大鼠皮肤对驻极体外静电场的影响

目的：研究聚丙烯驻极体透过大鼠皮肤的表面电位衰减情况,探讨大鼠皮肤对驻极体外静电场的影响及静电场对大鼠皮肤的作用机理。为研制优质的驻极体透皮给药贴剂奠定实验基础。方法：利用栅控恒压电晕充电系统将单电极和双裸面聚丙烯薄膜制备成正、负极性的驻极体,借助于等温表面电位衰减测量研究不同极性驻极体透过大鼠皮肤的等效表面电位衰减规律。结果：（1）＋1000V注极的单电极和双裸面聚丙烯驻极体透过大鼠皮肤的表面电位经过48小时保留了其初始值的92．9％和71．3％。（2）-1000V注极的单电极和双裸面聚丙烯驻极体透过大鼠皮肤的表面电位经过48小时后分别衰减了20．7％和18．8％。（3）聚丙烯驻极体透皮电位在72小时内具有和驻极体自身相近的稳定性。结论：（1）单电极和双裸面聚丙烯驻极体均具有优异的电荷储存稳定性。（2）驻极体的表面电位能很好的透过大鼠皮肤．相比双裸面驻极体,单电极驻极体透过大鼠皮肤的表面电位更高、稳定性更好。驻极体作为一种新的物理调控因子和驱动源可用于透皮给药贴剂的研制。     

静电场调控p53合成对成纤维细胞增殖周期的影响*

目的：研究驻极体静电场调控p53 合成对成纤维细胞生长和增殖的影响。方法：将表面电位为0 的PP 膜设 为对照组,将表面电位为5 000 V 和-5 000 V 的驻极体分别设为5 000 V 驻极体组（5 000 V 组）和-5 000 V 驻极 体组（-5 000 V组）。采用常温等离子体放电系统将聚丙烯薄膜分别制成5 000 V驻极体和-5 000 V驻极体。将正 极性和负极性的驻极体分别作用于对数生长期的成纤维细胞48 h,借助于等效表面电位测量系统检测细胞生长环 境的静电场稳定性。通过CCK-8 实验研究正极性和负极性驻极体对成纤维细胞增殖能力的影响,并与对照组做 比较,通过流式细胞仪研究正极性和负极性驻极体对成纤维细胞生长周期的影响。通过实时荧光定量PCR研究在 静电场环境下生长的成纤维细胞中p53 mRNA的表达。结果：正极性和负极性的驻极体可提供稳定的静电场作用 于成纤维细胞。负极性驻极体使细胞快速通过G1期促进成纤维细胞的生长,而正极性驻极体通过阻断G1期抑制 成纤维细胞生长。经负极性驻极体作用,成纤维细胞中p53 mRNA的表达量较对照组明显减少;经正极性驻极体 作用,成纤维细胞中p53 mRNA 的表达量较对照组显著增加。结论：电场可引起成纤维细胞的细胞周期发生变化, 从而调控细胞的分化与增殖。负极性驻极体具有促进成纤维细胞的生长作用,正极性驻极体可抑制成纤维细胞生 长。驻极体产生的静电场通过调控细胞内p53 mRNA 的表达实现对成纤维细胞生长的调控。     

多孔聚四氟乙烯/明胶复合驻极体膜储电性能研究

目的：研究多孔聚四氟乙烯，明胶复合驻极体膜的电荷储存能力。方法：通过恒压电晕充电和常温极化方法将多孔聚四氟乙烯，明胶复合制备成驻极体复合膜，分成对照组，研究在不同环境下多孔聚四氟乙烯，明胶驻极体复合膜表面电位的变化。结果：（1）与电晕充电方法比较，常温极化制备的多孔聚四氟乙烯，明胶复合驻极体具有较高的表面电位和较好的电荷储存能力；（2）环境湿度严重影响多孔聚四氟乙烯，明胶复合驻极体膜的电荷储存稳定性，在RH=34％的存放条件下．复合膜具有良好的电荷储存稳定性。结论：多孔聚四氟乙烯，明胶复合驻极体可作为驱动源和药物载体用于体外透皮给药制剂的研究。     

无花果叶乙醇、水提取物抑菌作用的比较研究

目的研究无花果叶乙醇提取物和水提取物的抑菌作用。方法采用纸片法抑菌实验观察比较无花果叶乙醇提取物和水提取物对金黄色葡萄球菌、大肠杆菌和枯草杆菌的作用。结果生药含量为100mg/mL的无花果叶乙醇提取物对金黄色葡萄球菌、大肠杆菌、枯草杆菌3种抑菌环的直径均大于8mm,生药含量为144mg/mL的无花果叶水提取物对金黄色葡萄球菌、大肠杆菌、枯草杆菌3种抑菌环的直径均小于8mm。结论无花果叶乙醇提取物具有明显的抑菌作用,无花果叶水提取物无抑菌作用。     

驻极体对烫伤大鼠皮肤微血管壁通透性变化的影响

通过检测烫伤部位皮肤组织匀浆中荧光标记的白蛋白的含量，观察了大鼠烫伤６，１２和２４ｈ后皮肤微血管壁通透性的变化以及－１００，－２５０，－５００，－７５０和－１０００Ｖ驻极体对这种变化的影响。结果指出：（１）烫伤后１２ｈ，大鼠皮肤血管壁通透性明显高于对照组（Ｐ〈０．０１），－２５０，－５００和－７５０Ｖ驻极体治疗组大鼠的血管壁通透性明显低于烫伤组（Ｐ〈０．０５），－１０００Ｖ驻极体治疗组皮肤血管壁通     

负极性聚丙烯驻极体对糖尿病大鼠皮肤结构的影响

目的:研究负极性驻极体作用在糖尿病大鼠皮肤两侧静电场的稳定性及其对糖尿病大鼠皮肤组织结构的影响,探讨负极性驻极体透皮给药的机制。方法:利用电晕充电技术将聚丙烯薄膜制备成不同表面电位的负极性驻极体,以糖尿病大鼠为模型,借助等温表面电位衰减测量和光学显微镜,研究大鼠皮肤两侧电场的稳定性及驻极体对大鼠皮肤显微结构的影响。结果:-1 500 V驻极体作用糖尿病大鼠24 h,透过糖尿病大鼠皮肤的电位是其初始电位的68%,显示糖尿病大鼠皮肤能处于较稳定的外电场中;糖尿病大鼠皮肤的角质层和全皮随-1 500 V驻极体作用时间的延长而逐渐恢复,表皮层和真皮层细胞排列变得逐渐清晰,但排列仍较为松散,皮下脂肪组织萎缩部分恢复。结论:负极性驻极体能为糖尿病大鼠皮肤两侧提供一定大小的静电场;驻极体产生的静电场可改善糖尿病大鼠皮肤的显微结构,使糖尿病皮肤角质层和真皮层细胞排列疏松,有利于药物透过皮肤。     

负极性驻极体与5-氟尿嘧啶对大鼠创面愈合的影响

目的:比较不同表面电位的负极性驻极体与5-氟尿嘧啶(5-FU)对大鼠创面愈合的影响。方法:利用电晕充电技术与药剂学方法制备不同表面电位的负极性驻极体贴剂、5-FU贴剂、-2 000 V驻极体5-FU贴剂,借助等温表面电位测量、光学显微镜等手段,研究负极性驻极体贴剂与-2 000 V驻极体5-FU贴剂外静电场的稳定性以及上述三类贴剂对大鼠创面愈合的影响。结果:不同表面电位负极性驻极体贴剂与-2 000 V驻极体5-FU贴剂的等效表面电位随时间增加,均按指数规律衰减,能够给创面提供较为稳定的外静电场;不同表面电位负极性驻极体贴剂对创面愈合具有促进作用,而且等效表面电位越大,创面愈合越快;5-FU对创面愈合具有抑制作用,而将-2 000 V驻极体与5-FU联用可减轻5-FU对创面愈合的抑制作用。结论:负极性驻极体对创面愈合有促进作用,5-FU能延缓创面愈合,若合理利用两者,可以调控创面愈合和抑制增生性瘢痕生长。     

纳米银对金黄色葡萄球菌的抗菌作用及其机制研究

目的以金黄色葡萄球菌为对象,研究纳米银的抗菌作用,并对抗菌机制进行探讨。方法金黄色葡萄球菌(ATCC6538)、双倍浓度营养肉汤和营养肉汤由中国食品药品检定研究院提供;纳米银粉末(≤100 nm,576832-5G,SIGMA-ALORICH)。采用最小抑菌浓度(MIC)实验,测定纳米银对金黄色葡萄球菌的振荡培养时(转速为300 r/min)最小抑菌浓度值;采取烧瓶振荡法测定质量浓度50.00、100.00、200.00、800.00μg/m L纳米银对金黄色葡萄球菌作用的光密度(OD)值;扫描电子显微镜观察纳米银处理后金黄色葡萄球菌结构的变化。结果振荡培养时,纳米银对金黄色葡萄球菌的MIC值为800.00μg/m L;纳米银使金黄色葡萄球菌的延滞期延长,浓度800.00μg/m L纳米银溶液能够完全抑制金黄色葡萄球菌在肉汤培养液中的增殖生长;用50.00μg/m L的纳米银作用金黄色葡萄球菌4 h,电子显微镜结果显示,金黄色葡萄球菌细胞壁破裂、胞内物质外流及细胞的死亡。结论纳米银对金黄色葡萄球菌有抗菌作用,可能进入细菌细胞内造成其死亡。     

电极和栅压对聚丙烯驻极体电荷储存稳定性的影响

目的:比较研究不同栅压注极的双裸面聚丙烯驻极体的电荷储存稳定性,探讨铝电极对聚丙烯驻极体电荷储存稳定性的影响,为研制优质驻极体透皮贴剂奠定基础。方法:利用栅控恒压电晕充电系统将含单面镀铝电极和双裸面聚丙烯薄膜制备成不同表面电位的负极性驻极体,借助于等温表面电位衰减测量和开路热刺激放电电流谱研究注极栅压和金属电极对聚丙烯驻极体电荷储存稳定性的影响。结果:1.注极栅压越高,双裸面驻极体的电荷储存稳定性越差。2.双裸面聚丙烯驻极体较单面镀铝驻极体具有更高比例的深能级捕获电荷,具有优异的电荷储存稳定性。结论:双裸面聚丙烯驻极体具有优异的电荷储存能力可用于驻极体透皮贴剂的研制。     

秦皮素抑菌活性及其机制研究

目的以金黄色葡萄球菌为供试菌株来研究秦皮素对其的抑制活性及其机制。方法利用牛津杯法、2,3,5-氯化三苯基四氮唑(TTC)染色、生长曲线的测定、细胞膜渗透性测定、SDS-PAGE蛋白谱变化方法等对秦皮素的抑菌活性及其机制进行研究。结果秦皮素能够影响金黄色葡萄球菌细胞膜的通透性,秦皮素作用20 h,菌体可溶性蛋白总量减少55.74%。结论秦皮素对金黄色葡萄球菌具有明显的抑制作用,其抑菌机制可能是通过抑制蛋白质的合成来实现的。     

In vitro resistance to human platelet microbicidal protein among urethral staphylococcal and enterococcal isolates with its correlation with prostatitis

The study was carried out to test the in vitro activity of human platelet microbicidal protein (hPMP) on most commonly isolated urethral pathogens and compare the same with clinical isolates from cases of chronic prostatitis (CP). Urethral isolates of Staphylococcus aureus (n=19), coagulase negative staphylococci (n=40) and Enterococcus faecalis (n=16) from patients with or without CP were tested. The hPMP susceptibility of bacterial strains was determined by exposing bacterial cells to serial dilutions of hPMP. A significantly higher proportion of CP-strains of coagulase negative staphylococci (91.3% vs 5.88%) was resistant to hPMP than was that of non-CP strains (P S.aureus studied, 77.8% were considered resistant to the bactericidal action of hPMP. All nine CP-strains of E.faecalis were highly resistant to hPMP. Most non-CP urethral isolates of S.aureus, coagulase negative staphylococci and E.faecalis were susceptible to the bactericidal action of hPMP, while CP isolates of all species were significantly more resistant to hPMP. Data from the present study may have significant implications in understanding the pathogenesis of CP.     

驻极体促进狗股直肌移植后功能的恢复

本文用成年狗14条，随机分成对照组和驻极体治疗组，以狗的股直肌为实验模型，用TeflonFEP驻极体对失神经支配的移植肌肉的功能恢复作了研究，结果表明：应用驻极体后，移植肌肉的电生理指标明显优于对照组，新生动作电位提早出现，移植肌肉获得神经再支配的时间较对照组提前，驻极体具有促进神经再生，延缓移植肌萎缩，促进移植肌肉功能恢复的作用。     

Bactericidal activity and synergy studies of BAL9141, a novel pyrrolidinone-3-ylidenemethyl cephem, tested against streptococci, enterococci and methicillin-resistant staphylococci

BAL9141 has been reported to have inhibitory activity against methicillin-resistant Staphylococcus aureus (MRSA), many enterococci, and streptococci with various resistant patterns. BAL9141 potency was assessed by time–kill curves alone or with subinhibitory concentrations of gentamicin (MIC/4). BAL9141 exhibited bactericidal activity alone against all the streptococci and staphylococci. Among ampicillin-susceptible enterococci, BAL9141 was bactericidal against some strains, but no BAL9141 inhibition was observed of ampicillin-resistant Enterococcus faecium . The activity of BAL9141 with gentamicin was slightly enhanced (not synergy) or indifferent against staphylococci. BAL9141 demonstrated bactericidal action alone against Enterococcus faecalis and some E. faecium strains (− 4.8 to −6.0 log₁₀ CFU/mL), but static effects were also noted. Drug interactions with gentamicin showed early synergy (4–8 h) for all enterococci, and indifference or synergy at 24 h (no antagonism). BAL9141 (≤8 mg/L) showed promising bactericidal activity alone and synergy with gentamicin against some of the vancomycin-resistant enterococci tested.     

In vitro action of fosfomycin combined with rifampicin, pefloxacin and imipenem on staphylococci (checkerboard method in a liquid medium)

The combined activity of fosfomycin with rifampin, pefloxacin and imipenem was investigated, by the checkerboard method performed in liquid medium, against 50 clinical isolates of staphylococci (25 Staphylococcus aureus and 25 coagulase-negative staphylococci). The combination of fosfomycin plus rifampin had an additive bacteriostatic effect and an antagonistic bactericidal effect. Fosfomycin combined with pefloxacin was found to be additive or moderately synergistic. Fosfomycin in combination with imipenem was generally highly synergistic, especially against meticillin-resistant strains; however the bactericidal effect was occasionally antagonistic.     

Bactericidal effect of extracorporeal shock waves on Staphylococcus aureus

Despite considerable knowledge about the effects of shock waves on eukaryotic soft tissues, no data are available concerning their effect on prokaryotic micro-organisms. In vitro studies on the bactericidal effect of extracorporeal shock waves on staphylococci were performed with energy levels that are standard for the disintegration of calculi. Suspensions containing 10(4)-10(5) cfu of Staphylococcus aureus/ml were sealed in plastic tubes and exposed to shock waves, resulting in a mean decrease of 3.1 log(10). Whereas impulse rates of > or =350 resulted in a decrease of cfu/ml equalling the detection limit, lower numbers of impulses did not result in an appreciable bactericidal effect. The bactericidal effect of extracorporeal shock waves might provide the basis for the development of novel therapeutic strategies for bacterial infections.     

New antimicrobial cystatin C-based peptide active against gram-positive bacterial pathogens, including methicillin-resistant Staphylococcus aureus and multiresistant coagulase-negative staphylococci

We describe the synthesis and antibacterial properties of a novel antimicrobial peptidyl derivative, (2S)-2-(Nalpha-benzyloxycarbonyl-arginyl-leucylamido-1-[(E)-cinnamoylamido]-3-methylbutane, structurally based upon the inhibitory centre of the human cysteine protease inhibitor, cystatin C. The derivative, here called Cystapep 1, displayed antibacterial activity against several clinically important gram-positive bacteria. It displayed minimal inhibitory and bactericidal concentrations of about 16 microg/ml for both Staphylococcus aureus and Streptococcus pyogenes. In radial agar diffusion assays, groups A, B, C and G streptococci as well as staphylococci were generally susceptible to the action of Cystapep 1, whereas pneumococci and enterococci were less susceptible. No activity against gram-negative bacteria was observed. Cystapep 1 also showed high activity against methicillin-resistant S. aureus (MRSA) and multiantibiotic-resistant coagulase-negative staphylococci (CNS), suggesting that its mechanism of action differs from those of most currently used antibiotics.     

驻极体5-氟尿嘧啶贴剂药物释放规律的线性回归分析

【摘 要】 目的:采用线性回归方法研究驻极体5-氟尿嘧啶（5-Fu）贴剂的药物释放规律。 方法:利用驻极体实验技术与药剂学方法研制驻极体5-Fu贴剂,采用高效液相色谱仪检测驻极体5-Fu贴剂药物累积释放量,并对相关实验数据进行回归分析,从而将驻极体5-Fu贴剂药物释放规律模型化。 结果:（1）驻极体可以为5-Fu贴剂提供稳恒静电场,该静电场大小与驻极体等效表面电位正相关。（2）驻极体5-Fu贴剂内静电场可改变贴剂黏性,从而实现对5-Fu药物释放量的调控;电场越强,贴剂黏性越小,贴剂累积释药量（Q）越大。（3）驻极体5-Fu贴剂的释药规律满足以下回归方程:V＞0时,Q=（0.003V+13.47）t1/2+0.136 6V1/2+47.574;V=0时,Q=13.767t1/2+48.052;V＜0时,Q=（-0.003 8V+13.471）t1/2+0.162 2（-V）1/2+48.442。 结论:驻极体静电场可对5-Fu贴剂释药量进行调节,其极性和等效表面电位是调控驻极体5-Fu贴剂释药速率的关键因素。