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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
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Problems solved by technology

However, due to its simple structure and multiple active sites, it is not suitable for the identification of targets by classical avidin-biotin-labeled affinity chromatography based on structural modification, and its direct target protein is still unclear

Method used

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  • Use of oroxylin A as transketolase inhibitor
  • Use of oroxylin A as transketolase inhibitor
  • Use of oroxylin A as transketolase inhibitor

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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...

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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

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Application Information

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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
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