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<i>Gastrodia elata</i> is widely used in traditional medicine and contains various types of metabolites with pharmacological activity. In the course of searching for neuroprotective molecules associated with the potential of <i>G. elata</i> in the treatment of neurodegenerative disorders, two new phenolic compounds (<b>1</b> and <b>2</b>) and a new tripeptide (<b>3</b>), together with 16 known compounds (<b>4</b>–<b>19</b>), were isolated from the rhizomes of <i>G. elata</i>. The structures of the compounds were determined by the interpretation of spectroscopic data, including nuclear magnetic resonance and mass spectrometry data. All obtained compounds were assessed for their ability to protect neuronal cells against neurotoxicity and neuroinflammation. Of these, <b>4</b> and <b>5</b> were found to possess moderate activities in HT22 hippocampal neuronal cells, whereas <b>2</b>, <b>6</b>, and <b>7</b> showed weak activities in R28 retinal cells. Additionally, compound <b>9</b> showed moderate inhibitory activity on lipopolysaccharide-induced nitric oxide production in BV2 microglial cells.