Department of Biomedical Sciences, Faculty of Allied Health Sciences, Universiti Kebangsaan Malaysia, Kuala Lumpur, Malaysia.
Hum Exp Toxicol. 2011 Feb;30(2):138-44. doi: 10.1177/0960327110368739. Epub 2010 Apr 12.
Stilbenes possess a variety of biological activities including chemopreventive activity. This study was conducted to evaluate the structural activity relationships of six methoxylated stilbene analogues with respect to their cytotoxic effects and antioxidant activities on HepG2 hepatoma and Chang liver cells. The cytotoxic and total antioxidant activities of six stilbene analogues were determined by MTT and Ferric Reducing Antioxidant Power (FRAP) assays, respectively. We found that the cis-methoxylated stilbene: (Z)-3,4,4'-trimethoxystilbene was the most potent and selective antiproliferative agent (IC₅₀ 89 µM) in HepG2 cells. For the total antioxidant activity, compounds possessing hydroxyl groups at the 4' position namely (E)-3-methoxy-4'-hydroxystilbene, (E)-3,5-dimethoxy-4'-hydroxystilbene (pterostilbene), (E)-4-methoxy-4'-hydroxystilbene showed the highest antioxidant activity. Structure activity relationship studies of these compounds demonstrated that the cytotoxic effect and antioxidant activities of the tested compounds in this study were structurally dependent.
二苯乙烯具有多种生物活性，包括化学预防活性。本研究旨在评估 6 种甲氧基二苯乙烯类似物的结构活性关系，研究它们对 HepG2 肝癌和 Chang 肝细胞的细胞毒性和抗氧化活性。通过 MTT 和 Ferric Reducing Antioxidant Power（FRAP）测定法分别测定了 6 种二苯乙烯类似物的细胞毒性和总抗氧化活性。结果发现，顺式甲氧基二苯乙烯：（Z）-3,4,4'-三甲氧基二苯乙烯是 HepG2 细胞中最有效和选择性的增殖抑制剂（IC₅₀ 为 89µM）。对于总抗氧化活性，在 4'位具有羟基的化合物，即（E）-3-甲氧基-4'-羟基二苯乙烯、（E）-3,5-二甲氧基-4'-羟基二苯乙烯（紫檀芪）、（E）-4-甲氧基-4'-羟基二苯乙烯表现出最高的抗氧化活性。对这些化合物的构效关系研究表明，本研究中测试化合物的细胞毒性和抗氧化活性与结构有关。
