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Results from studies of the antidiabetic and antihyperglycemic activity of a low-molecular-weight NGF mimetic, compound GR-2 [bis-(N-monosuccinyl-L-glutamyl-L-lysine)hexamethylenediamide], on a streptozotocin-induced diabetes model in Wistar rats are presented. GK-2 administered perorally at a dose of 5 mg/kg for 28 d significantly reduced the glycemia level in diabetic rats and increased the overall plasma antioxidant capacity. The glycemia level and plasma antioxidant capacity were in an inverse exponential relationship and were closely correlated to each other (correlation coefficient 0.899). [ABSTRACT FROM AUTHOR]

Wound-healing activity of the crystalline form of dihydroquercetin and its microtubular pseudopolymorphic modification obtained by crystal engineering was compared using the rat model of IIIA degree burn. The rate of wound healing in the group treated with microtubular pseudopolymorphic modification of dihydroquercetin was 4.8±0.1%, which was higher by 11.6% than in the group treated with crystalline form (4.3±0.1%). Bioavailability analysis on MDCK cell culture showed that the apparent permeability coefficient of microtubular pseudopolymorphic modification was higher than that of crystalline form by 31.1% (19.4±0.2×10–4 and 14.8±0.3×10–4 cm/sec, respectively). It was proven that the use of crystal engineering improved the biopharmaceutical parameters of dihydroquercetin and increased its pharmacological efficiency. [ABSTRACT FROM AUTHOR]

Dihydroquercetin (DHQ) is a commercially available bioflavonoid with a wide range of pharmacological activity. The low water solubility at room temperature of the commercial drug substance limits development of DHQ-related medicines. Basic concepts of crystal engineering were used to obtain DHQ cocrystals with benzaldehyde, vanillin, cinnamaldehyde, urea, and nicotinic acid. The formation of supramolecular complexes of DHQ with the coformers was confirmed using IR spectroscopy. An estimate of the physicochemical parameters of the cocrystals established that crystal engineering was promising for obtaining new DHQ forms with improved water solubility. [ABSTRACT FROM AUTHOR]

Flavonoids are of interest for pharmacy and medicinal chemistry due to a wide range of biological activities. The major goal for the design of new drugs based on flavonoids is to increase bioavailability of pharmaceutical substances. Crystal engineering is a useful tool for this purpose. This review presents a systematic analysis of the publications on crystal engineering of flavonoids published between 2000 and 2019. The data on objects, methods of supramolecular synthesis, analysis, and preclinical studies of its products are summarized. The trends in crystal engineering of flavonoids are considered and promising areas for further research are identified. The review may be of interest for researchers engaged in the design of drugs with low bioavailability, including bioflavonoids. [ABSTRACT FROM AUTHOR]