ABSTRACT: Lignans are compounds found in a variety of plant materials including flaxseed, pumpkin seed, sesame seed, soybean, broccoli, and some berries. The major lignan in flaxseed is called secoisolariciresinol diglucoside (SDG). Once ingested, SDG is converted in the colon into active mammalian lignans, enterodiol, and entero-lactone, which have shown promise in reducing growth of cancerous tumors, especially hormone-sensitive ones such as those of the breast, endometrium, and prostate. Known for their hydrogen-donating antioxidant activity as well as their ability to complex divalent transition metal cations, lignans are propitious to human health. The extraction methods vary from simple to complex depending on extraction, separation, fractionation, identification, and detection of the analytes. Flax lignan is also a source of useful biologically active components found in plant foods, such as phytochemicals, and it is considered a functional food. The safety issues in flaxseed are also briefly discussed.