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Application of curcumenol in preparation of an antitumor drug sensitizer

An anti-tumor drug, the technology of curcumol, which is applied in the field of cell biology and medicine, can solve the problems of low yield and purity, and achieve the effect of obvious tumor suppressing effect.

Inactive Publication Date: 2017-07-07
FUDAN UNIV
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

[0005] It is the extract of the Zingiberaceae plant Curcuma. The traditional method of extracting curcumol from Curcuma curcuma and Curcuma curcuma is basically extraction with methanol or water, followed by steam distillation, and recrystallization with ethyl acetate or absolute ethanol to obtain Curcuma. Alcohol [Hiroshi H, Kanji M, Yojiro S, et al.Structure of curcumol.[J]. Chem Pharm Bull, 1965, 13 (12): 1 484, Xu Hongxia, Zheng Shuchen, Zuo Shixian, etc. Wen Curcumol Antitumor Research on active ingredients - separation and identification of curcumol and curcumedione [J]. Chinese Herbal Medicine Communication, 1979, 10 (10): 11.], the yield and purity obtained are low, and subsequent purification such as silica gel column separation is required

Method used

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  • Application of curcumenol in preparation of an antitumor drug sensitizer
  • Application of curcumenol in preparation of an antitumor drug sensitizer

Examples

Experimental program
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Effect test

Embodiment 1

[0059]

[0060] Experimental results:

[0061] KB / VCR and MCF-7 / ADR are two commonly used multidrug-resistant cell lines, and in this example, these two kinds of cells also exhibit the characteristic of multidrug resistance. As shown in Table 1, compared with KB cells, the multiples of drug resistance of KB / VCR cells to VCR and ADR were 81.9 times and 94.4 times, respectively, while MCF-7 / ADR cells were more resistant to VCR and ADR than MCF-7 cells. The drug multiples were 38.1 times and 20.9 times respectively, showing that the drug-resistant cells used in the experiment had multidrug resistance, and the MDR activity was similar to the results reported in the literature.

[0062] The half maximal inhibitory concentration IC of curcumol on the parental cell lines KB and MCF-7 50 Respectively 56.9 μ M and 62.7 μ M, to the IC of drug-resistant cell line KB / VCR and MCF-7 / ADR 50 133.0 μΜ and 143.9 μΜ respectively, there was no significant difference between the two, and the ...

Embodiment 2

[0064] Example 2: The CCK-8 method detects the reversal effect of curcumol on the multidrug resistance activity of tumor cells

[0065] KB / VCR, MCF-7 / ADR and HCT-8 / VCR cells were inoculated into 96-well plates at a density of 3500 / well, and after 24 h, different concentrations of VCR, and different concentrations of VCR and curcumol were used together containing 10% α-MEM of fetal bovine serum was prepared and added to each well. After culturing for 48 h, the culture medium was discarded, and the CCK-8 kit was used to measure the activity of the drug-resistant cell line and its parental cells on VCR and VCR+curcumol in the same manner as in Example 1, and a curve was drawn. Three replicate wells were set for each concentration, and the experiment was repeated 3 times.

[0066] Experimental results:

[0067] The multiplicity of drug resistance of KB / VCR cells to VCR was 81.9 times, and that of MCF-7 / ADR cells to ADR was 20.9 times. When 10 μM curcumol was added, the sensitiv...

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Abstract

The invention belongs to the field of cell biology and medicine, and relates to the application of curcumol in the preparation of antitumor drug sensitizers. Curcumol is a natural product, which has the effect of reversing the multidrug resistance of tumor cells and can be used as a reversal agent for tumor multidrug resistance; Curcumol also has the effect of increasing the sensitivity of tumor multidrug-resistant cells to anti-tumor drugs, and can be used as chemotherapy Sensitizers are used. The present invention also provides a method for inhibiting the proliferation of tumor multidrug-resistant cells by using the pharmaceutical composition of the antitumor drug and curcumol in combination. The small-molecule compound curcumitol in the present invention is developed as a new anti-tumor drug or its auxiliary components, has obvious tumor-inhibiting effect, is green and environmentally friendly, and will provide a new approach and means for treating and curing tumors.

Description

technical field [0001] The invention belongs to the fields of cell biology and medicine, in particular, the invention relates to a new application of curcumol. The invention also relates to the corresponding pharmaceutical composition and its application method. Background technique [0002] Tumor is an abnormal lesion formed by the body under the action of various carcinogenic factors when a certain cell in a local tissue loses its normal regulation of its growth at the gene level, resulting in its clonal abnormal proliferation. The number of cancer cases in my country is quite large, accounting for 55% of the total number of cases in the world. [0003] Benign tumors have less impact on the body, mainly showing symptoms of local compression and obstruction. Malignant tumors have a serious impact on the body due to their immature differentiation, rapid growth, infiltration and damage to the structure and function of organs, and the possibility of metastasis. In addition ...

Claims

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Application Information

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IPC IPC(8): A61K31/35A61K45/06A61K31/475A61K31/704A61P35/00
CPCA61K31/35A61K31/475A61K31/704A61K45/06
Inventor 余龙朱恒锐
Owner FUDAN UNIV
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