Table 1.
Potency (IC50; µM) of pepper-derived compounds against several cancer cell lines 1.
| Compound | Cell Line and IC50 (µM) | References |
|---|---|---|
| Piperolactam A (1) | A549 (10.1); HCT15 (27.8); SK-MEL-2 (18.3); SK-OV-3 (18.3) | [85,86] |
| Piperolactam B (2) | A549 (21.7); HCT15 (21.3); SK-MEL-2 (11.6); SK-OV-3 (14.4); P-388 (46.1) | [85,86] |
| Piperolactam C (3) | A549 (>162.0); P-388 (78.0); HT-29 (69.0) | [85] |
| 4 | L1210 (1.6) | [87,88] |
| 5 | L1210 (2.6) | [87,88] |
| 6 | L1210 (2.3) | [87,88] |
| 7 | L1210 (1.6) | [87,88] |
| 8 | L1210 (1.8) | [87,88] |
| 9 | MCF-7 (2.0) | [89] |
| Piplartine or Piperlongumine (10) | 518A2 (2.6); A2780 (0.5); A549 (1.9); CEM (4.4); GBM10 (3.8); HCT116 (6.0); HCT8 (2.2); HL60 (5.3); HT1080 (3.4); HT-29 (1.4); JURKAT (5.3); K-562 (5.7); KB (5.6); MCF-7 (5.0); MOLT-4 (1.7); MRC-5 (35.0); SF188 (3.9); SKBR3 (4.0); T98G (4.9); WI38 (26.8); ZR-75-30 (5.9) | [88,90,91,92,93,94] |
| 11 | A549 (4.1); MCF-7 (4.2) | [88] |
| 12 | A549 (4.7); MCF-7 (4.9) | [88] |
| 13 | A549 (1.8); MCF-7 (1.6) | [88] |
| 14 | A549 (2.0); MCF-7 (1.8) | [88] |
| 15 | A549 (3.8); MCF-7 (5.0) | [88] |
| 16 | A549 (24.0); MDA-MB-231 (11.7) | [93] |
| 17 | A549 (18.0); MDA-MB-231 (23.7) | [93] |
| 18 | A549 (19.8); MDA-MB-231 (6.7) | [93] |
| 19 | A549 (3.9); MDA-MB-231 (6.1) | [93] |
| 20 | A549 (4.1); MDA-MB-231 (7.3) | [93] |
| 21 | A549 (4.8); MDA-MB-231 (2.7) | [93] |
| 22 | A549 (2.7); MDA-MB-231 (2.5) | [93] |
| 23 | A549 (2.2); MDA-MB-231 (2.1) | [93] |
| Pipermethystine 24 | HepG2 (not reported) | [95] |
| Piperlonguminine 25 | MCF-7 (6.0); MCF-12A (50.8); MDA-MB-231 (261.7); MDA-MB-468 (8.0); SW-620 (16.9) | [96] |
| Pellitorine 26 | HL60 (58.0); MCF-7 (8.0) | [97,98] |
| Sarmetine 27 | P-388 (ED50 = 13.0) | [99] |
| Piperine 28 | A549 (427.5); COLO-205 (46.0); HeLa (95.0); Hep-G2 (70.0); IMR-32 (89.0); MCF-7 (99.0) | [100,101,102] |
| Piperninaline 29 | L5178Y (17.0) | [103] |
| Dehydropiperninaline 30 | L5178Y (8.9) | [103] |
| Aduncamide 31 | KB (ED50 = 18.0) | [104,105] |
| 32 | Not active | [106] |
| 33 | Not active | [106] |
| 34 | Not active | [106] |
| Piperarborenine A 35 | A549 (4.23); HT-29 (6.21); P-388 (0.21) | [85] |
| Piperarborenine B 36 | A549 (1.39); HT-29 (2.41); P-388 (0.13) | [85] |
| Piperarborenine C 37 | A549 (0.23); HT-29 (0.26); P-388 (0.18) | [85] |
| Piperarborenine D 38 | A549 (0.28); HT-29 (0.35); P-388 (0.20) | [85] |
| Piperarborenine E 39 | A549 (0.19); HT-29 (0.22); P-388 (0.02) | [85] |
| Piperarboresine 40 | A549 (5.01); HT-29 (5.69); P-388 (4.87) | [85] |
| Piplartine-dimer A 41 | P-388 (8.48) | [85] |
| Chabamide 42 | A549 (67.3); CNE (67.0); COLO-205 (5.4); DU-145 (16.0); HeLa (24.0; 189.8); HepG2 (60.8); K-562 (10.8); MCF-7 (39.1); SGC-7901 (12.0) | [107,108] |
| Chabamide F 43 | COLO-205 (181.7); HeLa (119.4); HepG2 (44.6); HT-29 (259.7); MCF-7 (49.9) | [107] |
| Chabamide G 44 | COLO-205 (0.0369); HeLa (85.3); HepG2 (108.0); MCF-7 (51.4) | [107] |
| Chabamide H 45 | COLO-205 (69.5); HepG2 (253.5); MCF-7 (319.4) | [107] |
| Chabamide I 46 | COLO-205 (80.5); HeLa (263.4) | [107] |
| Chabamide J 47 | HT-29 (450.4) | [107] |
| Chabamide K 48 | COLO-205 (379.4); Hela (191.0); HepG2 (437.2); HT-29 (397.8) | [107] |
| cis-Yangonin 49 | A2780 (2.9); K652 (1.6) | [109] |
| trans-Yangonin 50 | A2780 (9.3); K652 (5.5) | [109] |
| Demethoxyyangonin 51 | A2780 (16.6); K652 (12.6) | [109] |
| Kavain 52 | A2780 (11.0); K652 (23.2) | [109] |
| Methysticin 53 | A375 (65.0); HaCaT (29.0) | [110] |
| 54 | A375 (65.0); HaCaT (29.0) | [110] |
| Flavokavain A 55 | MCF-7 (25.0); MDA-MB-231 (17.5) | [111,112] |
| Flavokavain B 56 | A2058 (18.3); ACC-2 (4.7); CaCo-2 (9.9); Cal-27 (26.7); DU-145 (3.9); H460 (18.2); HaCaT (13.6); HCT116 (7.5); HuH7 (15.9); HSC-3 (17.2); LAPC4 (32.0); LNCaP (48.3); MCF-7 (38.4); MCF-7/HER2 (13.6); MDA-MB-231 (12.3/45.0); NCI-H727 (11.3); PC-3 (6.2); RL (8.2); SKBR3/HER2 (10.0); SK-LMS-1 (4.4) | [112,113,114,115,116,117,118] |
| Flavokavain C 57 | A549 (40.3); CaSKi (39.9); CCD-18Co (160.9); EJ (8.3); HCT116 (12.7); HepG2 (60.0); HT-29 (39.0); L-02 (57.0); MCF-7 (47.6); RT-4 (1.5) | [119,120] |
| 58 | CaCo-2 (10.0); HaCaT (10.9); HCT116 (9.2); MCF-7 (10.5); NCI-H727 (11.0); PC-3 (9.6); RL (10.1) | [112] |
| 59 | CaCo-2 (11.2); HaCaT (10.4); HCT116 (7.7); HuH7 (15.0); MCF-7 (10.3); MDA-MB-231 (13.2); NCI-H727 (14.8); PC-3 (7.3); RL (9.0) | [112] |
| 60 | CaCo-2 (9.6); HaCaT (10.5); HCT116 (10.0); HuH7 (16.6); MCF-7 (15.9); NCI-H727 (9.9); PC-3 (8.7); RL (8.9) | [112] |
| 61 | CaCo-2 (9.2); HCT116 (12.4); MCF-7 (8.8); PC-3 (13.2); RL (5.4) | [112] |
| 62 | HCT116 (54.1); MCF-7 (7.3); | [121] |
| 63 | CaCo-2 (5.8); HaCaT (7.2); HCT116 (6.9); HuH7 (15.5); MCF-7 (9.4); MDA-MB-231 (12.9); NCI-H727 (11.4); PC-3 (5.1); RL (6.9) | [112] |
| 64 | CaCo-2 (3.9); HaCaT (5.3); HCT116 (4.3); HuH7 (8.9); MCF-7 (9.4); MDA-MB-231 (8.7); NCI-H727 (8.2); PC-3 (3.1); RL (5.9) | [112] |
| 65 | CaCo-2 (4.5); HaCaT (8.7); HCT116 (4.2); HuH7 (9.8); MCF-7 (8.9); MDA-MB-231 (13.0); NCI-H727 (4.0); PC-3 (8.1); RL (9.0) | [112] |
| 66 | CaCo-2 (8.8); HaCaT (7.7); HCT116 (6.8); HuH7 (14.1); MCF-7 (9.3); MDA-MB-231 (9.9); NCI-H727 (8.7); PC-3 (7.6); RL (8.3) | [112] |
| 67 | CaCo-2 (5.5); HaCaT (7.6); HCT116 (6.2); HuH7 (14.6); MCF-7 (7.7); MDA-MB-231 (10.7); NCI-H727 (5.5); PC-3 (5.5); RL (6.4) | [112] |
| 68 | CaCo-2 (5.7); HaCaT (7.6); HCT116 (5.4); HuH7 (12.7); MCF-7 (7.5); MDA-MB-231 (8.2); NCI-H727 (6.0); PC-3 (5.8); RL (6.5) | [112] |
| 69 | CaCo-2 (6.8); HaCaT (9.0); HCT116 (6.2); HuH7 (13.9); MCF-7 (9.5); MDA-MB-231 (11.1); NCI-H727 (11.3); PC-3 (7.1); RL (8.3) | [112] |
| 70 | CaCo-2 (2.6); HaCaT (2.8); HCT116 (2.7); HuH7 (4.9); MCF-7 (5.0); MDA-MB-231 (3.3); NCI-H727 (4.1); PC-3 (2.5); RL (3.4) | [112] |
| Grandisin 71 | EAT (0.2); HL60 (60.0); U937 (30.0); V79 (174.0) | [122,123] |
| 72 | A549 (6.90); SK-MEL-2 (4.50); SK-OV-3 (9.40) | [86] |
| 73 | 3T3-A31 (0.043) | [124] |
| Conocarpan 74 | A549 (11.2); HL60 (5.8); MCF-7 (7.8); SMMC-7721 (8.9); SW-480 (2.1) | [125] |
| Decurrenal 75 | MCF-7 (169.1) | [126] |
| Eupomatenoid-5 76 | 786-0 (TGI = 6.6); HT-29 (TGI = 48.5); K-562 (TGI = 338.5); MCF-7 (TGI = 21.2); NCI-H460 (TGI = 34.8); OVCAR-3 (TGI = 18.7); PC-3 (TGI = 21.0); UACC-62 (TGI = 27.9) | [127] |
| Capsaicin 77 | 3T3 (83.0); A375 (6.0); A2058 (200.0); AsPC1 (150.0); B16F10 (117.0); BxPC3 (150.0); HepG2 (50.0); MCF-7 (53.0); MCF-10A H-ras (56.0); MDA-MB-231 (21.7); PC-3 (20.0); RT-4 (80.0) | [128,129,130] |
| 78 | B16F10 (87.0); MCF-7 (32.0) | [128,129,130] |
| 79 | B16F10 (38.0); MCF-7 (28.0); MDA-MB-231 (87.0) | [131] |
| 80 | B16F10 (75.0); MDA-MB-231 (109.0) | [132] |
| 81 | B16F10 (50.0); MCF-7 (32.0); MDA-MB-231 (14.2) | [129] |
| 82 | B16F10 (120.0); MDA-MB-231 (75.0) | [132] |
| 83 | MCF-7 (142.4); MDA-MB-231 (104.6) | [133] |
| 84 | MCF-7 (144.6); MDA-MB-231 (173.2) | [133] |
| 85 | B16F10 (130.0); SK-MEL-28 (85.0) | [130] |
| 86 | A2058 (55.2); SK-MEL-25 (67.2); U-87 (86.9) | [134] |
| Capsanthin 87 | DU-145 (ND); PC-3 (ND) | [135,136] |
| Capsorubin 88 | A549 (< 20.0) | [135,136] |
| Ericifolin 89 | LNCaP (< 5.0) | [137] |
| Nilocitin 90 | HCT116 (19.4); HepG2 (22.8); MCF-7 (40.8) | [63] |
| Pedunculagin 91 | HCT116 (4.4); HepG2 (6.4); MCF-7 (18.4) | [63] |
| Castalagin 92 | HCT116 (7.4); HepG2 (9.8); MCF-7 (26.2) | [63] |
| Grandinin 93 | HCT116 (13.8); HepG2 (18.4); MCF-7 (22.1) | [63] |
1 IC50 = half of maximal inhibitory concentration; ED50 = median of effective dose; TGI = total growth inhibition; ND = not determined.