The present research aimed at studying different bioactive constituents and the potential hypolipidemic effect of the roasted ‎lemon powder along with the anticancer activity of its methanol extract. Volatile compounds and fatty acids′ profile in ‎roasted lemon were analyzed. Individual phenolic compounds and total phenolic and flavonoidal contents and DPPH● ‎scavenging capacity of the methanol extract were determined. The anticancer activity of the extract was evaluated in human ‎cell line from hepatocellular carcinoma (Hep-G2) and breast adenocarcinoma (MCF-7). The hypolipidemic effect of roasted ‎lemon was assayed in Triton X-100 induced hyperlipidemic rat. Results demonstrated D-Limonene to be the major volatile ‎compound while hisperdin was the main phenolic compound. Total phenolics, flavonoids and DPPH● scavenging activity ‎were 8.59± 0.098 mg gallic acid equivalent, 8.10± 0.17 mg catechin equivalent and 5.05± 0.07 mg trolox equivalent/g, ‎respectively. Linoleic acid was the major fatty acid while linolenic acid was present as 10.04%. The anticancer activity of ‎the extract showed IC50 to be 240 and 148µg/ml towards Hep-G2 and MCF-7, respectively. In-vivo experiment ‎demonstrated that intake of roasted lemon improved hyperlipidemia and reduced cardiovascular risk factor, ‎malondialdehyde, transaminases, creatinine and body weight gain. It could be concluded that roasted lemon methanol ‎extract showed anticancer activity towards Hep-G2 and MCF-7, with superiority to MCF-7. The roasted lemon possessed ‎hypolipidemic and antioxidant activities along with cardio-, hepato- and reno-protective effects with body weight reducing ‎ability. Such effects might be related to the presence of volatile compounds specially D- Limonene, the phenolic and ‎flavonoidal compounds and linolenic acid. ‎