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| Copolymers of flavanoid tannins and acrylic monomers |
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Chemotherapeutically active acetogenins
| Details |
Inventors: McLaughlin, Jerry L.; Hui, Yu-Hua;
Assignee: Purdue Research Foundation (West Lafayette, IN)
Primary Examiner: Raymond; Richard L.
Assistant Examiner: Russell; Mark W.
Attorney, Agent or Firm: Barnes & Thornburg
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. |
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DETAILED DESCRIPTION OF THE INVENTION The starting material for use in the invention is the bark of Annona bullata Rich.
(Annonaceae), and it is considered likely, by the screening of other parts of the plant, that other tissues such as twigs, wood, roots, seeds and leaves would also contain extractable quantities of the subject compounds.
The bark material is prepared for extraction by grinding in a conventional mill to a suitable particle size, usually in the range of about 0.
001-3 mm.
in diameter, and more preferably in the range of 0.
1-2 mm.
The ground material is extracted by percolating with 95% EtOH.
The ethanol solubles are concentrated to remove the bulk of the solvent, at least to the point of reducing the extract to a thick syrup.
The resultant concentrate is partitioned between water and a water-immiscible solvent, such as chloroform, in order to remove the water solubles which are freeze dried and labelled F002.
The chloroform solubles are recovered as a syrup residue using a solvent evaporator and labelled as F003.
The insoluble interface was dried at ambient temperature and labelled F004.
F003 then is partitioned between hexane and 90% aqueous MeOH in order to remove hexane solubles which are vacuum dried and labelled as F006.
The 90% aqueous MeOH solubles are recovered by vacuum evaporation to a thick syrup as a crude acetogenin-containing extract F005.
Separation and purification of pure acetogenins from the crude extract (F005) can be affected by the use of the proper combination of conventional techniques including, for example, column chromatography (CC), thin-layer chromatography (TLC), medium-pressure chromatography (MPC) and chromatotrons.
While not desiring to be limited thereto, the details of the separation procedure are illustrated by the following examples.
Fractionation of the ethanolic extract was guided by assay with the brine shrimp lethality test (BST) and confirmed by assays on tumor cell cultures.
Pesticidal tests were conducted at Eli Lilly Laboratories (Greenfield) in indicator organisms following standard procedures
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