公开(公告)号：US09198894B2

公开(公告)日：2015-12-01

申请号：US13823841

申请日：2011-10-19

申请人： Fengjuan Wu ,  Guifu Dai ,  Haiwei Xu ,  Zhiwen Jiang ,  Liping Zhu ,  Lijun Yan ,  Hongmin Liu ,  Yanan Wang ,  Weiyi Li ,  Ruijing Dong

发明人： Fengjuan Wu ,  Guifu Dai ,  Haiwei Xu ,  Zhiwen Jiang ,  Liping Zhu ,  Lijun Yan ,  Hongmin Liu ,  Yanan Wang ,  Weiyi Li ,  Ruijing Dong

IPC分类号： A61K31/365 ,  C07D307/33 ,  A61K31/341 ,  A61K45/06

CPC分类号： A61K31/341 ,  A61K31/365 ,  A61K45/06 ,  C07D307/33

摘要： 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.

摘要翻译： 本发明涉及具有穿心莲内酯衍生物的抗肿瘤药物的制备，属于制药领域，涉及14-脱氧-11,12-脱氢穿心莲内酯的15-亚苄基取代衍生物及其3,19- 酯衍生物。 通过实验证明，这些化合物显着抑制了各种癌细胞的集落形成和迁移能力，并且还抑制了体外血管内皮细胞的迁移能力。 本发明化合物显着抑制小鼠异种移植模型的肿瘤生长，侵袭，转移和血管生成，并抑制B16-F10恶性黑素瘤细胞的实验性肺转移。 因此，这类化合物可用作制备有效和低毒的抗肿瘤药物的活性成分。 因此，有可能扩大临床药物的可选范围，对充分利用穿心莲的植物资源具有重要意义。

公开(公告)号：US20130237596A1

公开(公告)日：2013-09-12

申请号：US13823841

申请日：2011-10-19

申请人： Guifu Dai ,  Haiwei Xu ,  Liping Zhu ,  Ruijing Dong ,  Fengjuan Wu ,  Yanan Wang ,  Zhiwen Jiang ,  Lijun Yan ,  Weiyi Li ,  Hongmin Liu

发明人： Guifu Dai ,  Haiwei Xu ,  Liping Zhu ,  Ruijing Dong ,  Fengjuan Wu ,  Yanan Wang ,  Zhiwen Jiang ,  Lijun Yan ,  Weiyi Li ,  Hongmin Liu

IPC分类号： A61K31/341 ,  A61K45/06 ,  C07D307/33

CPC分类号： A61K31/341 ,  A61K31/365 ,  A61K45/06 ,  C07D307/33

摘要： 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.

摘要翻译： 本发明涉及具有穿心莲内酯衍生物的抗肿瘤药物的制备，属于制药领域，涉及14-脱氧-11,12-脱氢穿心莲内酯的15-亚苄基取代衍生物及其3,19- 酯衍生物。 通过实验证明，这些化合物显着抑制了各种癌细胞的集落形成和迁移能力，并且还抑制了体外血管内皮细胞的迁移能力。 本发明化合物显着抑制小鼠异种移植模型的肿瘤生长，侵袭，转移和血管生成，并抑制B16-F10恶性黑素瘤细胞的实验性肺转移。 因此，这类化合物可用作制备有效和低毒的抗肿瘤药物的活性成分。 因此，有可能扩大临床药物的可选范围，对充分利用穿心莲的植物资源具有重要意义。