Use of oroxylin A as transketolase inhibitor

A technology of transketolase and melaleuca, which is applied in the field of biomedicine and can solve the problem of unclear target protein and the like

Pending Publication Date: 2018-07-24
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
View PDF2 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to its simple structure and multiple active sites, it is not suitable for the identification of targets by classica

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Use of oroxylin A as transketolase inhibitor
  • Use of oroxylin A as transketolase inhibitor
  • Use of oroxylin A as transketolase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] 1. Materials and methods

[0060] 1.1 Reagents and materials

[0061] Melaleucain A was purchased from Shanghai Standard Biotechnology Co., Ltd. (Shanghai, China) (purity ≥ 98%), made into a 20 mM stock solution with dimethyl sulfoxide (DMSO), and stored at -20°C. The human liver cancer cell line HepG2 was purchased from the Cell Bank of the Shanghai Branch of the Chinese Academy of Sciences. Dulbecco's modified Eagle's medium (DMEM) and phosphate buffered saline (PBS) were purchased from Hyclone (Thermo Fisher), and fetal bovine serum (FBS) was purchased from Gibco Life Technology Co (Australia). DMSO, penicillin streptomycin and trypsin were purchased from Gibco-BRL Co (Rockville, MD, USA). Ultrapure water was prepared with a Milli-Q Academic A10 water purification system (Millipore, Bedford, MA, USA). Unless otherwise stated, all chemicals were purchased from Sigma-Aldrich (St. Louis, MO, USA) and all were of analytical grade. The primary antibodies of p53, caspa...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention discloses a use of oroxylin A as a transketolase inhibitor. The transketolase inhibitor is used for treating cancer. The use of the transketolase inhibitor for treating the cancer is realized by inhibiting the activity and expression of the transketolase to inhibit a non-oxidize pentose phosphate pathway and activate a p53 signal channel, thereby playing an antitumor effect. DARTS isused for identifying a target protein directly combined with oroxylin A in the human liver cancer cell HepG2, a key enzyme-transketolase of the non-oxidize pentose phosphate pathway is discovered andis a direct combined target point of the oroxylin A, a KD value is 11.2 microM, and the interactive effect is proved by virtue of the molecular docking, enzymatic activity determination, protein expression and the antitumor effect variation after the transketolase interference. The research result shows that the oroxylin A is an effective transketolase inhibitor.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and relates to an application of kellin A, in particular to an application of kellin A as a transketolase inhibitor. Background technique [0002] Hepatocellular carcinoma is the most common malignant tumor in the world, commonly known as "the king of cancer", and effective treatment is urgently needed. In the proliferation of malignant tumor cells, 80% of the ribose used in RNA and DNA biosynthesis comes from the non-oxidative pentose phosphate pathway, which is crucial for tumor survival and proliferation. Enzymes that catalyze the non-oxidative pentose phosphate pathway are reversible, determine the direction of glucose metabolic flux, and are attractive potential therapeutic targets for cancer. However, there are no drugs that efficiently target the non-oxidative pentose phosphate pathway. [0003] Traditional Chinese medicine is the treasure of the Chinese nation. It contains a large n...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K31/352A61P35/00A61P35/02
Inventor 贾丹陈啸飞朱臻宇柴逸峰张川
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap