Synthesis and biological activity of new glycyrrhizic acid conjugates with amino acids and dipeptides
| Autor: | L. A. Baltina, R. M. Kondratenko, N. Z. Baschenko, O. A. Pl’yasunova |
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| Předmět: |
conjugates
immunostimulating and anti-HIV-1 activity synthesis Stereochemistry Anti-HIV Agents Cell Survival T-Lymphocytes HIV Core Protein p24 Biochemistry Article chemistry.chemical_compound Mice Cytopathogenic Effect Viral Bioorganic chemistry Molecule Animals Humans Cells Cultured chemistry.chemical_classification amino acids Dipeptide Molecular Structure Organic Chemistry Hemolysin Biological activity Dipeptides Glycyrrhizic Acid Amino acid Immunity Humoral chemistry HIV-1 Chromatography Thin Layer Selectivity Conjugate |
| Zdroj: | Scopus-Elsevier Russian Journal of Bioorganic Chemistry |
| Popis: | New glycyrrhizic acid (GA) conjugates were synthesized with the use of tert-butyl esters of amino acids or benzyl esters of dipeptides; they contained two residues of L-amino acids (Met, Phe, Pro, and Ile or dipeptides Gly-Leu and Gly-Phe). Activation of GA carboxy groups was carried out with the help of N-hydroxysuccinimide, N,N′-dicyclohexylcarbodiimide, or N-hydroxybenzotriazole with dicyclohexylcarbodiimide. A proline-containing GA derivative is a low-toxic substance; it raises the level of agglutinins by 3.7 times in the blood of mice and 3 times that of hemolysins compared with the control. Dipeptide GA derivatives possess an expressed anti-HIV-1 activity in cultures of MT-4 cells and are 90-70 times less cytotoxic than azidothymidine. The selectivity index of the compounds exceeds those of GA by 110 and 34 times, respectively. |
| Databáze: | OpenAIRE |
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