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Application of wheat flavone in preparation of antitumor drugs

An anti-tumor drug, tricin technology, applied in the field of medicine, can solve the problem of no cure for KRAS mutation and other problems

Pending Publication Date: 2021-08-03
MACAU UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Scientists have been working on developing drugs targeting KRAS mutations for a long time, but there is still no cure for KRAS mutations, and the reported new small molecule inhibitors may have some serious side effects

Method used

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  • Application of wheat flavone in preparation of antitumor drugs
  • Application of wheat flavone in preparation of antitumor drugs
  • Application of wheat flavone in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: Establishment and intervention of tumor-bearing mouse model

[0033] Preparation of lung cancer subcutaneous xenograft tumor model: lung cancer cell line LLC cultured and passaged. Cells were collected in the logarithmic phase of the cells, and the concentration was 5×10 5 Each cell suspension in 100 μL was subcutaneously injected into the right forelimb of C57BL / 6J mice, and the tumor grew to a volume > 50 mm after about 7 days 3 , which means successful tumor grafting.

[0034] After successful tumor inoculation, the mice were randomly divided into 4 groups, 6-7 in each group, and each specific group was: 1) control group (PBS group); 2) positive control cisplatin group (2 mg / kg); 3) High-dose group of ticlavone (50 mg / kg); 4) Low-dose group of ticlavone (25 mg / kg). The PBS control group and the high-dose and low-dose ticlavone groups were intraperitoneally injected once a day, 0.2 ml each time, and the tumor volume was measured and body weight was measu...

Embodiment 2

[0036] Embodiment 2: MTT test

[0037]HepG2, HCT-8, U-87MG, Miapaca-2, LLC, H2122, H358 and CCD-19Lu cells were seeded in 96-well microplates (3000-5000 cells / well). After the cells adhered, add 100 microliters of different concentrations (150, 75, 37.5, 18.75 and 9.375 micromole / liter) of tricoflavone as the test group, and DMSO as the control group; incubate for 72 hours, then add 10 microliters MTT solution with a concentration of 0.5 mg / ml was incubated in a 37°C incubator for 4 hours. After 4 hours, the supernatant was sucked off, 100 microliters of dimethyl sulfoxide (SDS) was added, and the absorbance was measured at wavelengths of 570 nm and 650 nm with an absorbance meter. IC50 was calculated using GraphPadPrism 7.0 software, and the above experiments were carried out three times independently.

[0038] Test results such as figure 2 Shown, where A-H represent LLC (mouse Lewis lung cancer cells), H2122 (human KRAS G12C mutant lung cancer cells), H358 (human KRAS ...

Embodiment 3

[0039] Embodiment 3: Colony formation experiment

[0040] LLC cells were seeded in 6-well plates with 500 cells per well. After the cells adhered, they were incubated in tricoflavone medium containing different concentrations (0, 12.5, 25, 50, 100 micromol / liter) for about 10 days, and the medium was replaced every three days. When colony formation was evident, LLC cells were fixed with 4% paraformaldehyde (PFA) for 30 min at 4°C. Then stain with crystal violet solution for at least 30 minutes. After washing away the crystal violet solution, the colonies were photographed.

[0041] The result is as image 3 as shown, image 3 Middle A shows that ceflavone shows a dose-dependent effect on the colony formation of LLC cells; image 3 Middle B shows that ceflavone shows a dose-dependent effect on the migration of LLC cells; image 3 Middle C represents the statistical results of the migration distance of LLC cells. All experiments were carried out independently three times, ...

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Abstract

The invention belongs to the field of medicines, and discloses application of wheat flavone in preparation of antitumor drugs, and tumors include lung cancer, glioma and pancreatic cancer. The wheat flavone provided by the invention has the effects of inhibiting a PRKCA / SPHK / S1P signal channel and an anti-apoptosis signal channel, and can effectively and obviously inhibit the growth of various tumors, especially KRAS lung cancer mutant tumor cells. The wheat flavone can also be used as a KRAS mutation inhibitor, a PRKCA inhibitor or an S1P regulator to regulate cell growth and apoptosis processes.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of tricoflavone in the preparation of antitumor drugs. Background technique [0002] Lung cancer is a serious threat to human health, with high morbidity and mortality, among which non-small cell lung cancer (NSCLC) is a relatively common type of lung cancer. Existing studies have shown that the occurrence of non-small cell lung cancer is closely related to the mutation of cancer gene KRAS. Scientists have long been committed to developing drugs targeting KRAS mutations, but there is still no cure for KRAS mutations, and the reported new small molecule inhibitors may have some serious side effects. [0003] PRKCA is one of the 10 members of the protein kinase C family. In many tumor types including NSCLC, PRKCA plays an important role in regulating cell invasion, proliferation and apoptosis. PRKCA is also highly expressed in NSCLC patients, so inhibiting PRKC...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P35/00A61P35/04
CPCA61K31/352A61P35/00A61P35/04
Inventor 颜培宇梁丽娴周华李润泽李佳馨谢莹刘良
Owner MACAU UNIV OF SCI & TECH
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