贵州十大功劳提取物异汉防己甲素对106例尘肺的疗效观察

报告用贵州中草药十大功劳提取物异汉防己甲素，在取得实验性矽肺良好效果的基础上，在省劳研所对１０６例尘肺（含矽肺、炭黑尘肺）患者进行了临床疗效观察，结果证明临床症状有不同程度好转，ｘ线胸片较治疗前好转，稳定率为１２．１％，７７．１％，铜蓝蛋白治疗后低于治疗前（Ｐ＜０．０５），有显著性差异，同时毒副反应少，说明本品是一较好的抗矽药，值得推广。

Molecular Epidemiology of Oxacillin-resistant Staphylococcus aureus and in vitro Activity of Glycopeptides against Staphylococcus species

The purpose of this subject was to investigate molecular epidemiology of oxacillin-resistant Staphylococcus aureus (MRSA) isolated from hospitalized patients, and to survey the in vitro activity of teicoplanin, vancomycin and other 9 antibiotics against Staphylococcus species . MRSA were detected by oxacillin-NaCl-containing screen agar. The homology of nosocomial MRSA from ICU and RCU was determined by pulse-field gel electrophoresis. Agar diffusion, E test and agar dilution were used to compare the in vitro activity of teicoplanin and vancomycin against Staphylococcus spp from 2001 to 2003 at Peking Union Medical College Hospital. WHONET-5.3 software was used to analyze the antimicrobial susceptibility data. From 2001 to 2003, the prevalences of MRSA were 56.5%, 65.3%, 64.7%, respectively. PFGE found most of MRSA from ICU and RCU were closely related. All of S.aureus and S.epidimidis isolates were susceptible to teicoplanin and vancomycin from 2001 to 2003. However, 1 isolate of S.haemolyticus was resistant and 9 isolates intermediate to teicoplanin. The minimal inhibitory concentration of teicoplanin did not correlate well with zone diameter, when inoculum increased by 100 folds, the zone diameters of teicoplanin decreased more greatly than those of vancomycin. In 2002, severe outbreaks caused by MRSA strains had been found in ICU and RCU wards. Teicoplanin and vancomycin had good activity against clinical isolates of Staphylococci spp . Teicoplanin was less active than vancomycin against S.haemolyticus . Most of S.haemolyticus isolates were intermediate to teicoplanin. Antimicrobial susceptibility testing of teicoplanin was influenced by the diffusion speed in the agar and inoculum size.

Surface Modification of Polycarbonate Urethane by Covalent Linkage of Heparin with a PEG Spacer

Heparin was grafted onto polycarbonate urethane (PCU) surface via a three-step procedure utilizing α, ωdiamino-poly(ethylene glycol) (APEG, M n =2 000) as a spacer. In the first step, isocyanate functional groups were introduced onto PCU surface by the treatment of hexamethylene diisocyanate (HDI) in the presence of di-n-butyltin dilaurate (DBTDL) as a catalyst. In the second step, APEG was linked to the PCU surface to obtain the APEG conjugated PCU surface (PCU-APEG). In the third step, heparin was covalently coupled with PCU-APEG in the presence of N-hydroxysuccinimide (NHS) and 1-ethyl-3-(3-dimethylamidopropyl) carbodiimide (EDAC). The amount of heparin (1.639 μg/cm 2 ) covalently immobilized on the PCU-APEG surface was determined by the toluidine blue method. The modified surface was characterized by water contact angle, attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR), X-ray photoelectron spectroscopy (XPS), and atomic force microscopy (AFM). The hemocompatibility was preliminarily studied by platelet adhesion test. The results indicated that heparin was successfully grafted onto the PCU surface, and meanwhile the hydrophilicity and hemocompatibility of the modified PCU surface were improved significantly compared with the blank PCU surface.

Methoxyl methyl ether isoamylene quercetin, a quercetin derivative, protects rat aorta endothelial cells against oxidation and apoptosis

Methoxyl methyl ether isoamylene quercetin （MIAQ） is one of the newly synthesized quercetin derivatives. The present study investigated the effect of MIAQ on rat aorta endothelial cells （RAECs） injured by hydrogen peroxide （H2O2）, as well as the potential mechanisms. We observed that MIAQ at 2.5-10μmol/L significantly enhanced the viability of injured RAECs, and the effect was more potent than quercetin and ct-tocopherol. However, M1AQ at the same concentration failed to show anti-oxidant activity in a cell-free system. In H2O2-injured endothelial cells treated with MIAQ （5-10μmol/L）, the level of nitric oxide （NO） and malondialdehyde was decreased, and the activities of superoxide dismutase and glutathione peroxidase was enhanced. In addition, RAECs treated with MIAQ （2.5-10 μmol/L） exhibited significant inhibiting apoptosis. In conclusion, MIAQ had protective effect on RAECs, possibly through increasing NO production and antioxidases activities, as well as inhibiting apoptosis. These findings suggest that MIAQ is possibly beneficial in the prevention of atherosclerosis and other diseases related to endothelial injury.

Determination of 8,2′-diprenylquercetin 3-methyl ether in plasma by UPLC-MS-MS and its pharmacokinetic application in rats

8,2＇-Diprenylquercetin 3-methyl ether with significant anti-breast cancer activity is the main constituent of Tibetan medicine Sinopodophylli Fructus. In the present study, we developed and validated a rapid and sensitive ultra performance liquid chromatography-tandem mass spectrometry （UPLC-MS/MS） method for the determination of 8,2＇-diprenylquercetin 3-methyl ether in rat plasma. 8-Prenylkaempferol was used as the internal standard. The separation was carried out using Waters ACQUITY UPLC BEH C18 column （2.1 mm×100 ram, 1.7 μm） with a mobile phase consisting of acetonitrile and 0.1% formic acid in water on a gradient program at a flow rate of 0.4 mL＇min-1 and temperature of 30 ℃. Triple quadrupole mass spectrometric detection in negative ion mode was used for multiple-reaction monitoring of the transitions at m/z 451.30→177.25 and m/z 353.25→298.15 for 8,2＇-diprenylquercetin 3-methyl ether and 8-prenylkaempferol, respectively. The calibration curves were linear within the concentration range 0.1-2000 ng/mL （r = 0.9954）. The recoveries were 103%-115%, and the results were consistent across low, middle and high concentration levels. The intra- and inter-day precisions were within 15%, and the bias was between --6%-15%. This method was simple, rapid and sensitive, which could be applied to the determination of 8,2＇-diprenylquercetin 3-methyl ether in plasma and pharmacokinetic study in rats. Pharmacokinetic test indicated that the peak plasma concentration occurred in 2 h after the female rats were intragastrically administered with 8,2＇-diprenylquercetin 3-methyl ether at the dose of 100 mg/kg, and the biological half-life was 6.79 h. The blood drug concentration maintained equal amount for 20 h, which was conducive to the in vivo effects of drugs.