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Application of diterpene ginkgolide

A diterpene lactone and compound technology, applied in the field of diterpene lactone compounds, can solve the problems of the JAK-STAT signaling pathway of Euphorbia chamaejasma extract that has not been reported in the literature

Active Publication Date: 2014-07-09
XIANGBEI WELMAN PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Therefore, so far, no literature has reported that the extract of Euphorbia chamaejasma has the effect of inhibiting the JAK-STAT signaling pathway

Method used

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  • Application of diterpene ginkgolide
  • Application of diterpene ginkgolide
  • Application of diterpene ginkgolide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0086] Embodiment 1 compound preparation

[0087] Extraction and separation of Euphorbia chamaejasme:

[0088] 10Kg root of Euphorbia fishceriana Steud. purchased from Shanghai Xujiahui Traditional Chinese Medicine Decoction Pieces Factory was extracted three times (50L×3) with 95% industrial alcohol at room temperature, the extracts were combined, concentrated under reduced pressure to remove the solvent to obtain ethanol extract. Disperse the ethanol extract in hot water and extract with petroleum ether (5L×3) and chloroform (5L×3) respectively to obtain 300g of petroleum ether extract and 883g of chloroform extract. For the chloroform part, the normal phase silica gel column [elution system is petroleum ether-acetone, petroleum ether-ethyl acetate, cyclohexane-acetone], gel column LH-20 [elution system chloroform-methanol=5:1] and Reverse-phase silica gel column (Rp-18) [elution system is methanol-water] for separation, crude crystals were purified by crystallization metho...

Embodiment 217

[0092] Example 217-hydroxy-jolkinolide B inhibits STAT3 signaling pathway

[0093] Experimental Materials:

[0094] 1) Cell line: HepG2 cells stably transfected with STAT3-luciferase reporter gene plasmid.

[0095] 2) IL-6 (purchased from Peprotech Asia)

[0096] 3) Drug to be tested: 17-hydroxy-jolkinolide B, prepared in Example 1;

[0097] 4) Luciferase detection kit (purchased from Promega)

[0098] experimental method:

[0099] 1) HepG2 cells in good growth state, digested with trypsin, resuspended the cells in αMEM medium and adjusted the cell concentration to 2×105 / ml, took 100 μl of the cell suspension and seeded it in a 96-well plate, and incubated at 37°C, 5% CO2 Cultivate in the incubator for 48 hours until the cells are completely attached to the wall;

[0100] 2) When the cells grow to a density of 60-70%, they are randomly divided into the following 3 groups:

[0101] a. Negative control group, without IL-6 and test drug;

[0102] b. IL-6 group, add IL-6 to...

Embodiment 3

[0112] Inhibitory effect on the growth of various tumor cells in the in vitro test of embodiment 3

[0113] In vitro culture of human embryonic kidney cancer 293 cells, human liver cancer HepG2 cells, human breast cancer MDA-MB-468, MDA-MB-231, MDA-MB-453, MCF-7 cells, human gastric cancer HGC cells, human lymphoma U937 cells , Human cervical cancer Hela cells. After the cells grow to the logarithmic growth phase, digest the cells with trypsin, centrifuge at 1000rpm for 5 minutes, discard the supernatant, suspend with an appropriate amount of medium, and adjust the cell concentration to 3.5 104 / ml. The cell suspension was inoculated into a 96-well cell culture plate, 100 μl per well, placed in a cell culture incubator (37° C., 5%) and cultured for 24 hours. Each medication group was added with 17-hydroxy-jolkinolide B diluted in cell culture medium, respectively. 100 μl of 17-hydroxyjolkinolide B, 17-hydroxyjolkinolide B acetic acid ester, and 17-hydroxyjolkinolide Bbenzoic a...

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Abstract

The invention relates to the technical field of medicines, in particular to application of diterpene ginkgolide. The invention discloses the application of diterpene ginkgolide shown as a general structural formula I or pharmaceutically acceptable salts thereof or prodrugs or isomers or plant extracts with the diterpene ginkgolide as a JAK-STAT signal transduction pathway inhibitor. The compound shown as the general structural formula I or pharmaceutically acceptable salts or prodrugs or isomers or plant extracts with the diterpene ginkgolide are used as the JAK-STAT signal transduction pathway inhibitor, have higher particularity, and can effectively inhibit a JAK-STAT signal transduction pathway, and meanwhile, compared with a cyclophosphamide group, the diterpene ginkgolide has low toxicity.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of a diterpene lactone compound. Background technique [0002] Janus kinases (JAKs) belong to the tyrosine kinase family consisting of JAK1, JAK2, JAK3 and TYK2. JAK plays an important role in cytokine signaling, and the downstream substrates of the JAK family of kinases include signal transducers and activators of transcription (STATs). The JAK-STAT signaling pathway is a cell signaling pathway that is closely related to cell growth, proliferation, and differentiation. Its basic process can be summarized as follows: ①Cytokines bind to their corresponding ligands; ③The JH1 domain of JAKs catalyzes the phosphorylation of tyrosine residues on the corresponding parts of STATs, and at the same time, the SH2 functional region of STATs interacts with the phosphorylated tyrosine residues in receptors to activate STATs; ④STATs Enter the nucleus and interact with other ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/365A61P37/02A61P29/00A61P19/08A61P3/00A61P25/00A61P35/00A61P9/00A61P37/08A61P37/06A61P11/06A61P19/02
Inventor 俞强王颖秦国伟王玉波
Owner XIANGBEI WELMAN PHARMA CO LTD
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