Method for preparation of 6'-malonyl formyl ginsenoside F1

Abstract

The invention discloses a method for preparation of 6'-malonyl formyl ginsenoside F1, including: step 1: smashing ginseng flower bud, using 95% ethyl alcohol to extract by hot reflux, obtaining totalextractive in paste by concentration; step 2: dissolving the total extractive with 25% ethyl alcohol and regulating the concentration to be 0.2 g crude drug / ml, filtering, loading quantity of sample is 0.8 BV, column bed diameter height ratio of LX-68 large hole absorption resin column is 1:9, using 40% ethyl alcohol of 3 BV to remove impurities first, then using 75% ethyl alcohol of 9 BV to elute, collecting eluent of 75% ethyl alcohol eluent of 8-9 BV, decompressing and concentrating until no alcohol exists, then performing freeze-drying to obtain crude lyophilized powder; step 3: performinghigh-speed countercurrent separation: the solvent system is n-butyl alcohol / ethyl acetate / methanol / water / chloroform with a volume ratio of 1:18:1:18:0.5, collecting elution flow components corresponding to 6'-malonyl formyl ginsenoside F1, obtaining 6'-malonyl formyl ginsenoside F1 after concentration.

Description

Technical field [0001] The invention belongs to the field of chemistry, and specifically relates to a method for preparing ginsenoside F1 derivatives. The ginsenoside F1 derivatives include 3-acetyl ginsenoside F1, 6'-acetyl ginsenoside F1 and 6'-malonyl formyl Ginsenoside F1. Background technique [0002] Previous studies have found that 3-acetyl ginsenoside F1, 6'-acetyl ginsenoside F1, and 6'-malonylformyl ginsenoside F1 have excellent tyrosinase inhibitory activity and can be used to prepare whitening cosmetics. From the chemical structure point of view, 3-acetyl ginsenoside F1, 6'-acetyl ginsenoside F1, 6'-malonyl formyl ginsenoside F1 are derivatives of ginsenoside F1, but ginsenoside F1 has an effect on tyrosine The inhibitory activity of the enzyme is extremely weak, far inferior to its derivatives. [0003] At present, the separation and preparation of 3-acetyl ginsenoside F1, 6'-acetyl ginsenoside F1, and 6'-malonylformyl ginsenoside F1 must rely on repeated silica gel ...

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Problems solved by technology

From the chemical structure point of view, 3-acetyl ginsenoside F1, 6'-acetyl ginsenoside F1, and 6'-malonylformyl ginsenoside F1 are derivatives of ginsenoside F1, but ginsenoside F1 is a derivative of tyrosine Enzyme inhibitory activity is extremely weak, far inferior to its derivatives

[0003] At present, the separation and preparation of 3-acetyl ginsenoside F1, 6'-acetyl ginsenoside F1, and 6'-malonylformyl ginsenoside F1 must rely on repeated silica gel column chromatography, however, repeated silica gel column chromatography dead adsorption Strong, large loss, not suitable for large-scale preparation at all

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