巴洛沙星的体外抗菌作用研究

目的评价巴洛沙星的体外抗菌作用。方法以琼脂稀释法测定巴洛沙星对临床分离菌的最低抑菌浓度，并与有关抗菌药进行比较；测定巴洛沙星的杀菌作用，观察巴洛沙星的抗菌活性影。结果巴洛沙星对革兰氏阳性菌及革兰氏阴性菌具广谱抗菌活性，尤其对葡萄球菌、肺炎球菌、肠球菌等革兰氏阳性菌活性优于诺氟沙星、氧氟沙星和环丙沙星。巴洛沙星有较强的杀菌作用，其MBC与MIC相一致，在体外具有较长的抗菌后效应。结论巴洛沙星是一种广谱抗菌药，抗菌作用强，临床应用前景好。     

清肺消炎丸体外抗菌活性研究

目的观察清肺消炎丸对9种肺炎常见病原菌的体外抗菌作用。方法采用琼脂稀释法,测定清肺消炎丸对9种药敏质控菌株的最低抑菌浓度(MIC)及最低杀菌浓度(MBC)。结果清肺消炎丸对肺炎链球菌、化脓性链球菌、金黄色葡萄球菌、流感嗜血杆菌的MIC分别为6.25、25、25、50mg/mL,相应的MBC分别为12.5、25、50、50mg/mL;对大肠杆菌、铜绿假单胞菌、肺炎克雷伯菌、变形杆菌及白色念珠菌均无明显体外抑菌活性。结论清肺消炎丸对肺炎链球菌、化脓性链球菌、金黄色葡萄球菌、流感嗜血杆菌具有体外抗菌作用,其中对链球菌的抗菌活性较高。     

安妥沙星琼脂稀释法体外抗菌活性测定临界浓度初步研究

目的 确定安妥沙星对葡萄球菌属、肠杆菌科、非发酵菌及嗜血菌属的琼脂稀释法体外抗菌活性测定临界浓度.方法 采用标准琼脂二倍稀释法测定安妥沙星对临床常见致病菌的最小抑菌浓度值,并与临床常用的氟喹诺酮类药物相比较分析,结合人体药代动力学参数,初步确定安妥沙星对常见细菌的临界浓度.结果 对临床分离致病菌的MIC测定值显示,安妥沙星的抗菌作用与左氧氟沙星接近,安妥沙星体外抗菌活性与左氧氟沙星相关性最好,安妥沙星一次口服300mg后药代动力学参数与左氧氟沙星一次口服400mg相似,综合PK/PD理论,初步设定安妥沙星琼脂稀释法体外抗菌活性测定的临界浓度为,嗜血菌敏感临界浓度为≤1,其它细菌敏感、中介与耐药临界浓度分别为≤2、4和≥8mg/L.结论 通过体外抗菌活性比较,结合药代动力学/药效学理论,初步确定了安妥沙星琼脂稀释法体外抗菌活性测定对常见细菌的临界浓度,供临床应用参考与验证.     

肚痛丸体内抗菌作用研究

目的：对肚痛丸提取液进行体内抗菌活性试验。方法：采用体外抗菌试验方法。结果：肚痛丸提取液对志贺菌、金黄色葡萄球菌、沙门菌、大肠杆菌和绿脓杆菌等感染的小鼠均有较好的治疗作用。结论：肚痛丸提取液在体内对肠道常见细菌具有显著的抗菌作用。     

氧哌嗪青霉素体外抗菌活性及其胆汁浓度测定方法的研究

本文应用琼脂平板稀释法测定氧哌嗪青霉素对40株常见致病菌的最低抑菌浓度(MI-C),并应用AVANTAGE分析仪对胆道感染致病菌对氧哌嗪青霉素的敏感性进行测定。结果表明,氧哌嗪青霉素对G~ 球菌的MIC为0.5～32μg/ml,对G~-杆菌的MIC为<0.0625～64μg/ml,对胆道常见致病菌的敏感率为75～100%。同时应用AVANTAGE分析仪自动化比浊法探讨了氧哌嗪青霉素胆汁浓度的测定方法。以吸收度(y)对浓度(x)回归,得回归方程为y=0.1878-0.002776x,R=-0.9975。表明在标准浓度2.5～40μg/ml范围内,氧哌嗪青霉素胆汁浓度与吸收度具有良好的线性关系。在三个浓度水平上回收率分别为98.4%、101.3%和105.0%。管间变异<5.7%、日内变异<5.6%、日间变异<6.2%,表明该测定方法较为精确,可以接受并进一步用于临床研究。     

头孢硫咪体外抗菌活性测定

目的：评价第一代头孢菌素头孢硫脒对近期从临床分离的致病菌的体外抗菌活性。方法：用对倍稀释法测定头孢硫咪的最小抑菌浓度（ＭＩＣ）并与头孢唑啉、头孢呋辛、头孢他啶体外抗菌活性进行了对比。结果：头孢硫脒对肺炎球菌、化脓性链球菌、ＭＳＳＡ、ＭＳＳＥ和卡他布汉氏菌有较强的抗菌活性。结论：头孢硫脒对Ｇ^＋球菌有较强的抑菌活性和杀菌活性,对肠球菌亦显示有很强的体外抗菌活性。     

国产美洛培南的体外抗菌活性

采用琼脂二倍稀释法测定国产美洛增南和其它５种药物对１３６株临床分离菌的体外抗菌活性,结果表明国产美洛增南与进口美洛增南的体外抗菌活性相近,优于头孢哌酮／舒巴坦、他唑西林和头孢他啶。国产美洛增南对金葡萄菌、铜绿假单孢菌、大肠埃希氏菌和肺炎克雷伯氏菌的抗菌活性优于亚胺培南／西司他丁,对表葡球菌和β－溶血性链球菌的抗菌活性比后者稍差。国产美洛培南的抗菌活性稍受接种菌量、培养基ｐＨ和血清浓度影响。     

注射用双黄连的体外抗菌活性研究

目的评价注射用双黄连的体外抗菌活性。方法采用平皿二倍稀释法测定注射用双黄连对多种临床分离菌的MIC值,以评价注射用双黄连的体外抗菌活性。结果注射用双黄连对包括革兰阳性菌和革兰阴性菌在内的多种细菌均具有一定的体外抗菌活性。结论注射用双黄连对多种革兰阳性菌和革兰阴性菌细菌具有体外抗菌作用。     

加替沙星体外抗菌活性研究

采用琼脂二倍稀释法测定加替沙星对651株临床分离致病菌的体外抗菌活性，并与左氧氟沙星、司帕沙星、环丙沙星、诺氟沙星、头孢唑林、头孢呋辛、头孢噻肟、头孢他啶、万古霉素、阿米卡星、阿莫西林、哌拉西林/三唑巴坦比较。结果表明，加替沙星具有强而广谱的体外抗菌活性。对甲氧西林敏感的金葡球菌（MSSA）、表葡球菌（MSSE）、肠球菌的MIC90分别为0.125、1、16mg/L，抗菌活性为左氧氟沙星的1-2倍、环丙沙星的2-4倍，逊于第三代头孢菌素类。对肺炎克雷伯氏菌、伤寒沙门氏菌、痢疾杆菌、奇异变形菌、粘质沙雷氏菌，MIC90分别为4、0.25、0.5、4.32mg/L，抗菌活性为左氧氟沙星、司帕沙星、环丙沙星的1-2倍，与第三代头孢菌素类相当。对聚团肠杆菌、阴沟肠杆菌、乙酸钙不动杆菌、铜绿假单胞菌的MIC90分别为32、32、16.4mg/L。加替沙星对革兰氏阳性、阴性菌均具强大抗菌作用。     

消炎止痛栓体外抗菌活性研究

目的:研究消炎止痛栓(主要成分为盐酸小檗碱、冰片、土霉素、盐酸丁卡因)的体外抗菌活性。方法:运用试管稀释法测定并分析消炎止痛栓在体外对标准菌株金黄色葡萄球菌、大肠埃希菌、铜绿假单胞菌的最低抑菌浓度(MIC)和最低杀菌浓度(MBC)。结果:消炎止痛栓对上述3种标准菌株的MIC分别为0.195、0.0488、0.0975mg.mL-1,MBC分别为0.390、0.0975、0.390mg.mL-1。结论:消炎止痛栓在体外对上述3种标准菌株具有良好的抗菌活性。     

A novel and eco-friendly procedure for the synthesis of some pyrazolo-thiadiazolo-pyrimidinones and its in vitro anti-bacterial activity

A novel series of 2-substituted-aminomethyl-8-phenyl-pyrazolo[3,4-d][1,3,4]thiadiazolo[3,2-a]pyrimidin-4(1H)-ones have been synthesized by treating 2-chloromethyl-8-phenyl-pyrazolo[3,4-d][1,3,4]thiadiazolo[3,2-a]pyrimidin-4(1H)-one with various nucleophiles. The chloromethyl derivative was prepared by treating 2-amino-3-mercapto pyrazolo[3,4-d]pyrimidine with one carbon donor, chloroacetic acid. The intermediate 2-amino-3-mercapto pyrazolo[3,4-d]pyrimidine was prepared by a novel, eco-friendly route starting from 2-amino-3-carbethoxy-1-phenyl-pyrazole. The target compounds exhibited broad-spectrum antibacterial activity (Kirby Bauer’s Method).     

丁香挥发油的抗茵作用研究

目的 对丁香挥发油进行体内外抗茵活性试验.方法 体外抗茼试验采用微量琼脂法.结果 丁香挥发油体外对产酸克雷伯茵、肠炎沙门氏菌、痢疾志贺氏菌、大肠杆菌、表皮葡萄球菌和金黄色葡萄球菌均有明显的抗菌作用;体内对金黄色葡萄球菌、大肠杆菌等感染的小鼠均有较好的治疗作用.结论 丁香挥发油在体内外对常见细茵具有显著的抗茼作用.     

Investigation of plants used in Jamaican folk medicine for anti-bacterial activity

We have started a systematic scientific study of folklore medicinal plants currently used as alternative medicine in Jamaican society. In this initial study, extracts of plants widely used by the islanders are studied for antibacterial activity against five common pathogens; Streptococcus group A, Staphylococcus aureus, Proteus mirabilis, Pseudomonas aeruginosa and Escherichia coli. These studies revealed that 25% (approx.) of the plant extracts had antimicrobial activity against at least one of the microbes used. Subsequent to these observations, extracts from Mikania micrantha were examined in detail. This led to the isolation of two sesquiterpenoids, mikanolide and dihydromikanolide, with activity against S. aureus and C. albicans. The results suggest that traditional folk medicine could be used as a guide in our continuing search for new natural products with potential medicinal properties.     

Determination of in vitro activity renin inhibitors by HPLC method

A high-performance liquid chromatographic assay has been developed to the separation of angiotensin I, tetradecapeptide and the tetrapeptide Leu-Val-Tyr-Ser. This purpose is achieved in a single step, using HPLC technique in the reversed phase system. The method is based on enzymatic hydrolysis of a substrate renin (TDP) with formation of angiotensin I (DP). After 1 h incubation at 37 degrees C the reaction mixture is introduced directly into the chromatographic system. A 200 microl reaction mixture is needed for analysis. Acetonitrile gradient in 0.01 M ammonium acetate buffer allows a satisfactory separation of hydrolysis products. The application of this technique for the determination of in vitro renin activity and evaluation the potency of human renin inhibitors, employing the artificial renin substrate tetradecapeptide, is demonstrated.     

Determination of immunological activity in vitro of some plant raw materials

Aqueous extracts of five tannin plant raw materials have been studied for the survivals of thymocytes from the thymus of Balb-c mice. The immunostimulation activity was compared with a preparation from calf thymi TFX and phenolic acids: ellagic and gallic acids. It was found that only the Fructus Myrtilli extract has revealed a statistically significant influence on the survival of thymocytes.     

纳豆激酶体外活性测定及影响因素考察

目的建立纳豆激酶(NK)体外活性测定方法,考察影响因素。方法采用对甲基苯磺酰-L-精氨酸甲酯(TAME)作为底物,用变色酸反应显色,在574 nm波长处比色测定酶活性。结果NK在0.05~0.25 mg/mL浓度范围内具有良好的线性关系;NK在pH 8.0,4℃,活性保持最久。结论TAME法测定NK活性操作简便,可较准确测定NK体外活性。温度、pH、某些溶剂对NK的活性有影响。     

Determination of antibacterial activity of polyenzyme preparations Gumseb using in vitro methods

A novel polyenzyme formulation Gumseb developed by Advanced Enzyme Technologies Ltd, Thane and Speciality Biochemicals Co., USA, was tested for antibacterial properties using ATCC strains and clinical isolates of Salmonella typhi, Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, Streptococcus pyogenes and Streptococcus pneumoniae. A modified antibiotic susceptibility test was used for the purpose. S. aureus, S. pyogenes and S. pneumoniae were found to be sensitive to the formulation at the chosen concentration. Next, to study the interaction between Gumseb and currently used antibiotic, a checkerboard Minimum Inhibitory Concentrations (MIC) was carried out for each organism. The assay was carried out with the aim of establishing whether the polyenzyme formulation had any potentiating effect on the antibiotic of choice. Synergistic effect was established when Gumseb was used in conjunction with penicillin against S. pyogenes. Partial synergy was established when it was used in conduction with Ceftazidime against P. aeruginosa and with Ciprofloxacin against methicillin sensitive, coagulase positive S. aureus. Antagonism was established when it was used in conjunction with Ampicillin against E. coli, with Ciprofloxacin against S. typhi and coagulase negative staphylococcal strain. The results indicate that Gumseb can be used in conjunction with those antibiotics with which a synergistic or a partially synergistic effect could be shown, as in the case of P. aerugionosa and S. aureus. These findings have particular importance since these organisms are responsible for hospital based infections and are notorious for antibiotic resistance. In cases where antagonism was established, it should not be used in combination with that particular antibiotic. However, it can be used individually since it has proved to have antibacterial activity and MIC could be determined for all five commonly encountered pathogens. Therefore, it has the potential of being a novel broad range antibacterial drug. These findings are significant given the alarming rise in incidence of antibiotic resistance in most clinically important pathogens.     

等温微量热技术比较原研和仿制头孢曲松钠体外抑菌效果

目的 开发一种基于等温微量热技术实时测定和比较原研(罗氏芬)与仿制(MY)头孢曲松钠体外抑菌效果的快速检测方法。方法 以金黄色葡萄球菌为测试菌株,利用微量热法,比较原研和仿制头孢曲松钠对金黄色葡萄球菌生长代谢的影响。以表达功率-时间曲线 (热谱曲线) 的特征参数：生长速率常数k、最大热功率Pm、热谱图出现主峰时间tm和传代时间tG为指标,量化评估原研和仿制头孢曲松钠对金黄色葡萄球菌生长代谢的影响。为验证等温微量热法结论,进一步采用管碟法和高效液相色谱法(HPLC)分别检测原研和仿制头孢曲松钠的抑菌活性。结果 热谱曲线的特征参数数据表明,原研头孢曲松钠与仿制头孢曲松钠均具有抑菌活性,但原研头孢曲松钠抑菌效果比仿制头孢曲松钠明显,这一结论与传统管碟法及HPLC法所得结论一致。然而,等温微量热法实验仅需24h,管碟法与HPLC法则需48h以上。结论 等温微量热技术具有灵敏度高、精密度好的特点,可实时检测和比较不同抗生素体外抑菌活性,在快速评价抗生素效价领域具备较好的应用前景。