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Biomedical subjects

Z Simon

Publications and source records attributed to Z Simon.

At least 37 records · Page 2Linked to original sources

[Recurrence prevention of papillomas of the bladder using lycurim instillation].

Following surgical removal of papillary tumours of the bladder from 60 patients the authors performed short instillations of the bladder with LYCURIM. The histological picture revealed tumours in the stage O-A-B1 and grade I-II-III. In a control group (n = 129) 89 recidive cases were observed in 2 years. Out of the 60 patients of the LYCURIM group 19 (31.7%) were free of tumours for 2 years and 43 (71.7%) for 11/2 years. A transient cystitis which occurred with short application of the medicament was easily cured. Toxic effects on the blood picture were not observed.

Administration, Topical↗

Steric mapping of some prostaglandin receptor sites.

The Minimal Steric (Topologic) Difference method was applied to map some prostaglandin receptors. Experimental data concerning luteinizing activity of corpora lutea, and pressor respectively depressor activity on sheep blood were considered. The linear correlation coefficients obtained were r = 0.927 (N = 12) for luteinizing activity, r = 0.943 (N = 15) for depressor activity, and r = 0.943 (N = 12) for pressor activity. Similarities and differences between these three receptors are discussed.

Allosteric Site↗

[Importance of a persisting left vena cava superior in pacemaker therapy (author's transl)].

Basing on the description of a specific case and a review of literature, the article discusses the relationship between persisting left ven cava superior and pacemaker therapy. The article covers the technical problems caused by the vascular anomaly, the complications which can be expected, the possibilities in respect of recognising the vascular anomaly, as well as the methods for coping with the special situation prevailing in a particular case.

Aged↗

The effect of deoxycorticosterone on the interstitial fluid pressure in normal rats.

Interstitial fluid pressure was measured by Guyton's capsular method in the subcutaneous tissue of rats after a single DOC i.p. injection. Regardless of the dose of DOC, the pressure-time curve showed three phases: latency, decrease and recovery. The maximum drop in pressure and the recovery time were dose-dependent. Maximum decrease in interstitial fluid pressure after 0.25; 0.50; 0.75; 1.00 mg/100 g body wt of DOC was 3.2; 7.1; 9.2 and 10.6 mmHg, respectively. It was found that the recorded pressure response is not exclusively caused by Starling forces. A correlation was found between the pressure decrease and the extracellular potassium loss. The role of potassium in the DOC-induced pressure response was verified by administration of the specific potassium ionophore, valinomycin. Due to the effect of valinomycin, potassium ion transport and, as a consequence, the interstitial pressure response, were accelerated.

Animals↗

[Analysis of histochemical changes caused by acute Wofatox poisoning in a model experiment].

Effect of Wofatox on the central nervous system, striated muscles and on the myocardium of rats has been studied by the aid of light- and electron microscopic histochemistry. A single intraperitoneal injection of LD50 of Wofatox resulted in a total inhibition of the activity of histochemically demonstrable acetyl-cholinesterase in the central nervous system. Each striated muscle fiber has shown different sensitivity to the inhibitor, but enzyme activity of end motor plates could not be totally inhibited. In lethal acute intoxication ultrastructural changes of the myocardiuim have shown characteristic features of cardiomyopathy.

Acute Disease↗

Quantitative structure-activity relationships in erythromycin group with MTD technique.

Quantitative structure-activity correlation studies were performed for a group of 17 erythromycin derivatives modified in the C-8--C-12 portion of the molecule. The minimal steric difference, MTD, was used as the structural parameter and logarithm of the biological potency measured by a standard assay, as the biological parameter. The influence of the sp2 hybridization at C-9 and of the presence of 11, 12-carbonate grouping on the antibacterial activity was shown. The reported results give a further support to our hypothesis on greater complementarity of the cyclic 11, 12-carbonates in the reaction on the bacterial ribosomes in comparison with their parent antibiotics.

Bacillus↗

[Histochemical analysis of the multiple effect of organophosphorous compounds (Wolfatox, DFP) in rats (author's transl)].

In vivo effects of Wofatox and DFP has been studied by light and electron microscopic histochemical methods in the central nervous system, in cardiac and striated muscles of rats. Singleintraperitoneal injection of Wofatox and DFP LD50 resulted in complete inhibition of the histochemically detectable acetyIcholinesterase (AChE) activity in the central nervous system. Various striated muscles exhibit different degrees of sensitivity towards inhibitors, neither can the enzyme activity of some motor end plates be completely inhibited. In addition to AChE inhibition in striated muscles, organophosphorous compounds induce also subacute myopathic changes. In the case of a lethal intoxication, ultra-structural alterations suggesting myocardial lesion can be observed.

Acetylcholinesterase↗

Potential anticancer agents. XX. 1. Steric fit analysis in aromatic nitrogen mustards area.

A series of 31 aromatic nitrogen mustards was treated by means of the Minimal Tropological Difference (MTD)-receptor site mapping procedure by respect to toxicity (LD50) and efficacy (TGI%) against Jensen sarcoma. The correlation equations obtained for the two cases are: (Formula: see text), The low correlation coefficients indicate a not too high dependence upon steric factors of TGI% and LD50. However these results suggested that: a) the ortho-substitution represents a favorable event for both toxicity and antitumor effectiveness (j = 1 and 18 being good vertices in both corresponding hypermolecules), b) despite this effect, the steric features involved in these two biologic parameters seems to be different.

Animals↗

Potential anticancer agents. XX. 2. Quantitative structure--activity relationships (QSAR) in aromatic nitrogen mustards area.

Quantitative structure--activity relationships have been fomulated for 27 aromatic nitrogen mustards derived from benzoic acids (9 monosubstituted and 18 disubstituted derivatives). Their toxicity (LD50) and antitumor activity against Jensen sarcoma were correlated with hydrolysis rate (log k66) lipophilicity constants (pi) and steric parameters (MDT). The chemical reactivity of the nitrogen mustard moiety (expressed as log k66) seems to be of main importance in determining the biological properties of these derivatives. The favorable effect of ortho-substitution was pointed out. Generally these results are in good agreement with those obtained by HANSCH et al. [7] on a different series of nitrogen mustards.

Animals↗