缺氧誘導(dǎo)因子1（HIF-1）有兩個亞基,，在缺氧情況下,，HIF-1α會過度表達(dá)，HIF-1α轉(zhuǎn)錄活性的增加與腫瘤進(jìn)展,、血管生成,、轉(zhuǎn)移和侵襲密切相關(guān)。
近日European Journal of Pharmacology雜志上的一則研究證實天然化合物補(bǔ)骨脂二氫黃酮甲醚 Bavachinin在體外和體內(nèi)有較強(qiáng)的抗血管生成活性,。Bavachinin濃度依賴性抑制人KB癌（HeLa細(xì)胞的衍生細(xì)胞株）HIF-1α活性,，其機(jī)制是通過促進(jìn)（VHL）與HIF-1α之間的相互作用。
此外,，Bavachinin降低與血管生成和能量代謝相關(guān)基因的表達(dá)如血管內(nèi)皮生長因子（VEGF）,、Glut1和己糖激酶2,。Bavachinin也抑制人類臍靜脈內(nèi)皮細(xì)胞（內(nèi)皮細(xì)胞）的管腔形成以及KB細(xì)胞在體外的遷移能力。體內(nèi)研究顯示,，給予KB移植瘤裸鼠每周三次注射Bavachinin,，共持續(xù)四星期能顯著減少腫瘤體積和CD31的表達(dá)。這些數(shù)據(jù)表明Bavachinin可以作為抑制腫瘤血管生成的治療劑,。（生物谷：Bioon.com）
doi:10.1016/j.ejphar.2012.06.028
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Anti-angiogenic and anti-tumor activity of Bavachinin by targeting hypoxia-inducible factor-1α
Manoj Nepala, b, Hwa Jung Choia, Bo-Yun Choia, b, Se Lim Kima, Jae-Ha Ryuc, Ho Hee Kimc, Young-Hoon Leed, Yunjo Soha,
Hypoxia-inducible factor-1 (HIF-1) consists of two subunits, the HIF-1β, which is constitutively expressed, and HIF-1α, which is oxygen-responsive. HIF-1α is over-expressed in response to hypoxia, increasing transcriptional activity linked to tumor progression, angiogenesis, metastasis, and invasion. This study aimed to demonstrate that the natural compound, Bavachinin, has potent anti-angiogenic activity in vitro and in vivo. Bavachinin inhibited increases in HIF-1α activity in human KB carcinoma (HeLa cell derivative) and human HOS osteosarcoma cells under hypoxia in a concentration-dependent manner, probably by enhancing the interaction between von Hippel–Lindau (VHL) and HIF-1α. Furthermore, Bavachinin decreased transcription of genes associated with angiogenesis and energy metabolism that are regulated by HIF-1, such as vascular endothelial growth factors (VEGF), Glut 1 and Hexokinase 2. Bavachinin also inhibited tube formation in human umbilical vein endothelial cells (HUVECs) as well as in vitro migration of KB cells. In vivo studies showed that injecting Bavachinin thrice weekly for four weeks significantly reduced tumor volume and CD31 expression in nude mice with KB xenografts. These data indicate that Bavachinin could be used as a therapeutic agent for inhibiting tumor angiogenesis.
