Two heterodimeric diterpenoids (1 and 2) comprising abietane lactone and nor-rosane constituent units were isolated from Euphorbia ebracteolata roots. Compound 1 exhibited a moderate inhibitory effect on α-glucosidase (IC50 = 7.94 μM), with a Ki value of 10.8 μM. In silico molecular docking has been performed to investigate the inhibition mechanism. Compound 2 inhibited the acetyl transfer activity of Mycobacterium tuberculosis GlmU (IC50 = 41.85 μM), which is a novel tuberculosis treatment target.