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Biomedical subjects

E Grunberg

Publications and source records attributed to E Grunberg.

At least 19 recordsLinked to original sources

Activity of oral amoxicillin, ampicillin, and oxytetracycline against infection with chlamydia trachomatis in mice.

The effects in mice of oral treatment with amoxicillin, ampicillin, and oxytetracycline against an otherwise lethal intranasal infection with Chlamydia trachomatis (mouse pneumonitis) were studied. When treatment was started 30 min after infection and continued once daily thereafter for a total of seven treatments, the mean protective doses of amoxicillin, ampicillin, and oxytetracycline were 9.5, greater than 50, and 31.3 mg/kg, respectively. If 14 oral treatments were given, these values were 1.6 mg/kg for amoxicillin, 12.7 mg/kg for ampicillin, and 12.3 mg/kg for oxytetracycline.

Administration, Oral↗

In vivo activity of amoxicillin and ampicillin against gram-positive bacteria: results of prophylactic studies.

In prophylactic treatment of intraperitoneal infections with Streptococcus pneumoniae (types 1 and 2) and Streptococcus pyogenes in mice, amoxicillin had a definite advantage over ampicillin in terms of protective effect. When the infecting agent was given to mice so as to produce an infection in the brain or lung (for example, S. pneumoniae given intracranially or intranasally), amoxicillin was also more effective prophylactically than ampicillin.

Administration, Intranasal↗

Activity of 10-chloro-5-(2-dimethylaminoethyl)-7H-indolo [2,3-c]-quinolin-6(5H)-one hydrochloride against experimental tumors in mice and rats.

10-Chloro-5-(2-dimethylaminoethyl)-7H-indolo [2,3-c]-quinolin-6(5H)-one hydrochloride (CIQ) was shown to exert significant antitumor activity against the Ehrlich carcinoma and sarcoma 180 transplantable tumors in mice by the intraperitoneal (ip) or oral (po) routes and when incorporated into diet. A solid tumor induced in BALB/c mice by the subcutaneous (sc) implantation of nonproducer murine sarcoma virus-transformed BALB/3T3 cells was also inhibited by CIQ after ip or po treatment but there was no effect against leukemia L1210 ascites or a transplantable murine renal adenocarcinoma. When tested in rats, CIQ significantly reduced the growth of Flexner-Jobling carcinoma, Murphy-Sturm lymphosarcoma and Walker 256 carcinosarcoma when administered by the ip or po routes. Pretreatment, but not posttreatment, with CIQ slightly inhibited the humoral antibody response of mice to sheep red blood cells. CIQ therefore differs from immunosuppressive agents such as imuran, methotrexate, cytosine arabinoside, or 6-mercaptopurine which affect the antibody response of mice to sheep erythrocytes when administered after immunization.

Adenocarcinoma↗

Studies on the in vitro development of drug resistance of Proteeae to sulfonamides, trimethoprim and combinations of a sulfonamide and trimethoprim.

A strain of Proteus mirabilis repeatedly subcultured in the presence of a combination of sulfisoxazole and 0.4 microgram/ml of trimethoprim and a strain of P. vulgaris subcultured in the presence of sulfamethoxazole and trimethoprim combined in a 5:1 ratio gradually developed resistance to the combinations. However, the level of resistance developed by the organisms exposed to the combination was always appreciably lower than the level of resistance developed by the same strains exposed to either the sulfonamide or trimethoprim alone.

Drug Combinations↗

Antiviral activity of 10-carboxymethyl-9-acridanone.

Intraperitoneal administration of 10-carboxymethyl-9-acridanone sodium salt (CMA) protected at least 50% of mice tested from otherwise lethal infections with Semliki forest, coxsackie B1, Columbia SK, Western equine encephalitis, herpes simplex, and pseudorabies viruses. The protective effect against influenza A2/Asian/J305 and coxsackie A21 viruses was less but was statistically significant. When administered either subcutaneously or orally, CMA protected at least 50% of mice against Semliki forest and pseudorabies viruses; the effect against coxsackie B1 and herpes simplex viruses was less but was statistically significant. Initiation of treatment could be delayed from 2 to 24 h after infection of mice with coxsackie B1, herpes simplex, Semliki forest, and Western equine encephalitis viruses without loss of an antiviral effect. CMA did not inactivate Semliki forest or coxsackie B1 viruses on contact and was without effect against any of the viruses tested in tissue culture by the tube dilution assay. The humoral antibody response in mice to both influenza virus and sheep erythrocytes was unaffected by CMA. After administration of CMA, an interferon-like substance was induced in mice or mouse cell culture but not in rabbits or rabbit cell culture.

Acridines↗

In vivo synergy between 6 beta-amidinopenicillanic acid derivatives and other antibiotics.

Both an oral and a parenteral form of a 6beta-amidinopenicillanic acid derivative were found to have appreciable activity against gram-negative bacteria and poor activity against gram-positive bacteria in vivo. When administered orally or parenterally, definite synergy was demonstrated between the amidinopenicillins and ampicillin, amoxicillin, benzylpenicillin, cefazolin, or carbenicillin in infections with a number of gram-negative bacteria, including Klebsiella, Enterobacter, Escherichia, Proteus, Salmonella, and Haemophilus species in mice. Synergy was also observed between the parenteral amidinopenicillin and benzylpenicillin in the Staphylococcus aureus infection but not in infections with other gram-positive organisms. No synergy was demonstrated between the parenteral amidinopenicillin and erythromycin or oxytetracycline in infections with gram-positive or gram-negative organisms. Synergy between the parenteral amidinopenicillin and gentamicin was observed only in the case of Escherichia coli.

Animals↗

Detection of drugs of abuse by radioimmunoassay: a summary of published data and some new information.

We review the status of radioimmunoassays for detection of abused drugs. Individual assays with use of 125I-labeled antigens are all performed in an identical manner and can be completed in 30 min to 1 h. Combined assays for simultaneous detection of two or more such drugs or assays in which a tritium-labeled antigen is used require 1-2 h for completion. All tests can be performed with 0.1 ml or less of specimen. The assays involving 125I reliably detect urinary concentrations of, per liter, 40-100 mug of morphine, 100 mug of barbiturates, methadone, methaqualone, or benzoylecgonine, and 1000 mug of amphetamine. The assay for morphine involving 3H detects 60 mug/liter. Each assay is capable of providing a qualitative and quantitative estimate of the drugs sought. The 125I-labeled antigens have a usable shelf life of at least two to four months after the antigen is iodinated; the tritium assay is stable for six months. The assays can be performed with use of paper discs that have been suspended in urine and then dried, in place of the liquid specimen. The assays appear to be equally applicable to detection of drugs in urine, blood, saliva, and tissues. All of them are done at ambient temperature and can be used equally well for emergency (stat) tests or mass screening. Except for the benzoylecgonine assay, the clinical reliability of these tests has been demonstrated.

Amphetamine↗

Ellipticine derivatives.

Several acyloxy and alkyl derivatives of ellipticine have been prepared. In addition, a modified synthesis leading to the hitherto unobtainable 8,9-dimethoxy- and 8,9-methylenedioxyellipticines is described. Some of the derivatives described herein exhibit antitumor activity. However, none of the compounds showed activity superior to that of the naturally occurring pyridocarbazoles, ellipticine and 9-methoxyellipticine.

Alkaloids↗

Mersalyl: a diuretic with antiviral properties.

Mersalyl (Salyrgan), an organic mercurial diuretic, was tested against human and animal viruses with in vivo model infections in mice and tissue culture systems. Mersalyl was active against coxsackieviruses A21 and B1 in mice if administered intraperitoneally immediately after infection. No effect was observed if intraperitoneal treatment was delayed 1 or 2 h postinfection, or if treatment was administered either subcutaneously or per os. Topical treatment with a 5% aqueous solution of mersalyl produced a statistically significant effect against herpes simplex dermatitis in mice but the substance was inactive against systemic infections in mice with herpes simplex as well as Columbia SK, influenza, Semliki Forest, and Sendai viruses. Contact inactivation of coxsackieviruses A21 and B1 and herpes simplex virus was observed, but mersalyl was inactive in tissue culture against coxackieviruses A21 and B1, herpes simplex, influenza, rhinovirus, Semliki Forest, Sendai, and vaccinia viruses.

Animals↗

Simultaneous detection of morphine and barbiturates in urine by radioimmunoassay.

This report describes a radioimmunoassay for the simultaneous detection of morphine and barbiturates. Morphine and barbiturate antibodies, obtained from goats, were mixed with 125l-labeled antigens. By adjusting concentrations of the morphine and barbiturate antibodies and radiolabeled antigens, closely superimposed standard curves for the two drugs would be obtained. As a consequence, similar response curves were obtained for urine specimens containing morphine or barbiturates. Although concentrations as low as 25 mug/liter could be measured, to ensure against false positive reactions the test should be performed at the 100 mug/liter concentration. Unknown samples positive by the dual assay were confirmed by separately testing the specimens with the individual radioimmunoassay specific for morphine or barbiturate. Equivalency tests of urines positive for morphine, positive for barbiturates, or negative for both demonstrated complete correlation between the single and dual assays. The mixed reagent retained its sensitivity and specificity for at least three months when stored at 4 or 25 degrees C. The dual radioimmunoassay is a rapid, simple procedure that can be adapted to automated processes and that is suitable for large- and small-scale screening.

Barbiturates↗

Biochemical and genetic basis of tetracycline resistance in Staphylococcus aureus.

Both the genetic and biochemical basis of tetracycline resistance in a number of staphylococcal strains was investigated. The strains examined could be classified into three groups: (i) those possessing a high basal level of resistance and in which resistance could be induced to higher levels (macro-inducible); (ii) those which had a high uninduced level of resistance, but which were virtually uninducible (macro-constitutive); (iii) one derivative which had a low basal level of resistance and was also uninducible (micro-constitutive). Resistance in macro-constitutive strains was plasmid mediated and typical of organisms possessing wild-type plasmids. The macro-constitutive pattern of resistance appeared to be correlated with a chromosomal location for the resistance genes, whereas the micro-constitutive pattern was correlated with loss of a region from the wild-type plasmid. Analysis of membrane proteins by sodium dodecyl sulfate polyacrylamide gel electrophoresis suggested that a number of membrane polypeptides became unstable in staphylococci possessing high-level tetracycline resistance. In particular, the absence of a polypeptide of 22,000 daltons was always associated with high-level resistance. There was no evidence that multiple gene copies are required for expression of tetracycline resistance in Staphylococcus aureus.

Gene Expression Regulation, Bacterial↗