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Assay-guided fractionation led to the isolation of nine β-dihydroagarofuran sesquiterpenoids from the fruits of Celastrus orbiculatus. All isolated β-dihydroagarofuran sesquiterpenoids were tested for their cytotoxic activity against human melanoma A375-S2 and human cervical carcinoma Hela cell lines. Among them, compounds 1-5 and 7 showed cytotoxic activity. Compound 3 exhibited promising cytotoxicity against both human melanoma A375- S2 and human cervical carcinoma Hela cell lines. The structure-activity relationship was discussed briefly.

Cytotoxic β-Dihydroagarofuran Sesquiterpenoids from the Fruits of Celastrus orbiculatus