A pharmacological composition for use in inhibiting differentiation, functional activities, and population of granulocytic myeloid-derived suppressor cells (gMDSCs) and/or suppressing, tumor metastasis in a subject in need thereof is disclosed. The composition comprises a therapeutically effective amount ofBidens pilosaextract, or more than one polyacetylenic compounds purified or isolated from theB. pilosaextract, and a pharmaceutically acceptable carrier.本發明係揭示一種醫藥組合物,在有需要的個體中抑制顆粒球骨髓來源抑制細胞(gMDSCs)的分化、功能活性以及細胞群體及/或抑制腫瘤轉移的用途。該組合物包含治療有效劑量的大花咸豐草萃取物,或超過一個由大花咸豐草萃取物分離而得的聚乙炔化合物,以及藥學上可接受載體。