Plant-derived foods are esteemed as natural preventives due to the constraints of contemporary pharmaceuticals, intensifying scrutiny of traditional medicinal flora. This study marked the first extensive evaluation of the anti-diabetic, anticancer, and anti-inflammatory effects of Costus pictus rhizomes, expanding beyond its well-known anti-diabetic properties in leaves. Hot air-dried C. pictus rhizomes underwent ultrasound-assisted extraction to produce the rhizome extract. Anti-diabetic effects were determined through enzymatic inhibition studies targeting "α-amylase and α-glucosidase," crucial enzymes in glucose regulation, revealing potent inhibitory effects with IC50 values of 266.591 and 324.938 µg/ml, respectively. The ubiquity of breast cancer and constrained therapeutic alternatives for triple negative breast cancer led to the utilization of the "MDA-MB 231 cell line" for the study. The rhizome extracts demonstrated cytotoxicity at an IC50 concentration of 770 µg/ml, with a pronounced decline in the "reactive oxygen species (ROS)" and "mitochondrial membrane potential (MMP)." They also regulated the cell cycle arrest at the G2/M phase and positively induced apoptosis, thus making it a potent anticancer candidate. Anti-inflammatory effects were assessed using "RAW 264.7 macrophage cell line" and exhibited dose-dependent reduction with IC50 of 495.074 µg/ml, declining nitric oxide (NO) levels. Antimicrobial studies provided insights into its effectiveness against pathogens. This pivotal understanding laid groundwork for advancing C. pictus rhizome extract as a potential ingredient in pharmaceuticals or functional foods, leading to favorable health outcomes.