来自Tinospora crispa的cis-Clerodane类型的二甲和它们的抗癌潜力
Se Yun Jeong1, Jisun Kim2, Ji Won Ha1
1School of Pharmacy, Sungkyunkwan University, Suwon, 16419, Republic of Korea.
Archives of pharmacal research
|January 20, 2026
概括
Tinospora crispa叶片提取物产生了四种新的cis-clerodane二甲类药物. 化合物3通过向关键生存途径,对肝癌和肺癌细胞表现出强大的抗癌活性.
科学领域:
- 自然产品化学 自然产品化学
- 药理学 药理学是指药理学的学科.
- 药用化学 医学化学
背景情况:
- 提诺斯波拉克里斯帕 (Tinospora crispa) 是东南亚的一个传统草药药.
- cis-Clerodane类型的二甲类是Tinospora属的特征代谢产物.
- 研究T. crispa的新生物活性化合物对于药物发现至关重要.
研究的目的:
- 从Tinospora crispa的叶子中分离和描述新的cis-clerodane类型的四角体.
- 评估隔离化合物的抗癌潜力,以对抗肝癌和肺癌细胞系.
- 阐明最强效化合物的抗癌活性背后的分子机制.
主要方法:
- 使用LC/MS和UV光谱库提取和分离化合物.
- 使用NMR光谱,HR-ESIMS,PANIC,Snatzke方法和计算计算 (ECD,DP4+) 进行结构阐明.
- 使用肝 (Hepa1c1c7,Hepa1-6) 和肺 (LLC1,A549) 癌细胞系进行抗癌活性查.
- 对信号通路 (Hippo,AKT) 和亡标记物的分子分析 (Bax,分裂的caspase-3,BCL-2).
主要成果:
- 从T. crispa的叶子中分离出了四种新的cis-clerodane类型的二甲 (1-4) 和一种已知的化合物 (5).
- 所有测试的化合物 (1-5) 都显著降低了A549和LLC1癌细胞活力.
- 化合物3表现出强大和特定的抗癌作用,调节肝癌中的Hippo信号传递,并抑制肺癌中的支持生存的AKT通路.
- 化合物3通过增加Bax和分裂caspase-3并降低肺癌细胞中的BCL-2来诱导亡.
结论:
- Tinospora crispa diterpenoids 对肝癌和肺癌模型具有度依赖的抗癌活性.
- 化合物3是抗癌药物开发的有希望的主要候选者,因为它对关键癌症生存途径具有强大和特定的影响.
- 对化合物3的作用机制和体内疗效的进一步研究是有必要的.
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