Rice bran and rice bran protein are important sources of minerals, energy, and vitamins. Other bioactive compounds are abundantly available to exert therapeutical activity. Healthpromoting activities of high-value compounds of rice bran were significant, as observed in recent studies. A variety of bioactive components present in rice bran and rice bran extract are responsible to exhibit therapeutical potential like chemopreventive, cardioprotective, hepatoprotective, immunomodulatory, neuroprotective, and lipid-lowering activity. Several bioactivity representative compounds like γ-oryzanol, ferulic acid, caffeic acid, tricin, protocatechuic acid, vanillic acid, coumaric acid, phytic acid, isoferulic acid, gallic acid, γ-amino butyric acid, sinapic acid, saturated and unsaturated fatty acids, vitamin E complexes, β-sitosterol, stigmasterol, campesterol, cyanidin-3-glucoside, peonidin-3-glucoside, quercetin, rutin, kaemferol, β-carotene, lutein, vitamin B and lycopene are known to display significant health benefits. The bioactive components produced therapeutical effects by regulation of different mechanisms like increasing faecal excretion, reducing oxidative stress, reducing the level of malondialdehyde (MDA), regulation of NF-kb activation, reduction of proinflammatory cytokines production, suppression of SREBP-1, reduction in the expression of anti-apoptotic protein Bcl-2, elevated the expression of proapoptotic protein Bax, up-regulating P53 expression and suppressing COX-2. Several research engines like PubMed, google scholar, science direct, etc. were used to collect the data on the mentioned keywords. Recent scientific works were included in this article. In this review paper, we profiled the high-value compounds and focused on their antioxidant, anti-hyperlipidemic, antidiabetic, and anticancer activity with their possible mechanism of action.