木层孔萘酚-1，一种新型的二萘并呋喃衍生物，以不依赖p53的方式激活p21启动子。

Xylarianaphthol-1, a novel dinaphthofuran derivative, activates p21 promoter in a p53-independent manner.

作者信息

Kotoku Naoyuki, Higashimoto Kenichi, Kurioka Masatoshi, Arai Masayoshi, Fukuda Akinori, Sumii Yuji, Sowa Yoshihiro, Sakai Toshiyuki, Kobayashi Motomasa

机构信息

Graduate School of Pharmaceutical Sciences, Osaka University, Yamada-oka 1-6, Suita, Osaka 565-0871, Japan.

出版信息

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3389-91. doi: 10.1016/j.bmcl.2014.05.083. Epub 2014 Jun 4.

DOI:10.1016/j.bmcl.2014.05.083

PMID:24939757

Abstract

Xylarianaphthol-1, a novel dinaphthofuran derivative, was isolated from a marine sponge-derived fungus of order Xylariales on the guidance of a bioassay using the transfected human osteosarcoma MG63 cells (MG63(luc+)). The chemical structure of xylarianaphthol-1 was determined from the (1)H and (13)C NMR analysis and was further confirmed by the total synthesis. Xylarianaphthol-1 activated p21 promoter stably transfected in MG63 cells dose-dependently. Expression of p21 protein in the wild-type MG63 cells was also increased by xylarianaphthol-1 treatment.

摘要

木层孔萘酚-1是一种新型的二萘并呋喃衍生物，它是在利用转染的人骨肉瘤MG63细胞（MG63(luc+)）进行生物测定的指导下，从一种属于炭角菌目的海洋海绵衍生真菌中分离得到的。通过(1)H和(13)C核磁共振分析确定了木层孔萘酚-1的化学结构，并通过全合成进一步证实。木层孔萘酚-1能剂量依赖性地激活稳定转染于MG63细胞中的p21启动子。用木层孔萘酚-1处理野生型MG63细胞也能增加p21蛋白的表达。