The objectives of this study were to investigate the lipase and α-Glucosidase inhibitory activity of the ethyl acetate and methanol extracts from Thaeogyroporus porentosus, and also isolate the bioactive compounds. The results showed that ethyl acetate extract at 25 and 1 mg/mL display lipase activity of 78% and α-Glucosidase inhibitory of 20% respectively, which methanol extracts at 25 and 10 mg/mL displayed an lipase inhibitory activity of 99 and α-Glucosidase inhibitory activity of 38 % respectively. The extract was examined of againt 5 cancer cell line (Lung cancer cell (Chago-K1), Gastric cancer cell (KATO-III), Hepatic cancer cell (Hep-G2 ), Breast cancer cell (BT474), Intestine cancer cell (SW620) and Fibroblast cell (Wi-38)). In addition, the ethyl acetate extract exhibited cytotoxic activity against lung and hepatic cancer cells which its IC₅₀ showed 32 and 40 μg/mL and the methanol extract exhibited cytotoxic activity against lung cancer cells which its IC₅₀ showed 79 μg/mL. The ethyl acetate crude extract was thus isolated by column chromatography technique. Due to unstable bioactive compounds of the extract isolation process was unsuccessful. However, ¹H-NMR data revealed that ethyl acetate extract compound of terpenoids and steroids.