ABSTRACT
The results of pharmacological tests showed that betulin bishemiphthalate possesses hepatoprotector, antioxidant, and immunotropic properties. Administered in combination with hydroxymethyluracil, that betulin bishemiphthalate prevented the loss of experimental animals upon irradiation.
Subject(s)
Adjuvants, Immunologic/pharmacology , Antioxidants/pharmacology , Liver/drug effects , Phthalic Acids/pharmacology , Radiation-Protective Agents/pharmacology , Triterpenes/pharmacology , Acute Disease , Adjuvants, Immunologic/toxicity , Animals , Antibody Formation/drug effects , Antioxidants/toxicity , Chemical and Drug Induced Liver Injury/prevention & control , Immunity, Cellular/drug effects , Lethal Dose 50 , Lipid Peroxidation/drug effects , Liver/enzymology , Mice , Phthalic Acids/toxicity , Radiation Injuries/mortality , Radiation Injuries/prevention & control , Radiation-Protective Agents/toxicity , Toxicity Tests, Acute , Triterpenes/toxicityABSTRACT
11-Deoxymisoprostol showed gastroprotector activity on the acute models of ulcers induced by acetylsalicylic acid and ethanol and produced curative effect on the chronic ulceration model induced by acetic acid. The positive effect is manifested by a decrease in the number of destructions and in the total area of chronic damage in the mucous membrane of the stomach. In addition, 11-deoxymisoprostol showed antiphlogistic activity on the acute edema models induced by carrageenan and formalin, by decreasing the model foot edema growth in experimental animals. The drug also decreased the level of lipid peroxidation in the rat blood serum on the background of acute ethanol ulceration.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Anti-Ulcer Agents/pharmacology , Misoprostol/pharmacology , Stomach Ulcer/prevention & control , Animals , Edema/chemically induced , Edema/prevention & control , Female , Lipid Peroxidation/drug effects , Male , Malondialdehyde/blood , Mice , Misoprostol/analogs & derivatives , Rats , Stomach Ulcer/chemically inducedABSTRACT
The assignment of NMR resonances of lupane triterpenoids was refined by the example of 3,28-dinicotinoylbetulin, obtained by acylation of betulin. Hepatoprotective, untiulcer, antiinflammatory, reparative, and anti-HIV activities were found for the compound. In addition, it was demonstrated to have immunomodulatory activity, for the first time detected among lupane triterpenoids. The English version of the paper: Russian Journal of Bioorganic Chemistry, 2002, vol. 28, no. 6; see also http://www.maik.ru.
Subject(s)
Adjuvants, Immunologic/chemical synthesis , Anti-HIV Agents/chemical synthesis , Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis , Triterpenes/chemical synthesis , Adjuvants, Immunologic/therapeutic use , Adjuvants, Immunologic/toxicity , Animals , Anti-HIV Agents/therapeutic use , Anti-HIV Agents/toxicity , Anti-Inflammatory Agents, Non-Steroidal/therapeutic use , Anti-Inflammatory Agents, Non-Steroidal/toxicity , Antibody Formation/drug effects , Arthritis/drug therapy , Betula/chemistry , Burns/drug therapy , Cell Line , Cell Survival/drug effects , Disease Models, Animal , Dose-Response Relationship, Drug , HIV Core Protein p24/analysis , HIV-1/drug effects , Humans , Lethal Dose 50 , Mice , Plant Bark/chemistry , Rats , Stomach Ulcer/drug therapy , Triterpenes/chemistry , Triterpenes/isolation & purification , Triterpenes/therapeutic use , Triterpenes/toxicityABSTRACT
Hemisuccinates, hemiphthalates, acetylsalicylates, cinnamates, and p-methoxycinnamates of lupeol, betulin, and 3-O-acetylbetulin were synthesized via interaction with corresponding acid anhydrides or acid chlorides. A number of betulin esters in position 3 and 28 were shown to exhibit a pronounced hepatoprotective effect similar to that of betulin and silibor. These experimental data were in a good agreement with the computer prediction of their biological activity. Betulin 3,28-bis-hemiphthalate was more effective than carsil in models of experimental hepatitis caused by carbon tetrachloride, tetracycline, and ethanol.
Subject(s)
Anti-Inflammatory Agents/chemical synthesis , Triterpenes/chemical synthesis , Animals , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/pharmacology , Liver/drug effects , Liver/pathology , Pentacyclic Triterpenes , Rats , Triterpenes/chemistry , Triterpenes/pharmacologyABSTRACT
It was shown on noninbred albino rats with various affections of the skin that pyrimidine derivatives stimulated the skin reparative regeneration and increased the efficacy of antibiotic therapy of Staphylococcus and Proteus infected wounds. The therapeutic effect of 2-methyl-4-amino-6-oxypyrimidine was much higher than that of oxymethyluracil or methyluracil. The pyrimidine derivatives proved to be universal accelerators for reparative regeneration, were compatible with antibiotics and increased their efficacy.
