1,3-oleic acid-2-linoleic acid glyceride, preparation, preparation method and applications thereof

A kind of linoleic acid glyceride, compound technology, application in antitumor drug application, preparation, compound 1,3-dioleic acid-2-linoleic acid glyceride, preparation field

Active Publication Date: 2016-01-20
ZHEJIANG KANGLAITE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The present invention separates one of the triglyceride components of coix seed oil - linoleic acid diolein, and prepares a compound with the structure of formula (I), that is, 1,3-dioleic acid for the first time -2-Glyceryl linoleate, there is no report about this compound and its pharmaceutical preparations for the treatment of tumors

Method used

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  • 1,3-oleic acid-2-linoleic acid glyceride, preparation, preparation method and applications thereof
  • 1,3-oleic acid-2-linoleic acid glyceride, preparation, preparation method and applications thereof
  • 1,3-oleic acid-2-linoleic acid glyceride, preparation, preparation method and applications thereof

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Embodiment 1

[0123] The preparation of embodiment 1 coix seed oil

[0124] Take 1000g of coix seed with moisture ≤10% and crush it into 10 meshes, extract with supercritical carbon dioxide, extract at 40°C, extract at 20Mpa, separate at 30°C, separate at 6Mpa, flow at 50L / h of carbon dioxide, and extract continuously for 2 hours to obtain coix seed crude oil; add 40% petroleum ether by weight of coix seed crude oil and 0.5% potassium hydroxide aqueous alkali refining; take the organic phase after liquid separation, first add activated neutral alumina with 3% oil weight to filter, and the filtrate Heating to 40°C, adding 2% oil weight, activated kaolin, filtering, removing the solvent under reduced pressure, then adding 8% oil weight activated neutral alumina, filtering, sterilizing under reduced pressure and dry heat at 180°C, cooling and filtering to obtain coix coix kernel oil;

Embodiment 2

[0125] The preparation of embodiment 2 coix seed oil

[0126] Take 1000g of coix seed with water content ≤10% and grind it into 100 mesh, extract with supercritical carbon dioxide, extraction temperature is 50°C, extraction pressure is 22Mpa, separation temperature is 40°C, separation pressure is 8Mpa, carbon dioxide flow rate is 500L / h, continuous extraction is 3h, and the separation is obtained coix seed crude oil; adding 46% petroleum ether by weight of coix seed crude oil and 1% sodium hydroxide aqueous alkali refining; after liquid separation, take the organic phase, first add 5% activated neutral alumina to filter the oil, and the filtrate Heating to 50°C, adding 4% oil weight, activated kaolin, filtering, removing solvent under reduced pressure, then adding 10% oil weight activated neutral alumina, filtering, sterilizing under reduced pressure and dry heat at 150°C, cooling and filtering to obtain coix kernel oil;

Embodiment 3

[0127] The preparation of embodiment 3 coix seed oil

[0128] Take 1000g of coix seed with water content ≤10% and crush it into 200 meshes, extract with supercritical carbon dioxide, extraction temperature is 60°C, extraction pressure is 24Mpa, separation temperature is 50°C, separation pressure is 10Mpa, carbon dioxide flow rate is 1500L / h, continuous extraction is 1.5h, separation Obtain coix seed crude oil; add 50% petroleum ether by weight of coix seed crude oil, and 2% potassium hydroxide aqueous alkali refining; take the organic phase after liquid separation, first add activated neutral alumina with 6% oil weight to filter , the filtrate was heated to 45°C, and 5% of the oil weight was added to filter through activated kaolin, the solvent was removed under reduced pressure, and then 10% of the oil weight was added to activate neutral alumina, filtered, sterilized under reduced pressure and dry heat at 160°C, cooled and filtered, Coix Seed Oil;

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Abstract

The present invention relates to a compound 1,3-oleic acid-2-linoleic acid glyceride having a structure represented by a formula (I). The present invention further provides a method for preparing the compound by using coix seed powder as a raw material and carrying out coix seed oil preparation, primary 1,3-oleic acid-2-linoleic acid glyceride separation and secondary separation. The present invention further relates to a pharmaceutical preparation containing the 1,3-oleic acid-2-linoleic acid glyceride, and a preparation method thereof, and applications of the compound and the preparation as the antitumor drugs. The formula (I) is defined in the specification.

Description

technical field [0001] The present invention relates to the fields of organic chemistry and pharmacy, in particular, the present invention relates to compound 1,3-dioleic acid-2-linoleic acid glyceride, preparation, preparation method and application in antitumor drugs. Background technique [0002] Coix seed is the mature and dry seed kernel of Coixlacryma-jobi L.varma-yuen (Roman.) Stapf, a plant of the genus Coix in the Poaceae family. Modern studies have found that coix seed has pharmacological effects such as analgesia, anti-inflammation, immune regulation, anti-ulcer, lowering blood fat and weight loss. In recent years, scholars at home and abroad have studied the chemical components of coix seed by TLC, HPLC-MS, GC and other methods, and found that its main active components include esters, unsaturated fatty acids, sugars and lactams. Among them, esters are the first discovered components with anti-tumor activity, and they are also the most reported and most concerne...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/587C07C67/48A61K31/231A61K9/08A61K9/48A61P35/00
CPCA61K9/0019A61K9/0053A61K9/10A61K9/4833A61K9/4858A61K31/231A61K47/44A61P35/00B01D15/08B01D15/22B01D15/426C11B1/104C11B3/06C11B3/10
Inventor 李大鹏
Owner ZHEJIANG KANGLAITE PHARM CO LTD
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