Anti-angiogenic and Anti-tumor Activities of 2′-Hydroxy-4′-methoxychalcone

• Published in: Biological & pharmaceutical bulletin Vol. 29; no. 5; pp. 1028 - 1031
• Main Authors: Lee, Yeon Sil, Lim, Soon Sung, Shin, Kuk Hyun, Kim, Yeong Shik, Ohuchi, Kazuo, Jung, Sang Hoon
• Format: Journal Article
• Language: English
• Published: Japan The Pharmaceutical Society of Japan 01.05.2006; Japan Science and Technology Agency
• Subjects: 2′-hydroxy-4′-methoxychalcone; angiogenesis; Angiogenesis Inhibitors - pharmacology; Animals; Anticoagulants - pharmacology; Antineoplastic Agents - pharmacology; calf pulmonary arterial endothelial cell; Carcinoma, Lewis Lung - drug therapy; Cattle; Cell Line; Cell Proliferation - drug effects; Chalcone - analogs & derivatives; Chalcone - pharmacology; Chalcones; Chick Embryo; Collagenases - metabolism; Endothelial Cells - drug effects; Fibroblast Growth Factors - pharmacology; Gelatinases - metabolism; Heparin - pharmacology; LLC-PK1 Cells; Mice; Mice, Inbred C57BL; proliferation; Sarcoma 180 - pathology; Swine
• ISSN: 0918-6158; 1347-5215
• DOI: 10.1248/bpb.29.1028

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.