Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2000-08-03
2002-11-26
Owens, Amelia (Department: 1651)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C549S285000
Reexamination Certificate
active
06486197
ABSTRACT:
FIELD OF THE INVENTION
This invention relates to novel FT-0554 substance useful for treatment for infection of parasite, especially helminth, and its production.
PRIOR ARTS
Parasitosis is reducing as a result of improvement in sanitary conditions and progress of anthelmintics. Recently, however, the import parasitosis, zoonotic parasitosis, opportunistic parasitosis and parasitosis originated from perishable foods are prevailing and become crucial problems. Further the parasitosis produces large economical burdens in the stock-farming and agriculture. For infection of helminth in the parasite, at present, avermectins, mebendazole, praziquantel, and others are used for treatment of helminth.
PROBLEMS TO BE SOLVED BY THE INVENTION
Anthelmintics used at present, such as avermectins, mebendazole and praziqbantel, are not always sufficient for satisfactory in usefulness and toxicity, and the anthelmintics, which can solve these problems, are strongly, required.
Consequently, the present invention provides novel FT-0554 substance, which can satisfy the above requirements, and its production.
MEANS FOR SOLVING THE PROBLEMS
We have studided NADH-fumarate reductase, which was one of the promising targets against anthelmintics, in the electron transport system of the helminth, and explored for screening in the microbial culture. We have found that novel FT-0554 substance had NADH-fumarate reductase inhibitory activity, and completed the present invention according to this acknowledge.
An object of the present invention is to provide FT-0554 substance shown by the compound of the formula [I]
Another object of the present invention is to provide a process for production of FT-0554 substance of formula [I]
which comprises culturing a microorganism belonging to fungus having FT-0554 substance producing activity, accumulating FT-0554 substance in the cultured medium and isolating FT-0554 substance from the cultured medium.
Further object of the present invention is to provide a microorganism belonging to fungi and having FT-0554 substance producing activity of the above process being
Aspergillus niger
FT-0554. Still further object of the present invention is to provide a microorganism belonging to fungi and having FT-0554 substance producing activity being
Aspergillus niger
FT-0554.
FT-0554 substance producing microorganism is the fungi having FT-0554 substance producing activity and is not limited. Preferable example of a microorganism used for production of FT-0554 is a fungus strain FT-0554 isolated from a newly collected sponge by the inventors of the present invention.
Taxonomical properties of the microorganism are illustrated as follows.
Taxonomical properties of a strain FT-0554.
(1) Cultured Properties on Various Media
Results of macroscopic observation of the strain of the present microorganism cultured at 25° C. for 7 days are shown in Table 1.
TABLE 1
Growth condition
Color of
Color of
on the medium
surface of
reverse side
soluble
Medium
(diameter of colony)
colony
of colony
pigment
Czapek-yeast extract agar
good (82 mm)
black brown
pale yellow
none
velvety, entire
Malt extract agar medium
good (81 mm)
black brown
pale yellow
none
velvety, entire
20% sucrose Czapek-yeast extract agar medium
good (82 mm)
black brown
pale yellow
none
velvety, entire
Potate-glucose agar medium
good (>85 mm)
black brown
pale yellow
none
velvety, entire
Miura agar medium
moderate (40 mm)
black brown
white
none
velvety, entire
(2) Morphological Properties
The microorganism of the present invention shows good growth on Czapek-yeast extract agar medium which contains seawater 50% (salt content 3.4%), malt extract agar medium, Czapek-yeast extract agar medium which contains sucrose 20% and potato-glucose agar medium, with abundance of conidia.
Microscopical observation of colonies grown on Czapek-yeast extract agar medium shows transparent hyphae with septa, straight grown conidiophore on the substrate mycelia with length 500 &mgr;m-2.5 mm, and foot-cell in the basement. Tops of conidiophores are hypertrophic from spherical to subspherical with forming vesicles of diameter 35-60 &mgr;m.
Plural aspergillae consist of metulae and phialides with the size of 8.4-11.4×2.4-3.4 &mgr;m and 5.4-8.6×2.8-3.3 &mgr;m, respectively. Whole of the vesicles is covered with metulae with forming conidial heads segmented from spherical to cylindrical. Conidia is globose with a size of diameter 3-4.5 &mgr;m having smooth to rough surface.
(3) Physiological Properties
1) Optimum Growth Condition
Optimum growth condition of the present strain is pH 5-7, temperature 16-36°C. and seawater concentration
1)
50-100%.
1)
: salt concentration 3.4% natural seawater is used
2) Growth Condition
Growth range of the strain is pH 3-10, temperature 12-45° C. and seawater concentration
2)
0-100%.
1
: salt concentration 3.4% natural seawater is used
3) Nature
Aerobic
As shown in the above, culture condition, taxonomical properties and physiological properties of the present microorganism strain FT-0554 are compared with the known microorganism strains. The present strain is identified as belonging to Aspergillus niger and referred to
Aspergillus niger
FT-0554.
The present microorganism strain has deposited as
Aspergillus niger
FT-0554 FERM P-16399 in National Institute of Bioscience and Human-Technology, Agency of Industrial Science and Technology, Ministry of International Science and Technology, 1-3, Higashi 1—chome, Tsukuba-shi, Ibaraki-ken, Japan on Sep. 1, 1997. Further, the present microorganism strain was transferred to the microorganism deposition under Budapest Treaty in National Institute of Bioscience and Human-Technology, Agency of Industrial Science and Technology, Ministry of International Science and Technology, 1-3, Higashi 1-chome, Tsukuba-shi, Ibaraki-ken, Japan on Jul. 31, 1998, and was given deposition No. FERM BP-6443 from the International Deposition Authority.
Production of FT-0554 substance of the present invention can be performed by culturing microorganism belonging to fungi having producing activity of FT-0554 substance and isolating from the cultured mass and purifying the product. The microorganism strain used in the present invention can be the above microorganism strain, its variants and mutants, and all strains having FT-0554 substance producing activity belonging to fungi.
Nutritional sources for production of the above FT-0554 substance can be a nutritional source for fungi. Examples of nitrogen sources are commercially available peptone, meat extract, corn steep liquor, cottonseed powder, peanut powder, soybean flour, yeast extract, NZ-amine, casein hydrolyzate, sodium nitrate, ammonium nitrate and ammonium sulfate. Example of carbon sources are carbohydrate such as glycerin, starch, glucose, galactose and mannose, or carbon source such as fats and oil, and inorganic salts such as sodium chloride, phosphate, calcium carbonate and magnesium sulfate. These can be used with or combination thereof.
Trace metallic salt and animal, vegetable or mineral oil as anti-form agent can be added if necessary. These are substance, which can be assimilated by the producing strain and are useful for production of FT-0554 substance, can be used. All the known medium for culturing the fungus can be used. Mass production of FT-0554 substance can preferably be performed by a liquid culture. Culturing temperature can be applied within the range of growing the producing microorganism strain and producing FT-0554 substance. Culturing can be performed by selecting suitable conditions depending on the nature of FT-0554 substance producing strain.
FT-0554 substance can be extracted by water immiscible organic solvent such as chloroform and ethyl acetate from the culture liquid. In addition to the above extraction method, known isolation method used for lipophilic substance, for example adsorption chromatography, gel filtration chromatography, scratching from thin layer chromatography, centrifugal counter current chromatography, HPLC, and the like with or without combination thereof or r
Iwai Yuzuru
Masuma Rokuro
Omura Satoshi
Shiomi Kazuro
Owens Amelia
The Kitasato Institute
Young & Thompson
LandOfFree
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