Antitumor efficacy of lidamycin on hepatoma and active moiety of its molecule

Table 1 Inhibition of proliferation by LDM, MMC, ADM and the LDM constituents LDC and LDP in hepatoma cells (mean±SD)

Drugs	IC50 (nmol/L)
	BEL-7402	SMMC-7721
LDM	0.003 ± 0.0006	0.064 ± 0.013
MMC	152.0 ± 27.3	1 136.6 ± 72.2
ADM	51.7 ± 6.5	378.0 ± 39.6
LDC	0.0032 ± 0.0005	0.0597 ± 0.0064
LDP	2 896.0 ± 345.5	1 896.0 ± 354.0

LDM: lidamycin; LDC: LDM enediyne chromophore; LDP: LDM apoprotein; ADM: adriamycin, MMC: mitomycin C.

Table 2 Inhibition of the growth of mouse hepatoma 22 by LDM and MMC

Experiment Groups		Dose(mg/kg)	Ivtimes	Number of mice		Body weight (g)		Tumorweight (g)	Inhibitionrate (%)	P
				Begin	End	Begin	End
I	Control		1	10	10	19.6	35	4.19 ± 1.36	---	---
	LDM	0.1	1	10	10	20.2	26.5	0.64 ± 0.17	84.7	< 0.01
		0.05	1	10	10	19.6	27.5	1.19 ± 0.50	71.6	< 0.01
		0.025	1	10	10	19.9	30.3	1.60 ± 0.61	61.8	< 0.01
		0.0125	1	10	10	19.5	30.7	1.65 ± 0.50	60.6	< 0.01
		0.00625	1	10	10	19.9	31.5	2.48 ± 0.78	40.8	< 0.01
	MMC	5	1	10	10	19.8	32.3	1.72 ± 0.40	58.9	< 0.01
		2.5	1	10	10	19.9	31.5	2.10 ± 0.84	49.9	< 0.01
		1.25	1	10	10	20	33.4	2.34 ± 0.83	44.2	< 0.01
II	Control		2	10	10	20.2	35.2	3.83 ± 1.22	---	---
	LDM	0.1	2	10	10	20.2	23.5	0.43 ± 0.16	88.8	< 0.01
		0.05	2	10	10	19.7	26.6	0.67 ± 0.20	82.5	< 0.01
		0.025	2	10	10	20.1	29.6	0.96 ± 0.30	74.9	< 0.01
		0.0125	2	10	10	20.3	32.8	1.55 ± 0.63	59.5	< 0.01
		0.00625	2	10	10	20	31.9	1.98 ± 0.77	48.3	< 0.01
	MMC	5	2	10	9	19.6	23.9	1.01 ± 0.29	73.6	< 0.01
		2.5	2	10	10	20.2	30.2	1.76 ± 0.76	54	< 0.01
		1.25	2	10	10	20.3	33.8	1.83 ± 0.48	52.2	< 0.01
III	Control		2	10	10	19.2	28.9	3.33 ± 1.04	---	---
	LDM	0.1	2	10	10	19.7	20.2	0.35 ± 0.06	89.5	< 0.01
		0.05	2	10	10	19.8	25.2	0.63 ± 0.23	81.1	< 0.01
		0.025	2	10	10	19.2	23.7	0.96 ± 0.45	71.2	< 0.01
		0.0125	2	10	10	19.4	27.8	1.59 ± 0.72	52.3	< 0.01
		0.00625	2	10	10	19.6	26.6	2.22 ± 0.81	33.3	< 0.05
	MMC	5	2	10	10	19.8	25.1	1.08 ± 0.59	67.6	< 0.01
		2.5	2	10	10	19.6	25.1	1.45 ± 0.88	56.5	< 0.01
		1.25	2	10	10	19.6	28.1	2.28 ± 0.96	31.5	< 0.05

Table 3 Inhibition of the growth of human hepatoma BEL-7402 xenografts by LDM and MMC in athymic mice

Groups	Dose(mg/kg)	Number of mice(begin/end)	BWC (g)	Tumor volume(mm3)	Inhibitionrate (%)
Control		6/6	-0.1	624.7 ± 360.1	-
LDM	0.05	6/6	+0.3	195.6 ± 94.1	68.7a
	0.025	6/6	-0.1	454.9 ± 302.3	27.2
MMC	1.25	6/6	-1.5	409.1 ± 225.9	34.5

^aP<0.05 vs control.