Abstract: Bioactive peptides are defined as fractions of proteins containing 2-20 amino acids.After a long time investigation, currently, they exert specific regulations on the life activities of organisms.Moreover, the bioactivities of peptides are highly dependent on the molecular, amino acid composition and sequence which are impacted by their protein sources and preparation methods.Herein, rapeseed/canola is the third-most abundant oil crop worldwide and its annual yield is huge.Rapeseed/canola meal, as the by-product of rapeseed oil extraction, contains rich proteins with an excellent amino acid profile.And it has been known as a kind of high-quality plant protein source.But it is currently just used as animal feed with a low economic value.Fortunately, it is remarkable that rapeseed protein has been generally recognized as safe and approved for food use in the EU and the US, therefore, the prospects of its application will be broader.Moreover, rapeseed/canola protein hydrolysate or peptides extracted by enzymatic hydrolysis or fermentative hydrolysis have been proven to exert various biological activities such as antioxidant, antihypertensive, chelating effects and so on.It is supposed that rapeseed peptides will contribute to a higher value utilization of rapeseed industry to some extent.Nowadays, enzymatic hydrolysis is widely employed, and protease enzymes including proteinase K, collagenase, subtilisin A, alcalase, flavourzyme and neutrase are generally selected.It is well known that the bioactivities of peptides depend are highly on their molecular weight distribution, amino acid composition and sequence.Concurrently, their structure characteristics are affected by the protein sources, methods of production, isolation, purification, and molecular interaction.For example, an increase in the degree of hydrolysis is helpful to improve the antioxidant activity of peptides.Taken the practical application into consideration, the relationship between molecular structure and activity is necessary to be fully illustrated, also the processing stability and microenvironment stability, such as the effects of thermal and high pressure.Based on the above, firstly, the present review summarizes the methods and technologies for the production, isolation and purification of rapeseed/canola peptides.Secondly, the relationships between peptides structure and the bioactivity, as well as the underlying mechanisms also been discussed.Moreover, this review tries to analyze the future research trends of rapeseed peptides.This review provides a comprehensive insight of rapeseed/canola peptides and a technical support for the development and utilization of rapeseed bioactive peptides in the future.