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Alpha-tubulin inhibitor and application thereof

A technology of tubulin inhibition and woody lactone, which is applied in the field of medicine and has the effects of wide application prospects, inhibition of tumor cell growth, and inhibition of tumor growth rate.

Inactive Publication Date: 2014-01-15
SHANGHAI XUANJIA BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] So far, there is no relevant research report on the active ingredients of inulin or woody incense having tubulin inhibitory activity

Method used

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  • Alpha-tubulin inhibitor and application thereof
  • Alpha-tubulin inhibitor and application thereof
  • Alpha-tubulin inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1: Inhibition of microtubule gene and protein expression by various lactone compounds described in the present invention

[0038] 1. Experimental drugs

[0039] Each lactone compound described in the present invention (inectinolide, isoinectinolide, dihydroinectinolide, dehydrogeninolactone, coustene lactone and dihydroinurinolide) The samples were dissolved in DMSO respectively, and were all prepared as 10 mM mother solution for storage, and then diluted with DMEM complete medium to the required concentration when the experiment was administered.

[0040] Paclitaxel drug solution: take an appropriate amount of paclitaxel (purchased from sigma, purity >98%), dissolve it in DMSO, prepare it as a 50 μM mother solution for storage, and dilute it with DMEM complete medium to a concentration of 50 nM when the experiment is administered.

[0041] 2. Experimental method

[0042] 1. Western Blot analysis

[0043] (1) Protein extraction: Human melanoma cell line A375 ...

Embodiment 2

[0080] Example 2: Inhibitory effect of various lactone compounds of the present invention on tumor cell spindle formation

[0081] 1. Experimental method: immunofluorescence chemical method

[0082] (1) Slide coating: Put the sterilized round coverslip into each well of a 12-well cell culture plate, cover each slide with 0.1 mg / mL poly-lysine, about 200 μL; put After 8-10 hours in an incubator at 37°C, blow dry in an ultra-clean platform.

[0083] (2) Administration: Take the human melanoma cell line A375 in good growth state and in the logarithmic growth phase, adjust the cell concentration to 8×10 4 cells / mL, administered after cell attachment, the administration concentration of each lactone compound described in the present invention was 2.5 μM, 5 μM, and cultured for 24 hours.

[0084] (3) Cell fixation: After administration, wash with PBS 2 to 3 times, add 10% formaldehyde fixative solution, and fix at room temperature for 1 hour; then wash the fixative solution with P...

Embodiment 3

[0090] Embodiment 3: Effects of various lactone compounds described in the present invention on tumor cell cycle

[0091] 1. Experimental materials

[0092] 1.1 Cell lines

[0093] The human melanoma cell line A375 used in the experiment was quoted from the ATCC cell bank. Cells were cultured in complete DMEM medium containing 10% FBS (fetal bovine serum), 1% double antibody (100u / mL penicillin and 100u / mL streptomycin).

[0094] 1.2 Experimental drugs and their preparation

[0095] The preparation of each lactone compound medicinal liquid described in the present invention: take 1 mg of each lactone compound powder described in the present invention respectively, dissolve with DMSO to make the concentration 10 mM, store it at -20° C. as the mother solution; According to the ratio, it was diluted with DMEM medium containing 10% FBS and 1% double antibody (100u / mL penicillin and 100u / mL streptomycin) to prepare 2.5μM, 5μM and 10μM.

[0096] Preparation of paclitaxel drug so...

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Abstract

The invention discloses an alpha-tubulin inhibitor and application thereof. The active ingredients of the alpha-tubulin inhibitor consist of effective quantities of at least one lactone compound of alantolactone, isoalantolactone, dihydro-alantolactone, dehydrocostunolide lactone, costunolide and dihydro-costunolide. The alpha-tubulin inhibitor disclosed by the invention can obviously inhibit alpha-tubulin and the mRNA (Messenger Ribonucleic Acid) level thereof, can inhibit the forming of spindles, block the cell cycle in the G2 / M period, induce cell apoptosis and the like, can effectively inhibit the tumor growth speed, can obviously inhibit growth of various tumor cells, particularly has an obvious effect on melanoma, can be expected to be used for preparing medicament preparations for resisting tumors and has wide application prospect, wherein the tumors comprise lung cancer, pancreatic cancer, prostatic cancer, neuroblastoma, melanoma and breast cancer.

Description

technical field [0001] The invention relates to an α-tubulin inhibitor and its application, belonging to the technical field of medicine. Background technique [0002] Microtubules are the main components of the cytoskeleton and are characterized by hollow tubular structures. As a component of microtubules, tubulin is mainly composed of α-tubulin and β-tubulin, which can form dimers and then arrange to form microtubules. Microtubules play an important role in cell morphology, cell division, signal transduction and material transport. Under normal circumstances, microtubules can depolymerize into tubulin heterodimers, aggregate into spindles in the early stage of cell division, and pull sister chromatids to move to the poles in mitosis to form two daughter cells to complete cell division. That is to say, tubulin plays a crucial role in the DNA division of the nucleus and is closely related to the G2 / M phase of the cell cycle. Because microtubules play an extremely importan...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P35/00
Inventor 张捷
Owner SHANGHAI XUANJIA BIOTECH CO LTD
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