title: Anti-angiogenic and anti-tumor activities of 2'-hydroxy-4'-methoxychalcone.
abstract: 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.
authors.affiliation: Silver Biotechnology Research Center, Hallym University, Chunchon, Korea.
authors.forename: Yeon Sil
authors.initials: YS
authors.lastname: Lee
authors.forename: Soon Sung
authors.initials: SS
authors.lastname: Lim
authors.forename: Kuk Hyun
authors.initials: KH
authors.lastname: Shin
authors.forename: Yeong Shik
authors.initials: YS
authors.lastname: Kim
authors.forename: Kazuo
authors.initials: K
authors.lastname: Ohuchi
authors.forename: Sang Hoon
authors.initials: SH
authors.lastname: Jung
mesh_terms: 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
chemical_list: 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