Polyether antibiotic MI215-NF3 substance, production process the

Details Polyether antibiotic MI215-NF3 substance, production process the Polyether antibiotic MI215-NF3 substance, production process the

1991-07-01

1993-06-01

Ivy, C. Warren

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514191, 514460, 514459, 549211, 549343, A61K 31555, C07D30902

Patent

active

052159817

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

This invention relates to a novel antibiotic substance MI215-NF3 and salts thereof and also relates to a process for production of the MI215-NF3 substance or salts thereof. This invention further relates to agent for control of chicken coccidiosis, which contains the MI215-NF3 substance or a salt thereof as an active ingredient. Furthermore, the present invention also pertains to a new microorganism, Actinomadura sp. MI215-NF3 strain which has characteristic capable of producing MI215-NF3 substance.


PRIOR ART

Various antibiotics of polyether type are known to have antibacterial activities. Monensin (see Japanese Patent Publication No. 113/70) and salinomycin (see "The Journal of Antibiotics", 27, 814-821), which belong to the polyether antibiotics, are used as agents for control of chicken coccidiosis.
Coccidiosis provides a serious problem in the poultry farming. There has hence been a continued desire for the discovery or development of a new compound which can exhibit superior anticoccidial activity and properties to the compounds previously known or used to date. Investigations are now made to achieve this end.


DISCLOSURE OF THE INVENTION

With a view toward discovering useful novel antibiotics, we, the present inventors, have therefore proceeded with investigations. As a result, we have succeeded in isolating a new strain belonging to the genus Actinomadura. We have also found that this new strain can produce a novel polyether antibiotic. This antibiotic is now named MI215-NF3 substance. Further, it has also been uncovered that this MI215-NF3 substance and its salts (carboxylates) exhibit an activity to control chicken coccidiosis. The present inventors have proceeded with the investigation further, to determine the chemical structure of MI215-NF3 substance, whereby MI215-NF3 substance has been confirmed to be a novel compound. In addition, it has also been found that MI215-NF3 substance can be represented by the following formula (I): ##STR1## wherein R is a hydrogen atom.
Accordingly, this invention provides the substance which is obtained by culturing a microorganism belonging to the genus Actinomadura and which has been named as MI215-NF3 substance by the present inventors, as well as salts thereof. This invention also provides a process for production thereof, and their use as an agent for control of chicken coccidioses.
In a first aspect of the present invention, therefore, there are provided MI215-NF3 substance having the above formula (I) and a salt thereof.
Although MI215-NF3 substance of the formula (I) is in the form of a free carboxylic acid where R is a hydrogen atom in the formula (I), R in the formula (I)generally can be a metal or ammonium group. Therefore, the present invention also embraces salts of MI215-NF3 substance therein. These salts can be in the form of an alkali metal salt where R is an alkali metal atom in the formula (I), for example, sodium salt, potassium salt and lithium salt, or in the form of an alkaline earth metal salt where R is an alkaline earth metal atom in the formula (I), for example, calcium salt and magnesium salt. They can also be salts of other metals, for example, aluminum salt and iron salt. The ammonium salt can also be included.
Physicochemical properties of MI215-NF3 substance according to the present invention are as follows.
The physicochemical properties of the sodium salt of MI215-NF3 substance will be described hereinafter.
(1) Appearance
Colorless plate crystals.
(2) Elemental analysis


______________________________________ Found Calculated (for C.sub.37 H.sub.63 O.sub.11 Na) ______________________________________ C 62.47% 62.87% H 8.96% 8.98% O 24.60% 24.90% Na 3.53% 3.25% ______________________________________
(3) Mass spectrometry (SIMS)
m/z 707(M+Na)
(4) Melting point
217-218.degree. C.
(5) Specific optical rotation [a].sup.25.sub.D=+ 30.6.degree. (c1.0, chloroform)
(6) Infrared absorption specturm (KBr pellet method)
As be shown in FIG. 1 of the accompanying drawings.
(7) Proton nuclear magnetic resonan

REFERENCES:
patent: 4582822 (1986-04-01), Hamill et al.
patent: 4683201 (1987-07-01), Hamill et al.

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