Rubiyunnanins C-H, cytotoxic cyclic hexapeptides from Rubia yunnanensis inhibiting nitric oxide production and NF-κB activation.
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.
Kunming Institute of Botany, Chinese Academy of Sciences, PR China.
Jun-Ting
JT
Fan
Jia
J
Su
Yan-Min
YM
Peng
Yan
Y
Li
Jia
J
Li
Yu-Bo
YB
Zhou
Guang-Zhi
GZ
Zeng
He
H
Yan
Ning-Hua
NH
Tan
D000818:Animals; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007371:Interferon-gamma / Q000378:metabolism; D008070:Lipopolysaccharides / Q000633:toxicity; D051379:Mice; D016328:NF-kappa B / Q000378:metabolism*; D009569:Nitric Oxide / Q000378:metabolism*; D009842:Oligopeptides / Q000737:chemistry* / Q000302:isolation & purification / Q000633:toxicity; D010456:Peptides, Cyclic / Q000737:chemistry* / Q000302:isolation & purification / Q000633:toxicity; D018517:Plant Roots / Q000378:metabolism; D017434:Protein Structure, Tertiary; D045470:Rubia / Q000378:metabolism*; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
D008070:Lipopolysaccharides; D016328:NF-kappa B; D009842:Oligopeptides; D010456:Peptides, Cyclic; D014409:Tumor Necrosis Factor-alpha; D009569:Nitric Oxide; D007371:Interferon-gamma