Drug – bio-affecting and body treating compositions – Fermentate of unknown chemical structure
Patent
1997-05-12
1999-12-28
Marx, Irene
Drug, bio-affecting and body treating compositions
Fermentate of unknown chemical structure
435 41, 435117, 435118, 435119, A61K 3500
Patent
active
06007812&
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to MK7634 substance having anthelmintic activity, process for production thereof and use thereof as an anthelmintic containing it.
RELATED ART
Illnesses called parasitic diseases generally caused by parasites living on hosts and give serious damages to human and animal health and agriculture.
In order to treat or prevent such parasitic diseases, various drugs have hitherto been searched for. For example, as anthelmintically active substances derived from microorganisms, destomycin, hygromycin, avermectin and the like have been reported. However, number of such substances is very small. Accordingly, appearance of novel anthelmintically active substance is always demanded.
The present inventors provide a novel compound having anthelmintic activity, establish advantageous process for producing it and provide an anthelmintic containing the compound, thereby satisfying the above demand.
DESCRIPTION OF THE INVENTION
To satisfy the above demand, the present inventors continued a search of a substance having anthelmintic activity and found that a substance having anthelmintic activity is produced in a culture of a strain belonging to imperfect fungi. The present inventors isolated the active ingredient and determined physicochemical properties thereof and thus completed the present invention.
Therefore, the present invention relates to a substance exhibiting the following physicochemical properties (referred to as MK7634 substance hereinafter), a process for producing it and a drug, in particular an anthelmintic, containing the MK7634 substance as an active ingredient. absorption) 1630, 1405, 1350, 1090, 970 ethylacetate mixed solvent of n-butanol, ethanol, chloroform and 17% ammonia (weight mixing ratio=4:5:2:5).
BRIEF DESCRIPTION OF THE DRAWINGS
FIG. 1 shows UV spectrum of the MK7634 substance in an aqueous solution .
FIG. 2 shows IR spectrum of the MK7634 substance by the KBr method.
FIG. 3 shows .sup.1 H-NMR spectrum (400 MHz) of monodansylated MK7634 substance in a mixed solution of deuterium oxide and deuterated methanol (mixing weight ratio=4:1).
FIG. 4 shows .sup.13 C-NMR spectrum (100 MHz) of monodansylated MK7634 substance in a mixed solution of deuterium oxide and deuterated methanol (mixing weight ratio=4:1).
BEST MODE FOR CARRYING OUT THE INVENTION
The present invention will be explained in detail hereinafter.
The MK7634 substance of the present invention can be obtained by, for example, culturing a microorganism belonging to imperfect fungi and capable of producing the MK7634 substance and collecting the MK7634 substance from its culture. As such a microorganism, though it is not limited to specific ones so long as it has the property mentioned above, a fungus producing the substance and belonging to the genus Curvularia is preferably mentioned. More specifically, Curvularla pallescens D2479 (sometimes referred to simply "the strain" or abbreviated as "D2479" hereinafter), which has been isolated by the present inventors from dead plant bodies, can be mentioned as a preferred fungus producing the substance.
Mycological characteristics of the strain are as follows. This strain was deposited at the Agency of Industrial Science and Technology, the National Institute of Bioscience and Human-technology (NIBH, Postal code: 305, 1-1-3 Higashi, Tsukuba-shi, Ibaraki-ken, Japan) on Nov. 17, 1994 and received an accession number of FERM P-14645, and transferred to international deposition under the Budapest Treaty on Oct. 30, 1995 and received an accession number of FERM BP-5276.
(1) Morphological Characteristics
As to colony formation, the strain actively forms cotton pile-like colonies in culture at 27.degree. C. for 2 weeks on a potato dextrose agar culture medium [PDA: a culture medium containing 4.0 g of potato extract powder, 20.0 g of glucose and 15.0 g of agar (NISSUI Pharmaceutical) in 1 liter of water (pH 6.0.+-.0.1), NISSUI Pharmaceutical Co., Ltd., Product Summary I, p92], and the colonies present light brown gray color earlier and dark brow
REFERENCES:
Moore-Landecker, E., "Fundamentals of the Fungi", 1982, Prentice Hall, pp. 257-268.
The Merck Index, 1996, pp. 1509-1510.
Betina, V. "Bioactive Secondary Metabolites of Microorganisms", 1995, Elsevier, pp. 172-173.
Laskin et al., "Handbook of Microbiology", vol. 5, CRC Press, 1977, p. 724.
The Merck Index, 1966, # 8991.
Chiba Noriko
Harimaya Kenzo
Kanda Mina
Kumazawa Shigenori
Okada Tadaaki
Marx Irene
Mitsubishi Chemical Corporation
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