Tsushima M, Maoka T, Katsuyama M, Kozuka M, Matsuno T, Tokuda H, Nishino H, Iwashima A
Kyoto Pharmaceutical University, Kyoto, Japan.
Biol Pharm Bull. 1995 Feb;18(2):227-33. doi: 10.1248/bpb.18.227.
As a screening study for anti-tumor promoters, 51 carotenoids with diverse structures were examined for their inhibitory effects on the Epstein-Barr virus activation activity of 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells. The results showed that most of the carotenoids exhibited inhibitory activity, and in general, no cytotoxicity on Raji cells was observed in the assay. Among the carotenoids, beta-cryptoxanthin, lutein, and lactucaxanthin showed the strongest inhibitory activity, superior to the well known anti-tumor promoter, beta-carotene. Heteroxanthin, peridinin, and halocynthiaxanthin showed cytotoxicity at the high concentration (1000 molar ratio per TPA), but indicated a strong inhibitory effect at the lower concentrations, which were only weakly toxic (500 and 100 molar ratios). Based on these results, the essential moiety for the activity of carotenoids was considered to be the 3-hydroxy-epsilon-end group.
作为一项针对抗肿瘤促进剂的筛选研究，对51种结构各异的类胡萝卜素进行了检测，考察它们对Raji细胞中12-O-十四烷酰佛波醇-13-乙酸酯（TPA）的爱泼斯坦-巴尔病毒激活活性的抑制作用。结果表明，大多数类胡萝卜素表现出抑制活性，并且在该测定中，一般未观察到对Raji细胞的细胞毒性。在这些类胡萝卜素中，β-隐黄质、叶黄素和莴苣黄素表现出最强的抑制活性，优于著名的抗肿瘤促进剂β-胡萝卜素。异玉米黄质、多甲藻黄素和海鞘黄质在高浓度（相对于TPA为1000摩尔比）时表现出细胞毒性，但在较低浓度（仅具有弱毒性的500和100摩尔比）时显示出强烈的抑制作用。基于这些结果，类胡萝卜素活性的必需部分被认为是3-羟基-ε-末端基团。
