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Application of dihydrotanshinone I in preparation of medicines for treating multi-drug resistant tumors, and preparation method of dihydrotanshinone I

A multi-drug resistance, dihydrotanshinone technology, applied in the direction of anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems that have not yet been found, achieve good clinical application prospects, inhibit the growth of multi-drug resistance tumors, less toxic effect

Inactive Publication Date: 2018-08-10
GUANGZHOU SHENNONG BIOLOGICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report and application of dihydrotanshinone I in the treatment of tumor multidrug resistance.

Method used

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  • Application of dihydrotanshinone I in preparation of medicines for treating multi-drug resistant tumors, and preparation method of dihydrotanshinone I
  • Application of dihydrotanshinone I in preparation of medicines for treating multi-drug resistant tumors, and preparation method of dihydrotanshinone I
  • Application of dihydrotanshinone I in preparation of medicines for treating multi-drug resistant tumors, and preparation method of dihydrotanshinone I

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Embodiment 1: the preparation process of dihydrotanshinone I

[0054] (1) After the salvia miltiorrhiza crude drug is pulverized, get 20 kilograms of pulverized medicinal materials and add 10 times the amount of sherwood oil to soak and extract, collect the filtrate after filtration and recycle, and reclaim the solvent to obtain 200 g of crude extract I;

[0055] (2) After mixing the crude extract I with the C18 reverse phase chromatography filler, the mobile phase was eluted with a 20%-60% acetonitrile aqueous solution with a gradient of 10 column volumes, and the target site was collected to obtain 26 g of the crude extract II;

[0056] (3) Utilize the normal phase chromatography silica gel column of the crude extract II, and use petroleum ether as the mobile phase: ethyl acetate=(1:9)-(3:2) to elute with a 10-fold column volume gradient to obtain dihydrotanshinone I 10g.

Embodiment 2

[0057] Example 2: Structural characterization of prepared dihydrotanshinone I

[0058] 2.1 Detection of the melting point of dihydrotanshinone I.

[0059] Take an appropriate amount of the sample obtained in Example 1, place it in a capillary tube for melting point determination, lightly tap the tube wall, place it vertically on a watch glass, put the capillary tube from the upper mouth and let it fall freely, repeat several times, so that the powder is tightly assembled in the capillary tube. Melt capped. The height of the loaded sample is 3 mm.

[0060] In addition, put the thermometer into the container containing the temperature transfer liquid, so that the distance between the bottom of the mercury bulb of the thermometer and the bottom of the container is more than 2.5cm; place. Heat the temperature-transfer fluid, and when the temperature rises to about 10°C lower than the specified lower melting point, immerse the capillary with the sample in the temperature-transfe...

Embodiment 3

[0068] Example 3: Comparison of anti-multidrug-resistant cell proliferation inhibition effects of dihydrotanshinone I and paclitaxel and other drugs

[0069] Experimental method: The multidrug-resistant cell MCF-7 / MDR and its parental cell MCF-7 were used as objects to investigate the effects of drugs such as dihydrotanshinone I and paclitaxel on the inhibition of cell proliferation.

[0070] Two kinds of cells in the growth phase with good growth and shape were taken, and 10 5 The number of cells per well was placed in a 96-well plate, 100 μL per well. After being incubated in an incubator for 18-24 hours to adhere to the wall, the MCF-7 cell group was added with each liquid sample, and the final concentrations were 4.5, 2.25, 1.13, 0.56, and 0.28 μmol / L; the MCF-7 / MDR group was added with The final concentration of the drug solution sample is shown in Table 2. For each concentration, 3 parallel wells were paralleled. After incubation in the incubator for 48 hours, the mediu...

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Abstract

The invention relates to the field of natural medicines, and discloses application of dihydrotanshinone I in preparation of medicines for treating multi-drug resistant tumors as well as a preparationmethod and a pharmaceutical composition of the dihydrotanshinone I. The dihydrotanshinone I disclosed by the invention has a remarkable inhibiting effect on drug-resistant tumor cells; the mechanism of the dihydrotanshinone I is that the killing of multi-drug resistant tumor cells is not affected by P-glycoprotein, and the intracellular drug concentration can be maintained at a normal level, so that the multi-drug resistance of tumors can be overcome. Furthermore, the killing effect of the dihydrotanshinone I on the multi-drug resistant tumor cells is significantly better than the representative antitumor drugs which are commonly used at present. The mechanism of the dihydrotanshinone I killing P-glycoprotein high-expression multi-drug resistant tumor cells is to induce apoptosis, and is consistent with parental drug-sensitive cells; furthermore, the dihydrotanshinone I has lower toxicity; therefore, the dihydrotanshinone I has a good clinical application prospect for the multi-drug resistant tumors.

Description

technical field [0001] The invention relates to the application of dihydrotanshinone I in antitumor, belongs to the field of natural medicines, and particularly relates to the application of dihydrotanshinone I in the preparation of drugs for treating multidrug-resistant tumors. Background technique [0002] The morbidity and mortality of malignant tumors are increasing year by year. Multidrug resistance (MDR) is one of the important reasons for the failure of tumor chemotherapy. Features of cross-resistance. The American Cancer Society estimates that more than 90% of the deaths of cancer patients are affected by drug resistance to varying degrees. Therefore, overcoming the multidrug resistance of tumors is an urgent clinical problem to be solved. [0003] The research on the mechanism of multidrug resistance mainly involves the overexpression of P-glycoprotein (P-glycoprotein, P-gp) on the tumor cell membrane. With fewer drugs, tumor cells develop multidrug resistance, s...

Claims

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Application Information

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IPC IPC(8): A61K31/58A61P35/00
CPCA61K31/58A61P35/00
Inventor 李莹雪丁韵芸黄静贤李紫薇
Owner GUANGZHOU SHENNONG BIOLOGICAL TECH
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