Yang Hui, Liu Ding-Quan, Liang Tong-Jun, Li Jia, Liu Ai-Hong, Yang Peng, Lin Kun, Yu Xiao-Qing, Guo Yue-Wei, Mao Shui-Chun, Wang Bin
a School of Pharmacy, Nanchang University , Nanchang 330006 , China.
J Asian Nat Prod Res. 2014 Dec;16(12):1158-65. doi: 10.1080/10286020.2014.965162. Epub 2014 Oct 8.
A novel minor bisindole alkaloid, racemosin C (1), characterized by a naturally unprecedented 8-hydroxy-2,4,6-cyclooctatrienone ring fused with two indole systems, was isolated from the green alga Caulerpa racemosa, together with one known related metabolite, caulersin (2). The structure of 1 was elucidated on the basis of extensive spectroscopic analysis, and by comparison with the data of related known compounds. A plausible biosynthetic pathway of 1 was proposed. Compounds 1 and 2 exhibited significant PTP1B inhibitory activity with IC50 values of 5.86 ± 0.57 and 7.14 ± 1.00 μM, respectively, compared with the positive control oleanolic acid (IC50 = 3.03 ± 0.20 μM). On the basis of the data obtained, the Caulerpa bisindole alkaloids may be considered as a new class of PTP1B inhibitors.
从绿藻总状蕨藻中分离出一种新型的微量双吲哚生物碱——总状蕨藻素C（1），其特征是具有一个天然前所未有的8-羟基-2,4,6-环辛三烯酮环与两个吲哚系统稠合而成，同时还分离出一种已知的相关代谢产物——蕨藻素（2）。通过广泛的光谱分析并与相关已知化合物的数据进行比较，阐明了1的结构。提出了1可能的生物合成途径。与阳性对照齐墩果酸（IC50 = 3.03±0.20μM）相比，化合物1和2分别表现出显著的蛋白酪氨酸磷酸酶1B（PTP1B）抑制活性，IC50值分别为5.86±0.57和7.14±1.00μM。根据所获得的数据，蕨藻双吲哚生物碱可被视为一类新型的PTP1B抑制剂。
