来自Solanum lyratum的生物活性索拉尼丹类类固醇化物
Tong Wu1, Xiao Du2, Hai-Hui Liu1
1Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China.
从Solanum lyratum中分离出六种新的类固醇类化合物. 利拉索拉诺B通过抑制JAK2/STAT3通路和上皮-介质酶过渡,有效地抑制肺癌细胞转移.
科学领域:
- 自然产品 化学 化学
- 药理学 药理学是指药理学的学科.
- 分子生物学分子生物学
背景情况:
- 索拉 (Solanum lyratum) 是一种生物活性化合物的植物来源.
- 类固醇类化合物具有不同的药理活性.
- 癌症转移涉及复杂的细胞信号通路.
研究的目的:
- 从Solanum lyratum中分离和表征新的类固醇化物.
- 评估分离化合物的抗癌潜力,特别是针对肺癌.
- 阐明活性化合物的抗转移作用背后的分子机制.
主要方法:
- 使用NMR,HRESIMS,UV,IR和ECD,对化物进行隔离和结构阐明.
- 对A549肺癌细胞的细胞毒性测定.
- 细胞迁移,入侵和粘附的评估.
- 对JAK2/STAT3信号通路和上皮层-介质细胞过渡 (EMT) 标记物的分析.
主要成果:
- 发现了6种新的索拉尼丹类类固醇化物 (lyrasolanosides A-F).
- 利拉索拉诺酸B显著抑制了A549细胞迁移,入侵和粘附.
- 利拉索拉诺B抑制了JAK2 / STAT3通路,并以外体依赖的方式降低化JAK2 / STAT3的调节.
- 利拉索拉诺B上调的E-cadherin和下调的N-cadherin和vimentin,表明抑制EMT.
结论:
- 利拉索拉诺酸B可以有效地抑制肺癌细胞转移.
- 抗转移机制涉及通过JAK2/STAT3通路抑制外体介导的上皮质-介质细胞过渡 (EMT).
- 利拉索拉诺酸B通过向转移来代表肺癌治疗的潜在治疗剂.
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