微量热法研究头孢菌素对大肠杆菌微生物活性的影响

用微量热法测定了两种头孢菌素头孢哌酮钠(CFZ)和头孢哌酮钠舒巴坦钠(CFZ-SBT)在37 ℃时对大肠杆菌DH5α代谢作用的影响. 根据产热曲线分别获得了大肠杆菌DH5α在不同浓度的头孢哌酮钠和头孢哌酮钠舒巴坦钠作用下的生长速率常数(k)、抑制率(I)、最大产热功率(Pm)以及最大产热功率所对应的时间tm等热动力学参数. 研究结果表明, 头孢哌酮钠和头孢哌酮钠舒巴坦钠对大肠杆菌的致死量分别为0.1和0.25 μg/mL. 通过研究k, I, Pm, tm和浓度(c)间的关系发现, 舒巴坦钠的加入没有增加头孢哌酮钠对大肠杆菌DH5α的抑制作用.     

金属离子化合物抗菌活性的微量热法

用微量热法测定了大肠杆菌在四种金属离子化合物作用下的生长代谢热谱。计算了大肠杆菌在指数生长期的生长速率常数k、传代时间G、生长抑制率I和发热量Q等参数；建立了热谱信息参量之间的关系，定量地讨论了金属离子化合物对大肠杆菌生长代谢的抑制，并发现可用P_max和t_r表征大肠杆菌和生长代谢的化合物的抗菌活性。     

微量热法研究硒对大肠杆菌生长代谢的作用

硒 是生物必需的微量元素之一．自从１９７３年Ｒｏｔｒｕｃｋ报导了第一个硒酶———红细胞谷胱甘肽过氧化物酶［１］,硒在生命科学中的研究取得了令人瞩目的进展．继红细胞谷胱甘肽过氧化物酶之后 ,从哺乳动物中还发现硒为多种酶所必需 ;此外 ,在不同的动物组织中一系列含硒蛋白被分离和鉴别．随着分子生物学技术的发展和硒在生物化学中的应用 ,人们对硒的生物化学本质有了更加深刻的认识 ,其中 ,遗传基因硒代半胱氨酸密码子ＵＧＡ的发现使硒的生物化学研究进入了一个新的阶段．与此同时 ,小分子有机硒化合物Ｅｂｓｅｌｅｎ生物活性的发现…     

抑制剂对大肠杆菌作用的透射电镜及微量热法研究

用透射电镜对大肠杆菌以及大肠杆菌受到３种不同抑制剂抑制时的形态进行了观察，结果发现不同的抑制剂对大肠杆菌的不同抑制作用表现在大肠杆菌的微观形态发生了不同的变化，同时结合微量热的方法，测试了３种不同抑制剂作用下大肠杆菌的生长代谢热谱，热谱曲线的分析结果与透射电镜观察结果吻合。     

采用微量热法研究重金属离子对脲酶催化水解反应的影响

利用微量热计Micro DSCⅢ对重金属离子影响脲酶催化水解反应的过程进行研究, 并探讨重金属离子联合抑制作用对脲酶催化反应的影响. 结果表明, 在25℃下, 重金属离子对脲酶水解反应热有影响, 在广泛浓度范围(0.1, 1, 10, 100和10³ mg/L)内, 这种影响不仅表现在抑制作用方面, 而且会促进其水解反应的进行, 如铜离子在100和1000 mg/L时抑制率分别为(0.49±0.20)%和(-11.93±1.34)%. 重金属离子浓度与抑制率具有显著或极显著的相关性, 抑制效果的顺序为砷离子>铅离子>镉离子>铜离子. 当重金属离子联合抑制时, 其抑制效果与抑制率较高的重金属离子的抑制作用接近.     

微量热法测定Vitex negundo Linn对大肠杆菌抑制作用的活性部位

开发药用植物首先必须确定其活性部位. 我们采用微量热法鉴定了一种植物Vitex negundo Linn的四种不同提取物: 正己烷提取物、氯仿提取物、乙酸乙酯提取物和甲醇提取物对大肠杆菌(E. coli)的抑制作用. 结果表明甲醇提取物对大肠杆菌生长的代谢热谱抑制作用最强. 通过计算该提取物作用下大肠杆菌的生长速率常数, 表明该提取物的抑制作用随浓度的升高而增强.     

微量热法研究Schiff碱钴配合物的抗菌活性

微量热法研究Ｓｃｈｉｆｆ碱钴配合物的抗菌活性黄在银＊屈松生冯英俞芸（武汉大学化学系武汉４３００７２）关键词二羟基苯甲醛葡萄糖Ｓｃｈｉｆ碱配合物，微量热法，抗菌活性，大肠杆菌１９９７－０８－１８收稿，１９９７－１１－０３修回国家自然科学基金及高等学校博...     

微量量热法研究黄连中小檗碱类生物碱对金黄色葡萄球菌生长代谢的影响

采用微量量热法研究中药黄连中具有抑菌作用的3种小檗碱类生物碱成分对金黄色葡萄球菌生长代谢的影响．在不同给药条件下,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、半数抑菌浓度（IC50）、最大输出功率（Pmax）及达峰时间（tp）和总产热量（Qt）为指标,对3种小檗碱类生物碱成分抑制金黄色葡萄球菌生长代谢程度进行客观地量化评价．结果表明,k、Pmax和Qt均随3种小檗碱类生物碱成分浓度的增加而相应的减小;tp随3种小檗碱类生物碱成分浓度的增加而相应的延长;其IC50分别为小檗碱101．4μg／mL、巴马汀241．0μg／mL和药根碱792．3μg／mL,即抑菌活性大小顺序为小檗碱〉巴马汀〉药根碱．初步构效关系研究提示,位于苯环的C2、C3上的亚甲二氧基或甲氧基较羟基更有助于提高其抑菌活性．     

微量热法研究硒对砷在大肠杆菌生长中的联合作用

以大肠杆菌为模型生物,结合生物学的细菌培养方法,用微量热法研究了硒代吗啉与亚砷酸钠对大肠杆菌的联合作用,初步探讨了它们之间的作用机理.结果表明,硒代吗啉和亚砷酸钠之间既有拮抗作用,也有协同作用,这依赖于两者的相对浓度.硒与砷的作用机理可能与细菌生长代谢过程中酶的合成有关.     

微量热法研究PCMB对精氨酸酶的抑制作用

利用微量热法研究了对－氯汞苯甲酸（ＰＣＭＢ）对精氨酸的酶促水解反应的抑制作用，确定它于竞争性不可逆抑制剂，在２９８．１５Ｋ和ＰＨ为９．４时ＰＣＭＢ与精氨酸酶作用的二级速度常数ｋ＋０＝９２．１７Ｌ／（ｍｏｌ．ｓ）。同时用ＰＣＭＢ作为修饰剂探讨了精氨酸酶的活性中心性质，推测该水解酶至多含有３个与酶活性有关的半胱氨酸残基，但主些残基不属于精氨酸酶的活性中心。     

Study of the Influence of Different Diphenol Compounds on Soil Microbial Activity by Microcalorimetry

Microcalorimetry was applied to follow the toxic effects caused by different diphenol compounds on microbial activity of Chinese fir soil. The activity of the microorganisms in soil was stimulated by adding 0.3 mL of a nutrient solution containing 2.5 mg of glucose and 2.5 mg of ammonium sulfate and the measurements were performed under a 35% controlled humidity at 28°C. Power‐time curves recorded on a microcalorimeter were followed by increasing the amount of diphenol compounds, which affected directly the total thermal effects evolved by the microorganisms. The curves showed a synergism on total thermal effect obtained by the addition of 2000 mg·kg^?1 of resorcinol, causing a consumption of resorcinol by the microorganisms as a new source of nutrients. Above this dose, the total thermal effect decreased exponentially. However, the addition of catechol and hydroquinone caused the total thermal effects to decrease directly. It was concluded that the increase in the diphenol concentration strongly affected the microbial life in this ecosystem. Microcalorimetry appears as a suitable technique to carry out both qualitative and quantitative comparative studies of microbial activity in soil.     

Effect of Lead Contamination on Soil Microbial Activity Measured by Microcalorimetry

Microcalorimetry was used to investigate the microbial activity in three types of soil (orchard soil, crop soil, forest soil) in Wuhan, China, and to evaluate the influence of different concentrations of lead (Pb²⁺) on soil microbial activity. The experimental results revealed that due to different physical and chemical characteristics of the soils, soil microbial activity in three soil samples were in a descending sequence: orchards soil, crops soil, forest soil. Six levels of Pb viz. 0, 10, 20, 40, 80, 160 μg·g⁻¹ were applied in these soils, and the results showed that an increase of the amount of Pb²⁺ is associated with a decrease in microbial activity in the soils due to the toxic effect of Pb²⁺. In order to gain further insight of the sequential change of microorganisms, determination of colony forming units (CFU) was performed to provide a negative linear correlation between the heat effect and the respective number of microorganisms in the system.     

Investigation of the Effect of Four Organic Acids in Radix Isatidis on E. coli Growth by Microcalorimetry

The inhibitory effects of four organic acids (OAs) in Radix Isatidis, a traditional Chinese medicinal herb, on Escherichia coli (E. coli) growth were investigated by microcalorimetry. The power‐time curves of E. coli growth with and without OAs were acquired, meanwhile the extent and duration of inhibitory effects on the metabolism were evaluated by growth rate constants (k₁, k₂), half inhibitory ratio (IC₅₀), maximum heat output (P_max) and peak time (t_p). The values of k₁ and k₂ of E. coli growth in the presence of the four OAs decreased with the increasing concentrations of OAs. Moreover, P_max was reduced and the value of t_p increased with increasing concentrations of the four drugs. The sequence of anti‐microbial activity of the four OAs was: syringic acid>2‐amino‐benzoic acid>salicylic acid>benzoic acid. IC₅₀ of the four OAs was respectively 56 µg/mL for syringic acid, 75 µg/mL for 2‐amino‐benzoic acid, 86 µg/mL for salicylic acid and 224 µg/mL for benzoic acid. The existence of the functional groups on phenyl ring improves the anti‐microbial activity compared to benzoic acid. The functional groups methoxyl at C(3) and C(5) improve anti‐microbial activity more strongly than the other functional groups, and the functional group amino at C(2) improve anti‐microbial activity more strongly than hydroxyl at C(2) on phenyl ring.     

Investigation of Antibacterial Activity of Two Kinds of Novel Schiff Bases on Escherichia coli by Microcalorimetry

The microcalorimetric method was used to study the antibacterial activity of two newly synthesized Schiff basecompounds(H_2L~(3')and H_2L~3)on Escherichia coli,trying to obtain the action on both of multiplying bacteria andnon-multiplying bacteria at one experiment.The metabolic power-time curves of the bacteria treated with the com-pounds were obtained,and the thermokinetic parameters were analyzed,from which the antibacterial activities ofthese compounds were evaluated.The results showed that both of the two compounds have good activity on aerobicmultiplying metabolism of E.coli,with the value of IC_(50)75.8 and 168.8 mg/L respectively,but have not effectiveaction on fermentation metabolism of E.coli.The action of the compounds on the non-multiplying metabolism wasinvestigated by taking the heat output of E.coli in the stationary phase as the guideline of the activity.The value ofMSC_(50)(minimum stationary-cidal concentration 50)of them is 118 and 187.5 mg/L,respectively.So,H_2L~(3')hasstronger antibacterial action on E.coli than H_2L~3 either for multiplying bacteria or non-multiplying bacteria,andtheir activity on the aerobic multiplying bacteria of E.coli is mainly shown.It does strongly suggest that the calo-rimetric method should play an important role in the fight against the drug-resistant bacteria.     

微量量热法研究大肠杆菌对粉防己碱和粉防己总生物碱的耐药性

微量量热法研究大肠杆菌对粉防己碱和粉防己总生物碱的耐药性;粉防己碱;粉防己总生物碱;耐药性;大肠杆菌;微量量热法     

The Action of the Selenomorpholine Compounds on Escherichia coli Growth by Microcalorimetry

The action of three kinds of the selenomorpholine compounds on a strain ofEscherichia coli was studied by microcalorimetry. Differences in their capacities to affect the metabolism of this bacterium were observed. The extent and duration of the effect on the metabolism as judged from the rate constant (k) of Escherichia coli (in log phase) varied with the different drugs. The kinetics show that selenomorpholine compounds had an effect on the metabolism process of Escherichia coli. The k of Escherichia coli in the presence of the drugs increased with the increasing concentrations of the drugs (C) at low concentration; but at high concentration, the rate constant decreased with the increasing concentrations of the drugs. The experimental results reveal that the sequence of antibiotic activity of selenomorpholines is: N-selenomorpholinemethyl succinimide and its hydrochloride>N-(α-selenomorpholinebenzyl) succinimide. This revised version was published online in August 2006 with corrections to the Cover Date.     

Influence of Open Chain and Cyclic Structure of Peptidomimetics on Antibacterial Activity in E. coli Strains

An efficient method for the synthesis of functionalized peptidomimetics via multicomponent Ugi reaction has been developed. The application of trifluoroethanol (TFE) as a reaction medium provided desired products with good yields. Further, using the developed cyclisation reaction, the obtained peptidomimetics were transformed into the cyclic analogues (diketopiperazines, DKPs). The goal of the performed studies was to revised and compare whether the structure of the obtained structurally flexible acyclic peptidomimetics and their rigid cycling analogue DKPs affect antimicrobial activity. We studied the potential of synthesized peptidomimetics, both cyclic and acyclic, as antimicrobial drugs on model E. coli bacteria strains (k12, R2–R4). The biological assays reveal that DKPs hold more potential as antimicrobial drugs compared to open chain Ugi peptidomimetics. We believe that it can be due to the rigid cyclic structure of DKPs which promotes the membrane penetration in the cell of studied pathogens. The obtained data clearly indicate the high antibiotic potential of synthesized diketopiperazine derivatives over tested antibiotics.