Takaishi Y, Ujita K, Tokuda H, Nishino H, Iwashima A, Fujita T
Faculty of Pharmaceutical Sciences, University of Tokushima, Japan.
Cancer Lett. 1992 Jul 31;65(1):19-26. doi: 10.1016/0304-3835(92)90208-d.
To search for possible antitumor promoters, we carried out a primary screening of thirty-seven dihydroagarofuran sesquiterpenes from Tripterygium wilfordii Hook fil. var. regelii Makino and Euonymus sieboldianus Blume, using their possible inhibitory effects on the Epstein-Barr virus early antigen (EBV-EA) activation which is induced by 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells. Some of these sesquiterpenes, triptofordin F-2 (Takaishi et al., 1988), 1,2,6,8,15-pentaacetoxy-9-benzoyloxy-4-hydroxy-beta-dihydroagarofuran and triptogelin A-1 (Takaishi et al., 1990) were observed to significantly inhibit the EBV-EA activation at low doses. Based on the results, the structural requirements for the activity of these compounds were discussed [corrected].
为了寻找可能的抗肿瘤促进剂,我们对雷公藤(Tripterygium wilfordii Hook fil. var. regelii Makino)和卫矛(Euonymus sieboldianus Blume)中的37种二氢沉香呋喃倍半萜进行了初步筛选,利用它们对12-O-十四烷酰佛波醇-13-乙酸酯(TPA)诱导的Raji细胞中EB病毒早期抗原(EBV-EA)激活的可能抑制作用。观察到其中一些倍半萜,如雷公藤素F-2(Takaishi等人,1988年)、1,2,6,8,15-五乙酰氧基-9-苯甲酰氧基-4-羟基-β-二氢沉香呋喃和雷公藤素A-1(Takaishi等人,1990年)在低剂量时能显著抑制EBV-EA的激活。基于这些结果,讨论了这些化合物活性的结构要求[已修正]。