Czech and Slovak Pharmacy, 2003 (vol. 52), issue 6
Articles
A Novel Group of Potential Antituberculotic Agents: Antimycobacterial N-Benzylsalicylamides
K. Waisser, M. Peřina, I. Boudová, J. Kuneš, J. Kaustová
Čes. slov. farm. 2003, 52(6)
Linking up with a previous study of antimycobacterial compounds, several groups of N-benzylsalicylamideswere prepared and their antimycobacterial activities against the strains Mycobacteriumtuberculosis,Mycobacterium kansasii, and Mycobacterium aviumwere evaluated.The obtained datawere analyzed by Free-Wilson method in comparison with their isosteric analogues of 3-hydroxypicolinicand 2-sulfanylbenzoic acids described in the previous communication.
A New Strategy of Therapeutic Drug Monitorining of Cyclosporine A Blood Levels inPatients after Renal Transplantation
M. Halačová, B. Jedličková, R. Průša
Čes. slov. farm. 2003, 52(6):267-271
Cyclosporine A (CyA), tacrolimus (FK 506), and mycophenolic acid are routinely utilised immunosupressivedrugs used in the prevention of allograft rejection and the treatment of several autoimmunediseases. The monitoring of CyA blood levels plays the most important role to individualizethe dosage regiment and to minimize acute rejection risk and drug toxicity. Inadequate low CyAdoses and levels may result in the rejection of transplanted organs.Toxic levels of CyA are associatedwith many serious side effects, including nephrotoxicity, hepatotoxicity, and a range of othercomplications. In the period of 1999-2002, 12 859 analyses of whole blood CyA levels...
Biological Effects of Resveratrol and Other Constituents of Wine
P. Kollár, H. Hotolová
Čes. slov. farm. 2003, 52(6):272-281
In recent years many scientific papers have been published concerning the positive effects of wineand its active principles, the polyphenol resveratrol being the most widely discussed compound. Theresults of epidemiological and experimental studies in man, animals, and in vitro have shown thatpolyphenols contained in wine, tea, fruit, and vegetables exert a positive effect on both the progressionand regression of atherosclerosis, possess an anticancerogenic action, and due to theirantioxidative effects they act against other processes connected with the reactive forms of oxygenproduction and lipid peroxydation in the blood plasma and membranes. Experimental...
Biologically Active Benzoxazoles
J. Vinšová
Čes. slov. farm. 2003, 52(6):282-290
This review presents a survey of preparations and biological activities of substituted benzoxazoles. The structural similarity of benzoxazole derivatives with nucleic bases, such as adenine andguanine, probably allows their easy interaction with biopolymers in the living systems. Consequently, these compounds posses a wide range of biological activities. Their preparation includes cyclocondensation reactions and contractions of ortho-fused heterocycles or their photochemical rearrangement. They are being studied predominantly for their antibacterial, antifungal, antiviral, and antitumor activities, and also as insecticides, herbicides, anthelmintics,...
The Release of Diltiazemiumchloride and Ibuprofen from Hydrophilic Matrix Tablets
L. Vostalová, M. Rabišková, G. Medvecká
Čes. slov. farm. 2003, 52(6):295-298
Hydrophilic matrix tablets based on hydroxypropylmethylcellulose (HPMC) and other cellulosederivatives rank among dosage forms with retarded effect widely used in contemporary pharmacotherapy.The active ingredient is released from them in dependence on its properties either bydissolution and diffusion, or erosion of the compact. The dissolution profile of the active ingredientcan be influenced by variables of formulation and manufacture, e.g. by the type of HPMCemployed,its concentration, other added auxiliary substances, and compression force which is reflected in thestrength of tablets.Two drugs with different solubility were used to study the effect...
Solubilization of Unilamellar Egg Yolk Phosphatidylcholine Liposomes by N-Alkyl-N,NdimethylamineN-oxides
A. Hrubšová, J. Karlovská, F. Devínsky, I. Lacko, P. Balgavý
Čes. slov. farm. 2003, 52(6):299-305
The solubilization of extruded (100 nm) unilamellar egg yolk phosphatidylcholine (EYPC) liposomesby a series of N-alkyl-N,N-dimethylamine N-oxides (CnNO, n=10-14 carbon atoms in the alkylsubstituent) was studied using turbidimetry. The solubilizing concentration of CnNO (cS) wasestimated as the CnNO concentration causing the half-maximum decrease in turbidance. From thelinear cS dependence on EYPC concentration, the lipid - aqueous phase molar partition coefficient(Kp) and theCnNO:EYPCmolar ratio in theCnNO+EYPCaggregates (nL:nEYPC) at cS wereobtained:Kp=82±25 and nL:nEYPC =0,70±0,20 for C10NO, Kp=507±215 and nL:nEYPC =0,60±0,16...
Anticomplementary Activity of Saponins from Cynara cardunculus L.
P. Mučaji, M. Bukovský, D. Grančai, M. Nagy
Čes. slov. farm. 2003, 52(6):306-309
Triterpene saponins of ursane and oleane type isolated from the involucral bracts of Cynara cardunculus L. (Asteraceae) were investigated in in vitro assays for their activity on the complement system. The anticomplementary activity of bidesmosidic saponins on the classical pathway activation of the complement was higher than the activity of monodesmosidic saponins, but esterificationof the carboxylic group of glucuronic acid in the sugar residue resulted in a significant decrease in anticomplementary activity.