Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1992-02-06
1994-06-21
Ivy, C. Warren
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
549343, A61K 3135
Patent
active
053228545
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a novel antibiotic, a method for preparing the same, and an antitumor agent and an antifungal agent comprising the antibiotic as an effective ingredient.
BACKGROUND ART
The main cause of the abnormal growth of cancer cells is the dysfunction of the signal transduction system for cell growth factors. For example, various types of tumor cells have been found to secrete tumor growth factor alpha (TGF-.alpha.) which enhances the autoproliferation of the tumor cells. An agent which can selectively inhibit the action of TGF-.alpha. can thus be expected to be useful as an anticancer agent.
Erbstatin and other agents of this sort are known. However, they are not sufficiently potent and, moreover, are not clinically useful because they lose their effects in blood.
Accordingly, an object of the present invention is to provide a novel substance which inhibits the action of tumor growth factors and inhibits the growth of tumor cells. Another object of the present invention is to provide an antitumor agent comprising the substance.
The inventors of the present invention screened various inhibitors using Epidermal growth factor (EGF), a cell growth factor similar to TGF-.alpha.. As a result, the inventors found that a novel substance, Reveromycin A, has potent inhibitory activity against EGF and inhibits the growth of various kinds of tumor cells. The present invention was achieved on the basis of this findings.
Furthermore, the inventors also found that Reveromycin A has antimicrobial activity against fungi and that a pharmaceutical composition comprising this substance is useful as an antifungal agent for achieving the present invention.
DISCLOSURE OF THE INVENTION
The present invention provides a novel antibiotic Reveromycin A, and a process for preparing the antibiotic Reveromycin A which comprises the steps of cultivating a strain which belongs to Streptomyces and produces the antibiotic Reveromycin A, and separating the antibiotic Reveromycin A from the cultured product. The Reveromycin A of the present invention has antitumor and antifungal activity. In accordance with other of its features, the present invention provides an antitumor agent comprising the antibiotic Reveromycin A as an effective ingredient, and an antifungal agent comprising the antibiotic Reveromycin A as an effective ingredient.
BRIEF DESCRIPTION OF DRAWINGS
FIG. 1 shows the ultraviolet absorption spectra of the antibiotic Reveromycin A of the present invention, in which--represents the spectrum measured in 100% methanol; --represents the spectrum measured in methanol/0.01N HCl; and .multidot. represents the spectrum measured in methanol/0.01N NaOH.
FIG. 2 shows the infrared absorption spectrum (KBr) of the antibiotic Reveromycin A.
FIG. 3 shows the 500 MHz .sup.1 H NMR spectrum (CD.sub.3 OD) of the antibiotic Reveromycin A.
FIG. 4 shows the 500 MHz .sup.13 C NMR spectrum (CD.sub.3 OD) of the antibiotic Reveromycin A.
BEST MODE FOR CARRYING OUT THE INVENTION
The antibiotic Reveromycin A of the present invention is a novel antibiotic represented by the following formula: ##STR2## which has the physicochemical properties described below.
Physicochemical properties of the antibiotic Reveromycin A: .multidot.1/2 H.sub.2 O); methanol); nm (.epsilon.)=238(25,300) and 260(sh, 12,200); 1380, 1250, 1160, and 970 cm.sup.-1 ; methanol and insoluble in aqueous acidic solution; negative in ninhydrine and Dragenforff's reagent.
The antibiotic Reveromycin A was isolated from the culture product obtained by cultivating Streptomyces sp. SN-593 which was isolated from soil collected in Kurafuchi Village, Gumma Prefecture, Japan. This strain Streptomyces sp. SN-593 has been deposited at the Fermentation Research Institute, Agency of Industrial Science and Technology (1-1-3, Higashi Tsukuba, Ibaraki 305, Japan) under the access number FERM P-11503 which was amended to the access number BP-3406 under the Budapest Treaty on May 20, 1991.
Streptomyces sp. SN-593 exhibits the following bacteriological chara
REFERENCES:
J. H. Antibiotics, vol. 44, No. 2 pp. 259-261 Feb. 1991 H. Osada et al "Reveromycin A, A new antibiotic which inhibits the mitogenic activity of epidermal growth factor".
Isono Kiyoshi
Kawanishi Gosei
Osada Hiroyuki
Takahashi Hidetoshi
Ivy C. Warren
Owens A.
Rikagaku Kenkyusho
Snow Brand Milk Products Co. Ltd.
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