Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Conjugate or complex
Patent
1991-04-15
1993-10-26
Rollins, John W.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Conjugate or complex
514934, A61K 3578
Patent
active
052564169
DESCRIPTION:
BRIEF SUMMARY
The invention relates to an extract of the Acanthospermum hispidum plant containing water-soluble components with a molecular weight >2,000.
The invention also relates to the use of the Acanthospermum hispidum extract as a medicament. Furthermore, the invention relates to the use of extracts of the Acanthospermum hispidum plant for the immunomodulation (influencing the immune state) of mammals, for the remedy of radiation sickness as well as for the prophylaxis and therapy of viral and retroviral diseases in mammals and for the therapy of tumors.
Finally, the invention relates to a method for producing an extract of parts of the Acanthospermum hispidum plant and effecting separation of the ingredients based on their molecular weight.
Acanthospermum hispidum (compositae) is a plant originating from South America which has spread worldwide throughout the Tropics. In traditional medicine West Africans have used Acanthospermum hispidum (A.h.) for the production of tea (extracts) useful in the treatment of jaundice. Furthermore, A.h. is used in the treatment of Herpes labialis, the juice of the leaves being swabbed on the affected area.
The therapeutic effect of said extracts (as well as that of the leaf juice) in the treatment of Herpes labialis is the following: pain relief within one to three hours after application, reduction of the healing process to two to three days and extension of the relapse intervals. If this natural remedy is applied within the first few hours after the symptoms have begun to appear, it will usually completely suppress any lesion formation. The extract is also effective against Herpes genitalis.
A list of the ingredients of A.h. can be taken from the monograph "The Biology and Chemistry of the Compositae", V. H. Heywood, J. B. Harborne and B. L. Turner (eds.), Academic Press, London, New York, San Francisco, 1977. Melampolides, galactosides, acetylenes were isolated from A.h. by the F. Bohlmann group in Berlin, and their chemical structure was clarified. (Phytochemistry, 1979, Vol. 18, pages 625-630; Planta Medica, 1986, pages 154-155; Phytochemistry, 1976, Vol. 15, pages 1776-1778). The essential oils of said plant were studied to find out their microbial and antifungal effect (S.RR. Jain et al., Planta Medica, 1972, Vol. 22, page 136; and S. R. Jain and A. Kar, Planta Medica, 1971, Vol. 20, page 118). Toxicological studies on the use of A.h. as a fodder plant were conducted by B. Ali and I. Adam in goat and mice (J. Comp. Pathology, 1978, Vol. 88, pages 443-448 and pages 533-544).
However, Acanthospermum hispidum or an extract of said plant has not been used widely so far, as it has not been possible to administer it orally due to the toxicity of some of its ingredients.
Thus, the object underlying the invention is to provide a non-toxic but therapeutically active Acanthospermum hispidum preparation. This object is achieved by the surprising finding that the removal of low molecular components from the Acanthospermum hispidum extract causes the toxic effect of the extract to disappear.
Thus, one subject matter of the invention is the provision of an extract of the Acanthospermum hispidum plant containing the water-soluble components thereof with a molecular weight >2,000.
A further subject matter of the invention is the provision of the mentioned extract of the Acanthospermum hispidum plant for use as a medicament, especially as an immunomodulator, in the remedy of radiation sickness, in the prophylaxis and therapy of viral diseases or retroviral diseases in mammals and in the therapy of tumors.
It is preferred that the extracts of the invention be aqueous Acanthospermum hispidum extracts. However, there have also been used other extracting agents such as ethanol, chloroform, isopropanol, gasoline, and the like. The invention will be discussed hereinafter and exemplified by an aqueous extract. The term "aqueous extract" shall be understood to mean a substantially aqueous extract, i.e., it may contain small amounts of a non-aqueous solvent, e.g., not more than 10, preferably
REFERENCES:
The Biology and Chemistry of the Compositae, Heywood et al., eds., Academic Press, 1977.
Bohlmann et al., Phytochemistry, 18, 625-630 (1979).
Jakupovic et al., Planta Medica, 154-155 (1986).
Nair et al., Phytochemistry, 15, 1776-1778 (1976).
Jain et al., Planta Med., 22(2), 136-139 (1972).
Jain et al., Planta Med., 20(2), 118-123 (1971).
Ali et al., J. Comp. Path., 88, 443-448; 533-544 (1978).
Munder et al., Augmenting Agents in Cancer Therapy, 441-458 (1981).
Eichmann Klaus
Modolell Manuel
Merck Patent GmbH
Rollins John W.
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