喉咽灵口服液的体外抗菌作用

目的：探讨喉咽灵口服液的体外抗菌作用。方法：为临床分离细菌为受试菌，采用连续倍比稀释法，观察喉咽灵口服液的最低抑菌浓度和最低杀菌浓度。结果：喉咽灵口服液对不同细菌的最小抑菌浓度是成品浓度64－128倍，最小杀菌浓度是成品浓度32－64倍。结论：喉咽灵口服液对所有受试菌均有不同程度的抑菌和杀菌作用，且抗菌谱广，抗菌作用强。     

复方苍耳子散提取物的体外抗菌作用研究

目的：探讨复方苍耳子散提取物的体外抗菌作用。方法：以临床分离细菌为受试菌,采用连续倍比稀释法,观察复方苍耳子散提取物的最低抑菌浓度和最低杀菌浓度。结果：复方苍耳子散提取物的最小抑菌浓度和最小杀菌浓度分别为３２～２０４８倍及１６～１０２４倍。结论：复方苍耳子散提取物对所有受试菌均有不同程度的抑菌及杀菌作用,且抗菌谱广,抗菌作用强。     

黄芩苷联合左氧氟沙星对铜绿假单胞菌生物膜的影响及相关机制

目的:通过在体外建立铜绿假单孢菌生物膜模型,研究黄芩苷联合左氧氟沙星对黏液型铜绿假单胞菌生物膜的协同杀菌效果并探讨其可能机制。方法:选取临床分离的呼吸道铜绿假单胞菌,采用平板培养法建立体外生物膜模型,连续稀释法分别测定左氧氟沙星和黄芩苷的最低抑菌浓度;采用多功能酶标仪测定左氧氟沙星单独作用以及与黄芩苷联用后生物膜内活菌的荧光强度;采用硫酸-苯酚法检测黄芩苷对藻酸盐含量的影响。结果:当黄芩苷浓度大于5 mg.L-1时,生物膜内活菌数减少(P<0.05);黄芩苷与左氧氟沙星存在协同抗菌作用,随着黄芩苷浓度升高,协同抗菌作用增强(P<0.05或P<0.01);黄芩苷可增强左氧氟沙星对生物膜内藻酸盐含量的降解作用。结论:黄芩苷与左氧氟沙星联用,可显著增强其抗菌活性,降低细菌耐药发生。     

重组溶葡球菌酶的体外抗菌活性研究

目的：评价重组溶葡球菌酶对545株临床分离葡萄球菌的体外抗菌活性。方法：采用平皿二倍稀释法，测定重组溶葡球菌酶对545株葡萄球菌的最低抑菌浓度（MIC）；采用试管二倍稀释法和平皿计数法测定此酶对45株葡萄球菌的最低杀菌浓度（MBC）；采用不同浓度重组溶葡球菌酶不同时间的杀菌结果绘制杀菌曲线，检测其对4株受试葡萄球菌的动态杀菌趋势；此外，测定不同培养条件对MIC的影响。结果：此酶对257株金葡球菌具有较强的体外抗菌活性，对288株凝固酶阴性葡萄球菌的抗菌活性相对较弱；结合MBC和杀菌曲线结果，可以判断此酶对敏感菌为快速杀菌作用，并呈浓度依赖性；pH，细菌接种量及高浓度血清蛋白对MIC有一定影响，受试浓度的二价金属离子对MIC影响不明显。结论：重组溶葡球菌酶主要对金葡菌体现强大的抗菌活性，对耐甲氧西林金葡菌（MRSA）和甲氧西林敏感金葡菌（MSSA）的抗菌作用没有明显差别，有进一步研究的价值。     

黄芩苷对单核细胞增生李斯特氏菌的体外抑菌作用研究

目的 研究黄芩苷对单核细胞增生李斯特氏菌的体外抑菌作用。方法 采用倍比稀释法研究黄芩苷对单核细胞增生李斯特氏菌的体外抑菌作用;用管碟法研究黄芩苷浓度对抑菌效果的影响;涂布平板法研究黄芩苷对单核细胞增生李斯特氏菌体外抑制率。结果 黄芩苷对单核细胞增生李斯特氏菌最低抑菌浓度为 0.062 5 g·L-1,浓度为0.5 g·L-1时的抑菌率为(57.0±4.6)%。结论 黄芩苷对单核细胞增生李斯特氏菌在体外有明显的抑制作用,其抑菌效果在一定范围内随浓度增加而增强。     

几种抗感冒制剂的体外抑菌作用对比研究

目的 对比医院制剂与其同类药抗感解毒颗粒的抑菌作用。方法 以呼吸道常见致病茵为受试菌，抗感解毒颗粒为对照药，采用连续倍比稀释法，观察它们的最低抑菌浓度和最低杀菌浓度。结果 本院自制岗梅感冒灵颗粒与板兰根蒲公英颗粒抑菌作用优于市场上的抗感解毒颗粒。结论 从微生物角度看：医院制剂岗梅感冒灵颗粒和板兰根蒲公英颗粒与抗感解毒颗粒相比效果好，抗菌作用强，国家应当保护有特色的医院制剂。     

三种中草药制剂对肠道致病菌体外抗菌作用的分析

目的：探讨分析三种中草药制剂对肠道致病菌体外抗菌作用。方法以连续稀释法检测三种中草药制剂（黄柏、黄连、黄芩）的最低抑菌浓度。结果三种中草药制剂对大肠杆菌的最低抑菌浓度：黄柏为6.3 g/L,黄连为1.6 g/L,黄芩为6.3 g/L;对金黄色葡萄球菌的最低抑菌浓度：黄柏为3.2 g/L,黄连为0.8 g/L,黄芩为1.6 g/L;对副溶血性弧菌的最低抑菌浓度：黄柏为0.8 g/L,黄连为0.8 g/L,黄芩为1.6 g/L;对沙门菌的最低抑菌浓度：黄柏为3.2 g/L,黄连为3.2 g/L,黄芩为12.5 g/L;对志贺菌的最低抑菌浓度：均为3.2 g/L。结论三种中草药制剂（黄柏、黄连、黄芩）对肠道致病菌体外抗菌作用较强。     

黄芩苷协同头孢唑啉对金黄色葡萄球菌生物膜的体外研究

目的研究黄芩苷对金黄色葡萄球菌(S.a)生物膜(BF)的破坏作用以及与头孢唑啉(CEZ)的协同杀菌效果。方法选取临床分离的编号为17546的S.a构建体外BF模型,试管二倍稀释法测定最低抑菌浓度(MICs)和最低杀菌浓度(MBCs),结晶紫染色法半定量BF,连续稀释法活菌计数。结果 BF经黄芩苷作用24h后BF半定量结果显示,黄芩苷组吸光度值为(1.284±0.076),黄芩苷+CEZ组第16h、24h分别为(0.931±0.206)、(0.611±0.738),均少于空白对照组(P<0.01)。黄芩苷+CEZ组第8h、16h、24hBF内的活菌计数分别为(6.906±0.376)×lgCFU/ml、(6.801±0.109)×lgCFU/ml、(6.014±0.340)×lgC-FU/ml,均少于空白对照组(P<0.01)。结论黄芩苷和CLA能破坏S.a已形成的BF,并可增强CEZ对BF内S.a的清除作用。     

清热平口服液的抗菌作用

目的观察清热平口服液的抗菌作用。方法采用二倍稀释法测定清热平口服液对标准菌株金黄色葡萄球菌、肺炎克雷伯菌、乙型溶血性链球菌及肺炎球菌的MIC(最低抑菌浓度)与MBC(最低杀菌浓度)。结果清热平口服液对4种菌株均有一定的抗菌作用。     

复方白鲜皮洗剂抗菌实验

目的:探讨复方白鲜皮洗剂的体外抗菌作用.方法:以临床妇科常见致病菌为受试菌,采用连续倍比稀释法,观察复方白鲜皮洗剂的最低抑菌浓度和最低杀菌浓度.结果:复方白鲜皮洗剂的MIC和MBC分别为白色念珠菌12.5%和25.0%(ml/ml),金黄色葡萄球菌12.5%和25.0%(ml/ml),绿脓杆菌均为6.25%(ml/ml).结论:复方白鲜皮洗剂对白色念珠菌、金黄色葡萄球菌、绿脓杆菌有一定的抑菌和杀菌作用.     

Quinolones in vitro

The first quinolone compound, nalidixic acid, showed activity against a limited number of Gram-negative micro-organisms. One step resistance developed hiin vitro and during treatment. Resistance was not mediated by transfer of R-plasmids, which is a characteristic of all quinolones. Newer quinolones like oxolinic acid, piromidic acid, cinoxacin and pipemidic acid exhibit an extended spectrum of activity against Gram-negative bacteria at lower MIC values. In recent years fluorinated quinolones were introduced like ciprofloxacin, norfloxacin, pefloxacin, ofloxacin, enoxacin and amifloxacin. These compounds exhibitin vitro a broad spectrum of activity against Gram-negative and Gram-positive bacteria at MIC values seventy to four hundred times less than those for nalidixic acid. Thein vitro activity of these compounds has been investigated in a large study of uncomplicated urinary tract infections in general practice (PINISU). No resistance was found. The fluorinated quinolones are very promising antimicrobial agents for a limited number of indications.     

Quinolones in vitro

The first quinolone compound, nalidixic acid, showed activity against a limited number of Gram-negative micro-organisms. ‘One step’ resistance developed hiin vitro and during treatment. Resistance was not mediated by transfer of R-plasmids, which is a characteristic of all quinolones. Newer quinolones like oxolinic acid, piromidic acid, cinoxacin and pipemidic acid exhibit an extended spectrum of activity against Gram-negative bacteria at lower MIC values. In recent years fluorinated quinolones were introduced like ciprofloxacin, norfloxacin, pefloxacin, ofloxacin, enoxacin and amifloxacin. These compounds exhibitin vitro a broad spectrum of activity against Gram-negative and Gram-positive bacteria at MIC values seventy to four hundred times less than those for nalidixic acid. Thein vitro activity of these compounds has been investigated in a large study of uncomplicated urinary tract infections in general practice (PINISU). No resistance was found. The fluorinated quinolones are very promising antimicrobial agents for a limited number of indications.     

High-throughput in vitro hemotoxicity testing and in vitro cross-platform comparative toxicity

For decades, hemotoxicity has been considered as simply changes in peripheral blood parameters or morphological changes observed in the bone marrow as a result of drug administration. The effects are actually the result of the drug acting at a much earlier level in the blood-forming system, usually at the level of the lympho-hematopoietic stem cell or its immediate differentiating progeny. To detect these early cellular responses, highly sensitive, non-subjective and fully standardized in vitro high-throughput testing platforms have been developed that detect changes in intracellular ATP concentrations which are directly proportional to and predict the proliferative/cytotoxic response of different cell populations.     

异十三基二乙胺体内外抗肿瘤作用研究

目的:探讨异十三基二乙胺(D-108)体内外抗肿瘤作用。方法:应用台盼蓝排染法、MTT法检测D-108对多种体外培养肿瘤细胞、人牙龈成纤维细胞(HGF)及Beagle犬骨髓基质干细胞(MSC)的细胞毒作用;Bliss法观察小鼠灌胃(i.g.)D-108急性毒性实验;在可耐受剂量下观察D-108对小鼠移植性实体瘤U14的抑制率。Giemsa染色法观察在D-108影响下,HL60细胞的形态学变化。结果:D-108对肿瘤细胞的体外细胞毒作用(IC50:0.22~2.19mg·L-1)强于HGF及MSC(IC50分别为5.55、3.57mg·L-1)。LD50为36.49mg·kg-1(i.g.)。D-108有效抑制U14在小鼠体内的生长,100mg·kg-1·d-1i.g.瘤质量抑制率为45.27%。HL60细胞经D-108处理后呈典型凋亡形态学改变。结论:D-108有较强的体内外抗肿瘤活性且毒性较小,并能诱导HL60细胞凋亡。     

Neoplastic transformation in vitro

Oncogenic transformation of cultured cells is considered to be analogous to the induction of tumors in animals. Two properties of transformed cells: the capacity to grow in soft agar and morphological alterations were used as a basis for quantitative studies on the transforming properties of chemicals. The majority of experiments on chemical carcinogenesis were so far performed on murine, hamster and rat cell systems. The most pertinent questions to be resolved now are connected with malignant transformation of human cells.     

力达霉素的体外代谢

旨在研究力达霉素在血浆和肝微粒体中的体外代谢性质,指导临床合理用药。选择HPLC-MS/MS测定方法,通过测定力达霉素的活性成分,考察力达霉素在大鼠、比格犬、猕猴和人血浆及肝微粒体中的代谢稳定性以及在人肝微粒体中对细胞色素P450(cytochrome P450,CYP450)各亚型酶的抑制作用。结果表明,力达霉素在4个种属血浆中均有代谢,其代谢速率为大鼠>比格犬>人>猕猴;在4个种属肝微粒体中,只有在猕猴肝微粒体中代谢;在浓度为0.000 5～10 ng·mL-1时,对人肝微粒体中细胞色素P450各亚型酶几乎无抑制作用。可见力达霉素在人体内的代谢性质与比格犬体内较相似,而且临床上当力达霉素与通过CYP450酶代谢的药物合用时,不会导致这些药物的代谢减慢。     

Particokinetics in vitro: dosimetry considerations for in vitro nanoparticle toxicity assessments.

The rapid growth in the use of in vitro methods for nanoparticle toxicity assessment has proceeded with limited consideration of the unique kinetics of these materials in solution. Particles in general and nanoparticles specifically, diffuse, settle, and agglomerate in cell culture media as a function of systemic and particle properties: media density and viscosity and particle size, shape, charge and density, for example. Cellular dose then is also a function of these factors as they determine the rate of transport of nanoparticles to cells in culture. Here we develop and apply the principles of dosimetry in vitro and outline an approach for simulation of nanoparticle particokinetics in cell culture systems. We illustrate that where equal mass concentrations (mug/ml) imply equal doses for dissimilar materials, the corresponding particle number or surface area concentration doses differ by orders of magnitude. More importantly, when rates of diffusional and gravitational particle delivery are accounted for, trends and magnitude of the cellular dose as a function of particle size and density differ significantly from those implied by "concentration" doses. For example, 15-nm silver nanoparticles appear approximately 4000 times more potent than micron-sized cadmium oxide particles on a cm(2)/ml media basis, but are only approximately 50 times more potent when differences in delivery to adherent cells are considered. We conclude that simple surrogates of dose can cause significant misinterpretation of response and uptake data for nanoparticles in vitro. Incorporating particokinetics and principles of dosimetry would significantly improve the basis for nanoparticle toxicity assessment, increasing the predictive power and scalability of such assays.     

Metabolism of strychnine in vitro

The in vitro metabolism of strychnine was studied in the 9000g supernatant fractions from rat and rabbit livers. The metabolism was markedly inhibited by cytochrome P-450 inhibitors, SKF-525A and n-octylamine, but only slightly by a microsomal FAD-containing monooxygenase inhibitor, methimazole. Five metabolites formed in vitro with rabbit liver were isolated and purified by Sep-Pak C18 cartridge chromatography and preparative TLC. Three of them were identified as 2-hydroxystrychnine, strychnine N-oxide, and 21 alpha, 22 alpha-dihydroxy-22-hydrostrychnine by comparison with their authentic samples by means of UV, NMR, and mass spectrometries. An additional two metabolites were tentatively identified as strychnine 21,22-epoxide and 11,12-dehydrostrychnine by spectral measurements. Four of these metabolites, with the exception of 2-hydroxystrychnine, were novel metabolites of strychnine. The in vitro formation of these metabolites by rabbit liver was determined by HPLC after partial purification. The major identified metabolite was strychnine N-oxide, which accounted for approximately 15% of the metabolized strychnine. All the other metabolites accounted for less than 1%. The presence of a larger quantity of other metabolites which have been neither isolated nor identified was also suggested.