DOI: 10.1021/acs.orglett.6c02633 ISSN: 1523-7060
Rearranged Jatrophane Diterpenoids from Euphorbia helioscopia with 5/6/6/4 and 5/6/6/5 Fused Skeletons and Potent Anti-ZIKV Activity
Xiong Qiu, Pan-Pan Pang, Ting-Ting Yue, Shao-Zhong Luo, Rui-Han Zhang, Wei-Lie Xiao, Chang-Bo Zheng, Xiao-Li LiAbstract
Three rearranged jatrophane diterpenoids, eupheilosnoids A–C (1–3), were isolated from Euphorbia helioscopia. Compound 1 possesses a fused 5/6/6/4 tetracyclic carbon skeleton, whereas compounds 2 and 3 feature a 5/6/6/5 ring system. Compounds 1–3 were evaluated for anti-ZIKV activity. Among them, compound 2 exhibited potent anti-ZIKV activity with an EC50 of 2.09 μM, which was significantly superior to that of the positive control ribavirin (RBV). Further studies revealed that compound 2 significantly inhibited the expression of ZIKV envelope protein (ZIKV-E).