Studies on the synthesis containing amino acid fragments and quinone communications system, as they may be potential drugs is an actual problem of biology. One of the sections of modern pharmaceutical and organic chemistry, that dynamicly develops is quinone chemical compounds, which occupy an important place is naphthoquinone and its derivatives, including amino acids. New synthesis of amino acid derivatives of 1,4-naphthoquinone are perspective in medicine and pharmacy, as they have low toxicity, antihypoxic, antiischemic and anticonvulsant actions. So aminoacid derivatives of 1,4-naphthoquinone is a promising class of chemical compounds to find compounds with cerebroprotective properties.

The thesis is intended to study membrane related processes of loach embryo Misgurnus fossilis L. under the effect of amino acid derivatives of 1,4-naphthoquinone. Dosedependent inhibition of embryos of Na+, K+-ATPase amino acid derivatives of 1,4-naphthoquinone have been shown. As established during the studies in vivo by the action of high concentration of active ingredient (10–6 M) investigated the activity of the enzyme significantly reduced compared to control.

In the early hours of germs found probable significant decrease in activity of the enzyme by the investigational membrane to high concentration (10–6 M) at 42,6 ± 0,7 %, but at 10–8 M concentration significant decrease in activity was not observed. On stage 16 and 64 blastomeres impact alanine derivative of 1,4-naphthoquinone leads to a significant decrease in activity of Na+, K+-ATPase compared with the control of concentrations between 10–6 and 10–8 M.

Compared with the control inhibitory effect of the substance persists in the next stages of blastomeres at concentration 10–6 M. Accordingly, the division VIII (270 min) development of embryos, there occurs probable decrease of 48,8 ± 2,5 %, and the division of X (330 min) enzyme activity of embryos in 42,3 ± 0,5 % was low compared with values in the control, which was 0,264 ± 0,014 mmol Ri / min per 1 mg protein. However, low concentrations of alanine 1,4-naphthoquinone derivative 270 minutes of unreliable revealed reduced activity of Na+, K+-ATPase to 9,2 ± 3,8 %. At the last stage of synchronous divisions of blastomeres (X division, 330 minutes) at low concentrations increased activity of the enzyme membrane by 16,6 ± 4,1 % was detected.

Type inhibition was determined by Dixon method. By linearization of concentration dependence of inhibition of Na+, K+-ATPase potassium salt of 2-α-1,4-naphthoquinone alanine in the presence of ATP incubation medium at a concentration of 1.5 and 3 mg in these coordinates, it was found that straight lines intersect. The analysis in Dixon coordinates showed the conditionally competitive type of inhibition. Established decrease of Na+, K+-ATPase activity, determines low changes in embryos ultrastructure after six hours of development and set up the type of inhibition. Electron microscopic study of ultrathin sections blastomeres of embryos of loach conducted in an environment with a high concentration of 10–6 M alanine 1,4-naphthoquinone derivative ater six hours in the development of (X division, 330 min). There following organelle damages in high concentration 10–6 M were found: oedema of SER channels, the increasing of lysosomes and secondary lysosomes number, as well as vacuoles, the destruction of plasma membrane, which leads to the metabolic disorders.

Obviously in high concentrations of biologically active amines derivatives of 1,4-naphthoquinone able to be involved in metabolic processes embryos and lead to increased intensity of exchange in embryos, which at this time rapidly developing and growing.

Ключові слова: 1, 4-naphthoquinone, amino acid derivatives of 1, 4-naphthoquinone, loach embryos, membrane potential, activity of Na+, K+-ATPase

Повний текст: PDF (Ukr)

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