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Epigallocatechin gallate (ECG) and daunorubicin (DNR) composition and use thereof

A technology of epicatechin gallate and daunorubicin, which is applied in the field of medicine and genetic engineering, can solve the problem of no combination of ECG and DNR, achieve enhanced anti-tumor effect, no toxic and side effects, and reduce treatment costs Effect

Inactive Publication Date: 2013-08-21
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] So far, there have been no reports of the combined use of ECG and DNR

Method used

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  • Epigallocatechin gallate (ECG) and daunorubicin (DNR) composition and use thereof
  • Epigallocatechin gallate (ECG) and daunorubicin (DNR) composition and use thereof
  • Epigallocatechin gallate (ECG) and daunorubicin (DNR) composition and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1E

[0044] The structural diagram of embodiment 1ECG, EC, EGC

[0045] Such as figure 1 As shown, the structural difference between ECG and EC and EGC is mainly that ECG has one more G ring than EC and EGC.

Embodiment 2E

[0046] Example 2 ECG, EC, EGC inhibit the difference in the activity of carbonyl reductase CBR1

[0047] The enzyme activity was analyzed with indolindione as the substrate and NADPH as the coenzyme. The coenzyme NADPH has a maximum absorbance value at 340nm, and a UV spectrophotometer is used for time scanning to detect the change in absorbance at a wavelength of 340nm to reflect the enzymatic reaction speed. The reaction system is 600 μl, the buffer system is 0.1M phosphate buffer, the appropriate amount of enzyme, the coenzyme NADPH is changed in different reactions, the substrate is indolindione, and the amount of inhibitor ECG. Three parallel tubes were made for each sample. The inhibitory effect of EC and EGC on carbonyl reductase CBR1 was significantly lower than that of ECG. The IC50 of ECG inhibiting CBR1 was 2.32μM ( figure 2 ), the inhibition rate of EC at 200 μM was 23.6%, and the inhibition rate of EGC at 200 μM was 36.6%.

Embodiment 3E

[0048] The antitumor effect of embodiment 3ECG, EC, EGC single drug

[0049] ECG, EC, EGC did not show a good anti-tumor effect when used alone. These three drugs were used at concentrations of 10 μM, 20 μM, 40 μM, 80 μM and 160 μM to act on the liver cancer cell line HepG2 ( image 3 ) and SMMC7721 ( Figure 4 ), the results showed that their IC50 values ​​were all over 160 μM, which indicated that they were not powerful anti-tumor drugs that could be used alone, but also indicated that the toxicity of the three was weak and could be used as adjuvant or synergistic drugs.

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Abstract

The invention belongs to the fields of medicines and genetic engineering and relates to an Epigallocatechin gallate (ECG) and daunorubicin (DNR) composition and use thereof. The invention provides a tumor cell proliferation inhibiting composition which contains the Epigallocatechin gallate (ECG) and daunorubicin. When the composition is used for preparing anti-tumor medicines, the heart toxicity of DNR can be lowered greatly, the anti-tumor effect of the DNR can be improved greatly and the dosage of DNR and medicine cost can be reduced relatively. The ECG is natural extract of tea leaves which is a common drink for two thirds of world population. Therefore, the resource is rich, the price is low, and toxic effect hardly appears in thousands of years of drinking. EGC is used as an assistant medicine of DNR. In the invention, the formula scheme of a high-efficiency and low-price antitumor medicine is provided, the tumor inhibition efficiency is improved, and the treatment cost of patients with tumor is reduced.

Description

technical field [0001] The invention belongs to the fields of medicine and genetic engineering, and relates to a composition of epicatechin gallate (ECG) and daunorubicin (DNR) and an application thereof. Background technique [0002] Anthracyclines are one of the most effective antitumor drugs, including DNR (DNR) and doxorubicin (DOX), which can treat a variety of cancers, including leukemia and solid tumors (Minotti, G., et al., Anthracyclines : molecular advances and pharmacological developments in antitumor activity and cardiotoxicity.PharmacolRev, 2004.56(2): p.185-229), has an anthracycline plane, which can be fitted between DNA base pairs and tightly bound to DNA , so that the nucleic acid contains a relatively high concentration of drugs. This chimerism can lead to obstacles in the DNA space structure, thereby inhibiting the synthesis of DNA and DNA-dependent RNA. The impact on RNA is particularly obvious, and it can selectively act on purine nucleosides . As a ce...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/704A61K31/353A61P35/00
Inventor 余龙丁丽娅黄维雪黄强唐丽莎
Owner FUDAN UNIV