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Application of a diterpene compound in the preparation of drugs or health products with anti-tumor effect

A technology of compound and diterpene, which is applied in the field of medicinal chemistry, can solve the problem of unreported inhibition of blood vessels and achieve good effects of angiogenesis

Active Publication Date: 2018-07-31
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Penduliflaworosin compound is a diterpenoid isolated from Euphorbiaceae Croton genus Crotoncrassifolius Geisel. There is no report in the prior art that it has the effect of inhibiting angiogenesis

Method used

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  • Application of a diterpene compound in the preparation of drugs or health products with anti-tumor effect
  • Application of a diterpene compound in the preparation of drugs or health products with anti-tumor effect
  • Application of a diterpene compound in the preparation of drugs or health products with anti-tumor effect

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1: Using the zebrafish (wild type) animal model, the angiogenesis-inhibiting activity of the compound is determined by quantitative endogenous alkaline phosphatase experiment

[0021] (1) Preparation of zebrafish embryos: put healthy male zebrafish and female zebrafish into a fish matching tank at a ratio of one to one for fish matching. Embryos were collected, put into embryo culture solution (0.2 g / L sea salt water) and cultured in an incubator at 28.5° C. for use.

[0022] (2) Administration: After the embryos were cultured for 24 hours (24hpf), the membranes of the embryos were removed with tweezers, and then the embryos were placed in a 96-well plate, one embryo per well, and 100 μL of embryo culture solution was added to each well. Blank group: fish eggs and 100 μL culture solution containing 0.2% DMSO. Drug group: fish eggs and 100 μL culture solution containing different concentrations of pendulilaworosin. Positive control group: fish eggs and 100 μ...

Embodiment 2

[0025] Example 2: Using a transgenic fluorescent zebrafish (Tg(fli1a:EGFP)y1 type) model to observe the effects of compounds on angiogenesis

[0026] (1) Preparation of zebrafish embryos: put healthy male zebrafish and female zebrafish into a fish matching tank at a ratio of one to one for fish matching. Embryos were collected, put into embryo culture solution (0.2 g / L sea salt water) and cultured in an incubator at 28.5° C. for use.

[0027] (2) Administration: After the embryos were cultured for 24 hours (24hpf), the membranes of the embryos were removed with tweezers, and then the embryos were placed in a 96-well plate, one embryo per well, and 100 μL of embryo culture solution was added to each well. Blank group: fish eggs and 100 μL culture solution containing 0.2% DMSO. Drug group: fish eggs and 100 μL culture solution containing different concentrations of pendulilaworosin.

[0028] (3) Experimental results: The whole process of blood vessel formation was further obse...

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Abstract

The invention relates to the field of medicinal chemistry, and in particular discloses application of a diterpene compound in preparing a medicine or a health care product having an anti-tumor effect. The diterpene compound has a structure which is as shown in the description. Experimental data show that the diterpene compound penduliflaworosin disclosed by the invention has a good inhibitory effect on angiogenesis, and the effect is equivalent to that of a positive control medicine SU5416 (semaxanib); therefore, the diterpene compound can be further used for preparing an anti-tumor medicine.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to the application of a diterpene compound in the preparation of medicines or health care products with antitumor effects. Background technique [0002] Angiogenesis refers to the growth of new capillary blood vessels from pre-existing capillaries and postcapillary venules. Tumor angiogenesis is an extremely complex process, which generally includes steps such as degradation of vascular endothelial matrix, migration of endothelial cells, proliferation of endothelial cells, formation of vascular rings by branching of endothelial cells, and formation of new basement membranes. Due to the abnormal structure and function of new blood vessels in tumor tissue, and the imperfect vascular matrix, such microvessels are prone to leakage. Therefore, tumor cells do not need to go through a complicated invasion process, directly penetrate into blood vessels and enter the blood stre...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/365A23L33/105A61P35/00
CPCA23V2002/00A61K31/365A23V2200/308A23V2250/20
Inventor 黄伟欢王国才李药兰
Owner JINAN UNIVERSITY