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Application of curcumenol derivative in preparation of antitumor drugs

A technology of anti-tumor drugs and derivatives, which is applied in the field of medicine and can solve the problems that there are no reports on the anti-tumor activity of curcumol derivatives

Inactive Publication Date: 2021-02-09
淮安市厚沐医疗技术咨询中心
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there is no report on the antitumor activity of the above-mentioned curcumol derivatives

Method used

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  • Application of curcumenol derivative in preparation of antitumor drugs
  • Application of curcumenol derivative in preparation of antitumor drugs
  • Application of curcumenol derivative in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Embodiment 1: in vitro experiment

[0018] 1. Materials and methods

[0019] 1. Test material

[0020] Glioma U251 cells were purchased from ATCC and cultured in RPMI 1640 medium containing 10% fetal bovine serum, 100 U / ml penicillin, and 100 μg / ml streptomycin at 37°C, 5% CO 2 Cultivate in an incubator and pass passage for 2-3 days.

[0021] Fetal bovine serum and RPMI 1640 medium were purchased from Gibco, USA.

[0022] Curcumol was purchased from Shanghai Baoman Biotechnology Co., Ltd., with an HPLC purity of ≥98%.

[0023] The chemical structures of curcumol derivatives 4a, 5a and 5b are as figure 1 As shown, it was synthesized according to the literature method, and the purity was not less than 98%.

[0024] 2. MTT method to determine the IC50 value of the compound on the inhibition of the proliferation of glioma U251 cells

[0025] Take the glioma U251 cells in the logarithmic growth phase, and use 2.5×10 per well 4 Cells were cultured in a 96-well plate at...

Embodiment 2

[0033] Embodiment 2: experiment in vivo

[0034] 1. Materials and methods

[0035] 1. Test material

[0036] Glioma U251 cells were purchased from ATCC and cultured in RPMI 1640 medium containing 10% fetal bovine serum, 100 U / ml penicillin, and 100 μg / ml streptomycin at 37°C, 5% CO 2 Cultivate in an incubator and pass passage for 2-3 days.

[0037] Fetal bovine serum and RPMI 1640 medium were purchased from Gibco, USA.

[0038] The chemical structure of curcumol derivative 4a is as figure 1 As shown, it was synthesized according to the literature method, and the purity was not less than 98%.

[0039] Male BALB / c nude mice aged 4-6 weeks, with a body weight of (20±2) g, were raised under SPF conditions for at least one week.

[0040] 2. Tumor transplantation test in nude mice

[0041] BALB / c nude mice were randomly divided into 4 groups: control group, derivative 4a low dose group, derivative 4a medium dose group and derivative 4a high dose group, 4 mice in each group. T...

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Abstract

The invention discloses application of a curcumenol derivative in preparation of antitumor drugs. Curcumenol is an important component of traditional Chinese medicine curcuma zedoary volatile oil, andis separated from various plants at present. Researches show that curcumenol has various activities and can inhibit proliferation of various tumor cells. It is found that the curcumenol derivative 4awith the chemical structure shown in the figure 1 has good inhibitory activity on glioma U251 cells and has the prospect of being developed into anti-glioma drugs.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the use of curcumol derivatives for preparing antitumor drugs. Background technique [0002] Glioma is the most common primary central nervous system tumor, accounting for about 50% of all primary intracranial tumors. The treatment of glioma is mainly surgical treatment, but because the tumor infiltrates and grows without obvious borders, the prognosis bad. Therefore, postoperative chemotherapy is very important for the prognosis of glioma after surgery. [0003] Curcumol is an important part of the volatile oil of traditional Chinese medicine Curcuma, which has been isolated from a variety of plants. Studies have shown that curcumol has various activities and can inhibit the proliferation of various tumor cells. However, the druggability of curcumol is relatively poor. Therefore, researchers have modified curcumol and prepared a variety of curcumol derivatives. The activit...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P35/00
CPCA61K31/352A61P35/00
Inventor 洪其昌其他发明人请求不公开姓名
Owner 淮安市厚沐医疗技术咨询中心
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