Key Laboratory of Marine Drugs, Ministry of Education of China, School of Medicine and Pharmacy, Ocean University of China, 5 Yushan Road, Qingdao 266003, China.
Laboratory for Marine Drugs and Bioproducts of Qingdao National Laboratory for Marine Science and Technology, Qingdao 266237, China.
Mar Drugs. 2021 Nov 16;19(11):641. doi: 10.3390/md19110641.
Angiogenesis, including the growth of new capillary blood vessels from existing ones and the malignant tumors cells formed vasculogenic mimicry, is quite important for the tumor metastasis. Anti-angiogenesis is one of the significant therapies in tumor treatment, while the clinical angiogenesis inhibitors usually exhibit endothelial cells dysfunction and drug resistance. Bis(2,3,6-tribromo-4,5-dihydroxybenzyl)ether (BTDE), a marine algae-derived bromophenol compound, has shown various biological activities, however, its anti-angiogenesis function remains unknown. The present study illustrated that BTDE had anti-angiogenesis effect in vitro through inhibiting human umbilical vein endothelial cells migration, invasion, tube formation, and the activity of matrix metalloproteinases 9 (MMP9), and in vivo BTDE also blocked intersegmental vessel formation in zebrafish embryos. Moreover, BTDE inhibited the migration, invasion, and vasculogenic mimicry formation of lung cancer cell A549. All these results indicated that BTDE could be used as a potential candidate in anti-angiogenesis for the treatment of cancer.
血管生成,包括新毛细血管从现有血管生长和恶性肿瘤细胞形成血管生成拟态,对肿瘤转移非常重要。抗血管生成是肿瘤治疗的重要方法之一,而临床应用的血管生成抑制剂通常表现出内皮细胞功能障碍和耐药性。双(2,3,6-三溴-4,5-二羟基苯甲醚)(BTDE)是一种来源于海洋藻类的溴酚化合物,具有多种生物活性,但它的抗血管生成功能尚不清楚。本研究表明,BTDE 通过抑制人脐静脉内皮细胞迁移、侵袭、管形成以及基质金属蛋白酶 9(MMP9)的活性,具有体外抗血管生成作用,并且 BTDE 还能阻断斑马鱼胚胎的节间血管形成。此外,BTDE 抑制肺癌细胞 A549 的迁移、侵袭和血管生成拟态形成。这些结果表明,BTDE 可用作治疗癌症的抗血管生成的潜在候选药物。