Organic compounds -- part of the class 532-570 series – Organic compounds – Cyclopentanohydrophenanthrene ring system containing
Patent
1989-03-29
1991-06-25
Rizzo, Nicholas S.
Organic compounds -- part of the class 532-570 series
Organic compounds
Cyclopentanohydrophenanthrene ring system containing
2604121, C07J 3100
Patent
active
050268830
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
This invention relates to the identification, isolation and preparation of an active principle by extraction from natural tissues, and in particular it relates to the identification, isolation and preparation of such an active principle by extraction from particular tissues of sharks.
In Japan, a preparation known as "deep-sea shark liver oil" has been used as a folk remedy for a long time. It is an oil prepared from shark's liver and is normally capsulated in soft capsules. The liver oil is said to be effective in treatment of many kinds of diseases, especially those which are related to the liver, such as hepatitis, nephritis, diabetes, etc. As well, when used externally, it is widely recognised that the liver oil is effective in treatment of scalds, burns or other types of skin trouble, and also is ideal as an ingredient for cosmetics.
SUMMARY OF THE INVENTION
The present inventors have been studying this material for many years, and recently have discovered the unexpected fact that an active substance exists in the aqueous component of shark's liver rather than the oil soluble component. This fact was recognised from a comparison of the practical use of the liver oil and a powder produced from the aqueous component of the liver by evaporation of the water. In comparative tests of a dosage of 900 mg of the liver oil per day and 60 mg of the powder per day, the latter gave a better clinical result than the former. Furthermore, where the liver oil was thoroughly washed with water, the resulting oil showed almost no effect. These facts indicate that the active substance of deep-sea shark liver is not oil-soluble as previously believed, but is water-soluble.
According to the present invention, there is provided an active principle which is isolated from an aqueous extract of the liver and/or gallbladder of a shark.
In a first aspect of the invention, there is provided a compound of the general formula I, in substantially pure form, ##STR1## wherein A is a cation, such as a sodium, potassium, calcium or ammonium ion, or an organic amine.
In other aspects, this invention provides a method for the preparation of a compound of general formula I in substantially pure form, together with compositions for pharmaceutical, dietary or cosmetic purposes which comprise such a compound.
By using activity assays which are described in detail below, it has been shown that the active principle is water-soluble and does not exist in the oil-soluble component of shark's liver. These assays have been used in a series of tests to ascertain whether the active principle exists only in the liver. All parts of the shark's body, such as the bones, meat, gallbladder, ovary, alimentary canal, etc., have been investigated, and it has been found that the gallbladder showed the same activities as liver in the assays. This result indicates that the active principle exists only in liver and gallbladder.
In general terms, the two bioassays referred to herein and used to identify sources of the active principle and to assess the degree of purity of an extract, are designed to identify characteristic pharmacological activities of the substance. In particular, the bioassays, designated as (A) and (B) are based on the following activities:
(A) The active principle prevents liver trouble in mice caused by carbon tetrachloride.
(B) The active principle increases the respiration rate in mice when a toxic substances such as nicotine is administered.
The present invention also provides a method for preparing an active principle as described above, which comprises the steps of preparing an aqueous extract of the liver and/or gallbladder of a shark, and isolating the active principle from the aqueous extract.
DETAILED DESCRIPTION
The following description sets out general procedures for isolation of the active principle from the aqueous extract of the liver and/or gallbladder of a shark, involving the steps of extraction with polar organic solvents, adsorption on suitable adsorbents and/or chromatography techniques.
REFERENCES:
patent: 2136453 (1938-11-01), Merker
patent: 3994878 (1976-11-01), Partridge
patent: 4296109 (1981-10-01), Laurent et al.
Snyder and Kirkland, Introduction to Modern Liquid Chromatography, (New York, J. Wiley and Sons, 1979), p. 477.
Honma et al., Rep. Sado. Mar. Biol. STN Niigata Univ., 0(17), 1-12, 1987--Biological Abstracts, vol. 86, 1988, Abstract 3404.
Ishida Hitoshi
Kosuge Takuo
Kosuge Yoshiki
Tsuji Kuniro
Broadbent James Meredyth
Kosuge Yoshiki
Rizzo Nicholas S.
Ward E. C.
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