Pair of panaxtriol saponins and preparation method of mixture of pair of panaxtriol saponins

A technology of triol saponins and mixtures, applied in the field of medicine, can solve problems such as undiscovered preparation methods and the like

Inactive Publication Date: 2019-05-21

陕西雅卓至尚企业管理咨询有限公司

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AI-Extracted Technical Summary

Problems solved by technology

[0003] 25Rmdt and 25Smdt and their mixture (racemate) are derivatives of PPD, so far no rep...

Abstract

The invention belongs to the technical field of medicine and relates to a pair of panaxtriol saponins and a preparation method of a mixture of the pair of panaxtriol saponins. The names of a pair of compounds are 20(R)-25-methoxyl-dammarane-3beta,12beta,20-triol (25 Rmdt for short) and 20(S)-25-me-thoxyl-dammarane-3beta,12beta,20-triol (25 Smdt for short). The compounds involved in the invention can be prepared by an acid hydrolyzing method, an alkaline hydrolyzing method and a synthesizing method; and the preparation method is simple and feasible. The 25 Rmdt, the 25 Smdt and the mixture (racemate) of the 25 Rmdt and the 25 Smdt can be prepared into varieties of clinically feasible dosage forms together with pharmaceutically acceptable carriers; it is proved, by researches, that the compounds and preparations of the compounds have an obvious antitumor effect, the compounds can be prepared into any medicinal and health care product dosage form for treating different cancers, and the compounds are mainly applied to prevention and treatment of malignant tumors and have a wide application prospect.

Application Domain

Organic active ingredientsSteroids +1

Technology Topic

ChemistryDosage form +3

Examples

Experimental program(1)

Example Embodiment

[0024] Example: Preparation of 25Rmdt and 25Smdt and their mixture (racemate) by sodium hydroxide hydrolysis

[0025] Weigh 10g of panax notoginseng fruit saponins and dissolve them in 1000ml of methanol aqueous solution with a sodium hydroxide concentration of 2.5mol/L and a concentration of 80% for hydrolysis under heating and reflux for 24h, neutralize the reaction solution with 2.5mol/L hydrochloric acid, and recover methanol under reduced pressure , The reaction solution was extracted with chloroform, the chloroform phase was washed with water, dried with anhydrous sodium sulfate, evaporated to dryness to collect the residue, separated by silica gel column chromatography, petroleum ether: ethyl acetate (10:1 to 1:1) gradient elution 86 fractions, fractions 52-55 were recrystallized with ethyl acetate to obtain 25Rmdt; fractions 56-58 were checked by TLC and combined, and the solvent was removed and ethyl acetate was recrystallized to obtain a mixture of 25Rmdt and 25Smdt. Rotation); Fractions 59-62 were checked by TLC and then combined, and 25Smdt was obtained after ethyl acetate recrystallization.

PUM

Description & Claims & Application Information

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