There is growing evidence for the protective effect of plant bioactives against diseases, and this has led to interest from the functional food and nutraceutical industries for the development of bioactive-enriched food and supplements. The oil palm fruit is a source of both lipid- and water-soluble bioactives. This chapter begins by considering lipid-soluble bioactives and their potential health benefits. It then moves on to considering water-soluble bioactives, which have only recently received attention. These include phenolic compounds and shikimic acid with potential health benefits against a whole spectrum of diseases including cardiovascular diseases, cancer and diabetes. These water-soluble compounds enter the aqueous stream (vegetation liquor) and are usually discarded as palm oil mill effluent. The valorization of palm oil milling waste for the production of functional food and nutraceuticals offers an opportunity for increased productivity and sustainability of the oil palm industry.