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Application and pharmaceutical composition of polysubstitution naphthalene derivative in preparing tumor angiogenesis resisting medicine

A naphthalene derivative and angiogenesis technology, applied in the field of biological activity application of compounds, can solve problems such as difficult development and unsatisfactory biological activity, and achieve the effects of enhancing sensitivity, inhibiting metastasis and recurrence, and reducing concentration

Active Publication Date: 2017-05-31
THE SECOND AFFILIATED HOSPITAL OF NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the biological activity of zoledronic acid in inhibiting tumor angiogenesis is not ideal, and it is difficult to develop it into a first-line anti-tumor drug

Method used

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  • Application and pharmaceutical composition of polysubstitution naphthalene derivative in preparing tumor angiogenesis resisting medicine
  • Application and pharmaceutical composition of polysubstitution naphthalene derivative in preparing tumor angiogenesis resisting medicine
  • Application and pharmaceutical composition of polysubstitution naphthalene derivative in preparing tumor angiogenesis resisting medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: Effect test of NY-06D on endothelial cell migration induced by tumor cell culture medium

[0021] The effect of NY-06D on the migration of vascular endothelial cells induced by tumor cell culture medium was detected by wound healing method: Human umbilical vein endothelial cell line ECV304 cells in the logarithmic growth phase were cultured under normal conditions for 24 hours. Scratch the middle of the 24h well plate with a 0.5mm cell scraper, cut off the cell monolayer, and wash it with PBS twice to remove the scraped free cells.

[0022] The experiment was divided into negative control group, induction group and treatment group. In the induction group, 10% human breast cancer cell MCF-7 culture solution was added to the control group as a positive control; in the treatment group, 100 μL of 10% human breast cancer cell MCF-7 culture solution was added, and then NY-06D solution was added. (concentration 0.2 mg / mL, prepared from 1640 complete medium, filtere...

Embodiment 2

[0024] Example 2: Effect test of NY-06D on tumor angiogenesis in lung cancer

[0025] New Zealand rabbits were randomly divided into NY-06D group, ZOL group, NY-06D+ZOL group, blank control group, a total of 4 groups, 2 rabbits in each group. According to the dose in Table 1, each group was administered twice a day, with an interval of 12 hours, for 3 consecutive days, and 1 hour after the last intragastric administration, the carotid artery was bled, left overnight at 4°C, and centrifuged at 2500r / min for 25 minutes to separate the serum and mix it evenly to eliminate bacteria. Filter and inactivate, and freeze at -70°C for later use. Under the same conditions, the blank control serum was prepared by intragastric administration with an equal volume of normal saline.

[0026] Table 1 Dosage of each group

[0027]

[0028] Human lung adenocarcinoma cell line A549 and human umbilical vein endothelial cell line CRL-1730 were cultured in DMEM containing 10% fetal bovine serum...

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Abstract

The invention provides application and a pharmaceutical composition of polysubstitution naphthalene derivative in preparing tumor angiogenesis resisting medicine. According to the application and the pharmaceutical composition, the polysubstitution naphthalene derivative is found to have activity for restraining tumor angiogenesis for the first time, tumor restraining and tumor angiogenesis resisting medicine prepared according to the discovery can be applied to treating or preventing diseases related to tumor or tumor angiogenesis. Meanwhile, the polysubstitution naphthalene derivative selectively targets tumor angiogenesis, remarkably improves the concentration of tumor angiogenesis resisting medicine in vascular endothelial cells, reduces the concentration of the tumor angiogenesis resisting medicine in normal tissues and organs to the maximum degree and overcomes side effects caused by whole-body medicine distribution.

Description

technical field [0001] The invention belongs to the technical field of biologically active applications of compounds, and specifically relates to the application and pharmaceutical composition of a multi-substituted naphthalene derivative in the preparation of anti-tumor angiogenesis drugs. Background technique [0002] Blood vessels are necessary for the morphogenesis and function maintenance of normal tissues and organs, and are closely related to human developmental disorders and various diseases caused by various etiologies. Malignant tumors are major diseases that threaten human health. Exploring safe and effective anti-tumor treatment strategies is a very challenging topic in the field of life science research. Studies have shown that tumor angiogenesis is closely related to tumor growth, invasion, metastasis, recurrence and prognosis. The microvessel density in tumor tissue has been considered as an important indicator for predicting tumor metastasis, recurrence and p...

Claims

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Application Information

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IPC IPC(8): A61K31/216A61K31/675A61P35/00A61P35/04
CPCA61K31/216A61K31/675A61K2300/00
Inventor 穆先敏尤强施伟
Owner THE SECOND AFFILIATED HOSPITAL OF NANJING MEDICAL UNIV