New cerebrosides from Euphorbia peplis L.: antimicrobial activity evaluation

The less polar fraction of the methanolic extract from the plant Euphorbia peplis L. exhibited interesting antifungal and antitubercular activity. A complex mixture of four glucocerebrosides was responsible for this activity. Two new cerebrosides were isolated for the first time from Euphorbiaceae, 4 was assigned as 1-O-(beta-D-glucopyranosyl)-(2S,3S,4E,8E)-2N-[(2'R)-2'-hydroxy-hexadecanoyl]-4 (E), 8 (E)-octadecadiene-1,3-diol and 3 as the 1-O-(beta-D-glucopyranosyl)-(2S,3S,4R,8Z)-2N-[(2'R)-2'-hydroxytetracosanoyl]-8 (Z)-octadecene-1,3,4-triol. The structures were determined on the basis of chemical and spectroscopic evidences. Mass spectrometry of dimethyl disulfide derivatives was useful for the determination of the double-bond positions in the long-chain bases.     

PATTERN OF RNA SYNTHESIS IN RABBIT CORTEX DURING SLEEP

The pattern of RNA biosynthesis in rabbit cerebral cortex was examined during periods of physiological sleep and wakefulness monitored with EEG techniques. The types of newly synthesized RNA were analysed by sedimentation on sucrose gradients. In experiments lasting 60 and 105 minutes the labelling ratio of RNA sedimenting in two regions of the gradient (28 S-50 S50 S) increased with decreasing percentages of EEG synchronization. Analysis of the radioactivity distributions of five homogeneous experiments in terms of moments confirmed the dependence of the RNA synthetic pattern on the electric state of the cortex. The possible nature of the RNA species involved in this effect is discussed.     

DISAGGREGATION OF BRAIN POLYSOMES INDUCED BY ELECTROCONVULSIVE TREATMENT

—The ribosome–polysome equilibrium of rabbit cerebral cortex is considerably modified after elicitation of epileptic seizures by means of electroshock. Under this condition the number of free ribosomes increases approximately 80 per cent at the expense of a comparable decrease in the polysomal population.     

Antimycobacterial activity of new 3,5-disubstituted 1,3,4-oxadiazol-2(3H)-one derivatives. Molecular modeling investigations

3H-1,3,4-Oxadiazol-2-one derivatives were synthesized and tested for their in vitro antimycobacterial activity. Oxadiazolone derivatives showed an interesting antimycobacterial activity against the reference strain of Mycobacterium tuberculosis H₃₇Rv. Molecular modeling investigations were performed and showed that the active compounds possess all necessary features to target the protein active site of the mycobacterial cytochrome P450-dependent sterol 14α-demethylase in the sterol biosynthesis pathway as the calculated free energy of binding were in agreement with the corresponding MIC values.