Application of 5-caffeoylquinic acid in preparing anti-tumor drugs

A technology of caffeoylquinic acid and anti-tumor drugs, applied in the field of drug preparation, to achieve the effects of inhibiting the formation of tumor vascular endothelial growth factor, inhibiting the formation of tumor neovascularization, and inhibiting the formation of neovascularization

Inactive Publication Date: 2011-04-06
BIOLOGY INST OF SHANDONG ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] At present, there is no relevant literature report on the antitumor activ

Method used

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  • Application of 5-caffeoylquinic acid in preparing anti-tumor drugs
  • Application of 5-caffeoylquinic acid in preparing anti-tumor drugs
  • Application of 5-caffeoylquinic acid in preparing anti-tumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The preparation method of 5-caffeoylquinic acid is as follows:

[0048] (1) Pulverize the ghost arrow feather, reflux extraction with 10 times the weight of 85% ethanol for 3 times, each time for 2 hours, after filtering the extract, concentrate under reduced pressure to recover the solvent, and obtain the ghost arrow feather aqueous extract;

[0049] (2) after degreasing the water extract of Guijianyu obtained in step (1) with 2 times the weight of sherwood oil, extract 3 times with 2 times the weight of chloroform, then use 2 times the weight of ethyl acetate to extract 3 times, Then extract 3 times with n-butanol of 2 times the weight, and obtain the n-butanol extract after drying under reduced pressure;

[0050] (3) The n-butanol extract prepared in step (2) was separated repeatedly through silica gel column chromatography (column chromatography silica gel, chromatographic column: 10cm×90cm), and was eluted using a chloroform-methanol system gradient to collect the ...

Embodiment 2

[0052] The preparation method of 5-caffeoylquinic acid is as follows:

[0053] (1) After the medicinal material honeysuckle is crushed, use 95% ethanol for the first time, and 50% ethanol aqueous solution for the last two times, the mass ratio is 1:10, adjust the pH of the solution to be 3, extract 3 times at 50 ° C, and combine the extracts , concentrated to no alcohol smell, and the supernatant was extracted.

[0054] (2) After filtering the extraction supernatant obtained in step (1), put the treated polyamide resin in a glass column (400×10mm), slowly add the supernatant from the previous step until the effluent becomes turbid, and then Gradient elution with water, 10%, 20%, 30%, 40% and 50% ethanol aqueous solution (adjust pH to 4.0 with hydrochloric acid), HPLC detection combined chlorogenic acid eluate, concentrated and crystallized in a refrigerator at 0°C. Suction filtration to obtain crude crystals of 5-caffeoylquinic acid;

[0055] (3) the 5-caffeoylquinic acid co...

Embodiment 3

[0057] A kind of antitumor drug containing 5-caffeoylquinic acid, this tumor drug dosage form is conventional tablet, and every hectogram medicine component is as follows:

[0058] 0.5 g of 5-caffeoylquinic acid, 69 g of lactose, 30 g of hydroxypropyl cellulose, and 0.5 g of magnesium stearate.

[0059] After mixing the above components, use 75% ethanol as a binder to make wet granules, sieve, and tablet to make 1000 tablets, each 0.1g, to obtain.

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Abstract

The invention relates to an application of 5-caffeoylquinic acid in preparing anti-tumor drugs, belonging to the technical field of drug preparation. The invention also relates to an anti-tumor drug containing the 5-caffeoylquinic acid, which is prepared from the following components by weight percent: 0.05-99% of 5-caffeoylquinic acid and 1-99.5% of pharmaceutically acceptable carrier. The 5-caffeoylquinic acid has the effect of inhibiting angiogenesis and can inhibit the growth and transfer of tumors by inhibiting tumor angiogenesis, thus realizing the purpose of tumor resistance.

Description

technical field [0001] The invention relates to the application of 5-caffeoylquinic acid in the preparation of antitumor drugs, belonging to the technical field of drug preparation. Background technique [0002] Neovascularization is considered an absolute requirement for the growth of tumors larger than 1-2 mm. In tumors smaller than this limit, oxygen and nutrients can be delivered to the cells by diffusion. However, when a certain size is reached, each tumor is dependent on angiogenesis in order to continue growing. Tumor-initiating cells in hypoxic areas respond by stimulating vascular endothelial growth factor (VEGF) production, which causes activation of quiescent endothelial cells to stimulate new blood vessel formation. Furthermore, VEGF in tumor areas without any angiogenesis can proceed through the ras signaling pathway. In situ hybridization experiments have demonstrated that VEGF mRNA is severely upregulated in a variety of human tumors, including lung, breast...

Claims

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Application Information

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IPC IPC(8): A61K31/216A61P35/00C07C69/732C07C67/48
Inventor 陈锡强刘可春何秋霞王思锋侯海荣王希敏袁延强韩利文王雪彭维兵
Owner BIOLOGY INST OF SHANDONG ACAD OF SCI
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