Pharmacy College of West China of Sichuan University, Chengdu, Sichuan 610065, China.
Molecules. 2012 Jul 5;17(7):8091-104. doi: 10.3390/molecules17078091.
Allylated biphenol neolignans contain a variety of chemopreventive entities that have been used as anti-tumor drug leads. Herein, 37 allylated biphenols were evaluated for anti-proliferative activity by the MTT assay and inhibitory effect on the migration and tube formation of HUVECs featuring anti-angiogenic properties. 3-(2-Methylbut-3-en-2-yl)-3′,5′-bis(trifluoromethyl)-[1,1′-biphenyl]-4-ol (5c) exerted an inhibitory effect on HUVECs compared to honokiol (IC₅₀ = 47.0 vs. 52.6 μM) and showed significant blocking effects on the proliferation of C26, Hela, K562, A549, and HepG2 (IC₅₀ = 15.0, 25.0, 21.2, 29.5, and 13.0 μM, respectively), superior to those of honokiol (IC₅₀ = 65.1, 62.0, 42.0, 75.0, and 55.4 μM, respectively). Importantly, compound 5c inhibited the migration and capillary-like tube formation of HUVECs in vitro.
烯丙基化联苯新木脂素含有多种化学预防实体，已被用作抗肿瘤药物先导物。在此，通过 MTT 法评估了 37 种烯丙基化联苯对增殖的抑制活性，以及对具有抗血管生成特性的 HUVECs 的迁移和管状形成的抑制作用。与厚朴酚（IC₅₀ = 47.0 对 52.6 μM）相比，3-(2-甲基丁-3-烯-2-基）-3′，5′-双（三氟甲基）-[1,1′-联苯]-4-醇（5c）对 HUVECs 具有抑制作用，并对 C26、Hela、K562、A549 和 HepG2 的增殖表现出显著的阻断作用（IC₅₀ = 15.0、25.0、21.2、29.5 和 13.0 μM，分别），优于厚朴酚（IC₅₀ = 65.1、62.0、42.0、75.0 和 55.4 μM，分别）。重要的是，化合物 5c 抑制了 HUVECs 的迁移和体外毛细血管样管状形成。
