類黃酮已經被研究出許多抗癌活性,包括抗增生、促進細胞凋亡、抗血管新生和細胞週期阻斷。約有30%的乳癌和卵巢癌病人有HER2基因放大或是HER2過表現的現象,且HER2過表現和細胞轉移及抗藥性有關。一系列新穎的黃酮類化合物被用來探討其對癌細胞的抗癌作用。我們發現了Cpd3 (5,7-Dihydroxy-3’,4’-Diaminoflavone)在HER2過表現癌細胞中有明顯的抗癌活性,包括抗增生、抗轉移以及促進細胞凋亡。此外,Cpd3可以增加HER2過表現細胞細胞中的HER2降解。這些結果表明,Cpd3可能是透過降低HER2的表現量以抑制HER2過表現細胞的細胞生長。
Flavonoids have been studied for their anti-tumor properties, including anti-proliferative, proapoptotic, anti-angiogenic and cell cycle arrest activities in several cancer cells. Her2 is amplified and/or overexpressed in about 30% of ovarian and breast cancers and is associated with metastasis and drug resistance. A series of novel flavones were used to explore their anticancer effects on cancer cells. We found a 5,7-Dihydroxy-3’,4’-Diaminoflavone, Cpd3, with significant anti-tumor activities in HER2-overexpressing cancer cells, including anti-proliferative, anti-metastatic, and proapoptotic activities. Moreover, Cpd3 could increase the HER2 degradation in HER2-overexpressing cells. These data suggest that cpd3 suppress the HER2-overexpressing cancer cells growth may via down-regulation of HER2.