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Sesquiterpene lactone compound, pharmaceutical composition comprising sesquiterpene lactone compound, as well as preparation method and application of sesquiterpene lactone compound

A technology of sesquiterpene lactone and compound, applied in the field of medicine, can solve problems such as no compound activity report, no literature report and the like

Inactive Publication Date: 2015-04-29
齐思超
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the process of studying the chemical components of the ethyl acetate extract of Inula inula, the inventors isolated and obtained new sesquiterpene lactone compounds 1 and 2, which have not been reported in the literature at present, let alone the activity reports of these two compounds

Method used

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  • Sesquiterpene lactone compound, pharmaceutical composition comprising sesquiterpene lactone compound, as well as preparation method and application of sesquiterpene lactone compound
  • Sesquiterpene lactone compound, pharmaceutical composition comprising sesquiterpene lactone compound, as well as preparation method and application of sesquiterpene lactone compound
  • Sesquiterpene lactone compound, pharmaceutical composition comprising sesquiterpene lactone compound, as well as preparation method and application of sesquiterpene lactone compound

Examples

Experimental program
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Effect test

Embodiment 1

[0021] Inula multibranches (5kg) were crushed and soaked in 95% ethanol (3×15L) at room temperature for 24 hours, filtered, combined extracts, and recovered under reduced pressure to obtain a crude extract, suspended evenly with water, extracted with ethyl acetate 3 times to get ethyl acetate extract (385mg), the extract was decolorized by MCI and eluted with 95% ethanol, then used a silica gel column 10:0→1:1 chloroform-acetone gradient elution for crude fractionation, combined the same fractions , to get 6 parts F1-F6; F1 was purified by Sephadex LH-20 column chromatography chloroform:methanol=1:1 and then eluted by methanol-water gradient of RP-18 column chromatography 25:75→100:0 to obtain 5 small parts F1a -F1e, F1d was purified by silica gel column chloroform:ethyl acetate=5:1 and then eluted by HPLC methanol:water gradient 80:20 and 92:8 to obtain compounds 1 (21mg) and 2 (20mg);

[0022] Compound 1 structure confirmed: light yellow powder; HR-ESIMS showed [M+H] + It i...

Embodiment 2

[0029] Inula cotton wool (5kg) was crushed, soaked in 95% ethanol (3×15L) at room temperature for 24 hours, filtered, combined extracts, recovered ethanol under reduced pressure to obtain a crude extract, added water to suspend evenly, and extracted with ethyl acetate for 3 times, to obtain ethyl acetate extract (322mg), the extract was decolorized by MCI and eluted with 95% ethanol, then used a silica gel column 10:0 → 1:1 chloroform-acetone gradient elution for crude fractionation, and the same fractions were combined, 6 parts F1-F6 were obtained; F1 was purified by Sephadex LH-20 column chromatography chloroform:methanol=1:1 and then eluted by methanol-water gradient of RP-18 column chromatography 25:75→100:0 to obtain 5 small parts F1a- F1e and F1d were purified by silica gel column chloroform:ethyl acetate=5:1 and then eluted by HPLC methanol:water gradient 80:20 and 92:8 to obtain compounds 1 (17mg) and 2 (26mg).

[0030] See Example 1 for structure confirmation of compo...

Embodiment 3

[0032] Inula angustifolia (5kg) was crushed and soaked in 95% ethanol (3×15L) at room temperature for 24 hours, filtered, combined extracts, and recovered under reduced pressure to obtain a crude extract. Extracted 3 times to obtain ethyl acetate extract (350g), the extract was eluted with different concentrations of MCI methanol-water gradient, the elution gradient was 20%, 40%, 60%, 80%, 100%, and the same fractions were combined , get 5 parts F1-F5; Get F4 and obtain 4 small parts F4a-F4d through the chloroform-ethyl acetate gradient elution of silica gel column 9:1→3:2, get F4c through Sephadex LH-20 column chromatography chloroform:methanol= After 1:1 purification, compound 1 (19 mg) was semi-prepared by HPLC methanol:water=82:18; F5 was eluted with a gradient of petroleum ether-ethyl acetate on a silica gel column 9:1→2:3 to obtain 3 small parts of F5a -F5c, compound 2 (22 mg) was prepared by taking F5a and semi-preparing it by HPLC methanol:water=94:6;

[0033] The str...

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Abstract

The invention relates to a sesquiterpene lactone compound, a pharmaceutical composition comprising the sesquiterpene lactone compound, a preparation method and the application of the sesquiterpene lactone compound, new sesquiterpene lactone 1 and new sesquiterpene lactone 2 separated from Inula Britannica, the preparation method for the new sesquiterpene lactone 1 and new sesquiterpene lactone 2, and the application of the new sesquiterpene lactone 1 and new sesquiterpene lactone 2 in preparation of an anti-tumor medicament. In-vitro anti-tumor activity screening shows that the compound disclosed by the invention has obvious activity on inhibiting the proliferation of tumor cells, can be made into clinically acceptable medicinal agents by combining with pharmaceutically acceptable carriers, and is used for treating cancer. The invention provides a lead compound for developing a new antitumor medicament, and has an important value on developing the resources of medicinal plants.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to sesquiterpene lactone compounds 1 and 2 separated from Inula inula, a pharmaceutical composition containing them, a preparation method and a medical application thereof. Background technique [0002] Tumor is a common and frequently-occurring disease, among which malignant tumor is the most serious disease that endangers human health. Chemotherapy drugs also produce toxic and side effects on normal human cells while killing cancer cells, which greatly limits its wide application and curative effect. Researchers are paying more and more attention to the active ingredients in natural plants, including vinblastine, camptothecin (camptothecin, hydroxycamptothecin), and elemene that have been successfully extracted from plants in my country; Kanglaite, polyporus polysaccharide, xianling polysaccharide, astragalus polysaccharide and ginsenoside extracted from coix seed; ac...

Claims

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Application Information

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IPC IPC(8): C07D307/83A61K31/365A61P35/00
CPCC07D307/83
Inventor 李程伟
Owner 齐思超
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