In this invention, we used the in vitro cell-based ALDH activity assay system to screen for the active purified components from Antrodia camphorata Mycelia extract (ACME), which can target OC-CICs. Consequently, we found ACME purified compounds (CH-190-WS-A and CH-190-WS-D) can significantly down regulate the ALDH activity of oral cancer cells or OC-CICs. Treatment of CH-190-WS-A and CH-190-WS-D significantly induced cell death and enhanced the differentiation capability of OC-CICs. Moreover, we found that treatment of CH-190-WS-A and CH-190-WS-D reduced the self-renewal ability and stemness properties of OC-CICs, and also lessen the tumorigenic properties including cell migration and anchorage independent growth of oral cancer cell.Overall, our studies reveal the ACME purified components can reduce stemness properties and tumorigenicity of OC-CICs. Eventually, we can discover drug candidates from ACME purified components for alternative oral cancer treatment.本發明係為具標靶癌幹細胞活性之樟芝菌絲體萃取物及篩選方法。首先利用活體外藥物篩選平台,進而以醛脫氫酶檢測套組篩選出樟芝菌絲體萃取物中可調降各類固態腫瘤細胞(如:頭頸癌)之醛脫氫酵素活性之活性物質,該活性物質係為CH-190-WS-A與CH-190-WS-D,CH-190-WS-A與CH-190-WS-D能降低頭頸癌起始細胞自我更新能力和幹細胞特性,並促進頭頸癌起始細胞之死亡和分化。藉由本案發明,可找到有效降低癌幹細胞基因表現的樟芝菌絲體萃取物之標靶藥物。