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Yarrow sesquiterpene lactone compound as well as extraction method and application of compound

A technology for sesquiterpene lactones and extraction methods, which is applied in the field of sesquiterpene lactone compounds and their extraction and application in Yarrow, and can solve the problems of insufficient research on sesquiterpene lactone compounds

Inactive Publication Date: 2013-01-02
HEBEI MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, the research on sesquiterpene lactones in yarrow is not enough, and other compounds with potential medicinal value in yarrow have yet to be developed

Method used

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  • Yarrow sesquiterpene lactone compound as well as extraction method and application of compound
  • Yarrow sesquiterpene lactone compound as well as extraction method and application of compound
  • Yarrow sesquiterpene lactone compound as well as extraction method and application of compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] The yarrow-derived sesquiterpene lactone compound of the present invention was prepared as follows.

[0033] a. Take 4.2 kg of flowers of yarrow, a compositae plant, soak in 16L of methanol at 20-23°C for 8-16 hours, filter, distill under reduced pressure to remove methanol in the filtrate, and dissolve the obtained extract in saturated chlorinated Sodium aqueous solution, extracted 3 times with water-saturated n-hexane, combined the water layers, extracted 3 times with water-saturated ethyl acetate, combined the ethyl acetate layers, dehydrated with anhydrous sodium sulfate, recovered ethyl acetate by distillation under reduced pressure, and obtained 149g of extract ;

[0034] b. The extract described in step a is separated by silica gel dry column chromatography, and eluted with ethyl acetate-methanol with a volume ratio of 95:5, then the silica gel column is divided into 15 sections, and the 7th to 11th sections Combined to obtain 59g of sesquiterpene-rich fractions...

Embodiment 2

[0038] a. Take 4.3 kg of flowers of yarrow, a compositae plant, soak them in 16L of methanol at 20~23°C for 16~24 hours, filter, distill under reduced pressure to remove methanol in the filtrate, and dissolve the obtained extract in saturated chlorinated Sodium aqueous solution, extracted twice with water-saturated n-hexane, combined the water layers, extracted twice with water-saturated ethyl acetate, combined the ethyl acetate layers, dehydrated with anhydrous sodium sulfate, recovered ethyl acetate by distillation under reduced pressure, and obtained 121g of extract ;

[0039] b. The extract described in step a is separated by silica gel dry column chromatography, and eluted with ethyl acetate-methanol with a volume ratio of 95:5, then the silica gel column is divided into 15 sections, and the 7th to 11th sections Combined to obtain 52g of sesquiterpene-rich fractions;

[0040] c. Carry out gradient elution with the cyclohexane-ethyl acetate described in step b with a volu...

Embodiment 3

[0043] The antitumor activity of Achillinin B and Achillinin C obtained in Example 1 was determined.

[0044] The selected cell lines are HeLa (human cervical cancer cells); HOC-21 (human ovarian clear carcinoma cells); HEC-1 (human endometrial cancer cells); T-98 and U251SP (human brain glioma cells ); A549 and QG-56 (human lung cancer cells); HLE (human liver cancer cells); MM1-CB and HMV-1 (human melanoma cells); KT (human breast cancer brain metastasis cells).

[0045] The experimental method used is the MTT experimental method.

[0046] Inoculate the above-mentioned suspensions of each tumor cell line into a 96-well plate, 90 μL per well (containing 1×10 4 cells), the compounds of the present invention, Achillinin B and Achillinin C, were dissolved in DMSO, and 10 μL of each of Achillinin B and Achillinin C at a final concentration of 100 μM were added respectively, and three replicate wells were set up in each group. Placed in saturated humidity, 37°C and 5% CO 2 Incu...

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Abstract

The invention discloses a yarrow sesquiterpene lactone compound as well as an extraction method and application of the compound. The compound is Achillinin B or Achillinin C according to the different substituent groups. The compound is obtained by sequentially carrying out leaching, extracting, silica gel dry column chromatography, thin layer chromatography and high-performance liquid chromatography separation on the flowers of yarrow. The human tumor cell lines in vitro experiment proves that the yarrow sesquiterpene lactone compound has antineoplastic activity and is high in activity for cervical cancer, lung cancer, liver cancer, brain glioma or melanoma, thus the yarrow sesquiterpene lactone compound can be used for preparing antineoplastic medicaments.

Description

technical field [0001] The present invention relates to a compound and its preparation method and its medical use, in particular to a sesquiterpene lactone compound, its preparation method and its application in the preparation of antitumor drugs. Background technique [0002] Yarrow Achillea LIpina The aboveground part of L is also called a wormwood, centipede grass, and flying centipede. Common chemical constituents in yarrow include succinic acid, fumaric acid, alpha-furoic acid, and aconitic acid, which can be used to reduce swelling, stop bleeding, and relieve pain. With the advancement of science and technology, it is of great practical significance to study, screen and extract more pharmacologically active ingredients in Yarrow. [0003] Chinese patent application CN101037428A discloses a yarrow sesquiterpene lactone compound and its purification method and anti-tumor cell proliferation activity. The structure of the compound described in the application is as follo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/10A61P35/00
Inventor 史清文张嫚丽董玫李勇
Owner HEBEI MEDICAL UNIVERSITY