Cholinesterase inhibitory effects of the extracts and compounds of Maclura pomifera (Rafin.) Schneider.

We have investigated anticholinesterase potential of the methanol extracts from the leaf, wood, flower, twig, and stem bark of the female and male individuals and rhizodermis and fruit from the female tree of Maclura pomifera (Rafin.) Schneider (Moraceae) along with its major isoflavonoids; osajin and pomiferin as well as their semi-synthetic derivatives; iso-osajin and iso-pomiferin. Anticholinesterase activity was determined by Ellman method using ELISA microplate reader. Osajin and pomiferin had a noticeable inhibition of AChE with IC(50) values of 2.239 and 0.096 mM, respectively, while their iso-derivatives were found to display less inhibition towards AChE. The extracts and compounds did not inhibit BChE. The extracts were analyzed for osajin and pomiferin contents by LC-DAD-MS and only the fruits and female flowers contained osajin (fruit: 8.87%, female flowers: 0.19%, w/w) and pomiferin (fruit: 13.6%, female flowers: 0.36%, w/w).

[Adsorption of substances on active charcoal. Part 2: basic esters of phenylcarbamic acid with beta-adrenolytic effect]. / Adsorpcia látok na aktívne uhlie 2. cast. Bázické estery kyseliny fenyl- karbámovej s beta-adrenolytickým úcinkom.

The paper is concerned with the study of adsorption on active charcoal in a set of selected substances from the group of aryloxyaminopropanol derivatives with carbamate substitution on the benzene ring with beta-adrenolytic effect (Group A) and a set of substances, derivatives of [(arylcarbonyl)oxylaminopropanol with the identical, but assumed ultra-short effect (Group B), where the effect was produced by replacing the phenolether group with a metabolically unstable ester functional group. The course of adsorption in buffer solution with pH 7 in dependence on time and concentration is examined. Adsorptivity of substances is evaluated according to Freundlich and Langmuir models. Affinity of substances of Group A to adsorption material decreases with increasing hydrophilicity.

[Testing bradycardial effects of a newly synthesized ultra-short beta blocker in laboratory rats]. / Testování bradykardického úcinku nove syntetizovaných potenciálních ultrakrátkých beta blokátoru na laboratorním potkanovi.

With the use of normotensive laboratory Wistar strain rats, changes in heart rate induced by three newly synthesized potential ultrashort beta-blockers were tested. The animals were administered the tested substances intravenously in general anesthesia. In all animals, heart rate was measured at predetermined time intervals. All obtained values were converted into the per cents of the heart rate deviation and the results were statistically processed. Using F-test, variability of dispersion was determined, and using Student t-test, statistical significance of the particular change was determined. In all three substances tested, a statistically demonstrable short-time bradycardiac effect was observed. The most marked decrease took place in the first minute after intravenous administration. Substance 44Bu induced the significantly deepest decrease in heart rate (by 13.00%), which lasted longest. No statistically significant difference was found between the actions of substances 42Bu and 43Bu. In all three substances tested, marked changes in the ECG record were observed immediately after intravenous administration. PQ and QT intervals and QRS complex were prolonged, and marked S wave, elevation of the T wave, and a decrease in R wave occurred. The changes were accompanied by a change in the electric cardiac axis.

Synthesis and pharmacological evaluation of novel potential ultrashort-acting beta-blockers.

The basic relationship between chemical structure and pharmacological activity of eight newly developed potential ultrashort-acting beta-adrenergic blockers was evaluated. The compounds studied are derivatives of arylcarbonyloxyaminopropanols and were prepared by four-step synthesis. All the compounds evaluated showed weak antiisoprenaline (beta-adrenergic receptor blocking) activity and antiarrhythmic (antiouabain) activity.

[Preparation and physico-chemical properties of alkyl esters of 2-, 3-, 4-(2-hydroxy-3-[4-diphenylmethyl) piperazine-1-yl] propoxy) phenylcarbamide]. / Príprava a fyzikálne chemické vlastnosti alkylesteru kyseliny 2-, 3-, 4-(2-hydroxy-3-[(4-difenylmethyl)piperazin-1-yl] propoxy) fenylkarbamové.

The paper is devoted to the synthesis and study of some physico-chemical properties of a group of substances--potential antagonists of beta-adrenergic receptors. The substances are derivatives of aryloxyaminopropanol, where the basic part consists of diphenylmethylpiperazine and the aromatic part is modified with alkyl esters (methyl to butyl) of carbamic acid in positions 2-, 3-, 4-. The representation of the elements was confirmed by elemental analysis. The substances were characterized by melting point, IR and UV spectra. Their solubility and surface activity were determined. The purity of prepared substances was examined by means of TLC.