forsskolii Hypoestes 中的 Fusicoccane 二萜作为热休克蛋白 90（Hsp90）调节剂。
Fusicoccane Diterpenes from Hypoestes forsskaolii as Heat Shock Protein 90 (Hsp90) Modulators.
机构信息
Dipartimento di Farmacia , Università degli Studi di Salerno , Via Giovanni Paolo II 132 , 84084 Fisciano ( SA ), Italy.
Department of Pharmacognosy, Faculty of Pharmacy , Umm Al-Qura University , 21955 Makkah , Saudi Arabia.
出版信息
J Nat Prod. 2019 Mar 22;82(3):539-549. doi: 10.1021/acs.jnatprod.8b00924. Epub 2019 Mar 6.
Ten new (1-10) and six known (11-16) fusicoccane diterpenes were isolated from the roots of Hypoestes forsskaolii. The structural characterization of 1-10 was performed by spectroscopic analysis, including 1D and 2D NMR, ECD, and HRESIMS experiments. From a perspective of obtaining potential Hsp90α inhibitors, the isolates were screened by surface plasmon resonance measurements and their cytotoxic activity was assayed using Jurkat and HeLa cancer cells. Compound 6, 18-hydroxyhypoestenone, was shown to be the most active compound against Hsp90, and its interactions were studied also by biochemical and cellular assays and by molecular docking.
从 Hypoestes forsskaolii 的根部分离得到了 10 个新的（1-10）和 6 个已知的（11-16） fusicoccane 二萜类化合物。通过光谱分析，包括 1D 和 2D NMR、ECD 和 HRESIMS 实验，对 1-10 的结构特征进行了表征。从获得潜在的 Hsp90α抑制剂的角度出发，通过表面等离子体共振测量对分离物进行筛选，并使用 Jurkat 和 HeLa 癌细胞测定其细胞毒性活性。化合物 6，18-羟基hypoestenone，对 Hsp90 的抑制活性最强，还通过生化和细胞测定以及分子对接研究了其相互作用。
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