Resveratrol inhibition of lipid peroxidation.

To define the molecular mechanism(s) of resveratrol inhibition of lipid peroxidation we have utilized model systems that allow us to study the different reactions involved in this complex process. Resveratrol proved (a) to inhibit more efficiently than either Trolox or ascorbate the Fe2+ catalyzed lipid hydroperoxide-dependent peroxidation of sonicated phosphatidylcholine liposomes; (b) to be less effective than Trolox in inhibiting lipid peroxidation initiated by the water soluble AAPH peroxyl radicals; (c) when exogenously added to liposomes, to be more potent than alpha-tocopherol and Trolox, in the inhibition of peroxidation initiated by the lipid soluble AMVN peroxyl radicals; (d) when incorporated within liposomes, to be a less potent chain-breaking antioxidant than alpha-tocopherol; (e) to be a weaker antiradical than alpha-tocopherol in the reduction of the stable radical DPPH*. Resveratrol reduced Fe3+ but its reduction rate was much slower than that observed in the presence of either ascorbate or Trolox. However, at the concentration inhibiting iron catalyzed lipid peroxidation, resveratrol did not significantly reduce Fe3+, contrary to ascorbate. In their complex, our data indicate that resveratrol inhibits lipid peroxidation mainly by scavenging lipid peroxyl radicals within the membrane, like alpha-tocopherol. Although it is less effective, its capacity of spontaneously entering the lipid environment confers on it great antioxidant potential.

[1,4-Disubstituted 1,3-dihydro-2H-1,5-benzo- and chlorobenzodiazepin-2-ones with activity on the central nervous system]. / 1,3-diidro-2H-1,5-benzo- e -clorobenzodiazepin-2-oni-1,4-disostituiti ad attività sul S.N.C.

In pursuing the study on pyridodiazepinone derivatives, in order to verify the variation of biological activity induced by replacement of the heteroaromatic with an aromatic nucleus and by the introduction of chlorine on the benzene ring, a series of 1-[(dialkylamino)alkyl]-4-phenyl-1,3-dihydro-2H-1,4-benzodiazepin- 2-ones and of 7-chloro-analogues were prepared. Some benzodiazepinones and their 7-chloro-analagous were subjected to pharmacological experimentation in order to evaluate and compare their effect upon mice with regard to exploratory activity, motor coordination and spontaneous motility. In addition their anti-strychnine, anti-cardiazole, anti-amphetamine and anti-reserpine activities were also evaluated.

[Pharmacologic activity of 5-[(dialkylamino)alkyl]-8-chloro-3,5-dihydro-2-methyl/phenyl-4H-pyrido[ 2,3-b][1,4]-diazepine-4-ones]. / Attività farmacologica di 5-[(dialchilammino) alchil]-8-cloro-3,5-diidro-2-metil/fenil-4H-pirido [2,3-b] [1,4]-diazepin-4-oni.

Some 5-[(dialkylamino)alkyl]-8-chloro-3,5-dihydro-2-methyl/phenyl-4H- pyrido[2,3-b] [1,4]-diazepin-4-ones previously prepared, were subjected to pharmacological experimentation in order to verify variation in biological activity induced by introduction of chlorine on the pyridine nucleus and by replacement of pyridinic with a benzenic ring. The effect upon mice with regard to exploratory activity, motor coordination, spontaneous activity, analgesic activity was tested and their anti-stricnine, anti-cardiazole, anti-amphetamine and anti-reserpine activities were also evaluated. The activities of the texted compounds were compared with those already showed by the analogues unchlorinated derivatives (B) and by isosters benzodiazepinones (D).

[The possible use of a ready-to-us film system for microbiological control in drug preparation]. / Possibilità di utilizzo di un sistema a film reidratabile nel controllo microbiologico di preparati farmaceutici.

Aim of this work was to verify the possibility of using a ready-to-use plate-count method to detect the microbial and fungal contamination on pharmaceutical products. The system consists of a flexible polypropylene film, supporting a suitable dehydrated medium, a second support containing guar, and an indicator on the internal surface. 33 raw materials, 11 natural origin materials, 20 medicinal product of official formula and 18 homeopathic products were analysed. As reference we chose the Italian Pharmacopoeia method. The two methods were comparable, showing no statistical differences, but for one case. This method, if our date will be further confirmed, could be used by the pharmacies and by the homeopathic industries.

In vitro antibacterial activity of antiseptics against vaginal lactobacilli.

The results of investigations carried out to evaluate the inhibitory activity in vitro of seven vaginal antiseptic douche solutions against several strains of vaginal lactobacilli isolated from asymptomatic women are reported. Some of the products examined showed marked antibacterial activity even at high dilutions and for short exposure times. The post-antibiotic effect of two of these antiseptics on vaginal lactobacilli was also evaluated. The results of these investigations suggest that uncontrolled use of antiseptic products could cause changes in the normal vaginal flora.

[Pyrido[2,3-b][1,4]diazepinones with CNS activity]. / Pirido[2,3-b][1,4]diazepinoni ad attività sul S.N.C.

In the interests of developing our research on compounds with a pyrazinone nucleus, cyclohomologues, characterised by the presence of one diazepinone nucleus, were prepared. The 5-[(dialkylamino)alkyl]-3,5-dihydro-2-methyl/phenyl-4H-pyrido[2,3- b][1,4]diazepin-4-ones obtained by means of condensation of the 2-(dialkylamino)alkylamino-3-aminopyridines with ethyl acetyl- or benzoyl- acetate, were subjected to pharmacological experimentation in order to evaluate their effect upon mice with regard to exploratory activity, motor coordination, and spontaneous activity. In addition their analgesic activity was evaluated and also their anti-strychnine, anti-cardiazole, anti-amphetamine and anti-reserpine activities.

[Preparation and pharmacologic activity of 1-dimethylaminopropyl-3-methyl-6-chlorquinoxaline-2(1H)-one]. / Preparazione ed attività farmacologica dell'1-dimetilamminopropil-3-metil-6-clorochinossalin-2(1H)-one.

In continuation of previous research 1-dimetilaminopropyl-3-methyl-6-chlorquinoxaline-2(1H)-one was prepared. This compound shows affects on conditioned avoidance response together with analgesic action and inhibition of explorative activity, while it induces only a small degree of motor incoordination and does not protect the animals from toxic doses of strychinine and physostigmine.

[Anilides with analgesic and antipyretic activity]. / Anilidi ad attività analgesica ed antipiretica.

Several trimethylcyclopentyl and trimethylcyclopentenyl acetanilides, mono- and di-substituted on the aromatic nucleus as well as the corresponding acyl derivatives from aniline it self and corresponding phenylacetanilides, were prepared and tested as analgesics and antipyretics. Several compounds exhibit considerable activity in some cases superior to that of acetanilide.