nude mice significantly.ZX-1201 inhibited the function of AQP1 via directly interaction and involved in the reversion process of ZX-1201 on TGF-β1. CTGF was an important protein in the reversion process of ZX-1201 on TGF-β1.ZX-1201 inhibited the migration of PANC-1 and CPFAC-1 cells induced by TGF-β1in vitro.ZX-1201 reversed the down-regu-lated of epithelial markers and up-regulated of mesenchymal markers, as well as the up-regulated of Snail and p-Smad2/3 induced by TGF-β1.And ZX-1201 reversed Epithelial-Mesenchymal Transition by down-regulating AQP1 and inhibiting translocation of β-catenin, the promotor of CTGF. According to these,ZX-1201 inhibited the migration of pancreatic cancer cells.We concluded that ZX-1201 inhibited the growth and metastasis of PANC-1 cells in vivo significantly.And AQP1,β-catenin and CTGF were the pivotal proteins in the process of ZX-1201 inhibiting PANC-1 cells migration induced by TGF-β1.

Objective To evaluate the myocardial blood supply in patients with metabolic syndrome (MS) using 99Tcm-MIBI SPECT MPI. Methods A total of 342 patients were divided into four groups according to the number of abnormal metabolic indices: no abnormal metabolic index (Group 1), one abnormal index (Group 2), two abnormal indices (Group 3), three or more abnormal indices (Group 4). Each patient underwent two-day protocol of gated stress and rest 99Tcm-MIBI MPI. One hundred and three of the 342 patients were clinically diagnosed as MS and underwent CAG within 1 month after MPI. χ2test was used to evaluate the difference among the four groups and Kappa test to analyze the correlation between MPI and CAG. Results Compared with CAG, the diagnostic sensitivity, specificity, positive and negative predictive values by 99Tcm-MIBI SPECT MPI for coronary artery diseases (CAD) in 103 MS patients were 80.5% (33/41), 85.5% (53/62), 78.6% (33/42) and 86.9% (53/61), respectively. The correlation coefficient between MPI and CAG was 0.657 (P<0.001). The abnormal MPI rates in group 1, 2, 3 and 4 were 23.3% (10/43), 32.9% (26/79), 54.4% (56/103), and 57.3% (67/117), respectively (χ2=23.22, P<0.001). Conclusions In MS patients,99Tcm-MIBI SPECT MPI can be useful for evaluating myocardial blood supply and the myocardial ischemia rates may correlate positively with the number of abnormal metabolic indices.

In order to clarify the metabolism pathways of scandoside methyl ester, the analysis of metabolites profiling in four kinds of liver microsomes was performed by using an ultra-performance liquid chromatography/ electrospray-tandem mass spectrometry (UPLC-ESI-MS). The data obtained from the 0 h-incubation and the 2 h-incubation were compared and analyzed. After incubation, 5 metabolites of scandoside methyl ester were found in rat, Beagles, rhesus monkey and human liver microsome. The results showed that scandoside methyl ester's major metabolic pathway in the liver microsomes is hydrolysis, oxidation and reduction reactions, and there are certain kinds differences between species. The study provides a research base for further research about iridoid compounds in vivo metabolic pathways.

Three new compounds, including a naphthoquinone, a reduced naphthoquinone derivative naphthalenone, and a tricarboxylic acid, along with five known naphthalenone derivatives were isolated from ethyl acetate extract of rice fermentation products of the fungus Pleosporales sp. by multiple column chromatographic methods, including Sephadex LH-20 gel column chromatography, silica gel column chromatography, reversed-phase HPLC, and chiral chromatography. Their structures were elucidated by MS, NMR, and specific rotation spectroscopic analyses as well as ECD calculations. Three novel compounds were named as pleospathone A (1), pleospathone B (2), and pleosporalic acid A (3). Five known compounds were separately identified as (3S,4R)-3,4,8-trihydroxy-6-methyl-3,4-dihydronaphthalen-1(2H)-one (4), (4R)-3,4-dihydro-4,6,8-trihydroxy-1(2H)-naphthalenone (5), (-)-scytalone (6), (3S,4S)-3,4-dihydro-3,4,6,8-tetrahydroxy-1(2H)-naphthalenone (7), and cis-4-hydroxyscytalone (8). Compounds 4-8 were isolated from the Pleosporales fungi for the first time. Compound 1 shows inhibitory activities against human cervical carcinoma cell line HeLa and murine leukemia cell line P388 with the IC₅₀ values of 78.93 and 98.80 μmol·L^-1, respectively.

Objective To evaluate the efficacy of intra-arterial hrombolytic therapy in patients with acute ischemic stroke having their time window over 3 h and analyze its influencing factors.Methods Sixteen patients with acute ischemic stroke having their time window over 3 h, admitted to Department of Neuroradiology of Central Hospital of Nancy University from January 2008 to January 2009, were treated by intra-arterial thrombolysis using chemical (rt-PA) and mechanical technique. These patients had carotid stroke for less than 3 h, vertebrobasilar stroke for less than 24 h or coma for less than 6 h. According to the images of DSA, the recanalization after thrombolysis was evaluated by thrombolysis in cerebral infarction (TICI) grades. CT scans 24 h after thrombolysis were operated to detect the hemorrhage complications. NIHSS at baseline and 24 h after thrombolysis and modified Rankin Scale (mRS) were recorded to evaluate the clinical efficacy. Results After intra-arterial thrombolysis, 7 (43.75%) in 16 patients got totally recanalization (TICI grade 3), another 7 partial recanalization (TICI grade 2), and the left 2 patients failed in recanalization (TICI grade 1); the total recanalization rate was 87.5%. A significant reduction of NIHSS scores after the thrombolysis was noted as compared with that before the thrombolysis. The atients with occlusion of anterior ciculation having time window over 5 h enjoyed no reduction of NIHSS scores after thrombolysis; mRS scores in patients having time window over 5 h were ignificantly higher as compared with those in patients having time window less than 5 h.The patients having ICA occlusion (n=5) had no reduction of NIHSS scores after thrombolysis, and enjoyed poorer prognosis as compared with whose occlusion lay in the middle cerebral artery (MCA,n=9) and basilar artery (BA, n=2). By CT scan 24 h after thrombolysis, 4 patients were detected with symptomatic intra cerebral hemorrhage (ICH, 25%) and all of them with occlusion in the internal carotid artery system: 1 patient with occlusion in MCA died of cerebral hernia causing by the large hematoma;the other 3 were all occlusion in ICA. Although reocclusion after thrombolysis occurred, 1 patient was benefitted from the affluent collateral perfusion and got a good prognosis. Conclusion For patientswith BA and MCA occlusion having time window over 3 h, intra-arterial thrombolytic therapy is effective and selective resulting from their high recanalization rate, improvement of neurological function and clinical end. The therapy should be individually chosen; mutiple factors as time window of stroke,location of stroke, ompensatory circulation and complications should be considered in evaluating the efficacy; and the hemorrhage complications should be avoided.

Objective :To study influence of amlodipine combined valsartan on autonomic nervous function and serum level of Rho‐associated protein kinase 1 (ROCK1) in hypertensive patients with renal injury .Methods :A total of 94 hypertensive patients with renal injury treated in our hospital were selected ,randomly and equally divided into amlo‐dipine group and combined treatment group (received amlodipine combined valsartan ) ,both groups were treated for one month .Serum ROCK1 level and autonomic nervous function indexes before and after treatment ,therapeutic effect and incidence of adverse reactions were analyzed and compared between two groups .Results :After treat‐ment ,total effective rate of combined treatment group was significantly higher than that of amlodipine group (95. 74% vs.82.97%,P＝0. 045).Compared with before treatment ,after treatment ,there were significant reduc‐tions in serum ROCK1 level [amlodipine group : (3. 25 ± 0.32 ) ng／ml vs.(1.24 ± 0. 45 ) ng／ml ,combined treat‐ment group :(3. 34 ± 0. 35) ng／ml vs.(0.22 ± 0.15 ) ng／ml] ,24hSBP standard deviation (24hSSD) ,24h DBP SD (24hDSD) ,daytime SBP SD (dSSD) ,nighttime SBP SD (nSSD) and nDSD in two groups ( P＝0.001 all) ,and a‐bove indexes of combined treatment group were significantly lower than those of amlodipine group , P＜ 0. 01 all. Compared with amlodipine group after treatment ,there were significant reductions in incidence rates of lower limb edema (27. 66% vs.10.63%) ,nausea and vomiting (27. 66% vs.8.51%) and dizziness and weakness (23. 40% vs. 8.51%) in combined treatment group ,P＜0. 05 all.Conclusion :Amlodipine combined valsartan possesses significant therapeutic effect on hypertensive patients with renal injury .It can significantly reduce serum ROCK1 level and im‐prove autonomic nervous function and prognosis in these patients .

Objective To observe the effect of underwater treadmill training on patients with incomplete spinal cord injury (SCI).Methods 11 patients with incomplete SCI were treated with underwater treadmill training, besides other comprehensive rehabilitation. Motor and sense scores were assessed using ASIA2000 standard and recorded before and after the underwater treadmill training. Walking distances, maximal walking velocity when training and changes of activities of daily living (ADL) before and after training were also recorded.Results After underwater treadmill training, the sense score of ASIA increased ( P<0.05), motor score of ASIA, and scores of walking distance, maximal walking velocity and ADL increased significantly ( P<0.01).Conclusion The underwater treadmill training along with other routine rehabilitation treatment may be helpful to improve motor and sensory functions and ADL of patients with incomplete SCI.