Vialinin A和thelephantin G是肿瘤坏死因子-α产生的有效抑制剂，可抑制sentrin/SUMO特异性蛋白酶1的酶活性。
Vialinin A and thelephantin G, potent inhibitors of tumor necrosis factor-α production, inhibit sentrin/SUMO-specific protease 1 enzymatic activity.
作者信息
Yoshioka Yasukiyo, Namiki Daisuke, Makiuchi Mao, Sugaya Kouichi, Onose Jun-Ichi, Ashida Hitoshi, Abe Naoki
机构信息
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.
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.
出版信息
Bioorg Med Chem Lett. 2016 Sep 1;26(17):4237-40. doi: 10.1016/j.bmcl.2016.07.051. Epub 2016 Jul 27.
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.
几种对三联苯化合物已从可食用的中国蘑菇小孔革菌中分离出来。对三联苯化合物瓶菌素A能强烈抑制肿瘤坏死因子-α的产生和释放。瓶菌素A抑制泛素特异性肽酶5的酶活性，泛素特异性肽酶5是RBL-2H3细胞中的靶分子之一。在此，我们研究了包括瓶菌素A在内的对三联苯化合物对sentrin/SUMO特异性蛋白酶1（SENP1）酶活性的抑制作用。瓶菌素A和小孔革菌素G对全长SENP1的半数最大抑制浓度值分别为1.64±0.23μM和2.48±0.02μM。这些发现表明，对三联苯化合物是有效的SENP1抑制剂。
Zotero 插件