Cytotoxic and Pro-Apoptotic Effects of Cassane Diterpenoids from the Seeds of Caesalpinia sappan in Cancer Cells

摘要: The chemical study on the seeds of Caesalpinia sappan led to isolation five new cassane diterpenoids, phanginins R‒T (1–3) and caesalsappanins M N (4 5), together with seven known compounds 6–12. Their structures were elucidated basis NMR HRESIMS analyses. absolute configurations 1 4 determined by corresponding CD spectra. All isolated tested for their cytotoxicity against ovarian cancer A2780 HEY, gastric AGS, non-small cell lung A549 cells. Compound displayed significant toxicity four lines IC50 values 9.9 ± 1.6 µM, 12.2 6.5 5.3 1.9 12.3 3.1 respectively. induced G1 phase cycle arrest in Furthermore, compound dose-dependently cells apoptosis as evidenced Hoechst 33342 staining, Annexin V positive cells, up-regulated cleaved-PARP enhanced Bax/Bcl-2 ratio. What’s more, also promoted expression tumor suppressor p53 protein. These findings indicate that diterpenoids might have potential anti-cancer agents, further vivo animal studies structural modification investigation are needed.