OBTAINING SUPRAMOLECULAR COMPLEXES OF ANGIDROLAGOQUILINE WITH GLYCYRRHISINOIC ACID AND ITS SALTS AND STUDYING THEIR SPECIFIC HEMOSTATIC ACTIVITY

Abstract

The hemostatic effect of drugs of the genus Lagochilus (Lamiaceae) is due to the content in its composition of four atomic alcohol diterpenoid lagochiline, alkaloid stahydrine, vitamin K and tannins. On the basis of lagochilin, a number of acetyl and isopropylidene derivatives were obtained. It has been shown that the hemostatic activity in a certain way depends on the number of free hydroxyl groups of lagochilin and its derivatives. However, lagochiline derivatives are poorly soluble in water, which limits their bioavailability. Chemical modification of lagochilin is carried out mainly by hydroxyl groups with the production of esters or succinates with dibasic anhydrides.
 For the first time, water-soluble supramolecular complexes based on the diterpenoid lactone an-hydrolagoquiline with the triterpene saponin glycyrrhizic acid (GA) and its monoammonium (MASGA) and monopotassium salts (MPSGA) in various molar ratios were obtained. The physicochemical and spectral characteristics of the resulting complex compounds have been studied. Screening studies were carried out to study the specific hemostatic activity of the obtained supramolecular complexes. Among Lagochilin Lagochirzine and their derivatives at a dose of 10 mg/kg, Lagochilin had the most active effect on bleeding time, followed by Anhydrolagochilin–Lagohirzin. The greatest effect on bleeding time at a dose of 10 mg/kg among supramolecular complexes with HA was shown by HA-AHL, which in a ratio of 2 : 1 it was impossible to determine the bleeding time, and in a ratio of 4 : 1 it reduced the bleeding time by 12 times, and the amount of blood loss by 42 times.