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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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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] 25Rmdt and 25Smdt and their mixture (racemate) are derivatives of PPD, so far no reports of these two compounds and their mixture and their preparation methods have been found

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0024] Embodiment: Sodium hydroxide hydrolysis method prepares 25Rmdt and 25Smdt and their mixture (racemate)

[0025] Weigh 10g of Panax notoginseng total saponins, dissolve in 1000ml of methanol aqueous solution with a concentration of 2.5mol / L and 80% sodium hydroxide, and heat to reflux for hydrolysis for 24 hours, 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 over anhydrous sodium sulfate, evaporated to dryness to collect the residue, separated by silica gel column chromatography, petroleum ether: ethyl acetate (10:1-1:1) gradient elution to obtain 86 fractions, fractions 52-55 were recrystallized from ethyl acetate to obtain 25Rmdt; fractions 56-58 were combined after TLC inspection, and after removing the solvent, ethyl acetate recrystallized to obtain a mixture of 25Rmdt and 25Smdt (race Spin body); Fra...

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PUM

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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.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a preparation method of a pair of nonoginsan triol saponins and a mixture thereof. The pair of compounds are named 20(R)-25-methoxy-dammarane-3β,12β,20-triol and 20(S)-25-methoxy-dammarane-3β,12β,20- Triol [20(R)-25-methoxyl-dammarane-3β, 12β, 20-triol (25Rmdt for short) and 20(S)-25-me-thoxyl-dammarane-3β, 12β, 20-triol (25Smdt for short) ]. 25Rmdt and 25Smdt and their mixtures (racemate) have significant anti-tumor effects, and can be made into any medicinal and health product dosage forms for different cancer treatments. They are mainly used in the prevention and treatment of malignant tumors and have broad application prospects. Background technique [0002] Studies by many scholars have shown that notoginseng saponins have obvious anti-tumor and immune regulation effects, improve microcirculation, and improve the quality of life and other biological activities. However, b...

Claims

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Application Information

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IPC IPC(8): C07J9/00A61K31/575A61P35/00
Inventor 程淑清牛清玲
Owner 陕西雅卓至尚企业管理咨询有限公司
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