Apoptolidin, originally isolated from a Nocardiopsis sp., induces apoptotic cell death in rat glial cells transformed with the adenovirus E1A oncogene (IC50 = 11 ng/ml). Apoptolidin is among the most selective cytotoxic agents tested by the NCI in human cancer cell lines.
Apoptolidin is soluble in ethanol, methanol, DMF and DMSO and has limited water solubility.
Apoptolidin is soluble in ethanol, methanol, DMF and DMSO and has limited water solubility.
| Mechanism of Action | The apoptotic activity of apoptolidin correlates with F0F1-ATPase inhibition; however, recent evidence suggests the existence of a secondary biological target or more complex mode of action. |
| References | Correlation of F0F1-ATPase inhibition and antiproliferative activity of apoptolidin analogues. Wender P.A. et al. Org. Lett. 2006, 8, 589. Apoptolidin: induction of apoptosis by a natural product. Daniel P.T. et al. Angew. Chem. Int. Ed. Engl. 2006, 45, 872. Understanding and exploiting the mechanistic basis for selectivity of polyketide inhibitors of F(0)F(1)-ATPase. Salomon A.R. et al. Proc. Natl Acad. Sci. USA 2000, 97, 14766. Apoptolidin, a new apoptosis inducer in transformed cells from Nocardiopsis sp. Kim J.W. et al. J. Antibiot. 1997, 50, 628. |