Fungal metabolites, asterric acid derivatives inhibit vascular endothelial growth factor (VEGF)-induced tube formation of HUVECs.
In the search for new naturally occurring anti-angiogenic compounds, we found that a culture broth of an unidentified fungal strain B90911 exerted inhibitory activity on capillary-like tube formation of human umbilical vein endothelial cells (HUVEC) in vitro. Four active compounds were isolated by bioassay-guided separation and their structures were identified to be sulochrin (1), methyl asterric acid (2), and two new asterric acid derivatives, 3-chloroasterric acid (3), and 3,5-dichloroasterric acid (4) by spectroscopic analyses. These compounds significantly inhibited the VEGF-induced tube formation of HUVEC, suggesting that asterric derivatives could be useful for further study as anti-angiogenic agents.
Lee
Hee Jung
HJ
Anticancer Research Laboratory, Korea Research Institute of Bioscience and Biotechnology, P.O. Box 115, Yuseong, Daejeon 305-600, Korea.
Lee
Jeong Hyeong
JH
Hwang
Bang Yeon
BY
Kim
Hang Sub
HS
Lee
Jung Joon
JJ
D020533:Angiogenesis Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D016228:Endothelial Growth Factors / Q000037:antagonists & inhibitors*; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects*; D005285:Fermentation; D005658:Fungi / Q000737:chemistry / Q000378:metabolism*; D006801:Humans; D008222:Lymphokines / Q000037:antagonists & inhibitors*; D013058:Mass Spectrometry; D019906:Nuclear Magnetic Resonance, Biomolecular; D010636:Phenols / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D010647:Phenyl Ethers / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D042461:Vascular Endothelial Growth Factor A; D042442:Vascular Endothelial Growth Factors
D020533:Angiogenesis Inhibitors; D016228:Endothelial Growth Factors; D008222:Lymphokines; D010636:Phenols; D010647:Phenyl Ethers; D042461:Vascular Endothelial Growth Factor A; D042442:Vascular Endothelial Growth Factors; C078941:asterric acid