Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-02-08
1997-04-01
Owens, Amelia
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514462, 549330, 549341, 549354, A61K 31335
Patent
active
056166095
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP92/01017 filed Aug. 7, 1992.
TECHNICAL FIELD
The present invention relates to anticancer compounds and a preparation process thereof, and more specifically to novel anticancer compounds contained in Rui-xiang-lang-du, that is, a Chinese herbal and crude drug, and a preparation process thereof.
BACKGROUND ART
Chinese herbal and crude drugs can be stated as the fruit of long-established wisdom of human beings. Confirming the existence of strong carcinostatic activities in Rui-xiang-lang-du (Stellera chamaejasme. L, Euphorbia fischeriana Steud., E. ebiacteola Hayata) in the course of a study on carcinostatic Chinese herbal and crude drugs, the essences of whose carcinostatic activities have not yet been identified, the present inventors filed a patent application on a process for the collection of its carcinostatic substance (Japanese Patent Application No. 58126/1990). The application, however, did not deal to such an extent as efficiently isolating a compound having carcinostatic activities and confirming its effectiveness against solid cancer.
DISCLOSURE OF THE INVENTION
The present inventors have proceeded with further research on a carcinostatically active component contained in the carcinostatic substance of Rui-xiang-lang-du, resulting in successful isolation of a component contributing to the carcinostatic activities of Rui-xiang-lang-du. In addition, the component has also been found to contain a novel compound represented by the formula described below.
Namely, a first object of the present invention is to provide stelleramacrin A and stelleramacrin B represented by the following formulas (I) and (II), respectively: ##STR2##
A second object of the present invention is to provide a process for the preparation of stelleramacrin A or stelleramacrin B from Rui-xiang-lang-du.
Another object of the present invention is to provide an anticancer agent containing stelleramacrin A or stelleramacrin B.
A further object of the present invention is to provide a therapeutic for solid cancer, said therapeutic containing gnidimacrin or pimelea factor P.sub.2 as an active ingredient.
BRIEF DESCRIPTION OF THE DRAWINGS
FIG. 1 is a proton NMR spectrum of stelleramacrin A according to the present invention.
FIG. 2 is a proton NMR spectrum of stelleramacrin
BEST MODES FOR CARRYING OUT THE INVENTION
Stelleramacrin A and stelleramacrin B (which may hereinafter be collectively called "stelleramacrin") according to the present invention, which are represented by the formulas (I) and (II), respectively, can each be obtained by extracting an aerial or subterranean part (rootstock) of Rui-xiang-lang-du with an organic solvent and then purifying the extract.
Described specifically, an aerial or subterranean part of Rui-xiang-lang-du, for example, is extracted with a lower alcohol such as methanol, ethanol or propanol and the extract is then extracted with a water-insoluble organic solvent such as petroleum ether to obtain a crude extract. In the next place, the crude extract is purified by chromatography on a silica gel column while using hexane-ethyl acetate or the like as an eluent, chromatography on an ODS column while using methanol-water, or a like method, whereby some active fractions are obtained. The active fractions are subjected to high-performance liquid chromatography and preparative thin-layer chromatography for further purification, whereby stelleramacrin represented by the formula (I) or (II) can be isolated as a compound having carcinostatic activities.
Although anticancer compounds other than stelleramacrin, for example, gnidimacrin [J. Nat. Prod. 1985, 48(3), 440-445], pemelea factor P.sub.2 (Abstracts of Lectures addressed at Natural Organic Compounds Forum, 27, 734-741), subtoxin A (Abstracts of Lectures addressed at Natural Organic Compounds Forum, 27, 734-741), huratoxin (Abstracts of Lectures addressed at Natural Organic Compounds Forum, 27, 734-741) and simplexin [Aust. Vet. J., 51(6), 325-326] are also contained, stelleramacrin is obtained in fractions di
REFERENCES:
Feng, W. "Studies on antitumor active compounds of stellera chamaejaisme L. and their mechanism of action" CA 117:184357 (1992).
Feng, W. et al "Studies on antitumor chinese medicines, (II) Antitumor constituents of stellera charmaejasime L." CA 116:207421 (1991).
Ikekawa Nobuo
Ikekawa Tetsuro
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