Cytotoxic constituents from the seeds of Vietnamese Caesalpinia sappan

Figures & data

Figure 1. Chemical structure of diterpenoids 1–5 from seeds of Vietnamese C. sappan.

Table 1. Cytotoxic activity of compounds 1–5 from the seed of C. sappan.

	IC50 values (μM)^a
Fractions/compounds	HL-60	HeLa	MCF-7	LLC
CH2Cl2 fraction^b	46.9 ± 10.5	117.5 ± 12.6	>200	>200
EtOAc fraction^b	58.7 ± 7.1	68.4 ± 5.9	117.6 ± 5.6	>200
n-BuOH fraction^b	>200	>200	>200	138.8 ± 8.6
1	16.4 ± 1.5	28.1 ± 3.6	>100	>100
2	19.2 ± 2.0	37.2 ± 3.4	>100	>100
3	11.7 ± 1.6	22.7 ± 2.8	>100	>100
4	22.5 ± 5.1	>50	>100	42.5 ± 5.1
5	46.9 ± 4.7	>50	>100	>100
Adriamycin^c	2.8 ± 0.4	5.6 ± 0.5	2.2 ± 0.1	1.8 ± 0.3

^aThe inhibitory effects are represented as giving 50% inhibition (IC₅₀) relative to the vehicle control. These data represent the average values of three repeated experiments (mean ± SD).

^bIn μg/mL

^cPositive control.

Figure 2. The increment of caspase-3 activity by compound 3 in HL-60 cells. After 12 h, 24 h, and 48 h incubation with the 3-treated HL-60 cells, the cell lysates were incubated at 37 °C with caspase-3 substrate (Ac-DEVD-AFC) for 1 h. The fluorescence intensity of the cell lysates was measured to determine the caspase-3 activity. The blank group was used as 0.1% DMSO-treated cells; camptothecin (7.8 µM) was used as a positive control. Data are presented as the mean ± SD of results from three independent experiments.

Figure 3. The induction of caspase-3 activation and PARP degradation by compound 3 in HL-60 cells. Western blot analysis of caspase-3 and PARP protein levels after exposure to compound 3. HL-60 cells were treated with compound 3 at the indicated concentrations. Protein (50 μg) from each sample was resolved by SDS-PAGE (10% (w/v) polyacrylamide gel).