Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Conjugate or complex
Patent
1993-04-21
1996-09-17
Kight, John
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Conjugate or complex
514783, A61K 3578
Patent
active
055566260
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a new chemotherapeutic drug having antineoplastic activity, extracted from the fruits of plants of the family Palma, the subfamily Phoenicoideae and the genus Phoenix.
In research aimed at the fight against cancer, one of the most representative lines of research is that of antitumoral chemotherapy. The antineoplastic chemotherapeutic agents isolated up to date have the widest of origins and chemical characteristics. Certain of these antiproliferative agents are extracted from plants, such as, for example, colchicine from Colchicum autumnale and vincaleucoblastin from Vinca rosea. However, all these substances, along with a certain specifically antitumoral activity, show a low selectivity with respect to the degenerated cells; for this reason their interference on the metabolism of healthy cells represents a large obstacle to their indiscriminate use.
The present inventor has already patented another antitumoral drug of plant nature (and more particularly the substance CIDI extracted from the fruit of Pittosporum tobira), prossessing highly selective antitumoral activity and a toxicity level greatly reduced with respect to all the other antineoplastic drugs. Continuing along this line of research, the present inventor has isolated a new antineoplastic chemotherapeutic agent, once again of plant origin, which also shows highly selective antitumoral activity and extremely low toxicity.
A first object of the present invention is therefore a process for obtaining substances and/or compositions having antineoplastic activity, characterized by the fact that parts and/or products of plants belonging to the family Palma--at whatever stage of their development and maturity--are subjected essentially to the following operations: with another solvent at least partially miscible with the first, to divide the components of the extract in the phases which form; using at least one or two organic liquids having solvent activity with respect to at least one of the components of the extract, followed by filtering of any precipitate which forms and evaporation to a dry state of the floating residue; and of those without antineoplastic activity.
The extracts can be brought to a dry state and purified before each successive stage of the process.
The plants of the family Palma are preferably of the subfamily Phoenicoideae and the genus Phoenix. In this regard, the plants can be selected, for example, from numerous species including Phoenix canadiensis, Phoenix dactylifera, Chamaerops excelsa, Chamaerops humilis and many others.
The solvent can be an alcohol. Good results have been obtained using ethyl alcohol.
The volume ratio between organic solvent and parts of plants to be treated is preferably between 1:10 and 10:1.
The treatment times are preferably between 5 minutes and 3 months. The treatment temperatures can vary, preferably between 5.degree. C. and 100.degree. C.
The total alcoholic extract of the drug, at a dilution of 1 mg/ml, can be analyzed on an HPLC (Perkin-Elmer series 250 liquid chromatograph), using a 125 mm-4 mm RP 18 column with a methanol-H.sub.2 O (80:20) mobile phase and wavelengths equal to 210 nm. Said total alcoholic extract shows approximately 14 peaks with RT of from 1.123 (1st peak) to 33.461 (14th peak); the most representative peaks are of RT 1,123 (3.36% area); RT 1.301 (3.01% area); RT 1.583 (63.34% area); RT 2.133 (14.88% area) and RT 2.636 (3.33% area).
Separation of the components of the extract can preferably be carried out chromatographically. Good results have been obtained using chromatography on a silica gel column or on an HPLC preparative column.
Extraction can be performed using methanol and collecting the components which have HPLC retention times of about 1.123, 1.301, 1.583, 2.133 and 2.636.
After extraction with ethanol, the solution obtained can be shaken with chloroform, forming two phases, an alcohol-chloroform phase of a green color, and an aqueous phase of bordeaux-red color. In this case the components having antineoplastic activity are found
REFERENCES:
Index of Garden Plants Ed. Mark Griffiths, pp. 832-833, (The MacMillan Press Ltd.), 1994.
M. I. Fernandez, et al. Constituents of a Hexane Extract , Phoenix Actylifera, Phytochemistry, 22(9) 2087-8, 1983.
Kight John
Lee Howard C.
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