Apicidin is a histone deacetylase inhibitor with anti-invasive and anti-angiogenic potentials.
Apicidin has been identified as a histone deacetylase (HDAC) inhibitor. Since HDAC inhibitors are emerging as an exciting new class of potential anti-cancer agents, in the present study, we have examined the inhibitory effect of apicidin on cancer invasion and angiogenesis. Apicidin induced di- and tri-acetylated forms of histone H4 and the morphological alteration in v-ras-transformed mouse fibroblast NIH3T3 cells. Apicidin dramatically inhibited the invasion of v-ras-NIH3T3 and human melanoma A2058 cells and it could be associated with its ability to regulate the activities of matrix metalloproteinases. Interestingly, apicidin strongly inhibited the formation of new vessels on chorioallantoic membrane and the tube formation of ECV304 human vascular endothelial cells. This is the first report to show the anti-angiogenic potential of apicidin and it could be developed as a new type of anti-cancer drug.
Kim
Seong Hwan
SH
Department of Genetic Engineering, Faculty of Life Science and Technology, Sungkyunkwan University, Suwon 440-746, Republic of Korea.
Ahn
Sanghun
S
Han
Jeung-Whan
JW
Lee
Hyang-Woo
HW
Lee
Hoi Young
HY
Lee
Yin-Won
YW
Kim
Mi Ran
MR
Kim
Kye Won
KW
Kim
Won Bae
WB
Hong
Sungyoul
S
D000482:Allantois / Q000187:drug effects; D020533:Angiogenesis Inhibitors / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002461:Cell Line, Transformed / Q000187:drug effects / Q000378:metabolism; D045744:Cell Line, Tumor; D002642:Chick Embryo; D002823:Chorion / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005780:Gelatin; D011905:Genes, ras / Q000235:genetics; D056572:Histone Deacetylase Inhibitors; D006801:Humans; D045726:Metalloproteases / Q000378:metabolism; D051379:Mice; D041681:NIH 3T3 Cells; D009361:Neoplasm Invasiveness; D009389:Neovascularization, Pathologic / Q000378:metabolism; D010456:Peptides, Cyclic / Q000494:pharmacology*
D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors; D010456:Peptides, Cyclic; C102351:apicidin; D005780:Gelatin; D045726:Metalloproteases