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Multifloroside ( 4 ), together with 10-hydroxyoleoside 11-methyl ester ( 1 ), 10-hydroxyoleoside dimethyl ester ( 2 ), and 10-hydroxyligustroside ( 3 ), are all secoiridoids, which are naturally occurring compounds that possess a wide range of biological and pharmacological activities. However, the anti-cancer activity of 1 - 4 has not been evaluated yet. The objective of this work was to study the anti-cancer activities of 1 - 4 in the human epidermoid carcinoma cell lines A431 and the human non-small cell lung cancer (NSCLC) cell lines A549. The results indicate that 1 - 4 differ in potency in their ability to inhibit the proliferation of human A431 and A549 cells, and multifloroside ( 4 ) display the highest inhibitory activity against A431 cells. The structure-activity relationships suggest that the o -hydroxy- p -hydroxy-phenylethyl group may contribute to the anti-cancer activity against A431 cells. Multifloroside treatment can also inhibit cell colony formation, arrest the cell cycle in the S-phase, increase the levels of reactive-oxygen-species (ROS), and mitochondrial membrane potential (MMP), but it did not significantly induce cell apoptosis at low concentrations. The findings indicated that multifloroside ( 4 ) has the tendency to show selective anti-cancer effects in A431 cells, along with suppressing the colony formation, inducing S cell cycle arrest, ROS production, and increasing MMP.

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Multifloroside Suppressing Proliferation and Colony Formation, Inducing S Cell Cycle Arrest, ROS Production, and Increasing MMP in Human Epidermoid Carcinoma Cell Lines A431