Antibiotic called "chloropolysporin", a process for its preparation, and its therapeutic and veterinary use
First Claim
Patent Images
1. An antibiotic substance named chloropolysporin and characterized by the following properties:
- (a) it takes the form of an amphoteric white powder, soluble in water;
(b) specific rotation;
[α
]25 -94.4°
(C═
0.09, 50%v/v aqueous methanol, sodium D-line);
(c) elemental analysis;
C, 49.88%;
H, 5.44%;
N, 5.65%;
Cl, 5.20%;
(d) on acid hydrolysis it yields;
neutral saccharides;
glucose, mannose and rhamnose;
amino acids;
monochloro-monohydroxy-phenylglycine;
(e) ultraviolet absorption spectrum;
as illustrated in FIG. 1 of the accompanying drawings, having absorption maxima λ
max at 280 nm (E1cm =45) in a 0.01N solution of hydrochloric acid and at 300 nm (E1cm =54.2) in a 0.01N aqueous solution of sodium hydroxide, the absorbences, E, being measured at a concentration of 1% w/v;
(f) infrared absorption spectrum;
the infrared absorption spectrum (ν
cm-1) measured on a KBr disc is as shown in FIG. 2 of the accompanying drawings;
(g) nuclear magnetic resonance spectrum;
the nuclear magnetic resonance spectrum (δ
ppm), measured at 400 MHz in a mixture of deuterium oxide and deuterohydrochloric acid of pH value about 3.0, using sodium 2,2-dimethyl-2-silapentane-5-sulfonate as the internal standard, is as illustrated in FIG. 3 of the accompanying drawings;
(h) solubility;
soluble in water and methanol, sparingly soluble in acetone, and insoluble in ethyl acetate, chloroform and benzene;
(i) color reactions;
positive in Ninhydrin and Rydon-Smith reactions;
(j) thin layer chromatography;
Rf value=0.65, using a cellulose sheet (Eastman) as adsorbent and a 15;
10;
3;
12 by volume mixture of butanol, pyridine, acetic acid and water as the developing solvent;
(k) high voltage paper electrophoresis;
using Toyo'"'"'s filter paper No. 51A in a 0.1M tris-hydrochloric acid buffer solution of pH 7.5 (3300 volt/60 cm, 1 hour);
the migration distance (detected by bioautography with Bacillus subtilis PCI
219) from the origin to the cathode was 4 cm.
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Abstract
A novel compound, called chloropolysporin, has antibiotic properties and would appear to be a member of the class of glycopeptide antibiotics containing chlorine. It may be produced by cultivating a suitable strain of microorganism of the genus Micropolyspora, especially Micropolyspora sp. SANK 60983 (FERM BP-538). It may be combined with conventional pharmaceutically acceptable carriers or diluents for therapeutic use or incorporated into edible excipients, such as feed or water, for use as a growth-promoting agent, especially for farm animals.
-
Citations
7 Claims
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1. An antibiotic substance named chloropolysporin and characterized by the following properties:
-
(a) it takes the form of an amphoteric white powder, soluble in water; (b) specific rotation;
[α
]25 -94.4°
(C═
0.09, 50%v/v aqueous methanol, sodium D-line);(c) elemental analysis; C, 49.88%;
H, 5.44%;
N, 5.65%;
Cl, 5.20%;(d) on acid hydrolysis it yields; neutral saccharides;
glucose, mannose and rhamnose;
amino acids;
monochloro-monohydroxy-phenylglycine;(e) ultraviolet absorption spectrum; as illustrated in FIG. 1 of the accompanying drawings, having absorption maxima λ
max at 280 nm (E1cm =45) in a 0.01N solution of hydrochloric acid and at 300 nm (E1cm =54.2) in a 0.01N aqueous solution of sodium hydroxide, the absorbences, E, being measured at a concentration of 1% w/v;(f) infrared absorption spectrum; the infrared absorption spectrum (ν
cm-1) measured on a KBr disc is as shown in FIG. 2 of the accompanying drawings;(g) nuclear magnetic resonance spectrum; the nuclear magnetic resonance spectrum (δ
ppm), measured at 400 MHz in a mixture of deuterium oxide and deuterohydrochloric acid of pH value about 3.0, using sodium 2,2-dimethyl-2-silapentane-5-sulfonate as the internal standard, is as illustrated in FIG. 3 of the accompanying drawings;(h) solubility; soluble in water and methanol, sparingly soluble in acetone, and insoluble in ethyl acetate, chloroform and benzene; (i) color reactions; positive in Ninhydrin and Rydon-Smith reactions; (j) thin layer chromatography; Rf value=0.65, using a cellulose sheet (Eastman) as adsorbent and a 15;
10;
3;
12 by volume mixture of butanol, pyridine, acetic acid and water as the developing solvent;(k) high voltage paper electrophoresis; using Toyo'"'"'s filter paper No. 51A in a 0.1M tris-hydrochloric acid buffer solution of pH 7.5 (3300 volt/60 cm, 1 hour);
the migration distance (detected by bioautography with Bacillus subtilis PCI
219) from the origin to the cathode was 4 cm. - View Dependent Claims (2, 3, 4, 5, 6, 7)
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Specification