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Application of cucurbitacine I

A technology of cucurbitacin and macrophages, applied in the field of biomedicine, can solve problems such as adverse events and enhance the prognosis of patients, and achieve the effects of inhibiting immunosuppression, tumor killing and immune activation expansion

Pending Publication Date: 2022-03-01
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

M1 and M2 types describe two opposite biological characteristics of macrophages. M1 type macrophages can inhibit cell proliferation and cause tissue damage, and are key effector cells to eliminate pathogens, viral infections, and cancer cells, while M2 type macrophages Can promote cell proliferation and tissue repair. In this mode, it can promote tumor growth to a certain extent. In the tumor microenvironment, tumor-associated macrophages are considered to be a polarized M2 phenotype, thereby enhancing tumor growth. progression and poor patient prognosis

Method used

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  • Application of cucurbitacine I
  • Application of cucurbitacine I
  • Application of cucurbitacine I

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Example 1 Cucurbitacin I promotes the increase of M1-related factors and the decrease of M2-related factors in tumor-induced macrophages

[0045] 1. PMA (phorbol ester-12-myristate-13-acetate) treatment successfully differentiated THP-1 cells: the content of CD68 in differentiated macrophages was known to increase, and RNA samples were collected for QCPR to detect whether they were differentiated success. Will 1*10 6 THP-1 mononuclear cells were inoculated in six-well plates, treated with 100ng / mL PMA for 48 hours to stimulate differentiation, continued to culture for 24-48 hours to remove the influence of PMA, and observed the state of the cells, see figure 1 and collect RNA samples from untreated macrophages and treated macrophages, and perform QPCR detection of differentiation-related factor CD68. The specific steps are as follows:

[0046] The method of RNA extraction is as follows:

[0047] (1) After adding Trizol, place it at room temperature for 5 minutes to f...

Embodiment 2

[0059] Example 2 Cucurbitacin I promotes the M1 polarization of macrophages induced by PMA

[0060] 1. Immunofluorescence experiment: the multi-channel high-resolution detection of fluorescence microscope is used, and the corresponding antigens on the cell surface are checked by using fluorescent antibodies as probes. The location and expression of different antigens in the cells can be determined, thereby determining the polarization of macrophages. Condition. The co-culture system was carried out using cell culture inserts (0.3 μm), and THP-1 monocytes (1×10 6 cells / mL) were inoculated into the upper chamber of the transwell device and treated with 100 ng / mL PMA for 72 hours to stimulate differentiation. The cells were washed 3 times with phosphate-buffered saline (PBS) and incubated for 24 h to exclude the interference of PMA. At the same time, the co-culture system was divided into two groups, one group was differentiated macrophages without any treatment, and the other ...

Embodiment 3

[0062] Example 3 The killing effect of cucurbitacin I on clear cell renal cell carcinoma 786-O has significant time and dose dependence

[0063] 1. Renal clear cell carcinoma cell line 786-O was inoculated into a 96-well plate at a density of 8000 cells per well for overnight culture, and each group included three parallels. The cells were treated with different concentrations (0, 0.25, 0.5, 1, 2, 4, 8, 16, 32, 64 μM) of the drug (cucurbitacin I), and then incubated at 37°C for 24-48 hours under the cultured cells. Drug-free dimethyl sulfoxide (DMSO) treatment was used as a control, and a blank group was set at the same time. One hour before the end of incubation, 10 μL of CCK-8 reagent was added to each well, and the absorbance was measured at 450 nm after incubation for one hour.

[0064] 2. The test results showed that cucurbitacin I significantly inhibited the viability of the 786-O cell line in a dose- and time-dependent manner ( Figure 5 ). The anti-proliferative eff...

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Abstract

The invention discloses application of cucurbitacine I, and belongs to the technical field of biomedicine. Experiments prove that cucurbitacine I can stimulate polarization of macrophages to M1 type and inhibit polarization of macrophages to M2 type to a certain extent in THP-1 derived macrophages. Meanwhile, the cucurbitacin I can also up-regulate the expression of factors such as TNF (Tumor Necrosis Factor) and iNOS (Induced Nitric Oxide Synthase) and down-regulate the expression of factors such as TGF-beta The invention finds that cucurbitacin I can be used as a novel M1 type macrophage activator / M2 type macrophage inhibitor, is a potential new anti-cancer drug aiming at macrophages in a tumor microenvironment, and can be used as an effective active component for preparing medicaments for various cancers such as liver cancer, kidney cancer, breast cancer, colorectal cancer and the like. The immunosuppressive effect generated by various factors in the tumor microenvironment can be inhibited, and the possibility of cancer treatment is further expanded from the two aspects of tumor killing and immune activation.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to an application of cucurbitacin I. Background technique [0002] Solid tumors include not only malignant cells, but also extracellular matrix and many other non-malignant cell types, including fibroblasts, endothelial cells, and inflammatory cells such as macrophages, neutrophils, mast cells, and lymphocytes, among others. Tumor promotes its own development through multiple mechanisms such as malignant proliferation, invasion and metastasis, and immune evasion, and creates a tumor microenvironment (TME) for itself to further resist the body's immunity and maintain development. Conventional treatments are still ineffective for many cancers. It is now clear that most malignant tumors contain large numbers of macrophages as a major component of host leukocyte infiltration and are key members of the stromal cells. It is now generally recognized that tumor-associated ...

Claims

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Application Information

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IPC IPC(8): A61K31/575A61P35/00A61P35/04
CPCA61K31/575A61P35/00A61P35/04
Inventor 杜红丽龚小程魏晋奋
Owner SOUTH CHINA UNIV OF TECH
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