Method of producing incisterol

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to production of sterol derivatives, and can be used in producing 4-hydroxy-17R-methylincisterol from ergosterol by photoisomeration. When carrying out the method, a weighed portion of ergosterol is dissolved in a weakly polar solvent while illuminating the solution with optical radiation in the near UV range. The obtained solution is chromatographically separated. The fraction which is cytotoxic for HeLa line of cancer cells and human myeloid leukaemia cells is sorbed. The pH is raised to neutral value and the solution is evaporated until a milky appearance is achieved. The weakly polar solvent is added and extracted, and the organic layer is separated on separating funnel. The organic layer is evaporated and dissolved. The obtained solution is separated by analytical HPLC with subsequent purification and separation of incisterol.

EFFECT: invention enables to obtain a 4-hydroxy-17R-methylincisterol preparation by chemical synthesis.

10 cl

 

The invention relates to the field of organic chemistry, namely the field of production of Sterol derivatives, and can be used to obtain 4-hydroxy-17R-methylincisterol of ergosterol using photoisomerization.

Known (RU, patent 2435599) method of preparation of the drug, influencing tissue metabolism, including deep cultivation of the fungus Pleurotus 1137 (VKPM F-819), followed by the separation of the mycelium from the culture fluid and the release of the mycelium extraction with ethanol at acidic pH environment of low molecular weight from 100 to 500 daltons biologically active substances, followed by separation of them dichloromethane derived Sterol 4-hydroxy-17R-methylincisterol with a defined molecular weight 332,2452 and gross formula C21H32O3.

The disadvantage of this method should recognize the complexity of the selection of the target product from the culture fluid of cultivation of the fungus Pleurotus 1137 (VKPM F-819).

During the patent information search is not a dedicated source of information that could be used as the nearest equivalent.

The technical problem to be solved in the course of the present work is to develop a method for the synthesis of drug ancesteral (4-hydroxy-17R-methylincisterol).

The technical result obtained by the implementation of the developed method consists in keeping the floor of the texts of the drug 4-hydroxy-17R-methylincisterol method of chemical synthesis.

To achieve the technical result it is proposed to use a method of chemical synthesis of the drug 4-hydroxy-17R-methylincisterol. According to the developed method dissolve a portion of ergosterol in slightly polar solvent in the lighting solution of the optical radiation in the near UV range, the resulting solution was separated chromatographically, collecting the fraction with cytotoxicity to cancer cell lines HeLa cells and myeloid leukemia person, bring the pH to neutral values and evaporated until opalescence of the solution, the remaining solution is added polar solvent, extracted and the organic layer is separated in a separating funnel, the organic layer evaporated and dissolved, the resulting solution was separated using analytical HPLC, followed by purification and isolation of ancesteral (4-hydroxy-17R-methylincisterol).

Preferably the solution illuminate the optical radiation with a wavelength of 210-350 nm when the optical power of 250 Watts.

In most variants of the method as a solvent of ergosterol using methylene chloride, chloroform, methanol, ethanol. However, the above list does not exhaust the possible choices of solvent.

Preferably a portion of ergosterol dissolve in polar RA is the solvent and irradiated middle UV with wavelength with constant stirring on a magnetic stirrer or prorokowanie air at a temperature of 6-8°C for 5-10 hours, followed by evaporation of the solution on a rotary evaporator without heating and dissolving the obtained residue in 96% ethanol.

In some embodiments of the chromatographic separation of irradiated solution of ergosterol spend on prepreparation HPLC system Gilson, consisting of 2 pumps with heads 25SC, manometric module, mixer, injector with a loop 500 ál, column thermostat and flow divider (1:10), UV detector with variable wavelength and daemon.

Usually for continuation of the synthesis of the selected fraction with cytotoxicity to cancer cell lines HeLa cells and myeloid leukemia person, expressed in the induction of apoptosis at concentrations of 1-100 µg/ml incubation medium.

In some embodiments of the process of evaporation of selected fractions with neutral pH spend on a rotary evaporator at a temperature of 45-55°C to 2/3 of the volume.

In most variants of realization of the developed method the organic layer after separating funnel evaporated on a rotary evaporator without heating and the residue is dissolved in 96% ethanol.

Preferably the resulting solution of ancesteral share using analytical HPLC on a system Agalint 1100, consisting of four channel pump with degasser, a column thermostat, autosampler, diode matrix UV detector and a control program ChemStstion.

In most cases re the implementation at the stage of extraction and purification of fraction, containing ancesteral, collected and evaporated on a rotary evaporator at a temperature of 45-55°C to 2/3 volume until opalescence of the solution, the remaining solution was added volume of methylene chloride, extracted and the organic layer is separated in a separating funnel, the organic layer evaporated on a rotary evaporator without heating, followed dissolved in methylene chloride and dried in a desiccator.

In practice, the method is implemented as follows.

1 g of ergosterol dissolved in 100 ml methylene chloride or chloroform or ethanol) and irradiated with UV light with a wavelength of 210-350 nm with constant stirring on a magnetic stirrer, or prorokowanie air at a temperature of 6-8°C for 5-10 hours. Then the solution is evaporated on a rotary evaporator without heating. The residue is dissolved in 96% ethanol at a concentration of 100 mg/ml

The resulting solution (aliquots (400 µl) was separated chromatographically on prepreparation HPLC system Gilson, consisting of 2 pumps with heads 25SC, manometric module, mixer, injector with a loop 500 ál, column thermostat and a separating flow (1:10), UV detector with variable wavelength and the control program. Used prepreparation column 24×250 mm with a sorbent of diasorb ST (10 μm). The composition of the mobile phase: 96% ethanol: 0.1% TFU in water / 60:40, at a flow rate of 10 the l/min and a temperature of 30°C. You can use the same chromatographic system and similar reversed-phase column. The analysis time 40 min, detection at a wavelength of 230 nm, interest peak has a retention time of 20-25 minutes

The fraction containing the peak of interest, collect, add 305 ammonia solution until a neutral pH of 6-8 and evaporated on a rotary evaporator at a temperature of 45-55°C to 2/3 volume until opalescence of the solution. To the remaining solution add an equal volume of methylene chloride, extracted and the organic layer is separated in a separating funnel. The organic layer evaporated on a rotary evaporator without heating and dissolved in 1 ml of 96% ethanol. The resulting solution (aliquot 100 ál) separated by analytical HPLC system Agalint 1100, consisting of four channel pump with degasser, a column thermostat, autosampler, diode matrix UV detector and a control program ChemStstion. Was used analytical column, 4.6×250 mm with a sorbent Luna C18(2) (5 μm). You can use the same chromatographic system and similar reversed-phase column.

The composition of the mobile phase: acetonitrile: water / 79:21, at a flow rate of 1 ml/min and a temperature of 25°C. analysis Time - 21 min, detection at a wavelength of 230 nm, the peak of interest is the retention time of 15-18 minutes Faction, with whom containing a series of interesting peak, collected and evaporated on a rotary evaporator at a temperature of 45-55°C to 2/3 volume until opalescence of the solution. To the remaining solution add an equal volume of methylene chloride. Extracted and the organic layer is separated in a separating funnel. The organic layer evaporated on a rotary evaporator without heating. Dissolved in 1 ml methylene chloride and dried in the desiccator. The output is 1-2 mg ancesteral.

1. The method of producing ancesteral, characterized by the fact that dissolved a portion of ergosterol in slightly polar solvent in the lighting solution of the optical radiation in the near UV range, the resulting solution was separated chromatographically, collecting the fraction with cytotoxicity to cancer cell lines HeLa cells and myeloid leukemia person, bring the pH to neutral values and evaporated until opalescence of the solution, the remaining solution is added polar solvent, extracted and the organic layer is separated in a separating funnel, the organic layer evaporated and dissolved, the resulting solution was separated using analytical HPLC, followed by purification and isolation of ancesteral.

2. The method according to claim 1, characterized in that the solution illuminate the optical radiation with a wavelength of 210-350 nm.

3. The method according to claim 1, characterized in that as the e of the solvent used methylene chloride, chloroform, methanol, ethanol.

4. The method according to claim 1, characterized in that a portion of ergosterol dissolved in a polar solvent and irradiated middle UV with wavelength with constant stirring on a magnetic stirrer or prorokowanie air at a temperature of 6-8°C for 5-10 h followed by evaporation of the solution on a rotary evaporator without heating and dissolving the obtained residue in 96% ethanol.

5. The method according to claim 1, characterized in that the chromatographic separation of a solution of ergosterol spend on prepreparation HPLC system Gilson, consisting of 2 pumps with heads 25SC, manometric module, mixer, injector with a loop 500 ál, column thermostat and a separating flow (1:10), UV detector with variable wavelength and daemon.

6. The method according to claim 1, wherein the selected fraction with cytotoxicity to cancer cell lines HeLa cells and myeloid leukemia person, expressed in the induction of apoptosis at concentrations of 1-100 µg/ml incubation medium.

7. The method according to claim 1, characterized in that the evaporation fraction with a neutral pH spend on a rotary evaporator at a temperature of 45-55°C to 2/3 of the volume.

8. The method according to claim 1, characterized in that the organic layer evaporated on a rotary evaporator without heating and the residue is dissolved in 96% ethanol.

9. Spasibo to claim 1, characterized in that the obtained solution ancesteral share using analytical HPLC on a system Agalint 1100, consisting of four channel pump with degasser, a column thermostat, autosampler, diode matrix UV detector and a control program ChemStstion.

10. The method according to claim 1, characterized in that at the stage of extraction and purification of the fraction containing ancesteral, collected and evaporated on a rotary evaporator at a temperature of 45-55°C to 2/3 volume until opalescence of the solution, the remaining solution was added volume of methylene chloride, extracted and the organic layer is separated in a separating funnel, the organic layer evaporated on a rotary evaporator without heating, followed by dissolving in methylene chloride and dried in a desiccator.



 

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