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Application of emodin anthraquinone derivative in preparation of anti-hepatocellular carcinoma drugs

A technology of anthraquinone derivatives and emodin, which is applied in drug combinations, antineoplastic drugs, and pharmaceutical formulations, can solve the problems of difficult extraction, limited structure optimization, activity screening, and poor bioavailability, and achieve obvious cytotoxicity , Inhibition of tumor cell growth, significant anti-liver cancer activity

Inactive Publication Date: 2013-10-23
SHANXI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Anthraquinone compounds have various biological activities such as catharsis, antibacterial, blood pressure lowering, antioxidation, antitumor, etc. However, due to their low water solubility and poor bioavailability, in addition to their purging effect, other pharmacological activities are still available. rarely used clinically
Although emodinoid anthraquinone derivatives exist in a variety of plants, their extraction is difficult due to their low content in plants, and the extraction process is relatively complicated, which limits further structural optimization and activity screening. The principle and mechanism of action and the structure-activity relationship of anthraquinone derivatives, we designed and synthesized 1,4-dimethyl-6,8-dimethoxy-9,10-anthraquinone, and preliminary experimental studies found that its effect on influenza The activity of viral neuraminidase has a certain inhibitory effect, and its use in the preparation of anticancer drugs remains to be further studied

Method used

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  • Application of emodin anthraquinone derivative in preparation of anti-hepatocellular carcinoma drugs
  • Application of emodin anthraquinone derivative in preparation of anti-hepatocellular carcinoma drugs
  • Application of emodin anthraquinone derivative in preparation of anti-hepatocellular carcinoma drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] 1,4-Dimethyl-6,8-dimethoxy-9,10-anthraquinone in vitro anticancer activity experiment:

[0022] The anticancer activity experiment was realized by cytotoxicity, and the proliferation inhibitory activity of the compound on seven tumor cell lines was measured by standard MTT colorimetry. The tested tumor cell lines are human liver cancer cell line HepG2, gastric cancer cell line SGC-7901, breast cancer cell line MCF-7, cervical cancer cell line HeLa, bile duct cancer cell line QBC-939, esophageal cancer cell line EC9706, colon cancer cell line SW480 , while using human normal liver cells HL-7702 as a control.

[0023] The specific steps are: take the cells in the logarithmic growth phase and in good condition, add 0.25% trypsin to digest, make a single cell suspension, count on a cell counting plate, and inoculate 100 μL per well in a 96-well plate. The number of cells was controlled at 5×104 / mL, cultured overnight in a 5% CO2 incubator at 37°C, and prepared samples of d...

Embodiment 2

[0035] Example 2 Interaction between 1,4-dimethyl-6,8-dimethoxy-9,10-anthraquinone and bovine serum albumin

[0036] Absorption Spectroscopy Research

[0037] Figure 5 Curve 1 is the ultraviolet absorption spectrum of bovine serum albumin, and curve 2-10 is the ultraviolet absorption spectrum after adding different concentrations of the compound in bovine serum albumin. It can be seen from the figure that the absorption peak of bovine serum albumin after adding different concentrations of the compound Increased strength. It indicated that there was an interaction between the compound and BSA, and a complex with certain stability was formed.

[0038] Effects of Compounds on the Fluorescence Spectrum of Bovine Serum Albumin

[0039] Figure 6 Curve 1 is the fluorescence spectrum of bovine serum albumin, and curve 2-10 is the fluorescence spectrum after adding different concentrations of this compound in bovine serum albumin. It can be seen from the figure that the fluoresce...

Embodiment 3

[0040] Example 3 Interaction experiment between 1,4-dimethyl-6,8-dimethoxy-9,10-anthraquinone and DNA

[0041] Absorption Spectroscopy Research

[0042] Figure 7 Curve 1 is the ultraviolet absorption spectrum of DNA, and curves 2-9 are the ultraviolet absorption spectra of DNA after adding different concentrations of the compound. It can be seen from the figure that the DNA absorption peak intensity decreases after adding different concentrations of the compound. According to literature reports, when small molecules are intercalated between the base pairs of the CT-DNA double helix, the absorption spectrum exhibits a color reduction effect, and the wavelength is red-shifted; -DNA, its absorption spectrum shows no obvious color enhancement effect or color reduction, and no red shift; therefore, the interaction between the compound and CT-DNA at this time should be dominated by intercalation.

[0043] Compound Effects on DNA Fluorescence Spectrum

[0044] Figure 8 Curve 1 ...

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Abstract

The invention provides application of an emodin anthraquinone derivative in preparation of anti-hepatocellular carcinoma drugs. The emodin anthraquinone derivative is a 1, 4-dimethyl-6, 8-dimethoxy-9, 10-anthraquinone. The derivative not only can well inhibit proliferation of hepatocellular carcinoma cells, induce their apoptosis, and also has very small toxicity to normal cells. The derivative can be used in conjunction with 5-FU, cis-platinum and other chemotherapy drugs to increase the sensitivity of the chemotherapy drugs, thus achieving the effect of inhibiting hepatocellular carcinoma cell growth. Therefore, the emodin anthraquinone derivative can be used for preparing anti-hepatocellular carcinoma drugs or adjuvant chemotherapy drugs.

Description

technical field [0001] The invention relates to the application of emodin anthraquinone derivatives, specifically 1,4-dimethyl-6,8-dimethoxy-9,10-anthraquinone in the preparation of anti-liver cancer drugs. Background technique [0002] Hepatocellular carcinoma (HCC) is a malignant tumor with high degree of malignancy, strong infiltration and metastasis, difficult treatment and high mortality. At present, the patients with liver cancer in my country account for more than half of the global liver cancer patients, which seriously threatens human life. Liver cancer is not sensitive to chemotherapy and radiotherapy, and only 15% of patients can be cured by surgery, and it is prone to early metastasis and postoperative recurrence. This aspect may be related to the multidrug resistance gene of liver cancer cells. The more important reason is that the occurrence and development of liver cancer is a multi-step and multi-factor process, involving a series of complex biological change...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61P35/00
Inventor 李玉英张立伟
Owner SHANXI UNIV
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