Biological active compounds in tea such as phenolic compounds have become a focus of research due to their health-beneficial impacts on the human body as well as disease prevention. Moreover, these substances also have beneficial functions as they work as food preservatives. Polyphenols are known to form a complex with protein molecules leading to change in several properties. In this review, the effect of protein-polyphenol interaction on the structure, functionality, nutritional and digestive system as well as the inhibition activity of cytochrome 450 (CYP450) and drug interaction were described. Also, the chemical bonding, which discovered leading to precipitation and changes of protein structure were explained. The feasibility of proteins-polyphenols interaction cause associated with the ability on the digestive system whether enhance the enzymatic activity for digestion or a negative effect of the enzyme inhibition activity. As the bioactive compounds attracting consumer attention in recent years and they do not provide only an advantage side, therefore, it should be significantly studied what impacts to the human body these substances include which are helpful for further investigation.