Hypolipidemic Activity of Solid Dispersion of Leucomisin

BACKGROUND: The sesquiterpene lactone leucomisin is a promising compound with hypolipidemic activity, but it is practically insoluble in water, which reduces its bioavailability. Therefore, we synthesized a solid dispersion of leucomisin with the glycyrrhizic acid disodium salt, samples of which were studied for hypolipidemic activity. AIM: To study the hypolipidemic activity of solid dispersion of leucomisin with glycyrrhizic acid disodium salt. METHODS: We synthesized the solid dispersion of leucomisin by "simple mixing" method. The study of hypolipidemic activity of the samples was carried out according to known methods on models of acute tween hyperlipidemia, acute ethanol hyperlipidemia, fatty liver dystrophy of rats. RESULTS: Based on the results of the experiments conducted, it was determined that the solid dispersion of leucomisin: Reduces triacylglycerols and cholesterol levels in rat serum in acute experimental hyperlipidemia induced by Tween-80, free fatty acids, serum triacylglycerols and triacylglycerol levels in rat liver in an ethanol-induced acute hyperlipidemia model; Lowers the level of triacylglycerols and increases the ratio of phospholipids to triacylglycerols in experimental fatty liver degeneration induced by tetrachloromethane in rats; Activates the antiperoxidation enzymes glutathione reductase and glutathione peroxidase and increases the redox potential of the glutathione system; and Reduces the activity of 3-hydroxy-3-methylglutaryl-coenzyme A reductase in rat liver and increases cholesterol excretion through the gastrointestinal tract. CONCLUSION: The synthesized solid dispersion of leucomisin showed pronounced hypolipidemic activity.

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Publication Details

Journal
Open Access Macedonian Journal of Medical Sciences
Published
2024-11-20
DOI
https://doi.org/10.3889/oamjms.2024.11935
Primary Topic
Pharmacological Effects of Natural Compounds
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article
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article

Hypolipidemic Activity of Solid Dispersion of Leucomisin

С. М. Адекенов, Л. И. Арыстан, Dmitry Leontyevich Savchenko
Open Access Macedonian Journal of Medical Sciences
Pharmacological Effects of Natural Compounds
article

Hypolipidemic Activity of Solid Dispersion of Leucomisin

С. М. Адекенов, Л. И. Арыстан, Dmitry Leontyevich Savchenko
article en

Abstract

BACKGROUND: The sesquiterpene lactone leucomisin is a promising compound with hypolipidemic activity, but it is practically insoluble in water, which reduces its bioavailability. Therefore, we synthesized a solid dispersion of leucomisin with the glycyrrhizic acid disodium salt, samples of which were studied for hypolipidemic activity. AIM: To study the hypolipidemic activity of solid dispersion of leucomisin with glycyrrhizic acid disodium salt. METHODS: We synthesized the solid dispersion of leucomisin by "simple mixing" method. The study of hypolipidemic activity of the samples was carried out according to known methods on models of acute tween hyperlipidemia, acute ethanol hyperlipidemia, fatty liver dystrophy of rats. RESULTS: Based on the results of the experiments conducted, it was determined that the solid dispersion of leucomisin: Reduces triacylglycerols and cholesterol levels in rat serum in acute experimental hyperlipidemia induced by Tween-80, free fatty acids, serum triacylglycerols and triacylglycerol levels in rat liver in an ethanol-induced acute hyperlipidemia model; Lowers the level of triacylglycerols and increases the ratio of phospholipids to triacylglycerols in experimental fatty liver degeneration induced by tetrachloromethane in rats; Activates the antiperoxidation enzymes glutathione reductase and glutathione peroxidase and increases the redox potential of the glutathione system; and Reduces the activity of 3-hydroxy-3-methylglutaryl-coenzyme A reductase in rat liver and increases cholesterol excretion through the gastrointestinal tract. CONCLUSION: The synthesized solid dispersion of leucomisin showed pronounced hypolipidemic activity.

Open Access Macedonian Journal of Medical SciencesVol. 12
Karaganda Medical University (KZ), Private Institution “Karaganda University of Kazpotrebsoyuz” (KZ)
Clean water and sanitation
Openalex Percentile: Top 72%
Pharmacological Effects of Natural Compounds
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