[Study of the specific toxic effects of the substance 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil, the original non-nucleoside inhibitor of human immunodeficiency virus type 1 (Retroviridae; Orthoretrovirinae; Lentivirus: Human immunodeficiency virus 1) reverse transcriptase].

INTRODUCTION: Combination antiretroviral therapy is currently the main component of treatment for human immunodeficiency virus (HIV) infected patients. At the same time, the high mutational potential of the virus and the frequency of side effects of existing drugs dictate the need for the development and preclinical study of new, more effective and safer compounds.The aim of the study is to evaluate the specific types of toxicity of a new non-nucleoside inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RNA-dependent DNA revertase) (NNRTI) based on the substance 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil, a benzophenone derivative. MATERIAL AND METHODS: The study investigated reproductive toxicity, embryotoxicity, immunotoxicity, genotoxic (in micronucleus test in and comet assay) and allergenic properties of the test itemcompound. It was tested on three species of animals in two doses: the estimated therapeutic dose (1 TD) and its tenfold equivalent (10 TD). Taking into account the metabolic coefficients, the doses for rats (Rattus) were 9 and 90 mg/kg, for mice (Mus musculus), 21 and 210 mg/kg, and for guinea pigs (Cavia porcellus), 8 and 80 mg/kg, respectively. RESULTS AND DISCUSSION: According to the obtained results, a favorable safety profile of the tested compound was established. Negative effects on the immune system, reproductive function, the body of pregnant animals and the fetus were not observed, as well as the compound did not have genotoxic and allergenic properties. CONCLUSION: These data allows to consider the studied compound as a promising therapeutic candidate for the treatment of HIV-1 infection.

[Cardioprotective effect of new functional food containing salmon oil with motherwort oil extract].

Combination of fish oil with herbal oil extract can extend functional properties of the products. A new functional food of salmon oil with oil extract of motherwort (8:2) was developed and studied. Qualitative profiling was evidenced about presence of flavonoids and iridoids. Quantification of vitamins A (210±3 IU/g), Е (2.8±0.1 mg/g), D3 (12.2±0.4 IU/g) and PUFA (43.3±0.4%, incl. 9.4±0.1% of omega-3 and 33.9±0.1% of omega-6) was done by modern methods. The developed product was found nontoxic (LD50>15 000 mg/kg b.w., intragastriсally, LD50>3000 mg/kg b.w., intraperitoneal). The 14 days intragastric administration of product to the rats (initial b.w. 200-250 g) at the doses of 2340 and 1170 mg/kg b.w. significantly increased the left ventricular pressure after ischemia comparing with control, and normalized the contraction and relaxation of the left ventricle. Biochemical data confirmed the decrease of aspartate amino transferase and creatine kinase activity in rats treated at all experimental doses. Application of fish oil combination with motherwort oil extract is promising for development of new functional foods with cardio protective properties.

Comparative analysis of requirements for quality of fish oil for food and medical applications.

Fish oil is reach natural source of vitamins А, Е, D and polyunsaturated fatty acids (PUFA) which are useful for supplementation, prophylaxis and therapy in food industry, medicine and veterinary. The analysis of regulatory documents for the quality of fish oil (based on concentration of main nutrients) leads to conclusion that content of vitamins A and D, and PUFA is controlled in medicinal preparations. With regard to fish oil for food application there is no unified approach. In particularly, content of vitamin D in food supplements with fish oil available on Russian market is not indicated by manufacturer or its concentration varies in 3-10 folds. Because of important biological functions and pharmacological activity, it is very important to have uniform standardization for vitamins and PUFA in fish oil for application in food industry and medicine. Development and unification of analytical methods became special attention for these reasons.