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Application of icaritin hydrate for preparing medicine capable of inhibiting STAT3 (Signal Transducer and Activator 3 of Transcription) signal pathway and preventing and curing oral carcinoma

A technology of hydrating icariin and signaling pathway, applied in the field of medicine, can solve the problem that the five-year survival rate of oral cancer patients is not significantly improved, and achieve the effects of inducing cancer cell apoptosis, inhibiting proliferation, and low biological toxicity.

Inactive Publication Date: 2019-12-03
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to its high regional metastasis, local recurrence and resistance to chemotherapy, the five-year survival rate of oral cancer patients has not improved significantly

Method used

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  • Application of icaritin hydrate for preparing medicine capable of inhibiting STAT3 (Signal Transducer and Activator 3 of Transcription) signal pathway and preventing and curing oral carcinoma
  • Application of icaritin hydrate for preparing medicine capable of inhibiting STAT3 (Signal Transducer and Activator 3 of Transcription) signal pathway and preventing and curing oral carcinoma
  • Application of icaritin hydrate for preparing medicine capable of inhibiting STAT3 (Signal Transducer and Activator 3 of Transcription) signal pathway and preventing and curing oral carcinoma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Application of icariin hydrate in inhibiting STAT3 signaling pathway in oral cancer cells.

[0045] The specific method is as follows:

[0046] Protein extraction, concentration determination and denaturation: After cultivating oral cancer cells with icariin hydrate at various concentrations (0, 2 μM, 4 μM, 8 μM, 16 μM) for a specified time, add 100 μL of lysate to a 10 cm dish, operate on ice, and collect oral cavity Cancer cell lysate. The cell lysate was then transferred to an EP tube, and protease inhibitors (lysate: PMSF = 100:1) were added. Place the EP tube in a centrifuge at 4°C and centrifuge at 12000 r.p.m. for 15 minutes; absorb the supernatant and transfer it to a new EP tube; detect the protein concentration by BCA method; dilute the protein sample according to the required concentration, generally 4 μg / μL; According to the ratio of protein sample solution:protein sample solution 1:4, add protein sample solution; heat at 96°C for 10min to denature the pro...

Embodiment 2

[0059] Effects of icariin hydrate on autophagy in oral cancer cells.

[0060] The specific method is as follows:

[0061] Cell autophagy MDC staining detection: 1×10 5 Oral cancer cells were inoculated in a 24-well plate with sterilized slides according to the conventional method; when the cell density reached 60%-70%, the culture medium was discarded, and the prepared concentrations (0, 2 μM, 4 μM, 8 μM, 16 μM) hydrated epimeditin for 48 hours, and 1 μM rapamycin for 3 hours as a positive control; discard the supernatant and carefully wash twice with PBS. Add 100 μL of MDC working solution (final concentration 50 nM) to each well, and incubate in the incubator for 30 minutes in the dark; discard the staining solution, wash twice with PBS, and quickly bring it into the microscope room; take out the slides, place them under a fluorescent microscope, and quickly Observe the occurrence of autophagy and take pictures.

[0062] At the same time, the effect of icariin hydrate on ...

Embodiment 3

[0065] Application of icariin hydrate in the prevention and treatment of oral cancer.

[0066] In vivo experiment:

[0067] (1) To investigate the inhibitory effect of icariin hydrate on the growth of oral cancer cells.

[0068] The specific method is as follows:

[0069] Inoculate the cells of the experimental group and the control group in a 96-well plate, each well containing oral cancer cells 3×10 3 Each time period of the experimental group and the control group was set up with 6 multiple wells; put them into the incubator, at 37 ℃, 5% CO 2 Cultured for 24 hours under certain conditions to allow the cells to adhere to the wall; replace the medium with hydrated icariin at various concentrations (0, 2 μM, 4 μM, 8 μM, 16 μM); incubate the culture plate in the incubator for the specified time for 24, 48, and 72 hours ; Change 100 μL of the mixed solution in each well, that is, cell suspension + drug solution + CCK8 = 100 μL, wherein CCK8 accounts for 10%; incubate the cult...

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Abstract

The invention belongs to the field of medicines, and particularly relates to an application of an icaritin hydrate for preparing a medicine capable of inhibiting a STAT3 (Signal Transducer and Activator 3 of Transcription) signal pathway and preventing and curing an oral carcinoma, in particular to the application of the icaritin hydrate of a formula I for preparing the medicine capable of inhibiting the STAT3 signal pathway. The icaritin hydrate of the embodiment of the invention can inhibit the STAT3 and the protein phosphorylation of an upstream pathway JAK2 (Janus Kinase 2) of the STAT3 inoral carcinoma cells, accelerates autophagic vacuole to be increased, accelerates an autophagy-related labelled protein to be transformed to LC3 (light chain)-II from LC3-I, increases the expressionof BECN1 and ATG9 proteins, and reduces the expression of an autophagy-related labelled protein p62 / SQSTM1. The invention takes an amphipathic block high-molecular polymer as a carrier to prepare an icaritin hydrate nanometer medicine preparation, the water solubility of the medicine is enhanced, encapsulation efficiency is 80% and above, an effect on inhibiting the oral carcinoma is better, and in addition, biotoxicity is small.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of hydrated icariin in the preparation of drugs for inhibiting STAT3 signal pathway and preventing and treating oral cancer. [0002] technical background [0003] Oral cancer is one of the most common head and neck cancers in the world, among which oral squamous cell carcinoma (OSCC) accounts for more than 90% of oral cancer, and its incidence rate shows a clear upward trend, which has become a common concern in the world one of the public health problems. The molecular mechanism of the occurrence and development of oral cancer is still unclear, and the treatment options are still surgery and radiotherapy and chemotherapy. Due to its high regional metastasis, local recurrence and resistance to chemotherapy, the five-year survival rate of oral cancer patients has not improved significantly. Therefore, it is imperative to develop new safe and effective drugs fo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K9/51A61K47/34A61P35/00A61P35/04
CPCA61K9/5153A61K31/352A61P35/00A61P35/04
Inventor 周刚杨建光谭雅芹
Owner WUHAN UNIV
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