2. Academic Validation
  3. Vialinin A and thelephantin G, potent inhibitors of tumor necrosis factor-α production, inhibit sentrin/SUMO-specific protease 1 enzymatic activity

Vialinin A and thelephantin G, potent inhibitors of tumor necrosis factor-α production, inhibit sentrin/SUMO-specific protease 1 enzymatic activity

  • Bioorg Med Chem Lett. 2016 Sep 1;26(17):4237-40. doi: 10.1016/j.bmcl.2016.07.051.
Yasukiyo Yoshioka 1,  Daisuke Namiki 2,  Mao Makiuchi 2,  Kouichi Sugaya 2,  Jun-Ichi Onose 2,  Hitoshi Ashida 3,  Naoki Abe 4
Affiliations

Affiliations

  • 1 Department of Nutritional Science and Food Safety, Faculty of Applied Bioscience, Tokyo University of Agriculture, 1-1-1 Sakuragaoka Setagaya-ku, Tokyo 156-8502, Japan; Organization of Advanced Science and Technology, Kobe University, Kobe, Hyogo 657-8501, Japan.
  • 2 Department of Nutritional Science and Food Safety, Faculty of Applied Bioscience, Tokyo University of Agriculture, 1-1-1 Sakuragaoka Setagaya-ku, Tokyo 156-8502, Japan.
  • 3 Organization of Advanced Science and Technology, Kobe University, Kobe, Hyogo 657-8501, Japan; Department of Agrobioscience, Graduate School of Agricultural Science, Kobe University, Kobe, Hyogo 651-8501, Japan.
  • 4 Department of Nutritional Science and Food Safety, Faculty of Applied Bioscience, Tokyo University of Agriculture, 1-1-1 Sakuragaoka Setagaya-ku, Tokyo 156-8502, Japan. Electronic address: abe@nodai.ac.jp.
PMID: 27491710 DOI: 10.1016/j.bmcl.2016.07.051
Abstract

Several p-terphenyl compounds have been isolated from the edible Chinese mushroom Thelephora vialis. Vialinin A, a p-terphenyl compound, strongly inhibits tumor necrosis factor-α production and release. Vialinin A inhibits the enzymatic activity of ubiquitin-specific peptidase 5, one of the target molecules in RBL-2H3 cells. Here we examined the inhibitory effect of p-terphenyl compounds, including vialinin A, against sentrin/SUMO-specific protease 1 (SENP1) enzymatic activity. The half maximal inhibitory concentration values of vialinin A and thelephantin G against full-length SENP1 were 1.64±0.23μM and 2.48±0.02μM, respectively. These findings suggest that p-terphenyl compounds are potent SENP1 inhibitors.

Keywords

SENP1; SUMO; TNF-α; Vialinin A.

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