Grain sorghum (GS) lipid contains valuable phytochemicals that may have potential critical health benefits. Although the chemical composition of GS lipids varies among studies due to different extraction methods, intrinsic factors, such as variety, and the analytical methods applied, it has been consistently reported that GS lipids contain phytosterols, policosanols, unsaturated fatty acids, aldehydes and steryl/wax esters. A series of hamster studies showed that GS lipids exerted health-benefiting effects on cholesterol metabolism and intestinal microbiota. In-vitro experiment with a colon cancer cell line also showed its possible role in cancer inhibition. Exact mechanisms and bioactive compounds related to these effects have not been elucidated. Studies are in progress to understand the possible health benefitting mechanisms as well as to determine the responsible bioactive compounds.