Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1986-11-07
1989-02-21
Rollins, John W.
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
C07D31162
Patent
active
048066591
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention pertains to a novel tannin composition and, more particularly, to a novel tannin composition used for treating mental disorders such as acute and chronic schizophrenia and the like.
BACKGROUND ART
Rhei Rhizoma is a kind of crude drug previously known, and used frequently in traditional chinese prescription (Kampo). The Rhei Rhizoma is so far known to possess an antibacterial effect, blood urea nitrogen-decreasing activity and anti-inflammatory effect. In the prior art, in order to obtain substances providing such effects, various compositions and/or compounds such as sennoside A have been isolated from Rhei Rhizoma. However, among the compounds isolated from Rhei Rhizoma, no components usable for treating mental disorders have been previously known at all.
Whereas, the following chemical compounds have been known as antipsychotic drugs used for treating schizophrenia:
Levomepromazine, chlorpromazine and thioridazine showing strong sedative effect; perphenazine, fluphenazine and haloperidol showing strong anti-hallucination and -delution effects; and sulpiride having mild sedative effect, and anti-hallucination and -delution effects. These drugs have been selectively used, according to their respective characteristics, in response to patient's symptoms and the progress of disease. However, it has been well-known that these drugs produce adverse effects which are extrapyramidal syndrome such as muscle rigidity, dyskinesia and parkinsonism, and autonomic symptoms such as salivation, dry mouth and constipation. Consequently, a drug without adverse effects for treating mental disorders has long been desired to be developed.
DISCLOSURE OF INVENTION
Therefore, one of the objects of the present invention is to provide a novel tannin composition.
Another object of the present invention is to provide a novel tannin composition extracted from Rhei Rhizoma.
A further object of the present invention is to provide such novel tannin composition having a potent antipsychotic effect, which can be used for treating acute and chronic schizophrenia, without causing any adverse effects.
These and other objects, together with the advantages thereof over the prior art, will become apparent from the following description and the appended claims.
A tannin according to the present invention is represented by the following general octameric structural formula: ##STR4## wherein
1 is an integer from 0 to 6, m is 0 or 1, n is an integer from 0 to 6, and l+m+n=6;
R.sub.1 is hydrogen or G, G representing galloyl group ##STR5##
X is ##STR6##
R.sub.2 is OH, . . . OG, or . . . OH; and filled dots mean bonding sites, and there is no possibly to bond between the mutual fourth positions in each unit, and there is only one bonding between the fourth position and the sixth position; and there is a total of three galloyl groups in the tannin.
In accordance with the present invention, the above tannin composition may be obtained by the following steps:
obtaining an extractive from Rhei Rhizoma with water or an aqueous solution of an organic solvent;
separating said extractive or its concentrated liquid by gel filtration chromatography using water, an aqueous solution of ethanol, ethanol and methanol sequentially, to obtain a methanolic eluate;
separating said methanolic eluate, its concentrated liquid or dried solid by gel filtration chromatography with a mixture of at least two solvents selected from the group consisting of water, ethanol, methanol and acetone, to obtain an eluate;
subjecting said eluate to high performance liquid chromatography [column: Nucleosil 5C.sub.18 (Macherey-Nagel) (4.times.250 mm); mobile phase: 14-80% CH.sub.3 CN/H.sub.2 O (25 mM oxalic acid); flow rate: 1 ml/min; column temperature: 40.degree. C.], to separate and obtain a fraction eluted at the retention time from 10 to 25 minutes; and
removing the solvent from said eluted fraction.
It is also disclosed, according to the present invention, that the above tannin composition is effective in treating mental disorders such as
REFERENCES:
Nonaka et al., Chem. Pharm. Bull, 29, pp. 2862-2870 (1981).
Skakun et al., Farmakal Toksikol, 49, No. 2, pp. 45-48 (1986).
Genichiro Nonaka
Itsuo Nishioka
Michihiro Fujiwara
Showa Ueki
Catchpole W.
Kabushiki Kaisha Tsumura Juntendo
Rollins John W.
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