This study investigated into the polyphenolic content, antioxidant and enzyme (α-amylase, α-glucosidase, tyrosinase, acetylcholinesterase [AChE], and butyrylcholinesterase [BChE]) inhibitory activities of 12 extracts of the endemic Asphodeline cilicica (AC) Tuzlaci, from Turkey. The total phenolic content for the methanol and acetone extracts of AC roots were 56.52 and 52.96 mg GAEs/g extract, respectively. Both the acetone and methanol extracts of AC roots exhibited an important antioxidant capacity. Likewise, the acetone and methanol extracts of AC roots revealed to be the most potent scavengers of DPPH radical (58.25 and 58.78 mg TEs/g extract). Acetone extract of AC roots inhibited α-amylase showing an acarbose equivalent value (mmol ACAEs/g extract) of 0.27, while against α-glucosidase the value recorded was 2.30. The acetone and methanol extracts of the different plant parts of AC inhibited AChE and BChE, while no/poor activity was noted for the water extracts. In the present study, extracts of AC showed inhibitory activity against key enzymes involved in diabetes and neurodegenerative complications, thereby advocating for the need for in-depth studies geared towards the discovery of pharmacophores from this endemic plant.