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发明公开
CN105796580A 一种蛋白酶体活性抑制剂PI在制备防治骨肉瘤药物或保健食品中的应用 无效 - 驳回

一种蛋白酶体活性抑制剂PI在制备防治骨肉瘤药物或保健食品中的应用
摘要：
本发明属医药技术领域，涉及一种蛋白酶体活性抑制剂PI在制备预防和治疗原发性和继发性骨肉瘤药物或保健食品中的应用。本发明的实验结果显示，所述的蛋白酶体抑制剂PI，对蛋白酶体的糜蛋白酶(CT)样活性具有选择性抑制作用；所述蛋白酶体抑制剂PI通过抑制NF-κB通路和活化未折叠蛋白反应(UPR)/内质网(ER)应激在骨肉瘤细胞中的信号级联反应等诱导骨肉瘤细胞凋亡；同时，所述PI通过下调c-Myc等信号通路来调节骨肉瘤细胞的细胞周期和生长；另一方面，所述PI通过下调Vimentin、Snail、Slug和上调E-cadherin表达逆转骨肉瘤细胞的EMT。结果表明，所述PI作为一种新型的天然蛋白酶体抑制剂，具有预防和治疗骨肉瘤的潜力，可用于制备预防和治疗原发性和继发性骨肉瘤药物或保健食品。
摘要（英）：

The invention belongs to the technical field of medicines and relates to a use of a proteasome activity inhibitor PI in preparation of a drug or a health food for preventing and treating osteosarcoma. An experiment result shows that the proteasome activity inhibitor PI has selective inhibition effects on proteasome chymotrypsin (CT)-type activity, the proteasome activity inhibitor PI can induce osteosarcoma apoptosis through inhibition of NF-kB pathway and activation of unfolded protein reaction (UPR)/endoplasmic reticulum (ER) stress signal cascade in osteosarcoma cells, the PI adjusts an osteosarcoma cell cycle and growth through decreasing of a c-Myc signal path and the PI reverses osteosarcoma cell EMT through decreasing of Vimentin, Snail and Slug and increasing of E-cadherin expression. The result shows that the PI can be used as a novel natural proteasome inhibitor, has a potential of osteosarcoma prevention and treatment and can be used for preparing a drug or a health food for preventing and treating idiopathic and secondary osteosarcoma.

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