Pharmaceutical formulations comprising labdanes for the treatment of tumors or leukemias

a technology for cancer and labdane, which is applied in the direction of biocide, plant/algae/fungi/lichens, drug compositions, etc., can solve the problems of unstable encapsulation, inefficient encapsulation, and early results that are disappointing

Inactive Publication Date: 2006-04-11
MEDEXIS SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Early results were, however, rather disappointing, owing mainly to their colloidal and biological instability, and their inefficient and unstable encapsulation of drug molecules.

Method used

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  • Pharmaceutical formulations comprising labdanes for the treatment of tumors or leukemias
  • Pharmaceutical formulations comprising labdanes for the treatment of tumors or leukemias
  • Pharmaceutical formulations comprising labdanes for the treatment of tumors or leukemias

Examples

Experimental program
Comparison scheme
Effect test

example 1

Labd-13-end,8α-ol,15-yl Acetate

[0052]Labd-13-end,8α,15 diol (I) (50 mg) was dissolved in 2 ml of Ac2O-Py (acetic anhydrate-pyridine) for 48 hours at room temperature. The reaction mixture evaporated in vacuum to remove the solvents The purity as well the identification of the compound labd-13-ene,8α-ol,15-yl acetate was tested by TLC (Thin Layer Chromatography) and GC-MS (Gas Chromatography-Mass Spectrometry), using chromatography data. Compound was obtained in its pure state (47 mg).

example 2

Labd-13-ene-8α-ol 15-yl-β(or -α)-D (or -L)-pyrano (or furano)sides as Monosaccharides or as Disaccharides

[0053]Labd-14-ene-8α-ol 13-yl-β(or -a)-D (or -L)-pyrano (or furano)sides as monosaccharides or as disaccharides. 3-yl-β(or -a)-D (or -L)-pyrano (or furano)sides as monosaccharides or as disaccharides, Labd-14-ene, 8, 13-epoxy As an example

[0054]Condensation of Labd-13-ene-8α,15-diol (I) with 2,3,4,6-tetra-O-acetyl-a-D-glucopyranosyl bromide was carried out in a two-phase system consisting of chloroform-1.25M aqueous potassium hydroxide solution and benzyltriethylammonium bromide as catalyst. After a simple work up, followed by column chromatography, the labdane glycosides glycosides were isolated in 30% yield.

example 3

Thiomidazolide Derivative of 3β-hydroxy-labd-14-ene-8,13-epoxy

[0055]3β-hydroxy-labd-14-ene-8,13-epoxy, was converted to its thiomidazolide (45% yield) by treatment with N,N′-thiocarbonydiimidazole (Rasmunssen, J. R. (1980) J. Org. Chem. 45, 2725-2727).

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Abstract

The present invention relates to novel compositions based on hydrated lipidic lamellar phases or liposomal compositions, prepared by combining different lipid molecules, synthetic and / or from natural sources, said compositions comprising at least one of a) labd-13-ene-8α, 15-diol and / or derivatives thereof; b) labd-14-ene-8, 13-diol or derivatives thereof; c) 3β-hydroxy-labd-14-ene-8, 13-epoxy and / or derivatives thereof, d) a plant extract containing the aforementioned labdanes or derivatives thereof. The compositions of the invention exhibit cytotoxicity against cancerous cells and are utilized for the treatment of tumors and leukemias.

Description

BACKGROUND OF THE INVENTION[0001]A very large number of diterpenoids possessing a labdane skeleton (FIG. 1) occur in nature (Connoly, J. D.; Hill, R. A Dictionary of Terpenoids, Chapman and Hall: London 1991). The interest in studying labdanes is heightened due to the wide range of biological activities of these compounds (Singh, M.; Pal, M.; Sharma, R. P. Plants Med., 1999, 65, 2-8.). They comprise a decalin system and a C-6 ring, which may be open or closed with an oxygen atom, as in manoyl oxide and its derivatives. Labdanes have been isolated from several plant families, such as Asteraceae, Labiateae, Cistacease, Pinaceae, Cupressaceae, Taxodiaceae, Acanthaceae, Annonaceae, Caprifoliaceae, Solanaceae, Apocynaceae, Verbenaceae and Zingiberaceae. In addition they have been isolated from marine algae of the genus Laurence, from Taonia atomaria and from the red alga Chondria tenuissima.[0002]The conifers are an important source of diterpenoids. Several labdanes have been detected in...

Claims

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Application Information

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Patent Type & Authority Patents(United States)
IPC IPC(8): A61K9/127A61K9/133C07D311/92A61K31/047A61K31/22A61K31/352A61P35/00A61P35/02
CPCA61K9/127A61K31/352A61K31/047A61P35/00A61P35/02
Inventor ANASTASSAKI, THALIAANGELOPOULOU, DEMETRAKOKKINOPOULOS, DEMETRIOSDIMAS, CONSTANTINOSDEMETZOS, CONSTANTINOS
Owner MEDEXIS SA
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