Table 4.
Gossypol and their derivative’s activities against different types of in vivo cancer models.
| Compound Tested | Animal Tumor Models | Anticancer Effects | Mechanisms | Dose (Route) | Duration | References |
|---|---|---|---|---|---|---|
| Breast cancer | ||||||
| Apogossypolone | Athymic nude female mice xenografted with MCF-7 breast carcinoma cells | Inhibited tumor growth | ↑Apoptosis; ↑autophagy | 120 mg/kg/day (i.p.) | 4 weeks | [105] |
| Gastrointestinal and associated cancers | ||||||
| Combination of apogossypolone and adriamycin | BALB/c nu/nu mice xenografted with SMMC-7721 hepatocellular carcinoma cells | Inhibited tumor growth | ↑Apoptosis; ↑DNA fragmentation | 100 or 200 mg/kg/day (intragastric) ± 5.5 mg/kg/week adriamycin (i.v.) | 28 days | [58] |
| Head and neck cancers | ||||||
| Apogossypolone | Athymic nude (nu/nu) mice xenografted with CNE-1 or CNE-2 nasopharyngeal carcinoma cells | Inhibited tumor growth and angiogenesis; enhanced antitumor activity of cisplatin (CNE-2 cells only) | ↑Apoptosis; ↓CD31 | 200 mg/kg/day (intragastric) ± 3 mg/kg; every 2 days (i.p.)cisplatin | [62] | |
| Hematologic cancers | ||||||
| ApoG2 | Female ICR SCID mice xenografted with WSU-FSCCL B cell lymphoma cells | Inhibited tumor growth | ↑Caspase-3; ↑caspase-8; ↑caspase-9; ↑PARP; ↑AIF | 25 mg/kg/day (i.p. or i.v.) | 5 days | [70] |
| Prostate cancer | ||||||
| (−)-Gossypol | Male BALB/c nude mice xenografted with PC-3 prostate carcinoma cells | Inhibited tumor growth and angiogenesis | ↓VEGF | 15 mg/kg/day (intratumoral) | 50 days | [106] |
| (−)-Gossypol | Male BALB/c nude mice xenografted with PC-3 prostate carcinoma cells | Inhibited tumor growth | ↓Bcl-2; ↑caspase-3; ↑caspase-8; ↓CD31; ↓PCNA | 2.5–10 mg/kg/day (i.p.) | 7 days | [74] |
| AT-101(R-(–)-gossypol acetic acid | SCID mice xenografted with VCaP prostate carcinoma cells | Inhibited tumor growth | ↑Apoptosis; ↑Bcl-2; ↑androgen receptor expression | 15 mg/kg; 5 days/week (p.o.) | 6 weeks | [104] |
Symbols and abbreviations: ↑, increase or upregulation; ↓ decrease or downregulation; AIF, apoptosis inducing factor; ApoG2, apogossypolone; i.p., intraperitoneal; i.v, intravenous; PARP, poly (ADP-ribose) polymerase; PCNA, proliferating cell nuclear antigen; p.o., per os; VEGF, vascular endothelial growth factor.