公开(公告)号：US20160354378A1

公开(公告)日：2016-12-08

申请号：US15032295

申请日：2015-07-03

Applicant: KOREA ADVANCED INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Seyun KIM ,  Yong-Mahn HAN ,  Young-Ran KIM ,  Seulgi LEE

IPC: A61K31/52

CPC classification number: A61K31/52

Abstract: The present invention relates to a composition for the prevention and treatment of liver toxicity originated from acetaminophen comprising TNP (N2-(m-Trifluorobenzyl), N6-(p-nitrobenzyl)purine) as an active ingredient. The present inventors confirmed that TNP known as a 5-inosito pyrophosphate inhibitor suppressed apoptosis caused by acetaminophen in human embryonic stem cell-derived liver cells, mouse liver cells, and human hepatoma cell lines, up-regulated glutathione converted in liver cells, and inhibited JNK phosphorylation that is a kind of response against stress increased by acetaminophen. The inventors further confirmed that TNP had the activity of protecting liver cells from the toxicity caused by acetaminophen in an animal model. Therefore, TNP can be efficiently used as an active ingredient for a composition for the prevention and treatment of liver toxicity caused by acetaminophen.

Abstract translation: 本发明涉及一种预防和治疗源于对乙酰氨基酚的组合物，其包含TNP（N2-（间三氟苄基），N6-（对硝基苄基）嘌呤）作为活性成分。 本发明人证实，称为5-Inosito焦磷酸盐抑制剂的TNP抑制由人胚胎干细胞来源的肝细胞，小鼠肝细胞和人肝癌细胞系中的对乙酰氨基酚引起的凋亡，肝细胞中转化的上调的谷胱甘肽，并被抑制 对乙酰氨基酚增加的一种抗应激反应的JNK磷酸化。 本发明人进一步证实，TNP具有在动物模型中保护肝细胞免受对乙酰氨基酚引起的毒性的活性。 因此，TNP可以有效地用作预防和治疗由对乙酰氨基酚引起的肝毒性的组合物的活性成分。