Chengdu Institute of Biology reveals the research results of Dendrobium nobile active ingredients targeting pyruvate carboxylase in the treatment of liver cancer

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 Metabolism is one of the main characteristics of tumors
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Tumor cells can accelerate glycolysis in an aerobic environment through the Warburg effect to provide energy for proliferation and migration

 Liver cancer is one of the important causes of cancer-related deaths worldwide, the highest incidence of cancer in the first 5 bits mortality rate of 2 Wei
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Surgical resection is a treatment method for the early stage of liver cancer, but the cure rate is not ideal, and the recurrence rate within 5 years is as high as 70%

 Dendrobium is one of our most precious Chinese herbal medicines, is respected as " Chinese nine immortality " in the first, known as " drug in gold " reputation, in our country as a folk medicine has 2300 years of history, has medicinal value there are 30 more than species, including Mount Holyoke Dendrobium, Dendrobium, drumstick Dendrobium and Dendrobium nobile and so on .
These plants are considered to be the nourishing " top grades " of Chinese medicine and have a variety of pharmacological effects, including anti-tumor, anti-aging, anti-diabetic and anti-inflammatory .
Erianin is a natural bibenzyl compound extracted from Dendrobium, and it is the quality standard component of Dendrobium Dendrobium in the Chinese Pharmacopoeia .
Studies have shown that Erianin has a strong effect on colon cancer, gastric cancer, lung cancer and bladder cancer, but its direct action target protein in the body and its molecular mechanism are not clear, which limits the understanding of the pharmacological effects of Dendrobium .

 Researcher Wang Fei’s team found that Erianin has excellent in vitro and in vivo anti-hepatocarcinoma proliferation and metastasis activities, and further uses photoaffinity labeling-click chemistry-based probe technology.

the PC determines intracellular target directly Erianin, which inhibits PC activity the IC ₅₀ value of ~ 9 nM, is by far the best activity reported PC activity of the best synthetic inhibitors (previously reported PC Inhibitor IC ₅₀ value ~ 1 μ M ) .
Through research methods such as transcriptome and metabolome, it is found that Erianin regulates the expression of cancer-related genes through PC and induces changes in metabolic intermediates, thereby promoting mitochondrial oxidative stress, inhibiting glycolysis, and leading to insufficient energy for cell proliferation, thereby Inhibit the proliferation and metastasis of liver cancer cells .
Through the activity determination and molecular docking of 14 natural small molecule compounds extracted from Dendrobium and the Erianin structure, it is found that some compounds also have good PC inhibitory activity and anti-tumor activity .
This study revealed for the first time that the intracellular target of Erianin is PC , and clarified that Erianin passes through PC.

 Researcher Wang Fei, Researcher Zhang Guolin, and Associate Researcher Jiao Wei are the co-corresponding authors of this paper
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Yuwen Sheng and Dr.
Yuwen Chen are the first authors of this article

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