Abstract

Five new podocarpane trinorditerpenes (1–5) and a dimeric trinorditerpene with an unprecedented skeleton bearing a 1,4-benzodioxane moiety (6) along with seven known compounds (7–13) were isolated from the stems of Celastrus angulatus (Celastraceae). These compounds' structures were elucidated by comprehensive spectroscopic analysis. In addition, the absolute configuration of 1 was determined by single crystal X-ray diffraction analysis. Compounds 3, 4, 7, and 12 exhibited moderate inhibitory activity against LPS-induced NF-κB activation in murine macrophage RAW264.7 cells at IC50 values of 25.08, 18.64, 15.33 and 3.89 μM, respectively. However, compound 6 exhibited potent cytotoxicity against the A549 and MDA-MB-231 human tumour cell lines with IC50 values of 4.47 μM and 5.86 μM, respectively. Compound 9 exhibited potent cytotoxicity against the HCT116 and BEL7404 human tumour cell lines with IC50 values of 6.77 μM and 9.45 μM, respectively.

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