Table 7.

Antitumor activities of components from Agrimonia pilosa Ledeb.

A. pilosa extract	Experimental model	Test dose range	Contrast	Route of administration	Pharmacological action	Mechanism of action	References
Quercetin	AGS cells	6.25, 12.5, 25, 50, and 100 μM	SN-38 (6.25, 12.5, 25, 50, and 100 μM)	NS	Sensitize AGS to SN-38	NS	[55]
Quercetin	AGS inoculate BALB/c nude mice	20 mg/kg, three times a week + IRI; 10 mg/kg, once a week	IRI; 10 mg/kg, once a week 20 mg/kg, three times a week	i.p.	Sensitize AGS to SN-38	NS	[55]
Agrimonolide	AGS cells	5, 10, 20, and 40 μM	Negative control	NS	Apoptosis-inducing	Bcl-2/Bax↑, p-p38↑ and caspase-3 protease activation	[56]
Beta-carotene	AGS cells	0, 20, 50, and 100 μmol/L	Negative control	NS	Apoptosis-inducing and DNA fragmentation	Bcl-2/Bax↑,p-53↑	[1]
Agrimol B	PC-3 cells	0, 6.25, 12.5, and 25 μmol/L	Negative control	NS	Arrest cancer cells at G0 phase	p27↑, SKP2↓，cMYC↓	[57]
Agrimol B	A549 cells	0, 6.25, 12.5, and 25 μmol/L	Negative control	NS	Arrest cancer cells at G0 phase	SKP2↓, cMYC↓, SPT16↓ and SSRP1↓, p27↑	[57]
Ellagic acid	PC-3 cells	0, 6.25, 12.5, and 25 μmol/L	Negative control	NS	Arrest cancer cells at G0 phase	c-MYC↓, SKP2↓, SPT16↓, SSRP1↓, p27↑	[57]
Ellagic acid	A549 cells	0, 6.25, 12.5, and 25 μmol/L	Negative control	NS	Arrest cancer cells at G0 phase	c-MYC↓, SKP2↓, SPT16↓, SSRP1↓, CRM1↓, p27↑	[57]
Agrimol B	PC-3 inoculated male BALB/c nude mice	10 mg/kg	Negative control	p.o.	Tumor growth reducing	NS	[57]
Apigenin	PC-3 cells	20, 40 μM	Negative control	NS	Apoptosis inducing	HDACs↓, especially HDAC1↓ and HDAC3↓	[58]
Apigenin	PC-3 xenografts in athymic nude mice	20 and 50 μg/mouse/day	Negative control	p.o.	Tumor growth reducing	HDACs↓ p21/waf1↑, Bax/bcl2↑	[58]
Quercetin	MCF-7 cells	0–100 μg/ml, IC50 = 0.87 μg/mL	Negative control	NS	Cytotoxicity	May be related to the presence of 2,3-double bond in ring C, carbonyl group at C-4 and ortho-hydroxylation in ring B	[59]
Agrimophol	K562 cells	0.1, 1, 10 mg/ml	Vincristine (50 IU/ml)	NS	Apoptosis inducing	NS	[60]
Agripinol A	HCT-116, MDA-MB-231 and PC-3 cells	(IC50 = 12.34 ± 0.93, 5.44 ± 0.35, 9.47 ± 0.70, 14.29 ± 1.24 μg/ml, respectively)	Fluorouracil	NS	Cytotoxicity	NS	[45]
Agripinol B	HCT-116, MDA-MB-231 and PC-3 cells	(IC50 = 12.34 ± 0.93, 5.44 ± 0.35, 9.47 ± 0.70, 14.29 ± 1.24 μg/ml, respectively)	Fluorouracil	NS	Cytotoxicity	NS	[45]
Agripinol C	HCT-116, MDA-MB-231 and PC-3 cells	(IC50 = 12.63 ± 1.40, 2.12 ± 0.16, 7.50 ± 0.86, 9.85 ± 1.08 μg/ml, respectively)	Fluorouracil	NS	Cytotoxicity	NS	[45]
Agrimoniin	MM2 inoculated C3H/H e and BALB/ c mice	1, 3, 10, 30 mg/kg	Negative control	i.p.	Prolonged the life span of mice bearing MM2	Direct inhibit tumor cell activity and increased the number of peripheral white blood cells and the ratio of monocytes	[61]
Quercetin and hyperoside in combination (1 : 1 ratio)	786-O renal cancer cells	3.8–60 μg/ml	Negative control	NS	Cancer cell proliferation inhibition	ZBTB10↑ Sp1, Sp3, and Sp4 mRNA↓	[62]