Tran M.H.,Vietnam National University, Ho Chi Minh City |
Nguyen M.T.T.,Vietnam National University, Ho Chi Minh City |
Nguyen H.D.,Vietnam Academy of Science and Technology |
Nguyen T.D.,Vietnam Academy of Science and Technology |
Phuong T.T.,Vietnam National Institute of Medicinal Materials VNIMM
Pharmaceutical Biology | Year: 2015
Context: Caesalpinia sappan Linn. (Leguminosae) has been used in folk medicines for the treatment of many diseases. The heartwood of this plant contains various phenolic components with interesting biological applications; however, the chemical and biological potentials of the seed of this plant have not been fully explored. Objective: This study identified the cytotoxic activity of compounds from the seeds of C. sappan. Materials and methods: The methanol extract of the seed of C. sappan was suspended in H2O and then partitioned with CH2Cl2, EtOAc, and n-BuOH, successively. Diterpenoid compounds were isolated from the CH2Cl2-soluble fraction by silica gel column chromatography methods using organic solvents. The compound structures were determined by detailed analysis of NMR and MS spectral data. Cytotoxic activity was measured using a modified MTT assay against HL-60, HeLa, MCF-7, and LLC cancer cells. The activation of caspase-3 enzyme and western blotting assay were performed to confirm inhibitory mechanism of active compound. Results: Five cassane-type diterpenoids were isolated and identified as phanginin I (1), phaginin A (2), phanginin D (3), phanginin H (4), and phanginin J (5). Compounds 1-4 showed effective inhibition against HL-60 cells with the IC50 values of 16.4± 1.5, 19.2 ± 2.0, 11.7 ± 1.6, and 22.5± 5.1 mM. Compounds 1-3 exhibited cytotoxic activity against HeLa cells with the IC50 values of 28.1 ± 3.6, 37.2 ±3.4, and 22.7 ± 2.8 mM. Treatment of HL-60 cell lines with various concentrations of 3 (0-30 mM) resulted in the growth inhibition and induction of apoptosis. Conclusion: These findings demonstrate that compound 3 (phanginin D) is one of the main active components of the seed of C. sappan activating caspases-3 which contribute to apoptotic cell death. © 2015 Informa Healthcare USA, Inc.