Kunming Institute of Botany, Chinese Academy of Sciences, PR China.
Bioorg Med Chem. 2010 Dec 1;18(23):8226-34. doi: 10.1016/j.bmc.2010.10.019. Epub 2010 Oct 31.
Six new (rubiyunnanins C-H, 1-6) and five known (7-11) cyclic hexapeptides were isolated from the roots of Rubiayunnanensis (Franch.) Diels. The structures and stereochemistry of 1-6 were established by extensive spectroscopic analyses and chemical methods. All compounds (1-11) not only exhibited cytotoxic activities against a panel of eleven cancer cell lines with IC₅₀ values ranging from 0.001 to 56.24 μM, but also exerted inhibitory activities against nitric oxide (NO) production in LPS and IFN-γ-induced RAW 264.7 murine macrophages with IC₅₀ values ranging from 0.05 to 12.68 μM. Furthermore, this is the first time it is being reported that compounds 2 and 7-10 significantly inhibited TNF-α-induced NF-κB activation in HEK-293-NF-κB luciferase stable cells with IC₅₀ values of 35.07, 0.03, 1.69, 12.64 and 1.18 μM, respectively.
从Rubia yunnanensis (Franch.) Diels 的根部分离得到了 6 个新的（rubiyunnanins C-H，1-6）和 5 个已知的（7-11）环状六肽。通过广泛的光谱分析和化学方法确定了 1-6 的结构和立体化学。所有化合物（1-11）不仅对一组 11 种癌细胞系具有细胞毒性活性，IC₅₀ 值范围为 0.001 至 56.24 μM，而且对 LPS 和 IFN-γ诱导的 RAW 264.7 鼠巨噬细胞中一氧化氮（NO）的产生具有抑制作用，IC₅₀ 值范围为 0.05 至 12.68 μM。此外，这是首次报道化合物 2 和 7-10 分别以 35.07、0.03、1.69、12.64 和 1.18 μM 的 IC₅₀ 值显著抑制 TNF-α诱导的 HEK-293-NF-κB 荧光素酶稳定细胞中 NF-κB 的激活。
