Table 1.

Growth Inhibitory Effects of Test Substances with Activity in the Hollow Fiber Model^a

	Compound	Cell Lines	In vitro ED50 µg/ml (µM or as indicated)b		Selected In Vivo Dosesc (mg/kg)	Growth Inhibition (%)		References
						ip	sc
1	Paclitaxel	KB	0.020	(0.023)	3.75, 7, 15, 30	70 – 85d	20 – 27e	Mi et al.24
		SW626	10 pg/ml	(12 pM)		98 – 100d	0 – 22e
2	Aculeatin A	MCF-7			6.25, 12.5, 25,50	10 – 58d	0e	Chin et al.34
3	Alvaradoin E	KB	0.10	(0.23)	0.195, 0.39,0.78, 1.56	40 – 58d	5 – 11e	Mi et al.29
		LNCaP	0.06	(0.14)		60 – 80d	10 – 19e
		Col2	0.10	(0.23)		31 – 74d	6 – 16e
4	Alvaradoin F	KB	0.10	(0.23)	0.195, 0.39, 0.78, 1.56	32 – 58d	2 – 18e	Mi et al.29
		LNCaP	0.05	(0.12)		59 – 72d	3 – 15e
		Col2	0.10	(0.23)		21 – 72d	1 – 10e
5	Alvaradoin G	KB	0.20	(0.39)	6.25, 12.5, 25	79 – 85d	13 – 60d	Phifer et al.90
		LNCaP	0.15	(0.29)		52 – 78d	24 – 58d
		Col2	0.96	(1.3)		84 – 86d	0 – 24e
6	Alvaradoin H	KB	0.15	(0.29)	0.78, 1.56, 3.125	43 – 58d	1 – 28e	Phifer et al.91
		LNCaP	0.15	(0.29)		47 – 67d	10 – 16e
7	3-Chlorodeoxylapachol	KB	3.2	(12)	6.25, 12.5, 25,50,100	0 – 65d	45 – 48d	Jones et al.92
8	Dioscin	Lu1	1.0	(1.2)	6.2, 12.5, 25	25 – 95d	0 – 2e	Mi et al.24
		LNCaP	1.5	(1.7)		37 – 72d	36 – 45e
		KB	18	(21)		79 – 100d	4 – 48e
9	13-Hydroxy-15-oxozoapatlin	KB	1.2	(3.6)	25, 50, 75, 100	0 – 69d	0e	Braca et al.93
		LNCaP	1.5	(4.5)		0 – 88d	0 – 2e
10	13-Methoxy-15-oxozoapatlin	SW626	0.20	(0.58)	25, 50, 100	0 – 92d	16 – 60d	Mi et al.24
		LNCaP	0.40	(1.2)		50 – 58d	0e
		Mel2	0.40	(1.2)		15 – 85d	11 – 60d
		KB	2.2	(6.4)		21 – 100d	6 – 45d
		MCF-7	0.30	(0.87)		34 – 89d	0 – 35e
11	Nitidulin	LNCaP	4.1	(9.7)	10, 20, 40	54 – 59d	0 – 18e	Chin et al.31
12	Picropolygamain	LNCaP	1.1	(3.1)	5, 10, 20	21 – 53d	3 – 34e	Rivero-Cruz et al.94
13	Silvestrol	LU1	0.79 ng/ml	(1.2 nM)	0.625, 1.25, 2.5, 5	12 – 63d	0 – 27e	Hwang et al.28
		LNCaP	0.98ng/ml	(1.5 nM)		15 – 83d	12 – 16e
		MCF-7	0.98 ng/ml	(1.5 nM)		20 – 77d	5 – 23e
14	Xanthochymolf	LNCaP	4.8	(8.0)	12.5, 25	44 – 60d	65 – 66d	Kim et al.95
15	Guttiferone Ef

^aAnimals were treated with PBS (control) or the indicated doses of test substance, once daily by intraperitoneal injection from day 3–6 after implantation. On day 7, mice were sacrificed, and fibers were retrieved and analyzed by MTT assay. Results are shown as the average percentage cell growth inhibition relative to control.

^bDoses are expressed as µg/ml or µM unless specified otherwise. All incubations with compound were 72 h in duration.

^cDoses were selected as described previously.²⁴

^dStatistical significance achieved with one or more dose levels.

^eStatistical significance not achieved with one or more dose levels.

^fThese compounds occurred in their plant of origin as an inseparable mixture, as reported by others.⁹⁶