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Home Weight Loss and Supplements Novel-anti-leukemic-diterpenoid-triepoxides

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 Novel anti-leukemic diterpenoid triepoxides

Details
Inventors: Kupchan, S. Morris; Court, William A.;
Assignee: Research Corporation (New York, NY)
Primary Examiner: Trousof; Natalie
Assistant Examiner: Jaisle; C. M. S.
Attorney, Agent or Firm: Behr & Woodbridge

There are provided novel diterpenoid triepoxides, derived from Tripterygium wilfordii Hook F. which possess high and surprising antileukemic activity at dosage levels of micrograms/kilogram body weight.

DETAILED DESCRIPTION We claim: 1.
A compound selected from the group having the formula: ##STR3## R is hydrogen or hydroxy.
2.
A compound of claim 1 wherein R is hydrogen.
3.
A compound of claim 1 wherein R is hydroxy.
4.
##STR4##



Description:
SUMMARY OF THE INVENTION Ethanolic extracts of Tripterygium wilfordii are subjected to a series of extraction, chromatographic and purification steps to yield the diterpenoid triepoxides triptolide and tripdiolide which possess high anti-leukemic activity.
The general formula of the compounds is shown below.
##STR1## It will be seen that tripdiolide (1) differs from triptolide (2) in the presence of a beta hydroxy group at the 2 position.
Triptonide (3) is also isolated.
In the process of isolation the root of Tripterygium wilfordii Hook are ground up and extracted with 95% ethanol and subjected to a series of extractions and column fractionations shown and outlined in FIG.
I and discussed in greater detail hereinbelow.
The active materials isolated were tested for anti-tumor activity in vitro against a standard animal tumor systems recognized in the testing arts.
The compounds disclosed and claimed herein demonstrate the significant anti-leukemic activity in the microgram/kilogram level, the level at which toxicity is not a significant consideration.
FIG.
1 showing the extraction step s is as follows: ##STR2## DESCRIPTION OF THE PREFERRED EMBODIMENTS In the process of the present invention dried ground roots of T.
wilfordii Hook are extracted with several batches of a lower alkanol, suitably ethanol, most preferably 95% ethanol.
The extracts combined and the solvent removed, suitably by evaporation, to yield a residue which is then partitioned between a lower alkyl lower alkanoate, suitably ethyl acetate, and water.
The aqueous layer is repeatedly washed with the ester solvent combined with the ester layer and the solvent removed, suitably by evaporation to yield a second residue.
The residue from the ester extraction is then subjected to column chromatography on silica gel, suitably on a silicAR type gel



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