Uses
Pironetin is an α/β unsaturated lactone isolated from Streptomyces species. Pironetin binds to α-tubulin and is a potent inhibitor of microtubule polymerization, and has cell cycle arrest and antitumor activity[1][2].
Definition
ChEBI: Pironetin is an aliphatic alcohol.
in vivo
Pironetin (0.78-6.25 mg/kg; intraperitoneal injection; daily; for 5 days; female CDF1-SLC mice) treatment shows a moderate antitumor effect, however, a severe weight loss is observed as a side effect[1].
| Animal Model: | Female CDF1-SLC mice (10 weeks) injected with P388 murine leukemia cells[1] |
| Dosage: | 0.78 mg/kg, 1.56 mg/kg, 3.13 mg/kg, 6.25 mg/kg |
| Administration: | Intraperitoneal injection; daily; for 5 days |
| Result: | Showed a moderate antitumor effect.
|
References
[1] Kondoh M, et al. Cell cycle arrest and antitumor activity of pironetin and its derivatives. Cancer Lett. 1998 Apr 10;126(1):29-32. DOI:
10.1016/s0304-3835(97)00528-4[2] Yang J, et al. Pironetin reacts covalently with cysteine-316 of α-tubulin to destabilize microtubule. ] Nat Commun. 2016 Jun 30;7:12103. DOI:
10.1038/ncomms12103
