提取优化和7α-acetoxy-6β-hydroxyroyleanone的反应性及其衍生物调节PKC异型的能力
Vera M S Isca1,2, Gabrielle Bangay1,3, Salvatore Princiotto1,4
1CBIOS - Center for Research in Biosciences and Health Technologies, Universidade Lusófona, 1749-024, Lisboa, Portugal.
这项研究探讨了Plectranthus grandidentatus提取物用于抗癌化合物,合成新的罗伊兰衍生物来调节乳腺癌治疗的蛋白激酶C (PKC). 衍生品RoyBz显示出显著的细胞毒性潜力,突出了其进一步开发的前景.
科学领域:
- 自然产品化学 自然产品化学
- 药用化学 医学化学
- 药理学 药理学是指药理学的学科.
背景情况:
- 蛋白激酶C (PKC) 与癌症发生有关.
- 普莱克兰修斯 (Plectranthus spp.) 的一种植物. 是一个丰富的阿比他的来源,包括7α-acetoxy-6β-hydroxyroyleanone (Roy).
研究的目的:
- 为了从P. grandidentatus中提取和分离罗伊.
- 在乳腺癌治疗中合成用于PKC调节的新型罗伊兰衍生物.
- 评估这些化合物的细胞毒性和PKC激活潜力.
主要方法:
- 对 CO2 超临界和超声波辅助酸提取用于罗伊隔离的比较.
- 化和乙化罗伊兰衍生物的化学合成.
- 对乳腺癌细胞系的细胞毒性测定.
- 评估PKC异形激活 (PKC-α,βI, δ, ε, ζ) 的情况.
- 分子对接分析. 分子对接分析.
主要成果:
- 超声波辅助的提取产生了更高度的罗伊.
- 罗伊Bz证明了对乳腺癌细胞系最重要的细胞毒性潜力.
- 在C-12位置的化是有效的,而脱化显示出更好的细胞毒性.
- 德罗伊激活了所有测试的PKC异型,而RoyPr对PKC-δ.表现出选择性.
- 分子对接突出了影响异形特异性的微环境因素.
结论:
- 罗伊及其衍生品,特别是RoyBz,在乳腺癌治疗方面表现有前途.
- 结构性修改影响细胞毒性和PKC异型选择性.
- 需要进一步的研究来探索这些royleanones的治疗潜力.
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