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Application of vanillin in preparation of nicotinamide-N-methyltransferase inhibitor

A technology of methyltransferase and nicotinamide is applied in the field of medicine to achieve the effect of increasing mitochondrial damage, increasing ROS production, and strengthening inhibition

Pending Publication Date: 2021-03-16
ZHEJIANG UNIV
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Problems solved by technology

However, there is no relevant research on the target and molecular mechanism of vanillin in colorectal cancer, as well as the effect of synergistic colorectal cancer chemotherapy

Method used

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  • Application of vanillin in preparation of nicotinamide-N-methyltransferase inhibitor

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Embodiment 1

[0022] 1. Technical method

[0023] 1. Cell model construction and identification of NNMT modified expression

[0024] In the present invention, firstly, the colorectal cancer cell line SW480 / NNMT with stable and high expression of NNMT and the control cell line SW480 / NC were established by genetic engineering method; the colorectal cancer cell line HT-29 / shNNMT with knockdown expression of NNMT was established and the control cell line HT-29 / NC. The specific method is as follows:

[0025] The full-length cDNA sequence (SEQ ID NO.1-3) of NNMT was cloned, connected with the pcDNA3.1+ plasmid vector, and the eukaryotic expression vector pcDNA3.1+ / NNMT was constructed; the colorectal cancer cell line SW480 was transfected, screened and isolated Cell lines were cloned, and cell lines with stable and high expression of NNMT were identified; at the same time, SW480 cell line transfected with pcDNA3.1 + empty plasmid was established as a control.

[0026] Design multiple pairs of ...

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Abstract

The invention discloses an application of vanillin in preparation of a nicotinamide-N-methyltransferase inhibitor. The inhibitor is prepared from traditional Chinese medicine monomer vanillin and pharmaceutically acceptable auxiliary materials. According to the invention, proliferation of various colorectal cancer cell strains is inhibited by inhibiting the expression of NNMT and enzyme activity in vitro and vivo, and an anti-tumor effect is achieved. Studies show that vanillin can weaken the drug resistance of colorectal cancer cell strains to 5-FU caused by high expression of NNMT in vitro,so that the chemotherapy sensitivity is enhanced; the apoptosis of the colorectal cancer cell strains with high expression of NNMT is increased by inducing ROS production and mitochondrial damage in cells; and the inhibitory effect of 5-fluorouracil on tumor proliferation and the apoptosis rate can be improved, so as to enhance the chemotherapy effect. The vanillin can be used as an NNMT inhibitorfor preparing anti-colorectal cancer drugs or adjuvant chemotherapy drugs, and has a good application prospect.

Description

technical field [0001] The invention relates to the technical field of medicine, relates to the application of vanillin in the preparation of nicotinamide-N-methyltransferase inhibitors, and is a method of preventing and treating colorectal cancer by using vanillin, a monomer of traditional Chinese medicine, as an NNMT inhibitor. Background technique [0002] The incidence and mortality of colorectal cancer in the world are increasing year by year. The incidence and mortality of colorectal cancer in my country rank among the top five among all cancers and continue to rise. Chemotherapy is one of the important measures for the clinical treatment of malignant tumors. Chemotherapy resistance is the main reason for the poor prognosis of colorectal cancer chemotherapy. problems that urgently need to be resolved. my country is rich in medicinal plant resources, and traditional Chinese medicine monomers have the advantages of safety and effectiveness, making them an important sour...

Claims

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Application Information

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IPC IPC(8): A61K31/12A61K45/06A61P35/00
CPCA61K31/12A61K45/06A61P35/00
Inventor 张钧李国丽谢鑫友于海涛童庆超曾进
Owner ZHEJIANG UNIV
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