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[摘要]
很多抗癌药物由于血脑屏障的限制对脑瘤作用比较差,不利于药物的吸收。紫杉醇是二萜类天然产物,其在体外能有效地抑制恶性脑胶质瘤的生长,但并不能显著提高恶性脑胶质瘤患者存活时间,其原因主要是紫杉醇在血浆中消除太快,血脑屏障渗透能力差等导致肿瘤部位吸收过低。为了解决这个问题,一种可靶向低密度脂蛋白受体相关蛋白-1(LRP-1)的19个氨基酸的肽Angiopep-2与3分子紫杉醇结合构成ANG1005,ANG1005与LRP-1结合作用后可以促使受体介导的药物通过跨细胞转运进入脑组织中。
[Key word]
[Abstract]
Owing to the limit of the blood-brain barrier (BBB) many anticancer drugs have undesirable effect on brain tumors with less benefit for drug absorption. Paclitaxel, a natural product belonging to diterpene, could effectively inhibit the growth of malignant glioma and brain metastases in vitro. However it could not significantly improve survival time of patient suffered from malignant glioma. The main reason is that paciltaxel is eliminated too fast in the plasma and the BBB penetration ability is too low causing lower absorption at tumor sites. To overcome this problem, a targeted low-density lipoprotein (LDL) receptor-related protein-1 (LRP-1) of 19-amino acid peptide Angiopep-2 and three molecular paclitaxel constitute ANG1005. After combination of ANG1005 and LRP-1, receptor-mediated drugs could be promoted to brain tissue through cell transportation.
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