Bioactive substances in foods can represent ''extranutritional'' const
ituents naturally present in small quantities in the food matrix, prod
uced upon either in vivo or industrial enzymatic digestion, the latter
being a result of food-processing activities. Bioactive constituents
of food evoke physiological, behavioral, and immunological effects. Ev
idence from both epidemiological and animal studies has suggested chem
opreventative roles for phytochemicals in certain forms of cancers and
in the control of hyperlipidemia. Secondary products of plant metabol
ism can modulate xenobiotic metabolizing and cholesterol synthetic enz
ymes. Unique physicochemical properties of food-derived peptides with
characteristic amino acid composition and sequences have been reported
to influence intestinal transit, modify nutrient absorption and excre
tion, and exhibit immunostimulating and antihypertensive activity. Bio
logically active peptides derived from casein, fish muscle, and plant
protein hydrolysates have been isolated, purified, and identified in p
eptide sequence studies. Therapeutic proteins (e.g., specific antibodi
es) derived from animal products such as milk may offer the potential
for developing specialized food products with prophylactic as well as
nutritive quality. This paper discusses the physicochemical mechanism
of action of specific bioactive substances naturally present in or der
ived from foods. The biotechnologies employed to develop these product
s and the issues concerning acceptance by consumer and regulatory bodi
es are also addressed.