Soluble chitosan-carrageenan polyelectrolyte complexes and their gastroprotective activity.

The soluble polyelectrolyte complexes (PEC) κ-carrageenan (κ-CG):chitosan was obtained. Binding constant value (2.11 × 10(7)mol(-1)) showed high affinity of κ-CG to chitosan. The complex formation of κ-CG:chitosan 1:10 and 10:1 w/w was shown by centrifugation in a Percoll gradient. Using atomic force microscopy we showed that the supramolecular structure of the complexes is different from each other and from the macromolecular structure of the initial polysaccharides. The gastroprotective and anti-ulcerogenic effect of κ-CG, chitosan and their complexes was investigated on the model of stomach ulcers induced by indometacin in rats. PEC κ-CG:chitosan have gastroprotective properties which depend on their composition. Complex κ-CG:chitosan 1:10 w/w possesses higher gastroprotective activity than the complex 10:1 w/w. These results suggest that the gastroprotective effect of complexes can be associated with their protective layer on the surface of the mucous membrane of a stomach, which avoids a direct contact with the ulcerogenic agent.

Antiulcer activity of preparations containing ultralow doses of antibodies in modeled chronic ulcer in rats.

Screening of three potential antiulcer preparations containing ultralow doses of antibodies to endogenous regulators of ulcer formation (gastrin, histamine, and H2 histamine receptors) on the model of acetic acid-induced gastric ulcer in rats revealed pronounced antiulcer effect of ultralow doses of antibodies to histamine. The dynamics of regeneration of the ulcer focus by morphological and histological characteristics was similar during treatment with ultralow doses of antibodies to histamine and with famotidine.

[Antiarrhythmic activity of alaglyzin].

The activity of alaglyzin, a new drug based on a clathrate complex of allapinine (well-known antiarrhythmic) with glycyrrhizic acid (GA), was studied on the models of arrhythmia induced by itraperitoneal injections of calcium chloride (CaCl2) and adrenaline (epinephrine) in rats. Alaglyzin is less toxic than allapinine (LD50 70 and 6 mg/kg, respectively), and the effective dose of the parent compound in the complex form is also about 12 times lower than that in the reference drug. The experiments showed a dose dependent action of alaglyzin. Pretreatment of the experimental animals with alaglyzin in a dose of 0.25 mg/kg prevented from the arrhythmia development in both tests, while a dose of 0.125 mg/kg was effective only in the CaCl2, test.

[Neurotropic activity of lambertian acid and its amino derivatives]. / Neirotropnaia aktivnost' lambertianovoi kisloty i ee aminoproizvodnykh.

The neurotropic activity of the originally synthesized methyl lambertianate (II), as well as lambertianic acid (I) and three amino derivatives (III-V) was studied. All compounds exhibit equally low toxicity, but differ in the type of influence upon CNS. The most pronounced action was observed for esters II and V. Compound II exhibited a strong antidepressant effect with stimulating action. Introduction of the amino group led to an opposite tendency: compound V exhibited an antipsychotic and sedative (calming) effect upon CNS, without any anticonvulsant action.

[Psychotropic effects of alkaloid lappaconitine and its various derivatives]. / Psikhotropnye svoistva alkaloida lappakonitina i ego nekotorykh proizvodnykh.

The psychotropic activity of (I, base), its N-oxide, and a complex of the base with 18-alpha-H-glycyrrhizic acid (1:2) was studied. It was established that I and its N-oxide exhibit dopaminopositive effect whereas the complex produces a serotoninopositive effect. Toxicities of the lipophilic I is half that of the hydrophilic; toxicity of N-oxide and the complex are 60 and 100 times lower than the activity of lappaconitine (base).

[Toxic effect of the novel phenol antioxidant SO-3 in the subchronic experiment]. / Izuchenie toksicheskogo deistviia novogo fenol'nogo antioksidanta CO-3 v subkhronicheskom éksperimente.

Subchronic tests on rats showed that a new phenolic antioxidant bis[3,(3, 5-di-tert-butyl-4-hydroxyphenyl)propyl] sulfide (SO-3) exhibits low toxicity upon peroral administration. Neither significant variations in the hematological and integral indices, nor pathological shifts in the activity of serum enzymes or pathomorphological changes in the internal organs were observed. Simultaneous administration of a sunflower oil with SO-3 led to a significant decrease in the blood cholesterol level, produced a hepatoprotector effect, and exhibited a protective action with respect to the mucous membranes of the gastrointestinal tract. Animals receiving large doses of SO-3 showed no signs of a prelipid stage of the arteriosclerosis typically observed in the control group.