Application of combretastatin

A use and drug technology, applied in the new use field of comproprietine, can solve problems such as targeted drug use and lack of tumor blood vessels

Inactive Publication Date: 2009-11-18
ZHEJIANG DADE PHARMACEUTICAL GROUP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The so-called angiogenesis inhibitors inhibit the formation of blood vessels, but there are no targeted drugs available for the tumor blood vessels that have grown

Method used

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  • Application of combretastatin
  • Application of combretastatin
  • Application of combretastatin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Efficacy of compridine on human colon cancer Ls174t xenografted tumor in nude mice

[0062] Cell culture: culture human colon cancer cell Ls-174t (purchased from Shanghai Institute of Materia Medica, mouse solid tumor) in vitro, and keep the cells in the logarithmic growth phase.

[0063] Transplantation: The prepared cells were inoculated subcutaneously in nude mice, and passaged 2-3 times after tumor formation.

[0064] Inoculation: Under sterile conditions, the tumor mass was inoculated into the underarm of one side of the animal.

[0065] Grouping and dose setting: Use a vernier caliper to measure the diameter of the transplanted tumor in nude mice, and wait until the tumor grows to 100-300mm 3 Afterwards, the animals were randomly grouped.

[0066] Administration route and time: choose with 80-200mm 3 Nude mice with large and small tumors were randomly divided into groups, and administered after the tumor volume was measured.

[0067] Intravenous administration...

Embodiment 2

[0088] Effects of compridine on the proliferation of human umbilical vein endothelial cells

[0089] Test reagents, drugs and instruments: HUVEC: human umbilical vein endothelial cells. Cells were purchased from ATCC, USA. The number of cell passages in the experiment did not exceed 6 generations.

[0090] Culture conditions: M199 medium, 20% fetal bovine serum, endothelial cell growth stimulating shadow, VEGF10ng / ml. M199, endothelial cell growth stimulating factor (ECSF) was purchased from GibcoBRL; trypsin was purchased from DIFCO; fetal bovine serum was purchased from Hyclone; microplate reader: POLARstar model, product of BMG, Germany; sultamine B was purchased from Sigma.

[0091] Test Method: Cell Proliferation Analysis: Sultanamine B method, ie SRB method.

[0092] The main test steps of SRB method:

[0093] i) The cells were cultured with 10% fetal bovine serum, and digested with 0.2% trypsin digestion solution during passage, so that the cells were always in the ...

Embodiment 3

[0108] Effect of compridine on blood flow of tumor tissue

[0109] After one week of adaptation, the nude mice were subcutaneously inoculated with human colon cancer Ls174t cells. After the tumor grew to 0.5 cm3, they were randomly divided into groups, with 5 mice in each group. The mice were intravenously injected with 100 mg / kg of compridine, with an injection volume of 10 ml / kg, and the control group was injected with the same volume of normal saline. 1, 6, and 24 hours after the administration of compridine, the mice were intravenously injected with Hoechst3334 210 mg / kg again. After 1 minute, the mice were killed by neck dislocation, and the tumors were taken out, quickly frozen in liquid nitrogen, and made into cryosections. Three slices were taken from each tumor, respectively in the middle and outer 1 / 3, and the thickness of the slices was 10 μM. The number of stained positive (blue fluorescent) spots was counted under a fluorescent microscope. The excitation wavelen...

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Abstract

The invention discloses the application of a compound shown as a formula I or a formula II. The application is characterized in that the compound is used for preparing medicine for destroying tumor vessels.

Description

technical field [0001] The invention relates to the field of medicines, in particular to the new application of compridine. Background technique [0002] More than one hundred years ago, it was discovered that tumor tissue is richer in blood vessels than normal tissue, but people have been debating whether the tumor is nourished by existing blood vessels or by new blood vessels, and it is generally believed that this vascular response is just a This inflammatory response is not necessary for tumor growth. In 1971, Folkman first proposed the Angiogenesis Theory, and boldly made the following assumptions: the survival of tumors depends on the formation of new blood vessels, the tumor can actively stimulate the formation of such blood vessels, and the tumor can secrete certain substances to induce blood vessels to grow towards them. And can grow branches (Folkman J. Tumorangiogenesis [J]. Adv Cancer Res, 1985, 43: 175-203). But this view was not accepted by people at the time...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/09A61K31/661A61P35/00
Inventor 王建国沈卫平
Owner ZHEJIANG DADE PHARMACEUTICAL GROUP CO LTD
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