METHOD OF ISOLATION OF NEW GLYCOSIDES FROM PTEROCARPUS MARSUPIUM AND THEIR THERAPEUTIC EFFECTS Russian patent published in 2023 - IPC A61K36/48 B01D11/02 A61P3/08 A61P3/10 

FIELD: pharmaceutical industry.

SUBSTANCE: invention relates to a composition for activating adenosine monophosphate-activated protein kinase (AMPK) and for inhibiting gluconeogenesis in mammalian cells. Composition for activating adenosine monophosphate-activated protein kinase (AMPK) and for inhibiting gluconeogenesis in mammalian cells containing at least 5 wt.% Pterocarpus marsupium extract, standardized to contain at least 0.5 wt.% pterocarposide (STR#1) and not less than 0.5 wt.% sabioside (STR#2), and the composition obtained by a method comprising the following steps: a) loading the powder of the Pterocarpus marsupium tree into the extractor, b) extracting with methanol to obtain an oleoresin, c) dissolving the oleoresin from step b) in water and extracting with toluene to obtain an aqueous layer and toluene layer, d) additional washing of the toluene layer from step c) with water to further obtain an aqueous fraction and a toluene fraction, e) mixing the aqueous fractions from step c) and step d) and spray drying to obtain an aqueous extract, f) fractionating the aqueous fraction from step e) with ethyl acetate to obtain an aqueous fraction and an ethyl acetate fraction, g) passing the ethyl acetate fraction from step f) through a solvent gradient column using 60–120 mesh silica gel to obtain enriched fraction 1 and fraction 2, h) passing enriched fraction 1 from step g) through an RP-18 isocratic silica gel column, then through an LH-20 column (Sephadex^®), and crystallization using a solvent at a temperature of -5 to 0°C to obtain a compound that is identified as the pterocarposide represented by STR#1, i) passing enriched fraction 2 from step g) through an RP-18 isocratic silica gel column, then through an LH-20 column (Sephadex^®) and crystallization using methanol at room temperature to obtain a compound that is identified as the sabioside represented by STR#2, j) loading the aqueous extract of Pterocarpus marsupium from step e) into the extractor, k) adding demineralized water to the extract, stirring for 3–4 hours at 65 to 70°C and leaving the solution for 8–10 hours to precipitate the insolubles, l) filtering the solution from step k) to remove the insolubles and obtain a clear filtrate, m) checking the insolubles from step l) for the presence of pterocarposide (STR#1) or sabioside (STR#2), discarding them if they are present in small amounts, n) collecting the filtrate from step l) and solvent extraction twice to obtain an aqueous layer and a solvent layer, o) concentrating the solvent layer from step n) recovering the solvent, p) extracting the aqueous layer from step n) with butanol three times and combining the butanol fractions, q) concentrating the butanol fractions and dissolving in water to standardize to a solution with a total dissolved solids content of 30%, r) spraying drying the solution from step q) obtaining compositions containing at least 5 wt.% Pterocarpus marsupium extract, standardized to contain at least 0.5 wt.% pterocarposide and not less than 0.5 wt.% sabioside represented by STR#1 and STR#2, respectively.

EFFECT: above composition is effective for activating adenosine monophosphate-activated protein kinase (AMPK) and for inhibiting gluconeogenesis in mammalian cells.

3 cl, 3 dwg, 2 ex