Table 2.
Antitumor activity in vivo of acetogenins and selected extracts rich in acetogenins.
| Acetogenin | Animal model | Antitumor activity | Reference |
|---|---|---|---|
| (3) Annonacin | Xenotrasplant MCF-7 tumor cells in nu/nu mice | Tumor growth-inhibitory effect Inhibition of the expression of the proteins ERα, cyclin D1 and Bcl-2 | Ko et al., 2011 |
| (5) Bullatacin | Xenotrasplant S180 and HepS mice tumor cells in nu/nu mice | Tumor growth-inhibition 65.8% (S180) and 63.4% (HepS) cancer cells. Antitumor activity related to an to the adjacent bis-THF and three hydroxy groups | Chen et al., 2012a |
| (6) Laherradurin | Xenotrasplant HeLa and SW480 tumor cells in nu/nu mice, 7.5 mg/kg/day | Tumor growth-inhibition 64% (HeLa) and 60% (SW480) cancer cells. Antitumor activity related to the adjacent bis THF with β-hydroxy γ-methyl γ-lactone | Schlie-Guzmán et al., 2009 |
| (7) Cherimolin-2 | Xenotrasplant HeLa tumor cells in nu/nu mice, 25 mg/kg/day Xenotrasplant SW-480 Tumor cells in nu/nu mice 5 mg/kg/day |
Tumor growth-inhibition 43% (Hela) cancer cells No significant tumor inhibition in SW-480 xenograft. Antitumor activity related to the non-adjacent bis THF γ-lactone | Schlie-Guzmán et al., 2009 |
| EEAML | AOM-induced colorectal cancer in male rats | Reduction of the colonic aberrant crypt foci (ACF) in vivo. Down-regulation of PCNA and Bcl-2 proteins, and up-regulation of Bax in colon. Activity attributed to annomuricin E due to its apoptosis effect by activating the expression of caspase 3, 7 and 9, and upregulation of Bax and downregulation of Bcl-2 | Moghadamtousi et al., 2015b |
|
Annona muricata L. (graviola capsules Raintree) |
Orthotopic tumor xenografts of pancreatic tumor cells (CD18/HPAF) in nu/nu mice Dosis: 50 mg/kg and 100 mg/kg, aqueous extract | Tumor growth-inhibition of 5.8% treated with 50 mg/kg and 50.3% treated with 100 mg/kg of graviola extract The extract reduced pancreatic cells viability through increment of intracellular ROS and necrosis cell death, and cell cycle arrest Diminished MMP3 levels in tumors reducing metastasis and invasion |
Torres et al., 2012 |
AOM, azoxymethane; CD18/HPAF, pancreatic cancer cells; EEAML, ethyl acetate extract of A. muricata leaves; HepS, mouse hepatitis virus; S180, murine sarcoma cells; SW480 (colon adenocarcinoma); ROS, reactive oxygen species; MMP3, matrix metallopeptidase 3.