The present invention relates to the preparation of anti-tumor drugs with andrographolide derivatives, which belongs to the field of pharmaceutical technology, and involves 15-benzylidene substituted derivatives of 14-deoxy-11,12-didehydro-andrographolide and their 3,19-ester derivatives. Proved by the experiments, these compounds significantly inhibited the colony formation and migration ability of various cancer cells, and also inhibited the migration ability of vascular endothelial cells in vitro. The compounds of this invention significantly inhibited the tumor growth, invasion, metastasis and angiogenesis on mouse xenograft models, and inhibited the experimental lung metastasis of B16-F10 malignant melanoma cells. Therefore, this class of compounds could be used as the active ingredients for the preparation of antineoplastic drugs, which are of efficiency and low-toxicity. Thereby it has potential to expand the selectable range of clinical drug and is of high significance to make full use of the plant resources of Andrographis paniculata.本発明は医薬技術分野に属し、アンドログラホリド誘導体の抗腫瘍薬の調製における使用を開示し、15-ベンジリデン-14-デオキシ-11,12-ジデヒドロアンドログラホリド誘導体及びその3,19エステル化物に関する。この種の化合物は腫瘍細胞のクローン形成及び移動を顕著に抑制でき、抗ヒト血管内皮細胞移動作用を有し、マウス移植腫瘍動物モデルにおいて強い腫瘍成長抑制、抗侵襲転移、抗血管生成作用を示し、マウスメラノーマB16-F10肺転移モデルにおいて良好な抗転移作用を示すことが実験により証明された。この種の化合物を活性成分として抗腫瘍薬の調製に用いると、高い効果と低い毒性を示すため、腫瘍の治療と転移予防に新たな医薬品経路を提供し、臨床用薬の選択可能範囲を広げることができ、アンドログラフィス・パニクラタ植物資源の十分な利用に重要な意味を持つ。【選択図】なし
