首页> 外国专利> APPLICATIONS OF TRIPTOLIDE AND DERIVATIVE THEREOF IN PREPARING MEDICAMENT FOR TREATING AND/OR PREVENTING LUNG-DAMAGING DISEASES

APPLICATIONS OF TRIPTOLIDE AND DERIVATIVE THEREOF IN PREPARING MEDICAMENT FOR TREATING AND/OR PREVENTING LUNG-DAMAGING DISEASES

机译:三环内酯及其衍生物在制备治疗和/或预防肺损伤疾病的药物中的应用

摘要

Provided in the present invention is a novel use of triptolide and of a derivative thereof. Triptolide can significantly inhibit elevation effects of GFP fluorescent protein and of P24 antigen in a phorbol ester-activated lymphocyte model, the higher the concentration of triptolide, the lower the percentage of GFP positive cells and the concentration of P24 antigen; hence, a negative dose-effect relation is present. Even when methylprednisolone is at a concentration as high as 400 uM, the inhibitory effects of same is not as good as that of triptolide at a concentration of 0.02 uM, while the ratio of apoptosis significantly exceeds that of triptolide at a concentration of 0.02 uM. The principle is such that triptolide inhibits G0/G1 phase cell ratio elevation and S phase cell ratio reduction caused by PMA, promotes a cell cycle to remain in an unactivated state; triptolide provides the effect of inhibiting lymphocyte proliferation and activation by regulating cell cycle and, at the same time, also provides the effect of inhibiting virus replication. The triptolide and the derivative thereof of the present invention can be used in place of or jointly with a glucocorticoid analogue for use in treating and/or preventing lung-damaging diseases.
机译:本发明提供了雷公藤甲素及其衍生物的新颖用途。雷公藤内酯醇可显着抑制佛波酯活化的淋巴细胞模型中GFP荧光蛋白和P24抗原的升高作用,雷公藤内酯醇浓度越高,GFP阳性细胞百分比和P24抗原浓度越低。因此,存在负剂量效应关系。即使当甲基强的松龙的浓度高达400uM时,其抑制效果也不如雷公藤甲素在0.02uM时的抑制效果,而其细胞凋亡率却大大超过雷公藤甲素在0.02uM时的抑制率。其原理是雷公藤甲素抑制PMA引起的G0 / G1期细胞比例升高和S期细胞比例降低,促进细胞周期保持未激活状态。雷公藤内酯醇具有通过调节细胞周期来抑制淋巴细胞增殖和激活的作用,同时还具有抑制病毒复制的作用。本发明的雷公藤内酯醇及其衍生物可代替或与糖皮质激素类似物一起用于治疗和/或预防肺损伤性疾病。

著录项

  • 公开/公告号WO2018210224A1

    专利类型

  • 公开/公告日2018-11-22

    原文格式PDF

  • 申请/专利权人 WANG XIAOHUI;

    申请/专利号WO2018CN86820

  • 发明设计人 WANG XIAOHUI;

    申请日2018-05-15

  • 分类号A61K31/585;A61K31/573;A61P11;A61P31/12;

  • 国家 WO

  • 入库时间 2022-08-21 11:58:07

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