Table 2.

Overview of the Anticancer Activity of N-AVAM Capsaicin Analogues

compound	type of cancer	IC50 (in cell culture)	effect on normal cells	experimental models used	phenotypic effects	mechanism of action	ref
5	small cell lung cancer	ND	ND	cell culture	inhibition of cell invasion	inhibition of AMPK pathway	73
5	breast cancer	MCF-7: 1.6 μM T47D: 0.75 μM	ND	cell culture	inhibition of cell proliferation	activation of TRPV1 and CB1 receptors	25, 26, 55
10	breast cancer	MCF-7: 0.4 μM EFM-19: 0.55 μM T47D: 0.35 μM	ND	cell culture	inhibition of cell viability	activation of TRPV1 and CB1 receptors	25, 26, 55
10	small cell lung cancer	DMS114: 15 μM	no effect on the viability of normal lung epithelial cells	cell culture	inhibition of cell viability	activation of calpain pathway	53
10	rat thyroid carcinoma	ND	ND	athymic mouse model	inhibition of tumor growth in athymic mice	activation of CB1 receptor	43
10	high grade astrocytoma	ND	ND	orthotopic scid mouse model	inhibition of tumor growth in scid mice	activation of TRPV1 receptor	61
10	melanoma	ND	ND	cell culture (melanoma cell line derived from a patient)	decrease in cell viability	ND	61
10	T-cell leukemia	ND	no apoptosis of normal T-lymphocytes	cell culture	induction of apoptosis	activation of FADD/Caspase-8 pathway	57
10	prostate cancer	TSU: ~100 nM PPC-1: ~1 μM	ND	cell culture	inhibition of cell viability	activation of CB1 receptors	57
10	epidermoid carcinoma	ND	ND	cell culture,	decrease in cell viability	ND	61
10	small cell lung cancer	ND	ND	cell culture	inhibition of cell invasion	inhibition of AMPK pathway	66
6	small cell lung cancer	DMS114: 43 μM	no effect on the viability of normal lung epithelial cells	cell culture	inhibition of cell viability	activation of calpain pathway	53
7	small cell lung cancer	DMS114: 15 μM	no effect on the viability of normal lung epithelial cells	cell culture	inhibition of cell viability	activation of calpain pathway	53
8	breast cancer	P388: 9 μg/mL J774:8 μg/mL WEHI: 3 μg/mL	normal bone marrow, IC50 = 40 μg/mL	cell culture	inhibition of cell proliferation	apoptosis via the caspase pathway	67
8	cervical cancer	HeLa: 62 μg/mL CaSki: 91 μg/mL ViBo: 149 μg/mL	no effect on the viability of normal human lymphocytes	cell culture	inhibition of cell proliferation	apoptosis via the caspase pathway	68
9	leukemia	P388: 49 μg/mL J774: 10 μg/mL WEHI: 31 μg/mL	normal bone marrow, IC50 = 73 μg/mL	cell culture	inhibition of cell proliferation	apoptosis via the caspase pathway	67
9	cervical cancer	HeLa: 57 μg/mL CaSki: 122 μg/mL ViBo: 74 μg/mL	PhAR decreased the viability of normal human lymphocytes. No selectivity for tumor cells was observed.	cell culture	inhibition of cell proliferation	apoptosis via the caspase pathway	68
11	cervical cancer	HeLa: ~50 μM Taxol-resistant HeLa: ~40 μM	ND	cell culture	inhibition of cell viability	ND	40, 70
11	histocytic leukemia	U937: ~25 μM	ND	cell culture	inhibition of cell viability	ND	40
11	melanoma	B16F10: ~10 μM	normal mouse fibroblast IC50 = 65 μM	cell culture	inhibition of cell viability	ND	40
11	breast cancer	MCF-7: ~25 μM	ND	cell culture	inhibition of cell viability	apoptosis via caspase pathway	69