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Rearranged Jatrophane Diterpenoids from Euphorbia helioscopia with 5/6/6/4 and 5/6/6/5 Fused Skeletons and Potent
Xiong Qiu1,2, Pan-Pan Pang3, Ting-Ting Yue1
1Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, Yunnan Characteristic Plant Extraction Laboratory Co., Ltd., Yunnan Key Laboratory of Research and Development for Natural Products, Institute of International Rivers and Eco-Security, School of Pharmacy and School of Chemical Science and Technology, Yunnan University, Kunming650500, People's Republic of China.
Abstract:
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).
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