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Neuroinflammation, predominantly mediated by microglial activation, is a key immunological response in the pathogenesis of neurodegenerative disorders. In our preliminary study, the aerial part of <i>Artemisia iwayomogi</i> inhibits LPS-induced microglial activation. The present study aims to identify chemical constituents with anti-neuroinflammatory properties in the aerial parts of <i>A</i>. <i>iwayomogi</i>. Two new guaianolide sesquiterpenes, iwayomogins A and B (<b>1</b> and <b>2</b>), along with thirteen known sesquiterpene lactones (<b>3</b>–<b>15</b>), one diterpene glycoside (<b>16</b>), and nine phenolic compounds (<b>17</b>–<b>25</b>) were isolated from the aerial parts of <i>A</i>. <i>iwayomogi</i> by repeated chromatography. The structures of the isolates were elucidated by their spectroscopic data. All isolates were evaluated for their inhibitory activities on nitric oxide (NO) production in LPS-induced BV-2 microglial cells. 2,3-Dehydro-1-<i>epi</i>-asperilin (<b>11</b>) exhibited the strongest inhibitory effect on NO production (IC₅₀ value of 1.78 μM). In the molecular docking study, three compounds (<b>1</b>, <b>2</b>, and <b>11</b>) showed good binding affinities with iNOS. Additionally, compounds <b>1</b>, <b>2</b>, and <b>11</b> inhibit pro-inflammatory cytokines (TNF-α and IL-6) in dose-dependent manners. The present study demonstrates that the chemical constituents from <i>A</i>. <i>iwayomogi</i> inhibit NO production and pro-inflammatory cytokine release in BV-2 cells. However, further evaluation with biological experiments utilizing in vivo models is necessary.