Actinomycetes are the source of biologically active substances with various chemical structure and spectrum of action. They are filamentous soil bacteria, representing the largest taxonomic unit. Actinomycetes account from 20 to 46% of the total diversity of soil microflora. The members of the genus Streptomyces are active producers of metabolites for biocontrol of phytopathogens population. They are promising objects of biotechnology, as producers of antibiotics of different chemical nature and a wide range of other biologically active substances. As a result of extensive screening of the collection strains and new isolates of soil streptomycetes, two strains actives against phytopathogenic microorganisms and phytonematodes were selected. Two antifungal compounds of polyene nature of Streptomyces netropsis IMV Ac-5025 antibiotic complex have been isolated and identified. One of them is the heptayen antibiotic AC1O5FWR (сandіdіn) and the second is a new unknown tetraene antibiotic. In the antibiotic complex of S. violaceus IMV Ac-5027 two compounds has been isolated and identified as anthracycline antibiotics by rhodilunantsin A and rhodilunantsin B. The antinematode activity of its compounds was shown for the first time. It was established that S. netropsis IMV Ac-5025 and S. violaceus IMV Ac-5027 synthesize a complex of biologically active substances among which 17 free amino acids (up to 2898 μg/g of ADB), lipids (up to 220 mg/g of ADB) including free fatty acids, phospholipids (over 18%), mono- and diglycerides, triglycerides (over 50%), sterols (cholesterol, ergosterol, sitosterol, stigmasterol, 24-epibrassinolide from squalene precursor), sterol esters, waxes, chitinase and chitosanase enzymes, phytohormone-stimulants, such as auxins (up to 114 μg/g of ADB), cytokinins (up to 106 μg/g of ADB), gibberellins (up to 13 μg/g of ADA), and insignificant amounts of antystress hormone − abscisic acid were determined. An important role of the above biologically active substances on plant bioregulation and on the plant-microbe and microbe-microbe interactions was shown. The strategy of creation of new multicomponent polyfunctional bioformulations with phytoprotective, growth-stimulating and adaptogenic properties in one biotechnological process have been developed. On the basis of the streptomycetes metabolites complex, the Phytovit (the strain-producer is S. netropsis IMV Ac-5025), Violar (the strain-producer is S. violaceus IMV Аc-5027) and Avercom nova (the strain-producer is S. avermitilis IMV Аc-5015 with chitosan) bioformulations were proposed. At the molecular and cellular levels were identified the pathways of bioregulatory action of new bioformulations on silencing activity, phenylpropanoid and sterol synthesis, which results in increased plant resistance to biotic and abiotic stresses (priming effect). At the plant organism level the bioregulatory effect of metabolic bioformulations is expressed trough the ability to change the hormonal balance, to stimulate the growth and development of plant, to increase their productivity, to reduce the plant damage and improve the quality of crop production. Thus, the system approach to the study of complex metabolites of soil strepomycetes was theoretically substantiated and experimentally demonstrated. It was determined the biological (phytoprotective, growth-stimulating, adaptogenic) activity of bioformulations in bioregulation of plants at the molecular, cellular, and organism levels. This gives backgrounds for the creation of fundamentally new multicomponent biological products for the ecologically oriented phytosanitary optimization of agrocenosis.