PHARMACOLOGICAL AND PHYSICO-CHEMICAL PROPERTIES OF COMPOSITIONS BASED ON BIOSURFACTANTS AND N-CONTAINING HETEROCYCLIC DERIVATIVES OF 1,4-NAPHTHOQUINONE

Abstract

Composite preparations based on rhamnolipid biosurfactants and N-containing heterocyclic 1,4-naphthoquinone derivatives were obtained. The formation of the compositions was confirmed by UV spectroscopy, dynamic light scattering and changes in the surface tension of the compositions in comparison with the original solutions. Physicochemical and biological properties of composite drugs have been studied. The anticonvulsant effect was assessed using the pentylenetetrazole (PTZ) model. Doses of PTZ for induction of clonic-tonic seizures (DCTC) and tonic extension (DTE) were calculated relative to control. The effect of rhamnolipid on increasing the permeability of cell membranes for compounds 1a-e was evaluated indirectly by studying anticonvulsant activity. Compound  (2-chloro-3-((3-(p-tolyl)-1H-pyrazol-5-yl)amino) naphthalene-1,4-dione) (1b) in combination with rhamnolipid was found to have a higher anticonvulsant activity DCTC and DTE averaged 239% and 244%, respectively, which may indicate an improvement of  the penetration of the compound when in complex with rhamnolipid into the cell and as a result, an increased anticonvulsant activity of the composite drug.