Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1999-07-28
2000-10-31
Cook, Rebecca
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514429, 514546, 514547, 514557, 514574, A61K 3134, A61K 31215, A61K 3119
Patent
active
061403601
DESCRIPTION:
BRIEF SUMMARY
This is a 371 of PCT/JP97/01929 filed Jun. 6, 1997
TECHNICAL FIELD
This invention relates to an antifungal agent comprising as an active ingredient a derivative of cryptoporic acid isolated from a fruiting body of Basidiomycetes. The compound is useful as an antibacterial or antifungal agent or a starting material for manufacturing these agents. The present invention thus pertains to the field of pharmaceuticals or their production.
BACKGROUND ART
Antimicrobial drugs, and especially antibiotics, have developed remarkably. In contrast, antifungal drugs are lacking in variety and effectiveness. In particular, the opportunistic mycoses of internal organs caused by infections with Candida, Aspergillus, and Cryptococcus due to a decreased bodily defense capability resulting from extensive administration of carcinostatic agents, immunosuppressants, steroid hormones, and acquired immunodeficiency syndrome (AIDS) in recent years are posing significant medical problems. Therefore, there is a strong demand for developing drugs for mycoses.
Biologically active agents contained in mushrooms have been examined in various ways since early times. Ganoderma applanatum, and Coriolus versicolor have been conventionally used as oriental drugs and folk remedies effective for stomach, esophageal, mammary, and prostate cancers. In particular, .beta.-D-glucan-protein complex (PS-K) extracted from cultured mycelium from Corliolus versicolor has been used widely as an anticancer medicament. It was reported in Korea that Lee et al. (1981) and Kim et al. (1982) obtained from Cryptoporus volvatus a protein-polysaccharide with anticancer activity from water extract and ergosterol from chloroform-methanol extract (Asakawa et al., Trans. Mycol. Soc. Japan 29: 281-296, 1998). Asakawa et al. reported obtaining various derivatives of cryptoporic acid as bitter elements from the Cryptoporus volvatus and that Cryptoporic acid different from those mentioned above has been obtained from culture extracts (M. Hirotani et al., Phytochemistry 30(5), 1555-1559 (1991)). It has also been reported that cryptoporic acid derivatives can be obtained from cultured Ganoderma neojaponicum. Furthermore, other cryptoporic acid derivatives and compounds analogous to cryptoporic acid derivatives are reported to have been obtained from Haploporus odorus (Y. Morita et al., Biosci. Biotech. Biochem. 59(19): 2008-2009 (1995)).
Biological activities of cryptoporic acid reportedly include active oxygen inhibitory activity (Asakawa et al., Trans. Mycol. Soc. Japan 29: 281-296, 1988), inhibition of germination of rice (T. Hashimoto et al., Tetrahydron Lett. 28(50): 6303-6304 (1987)), and an inhibitory effect on chemical carcinogenesis (T. Narisawa et al., Jpn. J. Cancer Res. 83: 830-834 (1992)).
Cryptoporic acid derivatives described above with partially known properties form a group of compounds described by formula 4. ##STR1## wherein R.sup.4 represents a hydrogen atom or a hydroxyl group, and R.sup.1, R.sup.2, and R.sup.3 may be the same or different from each other and each represents a hydrogen atom, an alkyl group (particularly a lower alkyl group, more specifically a methyl group), and an alkali metal such as sodium or potassium.
DISCLOSURE OF THE INVENTION
An objective of the present invention is to provide compounds useful as an antibacterial or antifungal agent or as a starting material for manufacturing these agents, and an antifungal agent.
The present inventors isolated sesquiterpene compounds, more specifically various cryptoporic acid derivatives consisting of sesquiterpene with the drimane skeleton and isocitric acid, from extracts of a fruiting body of Cryptoporus volvatus, a mushroom of the Polyporaceae family, and found that the cryptoporic acid derivatives possessed antifungal activity. The present inventors further sought novel biologically active components contained in mushrooms. They also studied ardently to find compounds which had strong antifungal activities on the fungi mentioned above that cause opportunistic visceral mycosis and w
REFERENCES:
patent: 5840927 (1998-12-01), Nozoe et al.
Asakawa et al., "Cyptoporic Acids A-G, Drimane-Type Sesquiterpenoid Ethers of Isocitric Acid from the Fungus Cryptoporus Volvatus", Phytochem., vol. 31 No. 2, pp. 579-592, 1992.
Kanou Muneaki
Masuda Jun'ichi
Nozoe Shigeo
Segawa Toshiaki
Takahashi Akira
Cook Rebecca
Toa Gosei Co., Ltd.
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