Anti-angiogenic and anti-tumor activities of 2'-hydroxy-4'-methoxychalcone.
In the present study, we evaluated the in vitro and in vivo anti-angiogenic and anti-tumor activities of 2'-hydroxy-4'-methoxychalcone (HMC). HMC decreased angiogenesis in both chick embryos in the chorioallantoic membrane assay and basic fibroblast growth factor (bFGF)-induced vessel formation in the mouse Matrigel plug assay. This compound also reduced the proliferation of calf pulmonary arterial endothelial cells and was found to possess relatively weak gelatinase/collagenase inhibitory activity in vitro. HMC, when administered subcutaneously at the dose of 30 mg/kg for 20 d to mice implanted with murine Lewis lung carcinoma, caused a significant inhibition of tumor volume by 27.2%. Intraperitoneal (i.p.) treatment at the same dosage for 10 d to ICR mice bearing sarcoma 180 caused a significant suppression in tumor weight by 33.7%. Taken together, out data demonstrate that the anti-angiogenic activities of HMC might be due to anti-proliferative activity under inhibition of the induction of COX-2 enzyme. Furthermore, the results suggest that the potent anti-angiogenic activity of HMC seems to be the possible mechanism of action in these animal models of solid tumors.
Lee
Yeon Sil
YS
Silver Biotechnology Research Center, Hallym University, Chunchon, Korea.
Lim
Soon Sung
SS
Shin
Kuk Hyun
KH
Kim
Yeong Shik
YS
Ohuchi
Kazuo
K
Jung
Sang Hoon
SH
D020533:Angiogenesis Inhibitors / Q000494:pharmacology*; D000818:Animals; D000925:Anticoagulants / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000494:pharmacology*; D018827:Carcinoma, Lewis Lung / Q000188:drug therapy; D002417:Cattle; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D002599:Chalcone / Q000031:analogs & derivatives* / Q000494:pharmacology; D047188:Chalcones; D002642:Chick Embryo; D017364:Collagenases / Q000378:metabolism; D042783:Endothelial Cells / Q000187:drug effects; D005346:Fibroblast Growth Factors / Q000494:pharmacology; D018093:Gelatinases / Q000378:metabolism; D006493:Heparin / Q000494:pharmacology; D018374:LLC-PK1 Cells; D051379:Mice; D008810:Mice, Inbred C57BL; D012510:Sarcoma 180 / Q000473:pathology; D013552:Swine
C487593:2',4'-dihydroxy-3'-methoxychalcone; D020533:Angiogenesis Inhibitors; D000925:Anticoagulants; D000970:Antineoplastic Agents; D047188:Chalcones; D002599:Chalcone; D005346:Fibroblast Growth Factors; D006493:Heparin; D017364:Collagenases; D018093:Gelatinases