Adenosine receptors (AR) play an important role in the regulation processes for body temperature and vigilance states. During our previous studies, we noticed that aminophylline (a non-selective, blood-brain-barrier penetrably AR antagonist) could attenuate the effects of YZG-330 [(2R,3S,4R,5R)-2-(hydroxymethyl-5-(6-(((R)-1-phenylpropyl)amino)-9H-purin-9-yl)tetrahydrofuran-3, 4-diol] on lowering the body temperature. Hereby, we focused ourselves on the character of thermal regulation effect of YZG-330 in mice and tried to specify the receptor subtype via giving typical adenosine receptor antagonists. The results showed that both of the magnitude and lasting time of the effect that YZG-330 played on decreasing body temperature are in a dose-dependent manner: within the next 3 hour after intragastric administration (ig) of 0.25, 1 or 4 mg . kg-1 YZG-330, the extreme values on body temperature decreasing were (1.2 ± 0.3) °C, (3.6 ± 0.4) °C (P<0.001) and (7.4±0.5) °C (P<0.001), separately; whereas the duration that body temperature below 34 °C were 0, (10±5) and (153±4) min, separately. Adenosine A1 receptor (A1R) antagonist (DPCPX) could effectively reverse YZG-330's effect on decreasing body temperature, with intraperitoneal administration of DPCPX (5 mg . kg-1) 20 min prior than YZG-330 (4 mg.kg-1, ig), the extreme value on body temperature decreasing was (3.5 ± 0.7) °C (P<0.001), the duration that body temperature below 34 °C was (8±6) min (P<0.001). However, adenosine A2a receptor antagonist, SCH-58261, did not show any influence on the effects of YZG-330 at all. Combined with the fact that 8-SPT (a non-selective, blood-brain-barrier impenetrably AR antagonist) did not reverse the effect of YZG-330, we come to the conclusion that central-adenosine A, receptor plays a significant role on the thermal regulation effect of YZG-330.

Object To isolate and identify the biflavonoids from the stem bark of Daphne giraldii Nitsche. Methods The flavonoids were isolated and purified by column chromatography on silica gel and Sephadex LH-20. Their structures were determined by spectroscopic methods, including IR, 1HNMR, 13 CNMR, HMBC and FAB-MS.Results Four biflavonoids daphnodorins A-D 1 (Ⅰ-Ⅳ) were isolated from the stem bark of D. giraldii. Conclusion The above four biflavonoids were isolated from the title plant only.

Objective To study the chemical constituents from the stem bark of Daphne giraldii. MethodsThe chemical constituents in the alcoholic extract from the stem bark of D. giraldii were isola-ted and purified using liquid/liquid extraction and silica gel column chromatography. The structures of the isolated compounds were determined on the basis of NMR, and mass spectra. ResultsSeven compounds were isolated from the alcohol extract. Their structures were identified as E-octadecyl caffeinate (Ⅰ), (+)-nortrachelogenin (Ⅱ), daphnoretin (Ⅲ), daphneticin (Ⅳ), 7, 8-dihydroxy coumarin (Ⅴ), 7-hydroxy coumarin (Ⅵ), and luteolin (Ⅶ) on the basis of 1H-NMR, 13C-NMR, and MS. ConclusionCompound Ⅰ is a new one. Compounds Ⅱ, Ⅳ, and Ⅶ are isolated from the title plant for the first time.

By using a combination of various chromatographic techniques including column chromatography over silica gel and Pharmadex LH-20 and reversed-phase HPLC, two minor new compounds, labda-12, 14-dien-6beta, 7alpha, 8beta, 17-tetraol (1), 2, 3-cis-6-acetyl-5-hydroxy-2-(hydroxymethylvinyl)-2, 3-dihydrobenzofuran-3-ol angelate (2), and a minor new natural product 6-methoxy-4-methyl-3, 4-dihydro-2H-naphthalen-1-one (3) have been isolated from an ethanolic extract of Heteroplexis micocephala. Their structures were elucidated with spectroscopic data analysis including 2D NMR experiments.

This study is to investigate the effect of compound B2 on the damage of PC12 cells induced by serum deprivation and to explore its related mechanisms. The binding characteristics of B2 to rat striatum adenosine A2A receptor was studied by radioligand 3H-MSX-2 binding assay. Cell viability was detected by MTT assay. ROS formation was measured after DCFDA fluorescent staining. B2 has affinity to rat adenosine A2A receptor (K1 = 0.37 micromol x L(-1)). B2 remarkably increased PC12 cell survival rate in serum deprivation-induced PC12 cells. The percentage of serum deprivation-induced death of PC12 was 49.6%, and the treatment of B2 (0.1-100 micromol x L(-1)) increased the cell viability to 63.3%, 74.9%, 86.3% and 88.1%, respectively. Adenosine A2A receptor antagonist SCH 58261 could significantly block the protective effect of B2. The cell viability with 0.1 micromol x L(-1) SCH 58261 decreased by 16.1%, 24.0% and 19.8%, in the presence of B2 (0.1-10 micromol x L(-1)). Serum deprivation-induced ROS formation was 3.5 times more than that of control group, and treatment with B2 significantly and dose-dependently inhibited ROS over-formation. The protective effect of B2 may be related with adenosine A2A receptor. Decrease of serum-deprivation induced ROS formation may also be one of the mechanisms.

Ten compounds were isolated from the 70% ethanol extract of linseed meal (Linum usitatissimum L) through a combination of various chromatographic techniques, including silica gel, macroporous adsorbent resin, Sephadex LH-20, and preparative HPLC. On the basis of spectroscopic data analysis, they were elucidated as 1-methylethyl-2-O-beta-D-glucopyranosyl-(1" --> 6')-beta-D-glucopyanoside (1), linustatin (2), neolinustatin (3), lotaustralin (4), linamarin (5), deoxyguanosine (6), deoxyadenosine (7), (+)-pinoresinol-4'-O-beta-D-glucopyranoside (8), 4-O-beta-D-glucopyranosylvanillyl alcohol (9) and tachioside (10), separately. Among them, compound 1 is a new compound, and compounds 6, 8 and 10 were isolated from the linseed meal for the first time.

Object To isolate and identiified the chemical constituents from the EtOAc soluble fraction of the rhizome of Semiliquidambar cathayensis Chang with anti inflammatory activity Methods The EtOAc soluble fraction of anti inflammatory activity was determined on the basis of the mouse ear irritant assay by croton oil The chemical constituents were isolated by silica gel column chromatography, and their structures were identiified by IR, MS and NMR spectroscopic methods including HMQC and HMBC experiments Results Four oleanolic acid derivatives, oleanolic acid, 3 oxo olean 12 en 28 oic acid 2?, 3? dihydroxyolean 12 en 28 oic acid, 2?, 3?, 23 trihydroxyolean 12 en 28 oic acid (arjunolic acid); three ellagic acid derivatives, ellagic acid 3, 3′ dimethylether, ellagic acid 3, 3′, 4 trimethylether, and ellagic acid 4 O ? D xylopyranoside 3, 3′ dimethylether, together with ? sitosterol and octadecylic acid were obtained and identified Conclusion All the nine compounds were isolated for the first time from the title plant

Objective To observe clinical curative effect of modified total cystectomy and Mainz Ⅱ neobladder. Methods Seventeen patients with bladder neoplasms were treated with modified total cystectomy and Mainz Ⅱ neobladder for urinary diversion. The paries posterior allantois with intestinum rectum and colon sigmoideum were taken 10 cm respectively, split the mesenterium edges, conduplicated and bilayer sutured from the junction of intestinum rectum and colon sigmoideum, bilateral ureters antireflux anastomosed respectively with colon sigmoideum and rectal papilla, then bilayer sutured paries anterior became Mainz allantois. Results There was no surgical mortality. The operative time was 340 ～ 420 mins (mean, 350 mins).Blood transfusion was 400 ～ 800 ml ( mean 600 ml). The follow-up was 4 ～ 18 months, urine and dejecta were shunt, uresis continence was fine and the operation had fewer severe complications. Conclusion Modified total cystectomy and Mainz Ⅱ neobladder to be an effective method for urinary diversion because of its simple operation, fewer severe complications, good uresis continence and high quality of life.

OBJECTIVETo study the chemical constituents of the red alga Acanthophora spicifera boergesen aiming at searching for bioactive leading compounds.

METHODCompounds were isolated by various chromatographic techniques including column chromatography over normal phase silica gel and Sephadex LH-20 gel and reverse phase HPLC as well as recrystallization. Their structures were determined by spectroscopic methods including IR, MS, 1D and 2D NMR techniques. MTT method was used for testing cytotoxicity of compounds against human cancer cell lines HCT-8, Bel-7402, BGC-823, A549 and HELA. Their inhibition against proliferation of dog vascular smooth muscle cells was also screened by MTT assay.

RESULTSix sterols were isolated from the ethanolic extract of the red alga Acanthophora spicifera. Their structures were identified as 6-hydroxycholest-4-ene-3-one (1), cholest-4-ene-3, 6-dione (2), cholest-5-ene-3 beta-ol (3), 5 alpha-cholestane-3, 6-dione (4), beta-sitosterol (5) and saringosterol (6).

CONCLUSIONCompounds 1-3 and 5 were obtained from this genus for the first time. Compounds 1, 2 and 4 showed moderate cytotoxic activity against human cancer cell lines.

Cell Line, Tumor ; Humans ; Inhibitory Concentration 50 ; Methanol ; chemistry ; Rhodophyta ; chemistry ; Sterols ; isolation & purification ; pharmacology

OBJECTIVETo develop a high performance liquid chromatography method for simultaneous determination of tour active constituents, dactylorhin B, loroglossin, dactylorhin A, militarine present in a Tibetan herb Gymnadenia conopsea.

METHODThe analysiswas achieved on a Pravil C18 column (4.6 mm x 150 mm, 5 microm) eluted with the mobile phases of methanol (A)-water (B) in gradient elution. The initial condition was 15% A, chsnhrf to 20% A in 10 min, to 45% A in 10 min, to 70% A in 15 min. The detection wavelength was set at 222 nm. The flow rate was 0.7 mL x min(-1). Orthogonal test was adopted to optimize extraction process of four active compounds from Gymnadenia conopsea.

RESULTThe assay displayed good linearity over the concentration ranges of 0.20-4.05 microg (r = 0.9999), 0.10-5.11 micro g (r = 0.9999), 0.10-5.11 microg (r = 0.9999) and 0.09-1.79 microg (r = 0.9999), respectively. The average recoveries (n=9) were 99.19%, 99.16%, 99.52% and 99.00% for dactylorhin B, loroglossin, dactylorhin A and militarine respectively.

CONCLUSIONThe method is simple, sensitive, reliable and reproducible which can be used for the quality study of Gymnadenia conopsea.

Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; analysis ; Orchidaceae ; chemistry