The effect pine bark activation by explosive autohydrolysis and mechanical treatment in a ball mill on the yield and properties of resinous and pectin substances and β-sitosterol was studied. Pine bark physicochemical properties after its activation by a batch of methods were studied. It was shown that the activation of pine bark by explosive autohydrolysis result in the highest increase in the yield of extractive substances. The conditions providing the highest yield of target products from the activated pine bark were determined: for resinous substances and β-sitosterol - the use of 0.5 n alkali solution; for pectin substances - the use of hydrochloric acid.