EP0058093A1
Expired / Lapsed
EP
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Glycoprotein having anti-tumour and lectin-like activity
Assignee: Kureha Corp
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Filing: 1982-02-10
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Granted: —
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Expires: 2002-02-10
Abstract
Abstract A glycoprotein suitable for use in treating tumours has a molecular weight of 5,000 to 300,000 as determined by the ultracentrifugation method; the ratio of the weight of its protein moiety, determined by Lowry-Folin's method, to the weight of its saccharide moiety, determined by the phenol - sulfuric acid method, being from 50:50 to 80:20; the amino acid at its N-end being tyrosine, leucine or alanine; the amino acid sequence at its C-end being leucine-phenylalanine-valine; its elementary composition being 35.2 to 49.3% of C, 4.8 to 8.0% of H, 4.3 to 12.3% of N, a trace amount to 2.5% of S, a trace amount to 1.2% of P and the balance being 0; its isoelectric point being from pH 2.5to 5.0; and having a nucleic acid component. The glycoprotein can be obtained from basidiomycetous fungus of genus Coriolus and can be formulated into a pharmaceutical composition with convention carriers or diluents.
Inventors
- 👤 Chikao Yoshikumi
- 👤 Takayoshi Fujii
- 👤 Takao Furusho
- 👤 Kenichi Matsunaga
- 👤 Minoru Ohara
- 👤 Akira Kobayashi
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-24 17:13
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/37; C07K14/375; A; A61; A61P; A61P35/00; A61K; A61K38/00
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
138 words
A glycoprotein having a molecular weight of from 5,000 to 300,000 as determined by the ultracentrifugation method; the ratio of the weight of its protein moiety, as determined by Lowry-Folin's method, to the weight of its saccharide moiety, as determined by the phenolsulfuric acid method, being from 50:50 to 80:20; the amino acid at its N-end being tyrosine, leucine or alanine; the amino acid sequence at its C-end being leucine to phenylalanine to valine, the terminal amino acid being leucine: its elementary composition being from 35.2 to 49.3% of C, from 4.8 to 8.0% of H, from 4.3 to 12.3% of N, from a trace amount to 2.5% of S, from a trace amount to 1.2% of P and the balance being O; its isoelectric point being from pH 2.5 to pH 5.0; and having nucleic acid component.
Claim 2
Dependent Claim
138 words
A glycoprotein having a molecular weight of from 5,000 to 300,000 as determined by the ultracentrifugation method; the ratio of the weight of its protein moiety, as determined by Lowry-Folin's method, to the weight of its saccharide moiety, as determined by the phenolsulfuric acid method, being from 50:50 to 80:20; the amino acid at its N-end being tyrosine, leucine or alanine; the amino acid sequence at its C-end being leucine to phenylalanine to valine, the terminal amino acid being leucine: its elementary composition being from 35.2 to 49.3% of C, from 4.8 to 8.0% of H, from 4.3 to 12.3% of N, from a trace amount to 2.5% of S, from a trace amount to 1.2% of P and the balance being O; its isoelectric point being from pH 2.5 to pH 5.0; and having nucleic acid component.
Claim 3
Dependent Claim
78 words
A glycoprotein according to claim 1, wherein the protein moiety comprises aspartic acid, threonine, serine, glutamic acid, proline, glycine, alanine, cysteine, valine, methionine, cystathionine, isoleucine, leucine, tyrosine, phenylalanine, tryptophan, ornithine, lysine, histidine and arginine, and the total weight of said aspartic acid, said threonine, said serine, said glutamic acid, said glycine, said alanine, said phenylalanine, said valine, said leucine and said isoleucine is more than 75% by weight of the total weight of all of said amino acids.
Claim 4
Dependent Claim
167 words
A glycoprotein according to claim 2, wherein the protein moiety consists of 10 to 20% by weight of aspartic acid, 4 to 6% by weight of threonine, 3 to 6% by weight of serine, 10 to 16% by weight of glutamic acid, a trace amount to 8% by weight of proline, 6 to 10% by weight of glycine, 6 to 13% by weight of alanine, a trace amount of cysteine, 5 to 12% by weight of valine, a trace amount to 4% by weight of methionine, a trace amount to 3% by weight of cystathionine, 3 to 8% by weight of isoleucine, 8 to 13% by weight of leucine, a trace amount to 5% by weight of tyrosine, 3 to 9% by weight of phenylalanine, a trace amount to 1% by weight of tryptophan, a trace amount to 2% by weight of ornithine, 1 to 4% by weight of lysine, a trace amount to 2% by weight of histidine and 1 to 4% by weight of arginine.
Claim 5
Dependent Claim
49 words
A glycoprotein according to any one of the preceding claims, wherein the saccharide moiety comprises fucose, ribose, arabinose, xylose, mannose, galactose, glucose and glucosamine, and the total weight of said xylose, said mannose and said glucose is more than 85% by weight of the total weight of said saccharides.
Claim 6
Dependent Claim
73 words
A glycoprotein according to claim 4, wherein the saccharide moiety consists of 0.5 to 4.0% by weight of fucose, a trace amount to 2.0% by weight of ribose, 0.3 to 6.0% by weight of arabinose, 2.0 to 40.0% by weight of xylose, 5.0 to 20.0% by weight of mannose, 0.5 to 8.0% by weight of galactose, 30.0 to 80.0% by weight of glucose and a trace amount to 3.0% by weight of glucosamine.
Claim 7
Dependent Claim
34 words
A glycoprotein according to any one of the preceding claims, wherein the nucleic acid component comprises uracil as a nucleic acid base in an amount of 0.01 to 0.50% by weight of the glycoprotein.
Claim 8
Dependent Claim
18 words
A glycoprotein according to any one of the preceding claims for use in the treatment of a tumour.
Claim 9
Dependent Claim
78 words
A process for producing a glycoprotein, which process comprises extracting fruit bodies or mycelia of a basidiomycetous fungus belonging to the genus Coriolus with hot water or an aqueous 0.01 to 2.ON alkali solution, subjecting the resultant extract to dialysis and/or ultra-filtration thereby removing a low molecular weight substance(s) having a molecular weight below 5,000, and collecting the fraction precipitating at a pH in the range of from 2.5 to 5.0 at the isoelectric point of the glycoprotein.
Claim 10
Dependent Claim
78 words
A process for producing a glycoprotein, which process comprises extracting fruit bodies or mycelia of a basidiomycetous fungus belonging to the genus Coriolus with hot water or an aqueous 0.01 to 2.ON alkali solution, subjecting the resultant extract to dialysis and/or ultra-filtration thereby removing a low molecular weight substance(s) having a molecular weight below 5,000, and collecting the fraction precipitating at a pH in the range of from 2.5 to 5.0 at the isoelectric point of the glycoprotein.
Claim 11
Dependent Claim
42 words
A process according to claim 8, wherein the basidiomycetous fungus is selected from Coriolus versicolor (Fr.) Quél., Coriolus hirsutus (Fr.) Quél., Coriolus pergamenus (Fr.) Pat., Coriolus consors (Berk.) Imaz., Coriolus pubescens (Fr.) Quél., Coriolus biformis (Klotz.) Pat. and Coriolus conchifer (Schw.) Pat.
Claim 12
Dependent Claim
30 words
A process according to claim 8 or 9, wherein the step of extracting is carried out at a temperature of from 80 to 100°C for from 1 to 8 hours.
Claim 13
Dependent Claim
38 words
A process according to any one of claims 8 to 10, wherein the glycoprotein is collected by the method of fractional precipitation at isoelectric points while adjusting the pH of the glycoprotein solution to from 2.5 to 5.0.
Claim 14
Dependent Claim
44 words
A process according to claim 11, wherein the method of fractional precipitation at the isoelectric point is carried out on a solution of ion strength of from 0.1 to 3.1µ at a temperature of from 5 to 25°C and for more than 0.5 hours.
Claim 15
Dependent Claim
24 words
A process according to any one of the preceding claims, wherein the fraction collected by precipitation is neutralized and subjected to dialysis or ultrafiltration.
Claim 16
Dependent Claim
46 words
A pharmaceutical composition which comprises a glycoprotein as claimed in any one of claims 1 to 7 or which has been produced by a process as claimed in any one of claims 8 to 13 as active ingredient, together with a pharmaceutically acceptable carrier or diluent.
Claim 17
Dependent Claim
13 words
A pharmaceutical composition according to claim 14 which is in unit dosage form.
References Cited (Backward Citations)
GB1331513A
Cited
GB1521168A
Cited
GB1565090A
Cited
US4202969A
Cited
GB1570538A
Cited
GB1538399A
Cited
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