Czech and Slovak Pharmacy, 1999 (vol. 48), issue 6
Articles
The Use of the Concept of the Pharmacophore in Drug Design
M. Smieško, M. Remko
Čes. slov. farm. 1999, 48(6):247-251
The application of the pharmacophore concept to design new drugs is discussed. The focus is on theapplication of computer-assisted drug design methods (CADD) in the discovery of new leads.
Chalcones and Their Heterocyclic Analogues as Potential Antifungal Chemotherapeutics
V. Opletalová, D. Šedivý
Čes. slov. farm. 1999, 48(6):252-255
Chalcones and their heterocyclic analogues show various biological effects, e.g. anti-inflammatory, antitumour, antibacterial, antituberculous, antiviral, antiprotozoal, gastroprotective, and others.The present review discusses in greater detail the fungistatic and fungicide properties of these compounds and presents also their chemical structures. The mechanism of antifungal effects of chalcones and their analogues has not been investigated in greater detail. Due to the presence of a reactive ketovinyl moiety in the molecule the compounds of this type are able to react with the thiol groups of enzymes. It cannot be excluded that chalcones interfere...
Production of Anthracene Derivatives by the Elicited Tissue Culture of Rheumpalmatum L.
M. Kašparová, T. Siatka
Čes. slov. farm. 1999, 48(6):256-261
With a few exceptions, the characteristic problem of cultivation of plant explants in in vitro culturesis a low production of secondary metabolites by these cultures. One of the methods, which canachieve an increase in the production of natural substances in in vitro cultures, is elicitation of cellcultures. The effect of the biotic elicitor Pseudomonas aeruginosa in the form of a homogenate andan aqueous suspension of dead cells on the production of anthracene derivatives by the tissue cultureof Rheum palmatum L. of different age and origin was examined. The culture was cultivated ona Murashige-Skoog medium with an addition of 10 mg.l-1 of a-naphthylacetic...
The Use of the Elicitor from Pseudomonas aeruginosa on the Production of Flavonoids by the Culture of Ononis arvensis L. in vitro
L. Tůmová
Čes. slov. farm. 1999, 48(6):262-264
The effect of the elicitor, killed cells of Pseudomonas aeruginosa, on the production of flavonoids by a callus and a suspension culture of Ononis arvensis L. was examined. The tested elicitor influenced the flavonoid production both in the callus and suspension culture. An increased content of flavonoids in the callus culture was observed with the use of the elicitor in concentrations I and II (5.81.10-2 and 5.81.10-4 g/l). The maximal production took place after a seven-day elicitation with concentration II. This production was higher by 83 % as compared with the control. In suspension cultures an increased production was observed in concentrations...
Determination of Selected Secondary Metabolites and Extractive Substances in Phila-delphus coronarius L.
D. Grančai, P. Mučaji, M. Nagy
Čes. slov. farm. 1999, 48(6):265-267
The paper deals with the determination of selected secondary metabolites in the branches and leaves of Philadelphus coronarius L. Colorimetric methods were employed to determine the content of flavonoids (0.63 % and 0.01 %, respectively) and phenolic substances (3.25 % and 0.70 %, respectively) in leaves or branches. Also the content of extractive substances was determined in ethanolic, aqueous-ethanolic (85 % and 60 % ethanol), and aqueous extracts. This yielded 9.56 %, 22.46 %, 24.93 %, and 33.15 % of extractive substances in leaves and 2.20 %, 6.04 %, 8.84 %, and 10.39 % of extractive substances in branches.
Effect of Biotic Elicitors on the Production of Flavonoids in Suspension Culture of Bellisperennis L.
T. Siatka, M. Kašparová
Čes. slov. farm. 1999, 48(6):268-271
The effect of two biotic elicitors (homogenates of Pseudomonas aeruginosa and Candida utilis) in a suspension culture of Bellis perennis L. cultivated in the dark and day light period were examined. The growth of the culture was not negatively affected by the action of elicitors. Increased productionof flavonoids in the culture depended on the sort, concentration and space of time of action of the elicitor, and on the manner of cultivation from the viewpoint of the light regimen. The best results were achieved with the use of the homogenate of Candida utilis after 24 hours in cultivation under the day light period and after 48 hours in cultivation...
In vitro Effect of Quinolones on Hydrophobicity of Acinetobacter baumannii
A. Hoštacká
Čes. slov. farm. 1999, 48(6):272-275
Effects of subinhibitory concentrations (sub-MICs) (1/4, 1/8, 1/16 or 1/32 of the MICs) of fourquinolone antibiotics on surface hydrophobicity of two Acinetobacter baumannii strains (R1 and R2) were tested. Hydrophobicity was evaluated by adherence of bacteria to xylene and their aggregationin ammonium sulphate solutions. Norfloxacin in concentrations of 1/4 or 1/8 of the MIC decreasedhydrophobicity of R1 strain and of R2 strain in concentration of 1/16 of the MIC. Ciprofloxacin was efficient for both strains mainly in concentration of 1/4 of their MICs. Enoxacin (1/8 MIC) more effectively reduced hydrophobic properties only in R2 strain. The other...
Studies of Local Anaesthetics CL. Models of Dependence of Local Anaesthetic Effectiveness of Basic Esters of Alkoxy-substituted Phenylcarbamic Acids on the Capacity Factor k'
J. Čižmárik, J. Lehotay, A. Bednáriková, K. Hroboňová
Čes. slov. farm. 1999, 48(6):276-280
On the basis of proposed six models of the dependence of local anaesthetic effectiveness of series ofalkoxysubstituted derivatives of phenylcarbamic acid, this activity was studies in dependence onthe capacity factor k' as the parameter of lipophilicity. The most suitable models proved to be y =(Cx + Ci).k' for surface anaesthesia, and y = Cx + Ci log k' for infiltration anaesthesia, y being thevalue of the decadic logarithm of surface or infiltration local anaesthetic activity, Cx the coefficientcharacterizing the nitrogenous base, Ci the coefficient characterizing the individual alkoxygroups,and k' the capacity factor from HPLC.
Substituted Benzo[b]thiophenes with Antileucotriene Activity
M. Nič, M. Havelková, M. Terinek, J. Paleček, J. Svoboda, A. Jandera, V. Panajotová, M. Kuchař
Čes. slov. farm. 1999, 48(6):281-286
The cyclizing reaction of cinnamic acid (Ia) with thionyl chloride was optimized and a series of 3-chloro-6-subst. benzo[b]thiophene-2-carbonyl chlorides Va-Vn was prepared. Chloride Va was transformed into a series of N-aryl-3-subst. (Cl, OCH3, OH) benzo[b]thiophene-2-carboxamides VII, IX, X. The drugs were subjected to an evaluation of selected antileucotriene activites in vitro and of the anti-inflammatory effect in vivo. In agreement with the assumed mechanism, inhibition of the ear inflammation is conditioned by the antileucotriene activity, whereas inhibition of the carrageenoedema is not due to this mechanism alone.
Dissolution and Supersaturation Episodes of Nimodipine in the Aqueous Solutions of the Cyclodextrins a-CD, HP-a-CD, M-b-CD, and HP-g-CD
F. Kopecký, B. Kopecká, P. Kaclík
Čes. slov. farm. 1999, 48(6):287-290
The dissolution curves of the substance of the calcium antagonist nimodipine in aqueous solutions of four cyclodextrins were determined at ambient temperature in the course of 14 days. The used cyclodextrins were a-cyclodextrin (a-CD), hydroxypropyl-a-cyclodextrin (HP-a-CD), methyl-b-cyclodextrin (M-b-CD, random-methylated), and hydroxypropyl-g-cyclodextrin (HP-g-CD) and their respective concentrations were always 0.05 mol/l. According to the measured dissolution curves, M-b-CD in aqueous medium was a highly efficient solubiliser, capable to dissolve otherwise sparingly soluble nimodipine into a time-stable aqueous solution, with the saturated concentration...
Czech Pharmaceutical Education under German Occupation in 1939-1945
L. Nováček
Čes. slov. farm. 1999, 48(6):291-293
When Czech universities were closed down in 1939, the already prepared reform of pharmaceuticalgraduate studies could not be implemented. The education of pharmacists, assistants, and aspirantswas taken over by the Central Union of Pharmacists through its departments, in particular theCzech Pharmaceutical Academy and the Czech Society of Pharmacists. Training of pharmaceuticalaspirants took place at the schools for aspirants in Prague and Brno. The experience obt ained atthese pharmaceutical courses and the new knowledge concerning drugs and pharmaceuticalpreparations provided by industry and research laboratories contributed to the improvement of...