New application of hexadecanoyl-sulfonic-glycerol-glucose ester and its preparation method

A technology of hexadecanyl sulfonate glycerol and glucolipid, which is applied in the application field of hexadecanyl sulfonate glycerol glucolipid in the preparation of drugs for the treatment of type II herpes virus infection, which can solve the problems of unsuitable for industrial production and high toxicity. question

Inactive Publication Date: 2008-10-22
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The solvents used for extraction and separation in this method are methanol, n-hexane, tetrachlor

Method used

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  • New application of hexadecanoyl-sulfonic-glycerol-glucose ester and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1, the preparation of hexadecanyl sulfonate glycerol glucolipid

[0032] Take 4 kg of air-dried and chopped Pteridophyta racemophyta of Chlorophyta, Phylophyta, Pteridaceae, and Pteridophyta plants, soak them in 40 kg of 95% ethanol, and heat and reflux for extraction 3 times, each time for 2 hours. The extracts were combined, concentrated and dried to obtain 188 g of crude extract. The ethanol extract was suspended in distilled water, extracted with ethyl acetate (5 times the volume), and then the aqueous phase sample was extracted with n-butanol (5 times the volume), and the samples of different extraction phases were collected for concentration and drying. The n-butanol extract was concentrated and dried to obtain 12.5 g of n-butanol extract. The n-butanol extraction part is separated by 100-200 mesh silica gel column chromatography, and gradient elution is adopted. The elution solvent system is chloroform: methanol (volume concentration), and the volume ...

Embodiment 2

[0038] Example 2, take the air-dried and chopped Pteridophyta racemosa, boil and extract twice with 10 times the amount of water, each time for 2 hours, and repeat 3 times. The extracts were combined, concentrated, and dried to obtain a crude extract. The following separation and purification methods are the same as in Example 1, that is, the crude extract is sequentially extracted with ethyl acetate and n-butanol, concentrated and dried n-butanol extract is obtained from the n-butanol extraction site, and then the n-butanol extraction site is extracted with a silica gel column Separation by chromatography and purification by gel column chromatography to obtain hexadecanyl sulfonate glycerol glucolipid. The yield of hexadecanoyl sulfonate glycerol glucolipid was 0.272mg / g dry algae. This product is amorphous white powder, mp: 197~198℃.

Embodiment 3

[0039] Embodiment 3, the preparation of medicinal preparation

[0040] 1) Ointment: Dissolve 15g of hexadecanyl sulfonate glyceroglucose lipid in 20ml of distilled water and mix evenly, then add 80-100g of base (14 grams of stearic acid, 8 grams of palmitate, 10 grams of propylene glycol, Add 1ml of Tween-20, 1 gram of diethylamine, and add distilled water to 100 grams (specific amount) to form a paste), mix evenly to make hexadecanyl sulfonate glycerol glucolipid ointment, wherein hexadecanyl sulfonate The sulfoglycerol glucolipid content is 15%, administered twice a day, and the actual dosage (hexadecanoyl sulfoglycerol glucolipid usage) is 15 mg / kg each time, continuously administered for 6 days.

[0041] In addition to being made into ointment, the compound can also be made into spray, film, suppository and liquid, and its dose size and service cycle are referred to the ointment.

[0042] 2) Aqueous agent: Dissolve hexadecanyl sulfonate glycerol glucolipid in distilled wa...

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Abstract

New application of 16-carbonyl sulfoacid glycerin glucose ester and a preparation method thereof relate to the new application and the preparation method of a compound. The 16-carbonyl sulfoacid glycerin glucose ester extracted from Caulerpa racemosa can be used for preparing the medicine for treating II type herpesvirus infection, which is in particular suitable for preparing the medicine for treating genital herpes. More particularly, Caulerpa racemosa is used as raw material, from which crude extract is extracted with water or ethanol; the crude extract is sequentially extracted by ethyl acetate and normal butanol; the part extracted with normal butanol is firstly separated by silicagel column and then separated by gel column to obtain the 16-carbonyl sulfoacid glycerin glucose ester. The invention has the advantages that the 16-carbonyl sulfoacid glycerin glucose ester is separated from Caulerpa racemosa for the first time; the compound has excellent activity for in vitro resistance of the II type herpesvirus; the growth characteristics of Caulerpa racemosa have threat towards a plurality of creatures and go against the stability of environment, thus the invention not only can change waste into valuable, but also provide sufficient raw material for industrial production.

Description

technical field [0001] The present invention relates to a new application and preparation method of a compound, in particular to the application of hexadecanyl sulfoglycerol glucolipid obtained by separating and extracting it from Pteris racemosus in the preparation of drugs for treating type II herpes virus infection . Background technique [0002] Glycolipids are compounds in which sugars are linked to lipids through glycosidic bonds, and the lipids are glycerolipids, which are glyceroglycolipids. Sulphonic acid glycerolipids are widely present in plants, including higher plants, mosses, ferns, algae, and most photosynthetic bacteria, especially in algae, which account for 10-70% of their total lipid content %. The structural diversity and special amphiphilicity of sulfoglyceroglycolipids enable them to have a variety of biological activities, including anti-human immunodeficiency virus and influenza virus activity, inhibition of polymerase activity, enhancement of immun...

Claims

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Application Information

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IPC IPC(8): A61K31/7032A61P31/22C07H1/08
Inventor 李药兰王辉沈伟哉岑颖洲
Owner JINAN UNIVERSITY
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