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Four compounds (<b>1</b>, <b>5</b>, <b>7</b>, and <b>8</b>) were first isolated from the genus <i>Belamcanda Adans</i>. nom. conserv., and six known compounds (<b>2</b>–<b>4</b>, <b>6</b>, <b>9</b>, and <b>10</b>) were isolated from the <i>rhizome</i> of <i>Belamcanda chinensis</i> (L.) DC. Their structures were confirmed by spectroscopic data. Herein, compounds <b>1</b>–<b>10</b> were rhapontigenin, trans-resveratrol, 5,7,4′-trihydroxy-6,3′,5′-trimethoxy-isoflavone, irisflorentin, 6-hydroxybiochannin A, iridin S, pinoresinol, 31-norsysloartanol, isoiridogermanal, and iristectorene B, respectively. All compounds were evaluated for their antiproliferative effects against five tumor cell lines (BT549, 4T1, MCF7, MDA-MB-231, and MDA-MB-468). Among them, compound <b>9</b> (an iridal-type triterpenoid) showed the highest activity against 4T1 and MDA-MB-468 cells. Further studies displayed that compound <b>9</b> inhibited cell metastasis, induced cells cycle arrest in the G1 phase, exhibited significant mitochondrial damage in 4T1 and MDA-MB-468 cells including excess reactive oxygen species, decreased mitochondrial membrane potential, and induced 4T1 and MDA-MB-468 cell apoptosis for the first time. In summary, these findings demonstrate that compound <b>9</b> exerts promising potential for triple-negative breast cancer treatment and deserves further evaluation.