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目的:建立新型的细胞水平组织因子抑制剂高通量药物筛选模型, 对本中心库存天然化合物进行筛选, 得到对TF有较好抑制作用的天然化合物, 用于进一步评估抗肿瘤转移药物。方法:利用发色底物法, 建立细胞水平TF抑制剂高通量筛选模型, 用该细胞株进行抗肿瘤转移药物筛选。结果:选用人乳腺癌细胞MDA-MB-435成功建立了快速稳定、灵敏度高、操作简便的抗肿瘤转移药物筛选模型。筛选1260种化合物, 经过初筛、复筛和体内评价发现短葶山麦冬皂苷-C(DT-13)对TF的抑制作用比较明显, 并具有一定的抗肿瘤转移作用。结论:通过建立的TF抑制剂筛选模型, 对库存天然产物进行筛选, 得到具有抗肿瘤转移的天然产物DT-13。
OBJECTIVE: To establish a new high-throughput screening model of tissue factor inhibitors at the cellular level and to screen natural compounds in the stock of our institute to obtain natural compounds that have a good inhibitory effect on TF for further evaluation of anti-metastatic drugs. Methods: By using the chromogenic substrate method, a high-throughput screening model of TF-inhibitor at the cellular level was established, and the cell line was used to screen anti-tumor metastatic drugs. Results: The human breast cancer cell line MDA-MB-435 was successfully used to establish a rapid, stable, sensitive and easy-to-use anti-metastatic drug screening model. 1260 compounds were screened. After preliminary screening, re-screening and in vivo evaluation, the inhibitory effect of Radix Ophiopogon japonicus-C (DT-13) on TF was obvious and had certain anti-tumor metastasis effect. Conclusion: The natural product DT-13 with anti-tumor metastasis was screened through the established TF inhibitor screening model.