B19（姜黄素的单羰基类似物）具有强大的抗血管生成活性。

Potent anti-angiogenic activity of B19--a mono-carbonyl analogue of curcumin.

作者信息

Sun Li, Liu Jin, Lin Sen-Sen, Shi Wen-Ting, Zhu Jing, Liang Guang, Yuan Sheng-Tao

机构信息

Jiangsu Center for Drug Screening, China Pharmaceutical University, Nanjing 210009, China.

Jiangsu Center for Pharmacodynamics Research and Evaluation, China Pharmaceutical University, Nanjing 210009, China.

出版信息

Chin J Nat Med. 2014 Jan;12(1):8-14. doi: 10.1016/S1875-5364(14)60002-9.

DOI:10.1016/S1875-5364(14)60002-9

PMID:24484590

Abstract

AIM

The compound B19 (C21H22O5) is a newly synthesized, mono-carbonyl analog of curcumin that has exhibited potential antitumor effects. This present study was performed to identify the anti-angiogenic activity of this compound.

METHODS AND RESULTS

B19 inhibited migration and tube formation of human umbilical vein endothelial cells, and arrested microvessel outgrowth from rat aortic rings. In addition, B19 suppressed the neovascularization of chicken chorioallantoic membrane. Mechanistic studies revealed that B19 suppressed the downstream protein kinase activation of vascular endothelial growth factor (VEGF) by decreasing phosphorylated forms of serine/threonine kinase Akt, extracellular signal-regulated kinase, and p38 mitogen-activated protein kinase, with or without stimulating vascular endothelial growth factor (VEGF).

CONCLUSIONS

B19 exerted anti-angiogenic activity in vitro and ex vivo, which suggests that it merits further investigation as a promising anticancer angiogenesis compound.

摘要

目的

化合物B19（C21H22O5）是一种新合成的姜黄素单羰基类似物，已显示出潜在的抗肿瘤作用。本研究旨在确定该化合物的抗血管生成活性。

方法与结果

B19抑制人脐静脉内皮细胞的迁移和管腔形成，并阻止大鼠主动脉环微血管的生长。此外，B19抑制鸡胚绒毛尿囊膜的血管生成。机制研究表明，无论是否刺激血管内皮生长因子（VEGF），B19均可通过降低丝氨酸/苏氨酸激酶Akt、细胞外信号调节激酶和p38丝裂原活化蛋白激酶的磷酸化形式来抑制VEGF的下游蛋白激酶激活。