This study, therefore, aimed to comparatively investigate the phenolic profiles, antioxidant activities, and inhibitory activities against the key enzymes involved in diabetes (α-glucosidase and α-amylase) and Alzheimer’s disease (acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and beta-secretase 1 (BACE-1)) in different fruit parts (exocarp, mesocarp (edible part), seed, and core) of Kadsura coccinea (Lem). The gene discussed is ACHE; the disease is early-onset autosomal dominant Alzheimer disease.