Use of ligustilide as an auxiliary drug for antineoplastic drugs

An anti-tumor drug, the technology of ligustilide, applied in the field of medicine, can solve the problems such as insufficient in-depth and detailed pharmacological research of ligustilide, and achieve the effect of promoting tumor cell survival and improving effect

Inactive Publication Date: 2019-01-04
SOUTHWEST UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] There are many pharmacological reports on ligustilide, mainly focusing on the research on the effects of cardiovascular and cerebrovascular, antimicrobial, analgesic, antipyretic and anti-inflammatory, and some cancers. The mixture of ligustilide, but the pharmacological research on ligustilide is not deep and detailed enough

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  • Use of ligustilide as an auxiliary drug for antineoplastic drugs
  • Use of ligustilide as an auxiliary drug for antineoplastic drugs
  • Use of ligustilide as an auxiliary drug for antineoplastic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 Effect of ligustilide on autophagic flow in cells

[0032] MCF-7, U251, and T-47D cells were used in the experiment, and the cells were first incubated with ligustilide at a concentration of 0, 10, 50, 100, and 200 μmol / L for 48 hours to extract and isolate proteins and perform Western Blot experiments. Experimental results such as figure 1 As shown in panel A in the middle, as the concentration of ligustilide increased, the expression of LC3-II protein gradually increased.

[0033] Then incubate with 50 μmol / L ligustilide for 0, 3, 6, 12, 24, and 48 hours respectively, and perform Western Blot experiment after protein extraction. The experimental results are shown in figure 1 In Figure B, the experimental results also showed that the expression of LC3-II protein was up-regulated, and similar results were obtained in drug-resistant breast cancer cells TR5 ( figure 1 Middle D panel). n-Butylphenylpeptide also obtained similar results to ligustilide ( figure...

Embodiment 2

[0034] Example 2 Ligustilide inhibits autophagy

[0035] U251 cells and MCF-7 cells were used in the experiment. First, the cells were incubated with ligustilide at concentrations of 0, 10, 50, 100, and 200 μmol / L for 48 hours, and the protein was collected for Western Blot experiment. Experimental results such as figure 2 As shown in panel A in the middle, the expression level of P62 protein gradually increased with the increase of the concentration.

[0036] Incubate with 50 μmol / L ligustilide for 0, 3, 6, 12, 24, and 48 hours respectively, and the results are shown in figure 2 In panel B, the expression of P62 protein was also up-regulated. Similar results were obtained for n-butylphenyl peptide ( figure 2 Middle C), similar results were obtained in drug-resistant breast cancer cells TR5 ( figure 2 Middle D panel). This experiment proves that ligustilide can inhibit cell autophagy.

Embodiment 3

[0037] The influence of embodiment 3 ligustilide on lysosome pH value

[0038] AO staining experiment was carried out on U251 cells to investigate the effect of ligustilide on the pH value of lysosome. Firstly, 0, 50, and 200 μM of ligustilide were given respectively. After 24 hours of administration, they were stained with 3 μg / ml AO dye solution for 10 minutes, and then the red fluorescence of lysosomes was observed under a fluorescent microscope. The results were as follows: image 3As shown, the red fluorescence decreased after administration of ligustilide, indicating that the pH value of lysosomes was neutralized. Similar results were found with MCF-7 cells. This experiment proves that ligustilide can neutralize the pH value of lysosome and interfere with lysosome function.

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Abstract

The invention discloses an application of ligustilide as an adjuvant drug of antitumor drugs. The research found that ligustilide can directly inhibit autophagy and then can perform combined effects with the antitumor drugs such as tamoxifen, cis-platinum and the like, the antitumor effect is improved, and the drug resistance of tumor cells to the antitumor drugs can be improved.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the use of ligustilide as an auxiliary drug for antitumor drugs. Background technique [0002] Autophagy is a dynamic process in which cells degrade their own organelles and proteins to meet the metabolic needs of the cell itself and the renewal of some organelles. The process of autophagy first forms autophagic vesicles from the double-membrane shedding from the ribosome-free attachment region of the rough endoplasmic reticulum, and the cellular organelles and proteins that need to be degraded in the cell, and then fuses with lysosomes to form autophagy Lysosomes, rely on lysosomes to degrade their encapsulated contents. The half-life of autophagosomes is about 8 minutes, which is an effective response of cells to environmental changes. [0003] Autophagy can be divided into three types: macroautophagy, microautophagy, and chaperone-mediated autophagy according to the diffe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/365A61P35/00
CPCA61K31/365
Inventor 齐红艺蒋竺芸李莉
Owner SOUTHWEST UNIV
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