4.7 Article

Triterpenes from the Aerial Parts of Cimicifuga yunnanensis and Their Antiproliferative Effects on p53N236S Mouse Embryonic Fibroblasts

Journal

JOURNAL OF NATURAL PRODUCTS
Volume 76, Issue 5, Pages 896-902

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/np4000262

Keywords

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Funding

  1. National Natural Science Foundation of China [U1132604]
  2. Knowledge Innovation Program of the CAS [KZCX2-XB2-15-03, KSCX2-EW-R-15]
  3. Top Talents Program of Yunnan Province [2009C1120]
  4. Foundation of State Key Laboratory of Phytochemistry and Plant Resources in West China [P2010-ZZ14]

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Nine new triterpene derivatives, yunnanterpenes A-F (1-6), 15,16-seco-cimiterpenes A and B (7, 8), and cimilactone C (9), and 15 known analogues (10-24) were isolated from the aerial parts of Cimicifuga yunnanensis. The new structures were established using a combination of MS, NMR, and single-crystal X-ray diffraction techniques. WT MEFs (wildtype mouse embryonic fibroblasts) and tumorigenic cell lines p53(-/-)+H-RasV12 and ps3(-/-)+p53(N236S)+H-RasV12 were used for evaluating active structures, targeting p53(N236S) (corresponding to p53(N239S) in humans) mutation. Compound 5 showed nonselective activities against these cell lines, with IC50 values of 5.8, 8.6, and 6.0 mu M, respectively. Compound 4 exhibited greater selectivity against the p53(-/-)+p53(N236S)+H-RasV12 cells (IC50 5.5 mu M) than against the WT MEFs cells (IC50 14.3 mu M).

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