Although 5-n-alkylresorcinols can be isolated from a wide array of sources, alkylresorcinols (ARs) in edible food sources are of the greatest advantage. The abundance of ARs in wholegrain cereals and their exclusive presence in the bran fraction, allows for ARs to be an excellent candidate as biomarkers of wholegrain intake. The role of ARs as biomarkers is extremely important for validation of the disease preventative properties and health benefits resulting from the inclusion of whole grains in the diet. Numerous studies on the pharmacokinetics of ARs in in vivo and in vitro have determined that levels of whole grains consumed in the diet correlate with levels of intact ARs measured in the faeces as well as AR metabolites extracted from urine samples of these individuals. Recently, it has been suggested that ARs can also be used as long-term biomarkers of whole grain intake. A small percentage of ARs consumed from whole grains often reside in the adipose tissue and accumulated proportions correlate with long term intake. In addition to the role of ARs as biomarkers, these phenolic lipids owe to their amphiphillic structure their varying degree of biological effects. ARs possess antimicrobial, antioxidant, and cytotoxic activity, as well as inhibitory or stimulatory effects on enzymes, and stabilizing or disruptive effects on the phospholipid bilayer of cell membranes. These effects are dependent on the chain length, degree of saturation, chain or ring constituents, and the concentration of AR homologues present; these factors affect their hydrogen donating capacity, amphiphillic or lipophilic nature, polarity, hydrophobicity, binding capacity, as well as their ease of integration and interaction with enzymes, proteins and membranes. The ability of ARs to reduce or inhibit triglyceride accumulation, tumour cell formation, thromboxane synthesis, and enhance liposome stability, makes them suitable for respective applications of obesity, cancer, and cardiovascular disease prevention (CVD), as well as liposomal drug delivery. However, future research, particularly that of in vivo studies, need to be conducted on the biological effects and health benefits of ARs before their potential application can be employed. Furthermore, a common trend is evident in studies on the bioactivity of ARs such that homologs of 15 to 17 carbon chains have more pronounced biological effects than their shorter and longer chain counterparts; Thus, emphasis should be placed on these chain lengths for future in vivo studies.