Table 3.
Gossypol and their derivative’s activities against different types of cancer cell lines in vitro.
| Compound Tested | Cell Lines Used | IC50 (μM) (Duration) | References |
|---|---|---|---|
| Adrenal cancer | |||
| Gossypol | SW-13, H295r (human adrenocortical carcinoma) | 1.3–2.9 | [46] |
| Apogossypol hexaacetate | H295r, SW-13 (human adrenocortical carcinoma) | 5.2–6.8 | [46] |
| Bladder cancer | |||
| Gossypol | UM-UC2 and UM-UC-9 (human bladder carcinoma) | 0–20 | [47] |
| Breast cancer | |||
| Gossypol | MDA-MD-231 (human breast carcinoma) | 14.37 | [11] |
| Gossypol | MCF-7, MDA-MD-231 (human breast carcinoma) | 3.99–4.64 (72 h) |
[7] |
| Gossypol | MCF-7, MCF-6/ADR, MDA-MD-231 (human breast carcinoma) | None reported | [48] |
| Gossypol | MCF-7 (human breast carcinoma) | None reported | [49] |
| ApoG2 | MCF-7 (human breast carcinoma) | None reported | [39] |
| Gossypolone | MCF-7, MCF-6/ADR, MDA-MD-231 (human breast carcinoma) | None reported | [43] |
| Gossypolone | MCF-7/ADR, MCF-7/WT (human breast carcinoma) | 0.28–0.36 | [50] |
| 6-Aminopenicillanic acid sodium gossypolone | MCF-7, MDA-MB435 (human breast carcinoma) | 29.06–40 | [51] |
| 6-Aminopenicillanic acid sodium gossypolone | 4T1 (mouse mammary carcinoma) | 28.25 | [51] |
| Gossypol-enriched cottonseed oil | MDA-MD-231, MDA-MD-468 (human breast carcinoma) | 21.85–26.39 | [52] |
| Ethylimine of (±)-gossypol | MCF-7/ADR, MCF-7/WT (human breast carcinoma) | 0.40–0.45 | [50] |
| Ethylimine of (±)- gossypolone |
MCF-7/ADR, MCF-7/WT (human breast carcinoma) | 0.29–0.35 | [50] |
| Methylimine of (±)-gossypolone | MCF-7/ADR, MCF-7/WT (human breast carcinoma) | 0.14–0.37 | [50] |
| Gastrointestinal and associated cancers | |||
| Gossypol | HCT116 (human colorectal carcinoma) | 8.8 | [53] |
| Gossypol | COLO 225 (human colon carcinoma) | 0.1–100 | [8] |
| Gossypol | HT-29 (human colorectal carcinoma) | 10 | [54] |
| 6-Aminopenicillanic acid sodium gossypolone | HCT116, SW620 (human colorectal carcinoma) | 6.56–17.35 | [51] |
| 6-Aminopenicillanic acid sodium gossypolone | CT26 (mouse colon carcinoma) | 6.59 | [51] |
| Gossypol | M85 (human gastric carcinoma) | 18.4–39.7 | [55] |
| ApoG2 | MKN28, MKN45, AGS (human gastric carcinoma) | 5.6–11.37 (72 h) |
[56] |
| ApoG2 | SGC-7901 (human gastric carcinoma) | 18.7 | [57] |
| ApoG2 | SMMC-7721 (human hepatocellular carcinoma) | 17.29–30.63 | [58] |
| ApoG2 | HepG2, Hep3B (human hepatocellular carcinoma) | None reported | [42] |
| Gynecologic cancers | |||
| Gossypol | SKOV-3 (human ovarian carcinoma) | 5.7 | [46] |
| Gossypol | KB (human cervical carcinoma) | 5.7 | [59] |
| Gossypol | RL95-2 (human endometrial carcinoma) | 3.4 | [46] |
| Gossypol | HeLa (human cervical carcinoma) | 17.8–31.3 | [55] |
| Apogossypol hexaacetate | Skov-3 (human ovarian carcinoma) | 9.0 | [46] |
| Apogossypol hexaacetate | RL95-2 (human endometrial carcinoma) | 7.3 | [46] |
| Gossypolone | KB (human cervical carcinoma) | 0.45 | [50] |
| Gossypolone | KB (human cervical carcinoma) | 2.4 | [59] |
| Ethylimine of (±)-gossypol | KB (human cervical carcinoma) | 1.00 | [50] |
| Ethylimine of (±)- gossypolone |
KB (human cervical carcinoma) | 0.55 | [50] |
| Methylimine of (±)-gossypolone | KB (human cervical carcinoma) | 0.50 | [50] |
| Head and neck cancers | |||
| Gossypol | Um-SCC-1, Um-SCC-17b, UM-SCC-5PT, UM-SCC-10BPT (human HNSCC) | 3–15 | [60] |
| Gossypol | UM-SCC-12, UM-SCC-23, UM-SCC-1, UM-SCC-6, UM-SCC-14A, UM-SCC-74B, UM-SCC-81B, UM-SCC-22A, UM-SCC-17B, UM-SCC-25 (human HNSCC) |
3.75–6.85 | [61] |
| ApoG2 | C666-1, CNE-1, CNE-2, HONE-1 (human nasopharyngeal carcinoma) | 0.908–66.01 | [62] |
| ApoG2 | CNE-2, HONE-1 (human nasopharyngeal carcinoma) | None reported | [63] |
| Hematologic cancers | |||
| Gossypol | HL60 (human acute myeloid leukemia) | 2.0–8.1 (24–48 h) |
[64] |
| Gossypol | Vector/Jurkat, Bcl-2/Jurkat, Bcl-xL/Jurkat (human T cell leukemia) |
4.3–26.6 | [65] |
| Gossypol | U266, ARK, MM1, H929, OC1-MY5, OPM2, ARP-1, KMS11, CAG (human multiple myeloma) | < 6 | [66] |
| Gossypol | Namalwa (human Burkitt lymphoma) | None reported | [67] |
| Gossypol | Namalwa (human Burkitt lymphoma) | None reported | [68] |
| Gossypol | KAS-6/1, MM1.S, OPM-1, OPM-2, U266 (human multiple myeloma) | 2.5–7.5 | [69] |
| ApoG2 | WSU-FSCCL (human B cell lymphoma) | 0.109 | [70] |
| Lung cancer | |||
| Gossypol | H1975 (human lung adenocarcinoma) | 10.05–11.73 | [71] |
| Gossypol | H1975 (human lung adenocarcinoma) | 34.17–36.35 | [72] |
| 6-Aminopenicillanic acid sodium gossypolone | A549 (human lung adenocarcinoma) | 8.77 | [51] |
| BI-97C1 | H460 (human large cell lung carcinoma) | 0.33–0.51 | [73] |
| Neural cancers | |||
| Gossypol | U87 (human malignant glioma) | 30.2–59.6 | [55] |
| Prostate cancer | |||
| Gossypol | PC-3 (human prostate carcinoma) | 9.096 | [11] |
| Gossypol | PC-3 (human prostate carcinoma) | 4.74 | [74] |
| Gossypol | PC-3, LNCaP (human prostate carcinoma) | 2.8–3.5 | [75] |
| Gossypol | MAT-lylu (rat prostate carcinoma) | 14.5 | [76] |
| Gossypol | MAT-lylu (rat prostate carcinoma) | None reported | [77] |
| Gossypol | PC-3 (human prostate carcinoma) | None reported | [78] |
| Gossypol | DU-145 (human prostate carcinoma) | None reported | [79] |
| Gossypol | PC-3 (human prostate carcinoma) | 10 (24–72 h) |
[80] |
| Gossypol | PC-3 (human prostate carcinoma) | None reported | [81] |
| ApoG2 | PC-3, LNCaP (human prostate carcinoma) | None reported | [82] |
| BI-97C1 | PC-3 (human prostate carcinoma) | 0.11–0.15 | [73] |
| 6-Aminopenicillanic acid sodium gossypolone | PC-3 (human prostate carcinoma) | 29.46 | [51] |
| Skin cancer | |||
| 6-Aminopenicillanic acid sodium gossypolone | B16-F10 (mouse melanoma) | 11.05 | [51] |
| Thyroid cancer | |||
| Apogossypol hexaacetate | TT (human thyroid carcinoma) | 18.9 | [46] |