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An indanone compound that double targets ovarian cancer cell tubulin and surrounding blood vessels, its preparation method and application

A compound and ovarian cancer technology, applied in the field of biomedicine, can solve the problems of poor water solubility, high incidence of drug resistance, narrow anti-tumor spectrum, etc., and achieve the effects of small molecular weight, inhibition of proliferation, and high anti-tumor activity

Inactive Publication Date: 2016-09-28
FUDAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the other hand, such tubulin inhibitors have poor water solubility and are difficult to administer through blood vessels; only against the proliferation of tumor cells themselves, the anti-tumor spectrum is very narrow, and the incidence of drug resistance during treatment is high

Method used

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  • An indanone compound that double targets ovarian cancer cell tubulin and surrounding blood vessels, its preparation method and application
  • An indanone compound that double targets ovarian cancer cell tubulin and surrounding blood vessels, its preparation method and application
  • An indanone compound that double targets ovarian cancer cell tubulin and surrounding blood vessels, its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1 Cell viability detected by CCK-8 method confirmed that compound 1 has anti-tumor effect on ovarian cancer A2780 and A2780cisR, see figure 1 shown. By CCK-8 method, we tested the cell viability of A2780 and A2780cisR cells treated with compound 1. It was found that compound 1 can inhibit the proliferation of ovarian cancer cells, and this inhibitory effect is concentration-dependent. Among them, at the concentration of 10 μg / mL, the tumor inhibition rate of the cells was 49.3%. At the same time, according to the tumor cell growth inhibition curve, the IC50 of compound 1 against A2780 and A2780cisR were 5.48 and 5.98 μg / mL, respectively.

Embodiment 2

[0040] Example 2 Detection of apoptosis rate by Hochest staining confirmed that compound 1 can promote the apoptosis of ovarian cancer SKOV3. See figure 2 shown. The apoptotic ability of ovarian cancer SKOV3 treated with Compound 1 was analyzed by Hochest staining. Among them, compared with the blank control group, the number of apoptotic cells in the ovarian cancer A2780 and A2780cisR cells treated with compound 1 increased, and the numbers were (76.3±64.2) and (26.1±14.2) in turn. There is a statistical difference (P figure 2 It can be seen that a lot of nuclear fragmentation and nuclear condensation can be seen in the ovarian cancer cells treated with compound 1, and some nuclear accumulation can also be seen in it.

Embodiment 3

[0041] Example 3 The Western Blot method was used to detect the expression of tubulin α in the tumor tissues of each group, and it was confirmed that compound 1 has the effect of promoting tubulin aggregation and inhibiting its depolymerization on ovarian cancer SKOV3 cells in vivo, see image 3 shown. Tublinα is the main component of microtubules, so we detected the expression of Tublinα in each group of tumor tissues by Western Blot method. The results showed that there were differences in the expression of Tublinα in each group, and the expression of Tublinα in the tumor tissue of the nude mice in the compound 1 group was the highest.

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Abstract

The invention belongs to the biomedical technical field, and in particular, relates to an indanone compound dual-targeting to tumor cell tubulin and tumor peripheral blood vessels, and a synthetic method and an application thereof. The indanone compound is designed and synthesized. The compound can be combined with tubulin of tumor cells, promotes the tubulin aggregation, disturbs the tubulin depolymerization, thereby disturbing a tumor cell mitosis process; a tumor blood vessel area can be destroyed through the action of the compound with tumor blood vessel endothelial cells. A lot of experiments confirm that through dual-targeting to the tumor cell tubulin and the tumor peripheral blood vessels, the compound can safely and effectively inhibit tumor cell proliferation, promote tumor cell apoptosis, inhibit tumor cell metastasis and inhibit tumor cell angiogenesis. The compound is small in molecular mass, relatively high in oral bioavailability, and relatively flexible in clinical medication, can dual-target to ovarian cancer cells and the peripheral blood vessels thereof, is higher in antitumor activity, and has more advantages in the clinical application.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and specifically relates to an indanone compound dual-targeting ovarian cancer cell tubulin and surrounding blood vessels, a preparation method and application thereof. Background technique [0002] Indanones have become a hot spot in the research and development of new anticancer drugs because of their unique pharmacological effects. In recent years, researchers at home and abroad have studied the preclinical application and anticancer mechanism of indenone compounds from different angles, and found that indenone compounds have significant curative effects on various cancer cells. [0003] There are more than 100 naturally occurring indanone compounds, and their basic structures include 1-indanone, 2-indanone, 1,2-indanedione, 1,3-indenedione, and ninhydrin. These indene ring structures exist in molecules such as natural products, synthetic drugs, and pesticides. Indanone is originally a r...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D207/34A61P35/00
CPCC07D207/34
Inventor 尧良清陈晨郑旦庆吴劼
Owner FUDAN UNIV
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