Department of Food and Nutritional Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
Department of Nutrition and Health Sciences, Toyo University, 1-1-1, Izumino, Itakura-machi, Ora-gun, Gunma 374-0193, Japan.
Molecules. 2021 Oct 28;26(21):6510. doi: 10.3390/molecules26216510.
The antiangiogenic activity of the ethanol extract of propolis collected from different regions in western Algeria was investigated using in vitro human umbilical vein endothelial cells (HUVECs). The ethanol extract with the strongest activity, i.e., Algerian propolis 1 (EEPA1), inhibited the formation of capillary networks in a dose-dependent manner (6.25-50 μg/mL) within 12 h and induced cell fragmentation of HUVECs at 50 μg/mL after treatment for 24 h. To identify the active compounds in EEAP1, a high-performance liquid chromatography (HPLC) analysis was performed, revealing that EEAP1 contains two major compounds. Both compounds were isolated by repeated column chromatography and identified as ω-hydroxyferulenol () and ferulenol (), which have a coumarin structure conjugated with a farnesyl group according to NMR, high-resolution electrospray ionization mass spectroscopy, and chemical modification. Compounds and inhibited the tube-forming activity of HUVECs, especially , which exhibited a stronger antiangiogenic effect even at a low concentration of 3.31 μg/mL. Moreover, suppressed the elongation and induced cell fragmentation at the same dose. The molecular changes in tube-forming HUVECs induced by were found to be related to the activation of the caspase signals. To confirm the plant origin of propolis, an HPLC comparative analysis of the ethanol extracts of some plants near beekeeping areas and that of Algerian propolis (EEAP1) was performed, and similar chromatographic patterns were observed. This result suggests that the plant origin of this Algerian propolis is the resin of .
从阿尔及利亚西部不同地区采集的蜂胶的乙醇提取物的抗血管生成活性，采用体外人脐静脉内皮细胞（HUVEC）进行了研究。活性最强的乙醇提取物，即阿尔及利亚蜂胶 1（EEPA1），在 12 小时内以剂量依赖性方式抑制毛细血管网络的形成（6.25-50 μg/mL），并在处理 24 小时后在 50 μg/mL 诱导 HUVEC 细胞碎裂。为了鉴定 EEAP1 中的活性化合物，进行了高效液相色谱（HPLC）分析，结果表明 EEAP1 含有两种主要化合物。两种化合物均通过反复柱层析分离，并根据 NMR、高分辨率电喷雾电离质谱和化学修饰鉴定为 ω-羟基桂皮醇（）和桂皮醇（），它们具有香豆素结构，与法呢基基团共轭。化合物和抑制 HUVEC 的管状形成活性，特别是，即使在低浓度 3.31 μg/mL 时也表现出更强的抗血管生成作用。此外，在相同剂量下抑制细胞伸长并诱导细胞碎裂。发现 诱导的管状形成 HUVEC 中的分子变化与半胱天冬酶信号的激活有关。为了确认蜂胶的植物来源，对一些养蜂区附近植物的乙醇提取物和阿尔及利亚蜂胶（EEAP1）的乙醇提取物进行了 HPLC 比较分析，并观察到相似的色谱模式。该结果表明，这种阿尔及利亚蜂胶的植物来源是树脂的。
