Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Conjugate or complex
Patent
1993-01-28
1996-09-24
Kight, John
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Conjugate or complex
514783, A61K 3578
Patent
active
055588662
DESCRIPTION:
BRIEF SUMMARY
DESCRIPTION
The present invention has as its subject substances and compositions having an antineoplastic activity, extracted from plants of the family Pittosporaceae, pharmaceutical preparations based on at least one of said substances and compositions, and processes for the extraction and, respectively, formulation thereof.
As it is known, one of the most promising lines of research which, at least from a theoretical point of view, is of easy application in research aimed at eliminating neoplastic diseases, is that of antitumoral chemotherapy. The antiproliferating agents which have been isolated up to the present time are of widely differing origins and heterogeneous chemical characteristics. Among these antiproliferating agents are also certain substances extracted from plants such as colchicine and vincaleucoblastin, the former extracted from Colchicum Autumnale and the latter from Vinca Rosea. Although these antiproliferating substances are more or less provided with a certain specifically antitumoral activity, their selectivity towards degenerated cells is generally rather poor. The danger deriving from the possibility of their interfering with the metabolism of healthy cells thus forms an important obstacle to their wider use.
It has now been surprisingly found that the present invention makes it possible to overcome the above mentioned limitations, providing a chemotherapeutic antineoplastic agent based on active principles of plant origin and provided with highly selective antitumoral activity and a toxicity level much lower than that of other antitumoral drugs.
First of all, the subject matter of the present invention is a process for obtaining substances and/or compositions having an antineoplastic activity, characterized by the fact that parts and/or products of plants from the family Pittosporacea--in whatever stage of their development or maturity--are made to undergo essentially the following operations: another solvent, at least partially miscible with the first, to distribute the components of the extract among the phases formed; least one further organic liquid having the properties of solvent for at least one of the components in the extract, followed by filtering of any suspension which may have formed and collection of the solid phase and its successive purification; those without antineoplastic activity.
The extracts can be dried and purified before each further stage of the process.
The plants of the family Pittosporacea are preferably of the genus Pittosporum. In this sense, the plants can be selected, for example, from the group comprising Pittosporum ondulatum, Pittosporum coriaceum, Pittosporum viridicolor, Pittosporum rhombipholium, Pittosporum eugenoides, Pittosporum crossifolium and Pittosporum Tobira and combinations thereof.
The solvent can be an alcohol. Good results have been obtained using ethyl alcohol.
The volume ratio between organic solvent and plant parts to be treated is preferably comprised between 1:10 and 10:1.
The treatment times are preferably comprised between 5 minutes and 3 months. The treatment temperatures can vary preferably between 5.degree. C. and 100.degree. C.
Separation of the components from the extract can be preferably of the chromatographic type. Good results have been obtained using chromatography on a silica gel column or on an HPLC preparatory column.
Extraction can be performed using ethanol and collecting the components which have HPLC retention times of about 1,157, 1.545, 1,883, 2,051, 2.273, 2,572 and 2,743.
(It must be specified that the analytic tests in HPLC, both in this case and in the following ones, were carried out using a Perkin-Elmer series 250 chromatograph with a 125 mm.multidot.4 mm RP 18 column with a mobile phase consisting of methanol-H.sub.2 O (80:20) and a wave length equal to 210 nm).
After extraction with ethanol, the solution thus obtained can be shaken with chloroform forming two phases, an alcohol-chloroform phase of an intense green color and an aqueous phase of an orange-yellow color. In this case the components
REFERENCES:
Chemical Abstract, vol. 72, 75619d (1970).
"Triterpenoid Sapogenins From Leaves of Pittosporum undulatum," Phytochemistry, vol. 22, No. 5, pp. 1235-1237 (1983).
"Triterpenoid Saponins From Leaves of Pittospurum undulatum", Phytochemistry , vol. 22, No. 11, pp. 2565-2569 (1983).
Chemical Abstract, vol. 94, 1274b (1981).
Saponin and Sapogenol. VI.sup.1) Sapogenol Constituents of Leaves of Pittosporum tobiran Ait., by I. Yosioka et al, Chem. Pharm. Bull., 20(7), 1499-1506 (1972).
Terpenes From Pittosporaceae, by E. Nemethy et al, Phytochemistry, vol. 21, No. 12, pp. 2981-2982 (1982).
"The Structure of a New Sesquiterpene Glycoside from the Flowers of Pittosporum tobira", by T. Suga et al, Chemistry Letters, pp. 445-448, 1988.
Chemical Abstract, vol. 104, 31777d (1986).
Chemical Abstract, vol. 77, 149711e (1972).
Chemical Abstract, vol. 72, 705v (1970).
Chemical Abstract, vol. 83, 128752c (1975).
Jay, M. et al, Phytochemistry, 1974, vol. 13, pp. 1565-1569.
Index of Garden Plants Ed. Mark Griffiths, pp. 902-903, (The MacMillan Press Ltd.), 1994.
"Journal of Natural Products" vol. 41, 1978--pp. 463-471. D. A. Van Den Berghe et al Screening of Higher Plants For Biological Activities.
"Screening of High Plants For Biological Activities" vol. 36, 1979 pp. 311-321--Margaretha Ieven et al.
Kight John
Lee Howard C.
LandOfFree
Antineoplastic chemotherapeutic of plant origin, having high sel does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Antineoplastic chemotherapeutic of plant origin, having high sel, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Antineoplastic chemotherapeutic of plant origin, having high sel will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1927136