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Application of GL-V9 in preparation of anti-melanoma drugs

A GL-V9 and anti-melanin technology, applied in the field of anti-tumor drugs, can solve the problems of lack of specific treatment, drug resistance, poor prognosis, etc., and achieve the effect of promoting early and late apoptosis

Inactive Publication Date: 2021-08-13
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Temozolomide and dacarbazine are commonly used drugs in anti-melanoma chemotherapy, but their treatment efficiency is low and the prognosis is poor
The most common oncogene in melanoma is the BRAF gene, and related BRAF inhibitors, such as sorafenib, vemurafenib, dabrafenib and other drugs, can induce melanoma metastasis and rapid regression, however, usually most Patient develops resistance to BRAF monotherapy after 6 months
Immunotherapy can improve the immune response of melanoma patients, but its clinical application is still limited by severe toxic side effects
Therefore, the effective treatment methods for malignant melanoma are relatively limited. Except for early surgical resection, the effect of general radiation therapy and chemotherapy is not good, and it is accompanied by a high degree of metastasis, lack of specific treatment, and poor prognosis. Natural medicinal materials that can help melanoma treatment is an important topic at present

Method used

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  • Application of GL-V9 in preparation of anti-melanoma drugs
  • Application of GL-V9 in preparation of anti-melanoma drugs
  • Application of GL-V9 in preparation of anti-melanoma drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment 1 MTT experiment

[0044] MTT solution can be reduced to blue-purple crystalline formazan by mitochondrial dehydrogenase in living cells, DMSO can dissolve formazan, and the color of the formed solution is directly proportional to cell viability, which can be used to detect cell viability. Cells were cultured in a 96-well ELISA plate according to the appropriate cell density, and the volume of cells in each well was 100 μl, and 100 μl of GL-V9 at a specified concentration was added to it at the same time; the cells given the drug were continued to be cultured in the incubator for 24 hours Afterwards, 20 μl MTT solution was added to each well; the supernatant was removed after continued incubation for 4 h, and 100 μl DMSO was added to each well, placed in a micro-oscillator to vibrate, and after the crystals were completely dissolved, the absorbance was detected with a wavelength of 570 nm. After sorting out the detected absorbance values, calculate the growth...

Embodiment 2

[0047] Example 2 Annexin V / PI apoptosis double staining experiment

[0048] After the specified time of drug action, centrifuge at 2000rpm for 5min to collect the cell suspension, discard the medium, wash the cells twice with pre-cooled PBS solution, add 400μL 1×Binding Buffer to suspend the cells, and the cell density is about 1×10 6 individual / mL. Add 5 μL of Annexin V to the cell suspension of each group, mix gently and incubate at 2-8°C in the dark for 15 minutes, then add 5 μL of PI, mix gently and incubate at 2-8°C in the dark for 5 minutes. Within 1 h, it was detected by flow cytometry.

[0049] The effect of different doses of natural product derivative GL-V9 on the apoptosis of human melanoma cell line A375 was determined by flow cytometry. The results of Annexin V / PI double staining experiment showed that ( figure 2 ), GL-V9 can significantly promote early and late apoptosis of A375 cells. This result preliminarily confirmed that GL-V9 can induce cell apoptosis ...

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Abstract

The invention provides an application of a flavonoid derivative GL-V9 in preparation of anti-melanoma drugs. Further research finds that the GL-V9 can significantly inhibit the growth activity of human melanoma A375 cells, and the inhibition rate of the GL-V9 can be close to 100% under a proper concentration condition. Moreover, the GL-V9 can significantly promote early and late apoptosis of A375 cells, and has application prospects in development of anti-melanoma drugs.

Description

technical field [0001] The invention belongs to the field of antitumor drugs, and in particular relates to the application of a GL-V9 compound in the preparation of anti-melanoma drugs. Background technique [0002] Melanoma is a highly malignant tumor derived from melanocytes, referred to as melanoma for short, mostly occurs in the skin, and can also be found in mucous membranes and internal organs, accounting for about 3% of all tumors. Cutaneous malignant melanoma accounts for the third place among skin malignant tumors (about 6.8%-20%). It occurs more frequently in adults and is more common in fair-skinned Caucasians than in dark-skinned Asians and Africans. It is rarely seen in children. Some patients have familial multiples. Malignant melanoma can evolve from congenital or acquired benign melanocytic nevi, or malignant transformation from dysplastic nevi, or it can be new. In recent years, the incidence and mortality of malignant melanoma have increased year by year...

Claims

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Application Information

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IPC IPC(8): A61K31/4025A61P35/00
CPCA61K31/4025A61P35/00
Inventor 郭青龙惠慧李慧杨林周煜新魏立彬张小博徐澍吴焘高源
Owner CHINA PHARM UNIV
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