Pregerminated brown rice (GBR) is assumed to be more beneficial than polished white rice (WR), with regard to nutrition and cardiovascular health. To support this with scientific evidence, cholesterol-lowering and antioxidative effects of GBR were studied in the present investigation. The most popular rice variety in Bangladesh BIRI-29 was used to prepare GBR and WR. Initially, we analyzed the proximate composition, antioxidative phytochemicals, in vitro 2, 2-diphenyl-1-picrylhydrazyl (DPPH)-free radical scavenging ability and anti-hemolytic effects of GBR. To examine the dietary impact and possible benefits of the GBR, experimentally-induced hypercholesterolemic (HC, 1% cholesterol) rats were fed with GBR against WR for 12 wk. At the end, plasma total cholesterol (TC), low- and high-density lipoprotein-cholesterol (LDL-C and HDL-C), triglyceride (TG), fecal TC, and hepatic TC, lipid peroxide (LPO) and proinflammatory TNFα levels were determined. Relative to WR, GBR contained higher amounts of total polyphenols, total flavonoids, β-carotene and lycopene, and exhibited a stronger in vitro DPPH-free radical scavenging ability and antihemolytic potentials. Levels of plasma TC, LDL-C, TG, and hepatic TC and TG significantly decreased, while plasma HDL-C and fecal TC levels significantly increased in the GBR-fed HC-rats, indicating dietary GBR demonstrates a stronger antilipidemic effect than WR. The hepatic levels of LPO and TNFα also decreased ( p <0.05) to a greater extent in GBR-fed HC-rats than those in the WR-fed rats. It is thus concluded that dietary GBR could be a natural treatment of hypercholesterolemia and related cardiovascular risk factors, and a source of antioxidants to reduce hemolysis and related anemia.