ABSTRACT
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.
Subject(s)
Carrageenan/chemistry , Chitosan/chemistry , Chitosan/pharmacology , Cytoprotection/drug effects , Stomach/drug effects , Animals , Female , Rats , Solubility , Stomach/pathology , Stomach Ulcer/prevention & controlABSTRACT
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.
Subject(s)
Anti-Ulcer Agents/immunology , Anti-Ulcer Agents/therapeutic use , Antibodies/immunology , Antibodies/therapeutic use , Stomach Ulcer/drug therapy , Acetates/toxicity , Animals , Famotidine/therapeutic use , Gastrins/immunology , Histamine/immunology , Male , Rats , Rats, Wistar , Receptors, Histamine H2/immunology , Stomach Ulcer/chemically inducedABSTRACT
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.
Subject(s)
Aconitine/analogs & derivatives , Anti-Arrhythmia Agents/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Arrhythmias, Cardiac/drug therapy , Glycyrrhizic Acid/administration & dosage , Aconitine/administration & dosage , Aconitine/toxicity , Animals , Anti-Arrhythmia Agents/toxicity , Anti-Inflammatory Agents, Non-Steroidal/toxicity , Arrhythmias, Cardiac/chemically induced , Disease Models, Animal , Dose-Response Relationship, Drug , Glycyrrhizic Acid/toxicity , Male , RatsSubject(s)
Analgesics/pharmacology , Morphinans/pharmacology , Analgesics/chemistry , Analgesics/therapeutic use , Analgesics/toxicity , Animals , Chloral Hydrate , Mice , Molecular Structure , Morphinans/chemistry , Morphinans/therapeutic use , Morphinans/toxicity , Nicotine/toxicity , Pain/drug therapy , Pentylenetetrazole/toxicity , Survival Rate , Toxicity TestsABSTRACT
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.
Subject(s)
Amines/pharmacology , Carboxylic Acids/pharmacology , Naphthalenes/pharmacology , Neuroprotective Agents/pharmacology , Amines/chemical synthesis , Amines/toxicity , Animals , Anticonvulsants/chemical synthesis , Anticonvulsants/pharmacology , Anticonvulsants/toxicity , Antidepressive Agents/chemical synthesis , Antidepressive Agents/pharmacology , Antidepressive Agents/toxicity , Brain/drug effects , Brain/physiology , Carboxylic Acids/chemical synthesis , Carboxylic Acids/toxicity , Male , Mice , Motor Activity/drug effects , Naphthalenes/chemical synthesis , Naphthalenes/toxicity , Neuroprotective Agents/chemical synthesis , Neuroprotective Agents/toxicity , Structure-Activity Relationship , Toxicity Tests, AcuteABSTRACT
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).
Subject(s)
Aconitine/pharmacology , Psychotropic Drugs/pharmacology , Acetylcholine/antagonists & inhibitors , Aconitine/analogs & derivatives , Aconitine/toxicity , Animals , Blepharoptosis/chemically induced , Cholinergic Agents/pharmacology , Cyclic N-Oxides/pharmacology , Cyclic N-Oxides/toxicity , Lethal Dose 50 , Male , Mice , Motor Activity/drug effects , Nicotine/antagonists & inhibitors , Pentylenetetrazole/antagonists & inhibitors , Psychotropic Drugs/toxicity , Reserpine/antagonists & inhibitors , Sleep/drug effects , Stereotyped Behavior/drug effectsSubject(s)
Carboxylic Acids/chemistry , Carboxylic Acids/pharmacology , Central Nervous System Agents/pharmacology , Motor Activity/drug effects , Naphthalenes/chemistry , Naphthalenes/pharmacology , Aggression/drug effects , Animals , Apomorphine/pharmacology , Central Nervous System Agents/chemistry , Chloral Hydrate/pharmacology , Clonidine/pharmacology , Cycadopsida , Levodopa/pharmacology , Male , Mice , Molecular Structure , Reserpine/pharmacology , Sleep/drug effects , Stereotyped Behavior/drug effects , Structure-Activity Relationship , TreesABSTRACT
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.
