Novel dna polymerase inhibitors, mikanolide and dihydromikanolide
AssigneeSociete de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
InventorsPoon Beng Teng, Marie-Christine Brezak Pannetier, Mohamed Moumen, Gregoire Prevost
Life of this patent
Estimating the term…
Abstract
The invention concerns DNA polymerase inhibitors, namely mikanolide and dihydromikanolide and dihydromikanotide-enriched extracts. Said compounds or mixtures can be used for preparing medicines designed to treat proliferative diseases, in particular cancer, viral diseases or parasitic diseases provoked by protozoae (for example malaria) or protists (for example, diseases caused by amoebae).
Claims11
Process for obtaining a dry extract of Mikania micrantha, Mikania scandens and Mikania cordata leaves, comprising at least 50% by weight of mikanolide and dihydromikanolide and at least 20% dihydromikanolide, the said process being characterised in that it comprises the following successive stages:
- grinding and drying Mikania micrantha, Mikania scandens and Mikania cordata leaves;
- addition, to the ground leaves of Mikania micrantha, Mikania scandens and Mikania cordata leaves, of a solvent chosen from toluene, ethyl acetate, toluene and ethyl acetate mixtures, toluene and acetone mixtures, ethyl acetate and heptane mixtures, and heptane and acetone of the mixtures in proportions of 7:3 to 3:7;
- filtration and recovery of the filtrate;
- concentration of the extract of the primary extract solution in order to obtain a concentration of 2.5 to 10% dry extract;
- dividing of the concentrated extract obtained in the preceding stage between the extraction solvent and a mixture comprising from 10% to 50% methanol or ethanol in water;
- washing of the alcohol-water phase with n-hexane or heptane;
- elimination of the alcohol of the alcohol-water phase;
- extraction of the aqueous phase obtained with ethyl acetate;
- drying of the ethyl acetate phase with a drying agent;
- evaporation of the solvents and recovery of the dry extract;
- purification of the dry extract obtained by a physico-chemical separation method;
- and
- obtaining, after elimination of the solvents, the desired extract.
Process for the preparation, from a dry extract of Mikania micrantha, Mikania scandens and Mikania cordata leaves comprising at least 50% by weight of mikanolide and dihydromikanolide and at least 20% dihydromikanolide, of a dihydromikanolide-enriched extract, characterized in that it consists of the hydrogenation of said extract, dissolved in ethyl acetate, at a temperature comprised between 10 and 35° C., in the presence of a hydrogenation catalyst under a pressure of 1 to 2 hydrogen atmospheres.
Dependencies are inferred from the claim text.