KDR Kinase Inhibitor Isolated from the Mushroom Boletopsis leucomelas

Akira Kaneko; Mariko Tsukada; Miyuki Fukai; Toshihiro Suzuki; Kazuto Nishio; Kazuhiko Miki; Kaoru Kinoshita; Kunio Takahashi; Kiyotaka Koyama

doi:10.1021/np100113e

KDR Kinase Inhibitor Isolated from the Mushroom Boletopsis leucomelas

J Nat Prod. 2010 May 28;73(5):1002-4. doi: 10.1021/np100113e.

Authors

Akira Kaneko¹, Mariko Tsukada, Miyuki Fukai, Toshihiro Suzuki, Kazuto Nishio, Kazuhiko Miki, Kaoru Kinoshita, Kunio Takahashi, Kiyotaka Koyama

Affiliation

¹ Department of Pharmacognosy and Phytochemistry, Meiji Pharmaceutical University, Noshio 2-522-1, Kiyose-shi, Tokyo 204-8588, Japan.

PMID: 20380423
DOI: 10.1021/np100113e

Abstract

Three novel p-terphenyl compounds, named boletopsins A (1), B (2), and C (3), and four known analogues (4-7) were isolated from fruiting bodies of the mushroom Boletopsis leucomelas. Compounds 1-7 were tested for KDR kinase inhibitory activity, and boletopsin C (3) was found to have an IC(50) value of 70.7 microM. Compound 3 also showed inhibition of proliferation of human umbilical vein endothelial cells, with an IC(50) value of 9.04 microM.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Agaricales / chemistry*
Endothelial Cells / drug effects
Fruiting Bodies, Fungal / chemistry
Humans
Inhibitory Concentration 50
Japan
Molecular Structure
Terphenyl Compounds / chemistry
Terphenyl Compounds / isolation & purification*
Terphenyl Compounds / pharmacology*
Umbilical Veins / cytology
Umbilical Veins / drug effects
Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors*

Substances

Terphenyl Compounds
boletopsin A
boletopsin B
boletopsin C
Vascular Endothelial Growth Factor Receptor-2