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This study aimed to provide scientific data on the anti-Alzheimer’s disease (AD) effects of phenolic compounds from Drynariae Rhizoma (DR) extract using a multi-component approach. Screening of DR extracts, fractions, and the ten phenolic compounds isolated from DR against the key AD-related enzymes acetylcholinesterase (AChE), butyrylcholinesterase (BChE), β-site amyloid precursor protein cleaving enzyme 1 (BACE1), and monoamine oxidase-B (MAO-B) confirmed their significant inhibitory activities. The DR extract was confirmed to have BACE1-inhibitory activity, and the ethyl acetate and butanol fractions were found to inhibit all AD-related enzymes, including BACE1, AChE, BChE, and MAO-B. Among the isolated phenolic compounds, compounds (<b>2</b>) caffeic acid 4-O-β-D-glucopyranoside, (<b>6</b>) kaempferol 3-O-rhamnoside 7-O-glucoside, (<b>7</b>) kaempferol 3-o-b-d-glucopyranoside-7-o-a-L-arabinofuranoside, (<b>8</b>) neoeriocitrin, (<b>9</b>) naringin, and (<b>10</b>) hesperidin significantly suppressed AD-related enzymes. Notably, compounds <b>2</b> and <b>8</b> reduced soluble Amyloid Precursor Protein β (sAPPβ) and β-secretase expression by over 45% at a concentration of 1.0 μM. In the thioflavin T assay, compounds <b>6</b> and <b>7</b> decreased Aβ aggregation by approximately 40% and 80%, respectively, and degraded preformed Aβ aggregates. This study provides robust evidence regarding the potential of DR as a natural therapeutic agent for AD, highlighting specific compounds that may contribute to its efficacy.