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Use of alkannin in preparing medicine for treating tumor disease

A shikonin and chemotherapeutic drug technology, applied in the direction of antineoplastic drugs, drug delivery, drug combination, etc., can solve the problem of drug efficacy reduction and achieve low toxicity and good clinical tumor chemotherapy effect

Inactive Publication Date: 2005-02-16
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented technology allows for better use of certain substances called shiritins (a type of plant extract) by treating cancer patients with these compounds or other agents like cisplatin. These techniques can help reduce side reactions caused by treatment without causing damage to healthy tissues.

Problems solved by technology

This patented technical problem addressed in this patents relating to improving the efficiency or safety of medical preparations containing shikimodium bark extract derived from plants belonging to genus Thymeriaceae.

Method used

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  • Use of alkannin in preparing medicine for treating tumor disease
  • Use of alkannin in preparing medicine for treating tumor disease
  • Use of alkannin in preparing medicine for treating tumor disease

Examples

Experimental program
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Effect test

Embodiment 1

[0029] Example 1 Identification of Drug Resistance Spectrum of Multidrug Resistant Cell K562 / ADR Cell Line

[0030] The multi-drug resistant cell line K562 / ADR was established by Hu Xun et al. in 1995 using the human erythroleukemia cell line K562 induced by the antitumor drug doxorubicin [15] .

[0031] Determination of resistance of drug-resistant cells to 11 typical antineoplastic drugs by MTT assay

[0032] Take the K562 and K562 / ADR cells in the exponential growth phase with good growth and shape, count them, centrifuge them, and divide them into 8×10 3The concentration of the number of cells / well was inoculated in a 96-well plate, and 100 μl of each well was added with a final concentration of 0.01, 0.02, 0.1, 0.2, 1, 2, 10, and 20 μg / ml of doxorubicin, epirubicin, and daunorubicin, respectively. 11 representative antineoplastic drugs, including vincristine, paclitaxel, methotrexate, fluorouracil, mitomycin C, etoposide, hydroxycamptothecin, homoharringtonine, etc. Th...

Embodiment 2

[0054] Example 2 Flow cytometry analysis of the accumulation ability of K562 and K562 / ADR cells to doxorubicin

[0055] Take well-grown K562 and K562 / ADR cells in the exponential growth phase, culture them with doxorubicin at a final concentration of 10 μg / ml in an incubator for 120 min, wash them twice with cold PBS, collect the cells, count them, and use Cold PBS made up 1 x 10 6 Cells / ml cell suspension, stored at 4°C until the sample is loaded, and the fluorescence intensity of doxorubicin in the cell is measured by flow cytometry. The detection excitation wavelength is 488nm, and the acceptance wavelength is 575nm. The arbitrary unit of intensity indicates the relative concentration of doxorubicin in the cell .

[0056] Results: K562 has a strong ability to accumulate doxorubicin. After co-cultivating with 10 μg / ml doxorubicin for 2 hours, the concentration of doxorubicin in K562 cells is about 5 times that of K562 / ADR cells, while K562 / ADR cells are due to Pgp Efflux l...

Embodiment 3

[0057] Example 3 Flow cytometry detection of Pgp expression in K562 / ADR cells

[0058] Take well-grown K562 and K562 / ADR cells in the exponential growth phase, wash them twice with cold PBS, collect the cells, count them, and make 1×10 cells with cold PBS. 6 Add 20 μl of anti-Pgp monoclonal antibody (R-PE-17F9) labeled with PE (Phycoerythrin) to the cell suspension of cells / ml, react at room temperature for 15 minutes in the dark, add PBS and wash twice , load the sample to flow cytometry, and express the expression level of Pgp with the fluorescence intensity.

[0059] Results: In the negative control K562 cells, the proportion of highly expressed Pgp was only 0.68%, while that of drug-resistant K562 / ADR cells was as high as 88.79%. At the same time, the average expression of membrane protein Pgp in drug-resistant cells K562 / ADR was 302.40 / 9.65=31 times that of K562. Therefore, the drug resistance mechanism of K562 / ADR cells is mainly caused by the overexpression of Pgp, se...

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Abstract

The invention provides a new utilization of alkannin, the molecular weight is: 288.2994, the chemical name is: (+)-5, 8-dihydroxy-2-(1-hydroxy-4-methyl-3-pentenyl)-1, 4-naphthoquinone, the molecular formula is: C16H16O5. the alkannin provided in the invention is compbined with medicine excepient or carrier for producing medicine for curing tumour. The effect of the alkannin to multi-medicine and medicine-resisting tumour cell is not affected by p-glycoprotein, and the killing effect to eh tumour is more excellent than current medicine, the mechanism of the alkannin killing tumour cell with Pgp high representation is inducing the cell to be dead, and consistent with the parent drug cell. The alkannin has low toxin, thus, the alkannin has a good application prospect.

Description

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Claims

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Application Information

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Owner ZHEJIANG UNIV
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