US4209507A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Novel anti-tumor substance and preparation thereof
Assignee: Sumitomo Chemical Co Ltd
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Filing: 1978-07-05
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Granted: 1980-06-24
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Expires: 1998-07-05
Abstract
Abstract Antitumor substances are prepared by culturing a microorganism, Acinetobacter calcoaceticus. The antitumor substances have potent antitumor activity as well as immunostimulatory activity and are effective in a very small amount without harmful effects such as toxicity.
Inventors
- 👤 Shigeo Ogino
- 👤 Noboru Yoshida
- 👤 Takao Kiyohara
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 09:20
CPC Classifications
C; C12; C12P; C12P21/00; C12P21/005; A; A61; A61K; A61K35/00; A61K35/66; A61K35/74; A61P; A61P31/00; A61P35/00; A61P37/00; A61P37/02; A61P37/04; C12N; C12N1/00; C12N1/20; C12N1/205; C12P1/00; C12P1/04; C12R; C12R2001/00; C12R2001/01; Y; Y10; Y10S; Y10S435/00; Y10S435/8215; Y10S435/822
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
160 words
A substance showing antitumor activity against the ascites form of Sarcoma 18 and Ehrlich carcinoma of mouse which is prepared by culturing the microorganism; Acinetobacter calcoaceticus var. microformis SC-1714 (ATCC-31299; FERM-P-4064) in a suitable medium and isolating the substance having the following properties: Physical and chemical properties 1. Appearance and solubility: obtained as white powders or films, soluble in water but insoluble in organic solvents. 2. Decomposition point: higher than 235° C. 3. Ultra-Violet absorption spectrum: as shown in FIG. 1 (for the product of Example 5), with strong absorption at around 260 nm 4. Infrared absorption spectrum (KBr tablet): as shown in FIG. 2 (for the product of Example 5), with specific absorptions at 3600, 1650, 1550 and 1100-1000 cm -1 5. Elemental analysis: C 33.7-38.9%; H 5.2-6.9%; N 2.3-3.0% 6. Color reactions: slightly positive to ninhydrin reaction , xanthoprotein reaction and biuret reaction; positive to Molisch reaction, anthrone-sulfuric acid reaction, phenol-sulfuric acid reaction and carbazole sulfuric acid reaction.
Claim 2
Dependent Claim
160 words
A substance showing antitumor activity against the ascites form of Sarcoma 18 and Ehrlich carcinoma of mouse which is prepared by culturing the microorganism; Acinetobacter calcoaceticus var. microformis SC-1714 (ATCC-31299; FERM-P-4064) in a suitable medium and isolating the substance having the following properties: Physical and chemical properties 1. Appearance and solubility: obtained as white powders or films, soluble in water but insoluble in organic solvents. 2. Decomposition point: higher than 235° C. 3. Ultra-Violet absorption spectrum: as shown in FIG. 1 (for the product of Example 5), with strong absorption at around 260 nm 4. Infrared absorption spectrum (KBr tablet): as shown in FIG. 2 (for the product of Example 5), with specific absorptions at 3600, 1650, 1550 and 1100-1000 cm -1 5. Elemental analysis: C 33.7-38.9%; H 5.2-6.9%; N 2.3-3.0% 6. Color reactions: slightly positive to ninhydrin reaction , xanthoprotein reaction and biuret reaction; positive to Molisch reaction, anthrone-sulfuric acid reaction, phenol-sulfuric acid reaction and carbazole sulfuric acid reaction.
Claim 3
Dependent Claim
129 words
Color reaction of hydrolyzed products: ninhydrin reaction intensified (after hydrolysis in 1 N HCl, at 105° C. for 24 hours); negative to phloroglucin reaction (after hydrolysis in 1 N H 2 SO 4 at 100° C. for 4 hours) 8. Stability: Stable at pH 5 to 8 at 0° to 60° C. Biological properties 1. Biological activity: having no antimicrobial activity, having antitumor activity against ascites form of Sarcoma 180 and Ehrlich carcimona of mouse, immunostimulating activity, anti-vaccinia virus activity, anti-inflammatory activity and activity for inhibiting secretion of acid in the stomach. 2. Acute toxicity: acute toxicity for mouse (ICR type, male, 20 to 25 g) by one dosage is as follows: LD 0 1 g or more/kg (oral administration) LD 100 300 mg/kg (intraperitoneal and and intravenous injection).
Claim 4
Dependent Claim
129 words
Color reaction of hydrolyzed products: ninhydrin reaction intensified (after hydrolysis in 1 N HCl, at 105° C. for 24 hours); negative to phloroglucin reaction (after hydrolysis in 1 N H 2 SO 4 at 100° C. for 4 hours) 8. Stability: Stable at pH 5 to 8 at 0° to 60° C. Biological properties 1. Biological activity: having no antimicrobial activity, having antitumor activity against ascites form of Sarcoma 180 and Ehrlich carcimona of mouse, immunostimulating activity, anti-vaccinia virus activity, anti-inflammatory activity and activity for inhibiting secretion of acid in the stomach. 2. Acute toxicity: acute toxicity for mouse (ICR type, male, 20 to 25 g) by one dosage is as follows: LD 0 1 g or more/kg (oral administration) LD 100 300 mg/kg (intraperitoneal and and intravenous injection).
Claim 5
Dependent Claim
42 words
An antitumor substance according to claim 1 wherein the microorganism is cultured in a culture medium containing a carbon source and a nitrogen source at a pH value of about 6.0 to 7.5 at a temperature of from 25° to 35° C.
Claim 6
Dependent Claim
92 words
An antitumor substance according to claims 1 having antitumor activity as well as immunostimulatory activity, which is prepared by culturing Acinetobacter calcoaceticus var. microformis SC-1714 (ATCC-31299: FERM-P-4064) in a culture medium containing a carbon source and a nitrogen source at a pH value of about 6.0 to 7.5 at a temperature of from 25° to 35° C., adding to the resulted culture broth a hydrophilic organic solvent, a salt or an acid to precipitate the substance having antitumor activity as well as immunostimulatory activity, collecting the precipitates and, if desired purifying them.
Claim 7
Dependent Claim
36 words
An antitumor composition containing the substance of claim 1 which is prepared by culturing Acinetobacter calcoaceticus var. microformis SC-1714 (ATCC-31299: FERM-P-4064) in a fluid culture medium and removing the microbial cells from the resulted culture broth.
Claim 8
Dependent Claim
52 words
A culture broth containing the substance of claim 1 which is prepared by culturing Acinetobacter calcoaceticus var. microformis SC-1714 (ATCC-31299: FERM-P-4064) in a fluid culture medium containing a carbon source and a nitrogen source at a pH value of about 6.0 to 7.5 at a temperature of from 25° to 35° C.
Claim 9
Dependent Claim
37 words
A process for producing the antitumor substance of claim 1 which comprises culturing a microorganism Acinetobacter calcoaceticus in a suitable medium, isolating the substance having antitumor activity from the resulted culture broth and, if desired, purifying it.
Claim 10
Dependent Claim
65 words
A process according to claim 6, wherein the microorganism is cultured in a culture medium containing a carbon source and a nitrogen source at a pH value of about 6.5 to 7.5 at a temperature of about 25° to 35° C. and, to the resulted culture broth, a hydrophilic organic solvent, a salt or an acid is added to precipitate the substance having antitumor activity.
Claim 11
Dependent Claim
14 words
A pharmaceutical composition comprising antitumor substance of claim 1 and a pharmaceutically acceptable carrier.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-06-24 | 1983-12-24 | 1984-06-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-06-24 | 1987-12-24 | 1988-06-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-06-24 | 1991-12-24 | 1992-06-24 | $7700.00 | Window Closed / Lapsed |