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Application of vilazodone and derivatives thereof in preparation of antitumor drugs

A technology of vilazodone and derivatives, applied in the field of medicine, can solve problems such as unreported

Pending Publication Date: 2022-01-28
FUDAN UNIV SHANGHAI CANCER CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with the existing antidepressant drugs, vilazodone is considered to have the characteristics of safety, high efficiency, and less side effects, but whether vilazodone has anti-tumor activity has not been reported in the prior art

Method used

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  • Application of vilazodone and derivatives thereof in preparation of antitumor drugs
  • Application of vilazodone and derivatives thereof in preparation of antitumor drugs
  • Application of vilazodone and derivatives thereof in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Example 1: Vilazodone inhibits the growth of various tumor cells

[0068] CCK8 colorimetric method was used to compare the effects of vilazodone hydrochloride on human breast cancer cell lines MDA-MB-231LM2 and MDA-MB-231, human colorectal cancer cell line HCT 116, colon cancer cell line SW480, and human ovarian cancer cell line A2780 , lung adenocarcinoma cell lines H1299 and A549, liver cancer cell lines MHCC-97L and SMMC-7721, gastric adenocarcinoma cell line SGC-7901, melanoma cell line A375, pancreatic cancer cell line Panc-1, leukemia cell line HL60, lymphoma Cell line MINO, esophageal cancer cell line EC109, thyroid cancer cell line TPC-1, nasopharyngeal cancer cell line 5-8F, renal clear cell adenocarcinoma cell line 786-O, glioma cell line U251, cervical cancer cell line SiHa cytotoxicity.

[0069] Various cells were seeded in 96-well plates at a density of 8000 cells / well. After 24 hours of seeding, the drugs were diluted to 0, 0.001, 0.01, 0.1, 1, 10, 20, 40...

Embodiment 2

[0071] Example 2: In vitro tumor growth inhibition experiment

[0072] see results Figure 1-20 : After 320μM vilazodone hydrochloride acts on different tumor cells for 48 hours, the inhibitory rates to tumor cells are 77.04±1.43% (breast cancer cell MDA-MB-231LM2, such as figure 1 shown), 71.16±4.79% (breast cancer cell MDA-MB-231, such as figure 2 shown), 85.03±0.88% (human colorectal cancer cell HCT116, such as image 3 shown), 86.19±0.71% (colon cancer SW480 cells, as shown in Figure 4), 87.76±0.35% (human ovarian cancer A2780 cells, as shown Figure 5 shown), 89.37±1.37% (lung adenocarcinoma cell H1299, such as Figure 6 shown), 93.92±0.43% (lung adenocarcinoma cell A549, such as Figure 7 shown), 84.49±1.13% (hepatoma cell MHCC-97L, such as Figure 8 shown), 86.40±2.12% (hepatoma cell SMMC-7721, as Figure 9 shown), 92.32±3.43% (gastric adenocarcinoma SGC-7901, such as Figure 10 shown), 81.38±0.46% (melanoma A375, such as Figure 11 shown), 77.91±2.40% (pancreat...

Embodiment 3

[0073] Example 3: Effect of vilazodone on tumor growth in nude mice with human breast cancer cell MDA-MB-231LM2 orthotopic transplantation

[0074] Adapt 6-8 week-old BALB / C female nude mice to the environment for about 1 week, digest LM2 cells with trypsin, centrifuge at 1000rpm for 5min, add 5mL of fresh DMEM without FBS, wash once, count, and adjust the concentration to 2× 10 7 / mL, each mouse was inoculated into the fat pad of the mouse with 100 μL. Wait for the tumor volume to grow to 1-20mm 3 After starting the drug. Randomly divided into 2 groups, 10 rats in each group, respectively vilazodone hydrochloride group (5 mg / kg) and solvent blank control group. The nude mice were randomly numbered, and after the tumor was implanted, the intraperitoneal injection of vilazodone hydrochloride was carried out by group. Vilazodone hydrochloride (1 mg / ml was dissolved in 5% DMSO+30% PEG300+10% Tween 80+55 % sterile water)) or solvent blank control (5% DMSO+30% PEG300+10% Tween ...

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Abstract

The invention provides application of vilazodone or a derivative thereof and a pharmaceutical composition containing the vilazodone or the derivative thereof in preparation of drugs for preventing and / or treating tumors. The compound has an obvious growth inhibition effect on various human tumor cells, and particularly has an obvious inhibition effect on tumor growth of nude mice inoculated with human tumor cells; the vilazodone or derivative thereof has broad-spectrum antitumor activity, and has good inhibitory activity on breast cancer, colorectal cancer, ovarian cancer, lung cancer, liver cancer, gastric cancer, leukemia, lymphoma, melanoma, pancreatic cancer, esophagus cancer, thyroid cancer, cervical cancer, renal clear cell adenocarcinoma, glioma, nasopharynx cancer and other tumors; and experiments show that vilazodone and the derivative thereof can become antitumor drugs.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of vilazodone and its derivatives in the preparation of antitumor drugs. Background technique [0002] With the aging trend of the population and the aggravation of environmental pollution, cancer has increasingly become the enemy that threatens human health. According to the report of the World Health Organization, cancer is the second leading cause of death in the world. In 2015, 8.8 million people died of cancer. Globally, nearly one-sixth of the deaths were caused by cancer. The types of cancer with the highest mortality rate in the world are: lung cancer (close to 1.69 million deaths in 2015), liver cancer (788,000), colorectal cancer (774,000), gastric cancer (754,000) and breast cancer (571,000). Its morbidity and mortality are not only related to gender, there are also obvious differences between developed and underdeveloped regions. [0003] Anti-tumor...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61P35/00A61P35/02
CPCA61K31/496A61P35/00A61P35/02
Inventor 金伟刘琪琦孙荷芬
Owner FUDAN UNIV SHANGHAI CANCER CENT
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