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[Isolation and properties of beta-lactamase of the cephalosporinase type from cells of Enterobacter aerogenes 6803]. [从产气肠杆菌6803细胞中分离头孢菌素酶型β -内酰胺酶及其性质]。
Pub Date : 1984-11-01
A Iu Sazykin, A S Krylov, S M Navashin

beta-Lastamase with the molecular weight of 32500 was isolated from the cells of clinical strain 6803 of Enterobacter aerogenes and purified. By the substrate profile determined microiodometrically beta-lactamase was classified as belonging to the cephalosporinase type. The activity of the electrophoretically homogenous enzyme was equal to 430 microM a minute per mg protein with respect to benzylpenicillin. The Km for benzylpenicillin, dicloxacillin, cephaloridin and cephalothin was 6.5410(-5), 3 X 10(-4), 2.1 X 10(-5) and 5.7 X 10(-5) M, respectively. The isoelectric point of the enzyme equal to 5.45 was estimated with the method of preparative isoelectrofocusing. The presence of the serine residue or residues was shown with the use of selective reagents applied to the functionally important groups. With the method of circular dichroism the ratio of alpha- and beta-structures in the enzyme molecule was determined, the slow hydrolysis of cephazolin was demonstrated and the values of Km and Kcat for this process were estimated.

从产气肠杆菌临床菌株6803细胞中分离得到分子量为32500的β - lastamase。根据底物谱测定-内酰胺酶被归类为属于头孢菌素酶型。相对于青霉素,电泳均相酶的活性等于每毫克蛋白质430微米/分钟。青霉素、双氯西林、头孢啶和头孢肽的Km分别为6.5410(-5)、3 × 10(-4)、2.1 × 10(-5)和5.7 × 10(-5) M。用制备等电聚焦法估计酶的等电点为5.45。丝氨酸残基或残基的存在表明使用选择性试剂应用于功能重要基团。用圆二色法测定了酶分子中α -和β -结构的比例,证明了头孢唑啉的缓慢水解,并估计了该过程的Km和Kcat值。
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引用次数: 0
[Effectiveness of tobramycin in young children with Salmonella infection]. 妥布霉素对幼儿沙门氏菌感染的疗效。
Pub Date : 1984-11-01
I A Vereshchagin, A I Bobrovitskaia, O D Zhuravleva, E R Bukhteeva, S S Ivanova

The intestinal form of salmonellosis caused by S. typhimurium and the host immunity were studied in 108 infants. 60 infants were treated with ampicillin and the other 48 infants with tobramycin. The recovery period in patients treated with tobramycin was 8 days less as compared to the patients treated with ampicillin After discontinuation of the tobramycin use the pathogen was not detected in the repeated platings. Bactericidal function of neutrophils in these patients returned to normal within 15 days after the beginning of the treatment. Tobramycin was shown to be a highly active antibiotic in the treatment of salmonellosis of infants. No side effects were observed.

对108例婴幼儿鼠伤寒沙门氏菌肠道菌型及宿主免疫进行了研究。60名婴儿接受氨苄西林治疗,另外48名婴儿接受妥布霉素治疗。停用妥布霉素后,与使用氨苄西林的患者相比,使用妥布霉素的患者的恢复期缩短了8天。这些患者的中性粒细胞杀菌功能在治疗开始后15天内恢复正常。妥布霉素被证明是一种治疗婴儿沙门氏菌病的高活性抗生素。未观察到任何副作用。
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引用次数: 0
[Growth rate of antibiotic-producing gram-negative bacteria on liquid nutrient media]. [产抗生素革兰氏阴性菌在液体营养培养基上的生长速率]。
Pub Date : 1984-11-01
O N Oparina, L E Bodunkova, I A Spiridonova, L N Ostanina, M V Baturina

Glycerol-yeast medium No. 3 may be used as a seed medium in screening of antibiotic-producing strains among Acetobacter, Gluconobacter, Chromobacterium, Agrobacterium, and other genera. The medium is transparent. It provides visual instrumental control of the growth rate of the seed material and estimation of biomass augmentation. The period of the exponential phase growth of the strains tested on medium No. 3 was 2-8 hours. When no growth on medium No. 3 is observed media Nos. 1 and 2 can be used as alternative seed media.

甘油酵母培养基No. 3可作为种子培养基在醋酸杆菌、葡萄糖杆菌、色杆菌、农杆菌和其他属中筛选产生抗生素的菌株。介质是透明的。它提供了可视化的仪器控制的种子材料的生长速度和生物量增加的估计。在3号培养基上试验的菌株的指数相生长周期为2 ~ 8 h。当3号培养基不生长时,可选用1号和2号培养基作为替代种子培养基。
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引用次数: 0
[Stability of antibiotics in disks as one of the indicators of their quality]. [以抗生素片的稳定性作为其质量的指标之一]。
Pub Date : 1984-11-01
T P Galkina, I N Khvoshchevskaia, S P Rezvan, S M Chaĭkovskaia

In connection with the new requirements to the content of antibiotics in discs and a new procedure for the disc labeling stability of antibiotics in discs was studied with the methods of storage under natural conditions and under conditions of accelerated ageing. It was shown that the method of accelerated ageing was not applicable to testing antibiotic stability in discs, since with the use of this method a significant decrease in the antibiotic activity was observed which did not correspond to the real decrease in activity determined with the method of storage under natural conditions. The expiry date of the discs with benzylpenicillin or semisynthetic penicillins was determined to be equal to 1.5 years when stored at 10 degrees C. The expiry date of the discs with thermostable antibiotics was determined to be equal to 3 years when stored at 10 degrees C. Though certain inactivation of the antibiotics was observed, their content in the discs remained within the required limits, i.e. 75-135 per cent of the activity indicated on the label.

结合对片剂中抗生素含量的新要求和片剂标示的新程序,采用自然贮存法和加速老化贮存法对片剂中抗生素的稳定性进行了研究。结果表明,加速老化法不适用于检测光盘中的抗生素稳定性,因为使用这种方法观察到抗生素活性的显著下降,这与自然条件下储存方法确定的活性的实际下降不符。装有青霉素或半合成青霉素的盘片在10℃储存时的有效期确定为1.5年。装有耐热抗生素的盘片在10℃储存时的有效期确定为3年。虽然观察到某些抗生素失活,但盘片中的含量仍在规定的限度内,即标签上所示活性的75- 135%。
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引用次数: 0
[Antitoxic effect of leukocytic interferon in in vivo experiments]. [白细胞干扰素的体内抗毒作用实验]。
Pub Date : 1984-11-01
A A Babaiants, G G Karganova

Leukocyte interferon of various species origin (human, swine, mice) protected mice from the lethal dose of staphylococcal toxin. Endogenic mouse interferon and exogenic serum mouse interferon had no such effect. The suspension of waste leukocytes had also a protective activity. The results of the study evidence the presence of antitoxic factor in the leukocytes.

来自不同物种(人、猪、小鼠)的白细胞干扰素保护小鼠免受葡萄球菌毒素致死剂量的侵害。内源性小鼠血清干扰素和外源性小鼠血清干扰素均无此作用。废白细胞悬浮液也有保护作用。研究结果证实白细胞中存在抗毒因子。
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引用次数: 0
[Combined use of prodigiozan and methyluracil with immunosuppressive drugs in adjuvant arthritis in rats]. [prodigiozan、methyluracil联合免疫抑制药物治疗大鼠佐剂性关节炎]。
Pub Date : 1984-11-01
S V Sibiriak, D N Lazareva, N A Kokhanchikova

The effect of the combined use of prodigiozan (0.5 mg/kg bw) prodigiozan with immunosuppressants on the development of adjuvant arthritis was studied on rats. The drugs were given during the prearthritis period from the 1st to the 16th day after injection of complete Freund's adjuvant. It was shown that the combined use of prodigiozan and cyclophosphamide (5 mg/kg) induced significant inhibition of the arthritis development and extraarticular signs of the disease. The efficacy of the combination was higher than that of cyclophosphamide alone. Azathioprine (4 mg/kg/bw) produced no immunosuppressant effect and did not influence the inhibitory effect of prodigiozan on the development of the adjuvant disease. Prednisolone (1.6 mg/kg) either did not inhibit the arthritis development. However, it eliminated the prodigiozan effect. Methyluracil did not change the effect of the immunosuppressants on the articular syndrome. Still, it increased the number of nodular affections in the animals treated with cyclophosphamide and prednisolone. The data obtained show the possibility of prodigiozan combination with certain immunosuppressants in autoimmune affections and confirm the suggestion that the inhibitory effect of this drug is mediated through macrophages.

以大鼠为实验对象,研究了神童碘(0.5 mg/kg bw)与免疫抑制剂联合应用对佐剂性关节炎发展的影响。在注射完全弗氏佐剂后第1 ~ 16天的关节炎前期给药。结果表明,联合使用prodigiozan和环磷酰胺(5mg /kg)可显著抑制关节炎的发展和疾病的关节外体征。联合用药的疗效高于单用环磷酰胺。偶氮噻吩啉(4 mg/kg/bw)不产生免疫抑制作用,不影响prodigiozan对佐剂病发展的抑制作用。强的松龙(1.6 mg/kg)也没有抑制关节炎的发展。然而,它消除了奇才效应。甲尿嘧啶不改变免疫抑制剂对关节综合征的影响。然而,在接受环磷酰胺和强的松龙治疗的动物中,它增加了结节性情感的数量。本研究结果表明,prodigiozan可能与某些免疫抑制剂联合作用于自身免疫性疾病,并证实了该药物的抑制作用是通过巨噬细胞介导的。
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引用次数: 0
[Effect of prodigiozan and lysozyme on the surface structures of macrophages after immunosuppression]. [巨噬细胞免疫抑制后巨噬细胞表面结构的影响]。
Pub Date : 1984-11-01
E G Shcherbakova, G A Rastunova

The state of macrophage surface structures is closely connected with the function 1 capacity of these cells. Peritoneal macrophages from mice subjected to strong 10-day immunosuppression with azathioprine (60 mg/kg), prednisolone (50 mg/kg) or their combination (25 and 30 mg/kg, respectively) were investigated with scanning electron microscopy. Azathioprine and especially its combination with prednisolone induced pronounced degenerative affections in the macrophages and lymphocytes, smoothing of their surfaces, predominance of large spread macrophages, and impairment of the intracellular cooperation. The macrophage alteration under the action of prednisolone was less pronounced. Prodigiozan, a bacterial polysaccharide (0.5 mg/kg) administered on the 4th and 9th days of the immunosuppression increased the macrophage resistance mainly to the damaging effect of prednisolone and was low effective after administration of azathioprine. The effect of lysozyme injected intramuscularly in a dose of 0.5 mg/kg daily within a period of the 3rd to the 10th days of the use of the immunosuppressants was evident from activation of the surface structures of the small macrophages and lymphocytes and reduction of cell alterations independent of the type of the immunosuppressants used. This indicates the necessity of a differential approach to the use of the macrophage activators for correcting the decreased infection resistance after medicamentous immunosuppression.

巨噬细胞表面结构的状态与巨噬细胞的功能能力密切相关。用扫描电镜观察氮唑嘌呤(60 mg/kg)、强的松龙(50 mg/kg)或它们的联合(分别为25和30 mg/kg)免疫抑制10天小鼠的腹腔巨噬细胞。硫唑嘌呤,特别是与强的松龙联合使用,可引起巨噬细胞和淋巴细胞明显的退行性反应,使其表面光滑,大扩散巨噬细胞占优势,细胞内合作受损。强的松龙作用下巨噬细胞的改变不明显。在免疫抑制第4天和第9天给予细菌多糖Prodigiozan (0.5 mg/kg)增加巨噬细胞的耐药性,主要是由于强的松龙的破坏作用,而在给予硫唑嘌呤后效果较低。在使用免疫抑制剂的第3天至第10天内,以每天0.5 mg/kg的剂量肌内注射溶菌酶的效果是明显的,从激活小巨噬细胞和淋巴细胞的表面结构和减少细胞改变来看,与所使用的免疫抑制剂的类型无关。这表明有必要采用不同的方法来使用巨噬细胞激活剂来纠正药物免疫抑制后感染抵抗力的下降。
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引用次数: 0
[Kanamycin concentrations in liver tissue and bile in acute experimental cholecystocholangiohepatitis]. [急性实验性胆囊胆管性肝炎患者肝组织和胆汁卡那霉素浓度]。
Pub Date : 1984-11-01
A V Alekseenko, A G Iftodiĭ, R V Seniutovich, I I Sidorchuk, S I Palianina

The levels of kanamycin in the bile and liver tissue were studied on 10 healthy dogs and 10 dogs with experimental acute abacterial cholecystocholangiohepatitis. It was shown that bile excretion of kanamycin in the dogs increased 6-7 times with development of acute inflammation in the biliary system.

研究了10只健康犬和10只实验性急性非细菌性胆囊胆管性肝炎犬胆汁和肝组织中卡那霉素的含量。结果表明,随着胆道系统急性炎症的发展,狗的胆汁卡那霉素排泄量增加了6-7倍。
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引用次数: 0
[Interaction of rifampicin with hepatocyte organoids in rats and its intracellular distribution]. [利福平与大鼠肝细胞类器官的相互作用及其细胞内分布]。
Pub Date : 1984-11-01
A E Guliaev, G Ia Kivman

Interaction of rifampicin with isolated subcellular fractions of the rat liver (binding and dissociation of the complexes) and intracellular distribution of the antibiotic were studied in the presence of the main organoids taken in the ratio close to the natural volume ratio of the hepatocyte cell components. The nuclei and mitochondria were most active during drug binding. The microsomes were less important. Rifampicin formed mobile complexes with organoids and was easily released from the subcellular fractions recovering its activity on washing. The intracellular distribution was the following: 37.7 per cent of rifampicin in the active form was accumulated in cytosol and the remaining amount was reversibly bound in the fractions of the nuclei, mitochondria and microsomes. The characteristic features of the cell pharmacokinetics of rifampicin, i.e. significant concentration in cytosol, possible deposition in the subcellular structures and at the same time the capacity for recovery of the activity might define the antimicrobial potential of this antibiotic in respect to the intracellular microorganisms.

研究了利福平与分离的大鼠肝脏亚细胞组分的相互作用(复合物的结合和解离)和抗生素的细胞内分布,主要类器官以接近肝细胞成分的自然体积比的比例存在。细胞核和线粒体在药物结合过程中最为活跃。微粒体就不那么重要了。利福平与类器官形成可移动的配合物,并且很容易从亚细胞组分中释放出来,在洗涤后恢复其活性。细胞内分布如下:37.7%的活性利福平积聚在细胞质中,其余的利福平可逆地结合在细胞核、线粒体和微粒体的部分中。利福平的细胞药代动力学特征,即在细胞质中的显著浓度,可能沉积在亚细胞结构中,同时恢复活性的能力,可能定义了这种抗生素在细胞内微生物方面的抗菌潜力。
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引用次数: 0
[Nutrient medium for determining the biological activity of heliomycin]. [测定heliomycin生物活性的营养培养基]。
Pub Date : 1984-10-01
E M Bershteĭn, N G Vasil'eva, M S Poliak, V M Grigor'eva, L N Astanina

It was shown that a nutrient medium containing only salt components except agar-agar could be used for assay of the biological activity of heliomycin. The optimal results were observed on the medium containing ammonium chloride, urea, disubstituted sodium phosphate, glucose and agar-agar. The medium provided satisfactory growth of Bac. subtilis ATCC 6633 as the test culture and formation of clear inhibition growth zones of the sufficient size. The medium is standard and its use allows obtaining reproducible results in assay of the heliomycin biological activity.

结果表明,除琼脂外,仅含盐组分的营养培养基可用于测定heliomycin的生物活性。在含氯化铵、尿素、二取代磷酸钠、葡萄糖和琼脂的培养基上观察到最佳效果。培养基提供了令人满意的Bac生长。以枯草杆菌ATCC 6633为试培养物,形成了足够大小的明显抑制生长带。该培养基是标准的,它的使用允许在测定heliomycin生物活性中获得可重复的结果。
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引用次数: 0
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Antibiotiki
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