Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1997-10-22
1999-07-06
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
514171, 514172, 514182, 536 6, A61K 3158, C07J 1700
Patent
active
059197706
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
This invention relates to the metabolites of ginseng saponins by human intestinal bacteria and its preparation for an anticancer and more particularly, to a novel saponin of a metabolite of Panax ginseng saponin by human bacteria and a novel preparation of anticancer agent containing a novel saponin of a metabolite of Panax ginseng saponin by human bacteria, which exhibits immunopotentiating actions including inhibitory actions on the vascularization of tumors and extravasation of cancer cells.
DESCRIPTION OF THE RELATED ART
In recent years much of the development of novel anticancer agents has widely focused on natural sources and synthetic compounds.
Among saponins extracted from Panax ginseng, for example, ginsenoside to inhibit the proliferation of liver cancer cells (reference: Japanese Patent No. 89-28759).
Further, both ginsenoside Rg.sub.3 rotopanaxadiol! and ginsenoside Rb.sub.2 naxadio 1! were reported to inhibit the vascularization of tumors and extravasation of cancer cells including inhibitory actions on the et al.: Biol. Pharm. Bull., 17. 635(1994)!.
In case of 20-0-.beta.-D-glucopyranosyl!-20(S)-protopanaxadiol, called as (1.fwdarw.6)-.beta.-D-glucopyranosyl!-20(S)-protopanaxadiol, called as "compound Y", which were isolated from soil strains of Panax ginseng saponin and intestinal flora of rats, their structure was already 2418(1972), Takino et al.: Medicinal ginseng '69 (Public Publishing Co., Ltd. 267(1989)!.
Also, the structure of 20(S)-protopanaxatriol, isolated by sapogenin of Panax ginseng saponin, was already established (Nagai et al.: Tetrahedron, 27, 881(1971)!.
The pharmacological actions of these compounds, for example, inhibition of glucose transplant related to cancer cells by the blockage of membrane Med., 60, 197(1994)!, including the report on methicillin-resistant bacteria and the inhibition of the excretion of drugs on the 260(1996), Hasegawa et al., Planta Med., 61, 409(1995)!.
In case of the conventional chemotherapeutics which exhibit their therapeutic effects by attacking the cancer cells directly, their adverse effects are quite severe. During several decades, any antineoplastic agents with new mode of mechanism have not yet to be on the market. Further, in the event that Panax ginseng saponins are applied for the treatment of some diseases, these substances are reported to be metabolized by intestinal bacteria and said bacteria is liable to be influenced by human's constitution and his food pattern. Thus, any individual differences in the metabolism of sanponins may lead to the individual differences in his treatment.
SUMMARY OF THE INVENTION
In view of these situations, the inventors of this invention have investigated the metabolism of ginseng saponin associated by human intestinal bacteria and succeeded in isolating and identifying the following compounds, i.e., a) protopanaxadiol saponins(ginsenoside Rb.sub.1, ginsenoside Rb.sub.2 and ginsenoside Rc), b) compound K, arabinofuranosyl(1.fwdarw.6)-.beta.-D-glucopyranosyl-20(S)-protopanaxadiol !, which are called as ginsenoside Mc. metabolites of ginsenoside Rd, and c) 20(S)-protopanaxatriol, a metabolite of ginsenoside Rg.sub.1 and ginsenoside Re which belongs to protopanaxatriol saponin.
The inventor ascertains that these intestinal flora metabolites are absorbed from intestinal tracts to blood and excreted via urine and feces. By assuring that said intestinal flora metabolites prove to be main substances of Panax ginseng saponin, the inventor has endeavored to develop the therapeutic dosage form containing the active ingredient of saponin, which is not influenced by the difference of intestinal bacteria. As a result of reviewing these physiological activities, the inventor has discovered a novel preparation of anticancer agent, which exhibits immunopotentiating actions including inhibitory actions on the vascularization of tumors and extravasation of cancer cells. Thus, this invention has finally completed.
Therefore, the object of this invention is to provide a new compound of -proto
REFERENCES:
Biol. Pharm. Bull., 17(5), pp. 635-639 (1994).
Chem. Pharm. Bull., 20(11), pp. 2418-2421 (1972).
Tetrahedron, 27, pp. 881-892 (1971).
Planta Med., 60, pp. 240-243 (1994).
Planta Med., 61, pp. 409-413 (1995).
Phytotherapy Res., 9, pp. 260-263 (1995).
Chemical abstracts, vol. 124, (Columbus, Ohio, USA), abstact No. 283952, J.H.Sung et al, "Metalbolism of Ginseng Saponins by Human Intestinal Bacteria", & Saengyak Hakhoechi, 1995, 26(4), 360-7.
Hideo Hasegawa
Huh Jae Doo
Masamori Uchiyama
Satoshi Matsumiya
Sung Jong Hwan
Happy World Inc.
Il Hwa Co., Ltd.
Raymond Richard L.
LandOfFree
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