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The bioactive components of <i>Canavalia lineata</i> (Thunb.) DC pods were investigated using bioactivity-guided isolation, and the chemical structures of flavonoids <b>1</b>–<b>3</b>, isoflavonoid derivatives <b>4</b>–<b>11</b>, and phenolic compounds <b>12</b> and <b>13</b> were identified by comparing NMR, MS, and CD spectral data with previously reported spectroscopic data. Compounds <b>1</b>–<b>13</b> were evaluated for their anti-inflammatory effects on LPS-stimulated RAW264.7 macrophages. Among these compounds, the isoflavonoid derivative cajanin (<b>7</b>) exhibited the most potent anti-inflammatory activity (IC₅₀ of NO = 19.38 ± 0.05 µM; IC₅₀ of IL-6 = 7.78 ± 0.04 µM; IC₅₀ of TNF-α = 26.82 ± 0.11 µM), exerting its anti-inflammatory effects by suppressing the activation and nuclear translocation of the transcription factor NF-κB by phosphorylating IκB and p65. These results suggested that cajanin (<b>7</b>) may be a potential candidate for improving the treatment of inflammatory diseases.