Chemotherapeutically active acetogenins
US5229419A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Sep 29, 1992 |
| Grant date | Jul 20, 1993 |
| Priority date | — |
| Expiry date | Sep 29, 2012 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D307/58
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Screening of crude extracts of the bark of Annona bullata Rich. (Annonaceae) showed cytotoxic and pesticidal activities. By monitoring with brine shrimp lethality, two novel extremely potent acetogenins, bullatacin (1) and bullatacinone (2), were isolated. Spectral and chemical methods identified bullatacin as a diastereomer of asimicin. Bullatacinone represents bullatacin with the lactone cleaved and reformed at the 4-OH. Unlike asimicin, which is more generally cytotoxic, 1 and 2 show some selective cytotoxicities in human tumor cell lines, and certain susceptible cells give ED.sub.50 values as low as 10.sup.-12 -10.sup.-15 mcg/ml. Bullatacin was pesticidal at concentration as low as 1 ppm, while bullatacinone lacked pesticidal activities.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.