Shimamura M, Hazato T, Ashino H, Yamamoto Y, Iwasaki E, Tobe H, Yamamoto K, Yamamoto S
Medical Research Center, Tokyo Metropolitan Institute of Medical Science (Rinshoken), 18-22 Honkomagome 3-chome, Bunkyo-ku, Tokyo 113-8613, Japan.
Biochem Biophys Res Commun. 2001 Nov 23;289(1):220-4. doi: 10.1006/bbrc.2001.5934.
On the basis of our previous finding that humulone, a bitter acid from beer hop extract, was a potent inhibitor of bone resorption and inhibited the catalytic activity of cyclooxygenase-2 (COX-2) and more potently the transcription of the COX-2 gene, we examined the effect of humulone on angiogenesis, using chick embryo chorioallantoic membranes (CAMs) and vascular endothelial and tumor cells. Humulone significantly prevented in vivo angiogenesis in CAM in a dose-dependent manner with an ED(50) of 1.5 microg/CAM. Humulone also inhibited in vitro tube formation of vascular endothelial cells. Moreover, it suppressed the proliferation of endothelial cells and the production of vascular endothelial growth factor (VEGF), an angiogenic growth factor, in endothelial and tumor cells. Thus, humulone is a potent angiogenic inhibitor, and may be a novel powerful tool for the therapy of various angiogenic diseases involving solid tumor growth and metastasis.
基于我们之前的发现，即啤酒花提取物中的苦味酸蛇麻酮是一种有效的骨吸收抑制剂，可抑制环氧合酶-2（COX-2）的催化活性，更有效地抑制COX-2基因的转录，我们使用鸡胚绒毛尿囊膜（CAM）以及血管内皮细胞和肿瘤细胞，研究了蛇麻酮对血管生成的影响。蛇麻酮以剂量依赖性方式显著抑制CAM中的体内血管生成，半数有效剂量（ED50）为1.5微克/CAM。蛇麻酮还抑制血管内皮细胞的体外管状结构形成。此外，它抑制内皮细胞的增殖以及内皮细胞和肿瘤细胞中血管内皮生长因子（VEGF，一种血管生成生长因子）的产生。因此，蛇麻酮是一种有效的血管生成抑制剂，可能是治疗包括实体瘤生长和转移在内的各种血管生成性疾病的新型有力工具。
