Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1986-08-28
1988-11-29
Fan, Jane T.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
549298, A61K 3134
Patent
active
047882166
DESCRIPTION:
BRIEF SUMMARY
This invention relates to pharmacologically active compounds. Moreover, the invention concerns pharmacological preparations containing the compounds as well as the use of the compounds in the treatment of various diseases.
The compound according to the invention consists of podophyllotoxin and derivatives thereof which have the formula ##STR2## wherein R.sub.1 is H or OH and R.sub.2 is H or CH.sub.3.
Podophyllotoxin and its derivatives have been found to have a plurality of outstanding pharmacological effects. Thus, they supress the activity of lymphatic T-cells ("killer cells") and can therefore be used to counteract reactions of immunity and rejection at transplantations. Besides, they inhibit cell division in the meta phase and can therefore be used for treatment of psoriatic diseases. The compounds also have biocidal and biostatic effects against such microorganisms as plasmodia, fungi and viruses, and they can therefore be used in the treatment of parasitic diseases, such as malaria, and viral diseases. Furthermore the compounds also act as anthelmintics.
The compound podophyllotoxin is previously known and has been extracted from plants, mainly from the genus Podophyllum. However, the compound has not earlier been used in its highly pure form according to the present invention, which has made possible its use in new indication fields. In previous works, an impure extract from Podophyllum species, so-called "podophyllin", has mostly been used, which has only contained 20-40% of podophyllotoxin. Moreover, the extract contains a great number of other components such as desoxypodophyllotoxin, dehydropodophyllotoxin, .alpha.- and .beta.-peltatin etc., depending on from which species the extract has been recovered. Several of these other components have been found to be considerably mutagenic.
The compound podophyllotoxin has the following physical data in its pure state:
Melting point: 183.degree.-184.degree. C. (substance free of solvent).
Optical rotation [.alpha]sup.20.sub.D : -132.5 (C0.2CHCl.sub.3).
Solubility in water: 120 mg/l.
Podophyllotoxin and its derivatives can be extracted from plant parts, especially roots or rhizomes, from various species of the genus Podophyllum, such as P. emodi Wall. and P. peltatum L. The compound also occurs in other plant species, for example of the genus Juniperus such as J. virginiana L.
In the preparation of highly pure podophyllotoxin or its derivatives according to the invention, dried and finely ground rhizomes of e.g. Podophyllum emodi or Podophyllum peltatum are extracted e.g. with ethyl acetate and the extract is concentrated and filtered through silica gel. The desired fraction of podophyllotoxin and derivatives thereof is thereafter chromatographed on acid alumina and yields a fraction substantially containing the five lignanes deoxypodophyllotoxin, podophyllotoxone, isopicropodophylline, podophyllotoxin and 4'-demethylpodophyllotoxin. Podophyllotoxin or another desired derivative is isolated from this mixture through a careful chromatography on silica gel, after which the desired fraction is recrystallized.
Highly pure podophyllotoxin and its derivatives accordidng to the invention have been found to have a number of excellent pharmacological effects and can be used against several diseases. In accordance with this, the present invention also comprises pharmacological preparations which are characterized in that they contain podophyllotoxin and/or its derivatives together with one or more pharmacologically acceptable carrier materials.
As carrier materials all those materials can be used which are known to be useful in the preparation of pharmacological preparations, provided they do not react unfavourably with the active compound or exert some unsuitable effect together therewith. The pharmacological preparations can be made for enteral, parenteral or dermal administration and they can for example be in the form of solid preparations such as tablets, powder, capsules, suppositories or vagitories, more or less semi-liquid preparations such as ointments, g
REFERENCES:
patent: 4122092 (1978-10-01), Kende et al.
patent: 4567253 (1986-06-01), Durst et al.
Gensler et al., J. Org. Chem. 1966, vol. 31, pp. 4004-4008, 3224-3226.
Gensler et al., J.A.C.S., vol. 82, 1960, pp. 6074-6081.
Kuramochi et al., CA 104:61623t.
Leander Kurt
Rosen Borje
Conpharm AB
Fan Jane T.
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