The isolation of three new mono-tetrahydrofuran ring acetogenins from the bark of Annona squamosa is described. Each of these compounds bears a carbonyl group at the C-9 position and two hydroxyls that flank the tetrahydrofuran ring. These compounds exibit selective cytotoxic activity against certain specific human tumor cells.

Purdue Research Foundation

Selectively cytotoxic acetogenin compounds

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.

annona bullata/neoplasms

Selectively cytotoxic acetogenin compounds

Chemotherapeutically active acetogenins

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