Application of dihydroergomine in preparation of antitumor drugs

A technology of dihydroergotamine and anti-tumor drugs, which is applied in the direction of anti-tumor drugs, drug combinations, active ingredients of heterocyclic compounds, etc., and can solve problems such as the lack of anti-tumor therapeutic effects of dihydroergotamine

Pending Publication Date: 2021-07-30
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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  • Application of dihydroergomine in preparation of antitumor drugs
  • Application of dihydroergomine in preparation of antitumor drugs
  • Application of dihydroergomine in preparation of antitumor drugs

Examples

Experimental program
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Embodiment 1

[0044] 1. Cell culture and plating: the high-glucose DMEM medium containing 10% fetal bovine serum is used to cultivate Huh7 and MHCC-97H liver cancer cells, and the Huh7 and MHCC-97H liver cancer cells in the logarithmic growth phase are inoculated at 6000 cells / well. in a 96-well plate.

[0045] 2. Drug treatment: After the liver cancer cells adhere to the wall, dihydroergotamine drug is diluted to treat the cells, so that the final concentration of dihydroergotamine reaches 0.078125μM, 0.15625μM, 0.3125μM, 0.625μM, 1.25μM, 2.5μM, 5μM , 10 μM, 20 μM, 40 μM, 80 μM, 160 μM, 320 μM, 640 μM and 1280 μM, set 3 duplicate wells for each group, the final volume of medium in each well was 100 μL, let the drug act on the cells for 24 hours and 72 hours.

[0046] 3. Detection of cell survival rate: Prepare CCK-8 working solution according to the ratio of CCK-8 reagent (Dongren Chemical Technology): complete medium = 1:10, discard the cell culture medium in each well, and add 100 μL CCK...

Embodiment 2

[0048] 1. Construct a nude mouse subcutaneous tumor model: culture human liver cancer cells (MHCC-97H) in vitro, digest the cells in the logarithmic growth phase with trypsin, centrifuge at 800rpm×3min, wash the liver cancer cells with PBS reagent 3 times, and adjust the number of cells after counting 1×10 8 / mL, inject 100 μL of liver cancer cell suspension into the back of BALB / c nude mice (4-6 weeks old, male or female) for subsequent experiments.

[0049] 2. Grouping: the tumor of the tumor-bearing mice is about 200mm long 3 , measure the body weight and tumor volume of the mice one by one, eliminate outliers in body weight and tumor volume, and then divide the tumor-bearing mice into a control group and an experimental group randomly.

[0050] 3. Treatment: According to the weight of the mice, the experimental group (DHE / DHE 4mg / kg) was given intraperitoneal injection of 5 μL / g dihydroergot injection every day; the control group (control / 97H control) was given daily intr...

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Abstract

The invention belongs to the technical field of medicines, and discloses application of dihydroergomine in preparation of antitumor drugs. The invention discloses the application of dihydroergomine and/or derivatives thereof in preparation of antitumor drugs for the first time, the dihydroergomine and/or derivatives thereof can significantly inhibit proliferation of tumor tissues and have no significant influence on the body weight of a drug-administered animal, and no drug treatment side effect is observed during drug administration; the dihydroergomine and/or the derivatives thereof can significantly inhibit proliferation of tumor tissues, have no side effects and can be used for preparing the antitumor drugs.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to the application of dihydroergotamine in the preparation of antitumor medicines. Background technique [0002] Primary hepatocellular carcinoma (Hepatocellular carcinoma, HCC, referred to as liver cancer) is one of the most common malignant tumors in clinical practice, with the incidence rate ranking fourth among malignant tumors and the mortality rate ranking third. Liver cancer has the characteristics of insidious onset and rapid progression. Most patients are diagnosed at an advanced stage and lose the opportunity for radical treatment such as surgery. The 5-year survival rate is only 14.1%, which seriously threatens the lives and health of our people. Targeted drug therapy such as sorafenib and lenvatinib is the first-line treatment for advanced liver cancer, but the number of patients benefiting from the treatment is small, and patients often develop acquired dr...

Claims

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Application Information

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IPC IPC(8): A61K31/48A61P35/00
CPCA61K31/48A61P35/00
Inventor 邹雪晶刘莉宋旸张冬艳刘珊珊段志娇黎雯雯
Owner NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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